Side-effects

In the 96-week study results of a phase II study in ARV-naive patients, the most common adverse events were neuropsychiatric (16%). Reported adverse events were nausea (13%), dizziness (9%), headache (9%), diarrhoea (7%), abnormal dreams (6%), and insomnia (8%). In every event, the percentage of events was higher in the efavirenz study arm.

Laboratory abnormalities were uncommon. There were ten reports of grade 4 creatine kinase elevations. The manufacturer recommends that the drug be used with caution in patients at increased risk of myopathy or rhabdomyolysis, such as patients receiving concomitant medications known to cause these conditions. Participants in the RAL study arm experienced less change in total cholesterol, LDL cholesterol, and triglycerides; also, smaller increases in the beneficial HDL cholesterol than did participants in the efavirenz study arm.1

In the 48-week reports from the phase III STARTMRK trial in treatment-naive patients, less than 5% on the RAL arm reported headache, nausea, dizziness, insomnia, diarrhoea, and fatigue. In both the RAL and EFV study arms, there were serious clinical events in 10%.

There were two deaths in the study, both participants in the RAL arm. Again, participants in the RAL study arm experienced less change in total cholesterol, LDL cholesterol, and triglycerides; but also, smaller increases in the beneficial HDL cholesterol than did participants in the efavirenz study arm.2  

In the BENCHMRK 1 and 2 phase III studies with ARV-experienced patients, raltegravir was generally well tolerated. Three of 133 patients (2%) experienced grade 3 ALT or AST elevations and stopped the drug. The frequency of drug-related adverse events was similar in both the placebo and the raltegravir ams of the study.3

In October 2008, the US FDA advised Merck that the package insert required revision to include, under 'postmarketing adverse reactions', both rash and Stevens-Johnson syndrome and to include in the patient package insert, the information that rash and severe skin reactions might be expected.

References

  1. Markowitz M et al. Sustained antiretroviral efficacy of raltegravir as part of combination ART in treatment-naive HIV-infected patients: 96-week data. Seventeenth International AIDS Conference, Mexico City, abstract TUAB0102, 2008
  2. Lennox J et al. STARTMRK, a phase III study of the safety and efficacy of raltegravir-based vs. efavirenz-based combination therapy in treatment-naïve HIV-infected patients. 48th Interscience Conference on Antimicrobial Agents and Chemotherapy, abstract H-896a, Washington, 2008
  3. Steigbigel RT et al. Raltegravir with optimized background therapy for resistant HIV-1 infection. N Engl J Med359(4): 339-54, 2008
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