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

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Showing 13141 - 13150 of 13315 results

Flupenthixol is a thioxanthene antipsychotic used in the treatment of schizophrenia and other psychoses, with the exception of mania and psychomotor hyperactivity due to an activating effect associated with this drug. It may also be employed as an antidepressant. Flupenthixol has a wide range of pharmacological actions. Flupenthixol blocks dopaminergic receptors, thus interfering with dopaminergic transmission in the brain. Flupenthixol also inhibits serotonin 5-HT, histamine H1, muscarinic and alpha-1 adrenergic receptors.
Status:
Possibly Marketed Outside US
Source:
NCT01876628: Phase 4 Interventional Completed Cellulitis
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Flucloxacillin is an isoxazolyl penicillin of the β-lactam group of antibiotics, which exerts a bactericidal effect upon many Gram-positive organisms including β-lactamase-producing staphylococci and streptococci. While no longer used in the United States, Flucloxacillin is supplied under a variety of trade names in other countries, including Floxapen, Flopen, Staphylex. Floxapen is indicated for the treatment of infections due to sensitive Gram-positive organisms, including β-lactamase-producing staphylococci and streptococci. Typical indications including, skin and soft tissue infections; respiratory tract infections; other infections caused by floxapen-sensitive organisms, like example, osteomyelitis, urinary tract infection, septicaemia, endocarditis. Floxapen is also indicated for use as a prophylactic agent during major surgical procedures when appropriate; for example cardiothoracic and orthopaedic surgery. Flucloxacillin, by its action on the synthesis of the bacterial wall, exerts a bactericidal effect on streptococci except those of group D (Enterococcus faecalis) staphylococci. It is not active against methicillin-resistant staphylococci. There is evidence that the risk of flucloxacillin induced liver injury is increased in subjects carrying the HLA-B*5701 allele. Despite this strong association, only 1 in 500-1000 carriers will develop liver injury. Consequently, the positive predictive value of testing the HLA-B*5701 allele for liver injury is very low (0.12%) and routine screening for this allele is not recommended. Flucloxacillin diffuses well into most tissue. Specifically, active concentrations of flucloxacillin have been recovered in bones: 11.6 mg/L (compact bone) and 15.6 mg/L (spongy bone), with a mean serum level of 8.9 mg/L. Flucloxacillin diffuses in only small proportion into the cerebrospinal fluid of subjects whose meninges are not inflamed. It is also excreted in small quantities in mother's milk. In normal subjects approximately 10% of the flucloxacillin administered is metabolised to penicilloic acid. The elimination half-life of flucloxacillin is in the order of 53 minutes.
Status:
Possibly Marketed Outside US
Source:
CURATODERM by Teijin Pharma
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Talcalcitol is a synthetic analogue of vitamin D3. Tacalcitol has been developed by Teijin in Japan with the aim of maintaining the potent cell-regulating properties of calcitriol without the calcium-related adverse effects. Tacalcitol differs structurally from calcitriol by hydroxylation in the 24 position instead of the 25 position. Tacalcitol can influence the principal pathogenetic factors of psoriasis by inducing normalisation of keratinocyte differentiation, performing an anti-proliferative action and finally modulating the inflammatory response. Tacalcitol has been launched as an ointment formulation for the treatment of psoriasis in various countries. High-dose formulations (ointment and lotion) are available in Japan.
Status:
Possibly Marketed Outside US
Source:
Апрофен
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Aprofene (widely known as aprophen or Апрофен (in Russia)), a Soviet drug, is an antagonist of muscarinic and nicotinic acetylcholine receptors. It had been used in Russia for the treatment of endarteritis (inflammation of the inner shell of the artery), peptic ulcer of the stomach and duodenum, spastic colitis (inflammation of the colon characterized by sharp contractions), cholecystitis (inflammation of the gallbladder) until was included in the list of psychotropic substances.
Roxatidine is an histamine H2-receptor antagonist. Roxatidine is a potent and selective inhibitor of basal and stimulated gastric acid secretion through competitive blockade of H2-receptors. Total pepsin secretion is reduced in a dose-dependent manner. There is an independent mucosal protection action. Roxatidine is indicated for the treatment of peptic ulcer, gastro-oesophageal reflux disease, gastritis, upper gastrointestinal haemorrhage and Zollinger-Ellison syndrome also it can be used as a premedication before anaesthesia. Roxatidine possessed a robust estrogenic activity.
Butetamate is a cough suppressant. It exerts antispasmodic, bronchodilator and anticholinergic properties.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (MIXED)


Eprozinol inhibits bronchoconstriction by an action on histamine H1 receptors and has been used in the treatment of asthma and bronchitis. No significant changes in cAMP and cGMP levels are observed in guinea pig trachea, with eprozinol or isoprenaline, at doses capable of inducing relaxation. Eprozinol is only a very weak phosphodiesterase inhibitor, at large concentrations. The anti-bronchoconstrictor activities of eprozinol and isoprenaline with regard to histamine are directly additive and show absolutely no interference with one another. Propranolol is without effect on in vivo anti-bronchoconstrictor activity of eprozinol on tracheal musculature. It is concluded, that the mechanisms brought into play by eprozinol to exert anti-bronchoconstrictor and bronchorelaxant activity, are completely independent of the adrenergic system. In a retrospective study of 199 cases of accidental or intentional acute poisoning with eprozinol, eprazinone and zipeprol, collected at the Poison Control Center were seven cases of seizures, all after ingestion of eight times the therapeutic dose. They resolved rapidly and without recurrence with symptomatic treatment.
Status:
Possibly Marketed Outside US
Source:
Skleronorm by Gruenenthal [W. Germany]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Etiroxate is a synthetic thyroxine derivative. It was used for the treatment of patients with hyperlipoproteinaemia. There were only slight side effects, such as gastric and autonomic nervous system symptoms. No statistically significant increase in anginal symptoms was found, even in patients with known coronary insufficiency. No negative effects on hepatic and renal function or the peripheral blood count were observed. Etiroxate caused a significant reduction in serum cholesterol, LDL-cholesterol, and serum apolipoprotein B. There was a significant decrease in HDL-cholesterol. Etiroxate might be used for the treatment and prevention of atherosclerotic disease.
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

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Oxeladin citrate is a cough suppressant, is a highly potent and effective drug used to treat all types of cough of various etiologies. Withdrawn from the Canadian, US, and UK markets in 1976 due to carcinogenicity. Oxeladine is a component of antitussive drug, Altussan, approved in Philippines.

Showing 13141 - 13150 of 13315 results