U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 2721 - 2730 of 2778 results

Ximelagatran (Exanta or Exarta, H 376/95) is an anticoagulant that has been investigated extensively as a replacement for warfarin that would overcome the problematic dietary, drug interaction, and monitoring issues associated with warfarin therapy. In 2006, its manufacturer AstraZeneca announced that it would withdraw pending applications for marketing approval after reports of hepatotoxicity (liver damage) during trials, and discontinue its distribution in countries where the drug had been approved (Germany, Portugal, Sweden, Finland, Norway, Iceland, Austria, Denmark, France, Switzerland, Argentina and Brazil). Ximelagatran is a prodrug that is rapidly converted after oral administration to the active compound melagatran. Melagatran is able to inhibit thrombin activity directly and quickly. The melagatran molecule binds to the arginine side pocket of thrombin, inactivating the thrombin. Following oral administration of ximelagatran, oral bioavailability (measured as melagatran) is 18% to 25%. Peak melagatran levels after a ximelagatran dose of 48 mg twice daily are achieved within approximately 2 hours. Ximelagatran is rapidly and extensively converted to melagatran in the liver and other tissues. This conversion is achieved by ester hydrolysis and reduction via two intermediate metabolites, hydroxymelagatran, and ethylmelagatran. The predominant compound in plasma is the active drug, melagatran. The elimination half-life of melagatran after an oral dose of ximelagatran is 2.5 to 4.3 hours.
Status:
Possibly Marketed Outside US
Source:
Japan:Mitiglinide Calcium Hydrate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Mitiglinide is a drug for the treatment of type 2 diabetes currently marked under tradename Glufast. Glufast® is available as the tablet for oral use, containing 5 mg or 10 mg of Mitiglinide calcium hydrate. The recommended dose is 10 mg three times daily just before each meal (within 5 minutes). Mitiglinide was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on January 29, 2004, and is currently co-marketed in Japan by Kissei and Takeda. Mitiglinide is a rapid-acting insulin secretion-stimulating agent, its belongs to the meglitinide (glinide) class of blood glucose-lowering drugs. Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) (K(ATP)) channels in pancreatic beta-cells.
Cyamemazine (Tercian), also known as cyamepromazine, is a typical antipsychotic drug of the phenothiazine class used primarily in the treatment of schizophrenia and psychosis-associated anxiety. Cyamemazine actually behaves like an atypical antipsychotic, due to its potent anxiolytic effects and lack of extrapyramidal side effects. Cyamemazine is used for the treatment of chronic psychotic states, anxiety, major depression.
Ifenprodil (marketed under the brands Vadilex; Dilvax; Creocral; Cerocral) is a selective NMDA receptor (glutamate) antagonist. Additionally, ifenprodil inhibits GIRK channels, and interacts with alpha1 adrenergic, serotonin, and sigma receptors. Ifenprodil acts as a vasodilator. Ifenprodil is a medicine available in a number of countries worldwide, but not in US.
Status:
Possibly Marketed Outside US
Source:
Japan:Mebhydrolin Napadisilate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Mebhydrolin (INN) or mebhydroline is a histamine H1-receptor antagonist. It is not available in the United States, but it is available in various other countries under the brand names Bexidal and Diazolin. It is used for symptomatic relief of allergic symptoms caused by histamine release, including nasal allergies and allergic dermatosis.
Tinoridine is a non-steroidal anti-inflammatory and analgesic agent. This agent has been proved pharmacologically to show antiedematous and analgesic actions. The mechanism of the anti-inflammatory action of Tinoridine is attributed to its biomembrane stabilizing action particularly on the lysosomes which are related to cell or tissue damage at the time of inflammation through the release of hydrolytic enzymes. Tinoridine may produce gastrointestinal disorders (nausea, loss of appetite, diarrhea, and constipation), vertigo drowsiness, dry mouth and itching.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Moxaverine, a derivative of papaverine, is a phosphodiesterase inhibitor. Moxaverine has been studied in phase III of a clinical trial for the treatment of ocular blood flow in patients with age- related macular degeneration and primary open angle glaucoma. In addition, it has been studied in phase II of the clinical trial for the treatment of ischemia. This compound is prohibited by FEI (International Federation of equine).
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Butoxamine is a selective antagonist of the beta2 adrenergic receptor. It was discovered in laboratories of Farbwerke Hoechst. Administration of 25-50 mg subcutaneously or 50-150 mg orally induced mescaline syndrome, disorders of consciousness and a psychotic episode with amnesia. At an oral dose of 5 mg, butoxamine inhibited metabolic changes induced by fasting and administration of catecholamines. Butoxamine was not developed further and is mainly used in biomedical research to study the functional role of beta2 receptors.
Status:
Possibly Marketed Outside US
Source:
Japan:Benexate Hydrochloride Betadex
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Benexate is an active ingredient of benexate.CD or benexate hydrochloride betadex, a beta-cyclodextrin complex. Benexate was approved for the treatment of Gastric Ulcer in Japan. The terapeuthic effect of benexate is associated with promotion of prostaglandin synthesis, inhibition of acid secretion and increase in mucosal blood flow.
Bendazac, (1-benzyl-1H-indazol-3-yl-oxy)-acetic acid, is structurally related to indomethacin. Its lysine salt has been reported to be absorbed better than the parent compound. It is applied topically as bendazac lysine 0.5% (wt/vol) aqueous solution for delaying the progression of cataract. Topical application of bendazac is associated with transient burning sensation. It reduces the secretion of the skin ulcer surface, promotes skin formation and accelerates tissue repair.

Showing 2721 - 2730 of 2778 results