Pharmacokinetics and protein binding of methocarbamol in renal insufficiency and normals
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We determined plasma methocarbamol concentrations over 24 h following a 1.5 g methocarbamol dose (off-dialysis day) to 8 chronic haemodialysis patients and compared these results to those from 17 healthy male volunteers.
The harmonic mean elimination half-life was similar between the two groups, 1.24 and 1.14 h, respectively. tmax and the weight-adjusted Cmax were 1.1 h and 27.0 mg · m−1 for haemodialysis patients and 1.1 and 23.1 mg · l−1 for normals. Relative systemic availability was assessed by comparing weight-normalized AUC × k10 products.
These results indicate no significant differences with respect to methocarbamol absorption, with the relative systemic availability in patients being 113%.
These data suggest that absorption and elimination of methocarbamol is similar between normal subjects and patients undergoing maintenance haemodialysis.
Key wordsmethocarbamol haemodialysis pharmacokinetics
- 1.Bruce RB, Turnbull LB, Newman JH (1971) Metabolism of methocarbamol in the rat, dog, and human. J Pharm Sci 60: 104–106Google Scholar
- 2.Gibson TP (1986) Renal disease and drug metabolism: An overview. Am J Kidney Dis 8: 7–17Google Scholar
- 3.Quintanilla AP (1986) Liver dysfunction in dialysis patients. Int J Artif Intern Organs 9: 1–2Google Scholar
- 4.Simon P, Meyrier A, Brissot P (1981) Uremia and the liver. II. Drugs and the liver in the uremic patient. Nephron 29: 7–13Google Scholar
- 5.Verbeeck RK (1982) Glucuronidation and disposition of drug glucuronides in patients with renal failure. A review. Drug Metab Disp 10: 87–89Google Scholar
- 6.Wagner JG (1967) Method of estimating relative absorption of a drug in a series of clinical studies in which blood levels are measured after single and/or multiple doses. J Pharm Sci 56: 652–653Google Scholar
- 7.Wagner JG (1978) Fundamentals of clinical pharmacokinetics. Drug Intelligence Publications, Hamilton, pp 347–348Google Scholar