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