Chemical formula: C₈H₁₁N₅O₃ Molecular mass: 225.205 g/mol PubChem compound: 135398513
Aciclovir interacts in the following cases:
Concomitant administration of acyclovir with interferon may result in mutually reinforcing their action.
Care is also required (with monitoring for changes in renal function) if administering intravenous aciclovir with drugs which affect other aspects of renal physiology (e.g. cyclosporin, tacrolimus).
If lithium is administered concurrently with high dose aciclovir IV, the lithium serum concentration should be closely monitored because of the risk of lithium toxicity.
Probenecid and cimetidine increase the AUC of aciclovir by this mechanism and reduce aciclovir renal clearance. However no dosage adjustment is necessary because of the wide therapeutic index of aciclovir.
An experimental study on five male subjects indicates that concomitant therapy with aciclovir increases AUC of totally administered theophylline with approximately 50%. It is recommended to measure plasma concentrations during concomitant therapy with aciclovir.
Concomitant administration of zidovudine and aciclovir may cause lethargy, neuritis, convulsions.
Haemodialysis significantly enhances the removal of aciclovir from the blood and may, therefore, be considered a management option in the event of symptomatic overdose.
Population group: only newborns (0 - 40 days old) , infants (40 days - 1 year old) , children (1 year - 12 years old)
Caution is advised when administering aciclovir I.V. to patients with impaired renal function. Adequate hydration should be maintained.
Dosage adjustment for patients with renal impairment is based on creatinine clearance, in units of ml/min for adults and adolescents and in units of ml/min/1.73m² for infants and children less than 13 years of age. The following adjustments in dosage are suggested.
Dosage adjustments in infants and children:
| Creatinine Clearance | Dosage |
|---|---|
| 25 to 50 ml/min/1.73m² | The dose recommended above (250 or 500 mg/m² body surface area or 20 mg/kg body weight) should be given every 12 hours. |
| 10 to 25 ml/min/1.73m² | The dose recommended above (250 or 500 mg/m² body surface area or 20 mg/kg body weight) should be given every 24 hours. |
| 0(anuric) to 10 ml/min/1.73m² | In patients receiving continuous ambulatory peritoneal dialysis (CAPD) the dose recommended above (250 or 500 mg/m² body surface area or 20 mg/kg body weight) should be halved and administered every 24 hours. |
| In patients receiving haemodialysis | In patients receiving haemodialysis the dose recommended above (250 or 500 mg/m² body surface area or 20 mg/kg body weight) should be halved and administered every 24 hours and after dialysis. |
Population group: only adolescents (12 years - 18 years old) , adults (18 years old or older)
Caution is advised when administering aciclovir I.V. to patients with impaired renal function. Adequate hydration should be maintained.
Dosage adjustment for patients with renal impairment is based on creatinine clearance, in units of ml/min for adults and adolescents and in units of ml/min/1.73m² for infants and children less than 13 years of age. The following adjustments in dosage are suggested:
Dosage adjustments in adults and adolescents:
| Creatinine Clearance | Dosage | |
|---|---|---|
| 25 to 50 ml/min | The dose recommended above (5 or 10 mg/kg body weight) should be given every 12 hours. | |
| 10 to 25 ml/min | The dose recommended above (5 or 10 mg/kg body weight) should be given every 24 hours. | |
| 0(anuric) to 10 ml/min | In patients receiving continuous ambulatory peritoneal dialysis (CAPD) the dose recommended above (5 or 10 mg/kg body weight) should be halved and administered every 24 hours. In patients receiving haemodialysis the dose recommended above (5 or 10 mg/kg body weight) should be halved and administered every 24 hours and after dialysis. | Caution is advised when administering Zovirax I.V. to patients with impaired renal function. Adequate hydration should be maintained. |
Dosage adjustment for patients with renal impairment is based on creatinine clearance, in units of ml/min for adults and adolescents and in units of ml/min/1.73m² for infants and children less than 13 years of age. The following adjustments in dosage are suggested:
Dosage adjustments in adults and adolescents:
| Creatinine Clearance | Dosage |
|---|---|
| 25 to 50 ml/min | The dose recommended above (5 or 10 mg/kg body weight) should be given every 12 hours. |
| 10 to 25 ml/min | The dose recommended above (5 or 10 mg/kg body weight) should be given every 24 hours. |
| 0(anuric) to 10 ml/min | In patients receiving continuous ambulatory peritoneal dialysis (CAPD) the dose recommended above (5 or 10 mg/kg body weight) should be halved and administered every 24 hours. In patients receiving haemodialysis the dose recommended above (5 or 10 mg/kg body weight) should be halved and administered every 24 hours and after dialysis. |
The use of aciclovir should be considered only when the potential benefits outweigh the possibility of unknown risks.
A post-marketing aciclovir pregnancy registry has documented pregnancy outcomes in women exposed to any formulation of aciclovir. The registry findings have not shown an increase in the number of birth defects amongst aciclovir exposed subjects compared with the general population, and any birth defects showed no uniqueness or consistent pattern to suggest a common cause. Systemic administration of aciclovir in internationally accepted standard tests did not produce embryotoxic or teratogenic effects in rabbits, rats or mice. In a non-standard test in rats, foetal abnormalities were observed but only following such high subcutaneous doses that maternal toxicity was produced. The clinical relevance of these findings is uncertain.
Caution should however be exercised by balancing the potential benefits of treatment against any possible hazard.
Following oral administration of 200 mg five times a day, aciclovir has been detected in breast milk at concentrations ranging from 0.6 to 4.1 times the corresponding plasma levels. These levels would potentially expose nursing infants to aciclovir dosages of up to 0.3 mg/kg/day. Caution is therefore advised if aciclovir is to be administered to a nursing woman.
There is no information on the effect of aciclovir on human female fertility.
In a study of 20 male patients with normal sperm count, oral aciclovir administered at doses of up to 1g per day for up to six months has been shown to have no clinically significant effect on sperm count, motility or morphology.
There have been no studies to investigate the effect of aciclovir on driving performance or the ability to operate machinery. A detrimental effect on such activities cannot be predicted from the pharmacology of the active substance, but the adverse event profile should be borne in mind.
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