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The Effect of Raltegravir on the Glucuronidation of Lamotrigine
Author(s) -
Luin Matthijs,
Colbers Angela,
Verweyvan Wissen Corrien P. W. G. M.,
EwijkBenekenKolmer Eleonora W. J.,
Kolk Mike,
Hoitsma Arjen,
Silva Hugo Gomes,
Burger David M.
Publication year - 2009
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270009345689
Subject(s) - lamotrigine , raltegravir , pharmacokinetics , glucuronidation , pharmacology , medicine , chemistry , anesthesia , psychiatry , epilepsy , biochemistry , family medicine , human immunodeficiency virus (hiv) , antiretroviral therapy , viral load , enzyme , microsome
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.