lamivudine (3TC, Epivir)
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Introduction
Tradename: Epivir.
Indications
- 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]
- post HIV exposure prophylaxis
- treatment of chronic hepatitis B infection*
* entecavir is preferred vs lamivudine
Dosage
- may be administered with or without food
- HIV infection*
- chronic hepatitis B infection
* 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
- rapidly absorbed following oral administration
- bioavailability is 80%
- 3TC penetrates the blood brain barrier into the CSF
- 1/2life is approximately 2.5 hours; 5-7 hours[4] (15-35 hours ESRD)[4]
- 70% is eliminated unchanged into the urine
elimination via liver
elimination via kidney
Monitor
- amylase
- bilirubin
- serum transaminases (serum ALT, serum AST)
- monitor for 6 months after discontinuation in patients with hepatitis B
- acute exacerbation of hepatitis B may occur after discontinuation[5]
- complete blood count (CBC)
Adverse effects
- common (> 10%)
- less common (1-10%)
- dizziness, depression, fever/chills, rash, anorexia, abdominal pain, dyspepsia, elevated amylase, neutropenia, anemia, elevated serum transaminases, myalgia, arthralgia
- uncommon (< 1%)
- minimal toxicity[7]
Drug interactions
- lamivudine increases serum concentrations of zidovudine
- Bactrim decreases lamivudine clearance
Laboratory
Mechanism of action
- synthetic cytidine analog
- inhibits HIV reverse transcriptase
- has activity against hepatitis B virus[7]
More general terms
Additional terms
Component of
- lamivudine/tenofovir
- doravirine/lamivudine/tenofovir
- dolutegravir/lamivudine (Dovato)
- abacavir/dolutegravir/lamivudine
- lamivudine/zidovudine (Combivir)
- abacavir/lamivudine/zidovudine (Trizivir)
- abacavir/lamivudine (Epzicom)
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ 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
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 4.0 4.1 4.2 Sanford Guide to antimicrobial therapy 2001
- ↑ 5.0 5.1 Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 6.0 6.1 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) - ↑ 7.0 7.1 7.2 Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
- ↑ 8.0 8.1 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: https://www.ncbi.nlm.nih.gov/pubmed/16525137
Lai C0L et al, Entecavir versus lamivudine for patients with HBeAg-negative chronic hepatitis B. New Engl J Med 2006; 354: 1011 PMID: https://www.ncbi.nlm.nih.gov/pubmed/16525138
Hoognagle JH, Hepatitis B - Preventable and now treatable. New Engl J Med 2006; 354:1074 PMID: https://www.ncbi.nlm.nih.gov/pubmed/16525145 - ↑ 9.0 9.1 NEJM Knowledge+ Complex Medical Care