Lamivudine + Raltegravir

Indications

Lamivudine + Raltegravir is used for: HIV Infection

Adult Dose

HIV Infection Indicated for use in combination with other antiretroviral products for the treatment of HIV-1 infection in adults and pediatric patients aged >6 years weighing at >30 kg 1 tablet (150 mg/300 mg) PO BID Hepatic impairment Mild-to-moderate: No dose adjustment required Decompensated liver disease: Safety and efficacy not established Severe: Not studied

Child Dose

HIV Infection Indicated for use in combination with other antiretroviral products for the treatment of HIV-1 infection in adults and pediatric patients aged >6 years weighing at >30 kg <6 years: Safety and efficacy not established >6 years and weight ?30 kg: 1 tablet (150 mg/300 mg) PO BID

Renal Dose

Renal impairment CrCl <50 mL/min: Should not be used with moderate-to-severe renal impairment

Administration

May take with or without food

Contra Indications

Hypersensitivity

Precautions

Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of NRTIs alone or in combination, including lamivudine and other antiretrovirals Post-treatment exacerbations of hepatitis in patients with HIV-1 and hepatitis B virus coinfection reported Pancreatitis reported; use with caution in pediatric patients with a history or prior antiretroviral nucleoside exposure, a history of pancreatitis, or other risk factors for pancreatitis; discontinue immediately if signs or symptoms of pancreatitis occur Hepatic decompensation reported with used with interferon- or ribavirin-based regimens; ribavirin can reduce the phosphorylation of pyrimidine NRTIs such as lamivudine Severe, potentially life-threatening, and fatal skin reactions reported with raltegravir, including Stevens-Johnson syndrome and toxic epidermal necrolysis; hypersensitivity reactions have also been reported and were characterized by rash, constitutional findings, and sometimes, organ dysfunction, including hepatic failure; discontinue if signs or symptoms occur Immune reconstitution syndrome reported with combination antiretroviral therapy and may include an inflammatory response to indolent or residual opportunistic infections or emergence of autoimmune disorders (eg, Grave disease, polymyositis, Guillain-Barré syndrome) Redistribution/accumulation of body fat including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and “cushingoid appearance” reported with ARTs Not recommended in combination with products containing the individual components (ie, lamivudine and raltegravir) or emtricitabine

Pregnancy-Lactation

Pregnancy Category: C Lactation: Breastfeeding is not recommended while taking lamivudine/raltegravir; additionally it is recommended that HIV-1 infected mothers not breastfeed their infants to avoid risking postnatal transmission of HIV-1

Interactions

Adverse Effects

Side effects of Lamivudine + Raltegravir : >10% (Lamivudine) Cough Diarrhea Fatigue and malaise Fever (pediatric) Headache Musculoskeletal pain Nausea Nervous system neuropathy Pancreatitis Peripheral neuropathy Nasal S/S Vomiting >10% (Raltegravir) Total cholesterol increased (16%) 1-10% (Lamivudine) Abdominal cramps, abdominal pain Anorexia and/or decreased appetite Arthralgia Chills Depression Dizziness Dyspepsia Insomnia Myalgia Rash Thrombocytopenia Creatine phosphokinase increased 1-10% (Raltegravir) AST increased (9%) Glucose increased (9%) Hyperbilirubinemia (9%) Fatigue (8%) Nasopharyngitis (6%) Abdominal pain (5%) Cough (5%) Rash (5%) Dizziness (4%) Insomnia (4%) Vomiting (4%) Arthralgia (3%) Extremity pain (3%) Influenza (3%) Nausea Diarrhea Pyrexia

Mechanism of Action

Lamivudine: Nucleoside reverse transcriptase inhibitor (NRTI); following phosphorylation, inhibits HIV reverse transcriptase by viral DNA chain termination; cytosine analog Raltegravir: Integrase inhibitor; inhibits catalytic activity of HIV-1 integrase, an HIV encoded enzyme required for viral replication