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At least 19 recordsLinked to original sources
PubMed1992

Metipranolol-induced adverse reactions: II. Loss of intraocular pressure control.

This paper reviews the behaviour of intraocular pressure (IOP) in glaucomatous eyes treated with metipranolol with and without drug-induced adverse reactions (ADRs). Two hundred and forty seven patients with open angle glaucoma who were receiving the three different strengths of metipranolol (0.1%, 0.3%, and 0.6%) in our Department and the 7 patients who participated in the metipranolol rechallenge trial were included in this study. Out of the 247 patients, there were 52 eyes of 29 patients who showed 78 episodes of ADRs associated with metipranolol. Forty five of these 78 episodes (57.6%) were associated with loss of IOP control. Two of the 7 eyes treated with metipranolol in the rechallenge trial showed loss of IOP control, 1 of them without any signs of ocular inflammation. We further studied all the glaucomatous eyes controlled with metipranolol 0.6% only and 22 eyes were identified with loss of IOP control but without recognisable signs or symptoms of ADR. Five other eyes in this group later developed metipranolol-induced ADRs. The possible pathophysiological mechanisms for the loss of IOP control are discussed and it is suggested that the active drug, metipranolol, could be directly implicated.

Eye Diseases↗
PubMed1992

[Are metipranolol eyedrops responsible for intraocular side effects?].

Metipranolol is a beta-blocker that has been used in ophthalmology and in systemic therapy for about 10 years. Reports about reversible uveitis under the product Glauline (metipranolol-containing eye drops) in England were the reason for extensive studies with metipranolol-containing eye drops produced with different methods. Analytical studies concerning the influence of irradiation sterilization on the drug containers, studies on the toxicity of the ophthalmic drug on tissue cultures, and prospective and retrospective clinical studies on 2,800 glaucoma patients were performed. Irradiation sterilization leads to the formation of free radicals on the surface of the containers and, depending on the radiation dose, to a decrease in the pH of the drug solution. In prospective studies involving 1,516 glaucoma patients, no intraocular side effects due to metipranolol-containing eye drops were found. In the retrospective examination including 1,306 glaucoma patients, 19 cases of uveitis were found. Thirteen cases of recurring iritis were diagnosed, which had already been observed before the onset of glaucoma therapy. In 2 cases the iritis led to secondary glaucoma and was treated with metipranolol. In 2 cases glaucoma was treated with pilocarpine (and dipivefrin) and metipranolol concomitantly. One case of rubeosis iridis was incorrectly classified as iritis. One case is possibly related to metipranolol despite the assessment to the contrary by the ophthalmologist in question. Following the results of these studies, an accumulation of cases of uveitis caused by metipranolol can be excluded.

Adolescent↗
PubMed1992

Metipranolol-induced adverse reactions: I. The rechallenge study.

Previously unreported adverse drug reactions can be difficult to detect and it may be even more difficult to establish a cause and effect relationship, particularly if the adverse reactions mimic naturally occurring disease. In a previous paper we reported 29 patients with granulomatous anterior uveitis, blepharoconjunctivitis, periorbital dermatitis, marginal keratitis and elevation in intraocular pressure (IOP), suspected to be caused by metipranolol (Glauline). With the approval of the District Ethics Committee 7 of those patients were rechallenged with metipranolol 0.3% compared to timolol maleate 0.5% in a double blind trial. The 7 metipranolol treated eyes developed an adverse reaction within 14 days. Metipranolol (Glauline) has been conclusively proven to cause granulomatous anterior uveitis, blepharoconjunctivitis and elevation in IOP, adverse effects never previously reported with any of the ophthalmic topical beta-blockers. The multidose preparations of metipranolol (Glauline) in all three strengths 0.1%, 0.3% and 0.6% and the single dose minim preparation of metipranolol 0.6% have now been withdrawn from clinical use in the United Kingdom.

Aged↗
PubMed1977

Experiments in animals on the pharmacological effects of metipranolol in comparison with propranolol and pindolol.

The beta-blocking agent 1-(4-acetoxy-2,3,5-trimethylphenyloxy)-3-isopropylamino-propan-2-ol (metipranolol) was compared with propranolol and pindolol. The beta-blocking activity on isoproterenol induced tachycardia was determined in rabbits (ED250bpm). The following doses in microgram/kg i.v. were required to produce the same inhibition: 410 propranolol; 160 metipranolol; 130 pindolol. When intrinsic sympathomimetic activity was determined in reserpinized rats metipranolol was found to produce less than 10% of the increase in heart rate induced by a standard isoproterenol dose (1 mg/kg i.p.), whereas propranolol caused less than 20% and pindolol ca. 60%. The membrane stabilising activity, determined by the elevation of the fibrillation threshold (ED delta100muA) in rabbit hearts, was found to be greatest with propranolol (0.98 mg/kg i.v.) and least with metipranolol (1.68 mg/kg), with pindolol occupying an intermediate position (1.10 mg/kg). The cardioprotective action to hypoxia stress of metipranolol in rats was found to be the best, requiring a dose of only 5 microgram/kg i.p. compared with values of 28 microgram/kg for pindolol and 250 microgram/kg for propranolol. These results show that metipranolol has a high beta-sympatholytic activity which is not accompanied by either marked intrinsic activity or membrane-stabilising properties. The relatively marked cardioprotective action, which is probably due to a metabolic action, is particularly noteworthy.

Adrenergic beta-Antagonists↗
PubMed1992

Analysis of ultrastructural changes in the myocardium of rats during withdrawal syndrome after gradual decreasing of metipranolol doses.

Hypersensitization of the myocardium occurring in rats after remission of metipranolol's beta-blocking effect in experiments manifested itself by marked proliferation of the mitochondrial apparatus of myocytes accompanied by an increase in SDH activity as well as its ultrastructural pattern return to control values after a shorter period of A characteristic feature of the withdrawal syndrome occurring in the myocardium of rats exposed to stress following discontinuation of premedication with metipranolol, is partial damage to the mitochondrial apparatus of myocytes associated with a decrease in SDH activity and presence of hyperactive nuclei. Based on the results obtained, the author concludes that, while the withdrawal syndrome sets in during gradual decrease in long-term metipranolol doses in the rat myocardium on stress, it lasts shorter than after sudden interruption of treatment, and myocardial metabolism as well as its ultrastructural pattern return to control values after a shorter period of time.

Animals↗
PubMed1979

[The effect of metipranolol on the carbohydrate metabolism in diabetics treated with glibenclamide (author's transl)].

Previous investigations on the effect of beta-receptor blockers on the carbohydrate metabolism of diabetics have reported varying effects, the most frequent being hypoglycaemic symptoms which were interpreted as potentiating effects caused by interference with the antidiabetic agents. For this reason, the effect of the beta-receptor blocker metipranolol on the carbohydrate metabolism of diabetics treated with glibenclamide was investigated in a double blind cross-over study comparing metipranolol with placebo. The results do not show any significant difference between the placebo and the metipranolol with respect to the blood or urinary sugar values or the plasma insulin levels. Whether or not this is a substance-specific property needs to be clarified by further comparative investigations using other beta-receptor blockers. There were similarly no significant differences in the most important parameters of hepatic and renal function.

Adult↗
PubMed1979

Effects of beta-blocking agent Metipranolol on metabolic variables in patients with ischemic heart disease, hyperkinetic syndrome, hyperthyreosis and in healthy subjects.

Metabolic effects of Metipranolol, a new beta adrenergic blocking agent, have been studied in patients with ischemic heart disease, hyperkinetic syndrome, hyperthyreosis and in healthy subjects. Administration of the drug (30 mg per day for one week) resulted in the decrease of noradrenaline excretion, blood free fatty acid level, and in lowering of blood pressure and heart rate, particularly in patients with ischemic heart disease and hyperkinetic syndrome. These alterations were accompanied by alleviation of clinical symptoms. It is suggested that Metipranolol by suppressing the activity of sympathetic nervous system and thereby diminishing lypolysis, exerts favourable clinical effects, most probably related to diminution of myocardial oxygen consumption.

Adrenergic beta-Antagonists↗
PubMed1992

Disposition kinetics and concentration-effect relationship of metipranolol in patients with cirrhosis and healthy subjects.

The disposition kinetics and heart rate reducing effect of deacetylmetipranolol (DMP), the active form of the beta-adrenoreceptor blocking agent metipranolol (MP), administered as a single 40 mg oral dose have been compared in 6 patients with cirrhosis and 6 healthy volunteers. The mean maximal DMP concentration was significantly higher and the time to reach the peak level shorter in the patients compared to the healthy subjects. There was also a significantly higher AUC of DMP, a shorter half-life of the rapid phase of the decline in DMP concentrations, a smaller central compartment and lower apparent DMP clearance in patients. A correlation with the albumin level was observed in cirrhotics for individual values of apparent DMP clearance (r = 0.92) and AUC (r = -0.89). The maximal reduction in heart rate was recorded in patients at plasma DMP levels which were already significantly lower than the peak levels. Median inhibitory concentrations (IC50) and maximum possible heart rate reductions (delta HRmax), obtained by fitting individual plots of the plasma DMP concentration-effect relationship to the inhibitory Emax model in the postdistributional phase of DMP disposition were significantly higher in cirrhotics than in healthy subjects. It is conjectured that down-regulation of adrenoreceptors due to chronic sympathetic activation in hepatic cirrhosis contributes to decreased sensitivity to the reduction in heart rate following a single dose of the beta-blocker.

Adult↗
PubMed1992

Reduction of cardiovascular side effects associated with ocular administration of metipranolol by inclusion in polymeric nanocapsules.

A new formulation of metipranolol base for ophthalmic administration was developed consisting of a colloidal suspension of polyepsiloncaprolactone nanocapsules with an oily core (Migliol 840) in which the drug is dissolved. Physicochemical properties of the nanocapsules show that the polymer coating around the oily droplets causes an important reduction of the droplet size, with no significant modification of the surface charge noted. When this formulation was administered to rabbits, a reduction of intraocular pressure similar to that seen with commercial eye drops was observed. Nevertheless, the evaluation of the cardiovascular side effects clearly showed lower conjunctival absorption of the encapsulated drug compared with the commercial drops. The direct (bradycardia) and the indirect evaluation (based on the study of the influence on the hypotensive and positive chronotropic effects of isoprenaline) showed that blockage of beta-adrenoreceptors was reduced greatly by the topical administration of the new formulation.

Animals↗
PubMed1992

[Comparison of the effects of diltiazem and isradipine in adrenergic beta receptor blockade in patients with stable angina pectoris].

In 20 patients with stable angina II-III according to NYHA by means of ergometry the effect of short-term administration of dilthiazem (90 mg in three doses), placebo and isradipine (5 mg in three doses) in block of beta-receptors of the sympathetic nerve (metipranolol 3 x 10 mg/day) was compared. As compared with placebo, dilthiazem and isradipine retarded significantly the development of stenocardia, reduced the S-T depression in lead V5 and increased the total work output during ergometry. Based on the results of this and previous work (9) it may be stated that concurrent administration of metipranolol reduced the frequency of side-effects of isradipine and prevented the reflex rise of the heart rate following its short-terms administration. The authors conclude that starting treatment of stable angina with isradipine is safer and more effective in combination with metipranolol than when monotherapy is used. Dilthiazem must be administered with metipranolol carefully with regard to possible development of severe bradycardia and its suitable dose should be established by titration.

Adult↗
PubMedDate not supplied

Ocular beta-blockers in glaucoma management. Clinical pharmacological aspects.

Topical beta-blockers reduce the intraocular pressure (IOP) by blockade of sympathetic nerve endings in the ciliary epithelium causing a fall in aqueous humour production. Two types of topical beta-blockers are available for use in glaucoma: nonselective, which block both beta 1- and beta 2-adrenoceptors; and cardioselective, which block only beta 1-receptors. Of the beta-Blockers commercially available, timolol, levobunolol, metipranolol and carteolol are nonselective, and betaxolol is cardioselective. Twice-daily timolol is probably the most effective agent in lowering IOP, although levobunolol is equally effective and can be used once daily with little difference in effect. Carteolol is used twice daily and any theoretical advantage in diminished side effects conferred by its partial beta-agonist activity compared with timolol has not been fully substantiated. Metipranolol is effective twice daily and does not have partial beta-agonist activity. Betaxolol has an effect comparable to timolol in lowering IOP, but is less effective in some patients. beta-Blockers can be used with other antiglaucoma medications, but their combined action with epinephrine (adrenaline) is suspect, particularly in the case of the nonselective beta-blockers, and the effect should be assessed in patients on an individual basis. Local stinging can be a problem in some patients with betaxolol. The most serious side effects of beta-blockers are the exacerbation of chronic obstructive airways disease with nonselective agents and the precipitation of bronchospasm in some patients. Betaxolol seems relatively free of adverse respiratory effects, although this may be dose-related and extreme caution should still be exercised in patients with any history of respiratory illness. Because of the lower risk of precipitating side effects, betaxolol is probably the beta-blocker of first choice for use in glaucoma; timolol or levobunolol are reserved for patients who do not respond satisfactorily to betaxolol and are quite free of respiratory disease.

Administration, Topical↗
PubMed1992

On the relationship between the inhibition of thrombin stimulated aggregation and thromboxane formation in isolated platelets treated with beta-adrenoceptor blocking drugs.

Thromboxane B2 (TXB2) formation in isolated, thrombin-stimulated rat platelets was time dependent and appeared after 5 s of incubation. Beta-adrenoceptor blocking (BAB) drugs inhibited thrombin-stimulated TXB2 formation in the following rank order of potency: metipranolol approximately alprenolol approximately propranolol > oxprenolol > practolol. Atenolol was ineffective in inhibiting TXB2 production in stimulated platelets. The inhibition of thrombin-stimulated TXB2 formation by BAB drugs correlated with their inhibitory effect on thrombin-stimulated platelet aggregation, arachidonic acid liberation from membrane phospholipids and with their membrane fluidization. The higher was the liposolubility of the beta-adrenoceptor blocking drugs investigated, the higher was their inhibition of stimulated TXB2 formation. Hydrophilic, selective atenolol and practolol revealed slight or no inhibitory effect on stimulated thromboxane production.

Adrenergic beta-Antagonists↗
PubMed1992

[Self-care in the prevention of sudden cardiac death].

In acute myocardial infarction a third up to half of death registered within the first month occur in the first hour of the onset of attack most frequently because of ventricular fibrillation. Immediate self administration of drugs stabilizing electrically the heart may prevent it. On the basis of experiments in dogs and in rats flunitrazepam (Rohypnol tabl. 1 mg), tramadol (Tramal caps. 50 mg) and the beta blocker metipranolol (Trimepranol tabl. 10 mg) were selected for clinical trial on high risk patients. As the chosen combinations of drugs were not yet tested in view of possible interactions, we studied their effect on circulation and cardiovascular reflexes in eight healthy volunteers. When the drugs were absorbed from the mouth mucosa, the decrease in the heart rate during deep breathing was observed already 15 minutes after the intake of drugs. The subjects started to feel relaxed; later on they had pleasant feelings and felt sleepy. There were no undesirable changes in the heart rate or blood pressure. In the three drug combination with metripranolol, the decrease in the heart rate was more marked. The tests in volunteers were without any undesirable effects and both combinations may, therefore, be given to selected high risk subjects, e g. convalescents from myocardial infarction. Randomized trial to prove the preventive effect already started.

Adult↗
PubMed1979

[Metabolic effects of a fixed combination (betablocker plus saluretic) in long-term treatment of arterial hypertension (author's transl)].

UNLABELLED: In 23 patients with essential hypertension of stage I and II according to the WHO, the effects of a fixed combination of a beta-receptor-blocker plus saluretic composed of 20 mg of metipranolol (Disorat 20) and 2.5 mg of butizid (Saltucin) = Torrat on blood pressure and important metabolic parameters (glucose, glucose tolerance, cholesterol, triglyceride, uric acid, plasma potassium and whole body potassium) were tested over a 6-month treatment period. RESULTS: blood pressure and pulse rate were significantly reduced; bradycardia (pulse rate less than 60/min) was not observed. The metabolic parameters showed no significant changes during the 6-month treatment period. In no case did the therapy have to be discontinued because of undesirable effects. The investigations show that the combination has a good antihypertensive effect with few side-effects and that it has no influence on important metabolic parameters during long-term therapy.

Adult↗
PubMed1992

Involvement of arachidonic acid and its metabolites in the inhibitory effect of beta-adrenoceptor blocking drugs on blood platelets.

Propranolol (PRO), alprenolol (ALP), metipranolol (MET) and oxprenolol (OXP) inhibited arachidonic acid (AA) liberation from membrane phospholipids, malondialdehyde (MDA) formation and thromboxane B2 (TXB2) production in stimulated platelets. The inhibition was dose-dependent and with slight variations followed the rank order of potency: PRO greater than or equal to ALP greater than or equal to MET greater than or equal to OXP. Atenolol (ATE) was without any inhibitory effect. Inhibition of the arachidonic acid pathway in stimulated platelets may significantly contribute to the antiaggregatory effect of beta-adrenoceptor blocking drugs.

Adrenergic beta-Antagonists↗
PubMed1992

[Histologic evaluation of potential new beta-adrenolytics].

The present paper investigated histological changes in the myocardium in two potential beta-adrenolytic agents, 4-[3-isopropylamino-2-hydroxypropoxy]-3-[propoxymethyl]acetophenone and 4-[3-isopropylamino-hydroxypropoxy]-3-[pentyloxymethyl]acetophenon e after intravenous administration in doses of 8 mg/kg and 24 mg/kg. It results from the found data that in both agents in the doses used there are no necrotic changes in the myocardium and the values of the impairment range within the 1st degree of Zbinden's classification, comparable to the standard metipranolol.

Acetophenones↗
PubMedDate not supplied

The effect of beta adrenergic blockade on pulmonary hypertension, right ventricular hypertrophy and polycythaemia, induced in rats by intermittent high altitude hypoxia.

Adult male rats were used to study the effect of a beta blocking agent on pulmonary hypertension and right ventricular hypertrophy induced by intermittent high altitude (IHA) hypoxia (8 hr daily, 5 days a week, stepwise up to the simulated altitude of 7000 m). Trimepranol was injected subcutaneously in a single dose of 10 mg/kg/b.w. one hour before each IHA exposure. Administration of the beta blocking drug caused significant changes of haematocrit values even in animals kept under normoxic conditions. The initial deep decrease was followed by a slow return to control values; prolongation of treatment led to a further significant decrease of the haematocrit curve. The polycythaemic response of IHA-exposed and Trimepranol-treated animals was, therefore, significantly less pronounced as compared with the hypoxic non-treated group. Administration of Trimepranol to IHA-exposed rats significantly decreased the values of right ventricular systolic and mean pressure, right ventricular hypertrophy as well as the degree of muscularization of pulmonary arteries. It may be assumed that the protective effect of Trimepranol is due to a) changes in pulmonary vascularization, b) reduction of polycythaemia, and c) lower cardiac output, induced by the negative inotropic and chronotropic effect of this drug.

Altitude Sickness↗