Potential benefits of cyproheptadine in HIV-positive patients under treatment with antiretroviral drugs including efavirenz

Expert Opin Pharmacother. 2012 Dec;13(18):2613-24. doi: 10.1517/14656566.2012.742887. Epub 2012 Nov 10.


Introduction: More than 50% of HIV-positive patients experience neuropsychiatric adverse reactions following efavirenz therapy. Discontinuation of efavirenz due to its neuropsychiatric side effects has been reported in 2 - 13% of patients. Dizziness, headache, nightmares, abnormal dreams, mild cognitive difficulty, sleep disturbance (somnolence and insomnia), impaired concentration, depression, hallucination, delusion, paranoia, anxiety, agitation, aggressive behavior, mania, emotional labiality, catatonia, melancholia, psychosis, and fatigue are the most reported efavirenz adverse reactions.

Areas covered: In this review, potential benefits of cyproheptadine in prevention and management of HIV/antiretroviral-associated neuropsychiatric complications are evaluated. The available evidence was collected by searching Scopus, PubMed, Medline, Cochrane central register of controlled trials, and Cochrane database systematic reviews.

Expert opinion: Cyproheptadine is a cheap and safe drug that does not have significant interactions with antiretroviral drugs. Cyproheptadine's common side effects including increasing appetite and weight gain can be useful in HIV-positive individuals with their decreased appetite and weight loss. There is limited evidence regarding the effectiveness of cyproheptadine in neuropsychiatric disorders. It is essential to evaluate cyproheptadine efficacy in the prevention and management of neuropsychiatric complications of HIV/antiretroviral infection in well-designed studies in the future.

Publication types

  • Review

MeSH terms

  • Alkynes
  • Anti-HIV Agents / adverse effects*
  • Anti-HIV Agents / therapeutic use
  • Benzoxazines / adverse effects*
  • Benzoxazines / therapeutic use
  • Cyclopropanes
  • Cyproheptadine / adverse effects
  • Cyproheptadine / therapeutic use*
  • Drug Interactions
  • Evidence-Based Medicine
  • HIV Seropositivity / drug therapy*
  • Humans
  • Neurotoxicity Syndromes / prevention & control*
  • Serotonin 5-HT2 Receptor Antagonists / adverse effects
  • Serotonin 5-HT2 Receptor Antagonists / therapeutic use*


  • Alkynes
  • Anti-HIV Agents
  • Benzoxazines
  • Cyclopropanes
  • Serotonin 5-HT2 Receptor Antagonists
  • Cyproheptadine
  • efavirenz