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{{Abacavir lamivudine zidovudine}}
{{CMG}}; {{AE}} {{SS}}
==Overview==
==Category==
Antiretroviral
==US Brand Names==
TRIZIVIR<sup>®</sup>
==FDA Package Insert==
'''  [[Abacavir lamivudine zidovudine description|Description]]'''
'''| [[Abacavir lamivudine zidovudine clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Abacavir lamivudine zidovudine microbiology|Microbiology]]'''
'''| [[Abacavir lamivudine zidovudine indications and usage|Indications and Usage]]'''
'''| [[Abacavir lamivudine zidovudine contraindications|Contraindications]]'''
'''| [[Abacavir lamivudine zidovudine warnings and precautions|Warnings and Precautions]]'''
'''| [[Abacavir lamivudine zidovudine adverse reactions|Adverse Reactions]]'''
'''| [[Abacavir lamivudine zidovudine drug interactions|Drug Interactions]]'''
'''| [[Abacavir lamivudine zidovudine overdosage|Overdosage]]'''
'''| [[Abacavir lamivudine zidovudine clinical studies|Clinical Studies]]'''
'''| [[Abacavir lamivudine zidovudine dosage and administration|Dosage and Administration]]'''
'''| [[Abacavir lamivudine zidovudine how supplied|How Supplied]]'''
'''| [[Abacavir lamivudine zidovudine labels and packages|Labels and Packages]]'''
==Mechanism of Action==
'''Abacavir''': Abacavir is a carbocyclic synthetic nucleoside analogue. Abacavir is converted by cellular enzymes to the active metabolite, carbovir triphosphate (CBV-TP), an analogue of deoxyguanosine-5′-triphosphate (dGTP). CBV-TP inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA. The lack of a 3′-OH group in the incorporated nucleotide analogue prevents the formation of the 5′ to 3′ phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated.  CBV-TP is a weak inhibitor of cellular DNA polymerases α, β, and γ.
'''Lamivudine''': Lamivudine is a synthetic nucleoside analogue. Intracellularly, lamivudine is phosphorylated to its active 5′-triphosphate metabolite, lamivudine triphosphate (3TC-TP). The principal mode of action of 3TC-TP is inhibition of RT via DNA chain termination after incorporation of the nucleotide analogue. 3TC-TP is a weak inhibitor of cellular DNA polymerases α, β, and γ.
'''Zidovudine''': Zidovudine is a synthetic nucleoside analogue. Intracellularly, zidovudine is phosphorylated to its active 5′-triphosphate metabolite, zidovudine triphosphate (ZDV-TP). The principal mode of action of ZDV-TP is inhibition of RT via DNA chain termination after incorporation of the nucleotide analogue. ZDV-TP is a weak inhibitor of the cellular DNA polymerases α and γ and has been reported to be incorporated into the DNA of cells in culture.
==References==
{{Reflist|2}}
[[Category:Antiretroviral]]
[[Category:Wikinfect]]

Latest revision as of 16:07, 9 January 2014

Abacavir lamivudine zidovudine
TRIZIVIR® FDA Package Insert
Description
Clinical Pharmacology
Microbiology
Indications and Usage
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Overdosage
Dosage and Administration
How Supplied
Labels and Packages

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Sheng Shi, M.D. [2]

Overview

Category

Antiretroviral

US Brand Names

TRIZIVIR®

FDA Package Insert

Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Overdosage | Clinical Studies | Dosage and Administration | How Supplied | Labels and Packages

Mechanism of Action

Abacavir: Abacavir is a carbocyclic synthetic nucleoside analogue. Abacavir is converted by cellular enzymes to the active metabolite, carbovir triphosphate (CBV-TP), an analogue of deoxyguanosine-5′-triphosphate (dGTP). CBV-TP inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA. The lack of a 3′-OH group in the incorporated nucleotide analogue prevents the formation of the 5′ to 3′ phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated. CBV-TP is a weak inhibitor of cellular DNA polymerases α, β, and γ.

Lamivudine: Lamivudine is a synthetic nucleoside analogue. Intracellularly, lamivudine is phosphorylated to its active 5′-triphosphate metabolite, lamivudine triphosphate (3TC-TP). The principal mode of action of 3TC-TP is inhibition of RT via DNA chain termination after incorporation of the nucleotide analogue. 3TC-TP is a weak inhibitor of cellular DNA polymerases α, β, and γ.

Zidovudine: Zidovudine is a synthetic nucleoside analogue. Intracellularly, zidovudine is phosphorylated to its active 5′-triphosphate metabolite, zidovudine triphosphate (ZDV-TP). The principal mode of action of ZDV-TP is inhibition of RT via DNA chain termination after incorporation of the nucleotide analogue. ZDV-TP is a weak inhibitor of the cellular DNA polymerases α and γ and has been reported to be incorporated into the DNA of cells in culture.

References