Pharmacokinetics and protein binding of methocarbamol in renal insufficiency and normals

  title={Pharmacokinetics and protein binding of methocarbamol in renal insufficiency and normals},
  author={Domenic A. Sica and Thomas J. Comstock and J. Davis and L Manning and Robert Powell and Armen P. Melikian and George Joseph Wright},
  journal={European Journal of Clinical Pharmacology},
SummaryWe 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… 
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The results showed that the drug inhibited the pseudoenzyme by un-competitive inhibition, and both Km and Vmax decreased by increasing the drug concentration.
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This first comprehensive study of the inhibitory effect of this class of drugs suggests that some of them may produce significant drug–drug interactions with opioids that are frequent comedications with skeletal muscle relaxants.
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