Betablocking drugs in essential hypertension: transdermal bupranolol compared with oral metoprolol.

In the present study the antihypertensive efficacy and tolerability of transdermal bupranolol (30 mg once-daily) was compared with oral metoprolol (100 mg once-daily). Blood pressure measurements were performed in the office, at home, and with ambulatory 24-h blood pressure devices. Systemic and local side-effects, as well as compliance and acceptance, were evaluated every two weeks. The treatment period lasted eight weeks. The results showed a significant decrease in blood pressure under the bupranolol transdermal therapeutic system in the office, at home, and with 24-h blood pressure measurements day- (08h00-20h00) and night-time (20h00-08h00). Under oral metoprolol there was a significant blood pressure decrease in the office, at home, and in the mean daytime values of the 24-h blood pressure measurements. The night-time values, however, demonstrated only a slight decrease in blood pressure, being significant only for diastolic values. Systemic side-effects were comparable in both groups. 69% of the patients had local side-effects at the patch side (erythema, papulous exanthema, pruritus). Six patients dropped out because of localized urticarial exanthema (five patients treated with transdermal bupranolol, one patient treated with oral metoprolol). In comparison to the oral form, twice as many patients had admitted to have been non-compliant with the patches (13 versus 7 patients). At the end of the study, 24 out of 32 patients preferred to be treated with capsules.

[Local anesthetic effect and subjective tolerance of a single dose of 0.25% bupranolol in probands with healthy eyes. Randomized parallel double-blind study]. / Lokalanästhetische Wirkung und subjektive Verträglichkeit einer Einzeldosis Bupranolol 0.25% bei Augengesunden. Randomisierte parallele Doppelblindstudie.

.25% Bupranolol in an oily solution decreases corneal sensitivity statistically significant from the 3. to the 15. minute after the application. The maximum of decrease is found between the 6. and the 15. minute in contrast to beta-blockers in aqueous solution (1.-3. minute). The topical subjective compatibility of 0.25% Bupranolol equals that of preserved 0.5% Timolol.

Evaluation of the antianginal and anti-ischemic efficacy of slow-release isosorbide-5-mononitrate capsules, bupranolol and their combination, in patients with chronic stable angina pectoris.

The effects of slow-release isosorbide-5-mononitrate (IS-5-MN), 25 mg once daily, bupranolol, 50 mg once daily, and their combination on exercise-induced ST-segment depression at comparable work load, maximal work load, exercise capacity, frequency of anginal episodes and sublingual nitroglycerin consumption were studied in 30 patients with chronic stable angina pectoris. The patients were assigned in a randomized, double blind protocol, to either form of monotherapy, for 12 days, and thereafter to combined therapy for 12 days. Exercise stress test was performed before treatment and at 2 and 16 h after drug administration on the first and 12th day of each treatment period. ST-depression at comparative work load at 2 h after dosing was reduced by 49% acutely after administration of IS-5-MN. This effect was not significantly altered after 12 days of treatment and during combined therapy. In those patients treated by bupranolol alone, an effect was observed only after 12 days - a 24% reduction in ST depression. At the 12th day of combined therapy ST-segment depression was reduced by 65%. At 16 h after dosing there was no significant reduction in mean values of ST-segment depression in either groups, but some patients in each group showed a sustained effect for 16 h. Both drugs increased maximal work load and exercise capacity at 2 h after administration. This effect was sustained in the IS-5-MN group also at 16 h after administration.(ABSTRACT TRUNCATED AT 250 WORDS)

Bupranolol, a beta 1- and beta 2-blocker, causes constriction of the pupil in men.

Two out of three normal eyes tested with frequent instillation of 30 microliters of drops of 0.5% bupranolol, a beta 1 + beta 2 blocking drug with some intrinsic sympathomimetic and local anesthetic activity, showed a miotic effect of the order of a 25% reduction of pupil area, as estimated by an open-loop iris-videorecorder. A slight contralateral effect was also observed. Blocking by the drug of tonic inhibitory beta-adrenergic activity on the sphincter muscle of the pupil is postulated.

[Betamed in the treatment of psychogenic disorders with a somatic component]. / Betamed in der Behandlung psychogener Störungen mit Somatisierungstendenz.

52 patients with acute neurotic anxious and psychosomatic syndromes or chronic anxious and vegetative neuroses were treated orally with the combination drug Betamed (1 tablet contain 60 mg bupranolol and 2.5 mg diazepam). The optimum daily dosage are 2 to 3 tablets; duration of treatment ranged from 2 to 12 weeks. The most responsive target symptoms are psychogenic disorders of the cardiovascular system, anxiety and insomnia, while no antidepressive effect was observed. Clinical improvement is often observed 2 to 3 weeks after the onset of treatment, and dosage reduction is possible frequently. Rarely observed side effects are minimal and mainly occur within one week after onset of treatment. Controls performed 2 to 4 weeks after discontinuation of treatment revealed reactivation of symptoms only in some patients with chronic anxiety and vegetative syndromes. In addition to the easy application and excellent tolerance of the combination drug emphasis is given on the minimal danger of drug dependence.