Acyclovir is a synthetic purine nucleoside analogue which is active against herpes simplex virus types 1 (HSV-1), 2 (HSV-2), and varicella-zoster virus (VZV).
Acyclovir is a synthetic purine nucleoside analogue which is active against herpes simplex virus types 1 (HSV-1), 2 (HSV-2), and varicella-zoster virus (VZV). The inhibitory activity of acyclovir is highly selective due to its affinity for the enzyme thymidine kinase (TK) encoded by HSV and VZV. This viral enzyme converts acyclovir into acyclovir monophosphate, a nucleotide analogue. The monophosphate is further converted into diphosphate by cellular guanylate kinase and into triphosphate by a number of cellular enzymes. Acyclovir triphosphate stops replication of herpes viral DNA. This is accomplished in three ways: 1) competitive inhibition of viral DNA polymerase, 2) incorporation into and termination of the growing viral DNA chain, and 3) inactivation of the viral DNA polymerase.
Acyvir 500 mg Lyophilized Powder for Solution for Infusion: Each vial contains Acyclovir Sodium equivalent to Acyclovir USP 500 mg.
Acyclovir IV for Infusion is indicated for the treatment of
Method of Preparation:
The required dose of Acyclovir IV for Infusion should be administered by slow intravenous infusion over a one-hour period. Acyclovir 250 mg IV for Infusion should be reconstituted in 10 ml of Water for Injections BP or Sodium Chloride Injection BP (0.9% w/v) and Acyclovir 500 mg IV for Infusion should be reconstituted in 10 ml of Water for Injections BP or Sodium Chloride Injection BP (0.9% w/v) to provide a solution containing 25/50 mg acyclovir per ml. From the calculated dose, determine the appropriate number of vials to be used. Shake the vial gently until the contents of the vial have dissolved completely. After reconstitution Acyclovir IV for Infusion may be administered by a controlled rate infusion pump. Alternatively, the reconstituted solution may be further diluted to give an acyclovir concentration of not greater than 5 mg/ml (0.5% w/v) for administration by infusion:- Add the required volume of reconstituted solution to Sodium Chloride 0.9% w/v infusion solution and shake well to ensure adequate mixing occurs.
Dosage:
| Disease | Patient Group | Dosage | Duration |
| Herpes simplex encephalitis | Adults and Adolescents(12 years of age and older) | 10 mg/kg every 8 hours | 10 days |
| Pediatrics(3 months to 12 years of age) | 20 mg/kg every 8 hours | 10 days | |
| Herpes simplex infections | Adults and Adolescents(12 years of age and older) | 5 mg/kg every 8 hours | 7 days |
| Pediatrics(Under 12 years of age) | 10 mg/kg every 8 hours | 7 days | |
| Severe initial clinical episodes of Herpes genitalis | Adults and Adolescents(12 years of age and older) | 5 mg/kg every 8 hours | 5 days |
| Varicella zoster infections(Chickenpox) | Adults and Adolescents(12 years of age and older) | 10 mg/kg every 8 hours | 7 days |
| Pediatrics(Under 12 years of age) | 20 mg/kg every 8 hours | 7 days | |
| Neonatal Herpes simplex infections | Neonatal Herpes Simplex Virus Infections(Birth to 3 months) | 10 mg/kg every 8 hours | 10 days |
Precipitation of acyclovir crystals in renal tubules can occur if the maximum solubility of free acyclovir is exceeded or if the drug is administered by bolus injection. When dosage adjustments are required they should be based on estimated creatinine clearance.
Most common side effects are headache, nausea, diarrhea, rash and phlebitis.
Coadministration of probenecid with acyclovir has been shown to increase the mean acyclovir half-life and the area under the concentration-time curve. Urinary excretion and renal clearance were correspondingly reduced.
Use in Pregnancy: Pregnancy category B. There are no adequate and well-controlled studies in pregnant women. Acyclovir should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Use in nursing mothers: Acyclovir should be administered to a nursing mother with caution and only when indicated. Geriatric Use: No overall differences in safety are observed between older and younger subjects.
Acyvir 500 mg Lyophilized Powder for Solution for Infusion: Each combo pack contains 1 vial of 500 mg Acyclovir Lyophilized Powder (as Acyclovir Sodium) for solution for infusion, 1/2 ampoules of 10 ml water for injections BP & 10 ml disposable syringe.
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