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Drugs reference index «Lamivudine (3TC)»

Lamivudine

( 3TC ) Pronunciation: (la-MIV-ue-deen)Class: Nucleoside reverse transcriptase inhibitor

Trade Names:Epivir- Tablets 150 mg- Tablets 300 mg- Solution, oral 10 mg/mL

Trade Names:Epivir-HBV- Tablets 100 mg- Solution, oral 5 mg/mL

Heptovir (Canada)

Pharmacology

Inhibits replication of HIV and hepatitis B virus (HBV).

Pharmacokinetics

Absorption

C max is approximately 1.28 mcg/mL (single dose of 100 mg). T max is 0.5 to 2 h. Absolute bioavailability is approximately 87%.

Distribution

Less than 36% protein bound. Vd is approximately 1.3 L/kg.

Metabolism

Metabolism of lamivudine is a minor route of elimination. The metabolite is trans-sulfoxide metabolite.

Elimination

The majority is eliminated unchanged in the urine. Mean half-life is 5 to 7 h. Cl is approximately 398.5 mL/min.

Special Populations

Renal Function Impairment

AUC, C max , and half-life are increased. It is recommended that dosage be modified in these patients.

Hepatic Function Impairment

Pharmacokinetics not altered by hepatic function impairment; therefore, dosage adjustment is not required.

Indications and Usage

Epivir

In combination with other antiretroviral agents for the treatment of HIV infection.

Epivir-HBV

Treatment of chronic hepatitis B associated with evidence of hepatitis B viral replication and active liver inflammation.

Contraindications

Standard considerations.

Dosage and Administration

HIV Infection ( Epivir )Adults and Children older than 16 yr of age

PO 150 mg twice daily or 300 mg once daily in combination with other antiretroviral agents.

Children 3 mo to 16 yr of age

PO 4 mg/kg twice daily (max, 150 mg twice daily) in combination with other antiretroviral agents. Dosage adjustment needed in patients with renal function impairment.

Chronic Hepatitis B ( Epivir-HBV )Adults

PO 100 mg/day. Safety and efficacy of treatment longer than 1 yr not established.

Children 2 to 17 yr of age

PO 3 mg/kg/day (max, 100 mg/day). Safety and efficacy of treatment longer than 1 yr not established.

Dosage Adjustments of Epivir in Renal Function ImpairmentAdults and Adolescents Epivir

Patients weighing 30 kg or more:

CrCl 50 mL/min or more

PO 150 mg twice daily or 300 mg once daily.

CrCl 30 to 49 mL/min

PO 150 mg once daily.

CrCl 15 to 29 mL/min

PO 150 mg first dose, then 100 mg once daily.

CrCl 5 to 14 mL/min

PO 150 mg first dose, then 50 mg once daily.

CrCl less than 5 mL/min

PO 50 mg first dose, then 25 mg once daily.

No additional dosing is needed after routine (4-h) hemodialysis or peritoneal dialysis. There are insufficient data to recommend a specific dose adjustment in children with renal function impairment; however, a reduction in dose and/or an increase in the dosing interval should be considered.

Dosage Adjustments of Epivir-HBV in Renal Function ImpairmentAdults Epivir-HBV CrCl at least 50 mL/min

PO 100 mg/day.

CrCl 30 to 49 mL/min

PO 100 mg first dose, then 50 mg/day.

CrCl 15 to 29 mL/min

PO 100 mg first dose, then 25 mg/day.

CrCl 5 to 14 mL/min

PO 35 mg first dose, then 15 mg/day.

CrCl less than 5 mL/min

PO 35 mg first dose, then 10 mg/day.

Storage/Stability

Store Epivir oral solution at 77°F and tablets at controlled room temperature (59° to 86°F). Keep oral solution tightly closed. Store Epivir-HBV tablets between 59° and 86°F and oral solution between 68° and 77°F. Keep containers tightly closed.

Drug Interactions

Drugs with active renal secretion via the organic cationic transport system (eg, trimethoprim)

Lamivudine Cl may be reduced, increasing plasma concentrations.

Interferon- and ribavirin-based regimens

Risk of hepatic decompensation may be increased.

Zalcitabine

Lamivudine and zalcitabine may inhibit the intracellular phosphorylation of one another. Use in combination is not recommended.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Unless otherwise stated, the following adverse reactions were reported in patients receiving lamivudine in combination with zidovudine for HIV infection or during postmarketing.

CNS

Headache (35%); fatigue and malaise (27%); neuropathy (12%); insomnia and other sleep disorders (11%); dizziness (10%); depression (9%); paresthesia, peripheral neuropathy (postmarketing).

Dermatologic

Skin rash (9%); alopecia, pruritus (postmarketing).

Children

Rashes (12%).

EENT

Ear, nose, throat infection (for HBV treatment) (25%); nasal signs and symptoms (20%); sore throat (for HBV treatment) (13%).

Children

Nasal discharge or congestion (8%); ear signs or symptoms including discharge, erythema, pain, swelling (7%).

GI

Nausea (33%); diarrhea (18%); nausea and vomiting (13%); anorexia and/or decreased appetite (10%); abdominal pain (9%); abdominal cramps (6%); dyspepsia (5%); pancreatitis, stomatitis (postmarketing).

Children

Diarrhea, nausea and vomiting (8%); stomatitis (6%); splenomegaly (5%).

Hematologic-Lymphatic

Anemia, lymphadenopathy, splenomegaly (postmarketing).

Children

Lymphadenopathy (9%).

Hepatic

Hepatic steatosis, lactic acidosis, posttreatment exacerbation of hepatitis B (postmarketing).

Children

Hepatomegaly (11%).

Hypersensitivity

Anaphylaxis, urticaria (postmarketing).

Lab Tests

Decreased absolute neutrophil count (ANC), hemoglobin, and platelets; increased ALT, amylase, AST, CPK, and bilirubin.

Children

Decreased ANC, hemoglobin, and platelets; increased ALT, AST, lipase, and total amylase.

Metabolic-Nutritional

Hyperglycemia, redistribution/accumulation of body fat (postmarketing).

Musculoskeletal

Musculoskeletal pain (12%); myalgia (8%); arthralgia (5%; for HBV treatment, 7%); muscle weakness, rhabdomyolysis (postmarketing).

Respiratory

Cough (18%); abnormal breath sounds/wheezing (postmarketing).

Children

Cough (15%); abnormal breath sounds/wheezing (7%).

Miscellaneous

Fever and chills (10%); weakness (postmarketing).

Children

Fever (25%).

Precautions

Warnings

Lactic acidosis with hepatomegaly and steatosis (including fatal cases) has been reported with the use of lamivudine alone or in combination.

Severe acute exacerbations of hepatitis B have been reported in patients who have discontinued lamivudine.

Monitor

Monitor hepatic function closely with both clinical and laboratory follow-up for at least several months after stopping lamivudine. Monitor patients being treated for chronic hepatitis B for loss of therapeutic response, which may affect advisability of continuing therapy.

Pregnancy

Category C .

Lactation

Excreted in breast milk. HIV-infected mothers should not breast-feed their infants.

Children

Epivir-HBV Hepatitis B

Safety and efficacy in children younger than 2 yr of age not established.

Epivir HIV infection

Safety and efficacy in children younger than 3 mo of age not established.

Elderly

Select dose with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.

Renal Function

Dosage adjustment recommended.

Emtricitabine- or lamivudine-containing products

Lamivudine should not be used in combination with other lamivudine- or emtricitabine-containing products.

Fat distribution

Accumulation/redistribution of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and “cushingoid appearance,” has occurred in patients receiving antiretroviral therapy. A causal relationship has not been established.

Hepatic decompensation

Has occurred in HIV/hepatitis C virus coinfected patients receiving combination antiretroviral therapy for HIV and interferon alfa with or without ribavirin. Closely monitor patients for treatment-associated toxicities.

HIV-HBV coinfection

Epivir-HBV tablets and oral solution contain a lower dose of the same active ingredient as Epivir tablets and oral solution (and lamivudine/zidovudine tablets used to treat HIV infection). The formulation and dosage of lamivudine in Epivir-HBV are not appropriate for patients infected with HBV and HIV.

Immune reconstitution syndrome

Has occurred.

Pancreatitis

Reported in patients receiving lamivudine, particularly in HIV-infected children with prior nucleoside exposure.

Posttreatment hepatitis exacerbations

In non–HIV-infected patients treated with lamivudine for chronic hepatitis B, clinical and laboratory evidence of exacerbations of hepatitis have occurred after discontinuing lamivudine.

Resistant HBV

In non–HIV-infected patients treated with lamivudine for chronic hepatitis B, emergence of lamivudine-resistant HBV has been detected and has been associated with diminished treatment response.

Overdosage

Symptoms

Data are limited. No signs or symptoms have been noted in the few cases of overdosage reported.

Patient Information

  • Instruct patient that the lamivudine tablets and oral solution are for oral ingestion only and to take only as prescribed.
  • Instruct patient that lamivudine is not a cure for HIV or HBV infections and that opportunistic infections, and other complications of HIV and HBV infections, may continue to develop.
  • Caution patient or guardian that long-term effects of lamivudine and results from controlled clinical trials evaluating therapeutic effects and adverse reactions are unknown.
  • Inform patient of potential adverse reactions.
  • Instruct patient to notify health care provider if signs of infection, such as a sore throat, fever, cough, or respiratory congestion, occur.
  • Instruct family to notify health care provider of changes in neurological status, such as memory loss or confusion.
  • Advise patient that it may take at least 4 wk for max effect.
  • Warn patient that the risk of transmission of HIV or HBV to others through sexual contact or exposure to the patient's blood is still present. Instruct patient in methods and precautions to prevent transmission of HIV or HBV.
  • Instruct parents or guardians to monitor patient, especially children, for signs and symptoms of pancreatitis.
  • Caution women to discontinue breast-feeding if receiving lamivudine because of the potential for adverse reactions from lamivudine in breast-feeding infants, as well as transmission of the HIV virus.
  • Advise women to notify health care provider if pregnant or planning to become pregnant, because lamivudine is transferred to the fetus through the placenta.
  • Stress the importance of regular exams and laboratory work. Encourage patient to comply with the treatment regimen.
  • Advise patient that Epivir-HBV tablets and oral solution contain a lower dose of the same active ingredient as Epivir oral solution and tablets, and lamivudine/zidovudine tablets. Advise patient not to take Epivir-HBV concurrently with Epivir or lamivudine/zidovudine.
  • Advise patients of the importance of taking lamivudine with combination therapy on a regular dosing schedule and to avoid missing doses.
  • Inform patients that redistribution or accumulation of body fat may occur during treatment with antiretroviral therapy.

Copyright © 2009 Wolters Kluwer Health.

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