Each film-coated tablet contains 100 mg Lamivudine.
Excipients/Inactive Ingredients: Microcrystalline cellulose, povidone K30, croscarmellose sodium, stearic acid, colloidal anhydrous silica, hypromellose, macrogol 6000, talc, titanium dioxide, red ferric oxide, yellow ferric oxide.
Pharmacotherapeutic group: Antivirals for systemic use, nucleoside and nucleotide reverse transcriptase inhibitors. ATC Code: J05AF05.
Pharmacology: Pharmacodynamics: Lamivudine is converted intracellularly in stages to the triphosphate. This triphosphate halts the DNA synthesis of retroviruses, including HIV, through competitive inhibition of reverse transcriptase and incorporation into viral DNA. Lamivudine is also active against hepatitis B virus.
Pharmacokinetics: Lamivudine is rapidly absorbed after oral doses and peak plasma concentrations are achieved in about 1 hour. Absorption is delayed, but not reduced, by ingestion with food. Bioavailability is between 80 and 87%.
Binding to plasma protein is reported to be up to 36%.
Lamivudine crosses the blood-brain barrier with a ratio of CSF to serum concentrations of about 0.12. It crosses the placenta and is distributed into breast milk.
Lamivudine is metabolised intracellularly to the active antiviral triphosphate. Hepatic metabolism is low and it is cleared mainly unchanged by active renal excretion. An elimination half-life of 5 to 7 hours has been reported after a single dose.
Lamivudine is indicated for the treatment of chronic hepatitis B with: Compensated liver disease with evidence of active viral replication, persistently elevated serum alanine aminotransferase (ALT) levels and histological evidence of active liver inflammation and/or fibrosis.
Decompensated liver disease.
For chronic hepatitis B: The adult dose is 100 mg once daily by mouth. A dose for children aged over 2 years is 3 mg/kg once daily to a maximum daily dose of 100 mg.
Patients with concomitant HIV and hepatitis B infection: The dosage regimen appropriate for HIV should be used.
Administration in renal impairment: Dosage of lamivudine should be reduced in patients with moderate to severe renal impairment (creatinine clearance (CC) below 50 ml/minute).
Adults with chronic hepatitis B infection: CC 30 to 49 ml/minute: 100 mg for the first dose then 50 mg once daily.
CC 15 to 29 ml/minute: 100 mg for the first dose then 25 mg once daily.
CC 5 to 14 ml/minute: 35 mg for the first dose then 15 mg once daily.
CC less than 5 ml/minute: 35 mg for the first dose then 10 mg once daily.
Haemodialysis patients: No further dose adjustment other than in accordance with creatinine clearance is required.
Peritoneal dialysis patients: Not recommended.
Children: Doses should be reduced according to creatinine clearance by the same proportions as in adults.
Method of Administration: Lamone 100 is orally taken without regard to meals.
Administration of lamivudine at very high dose levels in acute animal studies did not result in any organ toxicity. Limited data are available on the consequences of ingestion of acute overdoses in humans. No fatalities occurred, and the patients recovered. No specific signs or symptoms have been identified following such overdose.
If overdose occurs, the patient should be monitored and standard supportive treatment applied as required. Since lamivudine is dialysable, continuous haemodialysis could be used in the treatment of overdose, although this has not been studied.
Hypersensitivity to the active substance or to any of the excipients.
Lamivudine therapy should be stopped in patients who develop abdominal pain, nausea, or vomiting or with abnormal biochemical test results until pancreatitis has been excluded.
Treatment with lamivudine may be associated with lactic acidosis and should be discontinued if there is a rapid increase in aminotransferase concentrations, progressive hepatomegaly, or metabolic or lactic acidosis of unknown aetiology. Lamivudine should be used with caution in patients with hepatomegaly or other risk factors for hepatic disease. In patients with chronic hepatitis B, there is a risk of rebound hepatitis when lamivudine is discontinued, and liver function should be monitored in such patients. The possibility of HIV infection should be excluded before beginning lamivudine therapy for hepatitis B, since the lower doses used to treat the latter may permit the development of lamivudine resistant strains of HIV.
Dosage reduction may be necessary in patients with impaired renal function.
Effects on ability to drive and use machines: None known.
Pregnancy: There are no adequate and controlled studies to date using lamivudine in pregnant women, and the drug should be used during pregnancy only if the potential benefits justify the potential risks to the fetus.
Lactation: Lamivudine is distributed into milk in humans. Because of the potential for serious adverse effects of lamivudine in nursing infants, lactating women receiving lamivudine for the treatment of chronic HBV infection should not breastfeed infants.
Adverse effects commonly associated with lamivudine include abdominal pain, nausea, vomiting, diarrhoea, headache, fever, rash, alopecia, malaise, insomnia, cough, nasal symptoms, arthralgia, and musculoskeletal pain. Patients taking lamivudine for the treatment of chronic hepatitis B commonly also have increased serum levels of creatinine phosphokinase and alanine aminotransferase.
There have been rare instances of rhabdomyolysis. Pancreatitis has been reported rarely. Neutropenia and anaemia (usually when given with zidovudine), thrombocytopenia, and increases in liver enzymes and rare cases of hepatitis have occurred. Lactic acidosis, usually associated with severe hepatomegaly and steatosis, has been reported during treatment with nucleoside reverse transcriptase inhibitors.
The renal excretion of lamivudine may be inhibited by other drugs mainly eliminated by active renal secretion, for example trimethoprim. Usual prophylactic doses of trimethoprim are unlikely to necessitate reductions in lamivudine dosage unless the patient has renal impairment, but the co-administration of lamivudine with the high doses of trimethoprim (as co-trimoxazole) used in pneumocystis pneumonia and toxoplasmosis should be avoided. Although there is usually no clinically significant interaction with zidovudine, severe anaemia has occasionally been reported in patients given lamivudine with zidovudine.
Lamivudine may antagonize the antiviral action of zalcitabine and the two drugs should not be used together. Once daily triple nucleoside regimens of lamivudine and tenofovir with either abacavir or didanosine are associated with a high level of treatment failure and of emergence of resistance, and should be avoided.
Incompatibilities: In the absence of incompatibility studies, this medicinal product must not be mixed with other medicinal products.
Store in a well-closed container, in a dry place. Do not store above 30°C.
Shelf-Life: 36 months from the date of manufacturing.
J05AF05 - lamivudine ; Belongs to the class of nucleoside and nucleotide reverse transcriptase inhibitors. Used in the systemic treatment of viral infections.
FC tab 100 mg (brownish-yellow, caplet-shaped, engraved with logo "Click on icon to see table/diagram/image
" on one side, plain on the other side) x 3 x 10's, 1 x 30's, 100's.