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

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Showing 91 - 100 of 152 results

Ibutilide is a 'pure' class III antiarrhythmic drug, used intravenously against atrial flutter and fibrillation. At a cellular level it exerts two main actions: induction of a persistent Na+ current sensitive to dihydropyridine Ca2+ channel blockers and potent inhibition of the cardiac rapid delayed rectifier K+ current, by binding within potassium channel pores. In other words, Ibutilide binds to and alters the activity of hERG potassium channels, delayed inward rectifier potassium (IKr) channels and L-type (dihydropyridine sensitive) calcium channels. Ibutilide is indicated for the rapid conversion of atrial fibrillation or atrial flutter of recent onset to sinus rhythm. Ibutilide is marketed as Corvert by Pfizer.
Bisoprolol is a cardioselective beta1-adrenergic blocking agent. It lower the heart rate and blood pressure and may be used to reduce workload on the heart and hence oxygen demands. This results in a reduction of heart rate, cardiac output, systolic and diastolic blood pressure, and possibly reflex orthostatic hypotension. Bisoprolol can be used to treat cardiovascular diseases such as hypertension, coronary heart disease, arrhythmias, ischemic heart diseases, and myocardial infarction after the acute event. General side effects are: fatigue, asthenia, chest pain, malaise, edema, weight gain, angioedema. Concurrent use of rifampin increases the metabolic clearance of bisoprolol fumarate, shortening its elimination half-life.
Levocarnitine propionate or Propionyl L-carnitine (PLC) is the propionyl ester of L-carnitine. Propionyl-L-carnitine stimulates energy production in ischaemic muscles by increasing citric acid cycle flux and stimulating pyruvate dehydrogenase activity. The free radical scavenging activity of the drug may also be beneficial. Propionyl-L-carnitine improves coagulative fibrinolytic homeostasis in vasal endothelium and positively affects blood viscosity. It exhibits a high affinity for the muscle enzyme, carnitine acyl transferase, and as such readily converts into propionyl-CoA and free carnitine. Most studies of the therapeutic use of PLC are focused on the prevention and treatment of ischemic heart disease, congestive heart failure, hypertrophic heart disease, and peripheral arterial disease. PLC is marketed under the trade name Dromos®. It is indicated for patients with peripheral arterial occlusive disorders and for exercise intolerance enhancement in patients with chronic congestive heart failure. Dromos is marketed in Italy.
Mrtoprolol is a beta-adrenergic receptor blocking agent. In vitro and in vivo animal studies have shown that it has a preferential effect on beta-1 adrenoreceptors, chiefly located in cardiac muscle. Clinical pharmacology studies have confirmed the beta-blocking activity of metoprolol in man, as shown by (1) reduction in heart rate and cardiac output at rest and upon exercise, (2) reduction of systolic blood pressure upon exercise, (3) inhibition of isoproterenol-induced tachycardia, and (4) reduction of reflex orthostatic tachycardia. Mrtoprolol is indicated for the treatment of hypertension, angina pectoris and myocardial infarction
Clemastine is an antihistamine with anticholinergic (drying) and sedative side effects. Clemastine is a selective histamine H1 antagonist and binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. It is used for the relief of symptoms associated with allergic rhinitis such as sneezing, rhinorrhea, pruritus and acrimation. Also for the management of mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Used as self-medication for temporary relief of symptoms associated with the common cold.
Status:
First approved in 1961
Source:
Plegine by Ayerst
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Phendimetrazine is an appetite suppressant that is FDA approved for the treatment of exogenous obesity. It is clinically available anorectic agent, which display minimal interactions with monoamine transporters in vitro. On the other hand, their medications is known to be psychomotor stimulants when administered in vivo as indicated by their shared properties with illicit drugs like cocaine. The following adverse reactions are described, or described in greater detail, in other sections: Primary pulmonary hypertension; Valvular heart disease; Effect on the ability to engage in potentially hazardous tasks; Withdrawal effects following prolonged high dosage administration. Use of phendimetrazine tartrate is contraindicated during or within 14 days following the administration of monoamine oxidase inhibitors because of the risk of hypertensive crisis.
There is no information about biological and pharmacological application of Iron(II) fluoride (also known as ferrous fluoride). It is known, that this substance is used to catalyze some organic reactions.
Status:
Investigational
Source:
INN:nebracetam
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Nebracetam (WEB1881FU) is a pyrrolidinone nootropic. Like other racetams, it is an aminomethyl pyrrolidinone derivative of piracetam. It was first synthesized in Germany in the late 1980s, where it was manufactured by Boehringer Ingelheim. Nebracetam is a M1-muscarinic agonist. In Jurkat cells Nebracetam induced a rise of [Ca2+]i in the medium with 1 mM Ca2+ and without Ca2+ (plus 1 mM EGTA). The nebracetam-induced [Ca2+]i rise was blocked by atropine greater than pirenzepine greater than AF-DX 116. Nebracetam facilitates the ganglionic muscarinic transmission through acting on presynaptic sites. Nebracetam has been investigated as a cognition-enhancing drug, but most of the studies have taken place in animal models. It has been shown to protect neurons in animals exposed to low levels of oxygen and low blood sugar. Nebracetam is also protective against glutamate toxicity, presumably via its modulation of calcium entry. In animal models of Alzheimer’s disease, nebracetam improved memory in a dose-dependent manner. It also protected against ischemia- (lack of oxygen) induced neuronal death in a rat model of stroke. The compound has also been tested as a possible antidepressant, presumably because its mechanism of action (reducing dopaminergic and serotonergic uptake) is similar to other commonly used antidepressants. Some studies have taken place in humans. A single dose was shown to alter brain waves in healthy volunteers, who showed increased alpha activity and an associated decrease of slow activity and of fast activity in the frontal cortex. These results imply that nebracetam might improve linguistic learning and memory processing. A trial in dementia patients reported that significant clinical improvement occurred after 8 weeks. However, other studies did not replicate this finding.
Status:
Investigational
Source:
INN:semotiadil
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Levosemotiadil is an S-enantiomer of semotiadil. It is an antiarrhythmic drug with sodium and calcium channel blocking action, as well as potassium blocking activity. Levosemotiadil is bound strongly and enantioselectively to human serum albumin and human alpha1-acid glycoprotein. Since levosemotiadil is hydrophobic basic drug, it is likely that this drug is also bound to lipoprotein in human plasma. Levosemotiadil might be effective in prevention of lethal arrhythmias. It was shown, that levosemotiadil prevented ventricular fibrillation in 64% of the high-risk animals. Heart rate responses to myocardial ischemia and to graded doses of isoproterenol were blunted by the high dose of levosemotiadil. Levosemotiadil had been in phase II clinical trials by Santen Pharmaceutical for the treatment of arrhythmias. However, this study was discontinued.