Drug interactions

Raltegravir is not metabolised through the CYP3A enzyme, so is unlikely to have important interactions with other anti-HIV drugs. There is no known cross-resistance to raltegravir.1 2 3  Caution should be used when co-administering raltegravir with strong inducers of uridine diphosphate glucuronosyltransferase (UGT) 1A1 (e.g., rifampicin) due to reduced plasma concentrations of raltegravir.

A surprising occurrence reported with post-marketing raltegravir use is exacerbation of pre-existing depression. In four case reports, patients being treated for depression with antidepressants or antipsychotic medication at the time they initiated raltegravir therapy experienced a deterioration in their mental health. In all four men, this occurred within a month of starting therapy and one person required hospitalisation.

When the type or dose of the antidepressant was changed, symptoms improved within three months of their onset. All four patients continued to use raltegravir. Caution and close monitoring is advised when starting patients with depression on a raltegravir-containing regimen. (Anyone with depression had been excluded from participation in the raltegravir clinical trials.)4 

 

References

  1. Cooper D et al. Results from BENCHMRK-1, a phase III study evaluating the efficacy and safety of MK-0518, a novel HIV-1 integrase inhibitor, in patients with triple-class resistant virus. Fourteenth Conference on Retroviruses and Opportunistic Infections, Los Angeles, abstract 105aLB, 2007
  2. Steigbigel R et al. Results from BENCHMRK-2, a phase III study evaluating the efficacy and safety of MK-0518, a novel HIV-1 integrase inhibitor, in patients with triple-class resistant virus. Fourteenth Conference on Retroviruses and Opportunistic Infections, Los Angeles, abstract 105bLB, 2007
  3. Grinsztejn B et al. Safety and efficacy of the HIV-1 integrase inhibitor raltegravir (MK-0518) in treatment-experienced patients with multidrug-resistant virus: a phase II randomized controlled trial. Lancet 369(9569): 1261-1269, 2007
  4. Harris M et al. Exacerbation of depression associated with starting raltegravir: a report of four cases. AIDS 22: 1890-1892, 2008
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