A narrow-spectrum, 18-membered macrolide antibiotic isolated from the actinomycete Dactylosporangium aurantiacum subsp. hamdenensis with potential antibacterial activity. Although the exact mechanism of action has yet to be fully elucidated, fidaxomicin may bind to and inhibit bacterial DNA-dependent RNA polymerase, thereby inhibiting the initiation of bacterial RNA synthesis. When orally administered, this agent is minimally absorbed into the systemic circulation, acting locally in the gastrointestinal tract. Fidaxomicin appears to be active against pathogenic Gram-positive bacteria, such as clostridia, enterococci, and staphylococci, but does not appear to be active against other beneficial intestinal bacteria.


A salt of lithium that has been used experimentally as an immunomodulator.


The tromethamide salt form of lodoxamide, a synthetic mast cell stabilizing compound with anti-inflammatory activity. Upon administration to the eye, lodoxamide tromethamide inhibits type I immediate hypersensitivity reaction by preventing the antigen-stimulated calcium influx into mast cells, thereby inhibiting release of histamine. Lodoxamide tromethamide also prevents the release of slow-reacting substances of anaphylaxis (SRS-A) and inhibits eosinophil chemotaxis.


A synthetic broad-spectrum fluoroquinolone with antibacterial activity. Lomefloxacin inhibits DNA gyrase, a type II topoisomerase involved in the induction or relaxation of supercoiling during DNA replication. This inhibition leads to a decrease in DNA synthesis during bacterial replication, resulting in cell growth inhibition and eventually cell lysis.


A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.


A semi-synthetic, broad-spectrum, beta-lactamase resistant, second-generation cephalosporin antibiotic derived from cephasporium. The bactericidal activity of loracarbef results from the inhibition of bacterial cell wall synthesis through interference with the cross-linking of peptidoglycan units. This results in a reduction of cell wall stability and causes cell lysis. Loracarbef is more active against a variety of gram-negative organisms but less active against gram-positive pathogens compared to first-generation agents.


A carotenoid and red pigment produced by tomatoes, other red fruits and vegetables, and photosynthetic algae. It is a key intermediate in the biosynthesis of other carotenoids, and has antioxidant, anti-carcinogenic, radioprotective, and anti-inflammatory properties.


One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure.


Dye and chemical solution stains for medical purposes are mixtures of synthetic or natural dyes or nondye chemicals in solutions used in staining cells and tissues for diagnostic histopathology, cytopathology, or hematology.


An organic salt or ester of maleic acid that could be conjugated to free base compounds/drugs to improve the physiochemical properties including stability, solubility and dissolution rate. (NCI)


An oligosaccharide derived from starch that is used as a food additive and as a carbohydrate supplement. As a supplement, maltodextrin is used to provide and sustain energy levels during endurance-oriented workouts o sports, and to help build muscle mass and support weight gain.


An aromatic alpha hydroxy acid used in the treatment of urinary tract infections and as an oral antibiotic.


The dichloride salt of manganese, an essential trace element and a cofactor for many enzymes involved in a variety of biological activities in cells, with potential immunomodulating activity. Upon administration, manganese may act as an adjuvant and induce both humoral and cellular immune responses.


A saturated long-chain fatty acid with a 17-carbon backbone. Margaric acid is found naturally as a minor component of the fat and milk fat of ruminants.


A synthetic vitamin D derivative usually formulated for topical dermatological use, antipsoriatic Calcipotriene (calcipotriol) competes equally with active 1,25-hydroxy-2D3 (the natural form of vitamin D) for 1,25-hydroxy-2D3 receptors in regulating cell proliferation and differentiation. It induces differentiation and suppresses proliferation of keratinocytes, reversing abnormal keratinocyte changes in psoriasis, and leads to normalization of epidermal growth. (NCI04)


An indole derivative with antiemetic activity. As a selective serotonin receptor antagonist, dolasetron mesylate competitively blocks the action of serotonin at 5HT3 receptors, resulting in suppression of chemotherapy- and radiotherapy-induced nausea and vomiting. (NCI04)


A synthetic and active form of vitamin B12 that can cross the blood brain barrier without biotransformation, that may be used to treat or prevent vitamin B12 deficiency and its complications. Upon administration, mecobalamin is able to replace endogenous vitamin B12, increase vitamin B12 levels and improve vitamin B12 deficiency. Vitamin B12 is necessary for hematopoiesis, neural metabolism, DNA and RNA production, and carbohydrate, fat, and protein metabolism. It improves iron functions in the metabolic cycle and assists folic acid in choline synthesis. Its metabolism is interconnected with that of folic acid.


A synthetic, acetate derivative of the sex hormone progesterone. Medroxyprogesterone 17-acetate (NCI04)


A topical, synthetic glucocorticoid with metabolic, anti-inflammatory and anti-allergic properties. Medrysone exerts its effect by interacting with specific intracellular glucocorticoid receptors and subsequently binds to DNA to modify gene expression. This results in an induction of the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Consequently, an overall reduction in chronic inflammation and autoimmune reactions is accomplished.


Megestrol acetate is a progestogen with actions and uses similar to those of the progestogens in general. It also has anti-androgenic properties. It is given by mouth in the palliative treatment or as an adjunct to other therapy in endometrial carcinoma and in breast cancer. Megestrol acetate has been approved to treat anorexia and cachexia. (From Reynolds JEF(Ed): Martindale: The Extra Pharmacopoeia (electronic version). Micromedex, Inc, Englewood, CO, 1995)


The meglumine salt form of iodipamide, a tri-iodinated benzoate derivative and an ionic dimeric contrast agent used in diagnostic imaging. When administered in vivo, iodipamide is removed from the liver and secreted into the biliary tract. Like other organic iodine compounds, this agent blocks x-ray and appears opaque on x-ray film; thereby it enhances the visibility of the bile ducts and gallbladder during cholangiography and cholecystography procedures.


A menaquinone compound and form of vitamin K2 with potential antineoplastic activity. Menatetrenone may act by modulating the signalling of certain tyrosine kinases, thereby affecting several transcription factors including c-myc and c-fos. This agent inhibits tumor cell growth by inducing apoptosis and cell cycle arrest.


The oil extracted from various Brevoortia and Ethmidium species. Menhaden oil is used industrially in paint production and the tanning of leather as was as in livestock feeds.


A thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.


The hippurate salt form of methenamine, a prodrug and inactive weak base that slowly hydrolyzes in acidic urine to ammonia and the effective, urinary tract antiseptic formaldehyde. Formaldehyde probably exerts its antibacterial effect by denaturation of protein. Depending on the urinary concentrations, formaldehyde is either bactericidal or bacteriostatic. Formaldehyde urinary concentrations are dependent on urine pH, volume, and flow rate. Formaldehyde acts as an antibacterial agent against gram-positive and gram-negative organisms.


A methyl halide, bromomethane, and bromohydrocarbon that is composed of one carbon, one hydrogen, and three bromine atoms. It is both manufactured and naturally produced by marine algae, and it has a role as a pesticide, a fire extinguishing agent, and in the synthesis of other chemicals. It is characterized as a colorless gas with a chloroform-like odor at high concentrations. Exposure occurs by inhalation, ingestion, or contact.


Dye and chemical solution stains for medical purposes are mixtures of synthetic or natural dyes or nondye chemicals in solutions used in staining cells and tissues for diagnostic histopathology, cytopathology, or hematology.


A yellowish, oily, naturally occurring liquid with a clove-like aroma and is present in many essential oils. Methyleugenol is used as a flavoring agent, as a fragrance and as an anesthetic in rodents. Methyleugenol is mutagenic in animals and is reasonably anticipated to be a human carcinogen based on evidence of carcinogenicity in animals. (NCI05)


A methyl ester of methacrylic acid. Methyl methacrylate is a reactive resin, and the polymerized form is used as cement in dentistry, orthopaedic surgery and ophthalmology. The monomer form of this agent has relaxation effect on smooth muscle systemically, which might be a result of nitric oxide-mediated response.


A methyl derivative of noroxymorphone with selective, opioid-receptor antagonistic activity. Methylnaltrexone displaces opioids from peripheral opioid receptors in the gastrointestinal tract, the bladder, and the skin, resulting in decreases in opioid-related constipation, urinary retention, and pruritis, respectively. Methylnaltrexone does not cross the blood-brain barrier and does not affect the centrally-mediated analgesic effect of opioids.


alpha-methylbenzyl alcohol
methylphenyl carbinol


An aminoglycoside antibiotic isolated from Micromonospora sagamiensis var. nonreducans. Micronomicin is an analog of gentamicin and has broad-spectrum activity against both gram-positive and gram-negative bacteria.


A desoxynojirimycin derivative and inhibitor of alpha-glucosidase with antihyperglycemic activity. Miglitol binds to and inhibits alpha-glucosidase, an enteric enzyme found in the brush border of the small intestines that hydrolyzes oligosaccharides and disaccharides into glucose and other monosaccharides. This prevents the breakdown of larger carbohydrates into glucose and decreases the rise in postprandial blood glucose levels. Compared to acarbose, miglitol is systemically absorbed.


An isoquinoline derivative that is used as a short-acting non-depolarizing agent.


A reversible inhibitor of monoamine oxidase type A; (RIMA); (see MONOAMINE OXIDASE INHIBITORS) that has antidepressive properties.


A benzhydryl acetamide compound, central nervous system stimulant, and CYP3A4 inducing agent that is used in the treatment of NARCOLEPSY and SLEEP WAKE DISORDERS.


A non-sulfhydryl angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, moexipril is hydrolyzed into its active form moexiprilat, which competitively inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the actions of the potent vasoconstrictor angiotensin II and leads to vasodilation. It also prevents angiotensin II-induced aldosterone secretion by the adrenal cortex, thereby promoting diuresis and natriuresis.


A pregnadienediol derivative ANTI-ALLERGIC AGENT and ANTI-INFLAMMATORY AGENT that is used in the management of ASTHMA and ALLERGIC RHINITIS. It is also used as a topical treatment for skin disorders.


A modified form of lipid A, the biologically active part of Gram-negative bacterial lipopolysaccharide (LPS) endotoxin, and a Toll-like receptor 4 (TLR4) agonist, with potential immunostimulatory activity. As a vaccine adjuvant, monophosphoryl lipid A (MPLA) stimulates both cellular and humoral responses to the vaccine antigen. Compared to LPS, MPLA exerts a similar immunostimulatory activity but with reduced toxicity.


A heterocyclic biguanidine with activity against influenza and other viral infections. Although its mechanism of action is not fully known the effects seem to be due to an influence on the virus host-cell system.


The sulfate salt of morphine, an opiate alkaloid isolated from the plant Papaver somniferum and produced synthetically. Morphine binds to and activates specific opiate receptors (delta, mu and kappa), each of which are involved in controlling different brain functions. In the central nervous and gastrointestinal systems, this agent has widespread effects including analgesia, anxiolysis, euphoria, sedation, respiratory depression, and gastrointestinal system smooth muscle contraction.


The vegetable oil pressed from seeds or the essential oil extracted from the seeds of Brassica nigra, Brassica juncea, or Brassica hirta. Mustard oil is used as a cooking oil, a source of omega-3 fatty acids, and in various medicinal preparations.


An orally- and topically-active alkyl-phosphocholine compound with potential antineoplastic activity. Miltefosine targets cellular membranes, modulating cell membrane permeability, membrane lipid composition, phospholipid metabolism, and mitogenic signal transduction, resulting in cell differentiation and inhibition of cell growth. This agent also inhibits the anti-apoptotic mitogen-activated protein kinase (MAPK) pathway and modulates the balance between the MAPK and pro-apoptotic stress-activated protein kinase (SAPK/JNK) pathways, thereby inducing apoptosis. As an immunomodulator, miltefosine stimulates T-cells, macrophages and the expression of interleukin 3 (IL-3), granulocyte-macrophage colony stimulating factor (GM-CSF), and interferon gamma (INF-gamma). (NCI04)


A semisynthetic derivative of the antineoplastic anthracycline antibiotic doxorubicin. With a mechanism of action that appears to differ from doxorubicin, valrubicin is converted intracytoplasmically into N-trifluoroacetyladriamycin, which interacts with topoisomerase II, stabilizing the complex between the enzyme and DNA; consequently, DNA replication and repair and RNA and protein synthesis are inhibited and the cell cycle is arrested in the G2 phase. In addition, this agent accumulates in the cell cytoplasm where it inhibits protein kinase C (PKC). Valrubicin is less cardiotoxic than doxorubicin when administered systemically; applied topically, this agent shows excellent tissue penetration. Structurally, the trifluoro-acetyl moiety on the amino group of the glycoside and the valerate moiety appear to result in a lipophilicity that is greater than of doxorubicin, resulting in increased intracytoplasmic concentrations.


A synthetic cannabinoid and dibenzopyrane derivative with anti-emetic activity. Although the mechanism of action has not been fully elucidated yet, it has been suggested that nabilone is a highly selective and strong agonist for the cannabinoid receptors CB1 and CB2, both of which are coupled to Gi/o proteins. The CB1 receptors are expressed predominantly in central and peripheral neurons and receptor stimulation has been implicated in the reduction of chemotherapy-induced nausea.


A naphthylalkanone and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic and analgesic activities. Nabumetone is a prodrug that upon hepatic catalysis converts into the active moiety 6-methoxy-2-naphthylacetic acid (6MNA). 6MNA inhibits the activity of the enzymes cyclo-oxygenase I and II, resulting in decreased formation of precursors of prostaglandins and thromboxanes. The resulting decrease in prostaglandin synthesis is responsible for the therapeutic effects of nabumetone. The formation of thromboxane A2, by thromboxane synthase, is also decreased and results in an inhibition of platelet aggregation.


A topical, synthetic allylamine derivate similar to terbinafine with broad-spectrum antifungal activity. Naftifine can be fungicidal or fungistatic depending on the concentration and the organisms involved.


Decanoic acid ester of nandrolone that is used as an anabolic agent to prevent or treat WASTING SYNDROME associated with severe chronic illness or HIV infection (HIV WASTING SYNDROME). It may also be used in the treatment of POSTMENOPAUSAL OSTEOPOROSIS.


A beta-1 adrenergic receptor antagonist with antihypertensive and vasodilatory activity. Nebivolol binds to and blocks the beta-1 adrenergic receptors in the heart, thereby decreasing cardiac contractility and rate. This leads to a reduction in cardiac output and lowers blood pressure. In addition, nebivolol potentiates nitric oxide (NO), thereby relaxing vascular smooth muscle and exerting a vasodilatory effect.


A pyranoquinolone derivative that inhibits activation of inflammatory cells which are associated with ASTHMA, including EOSINOPHILS; NEUTROPHILS; MACROPHAGES; MAST CELLS; MONOCYTES; AND PLATELETS.


A yellow, green or blue colored, crystalline inorganic compound that produces toxic gases upon heating. Nickel sulfate is used in electroplating and as a chemical intermediate to produce other nickel compounds. Exposure to this substance can cause severe dermatitis, skin and asthma-like allergies and affects the lungs, kidneys, gastrointestinal tract and neurological system. Nickel sulfate is a known carcinogen and is associated with an increased risk of developing lung and nasal cancers. (NCI05)


A derivative of the NIACINAMIDE that is structurally combined with an organic nitrate. It is a potassium-channel opener that causes vasodilatation of arterioles and large coronary arteries. Its nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase.


A synthetic, nonsteroidal agent with antiandrogenic properties. Nilutamide preferentially binds to androgen receptors and blocks androgen receptor activation by testosterone and other androgens; this agent may inhibit androgen-dependent growth of normal and neoplastic prostate cells. (NCI04)


A synthetic benzamide with antiprotozoal activity. Nitazoxanide exerts its antiprotozoal activity by interfering with the pyruvate ferredoxin/flavodoxin oxidoreductase dependent electron transfer reaction, which is essential to anaerobic energy metabolism. PFOR enzyme reduces nitazoxanide, thereby impairing the energy metabolism. However, interference with the PFOR enzyme-dependent electron transfer reaction may not be the only pathway by which nitazoxanide exhibits antiprotozoal activity. Nitazoxanide is active against Giardia lamblia and Cryptosporidium parvum.


Nitric acid (HNO3). A colorless liquid that is used in the manufacture of inorganic and organic nitrates and nitro compounds for fertilizers, dye intermediates, explosives, and many different organic chemicals. Continued exposure to vapor may cause chronic bronchitis; chemical pneumonitis may occur. (From Merck Index, 11th ed)


A nipecotic acid derivative that acts as a GABA uptake inhibitor and anticonvulsant agent. It is used in the treatment of EPILEPSY, for refractory PARTIAL SEIZURES.


The orally bioavailable acetate salt of norethindrone, a synthetic progestin with some anabolic, estrogenic, and androgenic activities. As do all progestins, norethindrone binds to and activates nuclear progesterone receptors (PRs) in target tissues such as the pituitary and reproductive system; ligand-receptor complexes are translocated to the nucleus where they bind to progesterone response elements (PREs) located on target genes, followed by various transcriptional events and histone acetylation. Physiological effects include the inhibition of luteinizing hormone (LH) release, an increase in the endometrial luteal-phase, and alterations in endocervical mucus secretion.


Nonionic surfactant mixtures varying in the number of repeating ethoxy (oxy-1,2-ethanediyl) groups. They are used as detergents, emulsifiers, wetting agents, defoaming agents, etc. Octoxynol-9, the compound with 9 repeating ethoxy groups, is a spermatocide.


Dye and chemical solution stains for medical purposes are mixtures of synthetic or natural dyes or nondye chemicals in solutions used in staining cells and tissues for diagnostic histopathology, cytopathology, or hematology.


Oil extracted from fruit of the OLIVE TREE (genus Olea).


A prodrug of mesalamine (5-Aminosalicylic acid; 5-ASA) with anti-inflammatory activity. Unabsorbed olsalazine passes through gastrointestinal tract and is cleaved by azoreductases, produced by microflora in colon, into 2 active molecules of 5-ASA. 5-ASA exerts its anti-inflammatory action locally by inhibiting cyclooxygenase and lipoxygenase activities, thereby reducing the production of prostaglandins and leukotrienes. In addition, mesalamine may act as a scavenger of reactive oxygen free radicals.


A topical imidazole derivative with antifungal activity against Candida albicans, Malassezia furfur and dematophytes.


The bromide salt form of rocuronium, an intermediate-acting quaternary aminosteroid with muscle relaxant property. Rocuronium bromide competitively binds to the nicotinic receptor at the motor end plate, and antagonizes acetylcholine binding, which results in skeletal muscle relaxation and paralysis.


A strong dicarboxylic acid occurring in many plants and vegetables. It is produced in the body by metabolism of glyoxylic acid or ascorbic acid. It is not metabolized but excreted in the urine. It is used as an analytical reagent and general reducing agent.


An organoplatinum complex in which the platinum atom is complexed with 1,2-diaminocyclohexane, and with an oxalate ligand which is displaced to yield active oxaliplatin derivatives. These derivatives form inter- and intra-strand DNA crosslinks that inhibit DNA replication and transcription. Oxaliplatin is an antineoplastic agent that is often administered with FLUOROURACIL and FOLINIC ACID in the treatment of metastatic COLORECTAL NEOPLASMS.


An oxazole-propionic acid derivative, cyclooxygenase inhibitor, and non-steroidal anti-inflammatory drug that is used in the treatment of pain and inflammation associated with of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; and ARTHRITIS, JUVENILE.


A dibenzazepine carboxamide derivative with an anticonvulsant property. As a prodrug, oxcarbazepine is converted to its active metabolite, 10-monohydroxy. Although the mechanism of action has not been fully elucidated, electrophysiological studies indicate this agent blocks voltage-gated sodium channels, thereby stabilizing hyper-excited neural membranes, inhibiting repetitive neuronal firing, and decreasing the propagation of synaptic impulses.


A broad spectrum imidazole derivative with antifungal activity. Although the exact mechanism of action has yet to be fully elucidated, oxiconazole, like other azole antifungals, most likely inhibits the cytochrome P450-dependent demethylation of lanosterol. This prevents the synthesis of ergosterol which is a crucial component of fungal cell membrane. By disrupting fungal cell membrane synthesis and integrity, oxiconazole alters fungal cell membrane permeability, promotes loss of essential intracellular components and eventually inhibits fungal cell growth.


A benzophenone derivative used as a sunscreen agent. Oxybenzone absorbs UVB and UVA II rays, resulting in a photochemical excitation and absorption of energy. Upon return to ground state, the absorbed energy results in emission of longer wavelength radiation and decreased skin penetration of radiation which reduces the risk of DNA damage.


A tertiary amine possessing antimuscarinic and antispasmodic properties. Oxybutynin blocks muscarinic receptors in smooth muscle, hence inhibiting acetylcholine binding and subsequent reduction of involuntary muscle contractions. Oxybutynin is used to reduce bladder contractions by relaxing bladder smooth muscle.


A synthetic tertiary amine and antimuscarinic agent with antispasmodic and antisecretory activities. Oxyphencyclimine binds to and blocks the muscarinic receptor on smooth muscle. This agent has a direct relaxing effect on smooth muscle and therefore prevents spasms in the muscles of the gastrointestinal tract, inhibits gastrointestinal propulsive motility, decreases gastric acid secretion and controls excessive pharyngeal, tracheal and bronchial secretion.


The edible oil extracted from the pulp of the oil palm fruit. Palm oil is commonly used as a commercial cooking oil due to its stability at high temperatures.


A natural fatty acid amide that is both a food component and an endogenously synthesized compound, with potential analgesic and anti-inflammatory activities. Upon administration, palmidrol may inhibit the release of pro-inflammatory mediators from activated mast cells. This may reduce inflammation and pain.


A polypeptide that consists of the 1-34 amino-acid fragment of human PARATHYROID HORMONE, the biologically active N-terminal region. The acetate form is given by intravenous infusion in the differential diagnosis of HYPOPARATHYROIDISM and PSEUDOHYPOPARATHYROIDISM. (Reynolds JEF(Ed): Martindale: The Extra Pharmacopoeia (electronic version). Micromedex, Inc, Englewood, CO, 1995)


A serotonin uptake inhibitor that is effective in the treatment of depression.


A synthetic dye with imaging and food coloring property. It is a sodium or calcium salt of [4-(alpha-(4-diethylaminophenyl)-5-hydroxy- 2,4-disulfophenyl-methylidene)-2,5-cyclohexadien-1-ylidene] diethylammonium hydroxide inner salt. Patent blue V dye is used in sentinel lymph node (SLN) technique to guide nodal dissection or other imaging procedures.


A thienopyridine, with antiplatelet activity. Clopidogrel targets, irreversibly binds to and alters the platelet receptor for adenosine diphosphate (ADP), thereby blocking the binding of ADP to its receptor, inhibiting ADP-mediated activation of the glycoprotein complex GPIIb/IIIa, and inhibiting fibrinogen binding to platelets and platelet adhesion and aggregation. This results in increased bleeding time.


homosaccharidic polymer of sugar acids of fruit that forms gels with sugar at the proper pH.


A naturally-occurring saturated fatty acid with nine carbon atoms. The ammonium salt form of nonanoic acid is used as an herbicide. It works by stripping the waxy cuticle of the plant, causing cell disruption, cell leakage, and death by desiccation.


The essential oil extracted from the leaves of Mentha pulegium. Pennyroyal oil has antiseptic properties. It has been used for inducing abortions, repelling fleas and ticks, and for treating illnesses of the digestive system.


The essential oil extracted from the leaves of Mentha x piperita. Peppermint oil is used for its aromatic properties and as a flavoring and to treat illnesses of the digestive and respiratory system as well as pain.


A non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Perindoprilat inhibits ACE and, thus, the conversion of angiotensin I to angiotensin II; consequently, angiotensin II-mediated vasoconstriction and angiotensin II-stimulated aldosterone secretion from the adrenal cortex are inhibited and diuresis and natriuresis ensue.


A pyrethroid insecticide commonly used in the treatment of LICE INFESTATIONS and SCABIES.


An antiseptic and disinfectant aromatic alcohol.


An antipyrine derivative that functions as a free radical scavenger and neuroprotective agent. It is used in the treatment of AMYOTROPHIC LATERAL SCLEROSIS and STROKE.


An ethanolamine derivative with antihistaminic property. Phenyltoloxamine blocks H1 histamine receptors, thereby inhibiting phospholipase A2 and production of endothelium-derived relaxing factor, nitric oxide. Subsequent lack of activation of guanylyl cyclase through nitric oxide results in decreased cyclic GMP levels, thereby inhibiting smooth muscle constriction of various tissues, decreasing capillary permeability and decreasing other histamine-activated allergic reactions.


An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.


A broad spectrum antimicrobial agent. Phthalylsulfathiazole is used in the treatment of dysentery, colitis, and gastroenteritis.


A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed)


An orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity. Pioglitazone activates peroxisome proliferator-activated receptor gamma (PPAR-gamma), a ligand-activated transcription factor, thereby inducing cell differentiation and inhibiting cell growth and angiogenesis. This agent also modulates the transcription of insulin-responsive genes, inhibits macrophage and monocyte activation, and stimulates adipocyte differentiation.


A piperazinyl androstane derivative which is a non-depolarizing neuromuscular blocking agent (NEUROMUSCULAR NONDEPOLARIZING AGENTS). It is used as a muscle relaxant during ANESTHESIA and surgical procedures.


A natural estrogenic substance composed of estrone sulfate and piperazine. Estropipate diffuses through the cell membrane and binds to and subsequently activates the nuclear estrogen receptor found in the reproductive tract, breast, pituitary, hypothalamus, liver, and bone. The activated complex binds to the estrogen response element on the DNA and activates the transcription of genes involved in the functioning of the female reproductive system and secondary sex characteristics.


An analogue of the anthracycline antineoplastic antibiotic doxorubicin. Pirarubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. This agent is less cardiotoxic than doxorubicin and exhibits activity against some doxorubicin-resistant cell lines. (NCI04)


A short-acting, beta-adrenergic receptor agonist with bronchodilator activity. Pirbuterol selectively binds to beta-2 adrenergic receptors in bronchial smooth muscle, thereby activating intracellular adenyl cyclase, an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP levels cause relaxation of bronchial smooth muscle, relieve bronchospasms, improve mucociliary clearance and inhibit the release of mediators of immediate hypersensitivity from cells, especially from mast cells.


A sulfamoylbenzoic acid belonging to the class of loop diuretics. Piretanide is structurally related to furosemide and bumetanide.


A derivative of clindamycin with a 6-membered ring replacing clindamycin's 5-membered ring. Compared to clindimycin, pirlimycin has increased activity against gram-positive bacteria, including Staphylococcus aureus and coagulase negative species of Staphylococcus and Streptococcus. This agent is primarily used in the treatment of mastitis in cattle.


A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure.


An alkyl polyglycol ether of LAURYL ALCOHOL, chemically defined as an alcohol ethoxylate having an average alkyl chain of 12-14 carbon atoms, and an ethylene oxide chain of 9 ethylene oxide units. It is used as a detergent, and medically as a local anesthetic, and as a sclerosing agent for the treatment of ESOPHAGEAL AND GASTRIC VARICES and VARICOSE VEINS.


A synthetic long-acting polymer derivative of the female sex hormone estradiol. As the primary, most potent estrogen hormone produced by the ovaries, estradiol binds to and activates specific nuclear receptors. Estradiol exhibits mild anabolic and metabolic properties, and increases blood coagulability. Administration of polyestradiol phosphate leads to the marked decrease of testosterone levels and may exhibit a bone mass-preserving effect in patients with prostatic cancer. (NCI04)


A complex of polyethylene glycol conjugated with L-asparaginase. Asparaginase hydrolyzes L-asparagine to L-aspartic acid and ammonia, thereby depleting these cells of asparagine and blocking protein synthesis and tumor cell proliferation, especially in the G1 phase of the cell cycle. The agent also induces apoptosis in tumor cells. Pegylation decreases the enzyme's antigenicity. Asparagine is critical to protein synthesis in leukemic cells, which cannot synthesize this amino acid due to the absence of the enzyme asparagine synthase. (NCI04)


polylactic acid-polyglycolic acid copolymer

A co-polymer that consists of varying ratios of polylactic acid and polyglycolic acid. It is used as a matrix for drug delivery and for BONE REGENERATION.


polymyxin B / trimethoprim Ophthalmic Solution [Polytrim]


A yellowish, crystalline, inorganic compound that emits toxic chromium fumes upon heating. Potassium chromate is highly corrosive and is a strong oxidizing agent. This substance is used in the manufacture of dyes and in textile dyeing processes. Potassium chromate primarily affects the nose, throat and lungs causing ulcerations, shortness of breath, bronchitis, pneumonia and asthma but can also affect the gastrointestinal tract, liver, kidneys and immune system. This substance is a known human carcinogen and is associated with an increased risk of developing lung cancer and cancer of the sinonasal cavity. (NCI05)


A crystalline salt, KNO3; a strong oxidizer used especially in making gunpowder, as a fertilizer, and in medicine.


The potassium salt of perchloric acid and a member of the Hofmeister ions series with thyroid blocking properties. Potassium perchlorate is a competitive inhibitor of iodine uptake through inhibiting the sodium-iodide symporter (NIS) on the thyroid follicular cell membrane. This results in a potential decrease in thyroid hormone synthesis including thyroxine (T4) and tri-iodothyronine (T3). In addition, this agent decreases the accumulation of the radioactive imaging substance and Hofmeister series ion, pertechnetate Tc 99m, in the choroid plexus and in the salivary and thyroid glands through competitive displacing.


An inorganic compound used as a laxative, dietary supplement and for electrolyte-replacement purposes. Phosphate, a predominant intracellular anion, plays an important role in energy storage, osteoblastic and osteoclastic activities, regulating serum calcium concentrations and numerous cellular phosphate-transfer reactions. Potassium phosphate increases fluidity of the intestinal contents by retention of water by osmotic forces, thereby indirectly inducing intestinal smooth muscle constriction.


A morpholine derivative with local anesthetic property. Pramocaine decreases the permeability of the neuronal membrane to sodium ions by reversibly binding to and inhibiting voltage-gated sodium channels. This results in stabilization of the membrane and, thereby inhibiting the ionic fluxes required for membrane depolarization, hence resulting in the failure to initiate a propagated action potential and subsequent conduction blockade.


A synthetic non-halogenated double-ester derivative of the corticosteroid prednisolone with anti-inflammatory, antipruritic and vasoconstrictive properties. Following skin permeation, prednicarbate enters cells and binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of pro-inflammatory cytokine production by increasing the expression of lipocortins. These block phospholipase A-dependent release of arachidonic acid thereby inhibiting prostaglandin synthesis. This agent also decreases the number of circulating lymphocytes by suppression of the production of vasodilators such as prostacyclin and nitric oxide.


The acetate salt form of prednisolone, a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. As a glucocorticoid receptor agonist, prednisolone acetate binds to specific intracellular glucocorticoid receptors, and causes the ligand-receptor complex to be translocated to the nucleus where it initiates the transcription of glucocorticoid-responsive genes such as various cytokines and lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both potent mediators of inflammation. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis in sensitive tumor cell populations.


Combination of imipenem and cilastatin that is used in the treatment of bacterial infections; cilastatin inhibits renal dehydropeptidase I to prolong the half-life and increase the tissue penetration of imipenem, enhancing its efficacy as an anti-bacterial agent.


A long-acting beta-2-adrenergic receptor agonist.


A 3-propyl and 17b-methyl ether of estradiol that may be used vaginally to relieve vaginal atrophy and its associated symptoms. Upon intravaginal administration, promestriene acts on the vaginal mucosa and may decrease vaginal atrophy and its associated symptoms, such as vaginal dryness and itching.


A semisynthetic, acid stable, penicillin with antibacterial activity. Propicillin binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall and causes cell lysis.


A clear, colorless, viscous organic solvent and diluent used in pharmaceutical preparations.


A synthetic, highly-flammable, volatile, colorless liquid that is soluble in water and miscible with many organic solvents. Propylene oxide is used primarily as a chemical intermediate in the production of polyethers and propylene glycol. It is also used as a pesticide and a fumigant for the sterilization of packaged foods and plastic medical instruments. Acute inhalation exposure to vapors of this compound can result in respiratory tract irritation, coughing, difficulty in breathing (dyspnea) and buildup of fluid in the lungs (pulmonary edema) that can possibly lead to pneumonia. Inhale high concentrations of the vapors for short time periods may cause headache, motor weakness, incoordination, ataxia and coma. Contact with propylene oxide can irritate the eyes and skin. It is reasonably anticipated to be a human carcinogen. (NCI05)


The vitamin K-dependent cofactor of activated PROTEIN C. Together with protein C, it inhibits the action of factors VIIIa and Va. A deficiency in protein S; (PROTEIN S DEFICIENCY); can lead to recurrent venous and arterial thrombosis.


A benzoic acid derivative anesthetic agent, with local anesthetic activity. Upon administration, proparacaine stabilizes the neuronal membrane by binding to and inhibiting voltage-gated sodium channels. This inhibits the sodium ion influx required for the initiation and conduction of impulses within the neuronal cell, increases the threshold for electrical stimulation and results in a loss of sensation.


A methylxanthine and derivative of theophylline. Proxyphylline relaxes smooth muscles, particularly bronchial muscles. This xanthine most likely exerts its effect by inhibiting cAMP or cGMP phosphodiesterases, thereby increasing levels of the second messenger cAMP or cGMP intracellularly. Other mode of actions include an adenosine antagonistic effect on the activity of CD4 lymphocytes and mediator release from mast cells thereby decreasing lung sensitivity to allergens and other substances that cause inflammation. Proxyphylline also acts as a CNS stimulant and exerts a positive chronotropic and inotropic effect on the heart.


A protein-bound polysaccharide derived from the mushroom Trametes versicolor (Turkey Tail) with immunoadjuvant and potential antitumor activities. Although its mechanism of action has yet to be fully elucidated, in vitro and in vivo studies indicate that polysaccharide-K induces peripheral blood monocyte secretion of IL-8 and TNF-alpha, induces T cell proliferation, and prevents cyclophosphamide-induced immunosuppression. This agent has also been reported to stimulate macrophages to produce reactive nitrogen intermediates and superoxide anions and to promote apoptosis in the promyelocytic leukemia cell line HL-60.


A synthetic, pyrimidine C-5 nucleoside with antineoplastic activity. Pseudoisocytidine, after conversion into pseudoisocytidine triphosphate, is incorporated into DNA and RNA eventually halting tumor cell proliferation. Compared to 5-azacytidine and cytarabine, this agent shows enhanced stability and resistance to enzymatic deamination.


A fungistatic and antimicrobial derivative of aspergillic acid. Although the exact mechanism of action remains to be fully elucidated, pyrithione appears to interfere with membrane transport ultimately leading to a loss of metabolic control.


saturated 5-membered ring structure with one nitrogen heteroatom.


An intermediate compound in the metabolism of carbohydrates, proteins, and fats. In thiamine deficiency, its oxidation is retarded and it accumulates in the tissues, especially in nervous structures. (From Stedman, 26th ed)


A synthetic benzodiazepine derivative with anxiolytic, sedative and hypnotic properties. Quazepam and its major metabolite 2-oxoquazepam potentiate gamma-aminobutyric acid (GABA) activity by binding to the benzodiazepine-1 recognition site (BZ-1) within the GABA-A receptor, located in the limbic, neocortical and mesencephalic reticular system. This increases the frequency of GABA-activated chloride channel opening events, allowing the flow of chloride ions into the neuron leading to membrane hyperpolarization and decreased neuronal excitability.


A prodrug and non-sulfhydryl angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Quinapril is hydrolized into its active form quinaprilat, which binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This abolishes the potent vasoconstrictive actions of angiotensin II and leads to vasodilatation. Quinapril also causes a decrease in angiotensin II-induced aldosterone secretion by the adrenal cortex, thereby promoting diuresis and natriuresis, and increases bradykinin levels.


The gluconate salt form of quinidine, an alkaloid with antimalarial and antiarrhythmic (Class la) properties. Quinidine gluconate exerts its anti-malarial activity by acting primarily as an intra-erythrocytic schizonticide through association with the hemepolymer (hemozoin) in the acidic food vacuole of the parasite thereby preventing further polymerization by heme polymerase enzyme. This results in accumulation of toxic heme and death of the parasite. Quinidine gluconate exerts its antiarrhythmic effects by depressing the flow of sodium ions into cells during phase 0 of the cardiac action potential, thereby slowing the impulse conduction through the atrioventricular (AV) node, reducing the maximal rate of phase 0 depolarization and prolonging the refractory period. Quinidine gluconate also reduces the slope of phase 4 depolarization in Purkinje-fibres resulting in slowed conduction and reduced automaticity in the heart.


A substituted benzamide used for its prokinetic properties. It is used in the management of gastroesophageal reflux disease, functional dyspepsia, and other disorders associated with impaired gastrointestinal motility. (Martindale The Extra Pharmacopoeia, 31st ed)


A non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Ramiprilat inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and leads to vasodilation. This agent also causes an increase in bradykinin levels and a decrease in angiotensin II-induced aldosterone secretion by the adrenal cortex, thereby promoting diuresis and natriuresis.


A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.


A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.


The oil extracted from the seeds of Brassica napus. Rapeseed oil was traditionally used as an industrial lubricant but newer varieties are used for animal feed, vegetable oil for human consumption, and biodiesel.


An antipsychotic agent that is specific for dopamine D2 receptors. It has been shown to be effective in the treatment of schizophrenia.


A stilbene and non-flavonoid polyphenol produced by various plants including grapes and blueberries. It has anti-oxidant, anti-inflammatory, cardioprotective, anti-mutagenic, and anti-carcinogenic properties. It also inhibits platelet aggregation and the activity of several DNA HELICASES in vitro.


A naturally-occurring fatty acid ester form of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. Retinyl acetate binds to and activates retinoid receptors, inducing cell differentiation and decreasing cell proliferation. This agent also inhibits carcinogen-induced neoplastic transformation in some cancer cell types and exhibits immunomodulatory properties. (NCI04)


A naturally-occurring phenyl analogue of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. As the most common form of vitamin A taken for dietary supplementation, retinyl palmitate binds to and activates retinoid receptors, thereby inducing cell differentiation and decreasing cell proliferation. This agent also inhibits carcinogen-induced neoplastic transformation, induces apoptosis in some cancer cell types, and exhibits immunomodulatory properties. (NCI04)


Immunizing agent containing IMMUNOGLOBULIN G anti-Rho(D) used for preventing Rh immunization in Rh-negative individuals exposed to Rh-positive red blood cells.


OIL extracted from the hard outer brown layer of rice bran after the husk has been removed.


A natural antibiotic produced by Streptomyces mediterranei, Rifamycin (Ansamycin Family) is a commonly used antimycobacterial drug that inhibits prokaryotic DNA-dependent RNA synthesis and protein synthesis; it blocks RNA-polymerase transcription initiation. Rifamycin has an activity spectrum against Gram-positive and Gram-negative bacteria, but is mainly used against Mycobacterium sp. (especially M. tuberculosis) in association with other agents to overcome resistance. (NCI04)


A long-acting, cyclopentyl-substituted derivative of rifamycin used to treat mycobacterium infections.


An orally administered, semi-synthetic, nonsystemic antibiotic derived from rifamycin SV with antibacterial activity. Rifaximin binds to the beta-subunit of bacterial DNA-dependent RNA polymerase, inhibiting bacterial RNA synthesis and bacterial cell growth. As rifaximin is not well absorbed, its antibacterial activity is largely localized to the gastrointestinal tract.


A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.


A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.


An anilide used as a long-acting local anesthetic. It has a differential blocking effect on sensory and motor neurons.


A green, crystalline, solid dye that is one of the major components of magenta. Basic fuchsin is primarily used for bacterial identification, but is also used as a dye in textiles, leather, and printing inks. Exposure to basic fuchsin is irritating to the eyes and skin. The substance is reasonably anticipated to be a human carcinogen. (NCI05)


A honey bee secretion that is used in the nutrition of larvae and to stimulate development of adult queens. It contains B-complex vitamins such as pantothenic acid (vitamin B5) and vitamin B6 (pyridoxine), amino acids, minerals, enzymes, monosaccharides and 10-hydroxy-2-decenoic acid (10-HDA). Royal jelly has been shown to have antibacterial and immunomodulatory activities.


A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed)


An orally available, piperazine derivative with anti-anginal and potential antineoplastic activities. Ranolazine's mechanism of action for its anti-ischemic effects has yet to be fully elucidated but may involve the alteration of the trans-cellular late sodium current in the ischemic myocyte. By preventing the rise of intracellular sodium levels, ranolazine may affect the transport activity of sodium-dependent calcium channels and prevent the calcium overload during myocardial ischemia, thereby preventing cellular injury. Ranolazine's potential antineoplastic effect may depend on its inhibitory effect on fatty acid oxidation, which may sensitize tumor cells to apoptosis and decrease tumor cell proliferation; fatty acid oxidation provides energy and promotes tumor cell proliferation and survival.


An orally available salicylate and non-steroidal anti-inflammatory drug (NSAID), with anti-inflammatory, analgesic and antipyretic activities. As a prodrug, salsalate is hydrolyzed to salicylic acid which inhibits the expression of cyclooxygenase (COX) enzymes. This prevents the conversion of arachidonic acid into prostaglandin precursors and leads to decreased formation of prostaglandins that are involved in pain, fever and inflammation. In addition, salsalate appears to inhibit nuclear factor-kappa B (NF-kB), thereby preventing activation of the NF-kB-mediated pathway and the expression of genes involved in inflammation.


A highly selective, long-acting beta-2 adrenergic agonist with bronchodilatory activity. Salmeterol's benzene moiety resembles the structure of catecholamines, and occupies the active site of beta-2 adrenergic receptor, while the long, lipophilic side chain of salmeterol, binds to the so called 'exosite' near the beta-2 adrenergic receptors. The binding at the exosite allows the active portion of the molecule to remain at the receptor site and continually engage and disengage with the receptor, therefore providing a long duration of action. This agent stimulates intracellular adenyl cyclase to catalyze the conversion of adenosine triphosphate to cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP levels result in relaxation of bronchiolar smooth muscle, bronchodilation and increased bronchial airflow.


Dye and chemical solution stains for medical purposes are mixtures of synthetic or natural dyes or nondye chemicals in solutions used in staining cells and tissues for diagnostic histopathology, cytopathology, or hematology.


A selenium compound with the molecular formula H2SO3. It used as a source of SELENIUM, especially for patients that develop selenium deficiency following prolonged PARENTERAL NUTRITION.


An orange-yellow powder that is soluble in carbon disulfide and practically insoluble in both water and organic solvents. Selenium sulfide is used as an ingredient in antidandruff shampoos and as a constituent of fungicides. When heated to decomposition, it emits toxic fumes of sulfur oxides and selenium. The primary routes of potential human exposure to selenium sulfide are dermal contact and inhalation. Contact with selenium sulfide can cause severe redness or irritation of the skin. It is reasonably anticipated to be a human carcinogen. (NCI05)


A naturally occurring amino acid in both eukaryotic and prokaryotic organisms. It is found in tRNAs and in the catalytic site of some enzymes. The genes for glutathione peroxidase and formate dehydrogenase contain the TGA codon, which codes for this amino acid.


A synthetic imidazole derivative, containing a benzothiophene ring, with antifungal, antibacterial, anti-inflammatory and anti-pruritic activity. Besides its ability to inhibit the synthesis of ergosterol, the benzothiophene ring of sertaconazole is able to insert into the fungal cell wall instead of tryptophan. This increases the permeability of the cell wall. In addition, sertaconazole suppresses the release of cytokines.


A selective serotonin uptake inhibitor that is used in the treatment of depression.


A fluorinated isopropyl ether with general anesthetic property. Although the mechanism of action has not been fully elucidated, sevoflurane may act by interfering with the release and re-uptake of neurotransmitters at post-synaptic terminals, and/or alter ionic conductance following receptor activation by a neurotransmitter. Sevoflurane may also interact directly with lipid matrix of neuronal membranes, thereby affecting gating properties of ion channels. In addition, this agent may activate gamma-aminobutyric acid (GABA) receptors hyperpolarizing cell membranes. This results in a general anesthetic effect, a decrease in myocardial contractility and mean arterial pressure as well as an increased respiratory rate.


A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.


A benzothiazole derivative and dopamine agonist with antioxidant properties that is used in the treatment of PARKINSON DISEASE and RESTLESS LEGS SYNDROME.


A white, crystalline powder that is commonly used as a pH buffering agent, an electrolyte replenisher, systemic alkalizer and in topical cleansing solutions.


The disodium salt of carbonic acid with alkalinizing property. When dissolved in water, sodium carbonate forms carbonic acid and sodium hydroxide. As a strong base, sodium hydroxide neutralizes gastric acid thereby acting as an antacid.


A crystalline powder essential for the metabolism and development of plants and animals as a cofactor for enzymes. (NCI)


An inorganic compound used as a laxative, dietary supplement and for electrolyte-replacement purposes. Phosphate, a predominant intracellular anion, plays an important role in energy storage, osteoblastic and osteoclastic activities, regulating serum calcium concentrations, and numerous cellular phosphate-transfer reactions. Sodium phosphate increases fluidity of the intestinal contents by retention of water by osmotic forces, thereby indirectly inducing intestinal smooth muscle constriction. Sodium phosphate is also used in the renal excretion of hydrogen ions while promoting the reabsorption of sodium ions.


The sodium salt of selenium. As a trace mineral that is toxic in high doses, selenium is a cofactor for glutathione peroxidase, an anti-oxidant enzyme that neutralizes hydrogen peroxide. Selenium may be chemoprotective for certain cancers, particularly prostate cancer. High dietary supplementation with sodium selenate may inhibit the progression of hormone-refractory prostate cancer due, in part, to an antiangiogenesis effect. (NCI04)


A white, inorganic crystalline compound with various industrial uses. Sodium sulfate is found in many common electrolyte solutions used in clinical diagnostic purpose. Since this agent is poorly absorbed in the body, and could draw water out of the cells, sometimes it is used as a cathartic or diuretic.


A white crystal or powder with reducing property. Sodium sulfite exhibits bleaching, de-sulfurizing, and dechlorinating activities. This agent was used by food industry to help maintain the fresh appearance of food products. It is also a component in many drugs, which helps maintain their potency and stability. FDA has ruled sodium sulfite a new animal drug of low regulatory priority.


A water soluble salt and reducing agent that reacts with oxidizing agents. Although its exact mechanism of action is unknown, thiosulfate likely provides an exogenous source of sulfur, thereby hastening the detoxification of cyanide through the enzyme rhodanese (thiosulfate cyanide sulfurtransferase) which converts cyanide to the relatively nontoxic, excretable thiocyanate ion. In addition, this agent neutralizes the reactive alkylating species of nitrogen mustard, thereby decreasing skin toxicity related to nitrogen mustard extravasation. (NCI04)


A sulfonamide antibiotic used in the treatment of leprosy.


A prodrug and non-sulfhydryl angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril is converted in the body to its active metabolite spiraprilat. Spiraprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Spiraprilat also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow.


A phosphinic acid-containing angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Fosinoprilat specifically and competitively inhibits angiotensin-converting enzyme thereby decreasing the formation of the potent vasoconstrictor angiotensin II, resulting in diminished vasopressor activity. In addition, angiotensin II-mediated aldosterone secretion by adrenal cortex is decreased, which results in a decrease of sodium retention and an increase in water outflow.


ETHINYL ESTRADIOL and NORGESTREL given in fixed proportions.


A water-soluble, colorless crystal with an acid taste that is used as a chemical intermediate, in medicine, the manufacture of lacquers, and to make perfume esters. It is also used in foods as a sequestrant, buffer, and a neutralizing agent. (Hawley's Condensed Chemical Dictionary, 12th ed, p1099; McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed, p1851)


Dye and chemical solution stains for medical purposes are mixtures of synthetic or natural dyes or nondye chemicals in solutions used in staining cells and tissues for diagnostic histopathology, cytopathology, or hematology.


A topical imidazole derivative with broad-spectrum antifungal and antibacterial activity. Sulconazole is excreted in both the feces and urine.


A sulfonamide antibacterial agent used alone or with sulfathiazole and sulfacetamide as a topical, intravaginal antibacterial preparation.


A sulfonamide antibiotic used typically in combination with trimethoprim.


A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.


Oil derived from the seeds of SUNFLOWER plant, Helianthus.


A saturated 22-carbon aliphatic alcohol with antiviral activity. Docosanol has a distinct mechanism of action and inhibits fusion between the plasma membrane and the herpes simplex virus envelope, thereby preventing viral entry into cells and subsequent viral activity and replication. Docosanol is used topically in the treatment of recurrent herpes simplex labialis episodes and relieves associated pain and may help heal sores faster.


A white crystalline dicarboxylic acid found in many plants, particularly tamarinds and grapes. Tartaric acid is used to generate carbon dioxide through interaction with sodium bicarbonate following oral administration. Carbon dioxide extends the stomach and provides a negative contrast medium during double contrast radiography. In high doses, this agent acts as a muscle toxin by inhibiting the production of malic acid, which could cause paralysis and maybe death.


A penicillanic acid sulfone derivative and beta-lactamase inhibitor with antibacterial activity. Tazobactam contains a beta-lactam ring and irreversibly binds to beta-lactamase at or near its active site. This protects other beta-lactam antibiotics from beta-lactamase catalysis. This drug is used in conjunction with beta-lactamase susceptible penicillins to treat infections caused by beta-lactamase producing organisms.


A radiopharmaceutical used extensively in cholescintigraphy for the evaluation of hepatobiliary diseases. (From Int Jrnl Rad Appl Inst 1992;43(9):1061-4)


A semisynthetic, narrow-spectrum, beta-lactamase-resistant penicillin with antibacterial activity. Temocillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall, eventually causing cell lysis.


A dacarbazine derivative that is used as an alkylating antineoplastic agent for the treatment of MALIGNANT GLIOMA and MALIGNANT MELANOMA.


A synthetic allylamine derivative with antifungal activity. Terbinafine exerts its effect through inhibition of squalene epoxidase, thereby blocking the biosynthesis of ergosterol, an important component of fungal cell membranes. As a result, this agent disrupts fungal cell membrane synthesis and inhibits fungal growth.


A synthetic triazole derivative structurally related to fluconazole, antifungal Terconazole seems to disrupt cell wall synthesis by inhibiting biosynthesis of ergosterol or other sterols, damaging the fungal cell membrane, altering its permeability, and promoting loss of essential intracellular elements. Terconazole is active against Candida sp.. (NCI04)


An isomer of butanol that contains a tertiary butyl group that consists of three methyl groups, each separately attached to a central (tertiary) carbon.


An eight-carbon ester form of Testosterone. The number of ester carbon atoms correlate with the half-life of the prodrug. Testosterone inhibits gonadotropin secretion from the pituitary gland and ablates estrogen production in the ovaries, thereby decreasing endogenous estrogen levels. In addition, this agent promotes the maintenance of male sex characteristics and is indicated for testosterone replacement in hypogonadal males. (NCI04)


A long-acting intramuscular form of the androgen testosterone. Testosterone inhibits gonadotropin secretion from the pituitary gland and ablates estrogen production in the ovaries, thereby decreasing endogenous estrogen levels. In addition, this agent promotes the maintenance of male sex characteristics and is indicated for testosterone replacement in hypogonadal males, delayed puberty, and metastatic mammary cancer. (NCI04)


The undecanoate ester form of the androgen testosterone, with gonadotropin-secretory inhibiting and hormone replacement activity. As testosterone inhibits the secretion of gonadotropins from the pituitary gland, administration of testosterone decreases the secretion of luteinizing hormone (LH). By inhibiting LH secretion, the growth of Leydig cells, which are normally stimulated by LH to produce testosterone, may be suppressed. In addition, this agent promotes the maintenance of male sex characteristics and can be used for testosterone replacement in hypogonadal males.


difebarbamate / febarbamate / PHENobarbital

difebarbamate / febarbamate / phenobarbital


A lactone derivative of LEUCINE that acts as a pancreatic lipase inhibitor to limit the absorption of dietary fat; it is used in the management of obesity.


An imidazole derivative with sympathomimetic activity. Applied locally to the eye or nose, tetrahydrozoline binds to and activates alpha-adrenergic receptors, resulting in vasoconstriction and decreased nasal and ophthalmic congestion.


A thymus hormone polypeptide found in thymosin fraction 5 (a crude thymus gland extract) but now produced by synthesis. It is used alone or with interferon as an immunomodulator for the treatment of CHRONIC HEPATITIS B and HEPATITIS C. Thymalfasin is also used for the treatment of chemotherapy-induced immunosuppression, and to enhance the efficacy of influenza and hepatitis B vaccines in immunocompromised patients.


A synthetic anabolic steroid with estrogenic, androgenic and progestagenic activities. The 3alpha- and 3beta-hydroxy metabolites of tibilone activate estrogenic receptors (ERs) in bone and vaginal tissue leading to a decrease in bone turnover, and decreased vaginal dryness, respectively; derived from the 3beta-hydroxy metabolite, its delta4-isomer activates androgenic receptors (ARs) in the brain and liver and progestogenic receptors (PRs) in endometrial tissue, affecting sexual function, lipid metabolism, and endometrial function, respectively. In breast and endometrial tissue, tibolone metabolites inhibit sulfatase, preventing the conversion of circulating estrone sulfate and estradiol sulfate to estrone and estradiol, respectively; estrogen-mediated effects in the breast and uterus are thus reduced.


A synthetic imidazole derivative, fungicidal Terconazole inhibits cell wall synthesis by inhibiting the biosynthesis of ergosterol or other sterols, damaging the fungal cell membrane, altering its permeability, and promoting loss of essential intracellular elements. Tioconazole is active against pathogenic Candida. (NCI04)


An orally available, benzoic acid derivative and a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic, analgesic and potential anti-neoplastic activities. Tolfenamic acid inhibits the activity of the enzymes cyclooxygenase (COX) I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes. The decrease in prostaglandin synthesis results in the therapeutic effects of this agent. Tolfenamic acid also inhibits thromboxane A2 synthesis, by thromboxane synthase, which decreases platelet aggregation. In addition, this agent exerts anti-tumor effects through COX-dependent and independent pathways. Specifically, this agent induces the production of reactive oxygen species, causes DNA damage, increases nuclear factor-kappa B (NF-kB) activation and the expression of activating transcription factor 3 (ATF3) and NSAID-activated gene-1 (NAG1), and inhibits the expression of specificity proteins (Sp), which reduces the expression of Sp-dependent anti-apoptotic and growth-promoting proteins. Altogether, this enhances tumor cell apoptosis, and reduces tumor cell growth and angiogenesis.


A sulfamate-substituted monosaccharide with anticonvulsant property. Although the mechanism of action has not been fully elucidated, topiramate antagonizes kainate/AMPA subtype of the glutamate receptors, which are ligand-activated cation channels that mediate the fast component of excitatory postsynaptic currents in neurons of the central nervous system. This antagonistic action results in stabilizing hyper-excited neural membranes, inhibiting repetitive neuronal firing, and decreasing propagation of synaptic impulses, thereby impedes seizure occurrences. In addition, this agent augments gamma-aminobenzoic acid (GABA) activity and thereby attenuating GABAnergic inhibitory transmission.


A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue.


A pyridine and sulfonamide derivative that acts as a sodium-potassium chloride symporter inhibitor (loop diuretic). It is used for the treatment of EDEMA associated with CONGESTIVE HEART FAILURE; CHRONIC RENAL INSUFFICIENCY; and LIVER DISEASES. It is also used for the management of HYPERTENSION.


A non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, trandolapril is converted by de-esterification in the liver into its active form trandolaprilat. Trandolaprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Trandolaprilat also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow.


An anabolic steroid used mainly as an anabolic agent in veterinary practice.


The prodrug of a bifunctional sulfonate alkylating agent with myeloablative, immunosuppressive, and antineoplastic activities. Under physiological conditions, treosulfan converts nonenzymatically to L-diepoxybutane via a monoepoxide intermediate. The monoepoxide intermediate and L-diepoxybutane alkylate DNA at guanine residues and produce DNA interstrand crosslinks, resulting in DNA fragmentation and apoptosis. In escalated doses, this agent also exhibits myeloablative and immunosuppressive activities.


The hexacetonide salt form of triamcinolone, a synthetic glucocorticosteroid with immunosuppressive and anti-inflammatory activity. Triamcinolone hexacetonide binds to specific cytosolic glucocorticoid receptors and subsequently interacts with glucocorticoid receptor response element on DNA and alters gene expression. This results in an induction of the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Consequently, an overall reduction in chronic inflammation and autoimmune reactions are accomplished.


Tri-n-butyl phosphate, Bu3-P, TBP. Industrial chemical; used as a plasticizer, in hydraulic fluid, as a solvent and extractant for metal ions, and as a heat exchange agent.


Benzimidazole antiplatyhelmintic agent that is used for the treatment of FASCIOLIASIS and PARAGONIMIASIS.


A triclosan analogue with an antibacterial property. Triclocarban exerts its effect by inhibiting the activity of enoyl-(acyl-carrier protein) (ACP) reductase, widely distributed in bacteria, fungi and plants. ACP reductase catalyses the last step in each cycle of fatty acid elongation in the type II fatty acid synthase systems. As a result, this agent interrupts cell membrane synthesis and leads to bacterial growth inhibition.


triethanolamine polypeptide oleate condensate


A synthetic derivative of androstane with adrenocortical suppressive properties. Trilostane reversibly inhibits 3 beta-hydroxysteroid dehydrogenase delta 5-4 isomerase in the adrenal cortex, resulting in the decreased synthesis of mineralocorticoids and glucocorticoids and the decreased conversion of pregnenolone to progesterone. (NCI04)


A lipid soluble methotrexate derivative with potential antineoplastic activity. Trimetrexate glucuronate inhibits the enzyme dihydrofolate reductase, thereby preventing the synthesis of purine nucleotides and thymidylate, with subsequent inhibition of DNA and RNA synthesis. Trimetrexate glucuronate also exhibits antiviral activity. (NCI04)


A synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH). Possessing greater potency than endogenous LHRH, triptorelin reversibly represses gonadotropin secretion. After chronic, continuous administration, this agent effects sustained decreases in LH and FSH production and testicular and ovarian steroidogenesis. Serum testosterone concentrations may fall to levels typically observed in surgically castrated men. (NCI04)


An orally bioavailable oxazaphosphorine prodrug with antineoplastic activity. Trofosfamide (TFF) is metabolized predominantly to the cyclophosphamide analogue ifosfamide (IFO), which is then metabolized by liver cytochrome P450s to the active isophosphoramide mustard (IPM). IPM alkylates DNA to form DNA-DNA cross-links, which may result in inhibition of DNA, RNA and protein synthesis, and ultimately lead to tumor cell apoptosis.


A cyclic amine with activity against herpes simplex virus. Tromantadine inhibits absorption of virions to cell surfaces, as well as penetration and uncoating of the virus.


The tartrate salt form of brimonidine, an imidazole derivative and a selective alpha-2 adrenergic receptor agonist. Upon ocular administration, brimonidine tartrate acts on the blood vessels causing them to constrict which leads to a decrease in the production of aqueous humor. Brimonidine tartrate also enhances the outflow of aqueous humor. This drug is used in the treatment of glaucoma to reduce intraocular pressure.


The mesylate salt form of doxazosin, a quinazoline compound with smooth muscle relaxing activity. Doxazosin mesylate selectively antagonizes alpha-1-adrenergic receptors in smooth muscle of the bladder neck and prostate, thereby relaxing the smooth muscle and decreasing the obstruction and urethral resistance seen with benign prostate hyperplasia (BPH). This may improve BPH symptoms. This agent also blocks alpha-1-adrenergic receptors in peripheral vascular smooth muscle, which leads to vasodilatation and a subsequent decrease in peripheral vascular resistance.


A pentacyclic triterpenoid found in various fruits, vegetables and medicinal herbs, with a variety of potential pharmacologic activities including anti-inflammatory, antioxidative, antiviral, serum lipid-lowering, and antineoplastic activities. Upon administration, ursolic acid may promote apoptosis and inhibit cancer cell proliferation through multiple mechanisms. This may include the regulation of mitochondrial function through various pathways including the ROCK/PTEN and p53 pathways, the suppression of the nuclear factor-kappa B (NF-kB) pathways, and the increase in caspase-3, caspase-8 and caspase-9 activities.


typhoid Vi polysaccharide vaccine, S typhi Ty2 strain


A vinca alkaloid related to VINBLASTINE that is used as a first-line treatment for NON-SMALL CELL LUNG CANCER, or for advanced or metastatic BREAST CANCER refractory to treatment with ANTHRACYCLINES.


The acetate ester of a fat-soluble vitamin with potent antioxidant properties. Considered essential for the stabilization of biological membranes (especially those with high amounts of polyunsaturated fatty acid), vitamin E is a generic name for a group of compounds known as tocopherols and tocotrienols (tocols). This agent is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, resulting in a decrease in prostaglandin production. Vitamin E also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription. (NCI04)


A synthetic phenethylamine bicyclic derivative with antidepressant activity. Venlafaxine and its active metabolite, O-desmethylvenlafaxine (ODV), are potent inhibitors of neuronal serotonin and norepinephrine reuptake and weak dopamine reuptake inhibitors. This agent may reduce hormone-related vasomotor symptoms. (NCI04)


A phenoxypropanolamine derivative that is a selective beta-1-adrenergic agonist.


An ionic salt essential for the synthesis of cholesterol, protein, and fats. Zinc plays an important role in the proper functioning of the immune system. Zinc is required for the enzyme activities necessary for cell division, cell growth, and wound healing as well as the release of vitamin A from the liver. It plays a role in the acuity of the senses of smell and taste and is required to maintain prostate reproductive health and insulin function. Zinc is also involved in the metabolism of carbohydrates. Zinc chloride is administered orally or parenterally as a nutritional supplement.


A coordination complex of the zinc ion and pyrithione, a derivative of the naturally occurring antibiotic aspergillic acid with antimicrobial, antifungal and anti-seborrheic effects. Although the exact mechanism of action remains to be fully elucidated, pyrithione zinc appears to interfere with the membrane transport of ions and metabolites, ultimately leading to a loss of metabolic control. In addition, this agent causes an influx of copper, leading to a reduction in the activity of iron-sulphur proteins resulting in growth inhibition.


A compound given in the treatment of conditions associated with zinc deficiency such as acrodermatitis enteropathica. Externally, zinc sulfate is used as an astringent in lotions and eye drops. (Reynolds JEF(Ed): Martindale: The Extra Pharmacopoeia (electronic version). Micromedex, Inc, Englewood, CO, 1995)


A sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, zofenopril is hydrolyzed in vivo into its active form zofenoprilat. Zofenoprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Zofenoprilat also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow.


An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA.


A sulfonamide derivative with an anticonvulsant property. The exact mechanism of action remains to be elucidated. Zonisamide appears to block sodium and calcium channels, thereby stabilizing neuronal membranes and suppressing neuronal hyper-synchronization. Although zonisamide shows affinity for the gamma-aminobutyric acid (GABA)/benzodiazepine receptor ionophore complex, it does not potentiate the synaptic activity of GABA. In addition, this agent also facilitates both dopaminergic and serotonergic neurotransmission.


The racemic form of a nonbenzodiazepine, cyclopyrrolone with hypnotic and sedative activity and without significant anxiolytic activity. Although the exact mechanism of action remains to be fully elucidated, zopiclone is able to bind to and activate the omega-1 subtype of the alpha subunit of the gamma-aminobutyric acid-benzodiazepine GABA receptor complex (GABA-A), a chloride ionophore complex in the central nervous system (CNS). This leads to the opening of chloride channels, causing hyperpolarization, inhibition of neuronal firing, and enhancement of the inhibitory effect of GABA. This eventually leads to a hypnotic effect and allows for an induction of sleep.


An acylated inactive complex of streptokinase and human lysine-plasminogen. After injection, the acyl group is slowly hydrolyzed, producing an activator that converts plasminogen to plasmin, thereby initiating fibrinolysis. Its half-life is about 90 minutes compared to 5 minutes for TPA; (TISSUE PLASMINOGEN ACTIVATOR); 16 minutes for UROKINASE-TYPE PLASMINOGEN ACTIVATOR and 23 minutes for STREPTOKINASE. If treatment is initiated within 3 hours of onset of symptoms for acute myocardial infarction, the drug preserves myocardial tissue and left ventricular function and increases coronary artery patency. Bleeding complications are similar to other thrombolytic agents.


An organoplatinum compound that possesses antineoplastic activity.


A species of Clostridium that is the most significant cause of pseudomembranous colitis.


Long-chain polymer of glucose containing 17-20% sulfur. It has been used as an anticoagulant and also has been shown to inhibit the binding of HIV-1 to CD4-POSITIVE T-LYMPHOCYTES. It is commonly used as both an experimental and clinical laboratory reagent and has been investigated for use as an antiviral agent, in the treatment of hypolipidemia, and for the prevention of free radical damage, among other applications.


A 17-kDa single-chain polypeptide growth factor that plays a significant role in the process of WOUND HEALING and is a potent inducer of PHYSIOLOGIC ANGIOGENESIS. It binds to HEPARIN, which potentiates its biological activity and protects it from proteolysis. The growth factor is an extremely potent inducer of DNA synthesis in a variety of cell types from mesoderm and neuroectoderm lineages, and also has chemotactic and mitogenic activities. It was originally named acidic fibroblast growth factor based upon its chemical properties and to distinguish it from basic fibroblast growth factor (FIBROBLAST GROWTH FACTOR 2).


A TGF-beta subtype that was originally identified as a GLIOBLASTOMA-derived factor which inhibits the antigen-dependent growth of both helper and CYTOTOXIC T LYMPHOCYTES. It is synthesized as a precursor molecule that is cleaved to form mature TGF-beta2 and TGF-beta2 latency-associated peptide. The association of the cleavage products results in the formation a latent protein which must be activated to bind its receptor.


A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS.


A spiral bacterium active as a human gastric pathogen. It is a gram-negative, urease-positive, curved or slightly spiral organism initially isolated in 1982 from patients with lesions of gastritis or peptic ulcers in Western Australia. Helicobacter pylori was originally classified in the genus CAMPYLOBACTER, but RNA sequencing, cellular fatty acid profiles, growth patterns, and other taxonomic characteristics indicate that the micro-organism should be included in the genus HELICOBACTER. It has been officially transferred to Helicobacter gen. nov. (see Int J Syst Bacteriol 1989 Oct;39(4):297-405).


The citrate salt of an antineoplastic nonsteroidal selective estrogen receptor modulator (SERM). Tamoxifen competitively inhibits the binding of estradiol to estrogen receptors, thereby preventing the receptor from binding to the estrogen-response element on DNA. The result is a reduction in DNA synthesis and cellular response to estrogen. In addition, tamoxifen up-regulates the production of transforming growth factor B (TGFb), a factor that inhibits tumor cell growth, and down-regulates insulin-like growth factor 1 (IGF-1), a factor that stimulates breast cancer cell growth. Tamoxifen also down-regulates protein kinase C (PKC) expression in a dose-dependant manner, inhibiting signal transduction and producing an antiproliferative effect in tumors such as malignant glioma and other cancers that overexpress PKC.


An eicosanoid, derived from the cyclooxygenase pathway of arachidonic acid metabolism. It is a stable and synthetic analog of EPOPROSTENOL, but with a longer half-life than the parent compound. Its actions are similar to prostacyclin. Iloprost produces vasodilation and inhibits platelet aggregation.


A member of the CXC chemokine family that plays a role in the regulation of the acute inflammatory response. It is secreted by variety of cell types and induces CHEMOTAXIS of NEUTROPHILS and other inflammatory cells.


The sodium salt of levothyroxine, a synthetic levoisomer of thyroxine (T4) that is similar to the endogenous hormone produced by the thyroid gland. In peripheral tissues, levothyroxine is deiodinated by 5'-deiodinase to form triiodothyronine (T3). T3 enters the cell and binds to nuclear thyroid hormone receptors; the activated hormone-receptor complex in turn triggers gene expression and produces proteins required in the regulation of cellular respiration; thermogenesis; cellular growth and differentiation; and the metabolism of proteins, carbohydrates and lipids. T3 also exhibits cardiostimulatory effects.


A quaternary ammonium parasympathomimetic agent with the muscarinic actions of ACETYLCHOLINE. It is hydrolyzed by ACETYLCHOLINESTERASE at a considerably slower rate than ACETYLCHOLINE and is more resistant to hydrolysis by nonspecific CHOLINESTERASES so that its actions are more prolonged. It is used as a parasympathomimetic bronchoconstrictor agent and as a diagnostic aid for bronchial asthma. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1116)


An antiarrhythmia agent used primarily for ventricular rhythm disturbances.


Synthetic pentapeptide corresponding to the amino acids 32-36 of thymopoietin and exhibiting the full biological activity of the natural hormone. It is an immunomodulator which has been studied for possible use in the treatment of rheumatoid arthritis, AIDS, and other primary immunodeficiencies.


fatty acid with anticonvulsant properties.


A synthetic derivative of hydroxyurea with antiasthmatic properties. The leukotriene inhibitor zileuton blocks 5-lipoxygenase, which catalyzes the formation of leukotrienes from arachidonic acid; causes bronchodilation; decreases bronchial mucous secretion and edema; and may prevent or decrease the symptoms of asthma. (NCI04)


An ester of sulfisoxazole, a broad-spectrum sulfanilamide and a synthetic analog of para-aminobenzoic acid (PABA) with antibacterial property. Sulfisoxazole acetyl competes with PABA for the bacterial enzyme dihydropteroate synthase, thereby preventing the incorporation of PABA into dihydrofolic acid, the immediate precursor of folic acid. This leads to an inhibition of bacterial folic acid synthesis and de novo synthesis of purines and pyrimidines, ultimately resulting in cell growth arrest and cell death.


2-pyridinylmethylsulfinylbenzimidazole proton pump inhibitor that is used in the treatment of GASTROESOPHAGEAL REFLUX and PEPTIC ULCER.


A semisynthetic, beta-lactamase-stable, broad-spectrum, third-generation cephalosporin with antibacterial activity. Ceftiofur binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.


A synthetic derivative of emetine; used in the treatment of intestinal amoebiasis.


A synthetic trifluorinated glucocorticoid receptor agonist with antiallergic, antiinflammatory and antipruritic effects. Fluticasone binds and activates glucocorticoid receptor, resulting in the activation of lipocortin. Lipocortin, in turn, inhibits cytosolic phospholipase A2, which triggers a cascade of reactions involved in the synthesis of inflammatory mediators, such as prostaglandins and leukotrienes. Secondly, mitogen-activated protein kinase (MAPK) phosphatase 1 is induced, thereby leads to dephosphorylation and inactivation of Jun N-terminal kinase directly inhibiting c-Jun mediated transcription. Finally, transcriptional activity of nuclear factor (NF)-kappa-B is blocked, thereby inhibits the transcription of cyclooxygenase 2, which is essential for prostaglandin production.


A synthetic lipid-lowering agent with antilipidemic and potential antineoplastic properties. Fluvastatin competitively inhibits hepatic 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent lowers plasma cholesterol and lipoprotein levels, and modulates immune responses through the suppression of MHC II (major histocompatibility complex II) on interferon gamma-stimulated antigen-presenting cells such as human vascular endothelial cells. Due to its anti-inflammatory effects mediated by alterations of lipid metabolism, fluvastatin may possess chemopreventive and therapeutic antineoplastic properties.


A paramagnetic gadolinium-based contrast agent (GBCA), with imaging activity upon magnetic resonance imaging (MRI). When placed in a magnetic field, gadodiamide generates a large local magnetic field, which can enhance the relaxation rate of nearby protons. This change in proton relaxation dynamics, iincreases the MRI signal intensity of tissues in which gadodiamide has accumulated; therefore, visualization of those tissues is enhanced.


A synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictor activities. Halobetasol, a topical steroid, diffuses across cell membranes to interact with cytoplasmic corticosteroid receptors located in both the dermal and intradermal cells, thereby activating gene expression of anti-inflammatory proteins mediated via the corticosteroid receptor response element. Specifically, this agent induces phospholipase A2 inhibitory proteins, which inhibit the release of arachidonic acid, thereby inhibiting the biosynthesis of potent mediators of inflammation, such as prostaglandins and leukotrienes. As a result, halobetasol reduces edema, erythema, and pruritus through its cutaneous effects on vascular dilation and permeability.


A lymphohematopoietic cytokine that plays a role in regulating the proliferation of ERYTHROID PRECURSOR CELLS. It induces maturation of MEGAKARYOCYTES which results in increased production of BLOOD PLATELETS. Interleukin-11 was also initially described as an inhibitor of ADIPOGENESIS of cultured preadipocytes.


An organic, branched-chain alkane with five carbon atoms.


Formulated in various oral forms for use in lactose intolerance, Lactase Enzyme (Lactaid) is a dietary supplement that breaks down lactose (milk sugar) in dairy foods. It prevents gas, diarrhea, and bloating caused by consumption from dairy foods in people that lack the natural lactase enzyme. (NCI04)


A synthetic nonapeptide analogue of the natural gonadotrophin releasing hormone (GnRH) with potential antineoplastic activity. Deslorelin binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Continuous, prolonged administration of goserelin in males results in pituitary GnRH receptor desensitization and inhibition of pituitary secretion of follicle stimulating hormone (FSH) and luteinizing hormone (LH), leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production. (NCI04)


An oxicam derivative and a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic and analgesic activities. Unlike traditional nonselective NSAIDs, meloxicam preferentially inhibits the activity of cyclo-oxygenase II (COX-II), resulting in a decreased conversion of arachidonic acid into prostaglandin precursors. The resulting decrease in prostaglandin synthesis is responsible for the therapeutic effects of meloxicam.


A neurotrophic factor involved in regulating the survival of visceral and proprioceptive sensory neurons. It is closely homologous to nerve growth factor beta and BRAIN-DERIVED NEUROTROPHIC FACTOR.


L1 protein, human papillomavirus type 16 vaccine


A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.


A histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion. The drug is used for the treatment of duodenal ulcers.


A broad-spectrum antimicrobial fluoroquinolone. The drug strongly inhibits the DNA-supercoiling activity of DNA GYRASE.


Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.


A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.


A synthetic analog of natural prostaglandin E1. It produces a dose-related inhibition of gastric acid and pepsin secretion, and enhances mucosal resistance to injury. It is an effective anti-ulcer agent and also has oxytocic properties.


A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against PNEUMOCYSTIS PNEUMONIA in AIDS patients. Myelosuppression is its dose-limiting toxic effect.


A potent hepatotoxic and hepatocarcinogenic mycotoxin produced by the Aspergillus flavus group of fungi. It is also mutagenic, teratogenic, and causes immunosuppression in animals. It is found as a contaminant in peanuts, cottonseed meal, corn, and other grains. The mycotoxin requires epoxidation to aflatoxin B1 2,3-oxide for activation. Microsomal monooxygenases biotransform the toxin to the less toxic metabolites aflatoxin M1 and Q1.


A propiophenone-derived antidepressant and antismoking agent that inhibits the uptake of DOPAMINE.


A trans-carotenoid pigment widely distributed in nature. The compound is used as an oral suntanning agent and as a food and drug coloring agent. Oral ingestion of the compound causes canthaxanthin retinopathy.


A lithium salt, classified as a mood-stabilizing agent. Lithium ion alters the metabolism of BIOGENIC MONOAMINES in the CENTRAL NERVOUS SYSTEM, and affects multiple neurotransmission systems.


A selective serotonin reuptake inhibitor that is used in the treatment of DEPRESSION and a variety of ANXIETY DISORDERS.


An antiarrhythmic agent which exerts a potential- and frequency-dependent block of SODIUM CHANNELS.


A radionuclide imaging agent used primarily in scintigraphy or tomography of the heart to evaluate the extent of the necrotic myocardial process. It has also been used in noninvasive tests for the distribution of organ involvement in different types of amyloidosis and for the evaluation of muscle necrosis in the extremities.


One of the ANTI-ARRHYTHMIA AGENTS, it blocks VOLTAGE-GATED SODIUM CHANNELS and slows conduction within the His-Purkinje system and MYOCARDIUM.


A topically used antibiotic from a strain of Pseudomonas fluorescens. It has shown excellent activity against gram-positive staphylococci and streptococci. The antibiotic is used primarily for the treatment of primary and secondary skin disorders, nasal infections, and wound healing.


A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE that regulates the synthesis and release of pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE.


The type species of ERYTHROVIRUS and the etiological agent of ERYTHEMA INFECTIOSUM, a disease most commonly seen in school-age children.


A cytokine produced by a variety of cell types, including T-LYMPHOCYTES; MONOCYTES; DENDRITIC CELLS; and EPITHELIAL CELLS that exerts a variety of effects on immunoregulation and INFLAMMATION. Interleukin-10 combines with itself to form a homodimeric molecule that is the biologically active form of the protein.


Immunoglobulin preparations used in intravenous infusion, containing primarily IMMUNOGLOBULIN G. They are used to treat a variety of diseases associated with decreased or abnormal immunoglobulin levels including pediatric AIDS; primary HYPERGAMMAGLOBULINEMIA; SCID; CYTOMEGALOVIRUS infections in transplant recipients, LYMPHOCYTIC LEUKEMIA, CHRONIC; Kawasaki syndrome, infection in neonates, and IDIOPATHIC THROMBOCYTOPENIC PURPURA.


A species of parasitic protozoa that infects humans and most domestic mammals. Its oocysts measure five microns in diameter. These organisms exhibit alternating cycles of sexual and asexual reproduction.


A species of parasitic protozoa found in the intestines of humans and other primates. It was classified as a yeast in 1912. Over the years, questions arose about this designation. In 1967, many physiological and morphological B. hominis characteristics were reported that fit a protozoan classification. Since that time, other papers have corroborated this work and the organism is now recognized as a protozoan parasite of humans causing intestinal disease with potentially disabling symptoms.


Anti-CD3 monoclonal antibody that exerts immunosuppressive effects by inducing peripheral T-cell depletion and modulation of the T-cell receptor complex (CD3/Ti).


A multifunctional cytokine secreted by primarily by activated TH2 CELLS that may play a role as a regulator of allergic INFLAMMATION. It has been shown to enhance the growth and CELL DIFFERENTIATION of MAST CELLS, and can act on a variety of other immune cells.


A species of gram-negative, facultatively anaerobic, rod-shaped bacteria that occurs in water, sewage, soil, meat, hospital environments, and on the skin and in the intestinal tract of man and animals as a commensal.


A species of gram-positive, coccoid bacteria whose organisms are normal flora of the intestinal tract. Unlike ENTEROCOCCUS FAECALIS, this species may produce an alpha-hemolytic reaction on blood agar and is unable to utilize pyruvic acid as an energy source.


An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).


Any formulation containing amphotericin B as the active agent for the treatment of fungal infections.


one of the non-essential amino acids commonly occurring in the L-form; may be a neurotransmitter.


A tetracycline with broad-spectrum antibacterial and antiprotozoal activity. Chlortetracycline hydrochloride is bacteriostatic and inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit, thereby preventing the addition of amino acids to the growing peptide chain. This tetracycline is active against a wide range of gram-positive and gram-negative organisms, spirochetes, rickettsial species, certain protozoa and Mycoplasma and Chlamydia organisms.


The hydrochloride salt form of a semisynthetic, orally active pivalate ester of ampicillin with antibacterial activity. Upon absorption, pivampicillin is hydrolyzed into its active form ampicillin by esterases. Ampicillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall, eventually causing cell lysis.


The sodium salt form of cephapirin, a semi-synthetic, broad-spectrum, beta-lactam, first-generation cephalosporin antibiotic with bactericidal activity. Cephapirin sodium inhibits bacterial cell wall synthesis by inhibiting the final transpeptidation step of peptidoglycan synthesis and subsequent cross-linking of peptidoglycan units. This results in a reduction of cell wall stability and leads to cell lysis.


The sodium salt of the phenyl ester of carbenicillin, a broad-spectrum, semisynthetic penicillin derivative with antibacterial activity. Following absorption, carbenicillin phenyl sodium is rapidly hydrolyzed to the active carbenicillin, which binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall, thereby preventing the cross-linkage of peptidoglycans, which are critical components of the bacterial cell wall. This leads to a weakening of the bacterial cell wall, eventually causing bacterial cell lysis.