Product Information
Registration Status: ActiveSIN11152P
ZEFFIX TABLET 100mg is approved to be sold in Singapore with effective from 1999-06-10. It is marketed by GLAXOSMITHKLINE PTE LTD, with the registration number of SIN11152P.
This product contains Lamivudine 100mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by Glaxo Wellcome Operations in UNITED KINGDOM,GlaxoSmithKline Australia Pty Ltd (primary and secondary packager) in AUSTRALIA, andGlaxoSmithKline Pharmaceuticals S.A. in POLAND.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
A reverse transcriptase inhibitor and zalcitabine analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat Human Immunodeficiency Virus Type 1 (HIV-1) and hepatitis B (HBV).
Indication
For the treatment of HIV infection and chronic hepatitis B (HBV).
Mechanism of Action
Lamivudine is a synthetic nucleoside analogue and is phosphorylated intracellularly to its active 5'-triphosphate metabolite, lamivudine triphosphate (L-TP). This nucleoside analogue is incorporated into viral DNA by HIV reverse transcriptase and HBV polymerase, resulting in DNA chain termination.
Pharmacokinetics
- Absorption
- Lamivudine was rapidly absorbed after oral administration in HIV-infected patients. Absolute bioavailability in 12 adult patients was 86% ± 16% (mean ± SD) for the 150-mg tablet and 87% ± 13% for the oral solution. The peak serum lamivudine concentration (Cmax) was 1.5 ± 0.5 mcg/mL when an oral dose of 2 mg/kg twice a day was given to HIV-1 patients. When given with food, absorption is slower, compared to the fasted state.
- Distribution
- Apparent volume of distribution, IV administration = 1.3 ± 0.4 L/kg. Volume of distribution was independent of dose and did not correlate with body weight.
- Metabolism
- Metabolism of lamivudine is a minor route of elimination. In man, the only known metabolite of lamivudine is the trans-sulfoxide metabolite. This biotransformation is catalyzed by sulfotransferases.
- Elimination
Clearance
* Renal clearance = 199.7 ± 56.9 mL/min [300 mg oral dose, healthy subjects] * Renal clearance = 280.4 ± 75.2 mL/min [single IV dose, HIV-1-infected patients] * Total clearance = 398.5 ± 69.1 mL/min [HIV-1-infected patients]
Toxicity
The most common reported adverse reactions (incidence ≥15%) in adults were headache, nausea, malaise and fatigue, nasal signs and symptoms, diarrhea, and cough.
Active Ingredient/Synonyms
(-)-1-((2R,5S)-2-(Hydroxymethyl)-1,3-oxathiolan-5-yl)cytosine | (-)-2'-Deoxy-3'-thiacytidine | 2',3'-Dideoxy-3'-thiacytidine | 3'-Thia-2',3'-dideoxycytidine | 3TC | beta-L-2',3'-Dideoxy-3'-thiacytidine | beta-L-3'-Thia-2',3'-dideoxycytidine | Lamivudin | Lamivudina | Lamivudine | Lamivudinum | Lamivudine |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.