Abacavir

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Contents

[edit] BRAND NAMES

[edit] COMBINATION FORMULATIONS

[edit] STRUCTURE

Abacavir.jpg

[edit] MECHANISM OF ACTION

Abacavir (ABC) is a nucleoside analog reverse transcriptase inhibitor(NRTI). It is a guanosine analogue which is phosporylated to the active metabolite, carbovir triphosphate (CBV-TP), an analogue of deoxyguanosine-5 -triphosphate (dGTP) which interferes with HIV viral replication via RNA dependent DNA polymerase.

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.

[edit] INDICATIONS

Abacavir is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection.

[edit] DOSAGE

  • Adults: 600 mg daily, administered as either 300 mg twice daily or 600 mg once daily.
  • Pediatric patients aged 3 months and older: 8 mg/kg twice daily (up to a maximum of 300 mg twice daily)

[edit] DOSAGE FORMS AND STRENGTHS

  • Tablets: 300 mg, scored
  • Oral Solution: 20 mg/mL

[edit] CONTRAINDICATIONS

  • Previously demonstrated hypersensitivity to abacavir.
  • Moderate or severe hepatic impairment

[edit] WARNINGS AND PRECAUTIONS

  • Hypersensitivity: Serious and sometimes fatal hypersensitivity reactions have been associated with Abacavir and other abacavir-containing products.
  • Lactic acidosis and severe hepatomegaly with steatosis have been reported with the use of nucleoside analogues.
  • Immune reconstitution syndrome and redistribution/accumulation of body fat have been reported in patients treated with combination antiretroviral therapy

[edit] INTERACTIONS

  • Ethanol: Decreases elimination of abacavir.
  • Methadone: An increased methadone dose may be required in a small number of patients

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). There are no adequate and well-controlled studies in pregnant women. Abacavir should be used during pregnancy only if the potential benefits outweigh the risk.
  • Nursing Mothers: The Centers for Disease Control and Prevention recommend that HIV-1-infected mothers not breastfeed their infants to avoid risking postnatal transmission of HIV-1 infection. Although it is not known if abacavir is excreted in human milk, abacavir is secreted into the milk of lactating rats. Because of both the potential for HIV-1 transmission and the potential for serious adverse reactions in nursing infants, mothers should be instructed not to breastfeed if they are receiving Abacavir.

[edit] SIDE EFFECTS

The most commonly reported adverse reactions of at least moderate intensity (incidence ≥10%) in adult HIV-1 clinical trials were nausea, headache, malaise and fatigue, nausea and vomiting, and dreams/sleep disorders.


The most commonly reported adverse reactions of at least moderate intensity (incidence ≥5%) in pediatric HIV-1 clinical trials were fever and/or chills, nausea and vomiting, skin rashes, and ear/nose/throat infections

[edit] BIBLIOGRAPHY

[edit] REFERENCES