An organic compound derived from pyridine with potassium channel inhibition activity. Amifampridine inhibits potassium channel efflux, increasing the duration of the action potential, which results in an increase in the duration of calcium channel opening and enhanced acetylcholine (ACh) release. Increased ACh availability at the motor end plate allows muscles to contract.


A guanidine analog with specific affinity for tissues of the sympathetic nervous system and related tumors. The radiolabeled forms are used as antineoplastic agents and radioactive imaging agents. (Merck Index, 12th ed) MIBG serves as a neuron-blocking agent which has a strong affinity for, and retention in, the adrenal medulla and also inhibits ADP-ribosyltransferase.


A synthetic form of the naturally occurring female sex hormone progesterone. Etonogestrel binds to the cytoplasmic progesterone receptors in the reproductive system and subsequently activates progesterone receptor mediated gene expression. As a result of the negative feedback mechanism, luteinizing hormone (LH) release is inhibited, which leads to an inhibition of ovulation and an alteration in the cervical mucus and endometrium.


A clonidine derivative with selective alpha-2-adrenergic agonistic activity. Upon ocular administration, apraclonidine enhances aqueous humor uveoscleral outflow and decreases aqueous production by vasoconstriction. This may decrease intraocular pressure (IOP).


An analogue of GAMMA-AMINOBUTYRIC ACID. It is an irreversible inhibitor of 4-AMINOBUTYRATE TRANSAMINASE, the enzyme responsible for the catabolism of GAMMA-AMINOBUTYRIC ACID and is used as an anticonvulsant. (From Martindale The Extra Pharmacopoeia, 31st ed)


A synthetic steroidal substance with antineoplastic activity. Formestane binds irreversibly to and inhibits the enzyme aromatase, thereby blocking the conversion of cholesterol to pregnenolone and the peripheral aromatization of androgenic precursors into estrogens. (NCI04)


A synthetic derivate of hydroquinone and depigmenting agent. Although the exact mechanism of the depigmenting effects of mequinol remains unclear, it may exert its effect by oxidation of tyrosinase to cytotoxic products in melanocytes. Mequinol may also act by competitively inhibiting the formation of melanin precursors.


para-hydroxybenzoic acid
p-hydroxybenzoic acid


A synthetic derivative of L-arginine with antithrombotic activity. Argatroban is a univalent and direct inhibitor of fibrin-bound thrombin. This agent reversibly binds to the thrombin active site thereby preventing the thrombin-dependent reactions, which include conversion of fibrinogen to fibrin; the activation of factors V, VIII and XI; the activation of protein C; and platelet aggregation. Argatroban is highly selective for thrombin and is able to inhibit the action of both free and clot-associated thrombin. As a result, stabilization of blood clots and coagulation is inhibited.


A pyrazole with competitive alcohol dehydrogenase inhibitor activity. Fomepizole prevents the metabolism of ethylene glycol and methanol by alcohol dehydrogenase, thereby inhibiting the formation of their toxic metabolites, glycolate and oxalate (from ethylene glycol), and formic acid (from methanol). Fomepizole is indicated for use as an antidote in ethylene glycol and methanol poisoning. (NCI05)


An azacitidine derivative and antineoplastic antimetabolite. It inhibits DNA methyltransferase to re-activate silent genes, limiting METASTASIS and NEOPLASM DRUG RESISTANCE. Decitabine is used in the treatment of MYELODISPLASTIC SYNDROMES, and ACUTE MYELOID LEUKEMIA.


A linear furanocoumarin that has phototoxic and anti-inflammatory properties, with effects similar to METHOXSALEN. It is used in PUVA THERAPY for the treatment of PSORIASIS.


An antiprotozoal agent that was used in combination with tibroquinol. The combination agent was withdrawn from the market because of hepatoxicity.


A piperazinoazepine tetracyclic compound that enhances the release of NOREPINEPHRINE and SEROTONIN through blockage of presynaptic ALPHA-2 ADRENERGIC RECEPTORS. It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. It is used for the treatment of depression, and may also be useful for the treatment of anxiety disorders.


A furanyl adenine found in PLANTS and FUNGI. It has plant growth regulation effects.


A polycyclic aromatic hydrocarbon derived from anthracene or phthalic anhydride. Anthraquinone is used in the manufacture of dyes, in the textile and pulp industries, and as a bird repellant.


A nucleoside reverse transcriptase inhibitor analog of adenosine with activity against hepatitis B virus (HBV), herpes virus, and human immunodeficiency virus (HIV).


An inhibitor of ALPHA-GLUCOSIDASES that retards the digestion and absorption of DIETARY CARBOHYDRATES in the SMALL INTESTINE.


used as a solvent, plasticizer, and a wetting and penetrating agent; formula, C2H5NO.


A niacin derivative and nicotinic acid analog with activity as a hypolipidemic agent. Acipimox has special application for the treatment of hyperlipidemia in non-insulin-dependent diabetic patients.


An oral retinoid effective in the treatment of psoriasis. It is the major metabolite of ETRETINATE with the advantage of a much shorter half-life when compared with etretinate.


A colorless, odorless, highly water soluble vinyl monomer formed from the hydration of acrylonitrile. It is primarily used in research laboratories for electrophoresis, chromatography, and electron microscopy and in the sewage and wastewater treatment industries.


A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers.


A monobenzyl ether of hydroquinone with topical depigmentation activity. Although the exact mechanism of action of depigmentation is unknown, the metabolites of monobenzone appear to have a cytotoxic effect on melanocytes. Furthermore, the depigmentation effect might be mediated through the inhibition of tyrosinase, which is essential in the synthesis of melanin pigments, thereby causing permanent depigmentation of the skin.


A nutritional supplement containing a stable, water-soluble dipeptide comprised of the amino acids L-glutamine and L-alanine, with potential protective and absorption enhancing activities. Upon oral or enteral administration, alanylglutamine works locally in the gastrointestinal (GI) tract to both protect the integrity of the intestinal mucosa and maintain intestinal barrier functions. This reduces bacterial translocation, the risk of infection, infection-induced inflammatory damage and infection-associated symptoms, such as diarrhea, dehydration, malabsorption and electrolyte imbalances. Alanylglutamine also increases absorption of other chemicals, enhances epithelial repair, and inhibits apoptosis due to cellular damage, and stimulates cellular proliferation. Altogether, this improves absorption of nutrients, decreases weight loss, reduces diarrhea, decreases the risk of GI-associated infections and improves recovery. Upon absorption, alanylglutamine may also help inhibit muscle protein catabolism.


The dipropionate salt form of alclometasone, a synthetic corticosteroid with low to medium potency. Alclometasone dipropionate is a glucocorticoid receptor agonist that mimics the metabolic, anti-inflammatory, immunosuppressive, antipruritic, and vasoconstrictive effects of natural glucocorticoids. This drug interacts with specific intracellular receptors and binds to DNA to modify gene expression. This results in an induction of synthesis of certain proteins while inhibiting the synthesis of others. Alclometasone dipropionate is used for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. (NCI05)


A synthetic quinazoline compound with smooth muscle relaxing activity. Alfuzosin selectively binds to and 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) and prostate cancer. 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 polysaccharide and linear copolymer, consisting mainly of beta-1,4-linked D-mannuronic acid and alpha-1,4-linked L-glucuronic acid, that occurs in marine algae such as LAMINARIA, and in BIOFILMS produced by PSEUDOMONAS AERUGINOSA.


A substituted benzamide that acts as a dopamine receptor antagonist with antiemetic properties.


A synthetic neuroactive steroid, with anesthetic activity. Upon administration, alfaxalone binds to the gamma-aminobutyric acid (GABA)-A cell surface receptor, thereby enhancing the inhibitory actions of GABA-A in the brain. This leads to modulation of neuronal cell membrane chloride ion transport and induction and maintenance of anesthesia.


An agent, also known as altizide, belonging to the class of thiazide diuretics with antihypertensive activity.


A topical astringent that is used as an antiseptic agent. Aluminum acetate is used to treat inflammation, itching, and stinging of the infected skin and promotes healing.


An aluminum salt of sulfuric acid, an industrial chemical used in many industrial applications. In purification of drinking water, aluminum sulfate acts as a flocculating agent which causes impurities to coagulate and sediment, so that they are easily removed by filtration. It is also used as a mordant in textile dyeing and paper manufacture.


A synthetic glucocorticoid receptor agonist that mimics the metabolic, anti-inflammatory, and immunosuppressive activity of the natural glucocorticoids. Amcinonide interacts with specific corticosteroid receptors and was internalized, which leads to binding of DNA and modification of gene expression. This results in synthesis of anti-inflammatory mediators while inhibiting synthesis of inflammatory mediators. Consequently, an overall reduction in chronic inflammation and autoimmune reactions are achieved.


A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.


The hydroxy salt of ammonium ion. It is formed when AMMONIA reacts with water molecules in solution.


An imide derivative of naphthalic acid. Amonafide intercalates into DNA and inhibits topoisomerase II, resulting in protein-associated strand breaks and impaired DNA and RNA synthesis.


A morpholine antifungal agent for topical use. Amorolfine inhibits delta-14-reductase and delta-7,8-isomerase, which depletes ergosterol and causes ignosterol to accumulate in the fungal cytoplasmic cell membrane.


A synthetic quinazoline derivative, Anagrelide reduces platelet production through a decrease in megakaryocyte maturation. Anagrelide inhibits cyclic AMP phosphodiesterase, as well as ADP- and collagen-induced platelet aggregation. At therapeutic doses, it does not influence white cell counts or coagulation parameters. Anagrelide is used for treatment of essential thrombocythemia to reduce elevated platelet counts and the risk of thrombosis. (NCI04)


An opioid receptor agonist belonging to the piperidine class with analgesic activity. By binding to and activating opioid receptors in the central nervous sytem (CNS), anileridine mimics the endogenous opioids resulting in a decrease of nociceptve neurotransmitters and eventually an analgesic effect.


A synthetic indanedione anticoagulant. Anisindione interferes with the vitamin K-dependent hepatic synthesis of active clotting factors by inhibiting the reduction of vitamin K. This leads to an inhibition of gamma-carboxylation of glutamic acid residues to gamma-carboxyglutamic acid in clotting factors II, VII, IX and X. The consequential effects of this inhibition include a reduced activity of these clotting factors and prolonged blood clotting time.


The edible oil extracted from peanuts. Peanut oil is used primarily as a cooking oil and as a food ingredient.


An inorganic compound with the chemical formula As2O3 that is used for the treatment of ACUTE PROMYELOCYTIC LEUKEMIA in patients who have relapsed from, or are resistant to, conventional drug therapy.


An artemisinin derivative that is used in the treatment of MALARIA.


A water-soluble, semi-synthetic derivative of the sesquiterpine lactone artemisinin with anti-malarial, anti-schistosomiasis, antiviral, and potential anti-neoplastic activities. Upon hydrolysis of artesunate's active endoperoxide bridge moiety by liberated heme in parasite-infected red blood cells, reactive oxygen species and carbon-centered radicals form, which have been shown to damage and kill parasitic organisms. Additionally, in vitro studies demonstrate that this agent induces DNA breakage in a dose-dependent manner. Artesunate has also been shown to stimulate cell differentiation, arrest the cell cycle in the G1 and G2/M phases, inhibit cell proliferation, and induce apoptosis through mitochondrial and caspase signaling pathways. Artemisinin is isolated from the plant Artemisia annua.


A natural and synthetic xanthophyll and nonprovitamin A carotenoid, with potential antioxidant, anti-inflammatory and antineoplastic activities. Upon administration, astaxanthin may act as an antioxidant and reduce oxidative stress, thereby preventing protein and lipid oxidation and DNA damage. By decreasing the production of reactive oxygen species (ROS) and free radicals, it may also prevent ROS-induced activation of nuclear factor-kappa B (NF-kB) transcription factor and the production of inflammatory cytokines such as interleukin-1beta (IL-1b), IL-6 and tumor necrosis factor-alpha (TNF-a). In addition, astaxanthin may inhibit cyclooxygenase-1 (COX-1) and nitric oxide (NO) activities, thereby reducing inflammation. Oxidative stress and inflammation play key roles in the pathogenesis of many diseases, including cardiovascular, neurological, autoimmune and neoplastic diseases.


A fluoroquinolone antibiotic that inhibits bacterial DNA gyrase, thereby inhibiting DNA replication and transcription. Sparfloxacin was withdrawn from the U.S. market due to a high incidence of phototoxicity.


A natural clay-like mineral mixture of hydrated aluminum silicate containing magnesium, adsorbent Attapulgite (kaopectate) acts locally in the intestines to adsorb bacteria and toxins; reduce water loss; and treat diarrhea. Sometimes it is activated by heat to increase absorbency. (NCI04)


A naturally occurring dicarboxylic acid produced by Malassezia furfur and found in whole grain cereals, rye, barley and animal products. Azelaic acid possesses antibacterial, keratolytic, comedolytic, and anti-oxidant activity. Azelaic acid is bactericidal against Proprionibacterium acnes and Staphylococcus epidermidis due to its inhibitory effect on the synthesis of microbial cellular proteins. Azelaic acid exerts its keratolytic and comedolytic effects by reducing the thickness of the stratum corneum and decreasing the number of keratohyalin granules by reducing the amount and distribution of filaggrin in epidermal layers. Azelaic acid also possesses a direct anti-inflammatory effect due to its scavenger activity of free oxygen radical. This drug is used topically to reduce inflammation associated with acne and rosacea.


A narrow-spectrum, semisynthetic penicillin derivative with antibacterial activity. Azidocillin 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 semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.


A monosulfamyl belonging to the class of loop diuretics. Azosemide inhibits sodium and chloride reabsorption throughout the thick ascending limb of the loop of Henle.


A prodrug of ampicillin, a broad-spectrum, semisynthetic, beta-lactam aminopenicillin antibiotic with bactericidal activity. Bacampicillin is hydrolyzed in vivo by esterases to its active metabolite ampicillin. Ampicillin 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 saturated very long-chain fatty acid with a 22-carbon backbone. Behenic acid is a major component of ben oil, extracted from the seeds of the moringa tree.


A carboxyl-containing angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, benazepril is metabolized to its active form benazeprilat. Benazeprilat 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 resulting in vasodilation. Benazeprilat 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 antilipidemic agent that decreases the relative rate of hepatic triacylglycerol synthesis. Benfluorex was never approved for use in the United States and was withdrawn in the European Union because of an increased risk of pulmonary hypertension and valvular disease.


The benzathine salt form of a semisynthetic beta-lactamase resistant penicillin antibiotic with antibacterial activity. Cloxacillin 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.


A synthetic antiparkinson tertiary amine structurally related to atropine, Benztropine Mesylate acts as a central muscarinic antagonist and inhibits dopamine uptake. With antihistaminic and local anesthetic properties as well, it is indicated for symptomatic relief of parkinsonism and drug-induced extrapyramidal reactions. (NCI04)


A fungistatic compound that is widely used as a food preservative. It is conjugated to GLYCINE in the liver and excreted as hippuric acid.


A synthetic butylamino-benzoate derivative related to tetracaine and a peripherally acting antitussive, nonnarcotic Benzonatate reduces the cough reflex by anesthetizing and depressing mechanoreceptors in the respiratory passages, lungs, and pleura. It is recommended for cough relief in the common cold, bronchitis, pneumonia, and for chronic cough such as in asthma. (NCI04)


A nitroimidazole derivative having an antiprotozoal activity by interfering with parasite protein biosynthesis, influencing cytokines production and stimulating host phagocytosis. (NCI)


An intermediate acting agent belonging to the class of thiazide diuretics. Benzthiazide, also known as benzothiazide, is no longer commercially available in the United States.


A white colored, crystalline, inorganic compound that emits toxic fumes of beryllium oxides, hydrofluoric acid and other fluorinated compounds upon heating. Beryllium fluoride is mainly used to produce beryllium metal and alloys and is also used in the production of glass and nuclear reactors. Inhalation exposure to its dust irritates the nose, throat and lungs and can cause pneumonitis. Prolonged exposure can result in a chronic beryllium disease called berylliosis causing granuloma and fibrosis formation in the lungs. Beryllium is a known carcinogen and is associated with an increased risk of developing lung cancer. (NCI05)


A carotenoid that is a precursor of VITAMIN A. Beta carotene is administered to reduce the severity of photosensitivity reactions in patients with erythropoietic protoporphyria (PORPHYRIA, ERYTHROPOIETIC).


The 17,21-dipropionate ester of betamethasone, a synthetic glucocorticoid with metabolic, immunosuppressive and anti-inflammatory actions. Betamethasone dipropionate binds to specific intracellular glucocorticoid receptors and subsequently binds to DNA to modify gene expression. The synthesis of certain anti-inflammatory proteins is induced while the synthesis of certain inflammatory mediators is inhibited. As a result, there is an overall reduction in chronic inflammation and autoimmune reactions.


A slowly hydrolyzing muscarinic agonist with no nicotinic effects. Bethanechol is generally used to increase smooth muscle tone, as in the GI tract following abdominal surgery or in urinary retention in the absence of obstruction. It may cause hypotension, HEART RATE changes, and BRONCHIAL SPASM.


A bismuth salt of salicylic acid. Little absorbed from the gastrointestinal tract, bismuth subsalicylate exerts a local effect on the gastric mucosa, coating it and protecting it from the corrosive effects of acid and pepsin. This agent also has local antimicrobial properties. (NCI04)


A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS.


A diphenylmethane derivative with two hydroxyphenyl groups. Bisphenol A (BPA) is a colorless solid that is used in the synthesis of commercial plastics, including polycarbonates and epoxy resins, which are incorporated into a wide variety of consumer goods. Ingested BPA may exhibit estrogenic effects. Exposure to BPA may increase the risk of certain cancers.


A diester sympathomimetic amine with bronchodilator activity. As an ester prodrug, bitolterol is hydrolyzed by esterases to its active metabolite colterol (N-t-butylarterenol). Colterol selectively binds to and activates beta-2 adrenergic receptors in bronchiolar smooth muscle, thereby causing stimulation of adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased intracellular cAMP levels cause relaxation of bronchial smooth muscle. This increases air flow and prevents bronchospasms and may eventually lead to an improvement of airway function.


A pyrimidinone derivative with anti-allergic activity. Pemirolast blocks the antigen-mediated calcium ion influx into mast cells. This prevents mast cell degranulation, resulting in mast cell stabilization and inhibition of the release of inflammatory mediators, such as histamine and leukotrienes, which are involved in the allergic process. Pemirolast also prevents inflammatory mediator release from eosinophils.


A semi-synthetic cephalosporin and a beta-lactam antibiotic with bactericidal activity. Cefprozil's effect is dependent on its binding to penicillin-binding proteins (PBPs) located in the bacterial cytoplasmic membrane. Binding results in the inhibition of the transpeptidase enzymes, thereby preventing cross-linking of the pentaglycine bridge with the fourth residue of the pentapeptide and interrupting consequent synthesis of peptidoglycan chains. As a result, cefprozil inhibits bacterial septum and cell wall synthesis formation.


A recombinant version of the cardiac neurohormone, human B-type natriuretic peptide (hBNP) produced by the ventricular myocardium. Nesiritide binds to natriuretic peptide receptors on vascular smooth muscle and endothelial cells, through which it triggers guanylate cyclase dependent signal transduction resulting in increase of intracellular concentrations of cGMP. This leads to smooth muscle cell relaxation causing arterial and venous dilatation.


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 fixed-ratio combination of amoxicillin trihydrate and potassium clavulanate.


A nonsteroidal anti-inflammatory drug (NSAID) with analgesic and anti-inflammatory activities. Upon ophthalmic administration, bromfenac binds to and inhibits the activity of cyclooxygenase II (COX II), an enzyme which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins (PG). By inhibiting PG formation, bromfenac is able to inhibit PG-induced inflammation, thereby preventing vasodilation, leukocytosis, disruption of the blood-aqueous humor barrier, an increase in vascular permeability and an increase in intraocular pressure (IOP).


A brominated derivative of diphenhydramine, an ethanolamine derivative and histamine H1 receptor antagonist with anti-allergic, sedative, antiemetic and anticholinergic properties. Bromazine competitively and selectively blocks central and peripheral histamine H1 receptors, thereby alleviating the symptoms caused by endogenous histamine on bronchial, capillary and gastrointestinal (GI) smooth muscles. This prevents histamine-induced bronchoconstriction, vasodilation, increased capillary permeability, itching, and spasmodic contractions of GI smooth muscle. In addition, bromazine binds to and blocks peripheral and central muscarinic receptors.


A triazolo-benzodiazepine derivative with sedative, hypnotic, anxiolytic and anticonvulsant activities. Brotizolam binds to the benzodiazepine binding site on the gamma aminobutyric acid (GABA)-A receptor in the central nervous system (CNS). This leads to an increase in the opening of chloride channels, membrane hyperpolarization and increases the inhibitory effect of GABA on the CNS.


A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.


A barbiturate that exerts its effect by mimicking the inhibitory effect of gamma-aminobutyric acid (GABA) by binding to a site, distinct from the benzodiazepine binding site, on the GABA receptor. This leads to an increase in the duration of GABA-mediated opening of chloride channels and enhances the inhibitory effect of GABA. Consequently, its physiologic effects include sedation, hypnosis, reduction of anxiety, and respiratory depression and the drug causes tolerance and dependence.


A synthetic imidazole derivative with fungistatic properties. Butoconazole interferes with steroid biosynthesis by inhibiting the conversion of lanosterol to ergosterol, thereby changing the fungal cell membrane lipid composition. This alters cell permeability and leads to growth inhibition. Butaconazole nitrate is active against many dermatophytes and yeasts. It also contains antibacterial effects against some gram-positive organisms.


A four carbon acid, CH3CH2CH2COOH, with an unpleasant odor that occurs in butter and animal fat as the glycerol ester.


A synthetic alkylamine with non-sedative antihistaminergic activity. Acrivastine competitively blocks the histamine H1 receptor and limits the typical allergic and anaphylactic responses, including bronchoconstriction, vasodilation, increased capillary permeability, and spasmodic contraction of gastrointestinal smooth muscle, caused by actions of histamine on bronchial, and gastrointestinal smooth muscles, and on capillaries. This drug also prevents histamine-induced pain and itching of the skin and mucous membranes. (NCI05)


A cadmium halide in the form of colorless crystals, soluble in water, methanol, and ethanol. It is used in photography, in dyeing, and calico printing, and as a solution to precipitate sulfides. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)


A whitish, crystalline, inorganic compound that forms toxic fumes of cadmium oxides when heated. Calcium sulfate is used in electroplating, vacuum tubes, fluorescent screens, analytical chemistry, as a fungicide and as a chemical intermediate to produce cadmium containing pigments and stabilizers. Exposure to this substance irritates the eyes, skin and respiratory tract and causes damage to the lungs resulting in shortness of breath, chest pain and pulmonary edema, and can also damage the kidneys causing proteinuria and decreased renal function. Calcium sulfate is a known carcinogen and is associated with an elevated risk of developing lung cancer. (NCI05)


A yellow to orange colored, crystalline, inorganic compound that forms toxic fumes of cadmium oxides when heated. Cadmium sulfide is used as pigment in paints, plastics, textiles, ceramic and glass and is also used in solar cells, smoke and radiation detectors, light-emitting diodes and photomultipliers. Exposure to this substance irritates the eyes, skin and respiratory tract and causes damage to the lungs resulting in shortness of breath, chest pain and pulmonary edema, and can also damage the kidneys causing proteinuria and decreased renal function. Calcium sulfide is a known carcinogen and is associated with an elevated risk of developing lung cancer. (NCI05)


An orally bioavailable, hydroxycinnamic acid derivative and polyphenol, with potential anti-oxidant, anti-inflammatory, and antineoplastic activities. Upon administration, caffeic acid acts as an antioxidant and prevents oxidative stress, thereby preventing DNA damage induced by free radicals. Caffeic acid targets and inhibits the histone demethylase (HDM) oncoprotein gene amplified in squamous cell carcinoma 1 (GASC1; JMJD2C; KDM4C) and inhibits cancer cell proliferation. GASC1, a member of the KDM4 subgroup of Jumonji (Jmj) domain-containing proteins, demethylates trimethylated lysine 9 and lysine 36 on histone H3 (H3K9 and H3K36), and plays a key role in tumor cell development.


Commercial citrate of caffeine, though not a definite salt. It is the alkaloid caffeine, with a portion of adherent citric acid, as indicated by its pharmacopoeial name (citrated caffeine). Its general action and uses are the same as those given under caffeine. Caffeine citrate is used chiefly as a remedy for the idiopathic headache (migraine). This salt is very soluble in water, and is assimilated much more readily than pure caffeine when taken into the stomach. (NCI04)


The calcium salt form of heparin. As a glycosaminoglycan anticoagulant, heparin calcium binds to antithrombin III to form a heparin-antithrombin III complex. The complex binds to and irreversibly inactivates thrombin and other activated clotting factors IX, X, XI, and XII and prevents the transformation of fibrinogen to fibrin. (NCI)


A loosely cross-linked synthetic polycarboxylic-type hydrophilic polymer resin, laxative and anti-diarrheal Calcium Polycarbophil increases stool frequency, fecal water content, and fecal weight in a dose-dependent manner. It is used for idiopathic constipation, secretory diarrhea, and irritable bowel syndrome. (NCI04)


A steroid derivative that is the simplest sterol, characterized by the hydroxyl group in position C-3 of the steroid skeleton, and saturated bonds throughout the sterol structure, with the exception of the 5-6 double bond in the B ring.


Oil, derived from cultivars of BRASSICA NAPUS (RAPESEED) and other BRASSICA species, that are low in erucic acid and GLUCOSINOLATES. The word Canola stands for CANadian Oil Low Acid.


A saturated medium-chain fatty acid with an 8-carbon backbone. Octanoic acid is found naturally in the milk of various mammals and is a minor component of coconut oil and palm kernel oil.


The tromethamine salt of the (15S)-15 methyl analogue of naturally occurring prostaglandin F2 alpha (PGF2 alpha) with oxytocic activity. Mimicking endogenous PGF2 alpha, carboprost activates prostaglandin F receptor, a G-protein coupled receptor, on smooth muscle cells, thereby resulting in smooth muscle contractions. When administered intramuscularly on gravid subjects, this agent induces myometrium contractions, thereby initiating luteolysis and consequently parturition. Furthermore, carboprost's action on vascular smooth muscle and gastrointestinal tract sphincters leads to raised blood pressure and induces vomiting or diarrhea, respectively.


A propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic activities, used exclusively in veterinary medicine. Carprofen inhibits the activity of the enzymes cyclo-oxygenase (COX) I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes. This inhibits the formation of prostaglandins, by prostaglandin synthase, that are involved in pain, inflammation and fever. Ibuprofen also causes a decrease in the formation of thromboxane A2 synthesis, by thromboxane synthase, thereby inhibiting platelet aggregation.


A carbazole and propanol derivative that acts as a non-cardioselective beta blocker and vasodilator. It has blocking activity for ALPHA 1 ADRENERGIC RECEPTORS and, at higher doses, may function as a blocker of CALCIUM CHANNELS; it also has antioxidant properties. Carvedilol is used in the treatment of HYPERTENSION; ANGINA PECTORIS; and HEART FAILURE. It can also reduce the risk of death following MYOCARDIAL INFARCTION.


The sodium salt form of cefamandole formyl ester. Cefamandole nafate is a pro-drug that is hydrolyzed by plasma esterases to produce cefamandole, a semi-synthetic beta-lactam, second-generation cephalosporin antibiotic with bactericidal activity. Cefamandole 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 results in the weakening of the bacterial cell wall and causes cell lysis.


A semisynthetic, broad-spectrum, fourth-generation cephalosporin with antibacterial activity. Cefepime 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 semisynthetic, beta-lactamase-stable, third-generation cephalosporin with antibacterial activity. Cefetamet 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 third-generation, aminothiazolyl cephalosporin for parenteral use. Cefodizime has broad-spectrum activity and is stable to most beta-lactamases.


A semi-synthetic, broad-spectrum, beta-lactam, second-generation cephalosporin antibiotic with bactericidal activity. Ceforanide causes inhibition of bacterial cell wall synthesis by inactivating penicillin binding proteins (PBPs) thereby interfering with the final transpeptidation step required for cross-linking of peptidoglycan units which are a component of the cell wall. This results in a reduction of cell wall stability and causes cell lysis.


A third generation semi-synthetic cephalosporin and a beta-lactam antibiotic with bactericidal activity. Cefpodoxime's effect is dependent on its binding to penicillin-binding proteins (PBPs) located in the bacterial cytoplasmic membrane. Binding results in the inhibition of the transpeptidase enzymes, thereby preventing cross-linking of the pentaglycine bridge with the fourth residue of the pentapeptide and interrupting consequent synthesis of peptidoglycan chains. As a result, cefpodoxime inhibits bacterial septum and cell wall synthesis formation.


A semisynthetic, beta-lactamase-stable, third-generation cephalosporin with antibacterial activity. Ceftibuten 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 second generation semi-synthetic cephalosporin and a beta-lactam antibiotic with bactericidal activity. Cefuroxime's effect is dependent on its binding to penicillin-binding proteins (PBPs) located in the bacterial cytoplasmic membrane. Binding results in the inhibition of the transpeptidase enzymes, thereby preventing cross-linking of the pentaglycine bridge with the fourth residue of the pentapeptide and interrupting consequent synthesis of peptidoglycan chains. As a result, cefuroxime inhibits bacterial septum and cell wall synthesis formation.


A cardioselective beta-1 adrenergic antagonist that has intrinsic sympathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION.


A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.


Cetyltrimethylammonium compound whose salts and derivatives are used primarily as topical antiseptics.


A synthetic, solid, fatty alcohol and nonionic surfactant. Cetyl alcohol is used as an emulsifying agent in pharmaceutical preparations.


The gluconate salt form of chlorhexidine, a biguanide compound used as an antiseptic agent with topical antibacterial activity. Chlorhexidine gluconate is positively charged and reacts with the negatively charged microbial cell surface, thereby destroying the integrity of the cell membrane. Subsequently, chlorhexidine gluconate penetrates into the cell and causes leakage of intracellular components leading to cell death. Since gram positive bacteria are more negatively charged, they are more sensitive to this agent.


A chlorine compound and oxidizing agent with disinfectant, antiviral and anti-bacterial activities. Upon administration, chlorine dioxide may inactivate the pathogen and may prevent spreading.


The chloride salt form of acetylcholine, a synthetic, quaternary amino alcohol with cholinergic properties. Acetylcholine chloride mimics the parasympathomimetic effect of the endogenous compound acetylcholine. Administered as an ophthalmic solution, this drug stimulates the cholinoceptors in the sphincter muscle of the iris, causing the pupil to constrict. (NCI05)


The phosphate salt of chloroquine, a quinoline compound with antimalarial and anti-inflammatory properties. Chloroquine is the most widely used drug against malaria, except for those cases caused by chloroquine resistant Plasmodium falciparum. Although the mechanism of action is not fully understood, chloroquine is shown to inhibit the parasitic enzyme heme polymerase that converts the toxic heme into non-toxic hemazoin, thereby resulting in the accumulation of toxic heme within the parasite. Chloroquine may also interfere with the biosynthesis of nucleic acids.


A synthetic quinoline derivative with antibacterial activity. Although the mechanism of action is not fully understood, topical administration of chloroxine diminishes mitotic activity in the epidermis, thereby reducing excessive scaling associated with dandruff or seborrheic dermatitis of the scalp, including psoriasis and eczema.


A glucose-linked chloroethylnitrosourea with potential antineoplastic activity. Chlorozotocin alkylates DNA and proteins, induces the formation of interstrand DNA and DNA-protein crosslinks, and causes DNA strand breakage, thereby damaging DNA and resulting in cell death. This agent has been shown to exhibit antitumor and immunomodulatory effects in cell lines and animal models. Chlorozotocin is a mutagen and is less myelotoxic than other nitrosoureas. (NCI04)


The carbamate ester form of chlorphenesin, a preservative agent and centrally-acting muscle relaxant with some anti-bacterial and anti-fungal, muscle relaxing and potential antineoplastic activities. Although the exact mechanism of action (MoA) has yet to be fully elucidated, chlorphenesin may inhibit tumor cell proliferation and metastasis.


An orally bioavailable oxicam and non-steroidal anti-inflammatory drug (NSAID), with analgesic, anti-pyretic, anti-thrombotic and anti-inflammatory activities. Upon oral administration, lornoxicam binds to and inhibits the activity of the cyclooxygenase enzymes (COX) type 1 (COX-1) and type 2 (COX-2). This blocks COX-mediated signaling pathways, which leads to reduced prostaglandin and thromboxane production and decreased pain, fever and inflammation.


A major primary bile acid produced in the liver and usually conjugated with glycine or taurine. It facilitates fat absorption and cholesterol excretion.


The choline salt of salicylic acid, a nonsteroidal anti-inflammatory drug (NSAID), with analgesic, antipyretic, anti-inflammatory, anti-rheumatic and immunomodulating activities. Upon oral administration, salicylic acid irreversibly acetylates cyclooxygenases I and II, thereby inhibiting prostaglandin (PG) synthesis and the PG-associated inflammation, fever and pain. This agent may induce cancer cell apoptosis and modulate the immune response.


The choline salt of theophylline with an anti-asthmatic property. Oxtriphylline appears to inhibit phosphodiesterase and prostaglandin production, regulates calcium flux and intracellular calcium distribution, and antagonizes adenosine. Physiologically, this agent causes relaxation of bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates cardiac muscle, as well as induces diuresis and gastric acid secretion. It may also suppress inflammation and improve contractility of the diaphragm.


A dark red to brown colored, crystalline, inorganic compound that emits toxic chromium fumes upon heating. Chromium trioxide is highly corrosive and is a strong oxidizing agent. This substance is mainly used in the production of wood preservatives and organic chemicals, but is also used in metal finishing and chrome plating and as a corrosion inhibitor. Chromium trioxide primarily affects the nose, throat and lungs causing ulcerations, shortness of breath, bronchitis, pneumonia and asthma-like allergy 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 synthetic, broad-spectrum antifungal agent with additional antibacterial and anti-inflammatory activities. Ciclopirox exerts its action by binding to and chelating trivalent cations, such as Fe3+ and Al3+, thereby inhibiting the availability of essential co-factors for enzymes. This may lead to a loss of activity of enzymes that are essential for cellular metabolism, organization of cell wall structure and other crucial cell functions. In addition, ciclopirox exerts its anti-inflammatory activity by inhibiting 5-lipoxygenase and cyclooxygenase (COX).


One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors) used for hypertension. It is a prodrug that is hydrolyzed after absorption to its main metabolite cilazaprilat.


A quinoline and tetrazole derivative that acts as a phosphodiesterase type 3 inhibitor, with anti-platelet and vasodilating activity. It is used in the treatment of PERIPHERAL VASCULAR DISEASES; ISCHEMIC HEART DISEASE; and in the prevention of stroke.


A choleretic agent. Cinametic acid relaxes the sphincter of Oddi and regulates hepato-biliary function. In addition, this agent is used in liver function tests.


A monoterpene and cyclohexanol derivative that is the major component of EUCALYPTUS OIL. It is used in mouthwash, insect repellent, and as a cough suppressant, and also is widely used as a flavoring agent and solvent. It has antimicrobial properties.


A fibrate derivative with antilipidemic activity.


A key intermediate in metabolism. It is an acid compound found in citrus fruits. The salts of citric acid (citrates) can be used as anticoagulants due to their calcium chelating ability.


A semisynthetic macrolide antibiotic derived from ERYTHROMYCIN that is active against a variety of microorganisms. It can inhibit PROTEIN SYNTHESIS in BACTERIA by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation.


A beta-lactam antibiotic produced by the actinobacterium Streptomyces clavuligerus. It is a suicide inhibitor of bacterial beta-lactamase enzymes. Administered alone, it has only weak antibacterial activity against most organisms, but given in combination with other beta-lactam antibiotics it prevents antibiotic inactivation by microbial lactamase.


The phosphate salt form of clindamycin, a semi-synthetic, chlorinated broad spectrum antibiotic produced by chemical modification of lincomycin. Clindamycin phosphate is used in topical preparations.


A 1,5-benzodiazepine and partial gamma-aminobutyric acid (GABA) receptor agonist, with anxiolytic, sedative, and anticonvulsant activities. Clobazam binds to a specific site, distinct from the inhibitory neurotransmitter GABA binding site, on the benzodiazepine-GABA-A-chloride ionophore receptor complex located in the central nervous system (CNS). This binding causes an allosteric modification of the receptor and enhances the affinity of GABA to the receptor leading to an increase in the opening of chloride-channels. This leads to an increase in chloride ion conductance, neuronal hyperpolarization, inhibition of the action potential and a decrease in neuronal excitability.


This is the form in trademark preparations.


A glucocorticoid receptor agonist with metabolic, anti-inflammatory, and immunosuppressive activity. Clocortolone pivalate exerts its effect by interacting with specific intracellular 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 are accomplished.


A bacteriostatic antibiotic with activity against Gram-positive bacteria. Clofoctol is used in the treatment of upper and lower respiratory tract infections.


A reddish, toxic, metallic salt. Cobalt sulfate is used in the electrochemical industries, as a drier in paints and inks, as a coloring agent, in storage batteries and as a supplement for Vitamin B12 deficiency. Exposure to cobalt sulfate results in irritation of the skin, eyes and respiratory tract and affects the thyroid, lungs, heart and kidneys. Cobalt sulfate is mutagenic in mammalian cells and is reasonably anticipated to be a human carcinogen based on evidence of carcinogenicity in experimental animals. (NCI05)


The edible oil extracted from the kernel or meat of the coconut of Cocos nucifera. In addition to its use as a food ingredient and cooking oil, coconut oil is commonly used in skincare preparations and soaps.


A sulfate salt of copper. It is a potent emetic and is used as an antidote for poisoning by phosphorus. It also can be used to prevent the growth of algae.


A purine nucleoside antimetabolite and antibiotic isolated from the fungus Cordyceps militaris with potential antineoplastic, antioxidant, and anti-inflammatory activities. Cordycepin is an inhibitor of polyadenylation, activates AMP-activated protein kinase (AMPK) and reduces mammalian target of rapamycin (mTOR) signaling, which may result in both the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. mTOR, a serine/threonine kinase belonging to the phosphatidylinositol 3-kinase (PI3K)-related kinase (PIKK) family, plays an important role in the PI3K/AKT/mTOR signaling pathway that regulates cell growth and proliferation, and its expression or activity is frequently dysregulated in human cancers.


The synthetic hemisuccinate salt form of hydrocortisone, a corticosteroid with anti-inflammatory and immunosuppressive properties. Hydrocortisone acetate initially binds to the cytoplasmic glucocorticoid receptor; then the receptor-ligand complex is translocated to the nucleus where it initiates the transcription of genes encoding for anti-inflammatory mediators, such as 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.


The acetate ester of cortisone that is used mainly for replacement therapy in adrenocortical insufficiency and in the treatment of many allergic and inflammatory disorders.


The acetic acid ester of metacresol, an agent with antiseptic and analgesic properties. m-Cresyl acetate is used in an otic solution to treat bacterial and fungal infections of the outer ear, and in endodontic procedures.


A dihydropyridine derivative with diuretic and antihypertensive activity. Cicletanine exerts thiazide-like diuretic activity. In addition, this agent inhibits protein kinase C (PKC) and is able to reverse vasoconstriction through the inhibition of PKC-mediated inhibition of Na/K-ATPase phosphorylation.


A centrally acting skeletal muscle relaxant with antidepressant activity. The exact mechanism of action of cyclobenzaprine has not been fully determined, but this drug seems to primarily act at the brain stem to reduce tonic somatic motor activity, influencing both gamma and alpha motor neurons leading to a reduction in muscle spasms.


cyclohexane ring substituted by one or more ketones in any position.


A benzothiadiazide belonging to the class of thiazide diuretics. Cyclothiazide is indicated as adjunctive therapy in edema and in the treatment of hypertension. In addition, this agent is capable of inhibiting rapid desensitization of the ionotropic alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA)-type glutamate receptors, thereby potentiating glutamate responses which may induce seizures activity. Cyclothiazide was also found to inhibit gamma-aminobutyric acid (GABA)-A receptors.


An agent with anti-androgen and progestational properties. It shows competitive binding with dihydrotestosterone at androgen receptor sites.


A reddish, synthetic anthraquinone derivative. Danthron has been widely used as a laxative, but is no longer used to treat constipation and is currently used as an antioxidant in synthetic lubricants, in the synthesis of experimental antitumor agents, as a fungicide and as an intermediate for making dyes. This substance is a suspected mutagen and is reasonably anticipated to be a human carcinogen based on evidence of carcinogenicity in experimental animals. (NCI05)


A cyclic lipopeptide antibiotic that inhibits GRAM-POSITIVE BACTERIA.


A saturated medium-chain fatty acid with a 10-carbon backbone. Capric acid is found naturally in the coconut and palm kernel oils as well as the milk of various mammals.


A synthetic glucocorticoid prodrug, with anti-inflammatory and immunomodulating properties. Upon administration, the active metabolite of deflazacort, 21-desacetyl deflazacort, binds to and activates tissue glucocorticoid receptors. This results in the inhibition of specific leukocyte functions and the inhibition of proinflammatory cytokine production.


A benzothiadiazine sulfonamide derivative belonging to the class of the thiazide diuretics.


The bromide salt form of demecarium, a quaternary ammonium compound and a long-acting cholinesterase inhibitor with parasympathomimetic activity. When used topically, demecarium inactivates both pseudocholinesterase and acetylcholinesterase, thereby preventing acetylcholine breakdown and increasing acetylcholine activity. This causes contraction of the iris sphincter muscle (producing miosis) and the ciliary muscle (affecting the accommodation reflex). In so doing, this agent increases the outflow of the aqueous humor, thereby reducing intraocular pressure.


A synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents (ORAL CONTRACEPTIVES, COMBINED).


The acetate salt form of Dexamethasone, a synthetic adrenal corticosteroid with potent anti-inflammatory properties. In addition to binding to specific nuclear steroid receptors, dexamethasone also interferes with NF-kB activation and apoptotic pathways. This agent lacks the salt-retaining properties of other related adrenal hormones. (NCI04)


An alkylamine derivative with anticholinergic and sedative properties. Dexbrompheniramine is a histamine H1-receptor antagonist that competes with histamine for the H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels and respiratory tract. The antagonistic action of this agent blocks the activities of endogenous histamine, which subsequently leads to temporary relief from the negative histamine-mediated symptoms of allergic reaction such as bronchoconstriction, vasodilation, increased capillary permeability and spasmodic contractions of gastrointestinal smooth muscle.


An alkylamine, and first-generation histamine antagonist with anti-allergic activity. Dexchlorpheniramine competitively blocks H1 receptors, thereby preventing the actions of histamine on bronchial smooth muscle, capillaries and gastrointestinal (GI) smooth muscle. The antagonistic action of this agent blocks the activities of endogenous histamine, thereby preventing histamine-induced bronchoconstriction, vasodilation, increased capillary permeability, and GI smooth muscle spasms.


An alcoholic analogue of D-pantothenic acid and cholinergic agent. Dexpanthenol acts as a precursor of coenzyme A necessary for acetylation reactions and is involved in the synthesis of acetylcholine. Although the exact mechanism of the actions of dexpanthenol is unclear, it may enhance the effect of acetylcholine. Dexpanthenol acts on the gastrointestinal tract and increases lower intestinal motility. It is also applied topically to the skin to relieve itching and to promote healing.


Diamond. A crystalline form of carbon that occurs as hard, colorless or tinted isomeric crystals. It is used as a precious stone, for cutting glass, and as bearings for delicate mechanisms. (From Grant & Hackh's Chemical Dictionary, 5th ed)


An orally-active, semisynthetic, fourth generation, nonethinylated progestogen with antiproliferative, antiandrogenic, anti-inflammatory and antiangiogenic activities that is used in hormone therapy and as a female contraceptive. Upon oral administration, dienogest binds intracellular progesterone receptors which then translocate to the nucleus where the drug-receptor complex interacts with progesterone response elements, thus altering the expression of target genes. Dienogest reduces the production of estradiol, prevents ovulation and alters the cervical mucus and endometrium. In addition, dienogest appears to suppress the expression of cell cycle regulator cyclin D1. Altogether, this may prevent the growth of endometrial epithelial cells and may reduce symptoms associated with leiomyoma.


A clear, colorless liquid used as a plasticizer for fabricating flexible materials for many household products. It is also used in cosmetics, insecticides and aspirin.


A colorless, corrosive, oily liquid that darkens with age and has a faint peppermint odor. Diethyl sulfate is mainly used as an ethylating agent in organic synthesis and in the dye and textile manufacturing. Exposure to this substance results in severe irritation to the eyes, skin and respiratory tract. It is a possible mutagen and is reasonably anticipated to be a human carcinogen based on evidence of carcinogenicity in experimental animals and may be associated with developing laryngeal cancer. (NCI05)


A phenylpiperidine with antidiarrheal activity and an active metabolite of diphenoxylate. Difenoxin is chemically related to the narcotic opioid meperidine. Difenoxin acts primarily on the gastrointestinal wall by binding to opioid receptors on acetylcholine-containing nerves and inhibiting the release of acetylcholine from presynaptic nerve terminals. This leads to a reduction in intestinal motility. Difenoxin hydrochloride also mimics the action of endogenous opioid peptides at the CNS opioid receptors, (primarily mu-receptors), thereby inducing CNS effects.


The acetate salt form of diflorasone, a synthetic glucocorticoid with anti-inflammatory and immunosuppressive properties. Like other glucocorticoids, diflorasone enters the cell by diffusion across the cell membrane and binds to the glucocorticoid receptor (GR) in the cytoplasm. The receptor complex subsequently translocates to the nucleus and activates or represses genes by interacting with short, palindromic DNA sequences called glucocorticoid response element (GRE). Gene activation leads to the exertion of anti-inflammatory effects, e.g. upregulation of IkappaB, while gene repression inhibits production of pro-inflammatory cytokines such as interleukin-1 (IL-1), IL-2 and IL-6, thereby preventing activation of cytotoxic T-lymphocytes.


A topical corticosteroid and prednisolone acetate derivative, with anti-inflammatory activity. Upon instillation into the eye, difluprednate binds to and activates the glucocorticoid receptor (GR). The receptor-ligand complex binds to promoter regions of certain genes and initiates RNA transcription. This results in an induction of synthesis of phospholipase A2 inhibitory proteins, thereby inhibiting the synthesis of arachidonic acid and preventing the synthesis of certain inflammatory mediators, such as prostaglandins and leukotrienes. This reduces ocular inflammation and pain.


A glycoside compound, extracted from the leaves and seeds of the common foxglove, with anti-arrhythmic property. Digitalin inhibits the enzymatic activity of the sodium-potassium ATPase pump in cardiac tissue, thereby increasing intracellular sodium and calcium levels and providing a positive inotropic effect. This results in increased force of myocardial muscle contraction. This agent also has a vagal effect on the parasympathetic nervous system, and as such slows the ventricular heart rate as well as helps eliminate fluid from body tissues.


The purified component of HEMATOPORPHYRIN DERIVATIVE, it consists of a mixture of oligomeric porphyrins. It is used in photodynamic therapy (HEMATOPORPHYRIN PHOTORADIATION); to treat malignant lesions with visible light and experimentally as an antiviral agent. It is the first drug to be approved in the use of PHOTODYNAMIC THERAPY in the United States.


A colorless volatile poisonous liquid compound used as a solvent, fuel, aerosol, propellant and refrigerant. (NCI)


An orally bioavailable methyl ester of fumaric acid and activator of nuclear factor erythroid 2 [NF-E2]-related factor 2 (Nrf2, Nfe2l2), with potential neuroprotective, immunomodulating and radiosensitizing activities. Although the exact mechanism of action through which dimethyl fumarate exerts its neuroprotective and immunomodulatory effects have yet to be fully understood, upon oral administration, dimethyl fumarate is converted into its active metabolite monomethyl fumarate (MMF) and MMF binds to Nrf2. Subsequently, Nrf2 translocates to the nucleus and binds to the antioxidant response element (ARE). This induces the expression of a number of cytoprotective genes, including NAD(P)H quinone oxidoreductase 1 (NQO1), sulfiredoxin 1 (Srxn1), heme oxygenase-1 (HO1, HMOX1), superoxide dismutase 1 (SOD1), gamma-glutamylcysteine synthetase (gamma-GCS), thioredoxin reductase-1 (TXNRD1), glutathione S-transferase (GST), glutamate-cysteine ligase catalytic subunit (Gclc) and glutamate-cysteine ligase regulatory subunit (Gclm); this also increases the synthesis of the antioxidant glutathione (GSH). The intraneuronal synthesis of GSH may protect neuronal cells from damage due to oxidative stress. Dimethyl fumarate also appears to inhibit the nuclear factor-kappa B (NF-kB)-mediated pathway, modulates the production of certain cytokines and induces apoptosis in certain T-cell subsets. Its radiosensitizing activity is due to this agent's ability to bind to and sequester intracellular GSH, thereby depleting intracellular GSH and preventing its anti-oxidative effects. This enhances the cytotoxicity of ionizing radiation in hypoxic cancer cells. Nrf2, a leucine zipper transcription factor, plays a key role in redox homeostasis and cytoprotection against oxidative stress.


An odorless, corrosive, oily liquid with an onion-like odor that emits toxic fumes upon heating. Dimethyl sulfate is used in industry as a methylating agent in the manufacture of many organic chemicals. Inhalation exposure to its vapors is highly irritating to the eyes and lungs and may cause damage to the liver, kidney, heart and central nervous system, while dermal contact causes severe blistering. It is a possible mutagen and is reasonably anticipated to be a human carcinogen based on evidence of carcinogenicity in experimental animals. (NCI05)


A dipolar aprotic solvent and reagent that may be used in the production of fibers and pharmaceuticals, and as a non-aldehyde fixative.


A synthetic analogue of the naturally occurring prostaglandin F2 alpha. Prostaglandin F2 alpha stimulates myometrial activity, relaxes the cervix, inhibits corpus luteal steroidogenesis, and induces luteolysis by direct action on the corpus luteum. (NCI04)


An ester prodrug of epinephrine, with sympathomimetic activity. Due to its lipophilicity, dipivefrin penetrates more easily to the anterior chamber of the eye and is hydrolyzed to epinephrine, when applied locally. Epinephrine, an adrenergic agonist, enhances the outflow of aqueous humor and decreases the production of aqueous humor by vasoconstriction. The overall result is a reduction in intraocular pressure.


A semi-synthetic macrolide antibiotic pro-drug. Dirithromycin is converted by hydrolysis during intestinal absorption into the microbiologically active erythromycylamine. Eryhtromylamine binds to the 50 S subunit of the 70 S ribosome of susceptible organisms, thereby inhibiting bacterial RNA-dependent protein synthesis. This antibiotic is used in the treatment of infections of the respiratory tract, skin and soft tissue caused by gram-positive microorganisms, including S. aureus, S. pneumonia and pyogenes, gram-negative microorganisms, including H. influenzae, L. pneumophila, M. catarrhalis, and M. pneumoniae.


The hyclate salt form of doxycycline, a synthetic, broad-spectrum tetracycline antibiotic exhibiting antimicrobial activity. Doxycycline hyclate binds reversibly to the 30S ribosomal subunit, possibly to the 50S ribosomal subunit as well, thereby blocking the binding of aminoacyl-tRNA to the mRNA-ribosome complex. This leads to an inhibition of protein synthesis. In addition, this agent has exhibited inhibition of collagenase activity.


A pyridine derivate histamine H1 antagonist with pronounced sedative properties. Doxylamine succinate competitively blocks the histamine H1 receptor and limits the typical allergic and anaphylactic responses, including bronchoconstriction, vasodilation, increased capillary permeability, and spasmodic contraction of gastrointestinal smooth muscle, caused by actions of histamine on bronchial and gastrointestinal smooth muscles, and on capillaries. This drug also prevents histamine-induced pain and itching of the skin and mucous membranes.


A synthetic anabolic steroid related to dihydrotestosterone that has antiestrogenic effects. Dromostanolone inhibits the growth of estrogen receptor-presenting breast cancers; its virilizing effects limit its clinical usefulness. (NCI04)


The propionate salt form of dromostanolone, a synthetic anabolic steroid related to dihydrotestosterone that has antiestrogenic effects. Dromostanolone inhibits the growth of estrogen receptor-presenting breast cancers; its virilizing effects limit its clinical usefulness. (NCI)


An unclassified compound with local anesthetic effect. Dyclonine reversibly binds to activated sodium channels on the neuronal membrane, thereby decreasing the neuronal membrane's permeability to sodium ions, leading to an increased threshold for excitation. This reversibly stabilizes the membrane and inhibits depolarization, leading to the failure of a propagated action potential and subsequent conduction blockade. This results in a transient and reversible loss of sensation in a localized area of the body.


A highly purified omega-3 fatty acid that can decrease serum triglyceride levels. Icosapent ethyl reduces serum triglycerides without an increase in LDL cholesterol, but increases the cholesterol and triglyceride content in skeletal muscle.


A fluoroquinolone antibacterial and antimycoplasma agent that is used in veterinary practice.


A phenolic antioxidant found in a number of plants such as green and black tea. It inhibits cellular oxidation and prevents free radical damage to cells. It is under study as a potential cancer chemopreventive agent. (NCI)


A homocysteine-derived thiol derivative with mucolytic and free radical scavenging properties. Erdosteine and its metabolites modulate mucus production and viscosity, by which facilitating mucociliary transport and improving expectoration. This agent also suppresses the chemical-induced cough reflex as well as protects lung tissues from damages caused by cigarette smoking mediated through free radicals scavenging.


The lactobionate salt form of erythromycin, a broad-spectrum, topical macrolide antibiotic with antibacterial activity. Erythromycin lactobionate diffuses through the bacterial cell membrane and reversibly binds to the 50S subunit of the bacterial ribosome. This prevents bacterial protein synthesis. Erythromycin lactobionate may be bacteriostatic or bactericidal in action, depending on the concentration of the drug at the site of infection and the susceptibility of the organism involved.


The stearate salt form of erythromycin, a broad-spectrum, topical macrolide antibiotic with antibacterial activity. Erythromycin stearate diffuses through the bacterial cell membrane and reversibly binds to the 50S subunit of the bacterial ribosome. This prevents bacterial protein synthesis. Erythromycin stearate may be bacteriostatic or bactericidal in action, depending on the concentration of the drug at the site of infection and the susceptibility of the organism involved.


The cypionate salt form of estradiol, the most potent, naturally produced estrogen. Estradiol cypionate 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.


The parenterally-administered synthetic valerate ester of estradiol, a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. As the primary, most potent estrogen hormone produced by the ovaries, estradiol binds to and activates specific nuclear receptors. This agent exhibits mild anabolic and metabolic properties, and increases blood coagulability. (NCI04)


A viscous, hygroscopic amino alcohol with an ammoniacal odor. It is widely distributed in biological tissue and is a component of lecithin. It is used as a surfactant, fluorimetric reagent, and to remove CO2 and H2S from natural gas and other gases.


A synthetic preparation of oleic acid and ethanolamine, a first generation monoethanolamine with sclerotherapeutic activity. Ethanolamine oleate causes an acute, dose-related inflammatory reaction of the intimal endothelium of the vein. This leads to scarring at the inner wall of the veins and possible occlusion of the veins. The oleic acid component may also transiently activate coagulation and fibrinolytic systems through the release of tissue factor and activation of Hageman factor.


An aromatic hydrocarbon composed of a benzene ring linked to an ethyl group. Ethylbenzene is a constituent of petroleum and coal tar and is used as either a petroleum additive or a chemical intermediate in the production of polystyrene. High level exposure to airborne ethylbenzene is associated with eye and throat irritation.


A non-steroidal anti-inflammatory agent and cyclooxygenase-2 (COX-2) inhibitor with potent analgesic and anti-arthritic properties. It has been shown to be effective in the treatment of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; ANKYLOSING SPONDYLITIS; and in the alleviation of postoperative pain (PAIN, POSTOPERATIVE).


An orally-available combination of clofibrate and niacin linked together by an ester bond. In the body clofibrate and niacin separate, acting as a controlled-release formulation.


A phosphate salt of a semisynthetic derivative of podophyllotoxin. Etoposide binds to the enzyme topoisomerase II, inducing double-strand DNA breaks, inhibiting DNA repair, and resulting in decreased DNA synthesis and tumor cell proliferation. Cells in the S and G2 phases of the cell cycle are most sensitive to this agent. (NCI04)


A fluorinated nucleotide antimetabolite analog of the antiviral agent vidarabine (ara-A) with antineoplastic activity. Administered parenterally as a phosphate salt, fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite may inhibit DNA polymerase alpha, ribonucleotide reductase and DNA primase, thereby interrupting DNA synthesis and inhibiting tumor cell growth. (NCI04)


A propanediol compound with anticonvulsant and antiepileptic properties. Although the exact mechanism of action is unknown, Felbamate may be an antagonist at the strychnine-insensitive glycine-recognition site of the N-methyl-D-aspartate (NMDA) receptor-ionophore complex, thereby blocking the effects of the excitatory amino acids, suppressing neuronal firing, and preventing seizure activity. Felbamate also has weak inhibitory effects on gamma-aminobutyric acid (GABA) receptor binding sites which may contribute to its inhibitory effect on neuronal excitatory.


A synthetic phosphoramidate ester compound and organophosphate acetylcholinesterase inhibitor and neurotoxicant that is used as a pesticide. It is characterized as a highly toxic colorless or brown waxy solid, and exposure occurs by inhalation, ingestion, or contact.


The active form of fenofibrate, a synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity.


A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.


A chelating agent with strong binding affinity for thallium, cesium, and other ions. Ferric hexacyanoferrate is used for the treatment of acute and chronic thallium and cesium poisoning. This agent is not absorbed in the gastrointestinal tract and it chelates thallium or cesium ion in the intestines. The resulting complex is eliminated via the feces.


A glucaric acid-iron conjugate that is used in the treatment of IRON-DEFICIENCY ANEMIA, including in patients with chronic kidney disease, when oral iron therapy is ineffective or impractical.


A superparamagnetic iron oxide nanoparticle coated with a low molecular weight semi-synthetic carbohydrate, polyglucose sorbitol carboxymethyl ether, with potential anti-anemic and imaging properties. After intravenous administration, ferumoxytol replaces iron stores with fewer side effects compared to the use of oral iron. In addition, this agent generates T1 relaxation, producing a magnetic field and enhancing T2 relaxation, thereby darkening contrast media-containing structures in magnetic resonance imaging (MRI). Due to small particle size, ferumoxytol remains in the intravasculature for a prolonged period and so may be used as a blood pool agent.


The fumarate salt form of the mineral iron. Administration of ferrous fumarate results in elevation of serum iron concentration, which is then assimilated into hemoglobin, required for the transport of oxygen, or trapped in the reticuloendothelial cells for storage. This agent is used as a dietary supplement, and to prevent or treat iron deficiency related syndromes.


A form of mineral iron for oral administration, Ferrous Gluconate is absorbed in the stomach and small intestine and combines with apoferritin to form ferritin, which is stored in the liver, spleen, red bone marrow, and intestinal mucosa. Important in transport of oxygen by hemoglobin to the tissues, iron is also found in myoglobin, transferrin, and ferritin, and is as a component of many enzymes such as catalase, peroxidase, and cytochromes. (NCI04)


A sulfate salt of mineral iron formulated for oral administration and used as a dietary supplement, ferrous sulfate is absorbed in the stomach and small intestine and combines with apoferritin to form ferritin, which is stored in the liver, spleen, red bone marrow, and intestinal mucosa. Important in transport of oxygen by hemoglobin to the tissues, iron is also found in myoglobin, transferrin, and ferritin, and is a component of many enzymes such as catalase, peroxidase, and cytochromes.


An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.


A third-generation cephalosporin antibiotic that is stable to hydrolysis by beta-lactamases.


A third-generation oral cephalosporin antibacterial agent that is used to treat bacterial infections of the respiratory tract and skin.


The phosphate salt of a fluorinated nucleotide antimetabolite analog of the antiviral agent vidarabine (ara-A) with antineoplastic activity. Fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite may inhibit DNA polymerase alpha, ribonucleotide reductase and DNA primase, thereby interrupting DNA synthesis and inhibiting tumor cell growth.


A synthetic corticosteroid with antiinflammatory and antiallergic properties. Flunisolide is a glucocorticoid receptor agonist that binds to cytoplasmic glucocorticoid receptors and subsequently translocates to the nucleus where it initiates the transcription of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both are potent mediators of inflammation.


A synthetic glucocorticoid with anti-inflammatory and antipruritic activities. Fluocinolone binds the glucocorticoid receptor, followed by translocation of the ligand-receptor complex to the nucleus and transcription activation of genes containing glucocorticoid-responsive elements. Lipocortin-1 is one factor induced by fluocinolone that interacts with and inhibits cytosolic phospholipase 2 alpha, thereby preventing phospholipase translocation to the perinuclear membrane and subsequent release and conversion of arachidonic acid to inflammatory prostaglandins. In addition, MAPK phosphatase 1 is induced, thereby preventing the triggering of the MAPK cascade resulting in pro-inflammatory effects via Jun N-terminal kinase and c-Jun. Finally, fluocinolone binds to and inhibits nuclear factor kappa-B directly, resulting in inhibition of cyclooxygenase 2 transcription and subsequent prostaglandin synthesis.


A phthalic indicator dye that appears yellow-green in normal tear film and bright green in a more alkaline medium such as the aqueous humor.


The decanoate salt form of fluphenazine, a phenothiazine with antipsychotic activity. Fluphenazine decanoate exerts its actions by blocking postsynaptic dopamine D2 receptors in the limbic, cortical system and basal ganglia. This prevents the actions of dopamine, thereby reducing the hallucinations and delusions that are associated with schizophrenia.


A long-acting beta-adrenergic receptor agonist with bronchodilator activity. Formoterol 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 reduce mediator substance release from inflammatory cells, especially from mast cells.


The diphosphate ester of a synthetic, nonsteroidal form of estrogen. A well-known teratogen and carcinogen, diethylstilbestrol inhibits the hypothalamic-pituitary-gonadal axis, thereby blocking the testicular synthesis of testosterone, lowering plasma testosterone, and inducing a chemical castration.


A pharmacologic form of follicle-stimulating hormone used in the treatment of infertility.


A cyclohexane-gamma-aminobutyric acid derivative that is used for the treatment of PARTIAL SEIZURES; NEURALGIA; and RESTLESS LEGS SYNDROME.


A gadolinium complex of diethylenetriamine pentaacetic acid with ionic paramagnetic properties. Gadopentetate dimeglumine may provide contrast enhancement during magnetic resonance imaging (MRI) of intracranial lesions with abnormal vascularity or of abnormalities in the blood-brain barrier (BBB). (NCI04)


A hydrated nitrate salt of the group IIIa element gallium with potential use in the treatment of malignancy-associated hypercalcemia. Gallium nitrate localizes preferentially to areas of bone resorption and remodeling and inhibits osteoclast-mediated resorption by enhancing hydroxyapatite crystallization and reduction of bone mineral solubility. This agent also increases calcium and phosphorous deposition into bone and may increase collagen synthesis. (NCI04)


An omega-6 fatty acid produced in the body as the delta 6-desaturase metabolite of linoleic acid. It is converted to dihomo-gamma-linolenic acid, a biosynthetic precursor of monoenoic prostaglandins such as PGE1. (From Merck Index, 11th ed)


An isoflavonoid derived from soy products. It inhibits PROTEIN-TYROSINE KINASE and topoisomerase-II (DNA TOPOISOMERASES, TYPE II); activity and is used as an antineoplastic and antitumor agent. Experimentally, it has been shown to induce G2 PHASE arrest in human and murine cell lines and inhibits PROTEIN-TYROSINE KINASE.


A long-acting, third-generation sulfonylurea with hypoglycemic activity. Compared to other generations of sulfonylurea compounds, glimepiride is very potent and has a longer duration of action. This agent is metabolized by CYP2C9 and shows peroxisome proliferator-activated receptor gamma (PPARgamma) agonistic activity.


A potent, second-generation sulfonylurea with antihyperglycemic activity. Like other second-generation compounds, gliquidone exerts greater binding affinity to SUR1 and increased potency compared to first-generation compounds. In addition, this agent exerts peroxisome proliferator-activated receptor (PPAR) gamma agonistic activity.


A naturally occurring polyhydroxy acid (PHA) with metal chelating, moisturizing and antioxidant activity. Gluconolactone can be produced by enzymatic oxidation of D-glucose oxidation. Its ability in free radicals scavenging accounts for its antioxidant property. It is used in cosmetic product and as a coagulant in tofu processing. (NCI05)


An ester of glucose with phosphoric acid, made in the course of glucose metabolism by mammalian and other cells. It is a normal constituent of resting muscle and probably is in constant equilibrium with fructose-6-phosphate. (Stedman, 26th ed)


A carboxylic acid with structural similarity to glucose with detoxifying activity. The xenobiotic metabolism of various substances such as drugs, pollutants, bilirubin, androgens, estrogens, mineralocorticoids, glucocorticoids, fatty acid derivatives, retinoids, and bile acids involves glucuronidation, a process in which water-soluble, excretable glucuronides of these substances are formed via glycosidic linkages to glucuronic acid. UDP-glucuronic acid, formed in the liver through the linkage of glucuronic acid to uridine diphosphate (UDP) via a glycosidic bond, is an intermediate in the process of glucuronidation.


A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.


A GLUTATHIONE dimer formed by a disulfide bond between the cysteine sulfhydryl side chains during the course of being oxidized.


A widely used anti-inflammatory agent isolated from the licorice root. It is metabolized to GLYCYRRHETINIC ACID, which inhibits 11-BETA-HYDROXYSTEROID DEHYDROGENASES and other enzymes involved in the metabolism of CORTICOSTEROIDS. Therefore, glycyrrhizic acid, which is the main and sweet component of licorice, has been investigated for its ability to cause hypermineralocorticoidism with sodium retention and potassium loss, edema, increased blood pressure, as well as depression of the renin-angiotensin-aldosterone system.


A synthetic organophosphate compound that blocks the activity of enolpyruvylshikimate-3-phosphate (EPSP) synthase and is used as a broad-spectrum pesticide. It is characterized as a volatile, moderately toxic, colorless, odorless crystalline solid or powder, and exposure occurs by inhalation, ingestion, or contact.


A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.


A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.


A synthetic benzodiazepine derivative with anxiolytic property. Halazepam potentiates the inhibitory activities of gamma-aminobutyric acid (GABA) by binding to the benzodiazepine-GABA-A-chloride ionophore receptor complex located in the limbic, thalamic, and hypothalamic regions of the central nervous system (CNS). This increases the frequency of chloride channel opening, allowing the flow of chloride ions into the neuron and ultimately leading to membrane hyperpolarization and a decrease in neuronal excitability.


The decanoate ester of haloperidol, a phenylbutylpiperadine derivative with antipsychotic, neuroleptic and antiemetic effects. Haloperidol competitively blocks postsynaptic dopamine (D2) receptors in the mesolimbic system of the brain leading to anti-delusionary and anti-hallucinogenic effects. The antagonistic activity mediated through D2 dopamine receptors in the chemoreceptive trigger zone (CTZ) account for its antiemetic activity.


An antifungal agent used as a topical cream. It was discontinued in favor of newer antifungals with fewer side effects.


A non-infectious mixture containing recombinant hepatitis B surface antigen (HBsAg) in a liquid vehicle. Immunization with the hepatitis B vaccine induces the formation of specific anti-hepatitis B antibodies and an active immunity against hepatitis B infection.


A semi-synthetic penicillin compound with bactericidal properties. Hetacillin is a prodrug that is converted to ampicillin via esterases. Ampicillin binds to inactivated penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs, including transpeptidases, carboxypeptidases, and endopeptidases, participate in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. This results in the weakening of the bacterial cell wall and eventually causes cell lysis. (NCI05)


An acyl glycine produced by the conjugation of benzoic acid and glycine, found as a normal component in urine as a metabolite of aromatic compounds from food. Increased urine hippuric acid content may have antibacterial effects.


A synthetic tertiary amine alkaloid with antimuscarinic properties. Homatropine, a competitive inhibitor of acetylcholine at the muscarinic receptor, blocks parasympathetic nerve stimulation.


The methylbromide salt of homatropine, a synthetic tertiary amine alkaloid with antimuscarinic properties. Homatropine methylbromide, a competitive inhibitor of acetylcholine at the muscarinic receptor, blocks parasympathetic nerve stimulation, thereby inhibiting pepsin and gastrin secretion. When administered in high doses, this drug produces inhibitory effects on acetylcholine activity, specifically on smooth muscle located in the gastrointestinal, biliary, and genitourinary tracts, resulting in an anti-spasmodic effect.


A semisynthetic formulation of the cytotoxic plant alkaloid homoharringtonine isolated from the evergreen tree Cephalotaxus with potential antineoplastic activity. Omacetaxine binds to the 80S ribosome in eukaryotic cells and inhibits protein synthesis by interfering with chain elongation. This agent also induces differentiation and apoptosis in some cancer cell types.


A semisynthetic, broad-spectrum, fourth-generation cephalosporin with antibacterial activity. Cefpirome 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.


An isoxazole derivative that inhibits dihydroorotate dehydrogenase, the fourth enzyme in the pyrimidine biosynthetic pathway. It is used an immunosuppressive agent in the treatment of RHEUMATOID ARTHRITIS and PSORIATIC ARTHRITIS.


Hydrobromic acid (HBr). A solution of hydrogen bromide gas in water.


The probutate salt form of hydrocortisone, a synthetic glucocorticoid receptor agonist with antiinflammatory, antipruritic and vasoconstrictive effects. Binding and activation of the glucocorticoid receptor results in the activation of lipocortin that in turn inhibits cytosolic phospholipase A2. Lack of phospholipase A2 prevents the release of arachidonic acid, precursor for inflammatory mediator prostaglandins and leukotrienes, from the cell membrane. 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.


The synthetic acetate ester form of hydrocortisone, a corticosteroid with anti-inflammatory and immunosuppressive properties. Hydrocortisone acetate initially binds to the cytoplasmic glucocorticoid receptor; then the receptor-ligand complex is translocated to the nucleus where it initiates the transcription of genes encoding for anti-inflammatory mediators, such as 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.


The valerate salt form of hydrocortisone, a synthetic glucocorticoid receptor agonist with antiinflammatory, antipruritic and vasoconstrictive effects. Binding and activation of the glucocorticoid receptor results in the activation of lipocortin that in turn inhibits cytosolic phospholipase A2. Lack of phospholipase A2 prevents the release of arachidonic acid, precursor for inflammatory mediator prostaglandins and leukotrienes, from the cell membrane. 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 hydroxyester compound and a resin monomer used in desensitizing dentin. By applying 2-hydroxyethyl methacrylate locally to sensitive teeth, sensitive areas in the teeth get sealed and block the dentinal tubules at the dentin surface from stimuli that cause pain. This prevents excitation of the tooth nerve and relieves pain caused by tooth hypersensitivity.


An anthraquinone derivative that is naturally found in the yellow flower of Hypericum perforatum (St. John's wort) with antidepressant, potential antiviral, antineoplastic and immunostimulating activities. Hypericin appears to inhibit the neuronal uptake of serotonin, norepinephrine, dopamine, gamma-amino butyric acid (GABA) and L-glutamate, which may contribute to its antidepressant effect. Hypericin may also prevent the replication of encapsulated viruses probably due to inhibition of the assembly and shedding of virus particles in infected cells. This agent also exerts potent phototoxic effects by triggering apoptotic signaling that results in formation of reactive oxygen species.


A semisynthetic, inert, viscoelastic polymer. It is used as an ophthalmic lubricant and as an excipient in oral medications.


A fluorinated ether with general anesthetic and muscle relaxant activities. Although the exact mechanism of action has not been established, desflurane, administered by inhalation, appears to act on the lipid matrix of the neuronal membrane, resulting in disruption of neuronal transmission in the brain. This agent may also enhance the synaptic activity of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA).


An indole derivative and 5-HT3 RECEPTOR antagonist that is used for the prevention of nausea and vomiting.


An orally bioavailable, N-methyl-D-aspartate (NMDA) receptor antagonist, with potential central nervous system (CNS) stimulating, neuroprotective, anti-inflammatory and anti-fibrotic activities. Upon administration, ifenprodil targets, binds to and inhibits glutamanergic NMDA receptors (NMDARs), specifically the glycine-binding NMDA receptor subunit 1 (GluN1) and 2 (glutamate-binding NMDA receptor subunit 2; NMDA-type subunit 2B; GluN2B), thereby preventing NMDAR signaling. This inhibits neuronal excitotoxicity, and thereby potentially enhancing cognitive function. Additionally, ifenprodil inhibits G protein-coupled inwardly-rectifying potassium (GIRK) channels, and interacts with alpha1 adrenergic, serotonin, and activates sigma receptors. Ifenprodil exerts its anti-inflammatory effect through its effect on NMDA and possibly sigma-1 receptors. Although the exact mechanism has not fully been elucidated, this agent reduces the infiltration of neutrophils and T-cells into the lungs and prevents the release of pro-inflammatory cytokines. This may result in the reduction of the lung inflammatory response, inhibit fibrosis in the lungs and may reduce the severity of cough. NMDA receptors are multimeric ionotropic glutamate receptors composed of four subunits and are expressed on various cells and organs, such as in the brain, lungs, and on T-cells and neutrophils.


A naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, a natural compound present in a wide variety of plant food substances including members of the family Cruciferae with antioxidant and potential chemopreventive properties. Indole-3-carbinol scavenges free radicals and induces various hepatic cytochrome P450 monooxygenases. Specifically, this agent induces the hepatic monooxygenase cytochrome P4501A1 (CYP1A1), resulting in increased 2-hydroxylation of estrogens and increased production of the chemoprotective estrogen 2-hydroxyestrone.


A niacin formulation that contains no free niacin, but can be hydrolyzed to release free niacin in vivo. Use of inositol niacinate is associated with less flushing than that seen with the use of free niacin.


maize invert sugar
saccharide hydrolysate


A dimeric iso-osmolar, non-ionic, hydrophilic iodinated radiocontrast agent used in diagnostic imaging. Upon intravascular administration and during computed tomography (CT) imaging, iodixanol blocks x-rays and appears opaque on x-ray images. This allows body structures that absorb iodine to be visualized. The degree of opacity produced by iodixanol is directly proportional to the total amount of the iodinated contrast agent in the path of the x-rays. The visualization of body structures is dependent upon the distribution and elimination of iodixanol. Compared to other iodinated contrast agents, iodixanol appears to exhibit less nephrotoxicity.


A sterile, nonpyrogenic, aqueous solution intended for intravascular administration as a diagnostic radiocontrast agent. Ioversol is available in various concentrations, ranging from 240 to 350 milligrams of iodine per milliliter.


A synthetic visual lymphatic imaging agent. Injected into the periphery of the tumor site, isosulfan blue localizes to the lymphatic system and aids in the surgical identification of tumor sentinel nodes which stain blue. (NCI04)


An unsaturated pentahydrocarbon, Isoprene is found in certain plants or obtained by distillation of caoutchouc or gutta-percha. In plants, it is elementary in the formation of isoprenoids, fat-soluble vitamins, carotenoids and related pigments. Isoprenes contribute to flavors and fragrances of essential oils and other plant-derived substances. (NCI04)


The mononitrate salt form of isosorbide, an organic nitrate with vasodilator activity. Isosorbide mononitrate relaxes vascular smooth muscle by formation of the free radical nitric oxide (NO), which is identical to the endothelium-derived relaxing factor (EDRF). NO activates guanylyl cyclase, thereby increasing the synthesis of cGMP within smooth muscle, resulting in dephosphorylation of light chain myosin and relaxation of peripheral arteries and veins. In addition, isosorbide mononitrate relaxes coronary arteries, thereby increasing the blood circulation through the ischemic area. (NCI05)


A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.


The oil extracted from the seeds of Simmondsia chinensis. Jojoba oil is used primarily in cosmetics.


A second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell/basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.


A fibroblast growth factor that is a specific mitogen for EPITHELIAL CELLS. It binds a complex of HEPARAN SULFATE and FIBROBLAST GROWTH FACTOR RECEPTOR 2B.


The tromethamine salt of ketorolac, a synthetic pyrrolizine carboxylic acid derivative with anti-inflammatory, analgesic and antipyretic properties. Ketorolac tromethamine, a non-selective inhibitor of the cyclooxygenases (COX), inhibits both COX-1 and COX-2 enzymes. This agent exerts its anti-inflammatory effect by preventing conversion of arachidonic acid to prostaglandins at inflammation site mediated through inhibition of COX-2, which is undetectable in most tissues but is up-regulated at the inflammation sites. Since COX-1 is expressed virtually in all tissues, inhibition of COX-1 enzyme by this agent prevents normal state production of prostaglandins, which plays housekeeping roles in the protection of the gastrointestinal tract, regulating renal blood flow, and functioning in platelet aggregation. As a result, inhibition of COX-1 is usually associated with adverse effects such as gastrointestinal toxicity and nephrotoxicity.


A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed)


A phenyltriazine compound, sodium and calcium channel blocker that is used for the treatment of SEIZURES and BIPOLAR DISORDER.


A percutaneous enhancer. Upon application to the skin, laurocapram interacts with lipids in the stratum corneum and may enhance the ability of the skin to absorb a hydrophilic chemical.


The essential oil extracted from the flowers of several species of Lavandula. Lavender oil is used primarily for its aromatic properties in parfumery, aromatherapy, skincare products, and other consumer products.


The essential oil of Cymbopogon citratus. Lemongrass oils have been used as a pesticide or preservative and may have antifungal properties.


A synthetic piperidine derivative with antihistamine properties. Levocabastine is a second generation histamine-1 receptor antagonist. When applied locally into the eye as a topical solution, this agent reduces itching, rhinorrhea and symptoms of allergic rhinitis or conjunctivitis.


A potent synthetic agonist of GONADOTROPIN-RELEASING HORMONE with 3-(2-naphthyl)-D-alanine substitution at residue 6. Nafarelin has been used in the treatments of central PRECOCIOUS PUBERTY and ENDOMETRIOSIS.


salmon gonadotropin releasing hormone D-Arg6 analog ethyl amide


A naturally-occurring class of MONOTERPENES which occur as a clear colorless liquid at room temperature. Limonene is the major component in the oil of oranges which has many uses, including as flavor and fragrance. It is recognized as safe in food by the Food and Drug Administration (FDA).