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Biomedical subjects

R D Kulkarni

Publications and source records attributed to R D Kulkarni.

At least 55 records · Page 3Linked to original sources

Pharmacokinetics of single and multiple doses of clobazam in humans.

1. The pharmacokinetics of clobazam and its biotransformation product N-desmethylclobazam were investigated after single and multiple doses in normal subjects. 2. The relevant physicochemical properties of clobazam were measured and are presented. Different assay methods (radiochemical, fluorimetric and gas chromatographic) were applied and the results correlated. 3. After single doses the pharmacokinetic profile of clobazam includes time to peak levels 1--4 h after dosing, peak levels increasing linearly with the logarithm of dose, and terminal half-lives of about 18 hours. At least 87% of an oral dose is absorbed, as indicated by urinary recovery of labelled material. 4. In multiple-dose studies unchanged clobazam levelled off at minimum steady-state concentrations within one week of dosing. During 28 d of medication N-desmethylclobazam accumulated to near steady-state levels about eight times higher than those of the unchanged compound. 5. No pharmacokinetic interactions were discovered between clobazam and the antidepressant nomifensine.

Anti-Anxiety Agents↗

Beta-2 adrenoceptor blocking activity of penbutolol and propranolol at very low doses.

The relative potency of penbutolol, a new beta adrenergic receptor blocking agent, was compared with propranolol by a four-point assay on healthy male subjects. A dose-response relationship to intravenous doses of propranolol in the microgram range was obtained during a steady state of infusion of epinephrine. Two subjects underwent the entire assay according to the Latin square design and four others each underwent one schedule of design on different days. The potency of penbutolol thus assessed was consistent with reported results. This study emphasizes the importance of intersubject variation and differential receptor sensitivity in individuals. The use of epinephrine as a beta receptor adrenergic agonist for evaluation of selective beta adrenergic receptor blocking activities is discussed.

Adrenergic beta-Antagonists↗

Effect of disodium cromoglycate and Picrorhiza kurroa root powder on sensitivity of guinea pigs to histamine and sympathomimetic amines.

Four weeks pretreatment with disodium cromoglycate (DSCG) and the powdered roots of the herb Picrorhiza kurroa, Benth, rendered guinea pigs less sensitive to histamine when compared with appropriate controls. The bronchodilator effects of isoprenaline and adrenaline were found to be markedly enhanced. The severity and duration of the allergic bronchospasm was significantly less in animals pretreated with the two drugs. Furthermore, the total histamine content of the lung tissue in animals pretreated with DSCG and P. kurroa was significantly less than that in the untreated controls. The pretreatment was also found to exhibit inhibitory effect on the immunological release of histamine and SRS-A from chopped lungs.

Airway Resistance↗

Estimation of gastro-intestinal blood loss in volunteers treated with non-steroidal anti-inflammatory agents.

In a double-blind study of 24 healthy volunteers treated with daily doses of 150 mg flurbiprofen, 600 mg phenylbutazone, 2.1 g aspirin, or placebo for 7 days, assessments were made of faecal blood loss before, during and after treatment. Measurementl body showed that aspirin produced the greatest degree of blood loss. Although both flurbiprofen and phenylbutazone produced greater blood loss than did placebo, the difference from pre-treatment values was not significant, and the levels returned almost to normal in the post-treatment period.

Adult↗

Carbohydrate metabolism of Indian women taking steroid contraceptives.

Three parameters, serum glucose, insulin, and growth hormone levels, were used to measure carbohydrate metabolism in 25 women not using steroid contraceptives, 48 women using combination oral contraceptives, and 27 women using low-dose progestogen oral contraceptives. Women in the combination contraceptives group had significant modifications in the responses of all three parameters studied. A bias toward modification was also seen in the normal tests of the combination group. The low-dose progestogen, megestrol acetate, did not cause similar changes in glucose, insulin, and growth hormone values.

Adult↗

Intense surveillance of adverse drug reactions. An analysis of 338 patients.

A prospective study of adverse drug reactions was recently completed at the Clinical Pharmacology Unit of J. J. Group of Hospitals. 338 patients were included in this study, and adverse reactions were noted by a team of workers including a nurse and a physician. World Health Organization definitions were used to describe adverse reactions. A total of 20 per cent of the patients showed adverse reactions to drugs. There was no difference with regard to age, occupation, or religion of the patients. Reaction was more common in the undernourished and also with a larger number of drugs or longer duration of stay in the hospital. The common reactions were neurologic, gastrointestinal, and allergic. Significant information is obtained by analysis of the percentage reaction in patients receiving drugs and the percentage of reactions per doses administered. It is confirmed that short-term intense surveillance programs are capable of providing useful data on incidence and types of adverse drug reactions.

Body Weight↗