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PubMed1975

[Pharmacology of acebutolol in animals].

In the course of routine screening of beta-adrenoceptor blocking compounds, it was found that a number of compounds did not block the vascular and cardiac effects of isoprenaline in proportion. Moreover, it was also found that the anti-arrhythmic action was not wholly related to the beta-adrenoceptor blocking potency. In particular, the anti-ouabain arrhythmia properties were not dependent upon beta-blocking potency. It was, therefore, possible to select a compound which had both cardioselective beta-adrenoceptor blocking and anti-ouabain arrhythmic activities. The chosen compound was acebutolol. Acebutolol is a cardioselective beta-adrenoceptor blocking agent which has marked anti-arrhythmic against arrhythmia induced by methylchloroform and adrenalin in the cat, and also arrhythmia induced by ouabain in dogs and rabbits. It has less pronounced membrane stabilising properties than propranolol and has no demonstrable sympathomimetic action in normal anaesthetised cats or dogs. Bronchial beta-adrenoceptor blockade has been investigated in anaesthetised cats in which bronchoconstriction is evoked by PGF2 alpha. Isoprenaline prevents the effect of PGF2 alpha and this is restored by pre-treatment with propranolol. Acebutolol is 100 times less active than propranolol in these experiments.

Acebutolol↗
PubMed1975

Changes in myocardial collagen in normal development and after beta blockade.

During development the total mass of collagen increases to the same degree in each ventricle independently of the mass of muscle. At birth the concentration of collagen is the same in each ventricle. Thereafter a greater quantity of muscle is developed in the left ventricle than in the right ventricle, so that the concentration of collagen in the right ventricle comes to exceed that in the left. In the mature rabbit the concentration of collagen is higher in the atria than in the ventricles, higher in the right ventricle than in the left ventricle, and higher in the epicardium than in the endocardium. Beta blockade has no effect on the content of myocardial collagen.

Aging↗
PubMed1975

[The nature of differences in beta-adrenergic receptors].

Results of investigation of the affinity between teranol (practalol), alpheprol (alprenolol), propranolol to beta-adrenoreceptors of various organs confirmed the division of these receptors into two subtypes. The action of isadrin on beta1-adrenoreceptors of the myocardium and smooth muscles of the gastrointestinal tract was accompanied by changes in Ca2+ entrance into the cells. With the action of isadrin on beta2-adrenoreceptors of the trachea and the vessels there was seen an intensification of the Ca2+ ions from the cells and a reduction of the smooth muscle tone.

Alprenolol↗
PubMed1975

Sjogren's syndrome and drug reaction to practalol.

A case is reported of a patient who developed exfoliative dermatitis while being treated with practalol for angina pectoris. The patient also had trigeminal neuropathy, renal impairment and keratoconjunctivitis sicca. The antinuclear factor was diffusely positive but other antibodies were negative. At post mortem the patient was found to have acute pancreatitis, and peritonitis. It is postulated that the patient has antecedent Sjogren's syndrome and on introduction of practalol therapy developed a drug reaction with a generalised exfoliative dermatitis and exacerbation of keratoconjunctivitis sicca leading to bilateral corneal ulceration. The association of similar conditions in patients receiving practalol therapy is reviewed.

Aged↗
PubMed1976

[Effect of beta-adrenergic blockers on complement].

The authors, examined the effect of beta-adrenergic blockers Propranolol, Pindolol, Practonol and P11 on complement in the serum of guinea pigs after continuous administration. The follow-up was made dynamicaly: on the 10th, 20th and 30th day. There was a considerable lowering of the complement level on the 20th and 30th day in all animals treated with beta-adrenergic blockers. The experiments in vitro showed that the effect of Propranolol and and P11 on the serum of persons, guinea pigs and rabbits presented data on the complement inhibition, having the direct effect on the first component of the complementary systems.

Adrenergic beta-Antagonists↗

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