Overview of Antiretroviral Therapy
Kathryn Snyder
Quinton Taylor
Fixed Dose Combination Regimens | Components | Renal Dosing (CrCl) | Specific Considerations |
|---|---|---|---|
| Biktarvy® | Bictegravir / Emtricitabine / Tenofovir (Alafenamide) | <30: DC ok w/ HD |
↑ Metformin levels CI w/: rifampin, dofetilide, rifabutin Avoid close admin. with: laxatives, sucralfate, polyvalent cations (iron, calcium, etc.) |
| Dovato® | Dolutegravir/Lamivudine | 30-50: monitor for heme toxicities with lamivudine <30: dose-adjust components |
↑ Metformin levels Dose adjustment needed w/ rifampin CI w/ dofetilide and multiple AEDs Avoid close admin. with polyvalent cations (iron, calcium, etc.) |
| Symtuza® | Tenofavir alafenamide / Emtricitabine / Darunavir / Cobicistat | <30 DC ok w/ HD but dose after HD on dialysis days |
Test all pts for HBV prior to initiation Many CYP3A4 DDIs with cobicistat. CI w/ simvastatin, rifampin, multiple antipsychotics and AEs, ↑ risk of Cushing's syndrome w/ corticosteroids. Cobicistat can increase Cr w/o affecting glomerular filtration. |
| Triumeq® | Abacavir / Dolutegravir / Lamivudine | 30-50: monitor for heme toxicities with lamivudine <30: dose-adjust components |
↑ Metformin levels Dose adjustment needed with rifampin use CI w/ dofetilide and multiple AEDs Avoid close admin. with polyvalent cations (iron, calcium, etc.) |
| Genvoya® | Elvitegravir / Cobicistat / Emtricitabine / Tenofovir (Alafenamide) | <30 DC ok w/ HD |
Test all pts for HBV prior to initiation Many CYP3A4 DDIs with cobicistat. CI w/ simvastatin, rifampin, multiple antipsychotics and AEs, ↑ risk of Cushing's syndrome w/ corticosteroids. Cobicistat can increase Cr w/o affecting glomerular filtration. |
NRTI |
Dose Adj |
Side Effects |
Do Not Use With |
Also |
|---|---|---|---|---|
| Abacavir (ABC) | Hepatic dysfunction | ↑ LDL/TG ↑ risk MI |
Tenofovir Disoproxil Fumarate | Requires testing for HLA B5701 |
| Emtricitabine (FTC) | Renal | Rash, insomnia, rhabdo, hyperpigmentation in palms/soles | Lamivudine | Active against HBV |
| Lamivudine (3TC) | Renal | Nausea, HA, neuropathy, neutropenia, rash | Emtricitabine | Active against HBV |
| Tenofovir Alafenamide (TAF) | Discontinue if CrCl < 15 | ↑ lipids | AED's may ↑ levels | Tx of choice for HBV |
| Tenofovir Disoproxil Fumarate (TDF) | Renal | N/V, ↑ LFTs, ↑ CK, renal dysfunction, bone density loss | Abacavir | Active against HBV |
NRTI Additional Information
- Patients with HIV-HBV coinfection should be on a regimen with 2 NRTIs for adequate control of HBV (usually Tenofovir + emtricitabine). Abrupt discontinuation of this regimen can lead to HBV reactivation, which can be fatal.
- Class-wide side effect: Lactic acidosis, steatosis and lipoatrophy (though very rare with contemporary NRTIs)
- Resistance: M184V confers high resistance to emtricitabine and lamivudine, mid-level resistance to abacavir, but causes a hyper susceptibility to tenofovir
Integrase Inh. |
Renal Adj. |
Side Effects |
Major DDI |
Also |
|---|---|---|---|---|
| Raltegravir (RAL) | None | ↑ ALT | Rifampin, AED's | Do not crush |
| Dolutegravir (DTG) (Tivicay®) |
None | Hyperglycemia Weight gain |
Rifampin, Efavirenz ↑ Metformin |
Avoid w/ laxatives, sucralfate, Fe, Ca May ↑Cr w/o effect on renal function |
NNRTIs |
Hepatic Adjustment |
Side Effects |
Major DDI |
Also |
|---|---|---|---|---|
| Efavirenz | Stop if Child Pugh B/C |
Psychosis, vivid dreams, SI, mania, seizures; ↑ Lipids & glucose |
Azoles, antifungals, clopidogrel, some statins, clarithromycin, Buprenorphine |
Give before meals; discontinue if rash develops |
| Etravirine (ETR) | Use caution |
Hypersensitivity ↑ Lipids & glucose |
Clopidogrel, clarithromycin |
Give after meals |
| Nevirapine (NVP) | Stop if Child Pugh B/C | Steven Johnson Syndrome |
Azoles, OCP's, statins, clarithromycin |
Don't start if CD4 >250 in women, CD4 >400 in men; Don't admin with antacids |
| Rilpivirine (RPV) | None | Depressive disorders, SI, QT prolongation |
AED's, PPI's, dexamethasone |
Must be taken with full meal; NOT for HIV RNA >100k + CD4 <200; No antacids |
NNRTI Additional Information
- Class-wide side effect: hepatitis, rashes
- Resistance: K103N resistance to efavirenz and nevirapine
Protease Inhibitors |
Hepatic Dose Adj |
Side Effects |
Major DDI |
Special Points |
|---|---|---|---|---|
| Atazanavir (ATV) | Based on Childs Pugh |
Jaundice, Kidney stones, AV block, Pancreatitis, Rhabdomyolysis |
CYP3A4 Inhibitors PPI and H2 blockers |
Admin w/ meals |
| Darunavir (DRV) | CI in severe hepatic impairment |
Rashes Pancreatitis |
CYP3A4 Inhibitors Azoles can be used cautiously with drug level monitoring |
Stop if rash |
| Lopinavir (LPV) | None |
AV block, QT changes Pancreatitis Hepatitis |
CYP3A4 Inhibitors | Admin w/ meals |
Protease Inhibitor Additional Information
- All protease inhibitors must be boosted with one of the following:
- Ritonavir: can cause MSK pain, rhabdomyolysis, although not expected at usual doses
- Cobicistat: may increase Cr without effect on renal function
- Class-wide side effects: hepatitis, hypersensitivity reactions, increased cholesterol/TG, hyperglycemia, GI upset, lipodystrophy