Alovudine
Overview of the antiretroviral drug Alovudine
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Overview
Alovudine is an antiretroviral drug used in the treatment of HIV/AIDS. It belongs to the class of nucleoside reverse transcriptase inhibitors (NRTIs), which work by inhibiting the action of reverse transcriptase, an enzyme crucial for the replication of HIV.
Mechanism of Action
Alovudine is a thymidine analog that competes with the natural substrate, thymidine triphosphate, for incorporation into the viral DNA by reverse transcriptase. Once incorporated, it causes chain termination, thereby preventing the synthesis of viral DNA and subsequent replication of the virus.
Pharmacokinetics
Alovudine is administered orally and is absorbed in the gastrointestinal tract. It undergoes intracellular phosphorylation to its active triphosphate form. The drug is primarily excreted by the renal system.
Clinical Use
Alovudine is used in combination with other antiretroviral agents for the treatment of HIV-1 infection. It is not recommended as monotherapy due to the rapid development of resistance.
Side Effects
Common side effects of Alovudine include nausea, headache, and fatigue. More serious adverse effects can include lactic acidosis and hepatomegaly with steatosis.
Resistance
Resistance to Alovudine can develop through mutations in the reverse transcriptase enzyme. These mutations reduce the drug's efficacy, necessitating the use of combination therapy to prevent resistance.
Research and Development
Research is ongoing to improve the efficacy and safety profile of Alovudine, as well as to explore its use in combination with other antiretroviral drugs.
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Contributors: Prab R. Tumpati, MD