[Secondary effects associated with raltegravir].
Integrase inhibitors are a new therapeutic modality against HIV. Raltegravir is the first integrase inhibitor to have been approved by the health authorities for human use. This drug acts by inhibiting the HIV enzyme that catalyzes integration of the virus inside the genome of the host cell. In the host cell, there is no homologue to viral integrase and consequently the potential toxicity of this drug is probably low. The results of safety studies in animal models have shown that the recommended dose in humans is lower than the dose below which no secondary effects are observed. Studies of genotoxicity and carcinogenicity, as well as of fertility and embryo development, have been negative to date. During clinical trials, raltegravir has been shown to have a very good safety profile, with few adverse effects, which were mild-to-moderate and similar to those of the comparator. The most notable were diarrhea, nausea and headache. The lipid profile of raltegravir was better than that of efavirenz. In view of the above, the risk-benefit ratio for raltegravir is positive.
Gatell
José M
JM
Servicio de Infecciones, Hospital Clinic, IDIBAPS, Universidad de Barcelona, Barcelona, España. gatell0@attglobal.net
Zamora
Laura
L
D000014:Abnormalities, Drug-Induced / Q000209:etiology; D000818:Animals; D056486:Chemical and Drug Induced Liver Injury / Q000209:etiology; D002986:Clinical Trials as Topic / Q000706:statistics & numerical data; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D047108:Embryonic Development / Q000187:drug effects; D005260:Female; D005767:Gastrointestinal Diseases / Q000139:chemically induced; D015658:HIV Infections / Q000188:drug therapy*; D019427:HIV Integrase / Q000187:drug effects*; D019428:HIV Integrase Inhibitors / Q000009:adverse effects* / Q000627:therapeutic use / Q000633:toxicity; D006261:Headache / Q000139:chemically induced; D006801:Humans; D008297:Male; D051379:Mice; D009152:Mutagenicity Tests; D010146:Pain / Q000139:chemically induced; D011247:Pregnancy; D011760:Pyrrolidinones / Q000009:adverse effects* / Q000627:therapeutic use / Q000633:toxicity; D011817:Rabbits; D000068898:Raltegravir Potassium; D051381:Rats
D019428:HIV Integrase Inhibitors; D011760:Pyrrolidinones; D000068898:Raltegravir Potassium; D019427:HIV Integrase; C514801:p31 integrase protein, Human immunodeficiency virus 1