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

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Showing 171 - 180 of 209 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Zilpaterol is an agonist of β2-adrenergic receptor. Zilpaterol exerts bronchospasmolytic action. Zilmax® (4.8% Zilpaterol hydrochloride) is used to increase rate of bodyweight gain, improve feed efficiency, and increase carcass leanness in cattle fed in confinement for a period of 20-40 consecutive days at the end of the feeding period before slaughter.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Zilpaterol is an agonist of β2-adrenergic receptor. Zilpaterol exerts bronchospasmolytic action. Zilmax® (4.8% Zilpaterol hydrochloride) is used to increase rate of bodyweight gain, improve feed efficiency, and increase carcass leanness in cattle fed in confinement for a period of 20-40 consecutive days at the end of the feeding period before slaughter.
Status:
Possibly Marketed Outside US
Source:
NCT00460577: Phase 4 Interventional Completed Acute Bronchial Obstruction, Asthma
(2007)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Fenoterol is a beta2-adrenoreceptor agonist, used as a bronchodilator for the treatment and prevention of bronchospasms, associated with asthma and chronic obstructive airway disease, including bronchitis and pulmonary emphysema. Fenoterol is also used for tocolysis during premature labor. Marketing of fenoterol for treatment of asthma was suspended in Australia and New Zealand because of an increased risk of deaths, most likely due to excessive self-administration of the drug.
Status:
Possibly Marketed Outside US
Source:
Japan:Etilefrine Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Etilefrine is a cardiac stimulant used as an antihypotensive. Intravenous infusion of this compound increases cardiac output, stroke volume, venous return and blood pressure in man and experimental animals, suggesting stimulation of both α and β adrenergic receptors. However, in vitro studies indicate that etilefrine has a much higher affinity for β1 (cardiac) than for β2 adrenoreceptors. Intravenous etilefrine increases the pulse rate, cardiac output, stroke volume, central venous pressure and mean arterial pressure of healthy individuals. Marked falls in pulse rate, cardiac output, stroke volume and peripheral bloodflow, accompanied by rises in mean arterial pressure, occur when etilefrine is infused after administration of intravenous propranolol 2,5 mg. These findings indicate that etilefrine has both β1 and α1 adrenergic effects in man. The French Health Products Agency concluded that etilefrine and heptaminol have an unfavourable harm-benefit balance, and also placed restrictions on the use of midodrine.
Status:
Possibly Marketed Outside US
Source:
NCT00460577: Phase 4 Interventional Completed Acute Bronchial Obstruction, Asthma
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Fenoterol is a beta2-adrenoreceptor agonist, used as a bronchodilator for the treatment and prevention of bronchospasms, associated with asthma and chronic obstructive airway disease, including bronchitis and pulmonary emphysema. Fenoterol is also used for tocolysis during premature labor. Marketing of fenoterol for treatment of asthma was suspended in Australia and New Zealand because of an increased risk of deaths, most likely due to excessive self-administration of the drug.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Practolol is a beta-adrenergic antagonist that has been used in the emergency treatment of cardiac arrhythmias. Practolol is a cardio-selective beta-blocking agent with an intrinsic sympathomimetic action, but devoid of local anaesthetic effect. It has been found effective in post infarction arrhythmias. In early infarction it reduces the area of necrosis as measured by surface ST segment mapping. Practolol has also been shown to be an effective drug in treating angina. Long-term treatment revealed advantageous effects of practolol on the incidence of anginal attacks and the number of nitroglycerin tablets consumed in daily life. There was also a noticeable improvement in the ECG. The results obtained in a double-blind trial, with placebo, proved the effectiveness of the drug. The treatment enabled the patients to lead appreciably more active lives. A marked increase in work performance, depending on the dose applied, was confirmed in exercise tolerance tests. No side-effects which would call for discontinuance of the treatment were seen during long-term administration with doses up to 800 mg daily. Like other beta-adrenergic antagonists, practolol competes with adrenergic neurotransmitters such as catecholamines for binding at sympathetic receptor sites. Practolol binds at beta(1)-adrenergic receptors in the heart and vascular smooth muscle, inhibiting the effects of the catecholamines epinephrine and norepinephrine and decreasing heart rate, cardiac output, and systolic and diastolic blood pressure. Practolol, discovered in 1966, was removed from the market due to severe side effects including conjunctival scarring, fibrosis, and metaplasia.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Practolol is a beta-adrenergic antagonist that has been used in the emergency treatment of cardiac arrhythmias. Practolol is a cardio-selective beta-blocking agent with an intrinsic sympathomimetic action, but devoid of local anaesthetic effect. It has been found effective in post infarction arrhythmias. In early infarction it reduces the area of necrosis as measured by surface ST segment mapping. Practolol has also been shown to be an effective drug in treating angina. Long-term treatment revealed advantageous effects of practolol on the incidence of anginal attacks and the number of nitroglycerin tablets consumed in daily life. There was also a noticeable improvement in the ECG. The results obtained in a double-blind trial, with placebo, proved the effectiveness of the drug. The treatment enabled the patients to lead appreciably more active lives. A marked increase in work performance, depending on the dose applied, was confirmed in exercise tolerance tests. No side-effects which would call for discontinuance of the treatment were seen during long-term administration with doses up to 800 mg daily. Like other beta-adrenergic antagonists, practolol competes with adrenergic neurotransmitters such as catecholamines for binding at sympathetic receptor sites. Practolol binds at beta(1)-adrenergic receptors in the heart and vascular smooth muscle, inhibiting the effects of the catecholamines epinephrine and norepinephrine and decreasing heart rate, cardiac output, and systolic and diastolic blood pressure. Practolol, discovered in 1966, was removed from the market due to severe side effects including conjunctival scarring, fibrosis, and metaplasia.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Carazolol is a beta1/beta2 adrenoreceptor blocking agent. Activity and safety of the drug were evaluated in clinical trials that were conducted in healthy subjects and in patients suffering from either chronic bronchitis or asthma. The drug, however, was not developed for human use. Instead, carazolol is used in to reduce stress in animals during transportation. In veterinary medicine, carazolol is given by intramuscular injection to pigs is indicated in stress-inducing situations. In cattle, carazolol is intended to be used for the prevention of shipment stress caused by transportation and formation of new herds.
Status:
Possibly Marketed Outside US
Source:
Unknown by Masaki, N.|Iizuka, H.|Yokota, M.|Ochiai, A.
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Higenamine HCl (norcoclaurine) is a plant-based alkaloid widely used as nutritional supplement in food and beverage industries. It exists in variety of plants including Tinospora crispa, Nandina domestica, Gnetum Parvifolium C.Y. Cheng, sarum Heterotropoides, Nelumbo nucifera. It was initially isolated from Aconitum and identified as the active cardiotonic component of this medicinal plant used as local and traditional medicines in many Asian regions for the treatment of various diseases such as collapse, syncope, painful joints, oedema, bronchial asthma etc. Various pharmacological properties and potentially multi-spectral medical applications of higenamine have been reviled in many in vitro and in vivo studies conducted in animals and humans. Pharmacological properties of higenamine include positive inotropic and chronotropic effect, activating slow channel effect, vascular and tracheal relaxation effect, anti-thrombotic, anti-apoptotic and anti-oxidative effect, anti-inflammatory and immunomodulatory effect. Studies on higenamine showed potential therapeutic effects for diseases like heart failure, disseminated intravascular coagulation (DIC), shock, arthritis, asthma, ischemia/reperfusion injuries and erectile dysfunction. Higenamine has been tested as a candidate of pharmacologic stress agent in the detection of coronary artery diseases (CADs) in human clinical studies in China. In animal models, higenamine has been demonstrated to be a β2 adrenoreceptor agonist. It partly exerts its actions by the activation of adenylate cyclase, responsible for boosting the cellular concentrations of the adrenergic second messenger, cAMP. Via a beta-adrenoceptor mechanism higenamine, induced relaxation in rat corpus cavernosum, leading to improved vasodilation and erectile function. Related to improved vasodilatory signals, higenamine has been shown to possess antiplatelet and antithrombotic activity via a cAMP-dependent pathway, suggesting it may contribute to enhanced vasodilation and arterial integrity. Anti-apoptotic and cardiac protective effects of higenamine were shown to be mediated by the β2-AR/PI3K/AKT cascade. Higenamine is marketed as a dietary supplement for weight loss and sport performance, and is added to many fat burning supplements. Along with many other β2 agonists, higenamine is prohibited by World Anti-Doping Agency for use in sports.
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.

Showing 171 - 180 of 209 results