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Biomedical subjects

L A Salako

Publications and source records attributed to L A Salako.

15 recordsLinked to original sources

beta-Adrenoceptor blocking effects and pharmacokinetics of pindolol. A study in hypertensive Africans.

The beta-adrenoceptor blocking effects of pindolol were compared with those of a placebo in a double-blind trial in twelve hypertensive Africans. Heart rate and arterial blood pressure were measured at rest and immediately after exercise, before and at intervals up to 8 h after oral administration of the drugs. Plasma levels of pindolol were also determined. Pindolol reduced systolic blood pressure and antagonised exercised-induced tachycardia. The mean time to peak level of pindolol was 1.9 h and the mean half-life was 4.2 h. Comparison of plasma levels of pindolol and beta-adrenoceptor blocking activity showed good correlation between them. It is concluded that the pharmacokinetics and beta-blocking effects of pindolol in Africans are not dissimilar from published data for other races.

Adrenergic beta-Antagonists

Pharmacokinetics of pindolol in Africans.

The pharmacokinetics of pindolol were determined in 12 hypertensive African subjects after a single oral dose of the drug. The estimated pharmacokinetic parameters do not differ significantly in Africans from the values which have been obtained in other races.

Africa

Comparative beta-adrenoreceptor-blocking effects and pharmacokinetics or propranolol and pindolol in hypertensive Africans.

1. The beta-adrenoreceptor-blocking effects of pindolol were compared with those of propranolol and a placebo in a double-blind cross-over trial involving nine hypertensive African patients. 2. Heart rate, systolic blood pressure and diastolic blood pressure were measured at rest and immediately after exercise before and at intervals up to 6 h after oral administration of the drugs. In addition, plasma pindolol and propranolol concentrations were determined at the same intervals. 3. Pindolol diminished systolic blood pressure at rest and after exercise and antagonized exercise-induced tachycardia, but had no effect on resting heart rate. Propranolol diminished systolic blood pressure predominantly after exercise and reduced both resting and exercise heart rate. Both drugs had no effect on diastolic pressure. 4. The mean plasma concentration reached a peak at 2 h for each drug and this coincide with the interval at which maximal beta-adrenoreceptor-blocking effect was observed.

Adult

Abnormal cation composition and transport in erythrocytes from hypertensive patients.

Red cell sodium and potassium were determined in 100 untreated subjects with uncomplicated essential hypertension and compared with the values from 908 healthy normotensive control subjects. Red cell sodium concentration (expressed as mmol/l of erythrocytes) was significantly higher in hypertensive than in normotensive subjects. Red cell potassium concentration (in mmol/l of erythrocytes) was not significantly different in the two groups. Passive efflux of red cell potassium into buffered isotonic sucrose solution determined in eight hypertensive and nine normotensive subjects showed a lower potassium efflux rate in the hypertensive subjects. Comparison of active sodium efflux in sixteen hypertensive and fourteen normotensive subjects showed that ouabain-sensitive active sodium efflux was higher in red cells of normotensive than in those of hypertensive subjects.

Adolescent

Placebo-controlled, double-blind clinical trial of alprenolol in African hypertensive patients.

A placebo-controlled, double-blind clinical trial of alprenolol was carried out in 20 hypertensive Africans. The active drug and placebo were each administered for 8 weeks using a crossover design. Alprenolol was given in the form of a slow-release tablet preparation at a dosage of 200 mg twice daily. Four patients were withdrawn from the study either because of side-effects (2 patients) or non-compliance (2 patients). The mean reduction in blood pressure obtained in the 16 patients who completed the trial was less than that usually reported in Caucasians.

Adult

Determination of the isoniazid acetylator phenotype in a West African population.

The concentration of isoniazid in plasma after an oral dose of 10 mg/kg was estimated in 120 Nigerians (39 normal, 81 tuberculous). The concentrations were bimodally distributed giving a good discrimination between slow and rapid acetylators. The proportion of rapid to slow acetylators in the whole group was 60:40. This is similar to the results of the only other study of acetylator phenotype in West Africans.

Acetylation

Clinical trial of Ferastral in iron-deficient, non-pregnant patients in Ibadan, Nigeria.

Fifteen patients with proven iron-deficiency anaemia treated with intramuscular injections of Ferastral, iron-poly (sorbitol-gluconic acid) complex, have been studied. Fourteen showed a satisfactory rise in haematocrit. No local or systemic complications were observed. One patient with iron-deficiency anaemia due to a bleeding malignant lesion did not achieve a satisfactory haematocrit level although the bone marrow showed iron repletion following the injection. It is concluded that Ferastral is an effective drug in the treatment of iron-deficiency anaemia.

Anemia, Hypochromic

Investigations to characterize a new anti-arrhythmic drug, ORG 6001 including a simple test for calcium antagonism.

1 The compound Org 6001 (3alpha-amino-2beta-hydroxy-5alpha-androstan-17-one hydrochloride) was found in recent experiments to exhibit anti-arrhythmic activity. Evidence is presented in this paper concerning its mode of action. 2 Org 6001 was 1.8 times more potent than procaine as a local anaesthetic on desheathed frog nerve. 3 Org 6001 had no effect on the resting potential of isolated cardiac muscle of rabbit, but greatly reduced the maximum rate of depolarization tion (MRD). The action potential duration TAPD) WAS MARGINALLY PROLONGED IN ATRIAL AND VENTRICULAR MUSCLE. 4 Org 6001 preferentially shortened APD in that part of the Purkinje system in which APD is normally longer than elsewhere, so that APD

17-Ketosteroids

Plasma and erythrocyte cations and permeability of the erythrocyte membrane to cations in essential hypertension.

Untreated African patients with essential hypertension were found to have high plasma sodium and low plasma potassium. The red cel contents of these cations determined from the same sample of blood were found to be high for sodium and normal for potassium. The passive permeability of the erythrocytes for potassium was lower in hypertensives than in controls. The ouabain-sensitive active sodium efflux was lower in hypertensives than in controls. The relationships between the erythrocyte cation content and the total body content of the cations, and between the membrane function in red cells and other cells of the body are discussed.

Adult

beta-Adrenoceptor blockers in the treatment of hypertension.

Clinical drug trials have shown that pindolol, timolol and sotalol are effective hypotensive agents in Nigerians with mild to moderate hypertension (standing diastolic blood pressure below 120 mmHg). There was no significant difference between the three beta-blockers with respect to their antihypertensive effect irrespective of differences in their other pharmacological actions. There was also no correlation between the hypotensive effect of the drugs and the initial blood pressure. Timolol at 30 mg daily had an additive effect to the hypotensive action of binazine, a peripheral vasodilator. Increasing the dose of timolol to 60 mg daily did not produce further fall in the blood pressure. Pindolol at a dose of 30 mg per day also had an additive effect to the hypotensive action of the thiazide diuretics, methyldopa and debrisoquine. There was no significant difference between the hypotensive effect of sotalol and that of methyldopa. The three beta-blockers produced no side effects. This was considered to be a distinct advantage over most of the drugs currently available for treatment of hypertension in Nigeria.

Adrenergic beta-Antagonists