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cART

PharmacologyImmunologyInfectious Disease

Summary

Combination antiretroviral therapy is the use of at least three active antiretroviral drugs from two or more classes to suppress HIV replication. Combination is essential because monotherapy invariably selects resistance given the error-prone reverse transcriptase.

Detail

A standard initial regimen is two nucleoside reverse transcriptase inhibitors, usually tenofovir with emtricitabine or lamivudine, plus an integrase strand transfer inhibitor such as bictegravir or dolutegravir, and many are single-tablet once-daily formulations. Other classes are non-nucleoside reverse transcriptase inhibitors (efavirenz, rilpivirine), protease inhibitors (darunavir, atazanavir, typically pharmacologically boosted with ritonavir or cobicistat, both CYP3A4 inhibitors), the fusion inhibitor enfuvirtide, and the CCR5 antagonist maraviroc, which requires prior tropism testing. Therapy is now started at diagnosis regardless of CD4 count, and sustained viral suppression means HIV is untransmittable sexually. Class-specific toxicities are examinable: tenofovir disoproxil causes renal tubular injury and reduced bone density, abacavir causes a hypersensitivity reaction in HLA-B*5701 carriers who must be screened first, zidovudine causes macrocytic anaemia, protease inhibitors cause hyperglycaemia, dyslipidaemia, and lipodystrophy, and efavirenz causes vivid dreams and neuropsychiatric effects. Immune reconstitution inflammatory syndrome may follow rapid CD4 recovery.

Sources

  • Katzung Basic and Clinical Pharmacology
  • Harrison's Principles of Internal Medicine

Reviewed by AnkiBoss editorial — medical student review. Information here is for study reference only and is not medical advice. Spotted an error? Let us know.

Related pharmacology terms

cART — Medical Glossary