Pharmacokinetics of rilmenidine in healthy subjects

Journal Article · Wed Feb 24 04:00:00 EST 1988 · Am. J. Cardiol.; (United States)

DOI:https://doi.org/10.1016/0002-9149(88)90465-1· OSTI ID:5295835

Genissel, P; Bromet, N; Fourtillan, J B; Mignot, A; Albin, H

Rilmenidine is a novel alpha 2-adrenoceptor agonist, used in the treatment of mild or moderate hypertension at the oral dose of 1 mg once or twice daily. The pharmacokinetic parameters were investigated after single or repeated administration in healthy subjects, using labeled and unlabeled compounds. Rilmenidine was rapidly and extensively absorbed, with an absolute bioavailability factor close to 1 and a maximal plasma concentration achieved within 2 hours. Rilmenidine was not subject to presystemic metabolism. Distribution was independent of the free fraction because rilmenidine was weakly bound to plasma proteins (less than 10%). The volume of distribution was approximately 5 l.kg-1 (315 liters). Elimination was rapid with a total body plasma clearance of approximately 450 ml.min-1 and an elimination half-life of approximately 8 hours. Renal excretion was the major elimination process (two-thirds of the total clearance). Metabolism was very poor, with a renal elimination of rilmenidine as the parent drug (urinary fraction of rilmenidine was about 65% and no metabolite plasma levels were detected). Linear pharmacokinetics were demonstrated for rilmenidine from 0.5 to 2 mg but, at 3 mg, a slight deviation from linearity was observed. In repeated administration, the linear disposition of rilmenidine with dose was confirmed.

• Research Organization: Institut de Recherceh Internationales Servier, Neuilly-sur-Seine (France)
• OSTI ID: 5295835
• Journal Information: Am. J. Cardiol.; (United States), Journal Name: Am. J. Cardiol.; (United States) Vol. 61:7; ISSN AJCDA
• Country of Publication: United States
• Language: English

Related Subjects

550501* -- Metabolism-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ABSORPTION
AUTONOMIC NERVOUS SYSTEM AGENTS
AZOLES
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL AVAILABILITY
BIOLOGICAL HALF-LIFE
CARBON ISOTOPES
CARDIOVASCULAR DISEASES
DISEASES
DRUGS
HETEROCYCLIC COMPOUNDS
HYPERTENSION
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LABELLED COMPOUNDS
METABOLISM
ORAL ADMINISTRATION
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC OXYGEN COMPOUNDS
OXAZOLES
REACTION KINETICS
SYMPATHOLYTICS
SYMPTOMS
TRACER TECHNIQUES
VASCULAR DISEASES