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

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Showing 5541 - 5550 of 12702 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Etofamide is a luminal amoebicide acting principally on the bowel lumen with actions and uses similar to diloxanide furoate. Adverse drug reactions might include flatulence, vomiting, urticaria, pruritis. 100 patients suffering chronic intestinal amebiasis were treated with Etofamide, in a dose of 1,0 g per day, for three consecutive days. The tolerance of this antiamebic drug was excellent in all patients, and the parasitological cure rate obtained was 92%.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Etofibrate is an ethylene glycol diester of clofibrate and nicotinic acid. The drug was used under the names Tricerol and Lipo-Merz, among the others, for the treatment of severe hypertriglyceridemia and mixed hyperlipidemia. The mechanism of etofibrate action implies activation of PPAR-alpha receptors.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (MIXED)

Tritoqualine is an inhibitor of histidine decarboxylase, an enzyme that catalyzes the conversion of histidine to histamine. Tritoqualine does not act on histamine receptors. It was marketed since 1960 for the treatment of allergic conditions and is available under tradename Hypostamine.
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:
Canada:RACTOPAMINE HYDROCHLORIDE
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ractopamine hydrochloride, a beta-adrenoceptor agonist, is a phenethanolamine salt approved for use as a feed additive. Recently published studies indicate that the RR-isomer (butopamine) is the stereoisomer with the most activity at the beta-adrenoceptor. Butopamine was shown to be a non-selective ligand at the beta1 and beta2-adrenoceptors, but signal transduction is more efficiently coupled through the b2-adrenoceptor than the beta1 adrenoceptor. Therefore, the RR-isomer of ractopamine is considered to be a full agonist at the beta2-adrenoceptor and a partial agonist at the beta1¬adrenoceptor. These results are consistent with the pharmacological characterization of racemic ractopamine in isolated cardiac (atria) and smooth muscle (costo-uterine, vas deferens, trachea), which shows a maximal response at beta2- and a submaximal response at beta1¬adrenoceptors when compared with the full beta1 and beta2-adrenoceptor agonist isoproterenol. Butopamine is chemically similar to dobutamine but, unlike dobutamine, it is not a catecholamine. Butopamine induces a positive inotropic response in patients with congestive heart failure but for equal increments in cardiac output, butopamine increases heart rate more than dobutamine. Butopamine inproved cardiac performance in patients with ventricular dysfunction and congestive heart failure. Butopamine was prepared by Tuttle et al (unpublished data) and has a structure similar to dobutamine. This compound is refractory to the action of catechol-O-methyl transferase and thus it is orally active and has a longlasting action. Clinical findings in acute heart failure cases have been reported by Thompson et al. Intravenous administration produced an increase in the cardiac index and heart rate and shortening of systolic time intervals. A few patients experienced ventricular ectopy, especially with the higher doses used. No data pertaining to oral administration are available.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Dextromoramide is a synthetic strong-acting opioid and full mu-opioid receptor agonist. Dextromoramide is a Schedule I drug illegal to possess. The current indication for Palfium® (dextromoramide) is severe acute or chronic pain requiring opioids, such as post-operative pain, and pain associated with bone fractures, malignancies and acute renal/biliary colic attacks in adults.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Tisopurine (or Thiopurinol) was used in the treatment of gout. This drug reduces uric acid concentrations by interfering with the early stages of its synthesis, thus avoiding increased blood concentrations of hypoxanthine and xanthine. In addition, it was discovered, that tisopurine caused acute hepatitis.
Status:
Possibly Marketed Outside US
Source:
Japan:Proxyphylline
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Proxyphylline is a xanthine derivative that acts as a cardiac stimulant, vasodilator and bronchodilator. In combination with ephedrine it’s used for relief of acute bronchial asthma and for reversible bronchospasm associated with chronic bronchitis and emphysema. Proxyphylline is readily absorbed from the gastrointestinal tract and it’s not converted to theophylline in the body. The clinical studies are agreed with the property of proxyphylline to inhibit the cyclic nucleotide phosphodiesterases.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Phenothrin
Source URL:

Class (Stereo):
CHEMICAL (MIXED)


Conditions:

Phenothrin, also called sumithrin and d-phenothrin, a synthetic pyrethroid compound, is widely used to control agricultural and household insects, as well as to eliminate human louse infestation, but studies conducted in Paris, France and the United Kingdom have shown widespread resistance to phenothrin. Synthetic pyrethroids, including phenothrin, have a similar mode of action as organochlorines. They act on the membrane of nerve cells of insects blocking the closure of the ion gates of the sodium channel during re-polarization. This strongly disrupts the transmission of nervous impulses. At low concentrations insects suffer from hyperactivity. At high concentrations they are paralyzed and die. The EPA has not assessed its effect on cancer in humans. However, one study performed by the Mt. Sinai School of Medicine links sumithrin with breast cancer; the link made by sumithrin's effect on increasing the expression of a gene responsible for mammary tissue proliferation.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Dopexamine hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Dopexamine hydrochloride is a synthetic catecholamine, structurally related to dopamine, with marked intrinsic agonist activity at beta 2-adrenoceptors, lesser agonist activity at dopamine DA1- and DA2-receptors and beta 1-adrenoceptors, and an inhibitory action on the neuronal catecholamine uptake mechanism. The drug is administered by intravenous infusion, and is characterized by a rapid onset and short duration of action. Dopexamine is being tested as a treatment for heart failure and sepsis.

Showing 5541 - 5550 of 12702 results