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

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Showing 12661 - 12670 of 12951 results

Status:
Possibly Marketed Outside US
Source:
Japan:Sitafloxacin Hydrate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Sitafloxacin hydrate (DU-6859a, Gracevit), a new-generation, broad-spectrum oral fluoroquinolone that is very active against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, was recently approved in Japan for the treatment of respiratory and urinary tract infections. This is a new quinolone oral antibacterial to inhibit DNA replication of bacteria at the time of infection, and shows antibacterial action. Sitafloxacin is active against methicillin-resistant staphylococci, Streptococcus pneumoniae and other streptococci with reduced susceptibility to levofloxacin and other quinolones and enterococci. Sitafloxacin has also demonstrated activity against clinical isolates of Klebsiella pneumoniae (including about 67% of strains producing extended-spectrum, beta-lactamases and resistant to ciprofloxacin), Enterobacter cloacae, Pseudomonas aeruginosa with some activity against quinolone-resistant strains and Acinetobacter baumannii. The in vitro activity against anaerobes is comparable to imipenem or metronidazole. Sitafloxacin showed dual inhibitory activity against both enzymes: Streptococcus pneumoniae DNA gyrase and topoisomerase IV.
Pixantrone is a novel anthracenedione. It is a weak inhibitor of topoisomerase II. Pixantrone directly alkylates DNA forming stable DNA adducts and cross-strand breaks. Pixuvri is approved for the treatment of adult patients with multiply relapsed or refractory aggressive Non-Hodgkin lymphomas. It is used for patients whose cancer does not respond or has returned after they have received other chemotherapy treatments. The most frequent AE were seen in the blood (mainly neutropaenia), gastrointestinal (nausea, abdominal pain, constipation) and respiratory systems (cough, dyspnea). No drug-drug interaction studies have been submitted and no drug interactions have been reported in human subjects
Pirmenol is an antiarrhythmic agent, which exhibits effects on the fast action potential similar to other class 1 membrane active antiarrhythmic agents. Pirmenol depresses not only the fast Na+ channel, but also others, such as the slow Ca2+ and K+ channels. Pirmenol had sevenfold lower affinity for glandular-type muscarinic receptors (M3) than for cardiac-type muscarinic receptors (M2). This medicine regulates disturbed pulse by acting on the cardiac muscle. Usually, used for treatment of tachyarrhythmia (ventricular). The most commonly reported adverse reactions include constipation, discomfort in stomach, difficulty in urination (urinary retention), headache, insomnia, bitterness in the mouth, nausea, dry mouth and palpitation. Lidocaine, procainamide and quinidine a greater degree of arrhythmia conversion occurred when dosed 15 min after pirmenol than when these agents were dosed alone.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Melperone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Melperone is an antipsychotic drug which is used in Europe for the treatment of sleep disorders, agitation and confusion states. The exact mechanism of melperone action is unknown.
Status:
Possibly Marketed Outside US
Source:
Canada:PIPOTIAZINE PALMITATE
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pipotiazine (Piportil), also known as Pipothiazine, is a typical antipsychotic of the phenothiazine class used in the United Kingdom and other countries for the treatment of schizophrenia. Its properties are similar to those of chlorpromazine. Piportil® L4 (pipotiazine palmitate) is the palmitic ester of pipotiazine, a piperidine phenothiazine with antipsychotic properties and weak sedative activity. The esterification of pipotiazine is responsible for its prolonged duration of action. The onset of action appears usually within the first 2 to 3 days after injection and the effects of the drug on psychotic symptoms are significant within one week. Improvement in symptomatology lasts from 3 to 6 weeks, but adequate control may frequently be maintained with one injection every 4 weeks. However, in view of the variations in individual response, careful supervision is required throughout treatment. Piportil L4 has actions similar to those of other phenothiazines. Among the different phenothiazine derivatives, Piportil L4 appears to be less sedating and to have a weak propensity for causing hypotension or potentiating the effects of CNS depressants and anesthetics. However, it produces a high incidence of extrapyramidal reactions.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Carbuterol is a beta-adrenergic bronchodilator with selectivity for bronchial smooth muscle relative to cardiac and vascular tissues of several species including man. In vitro studies demonstrated that carbuterol was a direct acting beta-adrenergic agonist, not dependent on endogenous catecholamine release, and was devoid of alpha-adrenergic agonist activity. The activity of the racemate was shown to reside primarily in the l-enantiomer. Carbuterol inhibited immunologically induced release of histamine and slow reacting substance of anaphylaxis from passively sensitized fragmented rhesus monkey lung and also inhibited passive cutaneous anaphylaxis in rats. Acute toxicity studies in mice, rats and guinea pigs indicated a wide safety margin for carbuterol. Carbuterol is a safer and more effective bronchodilator than ephedrine.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Oxetorone is an antimigraine drug used for the disease-modifying treatment of migraines and marketed in several European countries. It works by non-selective inhibition of serotonin receptors and antihistamine agent. The therapeutic effects of oxetorone are primarily linked to antiserotonergic and also antihistamine and anti-adrenergic properties. Antidopaminergic properties are also suspected because hyperprolactinemia and extrapyramidal reactions have been observed. Adverse effects are: hypertonia, drowsiness at the start of treatment, diarrhoea and lymphocytic colitis. Acute intoxications by oxetorone, although uncommon, are potentially severe poisonings.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Josamycin is a macrolide antibiotic produced by Streptomyces narbonensis var. josamyceticus. Macrolides are inhibitors of protein synthesis. They impair the elongation cycle of the peptidyl chain by specifically binding to the 50S subunit of the ribosome. Josamycin has antimicrobial activity against a wide spectrum of pathogens. It is similar to erythromycin, but does not induce macrolide resistance in staphylococci and appears to have a lower incidence of gastrointestinal side effects. Josamycin is under investigation in US.
Status:
Possibly Marketed Outside US
Source:
Japan:Piroheptine Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Piroheptine is an antagonist of muscarinic acetylcholine receptors. The drug was used for the treatment of Parkinson's disease, however, it is no longer marketed.
Status:
Possibly Marketed Outside US
Source:
Fenoctimine sulfate by ZYF Pharm Chemical
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Fenoctimine is a nonanticholinergic inhibitor of gastric acid secretion in dogs and rats. Fenoctimine was more potent than cimetidine in the reduction of basal acid secretion in the gastric fistula rat and inhibited the production of gastric acid stimulated by histamine, gastrin tetrapeptide or bethanechol in the chronic gastric fistula dog. This compound is not an H2-antagonist but does inhibit the H+/K+-ATPase of hog gastric mucosa. The in vitro metabolism of fenoctimine by rat liver homogenates resulted in the oxidation of the aliphatic chain at the seven carbon, initially to an alcohol and then to a ketone. The unexpectedly weak effect of fenoctimine as a gastric antisecretory agent in humans, as well as anticholinergic effects, may be due to its extensive metabolism, which is different from that seen in dog and rat. The development of fenoctimine has been discontinued for unspecified reason.

Showing 12661 - 12670 of 12951 results