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

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Showing 8171 - 8180 of 8504 results

Status:
Possibly Marketed Outside US
Source:
Japan:Milacainide Tartrate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Milacainide (Ro 22-9194) is structurally related to lidocaine and has a pyridine ring in the side chain. Ro 22-9194 is a new Class I antiarrhythmic agent with a TXA, synthase inhibitory activity. In anesthetized, open-chest dogs Ro 22-9194 transiently decreased arterial blood pressure and affected AV conduction more selectively, with a prolongation of the HV interval, than sinoatrial nodal pacemaker activity. In isolated, blood-perfused atria of dogs, Ro 22-9 194 decreased myocardial contractility more than sinoatrial nodal pacemaker activity. Studies in guinea pig papillary muscles and single ventricular myocytes showed that Ro 22-9194 inhibits sodium channels in a use- and voltage-dependent manner, and belongs to the group comprising intermediate kinetic drugs and activated channel blockers. Epinephrine-, digitalis-, two-stage coronary ligation-, and 3-hr coronary ligation-reperfusion-induced ventricular arrhythmias, or aconitine-induced atrial arrhythmias, in dogs were potently suppressed by Ro 22-9194 administered orally or intravenously. In myocardial ischemia and reperfusion-induced arrhythmias of dogs, Ro 22-9194 had an antifibrillatory effect and prevented an increase in venous levels of TXB, released from the ischemic myocardium.
Status:
Possibly Marketed Outside US
Source:
XANBON by Kinex Pharmaceuticals| Ono Pharmaceutical
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Ozagrel is a thromboxane A2 synthesis inhibitor used for the treatment of cerebral vasospasm and asthma due to its antiplatelet and anti-inflammation properties.
Hippuric Acid is 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. Hippuric Acid is used therapeutically in the form of its salts (hippurates of calcium and ammonium). It is an ingredient of FDA-approved drug Hiprex (methenamine hippurate tablets USP). Each yellow capsule-shaped tablet of Hiprex contains 1 g Methenamine Hippurate which is the Hippuric Acid Salt of Methenamine (hexamethylene tetramine). The tablet also contains inactive ingredients. Hiprex (methenamine hippurate tablets USP) has antibacterial activity because the methenamine component is hydrolyzed to formaldehyde in acid urine. Hippuric acid has some antibacterial activity and also acts to keep the urine acid. The drug is generally active against E. coli, enterococci and staphylococci. Enterobacter aerogenes is generally resistant. The urine must be kept sufficiently acid for urea-splitting organisms such as Proteus and Pseudomonas to be inhibited. Hiprex is indicated for prophylactic or suppressive treatment of frequently recurring urinary tract infections when long-term therapy is considered necessary.
Thiamine disulfide is a vitamin B1 derivative. It is used as a component of vitamin complexes for the treatment of neurological and other disorders associated with disturbance of metabolic functions influenced by B-complex vitamins, including diabetic polyneuropathy, alcoholic peripheral neuritis and post-influenzal neuropathies, for the treatment of neuritis and neuralgia of the spinal nerves, especially facial paresis, cervical syndrome, low back pain, and ischialgia. It has being shown to be a potent inhibitor of human immunodeficiency virus (type-1) production, suggesting that thiamine disulfide may be important for AIDS chemotherapy.
Status:
Possibly Marketed Outside US
Source:
NCT01066676: Phase 4 Interventional Completed Osteoarthritis of the Hip or Knee
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Dexibuprofen, S(+)-ibuprofen, is a non-steroidal anti-inflammatory drug and active dextrorotatory enantiomer of ibuprofen. Pharmacotherapeutic effects of dexibuprofen are more potent with lesser side effects than that of the racemic mixture of both isomers. In the acute and chronic treatment of osteoarthritis, it exhibits equivalent efficacy and tolerability as that of celecoxib. Dexibuprofen is a non-selective inhibitor of cyclooxygenase (COX), which is an enzyme involved in prostaglandin (mediators of pain and fever) and thromboxane (stimulators of blood clotting) synthesis via the arachidonic acid pathway. Dexibuprofen is a non-selective cyclooxygenase inhibitor and hence, it inhibits the activity of both COX-1 and COX-2. The inhibition of COX-2 activity decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling while the inhibition of COX-1 is thought to cause some of the side effects of Dexibuprofen including GI ulceration. The major disadvantage of dexibuprofen is its low bioavailability, the account of its low solubility in physiological media.
Status:
Possibly Marketed Outside US
Source:
Inkazan by Ordzhonikidze All-Union Scientific-Research Pharmaceutical-Chemistry Institute
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Metralindole (Inkazan) is a reversible inhibitor of monoamine oxidase A (RIMA) which was used in Russia as an antidepressant. Inkasan (3-methyl-8-methoxy-3H, 1,2,5,6- tetrahydropyrazine /1.2.3-ab/-beta-carboline hydrochloride) has pharmacological properties characteristic of antidepressants. The clinical antidepressant effect of inkasan is combined with stimulating action. The drug is primarily indicated for patients in whom adynamic (anergic) disturbances are predominant in the clinical picture of depression.
Indium is a rare, soft silvery-white metal. It is used in some manufacturing process, butt here is no known biological role for indium in the human body. Although there are claims that indium increases hormone production, stimulates immune system function, and increases energy, there is no reliable scientific evidence to support such claims. In vitro, indium-III salts appears to have cytotoxic activity against melanoma. Indium cation (Indium-III), when complexed with 8-hydroxyquinoline (oxine), has been employed as a radioactive platelet label for thrombus imaging in animals and man. The short half-life (2.8 d) and high yield of gamma photons of 111In make it ideal for in vitro counting and external imaging. Indium In 111 ProstaScint (Capromab Pendetide) is indicated as a diagnostic imaging agent in newly-diagnosed patients with biopsy-proven prostate cancer, thought to be clinically-localized after standard diagnostic evaluation (eg chest x-ray, bone scan, CT scan, or MRI), who are at high-risk for pelvic lymph node metastases. It is not indicated for patients who are not at high risk. Indium In 111 ProstaScint is also indicated as a diagnostic imaging agent in post-prostatectomy patients with a rising PSA and a negative or equivocal standard metastatic evaluation in whom there is a high clinical suspicion of occult metastatic disease.
Indium is a rare, soft silvery-white metal. It is used in some manufacturing process, butt here is no known biological role for indium in the human body. Although there are claims that indium increases hormone production, stimulates immune system function, and increases energy, there is no reliable scientific evidence to support such claims. In vitro, indium-III salts appears to have cytotoxic activity against melanoma. Indium cation (Indium-III), when complexed with 8-hydroxyquinoline (oxine), has been employed as a radioactive platelet label for thrombus imaging in animals and man. The short half-life (2.8 d) and high yield of gamma photons of 111In make it ideal for in vitro counting and external imaging. Indium In 111 ProstaScint (Capromab Pendetide) is indicated as a diagnostic imaging agent in newly-diagnosed patients with biopsy-proven prostate cancer, thought to be clinically-localized after standard diagnostic evaluation (eg chest x-ray, bone scan, CT scan, or MRI), who are at high-risk for pelvic lymph node metastases. It is not indicated for patients who are not at high risk. Indium In 111 ProstaScint is also indicated as a diagnostic imaging agent in post-prostatectomy patients with a rising PSA and a negative or equivocal standard metastatic evaluation in whom there is a high clinical suspicion of occult metastatic disease.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Phenocoll is an antineuralgic, analgesic and antipyretic drug. It is a derivative of phenacetin and thus has the same mechanism of action (COX-2 inhibition). Hydrochloride and salicylate salts of phenocoll were used to control inflammation in such diseases as gout, influenza, malaria, rheumatism and pleuritis. The drug is no longer available for marketing.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Phenocoll is an antineuralgic, analgesic and antipyretic drug. It is a derivative of phenacetin and thus has the same mechanism of action (COX-2 inhibition). Hydrochloride and salicylate salts of phenocoll were used to control inflammation in such diseases as gout, influenza, malaria, rheumatism and pleuritis. The drug is no longer available for marketing.

Showing 8171 - 8180 of 8504 results