HIV medications
From IDWiki
Classes
Class | Examples | Mechanism of Action | Adverse Effects |
---|---|---|---|
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-nucleoside reverse-transcriptase inhibitor (NNRTI) | 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. | Metabolic syndrome |
Integrase strand transfer inhibitor (INSTI) | raltegravir, dolutegravir, bictegravir | Generally very well-tolerated; may cause weight gain and diabetes | |
Fusion inhibitor | |||
CCR5 entry inhibitor | maraviroc | Blocks entry of HIV into CD4 cells. | |
CD4-mAb | ibalizumab |
Specific Medications
Class | Medication | Abbr | Notes |
---|---|---|---|
NRTI | lamivudine | 3TC | |
emtricitabine | FTC | ||
tenofovir disoproxol fumarate | TDF | ||
tenofovir alafenamide | TAF | Fewer renal and bone effects. | |
zidovudine | AZT | ||
abacavir | ABC | Need to check HLA-B*5701 before starting therapy. | |
NNRTI | efavirenz | EFZ | |
nevirapine | NVP | ||
rilpivirine | RPV | Take with meal, not with PPI. | |
doravirine | DOR | ||
PI | lopinavir/ritonavir | LPV/r | GI side effects. |
darunivir | DRV | ||
ritonavir | RTV | ||
INSTI | dolutegravir | DTG | Increases metformin levels. Avoid in pregnancy. |
elvitegravir/cobicistat | EVG/c | Requires booster that has drug interaction. | |
raltegravir | RAL | First INSTI. BID dosing. Only INSTI that can be used in pregnancy. | |
bictegravir | BIC | ||
cabotegravir | CAB | Long-acting injectable available. | |
ibalizumab | CD4-receptor antibody. |
Single-Tablet Regimens
Brand name | NRTIs | Non-NRTI | First-line? | Notes |
---|---|---|---|---|
Atripla | tenofovir disoproxil fumarate / emtricitabine | efavirenz (NNRTI) | No | Older regimen. Neuropsychiatric symptoms, possibly including suicide. No dose adjustment with rifampin. |
Biktarvy | tenofovir alafenamide / emtricitabine | bictegravir (INI) | Yes | |
Complera | tenofovir disoproxil fumarate / emtricitabine | rilpivirine (NNRTI) | No | Avoid with viral loads (>100,000) or low CD4 (<200). Pill must be taken with food (>400kcal) and without PPIs. |
Delstrigo | tenofovir disoproxil fumarate / lamivudine | doravirine (NNRTI) | No | |
Dovato | emtricitabine | dolutegravir (INI) | Yes | Two-medication regimen |
Genvoya | tenofovir alafenamide / emtricitabine | elvitegravir/cobicistat (INI) | No | See Stribild, above. |
Odefsey | tenofovir alafenamide / emtricitabine | rilpivirine (NNRTI) | No | |
Stribild | tenofovir disoproxil fumarate / emtricitabine | elvitegravir/cobicistat (INI) | No | Includes a P450 inhibitor to boost elvitegravir levels, with resultant drug-drug interactions. Avoid if CrCl <70. |
Symfi | tenofovir disoproxil fumarate / emtricitabine | efavirenz (NNRTI) | No | |
Symtuza | tenofovir alafenamide / emtricitabine | darunavir/cobicistat (PI) | No | |
Triumeq | abacavir / lamivudine | dolutegravir (INI) | Yes | Highest barrier to resistance. Need to test for HLA-B5701 allele before starting. Avoid in hepatitis B coinfection. |
Crushing Medications
- See https://www.hivclinic.ca/main/drugs_extra_files/Crushing%20and%20Liquid%20ARV%20Formulations.pdf
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.