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Lamivudine
drug data and news
Lamivudine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Lamivudine | ||
| Brand Names/Synonyms | 3TC; Combivir; DRG-0126; Epivir; Epivir-Hbv; GR 109714X; HSDB 7155; Hepitec; Heptovir; LAMIVUDINE; Lamivudine; Lamivudine [Usan:Ban:Inn]; Trizivir; Zeffix | ||
| Indication | For the treatment of HIV infection and chronic hepatitis B (HBV) | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Lamivudine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1) and hepatitis B (HBV). Lamivudine is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. The lack of a 3'-OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated. | ||
| 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. | ||
| Lamivudine News (When available) |
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| Dosage Forms | SOLUTION; TABLET | ||
| Drug_Category | Anti-HIV Agents; Nucleoside and Nucleotide Reverse Transcriptase Inhibitors; ATC:J05AF05 | ||
| Absorption | Lamivudine was rapidly absorbed after oral administration in HIV-infected patients. Absolute bioavailability in adults is 86% ± 16% for the tablet and 87% ± 13% for the oral solution. | ||
| Interactions |
-->Interactions for Lamivudine: Lamivudine is predominantly eliminated in the urine by active organic cationic secretion. The possibility of interactions with other drugs administered concurrently should be considered, particularly when their main route of elimination is active renal secretion via the organic cationic transport system (e.g., trimethoprim). TMP 160 mg/SMX 800 mg once daily has been shown to increase lamivudine exposure (AUC) by 44%. No change in dose of either drug is recommended. There is no information regarding the effect on lamivudine pharmacokinetics of higher doses of TMP/SMX such as those used to treat Pneumocystis carinii pneumonia. No data are available regarding interactions with other drugs that have renal clearance mechanisms similar to that of lamivudine. Lamivudine and zalcitabine may inhibit the intracellular phosphorylation of one another. Therefore, use of lamivudine in combination with zalcitabine is not recommended.
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| Toxicity | Not Available | ||
| Organisms Affected | Human immunodeficiency virus | ||
| Chemical IUPAC Name | 4-amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-1H-pyrimidin-2-one | ||
| Chemical Formula | C8H11N3O3S | ||
| Molecular Weight | 229.257 g/mol | ||
| Smiles String | C1C(OC(S1)CO)N2C=CC(=NC2=O)N | ||
| Melting Point | 160-162 °C | ||
| Water Solubility | 70 mg/ml | ||
| State | Solid | ||
| LogP/Hphobicity | Not Available | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | The only detected metabolite of lamivudine is trans-sulfoxide. | ||
| Half Life | 5 to 7 hours | ||
| Protein Binding [%] | 36% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Lamivudine.html http://www.rxlist.com/cgi/generic3/combivir.htm http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/com1513.shtml | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00681 | ||
| CAS Registry Number | 134678-17-4 | ||
| KEGG Compound ID | C07065 | ||
| PubChem ID | SID:197069 | ||
| PharmGKB ID | PA450163 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2239194 |
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