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

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Showing 1991 - 2000 of 2052 results

Xamoterol (ICI 118,587) is a partial agonist of beta1-adrenoceptors. Xamoterol acts on the cardiac beta 1-adrenergic receptor, modifies the response of the heart to variations in sympathetic activity. At rest, it produces modest improvements in cardiac contractility, relaxation, and filling without increase in myocardial oxygen demand. The improvements are maintained during exercise although the attendant tachycardia is attenuated. The beneficial effects of xamoterol on both systolic and diastolic function suggested that it would be effective in patients with mild-to-moderate heart failure, and this was demonstrated in small placebo-controlled studies where effort tolerance and symptoms were improved. Xamoterol produced improvements in exercise capacity, clinical signs, symptoms and quality of life with a low incidence of adverse experiences. Xamoterol is effective as monotherapy in heart failure.
Status:
Possibly Marketed Outside US
Source:
Myco-polycid by Grünenthal
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Chlormidazole was the first azole introduced the treatment of topical mycosis. It demonstrated inhibitory activity against many fungi and some gram-positive cocci. It is used for the treatment of fungal and bacterial infections of nails and skin, including interdigital and periungual mycoses. Possible side effects are: local skin irritation, burning, itching.
Vincamine is the major alkaloid of Vinca minor. Although vincamine has been used therapeutically for almost three decades, the exact mechanisms of action and its effects are still unknown. Vincamine is a peripheral vasodilator that increases blood flow to the brain. Vincamine is beneficial to the nervous system's cells feeding and protecting processes and is utilized as an adjuvant in case of cerebrovascular insufficiency, age-related psycho-behavioral disorders, post concussion syndrome in head trauma, in case of post-stroke sequels. Vincamine may be used as a dietary nootropic supplement.
Status:
Possibly Marketed Outside US
Source:
Unknown by Ward, K.Jr.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Trichlormethine is a nitrogen mustard vesicant that has application in chemical warfare and has been used as a cytostatic alkylating agent in leukemia and lymphoma therapy. Trichlormethine was tested for carcinogenicity by subcutaneous injection in mice and rats. The study in mice was inadequate for evaluation. In rats, trichlormethine induced a high incidence of sarcomas (mostly spindle-cell type) in animals of each sex at the site of subcutaneous injection, as well as a few intestinal adenocarcinomas; neither tumor type was seen in controls. Trichlormethine caused vomiting, anorexia and blood-containing feces in dogs a few hours after a single intravenous injection of 1 mg/kg BW. Decreased peripheral lymphocyte counts were observed in rabbits injected intravenously and in mice injected subcutaneously with trichlormethine. Trichlormethine was tested for carcinogenicity by subcutaneous injection in mice and rats. ln rats, trichlormethine induced a high incidence of sarcomas (mostly spindle-cell type) in animals of each sex at the site of subcutaneous injection, as well as a few intestinal adenocarcinomas; neither tumor type was seen in controls. Trichlormethine is possibly carcinogenic to humans (Group 2B).
Status:
Possibly Marketed Outside US
Source:
NCT01636947: Phase 4 Interventional Completed Nausea
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Tropisetron (Tropisetron-AFT) is a potent and selective serotonin 3 (5-hydroxytryptamine3; 5-HT3) receptor antagonist with antiemetic properties, probably mediated via antagonism of receptors both at peripheral sites and in the central nervous system. Surgery and treatment with certain substances, including some chemotherapeutic agents, may trigger the release of serotonin from enterochromaffin-like cells in the visceral mucosa and initiate the emesis reflex and its accompanying feeling of nausea. Tropisetron (Tropisetron-AFT) selectively blocks the excitation of the presynaptic 5-HT3 receptors of the peripheral neurons in this reflex, and may exert additional direct actions within the CNS on 5-HT3 receptors mediating the actions of vagal input to the area postrema.
Status:
Possibly Marketed Outside US
Source:
VIRULEX FORTE by Kabi
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Moroxydine is an antiviral drug discovered in the 1950’s which was shown to be active against DNA and RNA viruses. Moroxydine analogues are potent anti-hepatitis C virus (HCV) agents.
Alprenolol is a beta adrenoreceptor blocking agent and 5HT1A antagonist, developed by AstraZeneca and now available as generic drug. It is used for treatment of hypertension, angina pectoris due to coronary atherosclerosis and acute myocardial infarction.
Status:
Possibly Marketed Outside US
Source:
NCT04111315: Phase 4 Interventional Recruiting Low Back Pain
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Dipyrone, also known as Metamizole (INN), is an ampyrone sulfonate analgesic, antispasmodic and antipyretic. It was withdrawn from US market in 1977 on the basis of reports of agranulocytosis. Depyrone is still used to treat severe and diffucult for relieving pains of different origin; headache, tooth-ache, pains in the joints, muscles, following traumas and operations, gall and kidney colics, neurites, neuralgias, traumatic cerebrasthenia; inflammation of upper respiratory ways of microbial or virus origin; chorea; febrile states. Mechanism of action of dipyrone is complex. It is believed that dipyrone exerts its action by inhibiting COX-3, and activates opioid and cannabioid systems either itself, or by products of its metabolic degradation.
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
Source:
Lentoquine by De Senac, J.-B.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Hydroquinidine is a pharmaceutical agent that acts as a class I antiarrhythmic agent (Ia) in the heart. Hydroquinidine is a d-rotatory alkaloid derived from cinchiona bark. It is closely related to quinidine, differing from the latter alkaloid only in containing two more atoms of hydrogen in the molecule. The drug causes increased action potential duration, as well as a prolonged QT interval. It is not approved by FDA, but marketed in Spain, France, Italy and Pakistan under the brand names Lentoquine, Sérécor LP, Idrochinidina Lirca and Austacute, respectively. Like all other class I antiarrhythmic agents, Hydroquinidine primarily works by blocking the fast inward sodium current (INa). Hydroquinidine is also used for the treatment of Malaria.

Showing 1991 - 2000 of 2052 results