Acyclovir

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ACYCLOVIR

Acyclovir 03

1.       TYPE OF DRUG- ACYCLOVIR
Aciclovir (ACV), also known as acyclovir and acycloguanosine, is an antiviral medication.

 

2.       INDICATIONS (USE)- ACYCLOVIR
For the treatment and management of herpes zoster (shingles), genital herpes, and chickenpox.

 

3.       MECHANISM OF ACTION (MOA)- ACYCLOVIR
Acyclovir, a synthetic acyclic purine nucleoside analog, is a substrate with a high degree of specificity for herpes simplex and varicella-zoster specified thymidine kinase. Acyclovir is a poor substrate for host cell-specified thymidine kinase. Herpes simplex and varicella-zoster specified thymidine kinase transform acyclovir to its monophosphate which is then transformed by a number of cellular enzymes to acyclovir diphosphate and acyclovir triphosphate. Acyclovir triphosphate is both an inhibitor of, and a substrate for, herpesvirus-specified DNA polymerase. Although the cellular α-DNA polymerase in infected cells may also be inhibited by acyclovir triphosphate, this occurs only at concentrations of acyclovir triphosphate which are higher than those which inhibit the herpesvirus-specified DNA polymerase. Acyclovir is selectively converted to its active form in herpesvirus-infected cells and is thus preferentially taken up by these cells. Acyclovir has demonstrated a very much lower toxic potential in vitro for normal uninfected cells because: 1) less is taken up; 2) less is converted to the active form; and 3) cellular α-DNA polymerase has a lower sensitivity to the action of the active form of the drug. A combination of the thymidine kinase specificity, inhibition of DNA polymerase and premature termination of DNA synthesis results in inhibition of herpes virus replication. No effect on latent non-replicating virus has been demonstrated. Inhibition of the virus reduces the period of viral shedding, limits the degree of spread and level of pathology, and thereby facilitates healing. During suppression there is no evidence that acyclovir prevents neural migration of the virus. It aborts episodes of recurrent herpes due to inhibition of viral replication following reactivation.

 

4.       ROUTES OF ADMINISTRATION- ACYCLOVIR
Oral,Injection.

 

5.       ONSET OF EFFECT OR ACTION- ACYCLOVIR
Within 24 hours.

 

6.     DOSAGE (DOSING INFORMATION)- ACYCLOVIR
Adults : herpes simplex : 200mg 5 times daily at 4hours intervals for 5 days. Herpes zoster : 800mg 5 times daily at 4 hours intervals for 7 days.

Proohylaxis or suppression : 200mg 4 times daily. Chiken pox : 800mg 5 times/day for 7-10 days.Children : Mucocutaneous Herpes simplex : 5 mg/kg/dosr 8 hourly for 7 days.H.

Simplex excephalitis : 1mg/kg/dose for 10-14 days. Prophylaxis : 5mg/kg/8 hourly.Newborns : herpes simplex infection – IV -10 mg/kg/8 hourly. 10-14 days.

 

7.       HALF LIFE (DURATION OF ACTION)- ACYCLOVIR
2.5-3.5 hours.

 

8.       ADVERSE EFFECTS OR SIDE EFFECTS – ACYCLOVIR
  • Pain in your lower back
  • Urinating less than usual or not at all
  • Easy bruising or bleeding or
  • Unusual weakness.
  • Nausea, vomiting, diarrhea, loss of appetite, stomach pain
  • Headache, feeling light-headed  or
  • Swelling in your hands or feet.

 

9.       CONTRAINDICATIONS – ACYCLOVIR
Hypersensitivity.

 

 

10.   DRUG INTERACTIONS – ACYCLOVIR
Probenecid decreases urinary excretion and increases half-life. Risk of renal impairment increased by other nephrotoxic drugs.

 

11.    EXCRETION- ACYCLOVIR
urinary excretion

 

Acyclovir 01

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