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Query: UMLS:C0020538 (hypertension)
 170,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Betaxolol is a cardioselective beta-adrenergic antagonist effective in the treatment of hypertension. The pharmacokinetic behavior of betaxolol enantiomers in healthy male subjects is reported. Betaxolol enantiomer concentrations were determined in samples collected up to 48 h after iv administration of a 10-mg dose over a 30-min period by constant-rate infusion in 12 subjects and after oral administration of 40-mg capsules to eight of the same subjects. Betaxolol extracted from whole blood was reacted with (+) or (-)-1-naphthylethyl isocyanate. The resulting diastereoisomeric derivatives were analyzed by reversed-phase HPLC with fluorimetric detection. Following the iv dose, there were no differences in clearance or volume of distribution for the two enantiomers (15.6 +/- 4.4 versus 16.4 +/- 4.1 L/h and 342 +/- 62 versus 340 +/- 65 L, respectively). Likewise, after the oral dose, there were no differences in the maximum concentration, time of maximum concentration, bioavailability, or apparent absorption rate constant (41.0 +/- 8.6 versus 42.0 +/- 7.0 ng/mL, 214 +/- 59 versus 215 +/- 56 min, 0.89 +/- 0.26 versus 0.94 +/- 0.23, and 1.0 +/- 0.6 versus 1.2 +/- 0.6 h-1, respectively). Thus, the pharmacokinetic behavior of racemic betaxolol accurately reflects the behavior of betaxolol enantiomers in this subject group.
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PMID:Human pharmacokinetics of betaxolol enantiomers. 186 31

Effects of betaxolol, a cardioselective beta-adrenoceptor antagonist, on blood pressure and hypertensive complications in stroke-prone spontaneously hypertensive rats (SHRSP) were investigated. Betaxolol was provided in a dose of 33 +/- 1.8 mg/kg/day, orally in drinking water, throughout the experimental period. The chronic treatment with betaxolol inhibited the development of hypertension in SHRSP and reduced values of blood urea nitrogen, creatinine, total cholesterol, free cholesterol, triglyceride, phospholipid and HDL-cholesterol in serum. Treatment with betaxolol apparently inhibited the incidence of hypertensive lesions such as cardiac fibrosis, mesenteric vasculitis, proliferative and/or necrotic vasculitis and glomeruli showing collapse or vasculitis in the kidneys. To shorten the time before the onset of hypertension and the subsequent stroke, SHRSP were kept on a SP diet containing 0.39% Na instead of the F-2 diet. When the SHRSP were kept on the SP diet, all of the control SHRSP had cerebral apoplexy and severe hypertensive lesions in the heart and kidney. When betaxolol was chronically administered to SHRSP, cerebral apoplexy and hypertensive lesions in the heart and kidney were inhibited, but the effect on blood pressure was slight. Treatment with betaxolol reduced serum creatinine levels. Our observations show that betaxolol reduces blood pressure and potently inhibits hypertensive complications in SHRSP.
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PMID:[Antihypertensive effects of betaxolol, a cardioselective beta-adrenoceptor antagonist, in stroke-prone spontaneously hypertensive rats (SHRSP)]. 197 70

A large french multicenter study has been conducted by 750 ophthalmologists with 5,872 patients with open angle chronic glaucoma or intraocular hypertension. The patients were treated twice a day for a period of six months with Betaxolol eye drops, a Beta-1 betablocker product, and cardioselective. Concerning the total population of patients, 35% had a cardiovascular systemic context, 12.1% had a pulmonary systemic context, 5.2% were diabetic patients. Efficacy, systemic tolerance, visual comfort have been evaluated during the study, for each group of patient. After six months of treatment, intra-ocular pressure of the 5,872 patients has been lowered from 22.61 mmHg to 18.25 mmHg. Patients have reported a global efficacy in 97% of cases, a good systemic tolerance in 91% of the cases. The investigations have reported a global efficacy in 96% of cases and a good systemic tolerance in 91%. Ocular comfort has been reported as acceptable by 89% patients and by 92% of the Investigators. The analysis of the results of the study allows us to say that the Beta-blocker-Beta-1 selective eye drop, can be used in treatment of intraocular hypertension or open angle chronic glaucoma with a high range of efficacy and safety.
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PMID:[Epidemiologic and tonometric results of a multicenter study of 5,872 patients with ocular hypertension or open-angle glaucoma treated with betaxolol]. 226 81

Betaxolol is a relatively cardioselective beta-adrenoceptor blocking drug, with no partial agonist (intrinsic sympathomimetic) activity and weak membrane-stabilising (local anaesthetic) activity. Its pharmacokinetic properties of most interest include high bioavailability after oral administration, and a long elimination half-life. It has a narrow dose-response range, which obviates the need for dose titration, with 10 to 20 mg once daily being the usual dosage. This dose reduces systolic and diastolic blood pressures by about 15 mm Hg in most patients with mild to moderate hypertension. In a few comparative studies betaxolol 20 mg daily was as effective as atenolol and moderate doses of propranolol, and more effective than acebutolol, in reducing blood pressure in such patients. Betaxolol has been well tolerated in most patients. Thus, betaxolol is an effective alternative to other beta-blocking drugs in patients with essential hypertension, with properties that may offer advantages in some patients.
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PMID:Betaxolol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension. 286 47

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

Assumption of upright posture is known to be associated with significant variations in renal function, which are thought to be mediated through the stimulation of the renin angiotensin system. The effect of an eight-week treatment with betaxolol, a selective beta-blocker, was studied in patients with moderate hypertension and normal renal function. Betaxolol induced the expected changes in systemic hemodynamics and reduced supine plasma renin activity and aldosteronemia. The glomerular filtration rate showed no variation but the tubular reabsorption of sodium increased. The renal adaptation to postural changes (decrease in glomerular filtration rate, increase in sodium reabsorption and in plasma renin activity) was unaffected by treatment. It is concluded that betaxolol does not impair the renal response to a physiological stimulus such as change in posture.
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PMID:Influence of treatment by betaxolol on the renal response to postural changes in moderate hypertension. 341 May 95

Betaxolol, a beta selective adrenoceptor antagonist recently approved for the treatment of hypertension, was determined by monitoring in chemical ionization mode with ammonia the [MH]+ ions of the trimethylsilyl derivatives of the drug and of its internal standard [2H5)betaxolol). Its pharmacokinetic profile obtained following administration of a 20 mg oral dose was characterized by a half-life of 22 h and a bioavailability of 85%. The main acid metabolite formed by elimination of the isopropylamino group may also be determined as the methyl TMS derivative but methylation with BF3-methanol should be used with caution since it may induce the opening of the cyclopropyl group. The routine electron capture determination procedure was compared to this mass spectrometric method and an excellent correlation was found (r = 0.9974). Both procedures have the same sensitivity (1 ng ml-1). Finally it was observed that under electron impact mode betaxolol trimethylsilyl side chain rearranged to lose TMS-O-CH=CH2; this elimination was confirmed by deuterium labelling studies.
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PMID:Determination of betaxolol, a new beta-blocker, by gas chromatography mass spectrometry: application to pharmacokinetic studies. 614 35

Betaxolol is a cardioselective beta-blocker, which has a bioavailability of 90% and a T 1/2 of 20 h. A four group, cross-over double-blind trial was conducted to select between betaxolol 20 mg and 40 mg for long term trials. 60 patients were allocated randomly to one of the sequences placebo-20 mg, 20 mg-placebo, placebo-40 mg and 40 mg-placebo, each treatment lasting for 2 weeks. Groups were homogenous for baseline diastolic blood pressure (DBP), age and male/female ratio, and were slightly unbalanced for weight. A two-way ANOVA (3 treatments, 2 sequences) showed no treatment-sequence interaction nor sequence effect. The mean reduction in DBP was 14.2 +/- 1.8 mm Hg following 20 mg and 18.0 +/- 1.8 following 40 mg betaxolol, and 4.0 +/- 1.2 mm Hg during placebo (p less than 0.001). Age, weight, baseline DBP and duration of hypertension did not influence the treatment effect. The 95% confidence intervals of the reduction in DBP were 10.4 - 17.9 for 20 mg and 14.3 - 21.6 mm Hg for betaxolol 40 mg. Aiming at a mean reduction to 90 mm Hg, betaxolol 20 mg would appear to be adequate in similar patient populations.
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PMID:Comparison of two doses of betaxolol and placebo in hypertension: a randomized, double-blind cross-over trial. 676 Nov 36

All available beta-blockers are effective in the treatment of high blood pressure. Differences in the pharmacokinetics are important as they can have an impact on their clinical use. Betaxolol, a beta-1-selective blocker has a long biological half-life which can control the blood pressure and pulse rate for 24 hours. The authors investigated 20 patients with mild and medium severe hypertension by out-patient monitoring of the blood pressure. Treatment was focused on influencing the morning rise of blood pressure and pulse rate. The results confirm the effectiveness of betaxolol (Lokren) in the administered dose of 10-20 mg once per day. A favourable response was obtained in 75% when checked by a sphygmomanometer. The morning readings of blood pressure at 5, 6 and 7 o'clock following treatment did not exceed 90 mmHg diastolic pressure. It was also found that there is a statistically significant difference in the effect exerted on pressure and pulse rate in daytime, while the difference at nighttime is not significant. This mild reduction on blood pressure and pulse rate during the night is an advantage in particular in elderly patients. Lokren treatment did not have any serious side-effects it did not affect laboratory values or ECG with the exception of the pulse rate.
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PMID:[Betaxolol hydrochloride in the treatment of mild and medium hypertension--long-term effects]. 748 51

The objective of this study was to assess the medium-term effects of betaxolol, a long-acting, lipid-soluble, cardioselective, beta-adrenergic antagonist, alone and in combination with nitrendipine on blood pressure (BP) and metabolism of lipid, lipoprotein and apolipoprotein in patients with mild to moderate hypertension. Forty-seven patients (21 men, 26 women, average age 54 years) participated in an open controlled clinical trial. After a 4-week washout period, all of the patients received betaxolol monotherapy at a dose of 5-10 mg daily for 6 months (Phase I). From month 7 through month 12 (Phase II), half of the total patients (Group B, n = 23) with diastolic blood pressure (DBP) of 95 mm Hg or more at the end of Phase I were also given nitrendipine (10-20 mg, once daily), while the remaining patients (Group A, n = 24) continued to receive only betaxolol. Systolic blood pressure (SBP), DBP, and heart rate (HR) were monitored once monthly. Serum lipid profiles were measured at study entry and after 6 and 12 months of therapy. Betaxolol significantly reduced SBP, DBP, and HR in both groups during Phase I, and the reductions in SBP and DBP were markedly less in Group B than in Group A. During Phase II, the additional reduction of SBP and DBP to levels similar to those in Group A was achieved by betaxolol in combination with nitrendipine, and HR was slightly but significantly increased. Betaxolol monotherapy reduced serum levels of high density lipoprotein cholesterol (HDL-C) and increased levels of triglyceride, apolipoprotein (apo) C-II and apo C-III. Combination therapy with betaxolol and nitrendipine increased serum apo A-I but did not affect other lipid profiles. Our results indicate that betaxolol is an effective antihypertensive drug which has a preferable effect on HR and HDL profiles when combined with nitrendipine.
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PMID:Medium-term effects of betaxolol monotherapy and combination therapy with nitrendipine on lipoprotein and apolipoprotein metabolism in patients with mild to moderate essential hypertension. 873 59


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