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

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Showing 741 - 750 of 1932 results

Status:
Possibly Marketed Outside US
Source:
NCT03509922: Phase 4 Interventional Completed Peripheral Artery Disease, PAD
(2018)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Sarpogrelate (brand name Anplag; former developmental code names MCI-9042, LS-187,118) is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. It blocks serotonin-induced platelet aggregation and has applications in the treatment of many diseases including diabetes mellitus, Buerger's disease, Raynaud's disease, coronary artery disease, angina pectoris, and atherosclerosis.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Phosmet is a non-systemic, organophosphate insecticide used on both plants and animals. Phosmet is mainly used on apple trees for control of coddling moth, though it is used on a wide range of fruit crops, ornamentals and vines for the control of aphids, suckers, mites and fruit flies. Phosmet is a moderately potent cholinesterase inhibitor.
Status:
Possibly Marketed Outside US
Source:
NCT00914420: Phase 4 Interventional Unknown status Coronary Artery Disease
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Trapidil, a platelet-derived growth factor antagonist, was originally developed as a vasodilator and anti-platelet agent and has been used to treat patients with ischemic coronary heart, liver, and kidney disease. Used to treat patients with ischemic coronary heart, liver, and kidney disease.
Lonazolac is a nonsteroidal anti-inflammatory drug. The mononuclear cell response to a synovial stimulus can be abolished by very low concentrations of lonazolac. This blockade can be completely released by the addition of prostaglandin E2. Lonazolac appears therefore as an agent able in addition to modulate the immune response. The release of histamine from human basophils was significantly decreased after preincubation of the cells with lonazolac Ca. Preincubation of human polymorphonuclear leukocytes with lonazolac Ca led to an inhibition of leukotriene generation induced by either the Ca ionophore or opsonized zymosan. Lonazolac Ca affected different enzymes of the platelet activating factor metabolism. After pre- and post-treatment with lonazolac-Ca, the numbers of animals with lung metastases and the score of metastases significantly decreased. Lonazolac-Ca is indicated for the treatment of painful inflammatory rheumatic diseases of the joints and the spine. Acute irritation in osteoarthritis and spondylosis. Soft tissue rheumatism. Post-traumatic and postoperative pain and swelling states.
Triflusal (trade names Disgren, Grendis, Aflen, Triflux, ets) is a member of the salicylate family with a well-established platelet aggregation inhibitory profile that differs from that of acetylsalicylic acid (ASA) in its pharmacokinetic and pharmacodynamic properties. Triflusal irreversibly inhibits cyclooxygenase-1 through its potency is lower than that of acetylsalicylic acid (ASA). Triflusal shows potent inhibition of vascular prostacyclin synthesis, and weak inhibition of platelet phosphodiesterase. Triflusal also favors the production of NO and increases the concentration of cyclic nucleotides. A number of experimental and clinical studies have shown that triflusal is a potentially useful choice in the treatment and prophylaxis of brain ischemia because of its antithrombogenic as well as neuroprotective effects. Triflusal anti-thrombogenic properties have been demonstrated clinically and experimentally, while its neuroprotective effects have been shown only in animal models. Triflusal is administered orally. It Is absorbed primarily in the small intestines and its bioavailability in humans ranges from 83% to 100%. Once absorbed, 99% of triflusal binds to plasma proteins in experimental animals as well as in humans. Triflusal readily crosses organic barriers, but its blood levels are always higher than tissue levels. Upon passage through the liver, triflusal is deacetylated, forming 2-hydroxy-4-trifluoro-methyl-benzoicacid (HTB) as the main active metabolite. Triflusal inhibits platelet aggregation and interaction of platelets with subendothelium. The antiplatelet effect of triflusal has been documented in experimental animals and in humans, in in vitro and ex vivo studies, and in in vivo models of thrombogenesis in animals. Triflusal inhibited collagen- or arachidonic acid-induced platelet aggregation in platelet-rich plasma more effectively than ADP-induced platelet aggregation. Independently of its antithrombotic effect, triflusal acts directly on the nervous tissue to reduce the damage caused by ischemic or cytotoxic insults. The daily oral intake of 600 mg triflusal led to HTB levels in the cerebrospinal fluid that had neuroprotective effects in experimental animals. Traditionally, antiplatelet drugs have been associated with an increased risk of bleeding complications.
Ornidazole is nitroimidazole derivative. It is an antiprotozoal drug that has proven to be effective against Trichomonas vaginalis, Entoamoeba histolytica, Giardia lamblia and Helicobacter pylori. The reduction of the nitro group and the generation of short-lived reactive intermediates are the basis of its parasiticidal activity. Ornidazole is a DNA-tropic drug with selective activity against microorganisms with enzyme systems capable of reducing the nitrogroup and catalyze the interaction between ferrodoxin proteins and nitrocompounds. After the drug penetrates the microbial cell, the mechanism of its action is based reducing the nitrogroup under the influence of the microorganism’s nitroreductases and the activity of the reduced nitroimidazole. The reduction products create compounds with DNA causing it to degrade, and disrupt the DNA replication and transcription processes. Furthermore, the drug’s metabolism products have cytotoxic properties and disrupt cellular respiration processes. It is indicated for the treatment of anaerobic systemic infections caused by ornidazole-sensitive microflora, prevention of infections caused by anaerobic bacteria, during operative treatment (especially middle and straight intestine surgeries), gynecological surgeries, severe intestinal ameobiasis, all extra-intestinal ameobiasis forms, giardiasis. Ornidazole was shown to be effective for the prevention of recurrence of Crohn's disease after ileocolonic resection.
Status:
Possibly Marketed Outside US
Source:
Unknown
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Hymecromone (4-methylumbelliferone) is already approved drug in Europe and Asia where it is used to treat biliary spasm. It is used as choleretic and antispasmodic drugs and as a standard for the fluorometric determination of enzyme activity. The concomitant administration of Hymecromone with products, containing metoclopramide, leads to mutual decrease of their action. Due to a danger of diarrhea with subsequent hypokalemia, Hymecromone should be applied with caution to patients on cardiac glycosides therapy (in these cases the sensitivity to them is increased). Hymecromone can be administered simultaneously with otherspasmolytics and analgesics. Very rare allergic reactions, itching, erythema, rashes; diarrhea which normally disappears by reduction of dose or discontinuance of therapy.
Status:
Possibly Marketed Outside US
Source:
Helmetina by Bernthsen, A.H.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Phenothiazine, the parent compound of a multitude of present-day drugs, has been employed on an extensive scale for its insecticidal, fungicidal, antibacterial and anthelmintic properties. Phenothiazine was formerly used as an insecticide and as a drug to treat infections with parasitic worms (antihelminthic) in livestock and people. It was introduced as antihelminthic in livestock in 1940 and is considered, with thiabendazole, to be the first modern antihelminthic. Almost a catholicon, its widespread use in animals and man has led to the uncovering of many adverse reactions encompassing effects on blood elements, neuromuscular problems and photosensitization. Its potential side effects have now limited its use. The chemical structure of phenothiazine provides a most valuable molecular template for the development of agents able to interact with a wide variety of biological processes. Synthetic phenothiazines (with aliphatic, methylpiperazine, piperazine-ethanol, piperazine-ethyl, or piperidine side-chain) and/or phenothiazine-derived agents e.g., thioxanthenes, benzepines, imonostilbenes, tricyclic antidepressants, dimetothiazine, and cyproheptadine have been effective in the treatment of a number of medical conditions with widely different etiology. These include various currently clinically used drugs for their significant antihistamic, antipsychotic, anticholinergic (antiparkinson), antipruritic, and/or antiemetic properties.
Status:
Possibly Marketed Outside US
Source:
NCT01822288: Phase 4 Interventional Completed Menopausal Syndromes
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tibolone (brand name Livial, Tibofem), also known as 7α-methylnoretynodrel, is a synthetic steroid drug with estrogenic, progestogenic, and weak androgenic actions which was introduced in 1988 and is used widely in Europe, Asia, Australasia, and, with the exception of the United States (where it is not available), the rest of the world. It is used mainly for treatment of endometriosis, as well as for the treatment of symptoms resulting from the natural or surgical menopause in post menopausal women. Women above 60 years of age should only start with LIVIAL treatment when they are intolerant of or contraindicated for other medicinal products approved for the treatment of oestrogen deficiency symptoms. Tibolone is used for the prevention of bone mineral density loss in postmenopausal women at high risk of future osteoporotic fractures who are intolerant of, or contraindicated for, other medicinal products approved for the prevention of bone mineral density loss. Tibolone has similar or greater efficacy compared to older hormone replacement drugs, but shares a similar side effect profile. It has also been investigated as a possible treatment for female sexual dysfunction. Tibolone is a 19-nortestosterone derivative and is related structurally to other 19-nortestosterone progestins. It is the 7α-methyl derivative of noretynodrel. Tibolone possesses a complex pharmacology. Its two major active metabolites, 3α-hydroxytibolone and 3β-hydroxytibolone, act as potent, fully activating agonists of the estrogen receptor (ER), with a high preference for ERα. Tibolone and its metabolite Δ-tibolone act as agonists of the progesterone and androgen receptors, while 3α-hydroxytibolone and 3β-hydroxytibolone, conversely, act as antagonists of these receptors. Lastly, tibolone, 3α-hydroxytibolone, and 3β-hydroxytibolone act as antagonists of the glucocorticoid and mineralocorticoid receptors, with preference for the mineralocorticoid receptor.
Status:
Possibly Marketed Outside US
Source:
ETOFYLLINE by Lespagnol, A. et al.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Etofylline [7-(2-hydroxyethyl)theophylline] is a N-7-substituted derivative of theophylline, a smooth muscle relaxant. Etofylline is used to relieve bronchoconstriction. It may act as a phosphodiesterase inhibitor and adenosine receptor antagonist.