The investigators concluded that no dose adjustment is necessary when citalopram and RAL are co-administered. However,monitoring patients for virologic failure of RAL is warranted as PK parameters of RAL were variably affected (as seen with the wide confidence intervals) when coadministered with citalopram.
Raltegravir vs citalopram
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Study Design
In an open-label, randomized cross-over study, 24 healthy subjects with median age of 47 (18-53) years old received citalopram 20 mg daily for 14 days followed by coadministration of citalopram 20 mg daily plus raltegravir (RAL) 400 mg twice daily for 5 days. After a washout period, subjects received RAL 400 mg twice daily for 5 days.
Study Results
Coadministration of citalopram 20 mg daily and RAL 400 mg twice daily decreased RAL exposure and maximum plasma concentration; geometric mean ratios (GMRs; citalopram + RAL / RAL) of AUC and Cmax for RAL were 0.77 [0.50, 1.19] and 0.64 [0.38, 1.09], respectively. However, concomitant administration of citalopram did not significantly affect mean plasma concentration (C12h) of RAL; GMRs (citalopram + RAL / RAL) [90% CIs] of C12h was 1.03 [0.71, 1.50].PK of citalopram and it's metabolite was not significantly impacted when coadministered with RAL, as shown below: GMRs (RAL + citalopram / citalopram) [90% CIs] of AUC, Cmax, and C24h for citalopram were 1.00 [0.98,1.03], 0.98 [0.95,1.01], and 1.03 [1.00,1.07], respectively. GMRs (RAL + citalopram / citalopram) [90% CIs] of AUC, Cmax, and C24h for desmethylcitalopram, an active metabolite of citalopram, were 0.99 [0.88,1.12], 0.97 [0.86,1.09], and 1.04 [0.92,1.18], respectively.
References
M Blonk, C Langemeijer, A Colbers, et al. Pharmacokinetic drug-drug interaction study between raltegravir and citalopram in healthy volunteers. 16th International Workshop On Clinical Pharmacology Of Hiv ; Hepatitis Therapy. Washington, DC. ; .
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