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Query: UMLS:C0002962 (angina)
 21,142 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

We examined the importance of a long plasma half-life (t1/2) on the antianginal effects of beta-blockade by comparing equivalent doses of once-daily atenolol 100 mg (t1/2 6-8 h) and betaxolol 20 mg (t1/2 20-22 h) in a double-blind placebo-controlled cross-over study of 20 patients with stable angina pectoris. At 20 h postdose, heart rate (HR) was lower with betaxolol than with atenolol whereas blood pressure (BP) was equally reduced by both drugs. Twenty-four-hour ambulatory HR recording demonstrated that this difference existed for the last 6 h of the dosage cycle. During treadmill exercise, HR remained lower with betaxolol than with atenolol and exercise time was significantly prolonged only by betaxolol. With placebo, radionuclide ventriculography demonstrated that left ventricular ejection fraction (LVEF) decreased during exercise. Betaxolol, but not atenolol, significantly attenuated the exercise-induced decrease in EF. Thus, the long plasma t1/2 of betaxolol is associated with a reduction in exercise-induced ischemia when tested toward the end of the 24-h dosage cycle. Plasma t1/2 therefore is of clinical relevance to the antianginal, but not antihypertensive, actions of beta-blockers.
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PMID:Twenty-four-hour beta-blockade in stable angina pectoris: a study of atenolol and betaxolol. 138 Oct 24

To assess the efficacy of oral betaxolol in the treatment of stable exertional angina pectoris and to determine the relationship between betaxolol doses/serum concentrations and clinical/hemodynamic responses the authors studied 24 patients prior to and following stepwise administration of 5, 10, 20, 40, and 80 mg doses. The major endpoint for the study was the achievement of clinical beta blockade (heart rate 50-60 beats/min and less than or equal to 20% rise in treadmill stage I heart rate). Betaxolol produced a decrease in mean angina pectoris frequency from 6.6 +/- 1.9 episodes/week with placebo to 0.2 +/- 0.5 episode/week during clinical beta blockade (p less than 0.00005). Mean treadmill exercise time increased from 3.1 +/- 1.7 min with placebo to 7.3 +/- 2.3 min with doses sufficient to reduce angina pectoris frequency greater than or equal to 75% (p less than 0.00005) and to 8.0 +/- 2.3 min during clinical beta blockade (p less than 0.00005). The mean doses of betaxolol required to produce a greater than or equal to 75% decrease in angina pectoris frequency and clinical beta blockade were 12 +/- 5 mg (range 5-40 mg) and 28 +/- 29 mg (range 5-80 mg) respectively. Mean serum concentrations associated with these clinical endpoints were 23.8 +/- 9.7 ng/mL and 59.7 +/- 54.0 ng/mL respectively. The results indicate that betaxolol, in widely ranging doses, is highly effective in reducing angina pectoris frequency and improving exercise capacity in patients with stable exertional angina pectoris.
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PMID:Efficacy of betaxolol in the treatment of stable exertional angina pectoris: a dose-ranging study. 216 38

Betaxolol is a new, highly cardioselective, once-a-day beta blocker with a long half-life (mean 16 hours). The antianginal efficacy of 2 doses of betaxolol (20 and 40 mg) given once daily was evaluated and compared with propranolol (40 or 80 mg) 4 times daily. Ninety-two patients completed the 10-week double-blind trial. The resting and exercise heart rate, blood pressure and double product were similar for all treatment arms of the study during placebo treatment. Significant decreases in these measures occurred during active drug treatment when compared with placebo. No significant intergroup differences were noted at rest. Maximal exercise heart rate and double product were significantly lower during treatment with betaxolol 40 mg daily than in the propranolol 40 mg 4 times/day treatment group (p less than 0.05). All patients had chest pain and greater than or equal to 1 mm of ST-segment depression during the baseline placebo exercise test. After 10 weeks of active treatment, 55% of the patients were free of chest pain during maximal exercise (difference not significant between treatments). In the betaxolol 40 mg/day group, fewer (6 of 19; 32%) of the patients developed ST-segment depression with exercise (p less than 0.05) compared with propranolol 80 mg 4 times daily (21 of 26; 81%). Betaxolol appears to be a useful once-a-day cardioselective beta blocker for the therapy of angina pectoris.
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PMID:Double-blind comparison of once daily betaxolol versus propranolol four times daily in stable angina pectoris. Betaxolol Investigators Group. 217 81

A series of para-substituted phenoxypropanolamines has been synthesized and tested for beta-adrenoceptor blocking activity. Some derivatives (8, 11, 12, 20, 21) exhibited greater in vitro potency than the reference drugs metoprolol and propranolol. This series, in contrast to propranolol but similar to metoprolol, possesses cardioselectivity. The 3-[p-[(cycloalkylmethoxy)ethyl]phenoxy]-1-substituted-amino-2-prop anol derivatives 8 (cyclopropylmethoxyethyl: betaxolol) and 11 (cyclobutylmethoxyethyl) produced antihypertensive effects in spontaneously hypertensive rats. Betaxolol (Kerlon, 8) was found to exhibit an appropriate preclinical pharmacological and human pharmacokinetic profile (elevated oral bioavailability and prolonged plasma half-life) for the treatment of chronic cardiovascular diseases such as hypertension and angina.
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PMID:Synthesis of a series of compounds related to betaxolol, a new beta 1-adrenoceptor antagonist with a pharmacological and pharmacokinetic profile optimized for the treatment of chronic cardiovascular diseases. 288 12

Betaxolol, a long-acting cardioselective beta-blocker, was tested alone and in combination with long-acting nitrates in a multicenter, double-blind, parallel, placebo-controlled study of 3 weeks duration in patients with stable angina pectoris. All patients underwent exercise tolerance tests (ETTs) using Bruce's protocol. During the 3- to 4-week single-blind placebo baseline phase, all other drugs except sublingual nitroglycerin and long-acting nitrates were withdrawn. Those patients (n = 115) whose time to onset of moderate angina was between 2.5 and 7.5 min and was within +/- 15% in 2 consecutive ETTs were randomized to betaxolol 20 mg/day (n = 54) or placebo (n = 53). Betaxolol, compared to placebo, increased time to onset of angina, time to 1 mm S-T segment depression, and total exercise time and decreased the double product, weekly anginal attacks, and sublingual nitroglycerin consumption (p < 0.01). Our results indicate that betaxolol given in fixed 20-mg daily doses was efficacious in stable angina pectoris and its combination with long-acting nitrates potentiated its effect.
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PMID:Betaxolol in the treatment of stable angina pectoris. 818 19

Although beta-blockers can not be used for the treatment of vasospastic angina, the effect of beta-blockers with vasorelaxant property on coronary vasospasm remains uncertain. In this study, we evaluated the effect of betaxolol, a new beta-blocker with calcium antagonistic property, as an additional therapy on vasospastic angina (VSA) with anginal attacks on effort. We enrolled 12 patients with VSA and anginal attacks with ST segment depression during exercise stress test. All patients received 1.25-5 mg of betaxolol for 3 months. Treadmill exercise stress test and adenosine triphosphate stress thallium-201 myocardial scintigraphy were performed before and 3 months after the onset of the betaxolol treatment. The other drugs including calcium antagonists, nitrates and nicorandil were continued. No patients experienced the exacerbation of angina during the betaxolol treatment. Exercise time to chest pain (317.5+/-72.1-454.2+/-75.5 s, P<0.01) and maximal ST segment depression (1.67+/-0.67-1.16+/-0.46 mm, P<0.01) obtained by exercise stress test, the defect score (8.6+/-2.7-5.3+/-2.1, P<0.01), the extent score (14.8+/-5.8-8.8+/-4.6%, P<0.01), the severity score (17.5+/-7.3-11.3+/-5.2, P<0.01) and washout rate (31.4+/-5.6-37.6+/-5.0%, P<0.01) obtained by the scintigraphy were improved by betaxolol. Our results suggest that betaxolol increases regional myocardial blood flow and improves exercise capacity in patients with VSA. Betaxolol may become a drug for a new potential therapy for VSA.
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PMID:Beneficial effects of betaxolol, a selective antagonist of beta-1 adrenoceptors, on exercise-induced myocardial ischemia in patients with coronary vasospasm. 1455 35