title: The effect of raltegravir on the glucuronidation of lamotrigine.
abstract: The authors studied the effect of raltegravir on the pharmacokinetics of the antiepileptic agent lamotrigine. Twelve healthy volunteers (group A) received 400 mg raltegravir twice daily from days 1 to 5. On day 4, a single dose of 100 mg lamotrigine was administered. After a washout period, participants received a second single dose of 100 mg of lamotrigine but now without raltegravir (day 32). In group B, 12 participants received the same treatment as in group A but in reverse order. On days 4 and 32, 48-hour pharmacokinetic curves were drawn. Geometric mean ratios (+90% confidence intervals [CIs]) of lamotrigine area under the plasma concentration-time curve (AUC(0-->48)) and peak plasma concentration (C(max)) for raltegravir + lamotrigine versus lamotrigine alone were 0.99 (0.96-1.01) and 0.94 (0.89-0.99), respectively. The mean ratio of the AUC(0-->48) of lamotrigine-2N-glucuronide to lamotrigine was similar when lamotrigine was taken alone (0.35) or when taken with raltegravir (0.36). Raltegravir does not influence the glucuronidation of lamotrigine.
authors.affiliation: Department of Clinical Pharmacy, Radboud University Medical Centre Nijmegen, Nijmegen, The Netherlands. m.vanluin@akf.umcn.nl
authors.forename: Matthijs
authors.initials: M
authors.lastname: van Luin
authors.forename: Angela
authors.initials: A
authors.lastname: Colbers
authors.forename: Corrien P W G M
authors.initials: CP
authors.lastname: Verwey-van Wissen
authors.forename: Eleonora W J
authors.initials: EW
authors.lastname: van Ewijk-Beneken-Kolmer
authors.forename: Mike
authors.initials: M
authors.lastname: van der Kolk
authors.forename: Arjen
authors.initials: A
authors.lastname: Hoitsma
authors.forename: Hugo Gomes
authors.initials: HG
authors.lastname: da Silva
authors.forename: David M
authors.initials: DM
authors.lastname: Burger
mesh_terms: D000328:Adult; D000927:Anticonvulsants / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004334:Drug Administration Schedule; D004347:Drug Interactions; D014453:Glucuronosyltransferase / Q000037:antagonists & inhibitors*; D019428:HIV Integrase Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D006801:Humans; D000077213:Lamotrigine; D008297:Male; D055118:Medication Adherence; D008875:Middle Aged; D011760:Pyrrolidinones / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D000068898:Raltegravir Potassium; D014227:Triazines / Q000008:administration & dosage / Q000493:pharmacokinetics*
chemical_list: D000927:Anticonvulsants; D019428:HIV Integrase Inhibitors; D011760:Pyrrolidinones; D014227:Triazines; D000068898:Raltegravir Potassium; D014453:Glucuronosyltransferase; D000077213:Lamotrigine