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Biomedical subjects

J Larribaud

Publications and source records attributed to J Larribaud.

At least 19 recordsLinked to original sources

Pharmacokinetic and pharmacodynamic interactions between nifedipine and propranolol or betaxolol.

Pharmacokinetic and pharmacodynamic interactions between nifedipine and two beta-blocking agents were investigated. Eighty mg propranolol twice daily, and 20 mg betaxolol once daily, were randomly administered orally to six young healthy male volunteers, either singly for four days, or combined with nifedipine for the two subsequent days. Nifedipine had similar effects on the pharmacodynamics of both drugs. Nifedipine significantly enhanced propranolol bioavailability and Cmax, but reduced its tmax, in three out of six subjects who were also good absorbers of beta-blockers when taken alone. These effects might be due to enhanced intestinal absorption and/or enhanced first-pass effect, induced by nifedipine.

Adrenergic beta-Antagonists

Pharmacokinetics of the new beta-adrenoceptor blocking agent betaxolol (SL 75212) in man after repeated oral administration.

(+/-)-1-(Isopropylamino)-3-[p-(2-cyclopropyl-methoxyethyl)-phenoxy]-2-propanol HCl (betaxolol, SL 75212) was given to groups of healthy volunteers, 10 mg daily for 7 days followed by 20 mg daily 7 days in one group, and increasing daily doses up to 60 mg/day for a total of 15 days in the other group. The pharmacokinetics were studied during dosing and in the washout period. The pharmacokinetic characteristics were unchanged after repeated doses, T/2 16-22 h, Vd 7.7-8.8 l/kg; clearance 0.28-0.33 l/h/kg.

Administration, Oral

Pharmacokinetics and metabolism of diltiazem in man.

Dilitazem, a coronary vasodilating agent, after oral administration of four different doses, was well and rapidly absorbed. The pharmacokinetics of the drug followed a two-compartment model, with a rapid distribution and an elimination with a half-life of 4-7 hours. After chronic treatment the pharmacokinetic parameters were practically unchanged and therefore no accumulation of the drug was observed. The comparison between capsule and tablet preparations showed that both forms had a similar bioavailability. Diltiazem was extensively metabilized and only a few percent of the drug was found in urine. Several metabolites, also present as conjugates, have been identified by means of gas chromatography-mass spectrometry.

Administration, Oral