lamivudine/raltegravir (Rx)

Brand and Other Names:Dutrebis
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Dosing & Uses

AdultPediatric

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
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Interactions

Interaction Checker

and lamivudine/raltegravir

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            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 (6)

            • 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.

            • 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 (31)

            • 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.

            • 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.

            • 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.

            • 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.

            • 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.

            • rifabutin

              rifabutin will decrease the level or effect of raltegravir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Rifabutin induces UGT1A1

            • 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.

            • 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.

            • zidovudine

              lamivudine and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • 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.

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            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

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            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

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            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.

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            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

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            Administration

            Instructions

            May take with or without food

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            Patient Handout

            A Patient Handout is not currently available for this monograph.
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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.