Lamivudine - Uses, Dose, Side effects, Brand Names

Lamivudine is commonly called 3TC is an antiviral medicine that is commonly used to treat HIV infection and Hepatitis B infection.

Lamivudine Uses:

  • Chronic hepatitis B (Epivir HBV):

    • Treatment of chronic hepatitis B associated with evidence of hepatitis B viral replication & active liver inflammation
  • Limitations of use:

    • Use only when an alternative antiviral agent with a higher genetic barrier to resistance is not available or appropriate.
    • Lamivudine-HBV has not been evaluated in patients coinfected with HIV, hepatitis C virus, or hepatitis delta virus; with decompensated liver disease; or in liver transplant recipients.
  • Treatment of HIV-1 infection (Epivir):

    • Treatment of HIV-1 in combination with other antiretroviral agents
  • Off Label Use of Lamivudine in Adults:

    • HIV-1 nonoccupational postexposure prophylaxis
    • Prevention of perinatal HIV transmission

Lamivudine Dose in Adults:

Note:

  • The formulation and dosage of Epivir HBV are not appropriate for patients infected with both HBV and HIV; tenofovir and lamivudine are a preferred nucleoside reverse transcriptase inhibitor (NRTI) backbone in a fully suppressive antiretroviral regimen and for the treatment of HBV coinfection.

Lamivudine Dose in the treatment of HIV-1 infection, (Epivir, 3TC [Canadian product]):

  • Oral (use in combination with other antiretroviral agents):
    • 150 mg BD or 300 mg OD

Note:

Lamivudine Dose in the postexposure prophylaxis of HIV-1 nonoccupational (nPEP) (Epivir) (off-label) ( HHS [nPEP] 2016): Oral:

Note:

  • Initiate therapy within 72 hours of exposure and continue for 28 days
  • Use in combination with other antiretroviral agents.
  • CrCl ≥60 mL/minute:

    • Lamivudine is not a component of the recommended antiretroviral regimens for these patients.
  • CrCl <60 mL/minute:

    • The dose should be adjusted according to on renal function.

Lamivudine Dose in the Treatment of hepatitis B (Epivir HBV, Heptovir [Canadian product]):

  • Oral: 100 mg OD
  • Treatment duration (AASLD practice guidelines):

    • Treatment duration for nucleoside nucleotide analog-based therapy (eg, lamivudine) is variable & influenced by HBeAg status, duration of HBV suppression, and presence of cirrhosis/decompensation:
    • Patients without cirrhosis:

      • Hepatitis B e antigen (HBeAg) positive immune-active chronic hepatitis:

        • Treat until HBeAg seroconversion; after seroconversion, prolonged duration of therapy is often required in patients treated with nucleoside/nucleotide analogs.
        • Optimal duration is unknown; however, consolidation therapy is generally a minimum of 12 months of persistently normal ALT & undetectable serum HBV DNA levels after HBeAg seroconversion
      • HBeAg-negative immune-active chronic hepatitis:

        • Indefinite antiviral therapy is suggested unless there is a competing rationale for discontinuation (risk/benefit decision)
        • Treatment discontinuation may be considered in patients with loss of HBsAg
        • However, there is insufficient evidence to guide decisions in these patients.
    • Patients with cirrhosis:

      • HBeAg-positive immune-active chronic hepatitis:

        • In patients who seroconvert on therapy, continue antiviral therapy indefinitely due to concerns with decompensation and death, unless there is a strong competing rationale for discontinuation.
      • HBeAg-negative immune-active chronic hepatitis:

        • Treatment discontinuation is not recommended due to the potential for decompensation & death.
    • Viral breakthrough ( AASLD practice guidelines) :

      • Patients with confirmed viral breakthrough (HBV DNA ≥100 units/mL with previously undetectable levels [<10 units/mL] or >1 log increase in HBV DNA) should either be switched to an alternative antiviral monotherapy agent with a high genetic barrier to resistance or receive a second antiviral agent with a complementary resistance profile
      • Consult current clinical practice guidelines for recommended agents.

Lamivudine Dose in the Treatment of hepatitis B/HIV coinfection (in patients with both infections requiring treatment) (Epivir):

Note:

    • The formulation and dosage of Epivir HBV are not appropriate for patients infected with both HBV and HIV.
    • Tenofovir and lamivudine are a preferred NRTI backbone in a fully suppressive antiretroviral regimen for the treatment of HIV/HBV coinfection.
  • Oral: 150 mg BD or 300 mg OD, in combination with other antiretrovirals in an antiretroviral (ARV) regimen.

Lamivudine Dose in Children:

Note:

  • Oral solution is available in 2 concentrations (10 mg/mL [eg, Epivir] and 5 mg/mL [EpivirHBV])
  • Use extra precaution during calculations to ensure accurate mg of lamivudine administered.
  • Gene mutation and antiretroviral resistance patterns should be evaluated (refer www.IASUSA.org for more information) when necessary.

Lamivudine Dose in the treatment of HIV-1 infection:

  • Use in combination with other antiretroviral agents: Oral:

    • Infants <3 months: Limited data available:

      • Oral solution: 4 mg/kg/dose twice daily.
    • Infants ≥3 months to Children <3 years:

      • Oral solution: 5 mg/kg/dose twice a day
      • Maximum dose: 150 mg/dose
    • Children ≥3 years and Adolescents:

Note:

  • The scored tablet is the preferred formulation in patients weighing ≥14 kg who are able to swallow a solid oral dosage form.
    • Twice-daily dosing:

      • Oral solution:
        • 5 mg/kg/dose twice a day
        • Maximum dose: 150 mg/dose
      • Oral tablet: Weight-band dosing for patients weighing ≥14 kg who are able to swallow tablets (using scored 150 mg tablets):
        • 14 to <20 kg: 75 mg ( / tablet) twice a day
        • 20 to <25 kg: 75 mg ( / tablet) in the morning and 150 mg (1 tablet) in the evening
        • ≥25 kg: 150 mg (1 tablet) twice a day
    • Once-daily dosing:

Note:

  • Not recommended as initial therapy in children.
  • Patients can be transitioned to once-daily treatment with the oral solution or tablet after stable on twice-daily treatment for ≥36 weeks with an undetectable viral load and stable CD4 count.
    • Oral solution:
      • 10 mg/kg/dose once a day
      • Maximum dose: 300 mg/dose
    • Oral tablet: Weight-band dosing for patients ≥14 kg who are able to swallow tablets (scored 150 mg tablets):
      • 14 to <20 kg: 150 mg (1 tablet) OD
      • 20 to <25 kg: 225 mg (1 + / tablet) OD
      • ≥25 kg: 300 mg (2 tablets) OD

Lamivudine Dose in the postexposure prophylaxis of HIV-1 nonoccupational (nPEP):

Note: Initiate therapy within 72 hours of exposure and continue for 28 days in combination with other retroviral agents: Oral:

  • Infants, Children, and Adolescents <16 years:

    • Weight-directed dosing:

      • Oral solution: 4 mg/kg (maximum dose: 150 mg/dose) BD has been recommended
      • However, based on newer pharmacokinetic data, a higher dose of 5 mg/kg/dose twice a day has been recommended for HIV treatment in patients ≥3 months of age.
    • Weight-band dosing:

      • Oral tablet: For patients ≥14 kg who are able to swallow tablets (scored 150 mg tablets):
        • 14 to <20 kg: 75 mg (1/2 tablet) BD
        • 20 to <25 kg: 75 mg (1/2 tablet) in the morning and 150 mg (1 tablet) in the evening
        • ≥25 kg: 150 mg (1 tablet) BD
  • Adolescents ≥16 years: Oral solution or tablet:

    • <50 kg:
      • 4 mg/kg twice a day
      • Maximum dose: 150 mg/dose
    • ≥50 kg:
      • 150 mg BD or 300 mg OD

Lamivudine Dose in the HIV-1 perinatal transmission, empiric therapy in neonates at high risk of transmission (HHS [perinatal] 2018):

Note:

  • Dosing addresses completion of courses initiated at birth
  • If the neonate is diagnosed as HIV positive, discontinue empiric dosing and transition to a treatment regimen and monitoring.
  • Recommended in combination with zidovudine and either raltegravir or nevirapine for empiric treatment of HIV in neonates at higher risk of perinatal transmission; see guidelines for additional information on high-risk definitions.
  • Duration of therapy undefined; some experts have suggested a full 6 weeks of therapy, and others suggest that lamivudine can be discontinued once a negative nucleic acid test (NAT) is returned.
  • Three-drug combination (with zidovudine and either raltegravir or nevirapine): Limited data available:

    • Infants ≤6 weeks:
      • Oral: Oral solution: 4 mg/kg/dose twice daily to complete up to a total duration of lamivudine therapy of 6 weeks.

Lamivudine Dose in the treatment of Hepatitis B, (non-HIV-exposed/-positive):

Note:

  • Use in HBV treatment is discouraged due to rapid resistance development
  • Consider use only if other anti-HBV antiviral regimens with more favorable resistance patterns cannot be used.
  • Epivir HBV:

    • Children ≥2 years and Adolescents:
      • Oral: 3 mg/kg/dose once a day
      • Maximum daily dose: 100 mg/day
  • Heptovir [Canadian product]:

    • Adolescents ≥16 years:
      • Oral: 100 mg once a day
  • AASLD practice guidelines (Lok 2009): Treatment duration:

    • Hepatitis Be antigen (HBeAg) positive chronic hepatitis:

      • Treat ≥1 year until HBeAg confirmed seroconversion and undetectable serum HBV DNA
      • Continue therapy for ≥6 months after HBeAg seroconversion
    • HBeAg negative chronic hepatitis:

      • Treat >1 year until hepatitis B surface antigen (HBsAg) clearance

Note:

  • Patients not achieving <2 log decrease in serum HBV DNA after at least 6 months of therapy should either receive additional treatment or be switched to an alternative therapy

Lamivudine Dose in the Hepatitis B/HIV coinfection, treatment of both infections:

  • Infants, Children, and Adolescents:

    • Dosing should be based on recommendations for the treatment of HIV infection (higher dose) not hepatitis B, as part of an appropriate cART regimen.

Lamivudine Pregnancy Risk Category: C

  • Lamivudine is highly transferable through the human placenta.
  • According to the data from the antiretroviral pregnancy registry, there has not been an increase in overall birth defects after first-trimester exposure.
  • Although maternal antiretroviral treatment (ART) may increase the risk of preterm birth, information is not available due to variability in maternal factors (disease severity and gestational age at therapy initiation).
  • A few studies have shown that stillbirths are more likely than low birth weight and infants of gestational age.
  • Based on data collected by the antiretroviral pregnancy registry, the risk of spontaneous abortions, induced abortions, and preterm birth is less in lamivudine-containing regimens compared with regimens without lamivudine.
  • Maternal ART is an important treatment option that has clear benefits. This should not be delayed due to concern about adverse neonatal outcomes.
  • All infants who have been exposed to antiretroviral medication should be followed up for a long time
  • Potential mitochondrial dysfunction should be considered for children who have significant organ abnormalities of unknown origin (especially the heart or CNS).
  • The use of nucleoside-reverse transcriptase inhibitors has been linked to cases of lactic acidosis, hepatic steatosis, and other complications related to mitochondrial toxicity.
  • These adverse events are very similar to other life-threatening, rare syndromes that can occur during pregnancy (e.g. HELLP syndrome).
  • NRTIs are generally well tolerated and the potential risks outweigh their benefits.
  • The Health and Human Services (HHS) Perinatal HIV Guidelines consider lamivudine a preferred NRTI for HIV infected pregnant females who are antiretroviral-naive, who have had ART therapy in the past but are restarting, who require a new ART regimen (due to poor tolerance or poor virologic response of current regimen), & who are not yet pregnant but are trying to conceive.
  • If lamivudine is well-tolerated and viral suppression is working, then females who get pregnant while on the drug may be able to continue taking it.
  • Pregnancy doesn't affect the pharmacokinetics or dosage adjustment of lamivudine.
  • According to the Health and Human Services (HHS), lamivudine is recommended in combination with abacavir and tenofovir dioproxil fumarate as a preferred NRTI backbone in initial treatment for antiretroviral-naive pregnant women.
  • If pretreatment HIV RNA levels are >100,000. copies/mL, the lamivudine/abacavir-backbone is not recommended.
  • The HHS Perinatal HIV Guidelines also recommend lamivudine with combination of abacavir, dolutegravir as a preferred INSTI regimen in initial treatment for pregnant women who are antiretroviral-naive and present after the first trimester. Dolutegravir combinations are not recommended for pregnant females before 14 weeks gestation, or in females trying to conceive.
  • The guidelines consider lamivudine with zidovudine to be an alternative NRTI backbone for initial therapy in antiretroviral-naive pregnant females.
  • These guidelines recommend that pregnant women with HIV/HBV-coinfected status have lamivudine and tenofovir dioproxil fumarate as a dual NRTI backbone.
  • Take care when you come in contact with hepatitis B coinfection.
  • Hepatitis B flares may occur after discontinuation of lamivudine.
  • To keep HIV-positive pregnant women below the limit of detection and reduce the chance of perinatal transmission, ART should be considered.
  • Pregnancy requires more frequent monitoring than non-pregnant women.
  • All HIV-positive women should continue ART after giving birth. ART can also be modified once the baby is born.
  • The AASLD chronic Hepatitis B treatment recommendations for HBsAg-positive pregnant ladies with HBV DNA >200,000 units/mL recommend antiviral therapy.
  • The level of HBV DNA in the blood is not known. A conservative recommendation is that it be >200,000 units/mL.
  • The AASLD advises against antiviral treatment to reduce the risk for perinatal transmission in pregnant HBsAg-positive women with HBV DNA levels =200,000 units/mL.
  • Lamivudine, one of the antivirals being studied in pregnant women is an example.
  • Most studies initiate antiviral treatment at 28 to 32 week gestation and discontinue antiviral therapy within 3 months. Monitor for ALT flares every 3 month for 6 months after discontinuation.
  • Long-term safety data for infants born to mothers who received antiviral drugs during pregnancy is not available.

Lamivudine use during breastfeeding:

  • Lamivudine can be found in breast milk, and in the serums of nursing infants.
  • Postnatal HIV transmission is not completely eliminated by infant or maternal antiretroviral treatment.
  • The multiclass-resistant virus was also detected in breastfed infants, despite the fact that maternal therapy has not been administered.
  • In the US, where there is a safe and affordable formula and low infant mortality from diarrhea and respiratory infections, it is advised that females with HIV infection stop breastfeeding in order to reduce the possibility of HIV transmission (HHS [perinatal] 2018).
  • Breastfeeding women with hepatitis B (not co-infected with HIV) is not a contraindication.
  • Antivirals are minimally expelled in breast milk and unlikely to cause significant toxicities.
  • Mothers should discuss the unknown risk of low-level infant exposure with their mothers.
  • They also need to be aware of the lack long-term safety data for infants born to mothers who have used antiviral drugs while breastfeeding.

Lamivudine Dose in Kidney Disease:

  • HIV-1 infection:

Note:

  • To avoid using the liquid formulation and because lamivudine is well tolerated, some recommend rounding the recommended daily doses upward to the lowest available tablet strength (100 or 150 mg of lamivudine) in patients with CrCl <30 mL/minute and those on dialysis.
    • CrCl ≥50 mL/minute:

      • Dosage adjustment not necessary.
    • CrCl 30 to 49 mL/minute:

      • Administer 150 mg OD.
    • CrCl 15 to 29 mL/minute:

      • Administer 150 mg first dose, then 100 mg OD.
    • CrCl 5 to 14 mL/minute:

      • Administer 150 mg first dose, then 50 mg OD.
    • CrCl <5 mL/minute:

      • Administer 50 mg first dose, then 25 mg OD.
    • Hemodialysis:

      • Administer 50 mg first dose, then 25 mg OD.
      • Negligible amounts are removed by 4-hour hemodialysis.
      • Supplemental dosing not needed
      • However, dosing after hemodialysis is recommended.
      • Peritoneal dialysis:

        • Administer 50 mg first dose, then 25 mg OD.
        • Negligible amounts are removed by continuous ambulatory peritoneal dialysis (CAPD) or automated peritoneal dialysis (APD).
        • Supplemental dosing not needed.
  • Treatment of hepatitis B patients:

    • CrCl ≥50 mL/minute:

      • Dosage adjustment not necessary.
    • CrCl 30 to 49 mL/minute:

      • Administer 100 mg first dose, then 50 mg OD.
    • CrCl 15 to 29 mL/minute:

      • Administer 100 mg first dose, then 25 mg OD.
    • CrCl 5 to 14 mL/minute:

        • Administer 35 mg first dose, then 15 mg OD.
    • CrCl <5 mL/minute:

      • Administer 35 mg first dose, then 10 mg OD.
    • Hemodialysis:

      • Manufacturer’s prescribing information recommends correcting dosage for the degree of renal impairment; assuming CrCl <5 mL/minute, administer 35 mg first dose, then 10 mg OD.
      • Negligible amounts are removed by 4-hour hemodialysis.
      • Supplemental dosing not needed
      • However, dosing after hemodialysis is recommended by some experts.
    • Peritoneal dialysis:

      • Manufacturer’s prescribing information recommends correcting the dosage for the degree of renal impairment.
      • Assuming CrCl <5 mL/minute, administer 35 mg first dose, then 10 mg OD
      • Negligible amounts are removed by CAPD or APD.
      • Supplemental dosing not needed.

Lamivudine Dose in Liver disease:

  • Dosage adjustment not necessary.
  • However, it has not been studied in the setting of decompensated liver disease.

Incidence data include patients on combination therapy with other antiretroviral agents.

Common Side Effects of Lamivudine:

  • Central Nervous System:

    • Headache
    • Fatigue
    • Malaise
    • Paresthesia
    • Peripheral Neuropathy
    • Neuropathy
    • Insomnia
    • Sleep Disorder
  • Dermatologic:

    • Skin Rash
  • Gastrointestinal:

    • Nausea
    • Diarrhea
    • Pancreatitis
    • Sore Throat
    • Vomiting
  • Hematologic & Oncologic:

    • Neutropenia
  • Hepatic:

    • Increased Serum Alanine Aminotransferase
    • Hepatomegaly
  • Infection:

    • Infection
  • Neuromuscular & Skeletal:

    • Musculoskeletal Pain
  • Respiratory:

    • Nasal Signs And Symptoms
    • Cough
  • Miscellaneous:

    • Fever

Less Common Side Effects Of Lamivudine:

  • Central Nervous System:

    • Dizziness
    • Chills
    • Depression
  • Endocrine & Metabolic:

    • Increased Amylase
  • Gastrointestinal:

    • Increased Serum Lipase
    • Anorexia
    • Decreased Appetite
    • Abdominal Pain
    • Abdominal Cramps
    • Stomatitis
    • Dyspepsia
  • Hematologic & Oncologic:

    • Lymphadenopathy
    • Splenomegaly
    • Thrombocytopenia
    • Decreased Hemoglobin
  • Hepatic:

    • Increased Serum Aspartate Aminotransferase
  • Neuromuscular & Skeletal:

    • Increased Creatine Phosphokinase
    • Myalgia
    • Arthralgia
  • Otic:

    • Ear Disease
  • Respiratory:

    • Abnormal Breath Sounds
    • Wheezing

Contraindications to Lamivudine:

  • Hypersensitivity to lamivudine and any component of the formulation

Warnings and precautions

  • Immune reconstitution syndrome:

    • The immune reconstitution syndrome may occur in patients who have received HIV treatment.
    • This can lead to an indolent or persistent opportunistic HIV infection. Patients might also develop autoimmune disorders such as Graves disease or polymyositis. These conditions require further treatment.
  • Hepatomegaly and lactic acidosis:

    • Patients who have developed severe hepatomegaly and steatosis due to lactic acidosis with nucleoside analogues have been diagnosed. T
    • reatment should be stopped for any patient with clinical or laboratory signs that suggest lactic acidosis.
    • Patients at high risk for liver disease should be cautious.
  • Pancreatitis

    • This has been observed in HIV-infected children with a history nucleoside abuse.
    • Treatment should be stopped if you experience pancreatitis symptoms.
  • Chronic Hepatitis B: [US-Boxed Warning]

    • Patients with HBV/HIV/HBV coinfection have reported severe acute exacerbations (some fatal) of hepatitis B.
    • It is important to monitor the liver function closely, with both laboratory and clinical follow-up, for at least a few months after stopping treatment.
    • If clinically indicated, initiate anti-hepatitis B medication (HBV).
  • Renal impairment

    • Patients with impaired renal function should be cautious
    • Recommendations for dosage reduction
  • Resistance

    • HIV: [US Boxed Warning]

      • HIV-1 resistance can develop in patients with chronic hepatitis B who have untreated or not yet diagnosed HIV-1 infection.
      • All patients should receive counseling and HIV testing before starting treatment with lamivudine to treat hepatitis B, and then every so often during treatment.
      • If used to treat HIV-1 infection, Lamivudine doses for hepatitis B are subtherapeutic.
      • HIV-1 treatment with monotherapy of Lamivudine is not possible using Lamivudine alone.
      • If untreated HIV-1 infection is not recognized or treated, or if the patient has been infected with HBV during treatment, Lamivudine resistance HIV-1 may develop quickly and limit treatment options.
      • Subtherapeutic use of Lamivudine for hepatitis B can also be used for HIV1/HBV coinfection treatment.
      • When lamivudine treatment is being offered to HIV-1 patients who are coinfected, it should be combined with other drugs in a combination that works.
    • HBV (Hepatitis B Virus):

      • Patients who were treated with lamivudine HBV with YMDD mutational HBV had a decreased treatment response (lower rates for HBeAg seroconversion & loss, more frequent return to positive HBV DNA, and more frequent ALT elevations than patients with no evidence of YMDD substitutions).
      • The emergence of lamivudine-resistant HBV variants has also been reported in HIV-1/HBV coinfected patients who received lamivudine-containing antiretroviral regimens.

Lamivudine: Drug Interaction

Risk Factor C (Monitor therapy)

Cabozantinib

MRP2 Inhibitors may increase the serum concentration of Cabozantinib.

Orlistat

May decrease the serum concentration of Antiretroviral Agents.

Trimethoprim

May increase the serum concentration of LamiVUDine.

Risk Factor D (Consider therapy modification)

Sorbitol

May decrease the serum concentration of LamiVUDine. Management: When possible, avoid chronic coadministration of sorbitol-containing solutions with lamivudine, but if this combination cannot be avoided, monitor patients more closely for possible therapeutic failure associated with decreased lamivudine exposure.

Risk Factor X (Avoid combination)

Cladribine

Agents that Undergo Intracellular Phosphorylation may diminish the therapeutic effect of Cladribine.

Emtricitabine

LamiVUDine may enhance the adverse/toxic effect of Emtricitabine.

 

Monitoring parameters:

Manufacturer’s labeling:

  • All patients:

    • Liver function
    • Signs/symptoms of lactic acidosis
    • Signs/symptoms of pancreatitis
  • HIV patients:

    • Coinfection with HBV (prior to therapy)
      • HIV viral load and CD4 count
      • Immune reconstitution syndrome
  • Hepatitis B patients:

    • Coinfection with HIV (prior to therapy);
    • Following discontinuation, monitor hepatic function closely with both clinical and laboratory follow/up for signs and symptoms of HBV relapse and exacerbation (continue for at least several months after stopping treatment)

Alternate recommendations:

  • Chronic Hepatitis B:

    • HBV DNA and ALT (HBV DNA usually done every 3 months until undetectable and then every 3 to 6 months thereafter)
    • HBeAg
    • Anti-HBe (in patients who are HBeAg-positive to monitor for seroconversion)
    • HBsAg
    • During therapy, consider monitoring amylase (if symptoms of pancreatitis) and lactic acid levels (if clinical concern)
    • Following discontinuation, monitor for recurrent viremia, ALT flares, seroreversion, and clinical decompensation every 3 months for at least 1 year
    • As antivirals do not eliminate the risk of hepatocellular carcinoma, continued monitoring for this complication is recommended in at-risk patients.

How to administer Lamivudine?

  • Oral:
  • It may be administered without regard to meals.

Mechanism of action of Lamivudine:

  • Lamivudine can be used as an analog of cytosine.
  • In vitro, lamivudine has been triphosphorylated. The principal mode of action is the inhibition of HIV reverse transcript via viral DNA chain termination
  • It inhibits reverse transcriptase activities that are DNA-dependent and RNA-dependent DNA polymerase.
  • Hepatitis B causes monophosphate lamivudine to be incorporated into viral DNA by the hepatitis Bvirus polymerase. This results in DNA chain termination.

Absorption:

  • Rapid

Distribution:

  • Into extravascular spaces
  • Children (n=38): CSF concentrations were 14.2% ± 7.9% of the serum concentration.

Protein binding:

  • Plasma: <36%

Metabolism:

  • Minor; only known metabolite is trans-sulfoxide metabolite

Bioavailability:

  • Absolute; Cp decreased with food although AUC not significantly affected
  • Children:
    • Oral solution: 66% ± 26%; relative bioavailability is 40% lower than with tablets
  • Adolescents and Adults:
    • Oral solution: 87% ± 13%; Tablet 150 mg: 86% ± 16%

Half-life:

  • Intracellular: 10 to 15 hours

Elimination:

  • Children 4 months to 14 years: 2 ± 0.6 hours
  • Adults: 5 to 7 hours; increased with renal impairment

Time to peak, plasma:

  • Pediatric patients 0.5 to 17 years: Median: 1.5 hours (range: 0.5 to 4 hours)
  • Adolescents 13 to 17 years: 0.5 to 1 hour
  • Adults:
    • Fed: 3.2 hours
    • Fasted: 0.9 hours

Excretion:

  • Primarily urine (majority as unchanged drug)
  • Weight-corrected oral clearance is highest at age 2 years, then declines from age 2 to 12 years, where values then remain comparable to adult values

International Brands of Lamivudine:

  • Epivir
  • Epivir HBV
  • 3TC
  • APO-LamiVUDine
  • APO-LamiVUDine HBV
  • Heptovir
  • 3TC-HBV
  • Cytivir
  • Epivir
  • Epivir 3TC
  • Glamivir
  • Heplav
  • Heptavir
  • Heptodin
  • Inhavir
  • Koide
  • Ladiwin
  • Lahep
  • Lamid
  • Lamidac
  • Lamidin
  • Lamidine
  • Lamiffix
  • Lamivir
  • Lamone 100
  • Tizacure
  • Valfix
  • Vandex
  • Vicondine
  • Vuclodir
  • Zeffix
  • Zeraffic

Lamivudine Brand Names in Pakistan:

Lamivudine Oral Solution 10 mg

Ladwin Hilton Pharma (Pvt) Limited

 

Lamivudine Tablets 100 mg

Lamidin Nova Med Pharmaceuticals

 

Lamivudine 100 mg Tablets

B-Fix Evergreen Pharmaceuticals Pvt Limited
Becotec Genera Pharmaceuticals
Becotec Genera Pharmaceuticals
Belum Navegal Laboratories
Guide Wilsons Pharmaceuticals
Hepaid Well & Well Pharma (Pvt) Ltd
Lamicot Fassgen Pharmaceuticals
Lamiwel Welmark Pharmaceuticals
Lamiwin Wns Field Pharmaceuticals
Lamrin Pharmedic (Pvt) Ltd.
Lamrin Pharmedic (Pvt) Ltd.
Lamudine English Pharmaceuticals Industries
Lumovid Gray`S Pharmaceuticals
Virogen Gene-Tech Laboratories
Zeffix Glaxosmithkline
Zilam Mass Pharma (Private) Limited