Dosing & Uses
Dosage Forms & Strengths
lamivudine/raltegravir
tablet
- 150mg/300mg
- Approved, but not commercially available in the United States
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
Dosage Modifications
Renal impairment
- CrCl <50 mL/min: Should not be used with moderate-to-severe renal impairment
Hepatic impairment
- Mild-to-moderate: No dose adjustment required
- Decompensated liver disease: Safety and efficacy not established
- Severe: Not studied
Dosage Forms & Strengths
lamivudine/raltegravir
tablet
- 150mg/300mg
- Approved, but not commercially available in the United States
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
Dosage Modifications
Renal impairment
- CrCl <50 mL/min: Should not be used with moderate-to-severe renal impairment
Hepatic impairment
- Mild-to-moderate: No dose adjustment required
- Decompensated liver disease: Safety and efficacy not established
- Severe: Not studied
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (6)
- aluminum hydroxide
aluminum hydroxide decreases levels of raltegravir by cation binding in GI tract. Contraindicated. Not recommended with or without dose separation.
- aluminum hydroxide/magnesium carbonate
aluminum hydroxide/magnesium carbonate will decrease the level or effect of raltegravir by enhancing GI absorption. Applies only to oral form of both agents. Contraindicated. Not recommended with or without dose separation
- aluminum hydroxide/magnesium trisilicate
aluminum hydroxide/magnesium trisilicate will decrease the level or effect of raltegravir by enhancing GI absorption. Applies only to oral form of both agents. Contraindicated. Not recommended with or without dose separation
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
lamivudine, elvitegravir/cobicistat/emtricitabine/tenofovir DF. Other (see comment). Contraindicated. Comment: Elvitegravir/cobicistat/emtricitabine/tenofovir is a complete regimen for HIV and should not be administered with other antiretrovirals.
raltegravir, elvitegravir/cobicistat/emtricitabine/tenofovir DF. Other (see comment). Contraindicated. Comment: Elvitegravir/cobicistat/emtricitabine/tenofovir is a complete regimen for HIV and should not be administered with other antiretrovirals. - emtricitabine
emtricitabine and lamivudine both increase risk of immune reconstitution syndrome. Contraindicated. Coadministration of emtricitabine containing products and lamivudine containing products should be avoided. Combination will result in therapeutic duplication.
emtricitabine, lamivudine. Other (see comment). Contraindicated. Comment: Coadministration of emtricitabine containing products and lamivudine containing products should be avoided. Combination will result in therapeutic duplication. - magnesium supplement
magnesium supplement will decrease the level or effect of raltegravir by Other (see comment). Contraindicated. Drug may form a chelate with polyvalent cations; may decrease absorption by the intestinal tract; applies to oral forms
Serious - Use Alternative (8)
- betibeglogene autotemcel
raltegravir, betibeglogene autotemcel. Other (see comment). Avoid or Use Alternate Drug. Comment: Do not take antiretroviral medications for at least 1 month before mobilization or expected duration for elimination of the medications, and until all cycles of apheresis are completed. Antiretroviral medications may interfere with manufacturing of apheresed cells.
lamivudine, betibeglogene autotemcel. Other (see comment). Avoid or Use Alternate Drug. Comment: Do not take antiretroviral medications for at least 1 month before mobilization or expected duration for elimination of the medications, and until all cycles of apheresis are completed. Antiretroviral medications may interfere with manufacturing of apheresed cells. - cabotegravir
raltegravir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.
lamivudine, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended. - elivaldogene autotemcel
elivaldogene autotemcel, raltegravir. Either decreases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Patients should not take antiretroviral medications for at least 1 month before initiating medications for stem cell mobilization, for the duration of the medications? elimination, and until all cycles of apheresis are completed.
elivaldogene autotemcel, lamivudine. Either decreases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Patients should not take antiretroviral medications for at least 1 month before initiating medications for stem cell mobilization, for the duration of the medications? elimination, and until all cycles of apheresis are completed. - magnesium hydroxide
magnesium hydroxide will decrease the level or effect of raltegravir by cation binding in GI tract. Avoid or Use Alternate Drug. Magnesium containing antacids reduce raltegravir plasma levels when taken within 6 hr of raltegravir dose
- sorbitol
sorbitol will decrease the level or effect of lamivudine by Other (see comment). Avoid or Use Alternate Drug. Sorbitol-containing solution decreased systemic exposure of lamivudine oral solution in a pediatric study (ARROW trial). Results showed lower rates of virologic suppression, lower plasma lamivudine exposure, and development of viral resistance more frequently than children receiving lamivudine tablets.
- sodium sulfate/?magnesium sulfate/potassium chloride
sodium sulfate/?magnesium sulfate/potassium chloride decreases levels of raltegravir by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug.
- sodium sulfate/potassium sulfate/magnesium sulfate
sodium sulfate/potassium sulfate/magnesium sulfate decreases levels of raltegravir by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug.
- tafenoquine
tafenoquine will increase the level or effect of lamivudine by Other (see comment). Avoid or Use Alternate Drug. Tafenoquine inhibits organic cation transporter-2 (OCT2) and multidrug and toxin extrusion (MATE) transporters in vitro. Avoid coadministration with OCT2 or MATE substrates. If coadministration cannot be avoided, monitor for substrate-related toxicities and consider dosage reduction if needed based on product labeling of the coadministered drug.
Monitor Closely (32)
- abacavir
abacavir and lamivudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- apalutamide
apalutamide will decrease the level or effect of raltegravir by increasing elimination. Use Caution/Monitor. Apalutamide induces UGT and may decrease systemic exposure of drugs that are UGT substrates.
- atazanavir
atazanavir and lamivudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- cabozantinib
lamivudine will increase the level or effect of cabozantinib by Other (see comment). Use Caution/Monitor. MRP2 inhibitors increase cabozantinib toxicity
- efavirenz
efavirenz and lamivudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- enfuvirtide
enfuvirtide and lamivudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- erdafitinib
lamivudine increases levels of erdafitinib by decreasing renal clearance. Modify Therapy/Monitor Closely. Consider alternatives that are not OCT2 substrates or consider reducing the dose of OCT2 substrates based on tolerability.
- fosamprenavir
fosamprenavir will decrease the level or effect of raltegravir by unknown mechanism. Use Caution/Monitor.
fosamprenavir and lamivudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor. - ganciclovir
ganciclovir, lamivudine. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Increased risk of hematologic toxicity.
- nirmatrelvir
nirmatrelvir will decrease the level or effect of raltegravir by Other (see comment). Use Caution/Monitor. Raltegravir is an UGT1A1 substrate. Ritonavir induces UGT 1A1.
- indinavir
indinavir and lamivudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- interferon alfa 2b
interferon alfa 2b, lamivudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of liver decompensation.
- nelfinavir
nelfinavir and lamivudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- nevirapine
lamivudine and nevirapine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- nirmatrelvir/ritonavir
nirmatrelvir/ritonavir will decrease the level or effect of raltegravir by Other (see comment). Use Caution/Monitor. Raltegravir is an UGT1A1 substrate. Ritonavir induces UGT 1A1.
- orlistat
orlistat will decrease the level or effect of raltegravir by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Loss of virological control reported in HIV-infected patients taking orlistat concomitantly. Exact mechanism is unclear, but may include a drug-drug interaction that inhibits systemic absorption of the antiretroviral drug. Monitor HIV RNA levels frequently and if increased HIV viral load confirmed, discontinue orlistat.
orlistat will decrease the level or effect of lamivudine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Loss of virological control reported in HIV-infected patients taking orlistat concomitantly. Exact mechanism is unclear, but may include a drug-drug interaction that inhibits systemic absorption of the antiretroviral drug. Monitor HIV RNA levels frequently and if increased HIV viral load confirmed, discontinue orlistat. - peginterferon alfa 2a
peginterferon alfa 2a, lamivudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of liver decompensation.
- rifabutin
rifabutin will decrease the level or effect of raltegravir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Rifabutin induces UGT1A1
- peginterferon alfa 2b
peginterferon alfa 2b, lamivudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of liver decompensation.
- ribavirin
ribavirin increases toxicity of lamivudine by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Use alternatives if available. Increased risk of lactic acidosis.
- rifampin
rifampin decreases levels of raltegravir by increasing hepatic clearance. Use Caution/Monitor.
- ritonavir
ritonavir and lamivudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- saquinavir
saquinavir and lamivudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- selenium
selenium will decrease the level or effect of raltegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer raltegravir at least 2 h before or 6 h after polyvalent cations. Note: Dose separation may not adequately avoid this interaction.
- sodium zirconium cyclosilicate
sodium zirconium cyclosilicate will increase the level or effect of raltegravir by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Check specific recommendations for drugs that exhibit pH-dependent solubility that may affect their systemic exposure and efficacy. In general, administer drugs at least 2 hr before or after sodium zirconium cyclosilicate.
- stavudine
lamivudine and stavudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- tenofovir DF
lamivudine and tenofovir DF both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- tipranavir
tipranavir and lamivudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- trimethoprim
trimethoprim increases effects of lamivudine by basic (cationic) drug competition for renal tubular clearance. Use Caution/Monitor. Potential for increased toxicity.
- ublituximab
ublituximab decreases effects of raltegravir by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely.
ublituximab decreases effects of lamivudine by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. - valganciclovir
valganciclovir, lamivudine. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Use alternatives if available. Increased risk of hematologic toxicity.
- zinc
zinc will decrease the level or effect of raltegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer raltegravir 2 hr before or 6 hr after administration of polyvalent cation containing products.
Minor (3)
- isavuconazonium sulfate
isavuconazonium sulfate will increase the level or effect of lamivudine by Other (see comment). Minor/Significance Unknown. Isavuconazonium sulfate, an OCT2 inhibitor, may increase the effects or levels of OCT2 substrates.
- sulfamethoxazole
sulfamethoxazole increases levels of lamivudine by decreasing renal clearance. Minor/Significance Unknown.
- zidovudine
lamivudine increases effects of zidovudine by pharmacodynamic synergism. Minor/Significance Unknown. Beneficial synergism.
Adverse Effects
>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
<1% (Raltegravir)
Asthenia GI disorders
Lipodystrophy
Skin disorders
Drug related hypersensitivity
Thrombocytopenia
Renal failure
Suicidal ideation
Frequency Not Defined (Lamivudine)
Body fat redistribution
Elevated amylase
Neutropenia
Hepatitis B exacerbation
Postmarketing Reports (Raltegravir)
Cerebellar ataxia
Diarrhea
Hepatic failure
Thrombocytopenia
Rhabdomyolysis
Psychiatric disorders: anxiety, depression (particularly in patients with a pre-existing history of psychiatric illness), including suicidal ideation and behaviors, paranoia
Skin: rash, Steven’s-Johnson syndrome
Warnings
Contraindications
Hypersensitivity
Cautions
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
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
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
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
Pharmacokinetics
Bioavailability: 60% (raltegravir, fasting)
Peak plasma time: 1 hr (raltegravir, fasting)
Once absorbed, lamivudine and raltegravir distribution, metabolism, and excretion are similar to those of the reference components administered individually as described
Administration
Instructions
May take with or without food
Images
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
