title: Pharmacokinetics of rilmenidine in patients with chronic renal insufficiency and in hemodialysis patients.
abstract: The pharmacokinetics of rilmenidine (1 mg orally) was studied in 3 groups of patients with stable chronic renal insufficiency. This was an open, single-blind study following a single administration, and after 15 days of treatment. Group 1 included 11 patients with a creatinine clearance between 15 and 80 mL/min. Group 2 included 17 patients with a creatinine clearance < 15 mL/min. Group III included 10 hemodialysis patients. In patients with chronic renal failure, total plasma clearance and renal clearance of rilmenidine decreased; terminal half-life was 30-42 hours, which is clearly longer than previous values achieved in healthy volunteers. After repeated administration (1 mg daily in group 1, 1 mg every other day in group 2, 1 mg at the end of each dialysis session in group 3), the area under the curve was significantly increased, corresponding to drug accumulation. The steady state was reached after 6 days in patients in group 1 and after 8 days in patients in group 2. The pharmacokinetics of rilmenidine was linear since the terminal elimination half-life and renal clearance were not significantly different after single and repeated administration of rilmenidine. A positive correlation was found between rilmenidine total plasma clearance and creatinine clearance, and between rilmenidine renal clearance and creatinine clearance. Mean rilmenidine hemodialysance was 85 mL/min, that is, 26% of the rilmenidine renal clearance value achieved in healthy volunteers (330 mL/min). Thus, the following dosage schedule can be proposed. In patients whose creatinine clearance ranges between 15 and 80 mL/min, a 1 mg dose every day can be recommended.(ABSTRACT TRUNCATED AT 250 WORDS)
authors.affiliation: Service de Nephrologie, CHU de Rouen, France.
authors.forename: M
authors.initials: M
authors.lastname: Aparicio
authors.forename: M
authors.initials: M
authors.lastname: Dratwa
authors.forename: N
authors.initials: N
authors.lastname: el Esper
authors.forename: J P
authors.initials: JP
authors.lastname: Fillastre
authors.forename: B
authors.initials: B
authors.lastname: Levaltier
authors.forename: R
authors.initials: R
authors.lastname: Lins
authors.forename: A
authors.initials: A
authors.lastname: Meyrier
authors.forename: F
authors.initials: F
authors.lastname: Mignon
authors.forename: J P
authors.initials: JP
authors.lastname: Ryckelynck
authors.forename: J
authors.initials: J
authors.lastname: Sennesael
mesh_terms: D000293:Adolescent; D000328:Adult; D000368:Aged; D000959:Antihypertensive Agents / Q000493:pharmacokinetics*; D003404:Creatinine / Q000378:metabolism; D015314:Dialysis Solutions / Q000378:metabolism; D005260:Female; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000378:metabolism; D007668:Kidney / Q000378:metabolism*; D007676:Kidney Failure, Chronic / Q000378:metabolism*; D008297:Male; D008875:Middle Aged; D010080:Oxazoles / Q000493:pharmacokinetics*; D006435:Renal Dialysis; D000077769:Rilmenidine; D016037:Single-Blind Method
chemical_list: D000959:Antihypertensive Agents; D015314:Dialysis Solutions; D010080:Oxazoles; D003404:Creatinine; D000077769:Rilmenidine