The drug atlas
Sexual Health / HIV/Antiretroviral therapy

Antiretroviral therapy (ART)

also: HAART · HIV treatment · INSTI · NRTI · NNRTI · PI

Overview

Combination therapy for HIV — typically two NRTIs plus a third agent (now usually an integrase inhibitor). Goal: undetectable viral load (U=U: untransmittable). Lifelong.

Mechanism

Each class blocks a different step of the HIV life cycle. NRTIs (e.g. tenofovir, emtricitabine, abacavir) are nucleoside analogues that terminate reverse-transcription. NNRTIs bind/inhibit reverse transcriptase allosterically. Integrase strand-transfer inhibitors (INSTIs, "-tegravir") block proviral DNA integration. Protease inhibitors ("-navir") block viral maturation. Combining classes prevents resistance.

Indications

  • HIV-1 infection (start ART in everyone, regardless of CD4)

The agents

Tenofovir + emtricitabineNRTI backbone

OD

Tenofovir: renal + bone toxicity (TDF) — TAF gentler.

Dolutegravir / bictegravirINSTI (3rd agent)

OD

First-line third agent; weight gain; few interactions.

EfavirenzNNRTI

OD nocte

CNS/vivid dreams; CYP inducer.

AbacavirNRTI

HLA-B*57:01 test before use — hypersensitivity.

Atazanavir / darunavirPI (boosted)

GI upset, lipid effects, many interactions.

Adverse effects

Abacavir hypersensitivityserious

Screen HLA-B*57:01 first — fever, rash, GI, do not rechallenge.

Tenofovir (TDF): renal impairment + reduced bone densityserious
INSTI: weight gaincommon
Efavirenz: CNS effects, vivid dreams, rashcommon
Lipodystrophy / dyslipidaemia (older agents, PIs)common
Immune reconstitution inflammatory syndrome (IRIS)serious

On starting ART with low CD4.

Cautions & contraindications

Abacavir if HLA-B*57:01 positiveall
Tenofovir DF in significant renal impairmentrenal
Many drug interactions (esp. PIs/boosters, efavirenz)all

CYP3A4 — check statins, rifampicin, contraception, PPIs.

Interactions

  • PIs/cobicistat inhibit CYP3A4 (↑statins, sedatives)
  • Efavirenz/rifampicin induce CYP
  • INSTIs chelated by antacids/divalent cations — separate dosing

Monitoring & kinetics

CD4 count + HIV viral load,U&E (tenofovir), bone health, lipids,HLA-B*57:01 before abacavir

Oral combinations, usually once daily (single-tablet regimens). Adherence is critical to prevent resistance.

Source: BHIVA — HIV treatment guidelines · BNF — Antiretrovirals