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.
