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Abacavir

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Description

Generic Name

Abacavir

Chemical names

Abacavir, 136470-78-5, Ziagen, Epzicom, Abacavir sulfate

Brand names

Ziagen, Abamune, Viral, Abcavir, Abec

IUPAC name

[(1S, 4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]cyclopent-2-en-1-yl]methanol

Pharmacokinetics

  • Absorption: Orally, Bioavailabilty-83%
  • Distribution: Crosses blood brain barrier, bound to plasma protein 50%
  • Metabolism: Hepatic
  • Elimination: Excreted through urine

Actions

Carbovir triphosphate inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA. Abacavir is converted by cellular enzymes to the active metabolite carbovir triphosphate, it is the analogue of dGTP (deoxyguanosine-5'-triphosphate). Viral DNA growth is terminated because the incorporated nucleotide lacks a 3'-OH group, which is needed to form the 5′ to 3′ phosphodiester linkage essential for DNA chain elongation.

Dosage/Dosage form

  • Ziagen tablets-300 mg oral
  • Ziagen solution 20mg/mL

Therapeutic uses

  • Occupational exposure
  • HIV treatment
  • Non occupational exposure

Adverse effects/Side effects

Fever, cough, anorexia, diarrhea, nausea, vomiting, headache, pancreatitis, fatigue.

Interaction

  • The serum concentration of Abacavir can be decreased when it is combined with the following drugs.
  • 1,10-Phenanthroline
  • 3,4-Dichloroisocoumarin
  • 4-(2-Aminoethyl)benzenesufonyl fluoride
  •  Alogliptin.
  • Amprenavir

Contraindications

During pregnancy and lactation, in patients with renal impairment, hypersensitivity, hepatic impairment.

Storage

Store at 20-25°C.

Information

Molecular weight

286.33

Molecular formula

C14H18N6O

CAS number

136470-78-5

Precautions

  • Take without regard to meals
  • Avoid alcohol because the abacavir partially metabolized through alcohol dehydrogenase enzyme system