Abacavir Uses Doses Side-effect Contraindication

Abacavir uses an oral drug used for HIV infection. mechanism of abacavir is converting into the active form carbovir triphosphate. Abacavir is in a class of nucleoside reverse transcriptase inhibitors (NRTIs)

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  • Abacavir Classof drug: Antiviral
  • Brand name: Ziagen
  • Storage of drug: At 20-250C

After oral administration rapidly absorbed bioavailability of abacavir is about 80%.

Abacavir is 50% bound to plasma proteins and crosses the blood-brain barrier.

The half-life of abacavir is about 1.5 hr after a single oral dose.

If any person has a severe renal disease or liver disease and a history of hypersensitivity don’t give abacavir.

The main side effect of abacavir is Anorexia, Headache,Β Nausea, Vomiting, Diarrhea, Rash, Fever, Cough, Dyspnoea, Fatigue, Malaise, Lethargy, and Abdominal Pain.

Indication & Dosage:

Abacavir uses is an oral drug used for HIV infection :

  • Adult: Combined with other antiretrovirals: 300 mg bid or 600 mg once daily.
  • Child: Combined with other antiretrovirals: >3 mth: 8 mg/kg bid. Max: 600 mg daily.
  • Renal impairment: Abacavir is avoid end-stage renal disease.
  • Hepatic impairment: Child pugh category A: 200 mg bid. Avoid moderate-severe impairment.

Mechanism of Action:

In intracellular abacavir is converting into the active form carbovir triphosphate. Abacavir competitively inhibits the reverse transcriptase of retroviruses. Which is interfering with HIV viral RNA-dependent DNA polymerase resulting in inhibition of viral replication.

  • Absorption: After oral administration rapidly absorbed bioavailability of abacavir is about 80%.
  • Distribution: Abacavir is 50% bound to plasma proteins and crosses the blood-brain barrier.
  • Metabolism: Undergoes metabolism intracellular to carbovir triphosphate which is the active metabolite.
  • Excretion: Elimination half-life: Abacavir half-life is about 1.5 hr after a single oral dose.Β  The drug abacavir is elimination by hepatic metabolism mainly by alcohol dehydrogenase and glucuronidation. After metabolite abacavir is excreted by the urine.

How to take Abacavir:

The drug may be taken with food and without food.

Contraindications of abacavir:

  • Moderate to severe renal impairment
  • Hepatic impairment
  • End-stage renal disease
  • history of hypersensitivity reactions.
  • Pregnancy and lactation.

Special Precautions about abacavir:

  • Renal or mild liver impairment
  • Risk for liver impairment.
  • Discontinued when hepatomegaly and unexplained metabolic acidosis develop, or liver function deteriorates.
  • May impair the ability to drive or engage in tasks requiring alertness.
  • Discontinue treatment as soon as hypersensitivity is suspect.

The Side effect of abacavir:

  • Anorexia
  • Headache
  • Nausea
  • Vomiting
  • Diarrhea
  • Rash
  • Fever
  • Cough
  • Dyspnoea
  • Fatigue
  • Malaise
  • Lethargy
  • Abdominal pain.
  • Pancreatitis and elevated blood glucose and TG concentrations.

After taking this drug chance of death due to: Severe hypersensitivity reactions.

Abacavir Interactions with another drug:

  • Alcohol may cause decreased elimination of abacavir.
  • Lactic acidosis with nucleoside analogs concomitantly.
  • Decreased serum concentrations of methadone.

In pregnant women, Abacavir can give teratogenic or embryocidal effects.

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