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At least 145 records · Page 8Linked to original sources
PubMed1982

Influence of labetalol, propranolol and practolol in patients with asthma.

The acute effect of non-selective beta-blockade alone (propranolol) or in combination with alpha-blockade (labetalol) and beta 1-selective blockade (practolol) on the airways was studied in 14 asthmatic patients. Severe bronchoconstriction was not seen in any patient after placebo (saline) or practolol (10 mg i.v.) while pronounced bronchoconstriction was seen in three patients after labetalol (20 mg i.v.) and in six patients after propranolol (5 mg i.v.). The effects of 2 weeks of oral medication with labetalol (200 mg x 2) and placebo were studied in the same patients. Four patients had symptoms of asthma during the labetalol period while none had asthmatic symptoms during the placebo period. The results suggest that coexistent alpha-adrenoceptor blockade fails to prevent asthmatic symptoms caused by beta-blockade.

Adolescent↗
PubMed1983

Evaluation of ocular toxicity of two beta blocking drugs, carteolol and practolol, in beagle dogs.

The ocular effects of two beta blocking drugs, carteolol and practolol, were assessed in beagle dogs. Practolol-treated dogs showed a tear flow reduction: histopathological examination showed lymphocytic infiltration in the lacrymal glands and electroretinogram showed a decrease in the amplitudes of the A + B-wave. By contrast, no drug-related abnormal changes were observed in carteolol-treated dogs. These results were thought to indicate that a tear flow measurement and electroretinogram examination should be used in the evaluation of the safety of beta blocking drugs.

Animals↗
PubMed1981

Peritoneal fibrosis due to practolol. Scanning electron microscopical and histological observations.

Three cases of peritoneal fibrosis induced by the beta adrenoceptor blocking agent practolol are presented. Histological and scanning electron microscopical specimens showed a thick layer of loose connective tissue with collagen bundles and fibroblasts. No evidence of mesothelial cells with characteristic microvilli was found. The conclusion is drawn that the basic feature of practolol peritonitis is the destruction of the mesothelial membrane and a slowly progressive formation of loose connective tissue. The reason for the increased formation of connective tissue and the cause of the excessive activity of fibroblasts are discussed.

Aged↗
PubMed1976

The effects of propranolol, practolol, and placebo on the clinical manifestations of thyrotoxicosis.

Thirty patients with thyrotoxicosis were randomly divided into 3 groups of ten which were treated for 8 weeks with either practolol, propranolol or placebo. The pills were administered in a double blind manner and the investigator had the option of doubling the dose at each visit. Propranolol and practolol were equally effective, and better than placebo, at relieving the patients general well-being as well as the tachycardia, subjective and objective tremor, skin warmness and moistness and the intensity of the thyroid bruit.

Auscultation↗
PubMed1970

Practolol in treatment of supraventricular cardiac dysrhythmias.

Practolol (I.C.I. 50172) was used to treat supraventricular dysrhythmias in 32 patients with a rapid ventricular rate and with heart disease of varied aetiology. In 26 patients the average reduction in ventricular rate was 75 per minute, while immediate reversion to sinus rhythm occurred in three patients. The slowing effect was mainly due to a direct action on the atrioventricular node. The effectiveness of practolol was unrelated to the type of dysrhythmia or its aetiology. No serious adverse clinical effects were noted.

Acetanilides↗
PubMed1978

Antinuclear antibodies in patients receiving non-practolol beta-blockers.

Antinuclear antibodies (ANA) were found in 54 (7.0%) out of 767 treated hypertensive patients compared with 59 (2.4%) out of 2470 healthy controls. Inclusion of a non-practolol beta-blocker in the treatment regimen did not significantly affect the incidence of ANA. ANA was found in significantly more patients being treated with methyldopa (13.0%) than patients receiving other hypotensive agents (3.8%). Non-practolol beta-blockers in combination with methyldopa did not increase the incidence of ANA further.

Adrenergic beta-Antagonists↗
PubMed1970

Practolol in treatment of angina pectoris. A double-blind trial.

Twenty-four patients with angina pectoris entered a double-blind trial of the cardioselective beta-adrenergic blocking agent practolol. Seventeen experienced less angina and consumed fewer glyceryl trinitrate tablets when on the active preparation. There was also a decrease in the mean number of attacks suffered by patients while on practolol and a reduction in the number of glyceryl trinitrate tablets taken. These results are of statistical significance at, at least, the 5% level.

Acetanilides↗
PubMed1977

Sclerosing peritonitis due to practolol: a report on 9 cases and their surgical management.

Nine patients with an unusual and serious intraabdominal complication of the beta-adrenergic blocking agent practolol seen since 1973 are reported. The striking and bizarre peritoneal changes induced by the drug have distinctive features that are not shown by other forms of peritoneal disease. The cases presented with small bowel obstruction, usually chronic in type and often associated with profound weight loss and an abdominal mass. Characteristic radiological features were present. The abnormalities at laparotomy were impressive, with a gross proliferation of the visceral peritoneum which formed a dense white cocoon which encased, constricted and markedly shortened the small bowel, usually from the duodenojejunal flexure to the ileocaecal valve. The obstruction was relieved by mobilizing the small bowel from the ensheathing tissue. Restoration of alimentary function after surgery was delayed but the long term result was satisfactory with full relief of symptoms and the absence of recurrent obstruction during the follow-up period. This complication may arise after treatment with the drug has been stopped, and although long term oral therapy has been discontinued, further cases will almost certainly present for some time to come.

Aged↗
PubMed1977

Effects of furosemide on glomerular filtration rate and clearance of practolol, digoxin, cephaloridine, and gentamicin.

Furosemide was shown to decrease inulin clearance in 20 of 27 normal subjects. The depression in inulin clearance occurred in both water-loaded and non-water-loaded subjects. The renal clearance of practolol, but not digoxin, was reduced when furosemide was given. The average total plasma clearances of gentamicin and of cephaloridine over a 6-hr period were decreased after furosemide. The reduced clearances of the antibiotics were associated with higher plasma levels, the increase in antibiotic concentration being as much as 100% at 1 hr after an intravenous bolus injection.

Adult↗
PubMed1992

Synthesis and binding to beta-adrenergic receptors of p-aminobenzyl analogues of practolol and atenolol.

The p-aminobenzyl analogues (8a and 8b, respectively) of the cardioselective beta-adrenergic receptor antagonists practolol and atenolol were prepared from the corresponding phenoxymethyloxiranes in 30 and 13% yields, respectively. The dissociation constants for the beta-adrenergic receptor were measured in membrane preparations of rat heart and lung. In membranes from the heart (which contain mostly beta 1-adrenergic receptors), the affinities of the derivatives and parent compounds were similar. By contrast, in membranes from the lung (which contain mostly beta 2-adrenergic receptors), the derivatives were more potent than the parent compounds. Thus, the cardioselectivities of the p-aminobenzyl analogues 8a and 8b were about one-sixth those of the respective parents.

Adrenergic beta-Antagonists↗
PubMed1977

Comparative evaluation of intravenous phenytoin, procainamide and practolol in the acute treatment of ventricular arrhythmias.

Ten patients with a persistent ventricular arrhythmia, but no other sign of heart disease, were studied by means of an exercise test performed 4 times with a fixed work load, over 30--40 min. No drug was given in the first exercise test and in the others phenytoin, procainamide or practolol were chosen at random for i.v. administration. Blood samples for determination of plasma concentration were frequently collected. The ECG was recorded continuously during the exercise test and was analysed minute by minute. Despite plasma levels within the suggested therapeutic range, only procainamide showed a statistically significant antiarrhythmic effect in this group of patients.

Adult↗
PubMed1987

In vitro pharmacologic activity of congener derivatives and model conjugates of propranolol and practolol.

Previous studies in our laboratory suggested that synthetized derivatives of isoproterenol and histamine could create agonists more potent and receptor and/or tissue selective than the parent compound. In the present study we have evaluated the hypothesis that our results with isoproterenol and histamine derivatives could be extended to include beta-adrenergic antagonists. With this purpose in mind, fourteen derivatives of propranolol and practolol were synthesized and tested in four in vitro systems. The congeners and conjugates were tested using biologic assays (blocking of cAMP accumulation) and/or radioligand binding assays in S-49 lymphoma cells and in rat adipocytes, heart and lung which contain beta 1 and/or beta 2 receptors. Our results indicate that structural modifications distant from the pharmacophore alter the pharmacologic profile of the parent compound. The relative potencies of the derivatives were dependent upon several key factors including the length of the methylene spacer chain and the nature of the substituents on the aromatic ring. The presence of a spacer group with four methylenes resulted in the most active compound in each series when tested on S-49 cells. The derivatives with a paramethyl toluidide group were more potent than the derivatives with a trifluoromethyl toluidide group. The dipeptide derivatives were more potent on adipocyte than S-49 cells, suggesting a preference for beta 1 receptors. Some of the same modifications that led to altered potency and which resulted in an increased receptor and/or tissue selectivity using the progenitors isoproterenol or histamine did extrapolate to the beta blockers. Our data suggest that alterations in receptor and/or tissue selectivity must be imparted by the carrier moiety of the drug and may be related to the biochemical microenvironment of the receptors.

Adipose Tissue↗
PubMed1986

Synthesis and biodistribution of 125I labeled bivalent analogs of practolol as potential myocardial imaging agents.

Iodinated bivalent ligands 3 and 4 and a monovalent ligand 5 were prepared from the cardioselective beta-antagonist, practolol. 125I-labeled 3, 4 and 5 were prepared by solid phase isotopic exchange reaction with carrier-free Na125I and examined in rats as potential receptor-site-directed myocardial imaging agents. Biodistribution of these agents in rats indicated that 125I-3 and 125I-4 were localized in the heart similarly to 125I-5 and the [125I]iodobenzoyl (6) that was previously reported. Localization of 125I-3 and 125I-4, was more persistent in the heart than that of 125I-monovalent ligands 5 and 6. Heart-to-blood ratios of 125I-3 and 125I-4 were significantly lower than those of 125I-5 and 125I-6, due mainly to slow blood clearance rates of 125I-3 and 125I-4.

Animals↗
PubMed1977

Allergic drug reactions: an in vitro model using a mixed function oxidase complex to demonstrate antibodies with specificity for a practolol metabolite.

Reactive metabolite products of the drug practolol were generated in vitro using the rat liver mixed function oxidase complex. The metabolites were spontaneously coupled to a non-agglutinating rabbit antibody to human O red blood cells, so forming a metabolite-antibody reagent. This reagent was then used to passively sensitize human O red cells which subsequently acted as indicator cells for detecting anti-metabolite antibodies.

Animals↗
PubMed1975

The uterine and cardiovascular effects of salbutamol and practolol during labour.

Intravenous salbutamol, a beta-adrenoceptor stimulant, given to nine patients in normal labour, with continous monitoring of uterine activity and of the maternal and fetal cardiovascular systems, was shown to decrease uterine activity significantly; maternal and fetal heart rates were significantly increased, and maternal systolic and diastolic arterial pressures were significantly decreased during the infusion, although no treatment had to be discontinued because of these effects. Apart from worsening of low back pain during the infusion in one patients, subjective side-effects were trival. With the salbutamol infusion continued at an effective maintenance rate, the carioselective beta-adrenoceptor blocking drug, practolol, given intravenously, reduced the maternal heart rate (although not significantly) but it did not alter the fetal heart rate; it also appeared to interfere transiently with the inhibiting action of salbutamol on uterine activity, but cerevical dilatation was arrested until the salbutamol infusion was discontinued. At least in five patients, labour remained suppressed until oxytoxin was infused intravenously.

Albuterol↗