Raltegravir Potassium and PKU

• Generic Name: raltegravir
• Dosage Forms: n.a.
• Other Brand Names: Isentress, Isentress HD

Treatment of HIV-1 infection in antiretroviral-naive (have not previously received antiretroviral therapy) or antiretroviral-experienced (previously treated) adults, adolescents, and pediatric patients ≥4 weeks of age; usually used in conjunction with 2 HIV nucleoside reverse transcriptase inhibitors (dual NRTIs).

For initial treatment in antiretroviral-naive adults and adolescents, experts state that raltegravir in conjunction with tenofovir alafenamide and emtricitabine or raltegravir in conjunction with tenofovir disoproxil fumarate (tenofovir DF) and emtricitabine (or lamivudine) are recommended INSTI-based regimens. Raltegravir in conjunction with abacavir and lamivudine (or emtricitabine) is an INSTI-based regimen option for initial treatment when recommended or alternative regimens cannot be used, but use only in those who are human leukocyte antigen (HLA)-B*5701 negative. Raltegravir (twice daily) in conjunction with ritonavir-boosted darunavir is another option for initial treatment in antiretroviral-naive adults and adolescents when recommended or alternative regimens cannot be used, but use only when tenofovir alafenamide, tenofovir DF, or abacavir cannot be used.

For initial treatment in antiretroviral-naive pediatric patients, experts state that an INSTI-based regimen of raltegravir and 2 NRTIs is a preferred regimen in those 2–12 years of age; also recommended as an alternative regimen for initial treatment in infants and children 4 weeks to <2 years of age weighing ≥3 kg.

Fixed combination containing lamivudine and raltegravir (lamivudine/raltegravir; Dutrebis) is used in conjunction with other antiretrovirals in adults, adolescents, and pediatric patients ≥6 years of age.

Postexposure prophylaxis of HIV infection following occupational exposure (PEP) in health-care personnel and others exposed via percutaneous injury (e.g., needlestick, cut with sharp object) or mucous membrane or nonintact skin (e.g., chapped, abraded, dermatitis) contact with blood, tissue, or other body fluids that might contain HIV.

USPHS recommends 3-drug regimen of raltegravir and emtricitabine and tenofovir DF as preferred regimen for PEP following occupational exposures to HIV. Alternative dual NRTIs for use with raltegravir are tenofovir DF and lamivudine, zidovudine and lamivudine, or zidovudine and emtricitabine.

Management of occupational exposures to HIV is complex and evolving; consult infectious disease specialist, clinician with expertise in administration of antiretroviral agents, and/or National Clinicians’ Postexposure Prophylaxis Hotline (PEPline at 888-448-4911) whenever possible. Do not delay initiation of PEP while waiting for expert consultation.

Postexposure prophylaxis of HIV infection following nonoccupational exposure (nPEP) in individuals exposed to blood, genital secretions, or other potentially infectious body fluids that might contain HIV when the exposure represents a substantial risk for HIV transmission. Used in conjunction with other antiretrovirals.

When nPEP indicated in adults and adolescents ≥13 years of age with normal renal function, CDC states preferred regimen is either raltegravir or dolutegravir used in conjunction with emtricitabine and tenofovir DF (given as emtricitabine/tenofovir DF; Truvada); recommended alternative in these patients is ritonavir-boosted darunavir used in conjunction with emtricitabine/tenofovir DF (Truvada).

Consult infectious disease specialist, clinician with expertise in administration of antiretroviral agents, and/or the National Clinicians’ Postexposure Prophylaxis Hotline (PEPline at 888-448-4911) if nPEP indicated in certain exposed individuals (e.g., pregnant women, children, those with medical conditions such as renal impairment) or if considering a regimen not included in CDC guidelines, source virus is known or likely to be resistant to antiretrovirals, or healthcare provider is inexperienced in prescribing antiretrovirals. Do not delay initiation of nPEP while waiting for expert consultation.