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Abacavir and Lamivudine

Pronunciation

(a BAK a veer & la MI vyoo deen)

Index Terms

  • Abacavir Sulfate and Lamivudine
  • Lamivudine and Abacavir

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Epzicom: Abacavir 600 mg and lamivudine 300 mg [contains fd&c yellow #6 (sunset yellow)]

Brand Names: U.S.

  • Epzicom

Pharmacologic Category

  • Antiretroviral, Reverse Transcriptase Inhibitor, Nucleoside (Anti-HIV)

Pharmacology

Nucleoside reverse transcriptase inhibitor combination.

Abacavir is a guanosine analogue which is phosphorylated to carbovir triphosphate which interferes with HIV viral RNA-dependent DNA polymerase resulting in inhibition of viral replication.

Lamivudine is a cytosine analog. After lamivudine is triphosphorylated, the principle mode of action is inhibition of HIV reverse transcription via viral DNA chain termination; inhibits RNA-dependent DNA polymerase activities of reverse transcriptase.

Use: Labeled Indications

HIV-1 infection: Treatment of HIV infection in combination with other antiretroviral agents

Contraindications

Hypersensitivity to abacavir, lamivudine, or any component of the formulation; patients who have the HLA-B*5701 allele; moderate or severe hepatic impairment

Canadian labeling: Additional contraindications (not in US labeling): Hepatic impairment (regardless of severity)

Dosing: Adult

HIV-1 treatment: Oral: One tablet (abacavir 600 mg and lamivudine 300 mg) once daily. Note: Abacavir/lamivudine is a component of a recommended initial regimen with dolutegravir for ART treatment-naive patients who are HLA B*5701 negative (HHS [adult] 2015).

Dosing: Pediatric

HIV-1 treatment: Children and Adolescents weighing ≥25 kg: Oral: One tablet (abacavir 600 mg and lamivudine 300 mg) once daily. Note: For patients who are HLA-B*5701 negative, abacavir plus lamivudine is a component of a recommended regimen (with dolutegravir) for all treatment-naive patients and a component of a recommended regimen (with efavirenz or ritonavir boosted atazanavir) for patients with pre-ART plasma HIV RNA <100,000 copies/mL (HHS [pediatric] 2014)

Dosing: Renal Impairment

CrCl ≥50 mL/minute: No dosage adjustment necessary.

CrCl <50 mL/minute: Use is not recommended.

Dosing: Hepatic Impairment

US labeling:

Mild impairment (Child-Pugh class A): Use is not recommended.

Moderate and severe impairment (Child-Pugh class B or C): Use is contraindicated.

Canadian labeling: Use is contraindicated (regardless of severity).

Administration

May be administered with or without food.

Hazardous agent (abacavir); use appropriate precautions for handling and disposal (NIOSH 2014 [group 2]).

Storage

Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

Drug Interactions

Cabozantinib: MRP2 Inhibitors may increase the serum concentration of Cabozantinib. Monitor therapy

Emtricitabine: LamiVUDine may enhance the adverse/toxic effect of Emtricitabine. Avoid combination

Ganciclovir-Valganciclovir: May enhance the adverse/toxic effect of Reverse Transcriptase Inhibitors (Nucleoside). Hematologic toxicity with zidovudine is of particular concern. Ganciclovir-Valganciclovir may increase the serum concentration of Reverse Transcriptase Inhibitors (Nucleoside). Management: Monitor patients receiving any of these combination closely for toxicity of the reverse transcriptase inhibitor. Avoid zidovudine. Intravitreal implants would not be affected. Consider therapy modification

Methadone: May diminish the therapeutic effect of Abacavir. Abacavir may decrease the serum concentration of Methadone. Monitor therapy

Orlistat: May decrease the serum concentration of Antiretroviral Agents. Monitor therapy

Protease Inhibitors: May decrease the serum concentration of Abacavir. Monitor therapy

Ribavirin (Oral Inhalation): May enhance the hepatotoxic effect of Reverse Transcriptase Inhibitors (Nucleoside). Monitor therapy

Ribavirin (Systemic): May enhance the hepatotoxic effect of Reverse Transcriptase Inhibitors (Nucleoside). Monitor therapy

Trimethoprim: May decrease the excretion of LamiVUDine. Monitor therapy

Adverse Reactions

See individual agents as well as other combination products for additional information. Rates of adverse reactions were defined during combination therapy with other antiretrovirals.

1% to 10%:

Central nervous system: Abnormal dreams, anxiety, depression, dizziness, fatigue, headache, insomnia, malaise, migraine, vertigo

Dermatologic: Skin rash

Gastrointestinal: Abdominal pain, diarrhea, gastritis

Hypersensitivity: Hypersensitivity (including multiorgan failure and anaphylaxis; ≤9%; higher incidence in subjects carrying the HLA-B*5701 allele)

Miscellaneous: Fever

<1% (Limited to important or life-threatening): Abnormal breath sounds, alopecia, anemia (including pure red cell aplasia and severe anemias progressing on therapy), aplastic anemia, erythema multiforme, exacerbation of hepatitis B, hepatitis, hyperglycemia, immune reconstitution syndrome, increased creatine phosphokinase, lactic acidosis, liver steatosis, lymphadenopathy, myasthenia, paresthesia, peripheral neuropathy, redistribution of body fat, rhabdomyolysis, seizure, splenomegaly, Stevens-Johnson syndrome, stomatitis, weakness, wheezing

ALERT: U.S. Boxed Warning

Hypersensitivity reactions:

Serious and sometimes fatal hypersensitivity reactions, with multiple organ involvement, have occurred with abacavir, a component of abacavir/lamivudine.

Patients who carry the HLA-B*5701 allele are at a higher risk of a hypersensitivity reaction to abacavir; although, hypersensitivity reactions have occurred in patients who do not carry HLA-B*5701 allele.

Abacavir is contraindicated in patients with a prior hypersensitivity reaction to abacavir and in HLA-B*5701–positive patients. All patients should be screened for the HLA-B*5701 allele prior to initiating therapy with abacavir or reinitiation of therapy with abacavir, unless patients have a previously documented HLA-B*5701 allele assessment. Discontinue abacavir/lamivudine immediately if a hypersensitivity reaction is suspected, regardless of HLA-B*5701 status and even when other diagnoses are possible.

Following a hypersensitivity reaction to abacavir, never restart abacavir or any abacavir-containing product because more severe symptoms, including death, can occur within hours. Similar severe reactions have also occurred rarely following the reintroduction of abacavir-containing products in patients who have no history of abacavir hypersensitivity.

Lactic acidosis and severe hepatomegaly:

Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogues and other antiretrovirals. Discontinue abacavir if clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity occur.

Exacerbations of hepatitis B:

Severe acute exacerbations of hepatitis B have been reported in patients who are co-infected with hepatitis B virus (HBV) and HIV-1 and have discontinued lamivudine, which is 1 component of abacavir/lamivudine. Hepatic function should be closely monitored with both clinical and laboratory follow-up for at least several months in patients who discontinue abacavir/lamivudine and are coinfected with HIV-1 and HBV. If appropriate, initiation of antihepatitis B therapy may be warranted.

Warnings/Precautions

Concerns related to adverse effects:

• Fat redistribution: May cause redistribution of fat (eg, buffalo hump, peripheral wasting with increased abdominal girth, cushingoid appearance).

• Hypersensitivity reactions: [US Boxed Warning]: Serious and sometimes fatal hypersensitivity reactions have occurred with abacavir, a component of abacavir/lamivudine. Patients who carry the HLA-B*5701 allele are at a higher risk for a hypersensitivity reaction to abacavir, although hypersensitivity reactions have occurred in patients who do not carry the HLA-B*5701 allele. All patients should be screened for the HLA-B*5701 allele prior to initiating or reinitiation of therapy unless patients have had a previously documented HLA-B*5701 allele assessment. Discontinue abacavir/lamivudine if a hypersensitivity reaction is suspected. Abacavir is contraindicated in patients who have the HLA-B*5701 allele or in patients with a prior hypersensitivity reaction to abacavir. Reintroduction of any abacavir-containing product can result in life-threatening or fatal hypersensitivity reactions, even in patients who have no history of hypersensitivity to abacavir therapy. Such reactions can occur within hours. An allergy to abacavir should be documented in the medical record of allele-positive patients. Reactions usually occur within 9 days of starting abacavir; ~90% occur within 6 weeks, although these reactions may occur at any time during therapy (HHS [adult] 2015). These reactions usually include signs or symptoms from two or more of the following: Fever, skin rash, constitutional symptoms (malaise, fatigue, aches), respiratory symptoms (eg, pharyngitis, dyspnea, cough), and GI symptoms (eg, abdominal pain, diarrhea, nausea, vomiting). Other signs and symptoms include lethargy, headache, myalgia, edema, abnormal chest x-ray findings, arthralgia and paresthesia. Anaphylaxis, liver failure, renal failure, hypotension, adult respiratory distress syndrome, respiratory failure, myolysis, and death have occurred in association with hypersensitivity reactions. Physical findings (lymphadenopathy, mucous membrane lesions, and rash [maculopapular, urticarial or variable]) may occur. Erythema multiforme has also been reported. Laboratory abnormalities (eg, elevated liver function tests, elevated creatine phosphokinase, elevated creatinine, and lymphopenia) may occur. Abacavir/lamivudine should be permanently discontinued if hypersensitivity cannot be ruled out, even when other diagnoses are possible and regardless of HLA-B*5701 status. Abacavir/lamivudine SHOULD NOT be restarted because more severe symptoms may occur within hours, including LIFE-THREATENING HYPOTENSION AND DEATH. If abacavir/lamivudine is restarted following an interruption in therapy not associated with symptoms of a hypersensitivity reaction, carefully evaluate the patient for previously unsuspected symptoms of hypersensitivity. Do not restart if hypersensitivity is suspected or cannot be ruled out regardless of HLA-B*5701 status. If abacavir/lamivudine is restarted, continually monitor for symptoms of a hypersensitivity reaction. Make the patient aware that reintroduction should only take place if medical care is readily accessible.

• Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment or activation of autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome) later in therapy; further evaluation and treatment may be required.

• Lactic acidosis/hepatomegaly: [US Boxed Warning]: Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogues and other antiretrovirals. Use with caution in patients with risk factors for liver disease (risk may be increased with female gender, obesity, pregnancy or prolonged exposure) and discontinue treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or hepatotoxicity (transaminase elevation may/may not accompany hepatomegaly and steatosis).

Disease-related concerns:

• Coronary heart disease: Use has been associated with an increased risk of myocardial infarction (MI) in observational studies; however, based on a meta-analysis of 26 randomized trials, the FDA has concluded there is not an increased risk. Consider using with caution in patients with risks for coronary heart disease and minimizing modifiable risk factors (eg, hypertension, hyperlipidemia, diabetes mellitus, and smoking) prior to use.

• Chronic hepatitis B: [US Boxed Warning]: Severe acute exacerbations of hepatitis B have been reported in patients who are co-infected with hepatitis B virus (HBV) and HIV-1 and have discontinued lamivudine, which is 1 component of abacavir/lamivudine. Monitor patients closely for several months following discontinuation of therapy for chronic hepatitis B; clinical exacerbations may occur. Lamivudine-resistant HBV variants have been reported in coinfected patients using lamivudine as part of an antiretroviral regimen.

• Hepatic impairment: Due to fixed dose of combination product, use is not recommended with mild hepatic impairment. The US labeling contraindicates use in patients with moderate or severe hepatic impairment. The Canadian labeling contraindicates use in hepatic impairment regardless of severity.

• Renal impairment: Due to fixed dose of combination product, use is not recommended with renal impairment (CrCl <50 mL/minute).

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

• Duplicate therapy: Concomitant use of other abacavir or lamivudine-containing products with the fixed dose combination product should be avoided.

Special handling:

• Hazardous agent: Abacavir is a hazardous agent; use appropriate precautions for handling and disposal (NIOSH 2014 [group 2]).

Other warnings/precautions:

• Appropriate use: Do not use abacavir and lamivudine (plus efavirenz or plus atazanavir/ritonavir) in adolescent and adult HIV-1 patients with a pre-ART HIV RNA >100,000 copies/mL (HHS [adult] 2015).

Monitoring Parameters

Amylase, bilirubin, blood glucose, serum creatine kinase, liver enzymes, hematologic parameters, triglycerides, viral load, and CD4 count; HLA-B*5701 genotype status prior to initiation of therapy; signs and symptoms of hypersensitivity.

Pregnancy Considerations

Animal reproduction studies have not been conducted with this combination. See individual agents. The Department of Health and Human Services (HHS) Perinatal HIV Guidelines consider abacavir in combination with lamivudine to be a preferred nucleoside reverse transcriptase inhibitor (NRTI) backbone for use in antiretroviral-naive pregnant women (do not use in women who are positive for the HLA-B*5701 allele). This backbone is not recommended with atazanavir or efavirenz if pretreatment HIV RNA is >100,000 copies/mL (HHS [perinatal] 2016). See individual agents.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience dizziness, headache, insomnia, loss of strength and energy, nausea, or diarrhea. Have patient report immediately to prescriber signs of allergic reaction with organ failure (fever, rash, fatigue, flu-like signs, nausea, vomiting, diarrhea, abdominal pain, pharyngitis, cough, or difficulty breathing), signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice), signs of lactic acidosis (fast breathing, tachycardia, abnormal heartbeat, vomiting, fatigue, shortness of breath, severe loss of strength and energy, severe dizziness, feeling cold, or muscle pain or cramps), signs of pancreatitis (severe abdominal pain, severe back pain, severe nausea, or vomiting), signs of kidney problems (urinary retention, hematuria, change in amount of urine passed, or weight gain), severe dizziness, passing out, angina, depression, mouth sores, muscle pain, burning or numbness feeling, edema, change in body fat, or signs of infection (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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