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

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Showing 981 - 990 of 1040 results

(R)-Timolol is the (R)-enantiomer of non-selective Beta antagonist Timolol. (R)-Timolol is a ß-adrenergic blocking agent that binds only to nonspecific sites in the particulate fraction of the heart, lungs, and brain. (R)-Timolol is an antihypertensive agent that increases ocular blood flow and reduces intraocular pressure. (R)-Timolol is one of the impurities in commercial formulation of (S)-Timolol.
Ethamsylate (2,5-dihydroxy-benzene-sulfonate diethylammonium salt) is a synthetic hemostatic drug indicated in cases of capillary bleeding. Ethamsylate acts on the first step of hemostasis by improving platelet adhesiveness and restoring capillary resistance. In addition it inhibits prostaglandin biosynthesis. Well-controlled clinical trials clearly showed the therapeutic efficacy of ethamsylate in dysfunctional uterine bleeding, with the magnitude of blood-loss reduction being directly proportional to the severity of the menorrhagia. Other well-controlled clinical trials showed therapeutic efficacy of ethamsylate in periventricular hemorrhage in very low birth weight babies and surgical or postsurgical capillary bleeding.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Unithiol was developed in the Soviet Union in the late 1950s. It only became more widely used in America and Western Europe since the mid-1970s, and particularly since the late 1970s when the Heyl Company in Germany began production. It remained the mainstay of chelation treatment of arsenic and mercury intoxication for more than half a century. Unithiol has been used in the management of acute and chronic poisoning with a number of different metals and metalloids, and is particularly useful for arsenic, bismuth and mercury. Unithiol can be given parenterally or orally depending on the clinical situation and severity of poisoning. Its action mechanism is close that of complexones. Active sulfhydryl groups enter into reactions with thiol poisons present in blood and tissues, form not toxic complex with them eliminated with urine. The poisons fixation results in the body enzyme systems changed under the poisons effect functions restoration. It is efficient as an antidote in case of intoxications by arsenic and heavy metals salts.
Status:
Possibly Marketed Outside US
Source:
NCT00460577: Phase 4 Interventional Completed Acute Bronchial Obstruction, Asthma
(2007)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Fenoterol is a beta2-adrenoreceptor agonist, used as a bronchodilator for the treatment and prevention of bronchospasms, associated with asthma and chronic obstructive airway disease, including bronchitis and pulmonary emphysema. Fenoterol is also used for tocolysis during premature labor. Marketing of fenoterol for treatment of asthma was suspended in Australia and New Zealand because of an increased risk of deaths, most likely due to excessive self-administration of the drug.
Ethamsylate (2,5-dihydroxy-benzene-sulfonate diethylammonium salt) is a synthetic hemostatic drug indicated in cases of capillary bleeding. Ethamsylate acts on the first step of hemostasis by improving platelet adhesiveness and restoring capillary resistance. In addition it inhibits prostaglandin biosynthesis. Well-controlled clinical trials clearly showed the therapeutic efficacy of ethamsylate in dysfunctional uterine bleeding, with the magnitude of blood-loss reduction being directly proportional to the severity of the menorrhagia. Other well-controlled clinical trials showed therapeutic efficacy of ethamsylate in periventricular hemorrhage in very low birth weight babies and surgical or postsurgical capillary bleeding.
Minodronic acid (RECALBON®, Bonoteo®), a third-generation bisphosphonate, was approved in Japan for the oral treatment of osteoporosis. This drug increases the bone mineral density and the strength by inhibiting osteoclastic bone resorption. Nitrogen-containing bisphosphonates, such as minodronic acid (RECALBON®, Bonoteo®) induce osteoclast apoptosis by inhibiting farnesyl pyrophosphate synthase (FPPS), a key enzyme in the mevalonate pathway. Inhibition of FPPS in osteoclasts prevents the biosynthesis of isoprenoid lipids that are required for the prenylation of small GTPase signaling proteins necessary for osteoclast function. Similarly, nitrogen-containing bisphosphonates have been shown to inhibit farnesyl pyrophosphate/geranyl pyrophosphate synthase activity.
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
Source:
NCT00292747: Phase 4 Interventional Terminated Dysmenorrhea
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Drotaverine, an antispasmodic drug, is a synthetic derivative of the natural isoquinoline alkaloid of Papaver somniferum, papaverine. It inhibits cyclic-3',5'-nucleotide-phophodiesterase (PDE) enzymes with concentration-dependent specificity, in addition, it behaves as a L-type voltage- operated calcium channel (L-VOCC) blocker. Drotaverin also acts as a cytostatic compound for several human tumor cell lines. Drotaverine is an effective medicine to treat spasm or twitches of the smooth muscles in the stomach and heart. It is used to relieve pain caused due to irritable bowel syndrome, headache, menstrual periods, and is also used to relieve cervical spasm during labor.
Status:
Possibly Marketed Outside US
Source:
NCT04601324: Phase 4 Interventional Withdrawn Allergic Rhinitis
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Rupatadine is characterised as a non-sedating H1 anti-histamine and platelet-activating factor (PAF) receptor antagonist. Rupatadine is indicated for the treatment of allergic rhinitis and urticaria. Rupatadine is a safe and well tolerated drug in patients over 2 years old, with no central nervous system or cardiovascular effects and it can be taken with or without foods.