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Acyclovir

An oral coagulant drug used in rat poisoning,a symmetrical isocoumarin can be considered as the "parent" of the widely used anticoagulant drug, warfarin. More

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Description

An oral coagulant drug used in rat poisoning,a symmetrical isocoumarin can be considered as the "parent" of the widely used anticoagulant drug, warfarin.

Generic Name

Acyclovir

Chemical names

Acyclovir, Aciclovir, Acycloguanosine

Brand names

Accrivir, Aciherpin, Aciherpin crm, Acirax, Aciv, Acivir injction, Acivir eye ointment, Acivir skin cream, Zovirax.

IUPAC name

2-amino-9-[(2-hydroxyethoxy) methyl]-6,9-dihydro-3H-purin-6-one

Pharmacokinetics

  • Absorption: oral bioavailability 10 to 20% slightly absorbed through skin and ophthalmic.
  • Distribution: 9-33%, crosses placenta
  • Excretion: through kidneys

Actions

Viral (HSV-1, HSV-2 and VZV) thymidine kinase converts aciclovir to the aciclovir monophosphate, aciclovir monophosphate then converted into the aciclovir diphosphate by cellular guanylate kinase, and finally by phosphoenolpyruvate carboxykinase, phosphoglycerate kinase, and pyruvate kinase the diphosphate coverts into the triphosphate. Aciclovir triphosphate inhibits competitively the viral DNA polymerase and for incorporation into viral DNA competes with the natural deoxyguanosine triphosphate. Once incorporated, aciclovir triphosphate inhibits DNA synthesis by acting as a chain terminator. Aciclovir is selective and low in cytotoxicity as the cellular thymidine kinase of uninfected, normal; the cell does not use aciclovir effectively as a substrate.

Dosage/Dosage form

  • Accrivir-200 mg
  • Aciherpin-200,400,800 mg
  •  Aciherpin crm-5g
  •  Acirax-200 mg
  •  Aciv-200,400,800 mg
  • Acivir injction-25 mg
  •  Acivir eye ointment-3%/5g
  •   Acivir skin cream-5g
  • Acyclovir susoension-200 mg/5mL orally

Therapeutic uses

Used to treat infection caused by viruses such as shingles, chicken pox, treatment of initial and recurrent mucocutaneous herpes simplex virus infections, varicella-zoster infections.

Adverse effects/Side effects

Anemia, hemoglobinemia, leukocytoclastic vasculitis, leukopenia, lymphadenopathy, and thrombocytopenia. Rash, pruritus, or urticaria occasionally occurs during oral or IV acyclovir therapy.

Interaction

  • The serum concentration of Aciclovir can be increased when it is combined with Teriflunomide.
  • The serum concentration of Tizanidine can be increased when it is combined with Aciclovir.
  • Increase liquid intake

Contraindications

Geriatrics, children, pregnancy and lactation, in patients with hypersensitivity reactions, agitation, drowsiness.

Storage

Keep container tightly closed in a dry and well-ventilated place. Store at 15-25°C. 

Information

Molecular weight

225.208 g/mol

Molecular formula

C8H11N5O3

CAS number

59277-89-3

Precautions

Acyclovir should be used with caution in patients with underlying neurologic abnormalities and in patients with serious renal, hepatic, or electrolyte abnormalities or substantial hypoxia.