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Acetohexamide
Description: A sulfonylurea hypoglycemic agent that is metabolized in the liver to 1-hydrohexamide. (PubChem) Pharmacology: Acetohexamide is an intermediate-acting, first-generation oral sulfonylurea. It lowers blood sugar by stimulating the pancreatic beta cells to secrete insulin and by helping the body use insulin efficiently. The pancreas must produce insulin for this medication to work. Acetohexamide has one-third the potency of chlorpropamide, and twice the potency of tolbutamide; however, similar hypoglycemic efficacy occurs with equipotent dosage of sulfonylureas. Mechanism of action: Sulfonylureas such as acetohexamide bind to an ATP-dependent K+ channel on the cell membrane of pancreatic beta cells. This inhibits a tonic, hyperpolarizing outflux of potassium, which causes the electric potential over the membrane to become more positive. This depolarization opens voltage-gated Ca2+ channels. The rise in intracellular calcium leads to increased fusion of insulin granulae with the cell membrane, and therefore increased secretion of (pro)insulin. Drug type: Approved. Small Molecule. Drug category: Hypoglycemic Agents. Sulfonylureas
Preferred ID: CHEBI:28052 Type: term ID# ILX:0100236 Score: 0
Adalimumab
Description: Anti-TNF antibody, expressed in mammalian cell culture, 1330 residues, MW
Preferred ID: ILX:0100305 Type: term ID# ILX:0100305 Score: 0
Amantadine
Description: An antiviral that is used in the prophylactic or symptomatic treatment of influenza A. It is also used as an antiparkinsonian agent, to treat extrapyramidal reactions, and for postherpetic neuralgia. The mechanisms of its effects in movement disorders are not well understood but probably reflect an increase in synthesis and release of dopamine, with perhaps some inhibition of dopamine uptake. (PubChem) Pharmacology: Amantadine is an antiviral drug which also acts as an antiparkinson agent, for which it is usually combined with L-DOPA when L-DOPA responses decline (probably due to tolerance). It is a derivate of adamantane, like a similar drug rimantadine. The mechanism of action of amantadine in the treatment of Parkinson's disease and drug-induced extrapyramidal reactions is not known. It has been shown to cause an increase in dopamine release in the animal brain, and does not possess anticholinergic activity. Mechanism of action: The mechanism of its antiparkinsonic effect is not fully understood, but it appears to be releasing dopamine from the nerve endings of the brain cells, together with stimulation of norepinephrine response. The antiviral mechanism seems to be unrelated. The drug interferes with a viral protein, M2 (an ion channel), which is needed for the viral particle to become "uncoated" once it is taken inside the cell by endocytosis. Drug type: Approved. Small Molecule. Drug category: Analgesics, Non-Narcotic. Antiparkinson Agents. Antiviral Agents. Dopamine Agents
Preferred ID: CHEBI:2618 Type: term ID# ILX:0100526 Score: 0
Ambenonium
Description: Ambenonium is a cholinesterase inhibitor used in the management of myasthenia gravis. (Wikipedia) Pharmacology: Ambenonium, similar to pyridostigmine and neostigmine, is used for the treatment of muscle weakness and fatigue in people with myasthenia gravis. It is postulated to exert its therapeutic effect by enhancing cholinergic function by inhibiting the hydrolysis of acetylcholine by acetylcholinesterase. Increased levels of acetylcholine has peripheral effects, as acetylcholine is also used in the brain, where it tends to cause excitatory actions. The glands that receive impulses from the parasympathetic part of the autonomic nervous system are also stimulated in the same way. This is why an increase in acetylcholine causes a decreased heart rate and increased production of saliva. Ambenonium is used less commonly than neostigmine or pyridostigmine but may be preferred in patients hypersensitive to the bromide ion. Ambenonium produces fewer muscarinic side effects than neostigmine, but more than pyridostigmine. Mechanism of action: Ambenonium exerts its actions against myasthenia gravis by competitive, reversible inhibition of acetylcholinesterase. The disease myasthenia gravis occurs when the body inappropriately produces antibodies against acetylcholine receptors, and thus inhibits proper acetylcholine signal transmission (when acetylcholine binds to acetylcholine receptors of striated muscle fibers, it stimulates those fibers to contract). Ambenonium reversibly binds acetylcholinesterase, and as acetylcholinesterase is responsible for the hydrolysis of acetylcholine, this inhibition increases levels of acetylcholine. In turn this facilitates transmission of impulses across the myoneural junction and effectively treats the disease. Drug type: Approved. Small Molecule. Drug category: Antiarrhythmic Agents. Antimyasthenics
Preferred ID: ILX:0100527 Type: term ID# ILX:0100527 Score: 0
Amlexanox
Description: Amlexanox is an antiallergic drug, clinically effective for atopic diseases, especially allergic asthma and rhinitis. Amlexanox as a topical paste is a well tolerated treatment of recurrent aphthous ulcers. Recurrent aphthous ulcer (RAU) is the most prevalent oral mucosal disease in humans, estimated to affect between 5% and 50% of the general population. Pharmacology: Amlexanox is a mucoadhesive oral paste which has been clinically proven to abort the onset, accelerate healing and resolve the pain of aphthous ulcers (canker sores). It decreases the time ulcers take to heal. Because amlexanox decreases the healing time, it also decreases the pain you feel. Recent studies have also shown that the majority of ulcers can be prevented by application of the paste during the prodromal (pre-ulcerative) phase of the disease. Recurrent Aphthous Ulcers (RAU) also known as Recurrent Aphthous Stomatitis (RAS) is recognized as the most common oral mucosal disease known to man. Estimates suggest that 20% - 25% of the general population suffer at least one incidence of aphthous ulcers each year. Mechanism of action: As a benzopyrano-bipyridine carboxylic acid derivative, amlexanox has anti-inflammatory and antiallergic properties. It inhibits chemical mediatory release of the slow-reacting substance of anaphylaxis (SRS-A) and may have antagonistic effects on interleukin-3. Drug type: Approved. Investigational. Small Molecule. Drug category: Anti-Allergic Agents. Anti-inflammatory, Locally Applied. Antiulcer agent (topical)
Preferred ID: ILX:0100548 Type: term ID# ILX:0100548 Score: 0
Amlodipine
Description: A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of angina pectoris and hypertension. (PubChem) Pharmacology: Amlodipine, a calcium-channel blocker, is used alone or with benazepril, an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Amlodipine is similar to the peripheral vasodilator nifedipine and other members of the dihydropyridine class. Mechanism of action: Amlodipine is a calcium channel blocking agent. It inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload. Another possible mechanism is that amlodipine inhibits vascular smooth muscle carbonic anhydrase I activity with consecutive pH increase which may be involved in intracelluar calcium influx through calcium channels. Drug type: Approved. Small Molecule. Drug category: Antianginals. Antihypertensive Agents. Calcium Channel Blockers. Vasodilator Agents
Preferred ID: ILX:0100549 Type: term ID# ILX:0100549 Score: 0
Alteplase
Description: Human tissue plasminogen activator, purified, glycosylated, 527 residues purified from CHO cells Pharmacology: Activase binds to fibrin in a thrombus and converts the entrapped plasminogen to plasmin. It also produces limited conversion of plasminogen in the absence of fibrin. Mechanism of action: Cleaves the Arg-Val bond in plasminogen to produce active plasmin. Drug type: Approved. Biotech. Drug category: Thrombolytic Agents
Preferred ID: ILX:0100514 Type: term ID# ILX:0100514 Score: 0
Antihemophilic Factor
Description: Human recombinant antihemophilic factor (AHF) or Factor VIII, 2332 residues, glycosylated, produced by CHO cells Pharmacology: Antihemophilic Factor binds factor IXa along with calcium and phospholipid, This complex converts factor X to factor Xa to facilitate clotting cascade. Mechanism of action: Antihemophilic factor (AHF) is a protein found in normal plasma which is necessary for clot formation. The administration of AHF provides an increase in plasma levels of AHF and can temporarily correct the coagulation defect of patients with hemophilia A (classical hemophilia). Drug type: Approved. Biotech. Investigational. Drug category: Coagulants. Thrombotic Agents
Preferred ID: ILX:0100793 Type: term ID# ILX:0100793 Score: 0
Aroclor 1242
Description: Organic Compound;Coolant;Plasticizer;Polychlorinated Biphenyl;Aromatic Hydrocarbon;Organochloride; Aroclor 1242 is a commercial mixture of PCBs with an average chlorine content of 41.5%. It is composed of mono- to hexachlorinated homologs.
Preferred ID: ILX:0100903 Type: term ID# ILX:0100903 Score: 0
Brompheniramine
Description: Histamine H1 antagonist used in treatment of allergies, rhinitis, and urticaria. (PubChem) Pharmacology: Brompheniramine is an antihistaminergic medication of the propylamine class. It is a first-generation antihistamine. In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Brompheniramine is a histamine H1 antagonist (or more correctly, an inverse histamine agonist) of the alkylamine class. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies. Mechanism of action: Brompheniramine works by acting as an antagonist of the H1 histamine receptors. It also functions as a moderately effective anticholingeric agent, likely an antimuscarinic agent similar to other common antihistamines such as diphenhydramine. Its effects on the cholinergic system may include side-effects such as drowsiness, sedation, dry mouth, dry throat, blurred vision, and increased heart rate. Drug type: Approved. Small Molecule. Drug category: Anti-Allergic Agents. Histamine H1 Antagonists
Preferred ID: ILX:0101476 Type: term ID# ILX:0101476 Score: 0
Cisatracurium Besylate
Description: Cisatracurium Besylate is a nondepolarizing skeletal muscle relaxant for intravenous administration. Cisatracurium Besylate acts on cholinergic receptors, blocking neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors such as neostigmine. The neuromuscular block produced by cisatracurium besylate is readily antagonized by anticholinesterase agents once recovery has started. As with other nondepolarizing neuromuscular blocking agents, the more profound the neuromuscular block at the time of reversal, the longer the time required for recovery of neuromuscular function. Compared to other neuromuscular blocking agents, it is intermediate in its onset and duration of action. Pharmacology: Cisatracurium Besylate is a nondepolarizing skeletal muscle relaxant for intravenous administration. Cisatracurium Besylate acts on cholinergic receptors, blocking neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors such as neostigmine. The neuromuscular block produced by cisatracurium besylate is readily antagonized by anticholinesterase agents once recovery has started. As with other nondepolarizing neuromuscular blocking agents, the more profound the neuromuscular block at the time of reversal, the longer the time required for recovery of neuromuscular function. Compared to other neuromuscular blocking agents, it is intermediate in its onset and duration of action. Mechanism of action: Cisatracurium Besylate binds to the nicotinic acetycholine (cholinergic) receptors in the motor endplate and blocks access to the receptors. In the process of binding, the receptor is actually activated - causing a process known as depolarization. Since it is not degraded in the neuromuscular junction, the depolarized membrane remains depolarized and unresponsive to any other impulse, causing muscle paralysis. Drug type: Approved. Small Molecule. Drug category: Neuromuscular Blocking Agents
Preferred ID: ILX:0102199 Type: term ID# ILX:0102199 Score: 0
Clarithromycin
Description: 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. (PubChem) Pharmacology: Clarithromycin, a macrolide antibiotic similar to erythromycin and azithromycin, is effective against Mycobacterium avium complex (MAC) and is used for the treatment of Helicobacter pylori-associated peptic ulcer disease, community-acquired pneumonia, sinusitis, and chronic bronchitis. Clarithromycin is also used to treat respiratory tract, sexually transmitted, otitis media, and AIDS-related infections. Mechanism of action: Clarithromycin is first metabolized to 14-OH clarithromycin. Like other macrolides, it then binds to the 50 S subunit of the 70 S ribosome of the bacteria, blocking RNA-mediated bacterial protein synthesis. Clarithromycin also inhibits the hepatic microsomal CYP3A4 isoenzyme and P-glycoprotein, an energy-dependent drug efflux pump. Drug type: Approved. Small Molecule. Drug category: Anti-Bacterial Agents. Macrolides. Other Macrolides. Protein Synthesis Inhibitors
Preferred ID: ILX:0102209 Type: term ID# ILX:0102209 Score: 0
Cyproheptadine
Description: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc. (PubChem) Pharmacology: Cyproheptadine is a piperidine antihistamine. Unlike other antihistamines, this drug also antagonizes serotonin receptors. This action makes Cyproheptadine useful in conditions such as vascular headache and anorexia. Cyproheptadine does not prevent the release of histamine but rather competes with free histamine for binding at HA-receptor sites. Cyproheptadine competitively antagonizes the effects of histamine on HA-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. Most antihistamines possess significant anticholinergic properties, but Cyproheptadine exerts only weak anticholinergic actions. Blockade of central muscarinic receptors appears to account for Cyproheptadine's antiemetic effects, although the exact mechanism is unknown. Cyproheptadine also competes with serotonin at receptor sites in smooth muscle in the intestines and other locations. Antagonism of serotonin on the appetite center of the hypothalamus may account for Cyproheptadine's ability to stimulate appetite. Cyproheptadine also has been used to counter vascular headaches, which many believe are caused by changes in serotonin activity, however it is unclear how Cyproheptadine exerts a beneficial effect on this condition. Mechanism of action: Cyproheptadine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Drug type: Approved. Small Molecule. Drug category: Anti-Allergic Agents. Antihistamine derivatives. Antipruritics. Gastrointestinal Agents. Histamine H1 Antagonists. Serotonin Antagonists
Preferred ID: ILX:0102748 Type: term ID# ILX:0102748 Score: 0
Cysteamine
Description: A radiation-protective agent that oxidizes in air to form cystamine. It can be given intravenously or orally to treat radiation sickness. The bitartrate has been used for the oral treatment of nephropathic cystinosis. (PubChem) Pharmacology: People born without the ability to metabolize the amino acid cystine suffer from cystinosis, a rare inherited disorder characterized by the deposition and accumulation of cystine crystals throughout the body. These crystals cause considerable damage, particularly in the kidney. Kidney failure can occur by the age of 10 in untreated patients. Cysteamine prevents the accumulation of cystine crystals and is prescribed to prevent further kidney damage. Cysteamine helps to convert cystine into less harmful chemical forms that can be removed from cells. Mechanism of action: The free thiol cysteamine depletes cystinotic leukocytes and other cells of cystine, whose accumulation is considered the cause of organ damage in cystinosis. Drug type: Approved. Investigational. Small Molecule. Drug category: Nephropathic cystinosis therapy. Radiation-Protective Agents
Preferred ID: CHEBI:17141 Type: term ID# ILX:0102753 Score: 0
Desloratadine
Description: Desloratadine is a tricyclic antihistamine, which has a selective and peripheral H1-antagonist action. It is used to treat allergies. It has a long-lasting effect and does not cause drowsiness because it does not readily enter the central nervous system. Pharmacology: Desloratadine is a long-lasting antihistamine. Desloratadine is a second-generation H1-receptor antagonist which has a selective and peripheral H1-antagonist action. Histamine is a chemical that causes many of the signs that are part of allergic reactions, for example, swelling of tissues. Histamine is released from histamine-storing cells (mast cells) and attaches to other cells that have receptors for histamine. The attachment of the histamine to the receptors causes the cell to be "activated," releasing other chemicals which produce the effects that we associate with allergy. Desloratadine blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine. Unlike most other antihistamines, Desloratadine does not enter the brain from the blood and, therefore, does not cause drowsiness. Mechanism of action: Like other H1-blockers, Desloratadine competes with free histamine for binding at H1-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Drug type: Approved. Investigational. Small Molecule. Drug category: Antihistamines. Cholinergic Antagonists. Histamine H1 Antagonists, Non-Sedating
Preferred ID: ILX:0103123 Type: term ID# ILX:0103123 Score: 0
Diethylpropion
Description: A appetite depressant considered to produce less central nervous system disturbance than most drugs in this therapeutic category. It is also considered to be among the safest for patients with hypertension. (From AMA Drug Evaluations Annual, 1994, p2290) Pharmacology: Diethylpropion is a sympathomimetic stimulant drug marketed as an appetite suppressant. Chemically, it is the N,N-diethyl analog of cathinone. Its mechanism of action is similar to other appetite suppressants such as sibutramine, phentermine and dextroamphetamine. Mechanism of action: Diethylpropion is an amphetamine that stimulates neurons to release or maintain high levels of a particular group of neurotransmitters known as catecholamines; these include dopamine and norepinephrine. High levels of these catecholamines tend to suppress hunger signals and appetite. Diethylpropion (through catecholamine elevation) may also indirectly affect leptin levels in the brain. It is theorized that diethylpropion can raise levels of leptin which signal satiety. It is also theorized that increased levels of the catecholamines are partially responsible for halting another chemical messenger known as neuropeptide Y. This peptide initiates eating, decreases energy expenditure, and increases fat storage. Drug type: Approved. Illicit. Small Molecule. Drug category: Anorexigenic Agents. Appetite Depressants. Stimulants
Preferred ID: ILX:0103222 Type: term ID# ILX:0103222 Score: 0
Diethylstilbestrol
Description: A synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders. It was also used formerly as a growth promoter in animals. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), diethylstilbestrol has been listed as a known carcinogen. (Merck, 11th ed) Pharmacology: Diethylstilbestrol is a synthetic estrogen that was developed to supplement a woman's natural estrogen production. In 1971, the Food and Drug Administration (FDA) issued a Drug Bulletin advising physicians to stop prescribing DES to pregnant women because it was linked to a rare vaginal cancer in female offspring. Mechanism of action: Estrogens diffuse into their target cells and interact with a protein receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. The combination of an estrogen with a progestin suppresses the hypothalamic-pituitary system, decreasing the secretion of gonadotropin-releasing hormone (GnRH). Drug type: Approved. Small Molecule. Drug category: Antineoplastic Agents, Hormonal. Carcinogens. Estrogens, Non-Steroidal
Preferred ID: CHEBI:41922 Type: term ID# ILX:0103223 Score: 0
Diatrizoate
Description: A commonly used x-ray contrast medium. As diatrizoate meglumine and as Diatrizoate sodium, it is used for gastrointestinal studies, angiography, and urography. (PubChem) Pharmacology: Diatrizoate is the most commonly used water-soluble, iodinated, radiopaque x-ray contrast medium. Radiopaque agents are drugs used to help diagnose certain medical problems. They contain iodine, which blocks x-rays. Depending on how the radiopaque agent is given, it localizes or builds up in certain areas of the body. The resulting high level of iodine allows the x-rays to make a "picture" of the area. The areas of the body in which the radiopaque agent localizes will appear white on the x-ray film. This creates the needed distinction, or contrast, between one organ and other tissues. The contrast will help the doctor see any special conditions that may exist in that organ or part of the body. Mechanism of action: Diatrizoate is an iodine-containing X-ray contrast agent. Iodated contrast agents were among the first contrast agents developed. Iodine is known to be particular electron-dense and to effectively scatter or stop X-rays. A good contrast agent requires a high density of electron-dense atoms. Therefore, the more iodine, the more "dense" the x-ray effect. Iodine based contrast media are water soluble and harmless to the body. These contrast agents are sold as clear colorless water solutions, the concentration is usually expressed as mg I/ml. Modern iodinated contrast agents can be used almost anywhere in the body. Most often they are used intravenously, but for various purposes they can also be used intraarterially, intrathecally (the spine) and intraabdominally - just about any body cavity or potential space. Drug type: Approved. Small Molecule. Drug category: Contrast Media
Preferred ID: ILX:0103198 Type: term ID# ILX:0103198 Score: 0
Dienestrol
Description: Dienestrol is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist. Estrogens work partly by increasing a normal clear discharge from the vagina and making the vulva and urethra healthy. Using or applying an estrogen relieves or lessens: dryness and soreness in the vagina, itching, redness, or soreness of the vulva. Conditions that are treated with vaginal estrogens include a genital skin condition (vulvar atrophy), inflammation of the vagina (atrophic vaginitis), and inflammation of the urethra (atrophic urethritis). Pharmacology: Dienestrol is a synthetic, non-steroidal estrogen. Estrogens passively diffuse into target cells of responsive tissues, complex with the estrogen receptors, and enter the cell's nucleus to initiate or enhance gene transcription of protein synthesis after binding to DNA. Mechanism of action: Estrogens diffuse into their target cells and interact with a protein receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. The combination of an estrogen with a progestin suppresses the hypothalamic-pituitary system, decreasing the secretion of gonadotropin-releasing hormone (GnRH). Drug type: Approved. Small Molecule. Drug category: Estrogens, Non-Steroidal
Preferred ID: CHEBI:4518 Type: term ID# ILX:0103220 Score: 0
Dicumarol
Description: An oral anticoagulant that interferes with the metabolism of vitamin K. It is also used in biochemical experiments as an inhibitor of reductases. (PubChem) Pharmacology: Dicumarol is an coumarin-like compound found in sweet clover. It is used as an oral anticoagulant and acts by inhibiting the hepatic synthesis of vitamin K-dependent coagulation factors (prothrombin and factors VII, IX, and X). It is also used in biochemical experiments as an inhibitor of reductases. Mechanism of action: Dicumarol inhibits vitamin K reductase, resulting in depletion of the reduced form of vitamin K (vitamin KH2). As vitamin K is a cofactor for the carboxylation of glutamate residues on the N-terminal regions of vitamin K-dependent proteins, this limits the gamma-carboxylation and subsequent activation of the vitamin K-dependent coagulant proteins. The synthesis of vitamin K-dependent coagulation factors II, VII, IX, and X and anticoagulant proteins C and S is inhibited. Depression of three of the four vitamin K-dependent coagulation factors (factors II, VII, and X) results in decresed prothrombin levels and a decrease in the amount of thrombin generated and bound to fibrin. This reduces the thrombogenicity of clots. Drug type: Approved. Small Molecule. Drug category: Anticoagulants. Enzyme Inhibitors. Uncoupling Agents
Preferred ID: ILX:0103213 Type: term ID# ILX:0103213 Score: 0
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