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

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Showing 361 - 370 of 657 results

Status:
Possibly Marketed Outside US
Source:
Japan:Landiolol Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Landiolol (Onoact) is an intravenously administered, ultra short-acting β1-blocker with an elimination half-life of 3-4 min and ≈8-fold greater cardioselectivity than esmolol in vitro. It is approved in Japan for the treatment of intraoperative and postoperative tachyarrhythmias, but in clinical practice is also used to prevent postoperative tachyarrhythmias, such as atrial fibrillation after coronary artery bypass grafting. Randomized controlled trials in patients undergoing open-heart surgery demonstrated that various dosages of landiolol (0.0005-0.04 mg/kg/min) [0.5-40 μg/kg/min] were more effective than diltiazem in converting postoperative atrial fibrillation to normal sinus rhythm during the first 8 h after surgery, and were more effective than placebo (or no landiolol) in preventing the development of atrial fibrillation during the first week after surgery (primary efficacy endpoints). Landiolol was generally well tolerated in clinical trials, with a relatively low risk of hypotension and bradycardia, although routine monitoring of cardiac function during landiolol administration is important. In general, adverse events such as reduced blood pressure resolve quickly after discontinuation of landiolol. Thus, as an ultra short-acting β1-blocker with a rapid onset of action and readily titratable and rapidly reversible effects, landiolol represents an important agent for the management of intraoperative and postoperative tachyarrhythmias.
Status:
Possibly Marketed Outside US
Source:
Japan:Denopamine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Denopamine is a selective agonist of beta-1 adrenergic receptor. The drug was approved in Japan under the name Kalgut for the treatment of chronic heart failure.
Status:
Possibly Marketed Outside US
Source:
Japan:Bucumolol Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Bucumolol is a beta-adrenergic antagonist. It can be used in the treatment of myocardial ischemia and hypertension.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Butofilolol (trade name Cafide) is a beta-blocker drug for the treatment of high blood pressure (essential hypertension). Butofilolol constitute a good therapeutic approach to hypertension in plethoric subjects when the weight reduction has failed to correct it adequately
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Alifedrine, a beta-adrenergic partial agonist, significantly improved performance of the failing heart. Alifedrine resulted in a significant dose-dependent increase in cardiac output. There were significant reductions in peripheral resistance, but little observed change in arterial pressure. With intravenous alifedrine, there were significant increases in stroke volume with little change in heart rate. With the 40 mg oral dose, there was a small increase in heart rate There were no clinically or statistically significant changes in arterial (non-invasive), pulmonary artery, pulmonary capillary or right atrial pressures with any dose of alifedrine. No significant arrhythmias were noted clinically with the doses studied.
Status:
Possibly Marketed Outside US
Source:
Japan:Befunolol Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Befunolol is a beta-adrenergic receptor blocker approved in Japan for the treatment of open-angle glaucoma. The current drug status is unknown.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Epanolol has been shown in animal models to be a selective beta-adrenoceptor partial agonist with agonist activity about 20 to 25% of that of the full agonist isoprenaline. Epanolol is a once-daily agent for the treatment of angina pectoris. The pharmacodynamic consequences in man of the degree of agonist activity possessed by the beta 1-selective partial agonist epanolol include little reductions at rest in heart rate, blood pressure, various measures of cardiac haemodynamic parameters, peripheral blood flow and renal function. On exercise there is attenuation of the heart rate and systolic blood pressure responses, with less perceived exertion than with atenolol. The lack of significant accumulation of epanolol indicates that no alteration of dose is necessary when using epanolol in elderly patients with normal renal and hepatic function.
Status:
Possibly Marketed Outside US
Source:
Japan:Trimetoquinol Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Trimetoquinol hydrochloride dilates bronchial muscle selectively by stimulating Beta 2-receptors. It is used for the relief of bronchoconstriction associated with bronchitis, asthmatic bronchitis and bronchial asthma. Since the concurrent use of the drug with catecholamines such as Epinephrine and Isoproterenol may induce arrythmia or cardiac arrest in some cases, concurrent use is not recommended. Adverse reactions : Palpitation may occur occasionally, and alteration of blood pressure and precordial pain may appear rarely; headache may occur occasionally; tremor, dizziness, feverish sensation may also be encountered in a rare incidence; occasionally, nausea and anorexia may appear.
Status:
Possibly Marketed Outside US
Source:
Zevtera by Avir Pharma Inc [Canada]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Ceftobiprole is a fifth-generation cephalosporin antibiotic. It was discovered by Basilea Pharmaceutica and was developed by Johnson & Johnson Pharmaceutical Research and Development. The drug is demonstrates activity against clinically important gram-positive pathogens, including methicillin-resistant Staphylococcus aureus, penicilliin-resistant Staphylococcus pneumoniae, and Enterococcus faecalis. The drug also has demonstrated activity against gram-negative bacteria including Citrobacter spp., Escherichia coli, Enterobacter spp., Klebsiella spp., Serratia marcescens, and Pseudomonas aeruginosa. The drug has gained regulatory authorization from European states for the treatment of hospital-acquired pneumonia (HAP, excluding ventilator-associated pneumonia, VAP) and community-acquired pneumonia (CAP).
Zinterol (MJ-9184-1) is an beta-adregenrgic agonist demostrated activity toward beta1-3 receptors. Oral zinterol caused a fast-appearing and long-lasting bronchodilator effect in patients with with stable chronic obstructive lung disease, however it seems development of zinterol was discontitued.

Showing 361 - 370 of 657 results