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Absorption, metabolism, and excretion of intravenously and orally administered [14C]telmisartan in healthy volunteers.
- Source :
-
Journal of clinical pharmacology [J Clin Pharmacol] 2000 Dec; Vol. 40 (12 Pt 1), pp. 1312-22. - Publication Year :
- 2000
-
Abstract
- The study was conducted in healthy male volunteers to evaluate the absorption, metabolic pattern, and mode of elimination of telmisartan, a nonpeptide angiotensin II receptor antagonist. [14C]telmisartan was administered orally in solution as a single 40 mg dose to 5 subjects. A further 5 subjects received short-term intravenous infusion of [14C]telmisartan 40 mg. Measurement of total 14C radioactivity in plasma showed that about 50% was absorbed following oral administration, with maximum plasma concentration observed after 0.5 to 1 hour. Absolute bioavailability was 43%. On average, 84% of total radioactivity in plasma reflected the parent compound. The remainder of total radioactivity could be ascribed to the glucuronide conjugate of telmisartan, which represented the only metabolite in man. About 99.5% of telmisartan was bound to plasma protein, mainly to albumin and alpha-1-acid glycoprotein. Telmisartan was reversibly distributed into erythrocytes. More than 90% of administered dose was excreted within 120 hours, and the excretion balance was complete 144 hours after dosing. Radioactivity was almost exclusively (> 98%) excreted via the feces; urinary excretion accounted for < 1% of the dose, irrespective of the route of administration. In the small fraction excreted into urine, the glucuronide conjugate of telmisartan was predominant. Although some telmisartan glucuronide was detected in plasma, only unchanged drug was identified in the feces. No changes in vital signs, electrocardiogram, or clinical laboratory tests were detected following telmisartan administration, and adverse events, predominantly unrelated to treatment and of mild intensity, were infrequent. One subject fainted and, on another occasion, reported faintness; these events were probably due to the antihypertensive action of the intravenous study medication.
- Subjects :
- Absorption
Administration, Oral
Adolescent
Adult
Angiotensin-Converting Enzyme Inhibitors adverse effects
Angiotensin-Converting Enzyme Inhibitors blood
Angiotensin-Converting Enzyme Inhibitors chemistry
Angiotensin-Converting Enzyme Inhibitors urine
Benzimidazoles adverse effects
Benzimidazoles blood
Benzimidazoles chemistry
Benzimidazoles urine
Benzoates adverse effects
Benzoates blood
Benzoates chemistry
Benzoates urine
Carbon Radioisotopes
Humans
Infusions, Intravenous
Male
Middle Aged
Structure-Activity Relationship
Telmisartan
Angiotensin-Converting Enzyme Inhibitors pharmacokinetics
Benzimidazoles pharmacokinetics
Benzoates pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 0091-2700
- Volume :
- 40
- Issue :
- 12 Pt 1
- Database :
- MEDLINE
- Journal :
- Journal of clinical pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 11185629