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lamivudine (3TC, Epivir)

Tradename: Epivir. Indications: 1) treatment of HIV infection - used in combination with zidovudine (AZT)* - in combination with zidovudine * lopinavir/ritonavir may be treatment of choice for pregnant women with HIV1 [6] 2) post HIV exposure prophylaxis 3) treatment of chronic hepatitis B infection* * entecavir is preferred vs lamivudine - more effective than lamivudine (about 10%) [8] - with higher barrier to resistance than lamivudine [9] Dosage: 1) may be administered with or without food 2) HIV infection* a) 150 mg PO BID (> 50 kg) b) 2 mg/kg PO BID (< 50 kg) 3) chronic hepatitis B infection a) 100 mg PO QD b) patient should be established as HIV negative prior to use at this dose * Must be used with AZT (zidovudine). Dose adjustment for renal impairment: creatinine clearance recommended dosage > 50 mL/min 150 mg BID 30-49 mL/min 150 mg QD 15-29 mL/min 150 mg 1st dose, then 100 mg QD 5-14 mL/min 150 mg 1st dose, then 50 mg QD < 5 mL/min* 50 mg 1st dose, then 25 mg QD * dose after hemodialysis Pharmacokinetics: 1) rapidly absorbed following oral administration 2) bioavailability is 80% 3) 3TC penetrates the blood brain barrier into the CSF 4) 1/2life is approximately 2.5 hours; 5-7 hours [4] (15-35 hours ESRD) [4] 5) 70% is eliminated unchanged into the urine Monitor: 1) amylase 2) bilirubin 3) serum transaminases (serum ALT, serum AST) a) monitor for 6 months after discontinuation in patients with hepatitis B b) acute exacerbation of hepatitis B may occur after discontinuation [5] 4) complete blood count (CBC) Adverse effects: 1) common (> 10%) - headache, insomnia, malaise, fatigue, pain, diarrhea, nausea/vomiting, peripheral neuropathy, paresthesia, nasal congestion, cough 2) less common (1-10%) - dizziness, depression, fever/chills, rash, anorexia, abdominal pain, dyspepsia, elevated amylase, neutropenia, anemia, elevated serum transaminases, myalgia, arthralgia 3) uncommon (< 1%) - pancreatitis, thrombocytopenia, hyperbilirubinemia 4) minimal toxicity [7] Drug interactions: 1) lamivudine increases serum concentrations of zidovudine 2) Bactrim decreases lamivudine clearance Laboratory: - lamivudine in serum/plasma Mechanism of action: 1) synthetic cytidine analog 2) inhibits HIV reverse transcriptase 3) has activity against hepatitis B virus [7]

Interactions

drug interactions drug adverse effects of antiretroviral agents

Related

Acquired Immuno-Deficiency Syndrome (HIV infection stage 3, AIDS)

General

nucleoside reverse transcriptase inhibitor (NRTI)

Properties

MISC-INFO: elimination route LIVER KIDNEY pregnancy-category C safety in lactation -

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998 Department of Veterans Affairs, VA National Formulary
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Sanford Guide to antimicrobial therapy 2001
  5. Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: 260704 (subscription needed) http://www.prescribersletter.com
  6. Zuger A Use of Antiretroviral Drugs in Pregnancy. Physician's First Watch, April 22, 2014 David G. Fairchild, MD, MPH, Editor-in-Chief Massachusetts Medical Society http://www.jwatch.org - Panel on Treatment of HIV-Infected Pregnant Women and Prevention of Perinatal Transmission. Recommendations for use of antiretroviral drugs in pregnant HIV-1-infected women for maternal health and interventions to reduce perinatal HIV transmission in the United States. 2014. AIDSinfo. Clinical Guidelines Portal. March 28, 2014. http://aidsinfo.nih.gov/Guidelines/HTML/3/perinatal-guidelines/0 (corresponding NGC guideline withdrawn March 2016)
  7. Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
  8. Chang T-T et al, A comparison of entecavir and lamivudine for HBeAg-positive chronic hepatitis B. New Engl J Med 2006; 354:1001 PMID: 16525137 - Lai C0L et al, Entecavir versus lamivudine for patients with HBeAg-negative chronic hepatitis B. New Engl J Med 2006; 354: 1011 PMID: 16525138 - Hoognagle JH, Hepatitis B - Preventable and now treatable. New Engl J Med 2006; 354:1074 PMID: 16525145
  9. NEJM Knowledge+ Complex Medical Care

Component-of

abacavir/dolutegravir/lamivudine abacavir/lamivudine (Epzicom) abacavir/lamivudine/zidovudine (Trizivir) dolutegravir/lamivudine (Dovato) doravirine/lamivudine/tenofovir efavirenz/lamivudine/tenofovir lamivudine/nevirapine/zidovudine lamivudine/zidovudine (Combivir)