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Kinetics and cardiac effects of propranolol in humans
- Source :
- Klinische Wochenschrift. 60:521-525
- Publication Year :
- 1982
- Publisher :
- Springer Science and Business Media LLC, 1982.
-
Abstract
- Six healthy volunteers received single 20-mg intravenous (IV) and 80-mg oral doses of propranolol on two occasions in random sequence. Serum propranolol concentrations were determined by gas chromatography in multiple samples drawn during 24 h after each dose. Mean (+/- SE) kinetic variables for IV propranolol were: elimination half-life (t 1/2 beta), 5.3 (+/- 0.6) h; volume of distribution, 2.3 (+/- 0.3) l/kg; total clearance, 4.9 (+/- 0.3) ml/min/kg; predicted extraction ratio, 0.23 (+/- 0.02). After single oral doses, t 1/2 beta (3.8 +/- 0.2 h) tended to be smaller than after the IV dose, and actual systemic availability (0.60 +/- 0.07) was less than that based on the predicted extraction ratio. During multiple oral dosage (80 mg every 12 h), observed steady state serum levels (47 +/- 5 ng/ml) tended to be less than those predicted based on the single oral dose (61 +/- 5 ng/ml), thus providing no evidence for reduced propranolol clearance at steady-state. Echocardiographic measurements of left ventricular performance (posterior wall velocity, diastolic dimensions) made during the single-dose oral study indicated significant impairment of function; impairment was maximal at 3 h post-dosage, and corresponded to the time of the peak serum propranolol concentration (341 ng/ml).
- Subjects :
- Adult
Male
medicine.medical_specialty
Kinetics
Extraction ratio
Diastole
Administration, Oral
Propranolol
Pharmacology
Single oral dose
Pharmacokinetics
Internal medicine
Drug Discovery
medicine
Humans
Genetics (clinical)
Volume of distribution
Dose-Response Relationship, Drug
Chemistry
General Medicine
Myocardial Contraction
Endocrinology
Injections, Intravenous
Molecular Medicine
Female
Steady state (chemistry)
Half-Life
medicine.drug
Subjects
Details
- ISSN :
- 14321440 and 00232173
- Volume :
- 60
- Database :
- OpenAIRE
- Journal :
- Klinische Wochenschrift
- Accession number :
- edsair.doi.dedup.....961cf29e6a95d14347f6a92624771f44