HIV medications

Classes

Class	Examples	Description
Nucleoside reverse-transcriptase inhibitor (NRTI)	tenofovir, emtricitabine, abacavir	Nucleoside/nucleotide analogues that get incorporated into viral DNA by reverse transcriptase, causing missense or non-sense mutations. The backbone of HIV treatments, with a high barrier to resistance.
Non-NRTI	efavirenz	Actively inhibit reverse transcriptase at its active site. Resistance develops with a single point mutation.
Protease inhibitor (PI)	dirunavir	Inhibits protease, which is required for processing proteins in the creation of the virion. Causes a metabolic syndrome.
Integrase inhibitor (INSTI)	raltegravir, dolutegravir, bictegravir	Extremely potent with few side effects. Take separate from PPIs etc.
Fusion inhibitor
CCR5 inhibitor
CD4-mAb	ibalizumab	Blocks entry of HIV into CD4 cells.

Specific Medications

Medication	AKA	Class	Notes
lamivudine	3TC	NRTI
emtricitabine	FTC	NRTI
tenofovir disoproxol	TDF	NRTI
tenofovir alafenamide	TAF	NRTI	Fewer renal and bone effects.
zidovudine	AZT	NRTI
abacavir	ABC	NRTI	Need to check HLA-B5701 before starting therapy.
efavirenz	EFZ	NNRTI
rilpivirine	RPV	NNRTI	Take with meal, not with PPI.
doravirine	DOR	NNRTI
lopinavir/ritonavir	LPV/r	PI	GI side effects.
darunivir	DRV	PI
dolutegravir	DTG	INSTI	Increases metformin levels. Avoid in pregnancy.
elvitegravir/cobicistat	EVG/c	INSTI	Requires booster that has drug interaction.
raltegravir	RAL	INSTI	First INSTI. BID dosing. Only INSTI that can be used in pregnancy.
bictegravir	BIC	INSTI
cabotegravir	CAB	INSTI	Long-acting injectable available.
ibalizumab			CD4-receptor antibody.

Single-Tablet Regimens

Brand name	NRTIs	Non-NRTI	Notes
Triumeq	ABC/3TC	DTG (INI)	Highest barrier to resistance. Need to test for HLA-B5701 allele before starting. Avoid in hepatitis B coinfection.
Atripla	TDF/FTC	EFZ	Older regimen. Neuropsychiatric symptoms, possibly including suicide.
Complera	TDF/FTC	RPV	Avoid with viral loads (>100,000) or low CD4 (<200). Pill must be taken with food (>400kcal) and without PPIs.
Stribild	TDF/FTC	EVG/c (INI)	Includes a P450 inhibitor to boost elvitegravir levels, with resultant drug-drug interactions. Avoid if CrCl <70.
Genvoya	TAF/FTC	ELV/c (INI)
Biktarvy	TAF/FTC	BIC (INI)

Considerations

• Hepatitis B: Avoid Triumeq; use TDF/FTC-based regimen instead
• CKD: Avoid Stribild in CrCl <70

Further Reading

• Andany N and Gold WL. Five things to know about single-tablet antiretroviral treatment (once daily). CMAJ. 2016;188(13)971.
• Gandhi M and Gandhi RT. Single-Pill Combination Regimens for Treatment of HIV-1 Infection. N Engl J Med. 2014;371:248-259.