Generic Name (Abbreviation) Trade Name |
Formulations | Dosing Recommendationsa | Elimination/ Metabolic Pathway | Serum Half-Life | Adverse Eventsb |
---|---|---|---|---|---|
Atazanavir (ATV/c) Note: Generic products of ATV are available. |
Reyataz
Generic
Evotaz
|
Reyataz In ARV-Naive Patients
With TDF or in ARV-Experienced Patients
With EFV in ARV-Naive Patients
Evotaz
For dosing recommendations for patients who also are receiving H2 antagonists and PPIs, refer to Table 24a. |
ATV
COBI
Dose adjustment is recommended in patients with hepatic insufficiency (see Appendix B, Table 12). |
7 hours |
Indirect hyperbilirubinemia Cholelithiasis Nephrolithiasis Renal insufficiency Serum transaminase elevations Hyperlipidemia (especially with RTV boosting) Skin rash Hyperglycemia Fat maldistribution An increase in serum creatinine may occur when ATV is administered with COBI. PR interval prolongation: First-degree symptomatic AV block has been reported. Use with caution in patients who have underlying conduction defects or who are on concomitant medications that can cause PR prolongation. |
Darunavir (DRV/c) |
Prezista
Prezcobix
Also available as part of the STR Symtuza (DRV/c/TAF/FTC) |
Prezista In ARV-Naive Patients or ARV-Experienced Patients with No DRV Mutations
In ARV-Experienced Patients with One or More DRV Resistance Mutations
Unboosted DRV is not recommended. Prezcobix
See Appendix B, Table 1 for dosing information for Symtuza. |
DRV
COBI
|
15 hours when combined with RTV 7 hours when combined with COBI |
Hepatotoxicity Diarrhea, nausea Headache Hyperlipidemia Serum transaminase elevation Hyperglycemia Fat maldistribution An increase in serum creatinine may occur when DRV is administered with COBI. Skin rash: DRV has a sulfonamide moiety; however, incidence and severity of rash are similar in those with or without a sulfonamide allergy—Stevens-Johnson syndrome, toxic epidermal necrolysis, acute generalized exanthematous pustulosis, and erythema multiforme have been reported. |
Lopinavir/Ritonavir Note: LPV is only available as a component of an FDC tablet that also contains RTV. |
Kaletra
|
Kaletra
With EFV or NVP in PI-Naive or PI‑Experienced Patients
Food Restrictions Tablet
Oral Solution
|
CYP3A4 inhibitor and substrate |
5–6 hours |
GI intolerance, nausea, vomiting, diarrhea Pancreatitis Asthenia Hyperlipidemia (especially hypertriglyceridemia) Serum transaminase elevation Hyperglycemia Insulin resistance/diabetes mellitus Fat maldistribution Possible increase in the frequency of bleeding episodes in patients with hemophilia PR interval prolongation QT interval prolongation and Torsades de Pointes have been reported; however, causality could not be established. |
Ritonavir Note: Generic is available. Although RTV was initially developed as a PI for HIV treatment, RTV is currently used at a lower dose of 100 mg to 200 mg once or twice daily as a PK enhancer to increase the concentrations of other PIs. |
Norvir
Also available as part of the FDC tablet Kaletra (LPV/r) |
As a PK Booster (or Enhancer) for Other PIs
Food Restrictions
|
CYP3A4 > 2D6 substrate Potent CYP3A4 and 2D6 inhibitor Inducer of UGT1A1 and CYPs 1A2, 2C8, 2C9, and 2C19 |
3–5 hours |
GI intolerance, nausea, vomiting, diarrhea Paresthesia (circumoral and extremities) Hyperlipidemia (especially hypertriglyceridemia) Hepatitis Asthenia Taste perversion Hyperglycemia Fat maldistribution Possible increase in the frequency of bleeding episodes in patients with hemophilia |
a For dose adjustments in patients with hepatic insufficiency, see Appendix B, Table 12. b Also see Table 20. Key: ARV = antiretroviral; ATV = atazanavir; ATV/c = atazanavir/cobicistat; AV = atrioventricular; COBI = cobicistat; CrCl = creatinine clearance; CYP = cytochrome P; DRV = darunavir; DRV/c = darunavir/cobicistat; EFV = efavirenz; FDC = fixed-dose combination; FTC = emtricitabine; GI = gastrointestinal; H2 = histamine H2 receptor; LPV = lopinavir; LPV/r = lopinavir/ritonavir; NVP = nevirapine; PI = protease inhibitor; PK = pharmacokinetic; PO = orally; PPI = proton pump inhibitor; RTV = ritonavir; STR = single-tablet regimen; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate; UGT1 = uridine diphosphate glucuronyl transferase 1 family |