Acloveer is a synthetic purine neucleotide analogue, which acts against human herpes viruses. The enzyme thymidine kinase (TK)encoded by HSV, VZV and EBV converts acyclovir into acyclovir monophosphate, a neucleotide analogue, which is further converted to diphosphate and triphosphate by cellular enzymes. Acloveer triphosphate interferes with DNA polymerase and inhibits viral DNA replication with resultant chain termination following its incorporation into the growing viral DNA chain.
Acloveer exerts its antiviral effect on herpes simplex viruses (HSV) and varicella-zoster virus by interfering with DNA synthesis and inhibiting viral replication. The exact mechanisms of action against other susceptible viruses have not fully elucidated. In vitro studies with herpes simplex viruses indicate that acyclovir triphosphate is the pharmacologically active form of the drug; the triphosphate functions as both a substrate for and preferential inhibitor of viral DNA polymerase.
Aciclovir is a synthetic purine nucleoside with inhibitory activity against herpes simplex virus(HSV-1 & HSV-2) and varicella-zoster virus (VZV). The activity of Aciclovir is highly selective due to its affinity for the enzyme thymidine kinase encoded by HSV and VZV. This viral enzyme converts Aciclovir into Aciclovir monophosphate, a nucleotide analogue. The monophosphate is further converted into diphosphate and finally triphosphate by a number of cellular enzymes. In vitro, Aciclovir triphosphate stops replication of herpes viral DNA. This is accomplished in 3 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.
Acloveer IV for Infusion is used for the treatment of- Herpes Zoster, Genital Herpes, Chickenpox, Herpes Simplex Infections, Herpes Simplex Encephalitis
Acloveer eye ointment is used for treatment of Herpes Simplex Keratitis.
Acloveer Oral is used for Herpes Zoster Genital Herpes, Chickenpox, Herpes Simplex Infections, Herpes Simplex Encephalitis
Acloveer cream are used for the treatment of herpes simplex virus infections of the skin including initial and recurrent genital herpes and herpes labialis.
Acloveer is also used to associated treatment for these conditions: Bell's Palsy, Chickenpox, Cytomegalovirus (CMV) Infection, Encephalitis, Herpes Simplex, Herpes Simplex Infection, Herpes Zoster, Herpes simplex of the oral-labial, Herpes simplex type I reactivation, Recurrent Genital Herpes (RGH), Recurrent Herpes Labialis, VZV re-activation, Acute Genital herpes, Acute Herpes labialis, Acute Herpetic keratitis, Severe Genital herpes
|Acyclovir Other Names||Aciclovir, Aciclovirum, Acycloguanosine, Acyclovir|
Acyclovir is 9-33% protein bound in plasma.
|Therapeutic Class||Anti Viral|
|Manufacturer||Knoll Healthcare Pvt Ltd, Knoll Pharmaceuticals Ltd|
|Last Updated:||June 23, 2021 at 9:09 am|
Apply ointment into lower conjunctival sac five times daily at 4 hours interval; continue for minimum 3 days after healing.
Acloveer cream should be applied to lesions or impending lesions 5 times daily (at 4 hourly intervals omitting the night-time dose). Treatment should continue for 5 days. If healing does not occur, treatment may be extended for up to 10 days.
The total daily dosage of Aciclovir should be based on the type or severity of infection and given in equally divided doses based on consideration of degree of susceptibility of the pathogens, renal function and body-weight.
• Acute Herpes Zoster:
800 mg every 4 hours, 5 times daily for 7 to 10 days.
• Genital Herpes:
Initial Genital Herpes: 200 mg every 4 hours, 5 times daily for 10 days.
Chronic suppressive therapy for recurrent disease: 400 mg 2 times daily for up to 12 months.
Intermittent therapy: 200 mg every 4 hours, 5 times daily for 5 days.
Children (2 years of age and older): 20 mg/kg/dose 4 times daily (80 mg/kg/day) for 5 days.
Adults and Children (>40 kg): 800 mg 4 times daily for 5 days.
The required dose of Aciclovir IV should be administered by slow intravenous infusion over a one-hour period.
• Herpes Simplex (HSV-1 and HSV-2) Infections:
Adults and Adolescents (≥12 years): 5 mg/kg, 8 hourly for 7 days.
Pediatrics (<12 years): 10 mg/kg 8 hourly for 7 days.
• Severe Initial Herpes Genitalis:
Adults and Adolescents (≥12 years): 5 mg/kg 8 hourly for 5 days.
• Herpes Simplex Encephalitis:
Adults and Adolescents (≥12 years): 10 mg/kg 8 hourly for 10 days.
Pediatrics (3 months to 12 years of age): 20 mg/kg 8 hourly for 10 days.
• Neonatal Herpes Simplex (Birth to 3 months):
10 mg/kg 8 hourly for 10 days.
• Varicella Zoster:
Adults and Adolescents (≥12 years): 10 mg/kg 8 hourly for 7 days.
Pediatrics (<12 years): 20 mg/kg 8 hourly for 7 days.
Dose adjustment of Tablet for patients with acute or chronic renal impairment, based on Creatinine Clearance, Cr Cl (mL/min/1.73 m2):
For Cr Cl= > 25 : 800 mg 4 hourly 5 times daily
For Cr Cl = 10 to 25 : 200 mg 4 hourly 5 times daily or 400 mg 12 hourly or 800 mg 8 hourly
For Cr Cl = 0 to 10 : 200 mg 12 hourly or 400 mg 12 hourly or 800 mg 12 hourly
Dose adjustment of IV for patients with acute or chronic renal impairment, based on Creatinine Clearance, Cr Cl (mL/min/1.73 m2):
For Cr Cl = > 50 : 100% of recommended dose, 8 hourly
For Cr Cl = 25 to 50 : 100% of recommended dose, 12 hourly
For Cr Cl = 10 to 25 : 100% of recommended dose, 24 hourly
For Cr Cl = 0 to 10 : 50% of recommended dose, 24 hourly
Caution: Rapid or bolus intravenous injection must be avoided. Intramuscular or subcutaneous injection must be avoided.
Reconstitution procedure of IV infusion
Vial containing 250 mg Aciclovir will be reconstituted with 50 ml infusion solution and vial containing 500 mg Aciclovir will be reconstituted with 100 ml infusion solution. Besides, Vial containing 1 gm Aciclovir will be reconstituted with 250 ml infusion solution. 10 ml of the infusion solution will be added to the vial containing 250 mg, 500 mg and 1 gm Aciclovir. Shake well and transfer the required amount of solution to the infusion container. The final concentration of Aciclovir will be not more than 5 mg/ml.
The reconstituted solution should be used within 12 hours. Refrigeration of reconstituted solution may result in the formation of a precipitate which will re-dissolve at room temperature.
Compatible infusion fluids
Sodium Chloride Intravenous Infusion BP (0.45% and 0.9% w/v)
Sodium Chloride (0.18% w/v) and Glucose (4% w/v) Intravenous Infusion BP
Sodium Chloride (0.45% w/v) and Glucose (2.5% w/v) Intravenous Infusion BP
It is recommended that Acloveer IV Injection for Intravenous Infusion should be administered for five to seven days in the treatment of most infections and for at least ten days in the treatment of Herpes simplex encephalitis.
Each 250 mg vial of Acloveer IV Injection should be reconstituted by the addition of 10 ml of either Water for Injection or Sodium Chloride Intravenous Infusion (0.9% w/v). This provides a solution containing 25 mg Acloveer per ml.
Each 500 mg vial of Acloveer IV Injection should be reconstituted by the addition of 10 ml of either Water for Injection or Sodium Chloride Intravenous Infusion (0.9% w/v). This provides a solution containing 50 mg Acloveer per ml.
Transient mild stinging immediately following application may occur in a small proportion of patients. Local irritation and inflammation such as blepharitis and conjunctivitis have also been reported.
Skin rashes which, resolve after withdrawal of the drug have been reported with acyclovir. The most common adverse effect is mild pain including transient burning and stinging at the site of application following acyclovir cream.
Aciclovir should be administered with caution in patient with renal impairment and doses should be adjusted according to creatinine clearance.
Renal impairment. Pregnancy, lactation. Neurological abnormalities with significant hypoxia, serious hepatic or electrolyte abnormalities. Maintain adequate hydration.
Acloveer cream is not recommended for application to mucous membrane such as eye, mouth, vagina etc.
Concomitant administration of probenecid and acyclovir has reportedly increased the mean plasma half-life and decreased urinary excretion and renal clearance of acyclovir. Amphotericin B has been shown to potentiate the antiviral effect of acyclovir against pseudorabies virus in vitro when both drugs are added to the culture medium. Ketoconazole and acyclovir have shown dose-dependent, synergistic, antiviral activity against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) in in-vitro replication studies.
- Drink plenty of fluids. Dehydration with acyclovir predisposes patients to nephrotoxicity.
- Take with or without food. The absorption is unaffected by food.
Volume of Distribution
The volume of distribution of acyclovir is 0.6L/kg.
The clearance of acyclovir varies from 2.5-3 hours depending on the creatinine clearance of the patient. The plasma half life of acyclovir during hemodialysis is approximately 5 hours. The mean half life in patients from 7 months to 7 years old is 2.6 hours.
The renal clearance of acyclovir is 248mL/min/1.73m. The total clearance in neonates if 105-122mL/min/1.73m
Pregnancy & Breastfeeding use
Pregnancy category B. There are no adequate and well-controlled studies in pregnant women. Acloveer should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Use in nursing mothers: Acloveer 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.
The use of Acloveer sterile eye ointment should be considered only when the potential benefits outweigh the possibility of unknown risk.
Acloveer IV Injection is contraindicated in patients known to be hypersensitive to Acloveer or Valacyclovir.
Acloveer ophthalmic is contraindicated to the patients with known hypersensitivity to acyclovir.
Acloveer oral is contraindicated in patients known to be hypersensitive to acyclovir. For the patients with severe renal impairment, a reduction of the doses is recommended.
Acloveer cream is contraindicated in patients known to be hypersensitive to acyclovir.
The dose of Acloveer IV injection in children aged 1-12 years should be calculated on the basis of body surface area. Children in this age group with Herpes simplex infections (except Herpes simplex encephalitis) or Varicella zoster infections should be given Acloveer Infusion in doses of 250 mg per square metre of body surface area (equivalent to 5 mg/kg in adults). Immunocompromised children in this age group with Varicella zoster virus infection or with Herpes simplex encephalitis should be given Acloveer IV Infusion in doses of 500 mg per square metre of body surface area (equivalent to 10 mg/kg in adults). Children with impaired renal function require an appropriately modified dose, according to the degree of impairment.
HSV infections in children over 2 years should be given adult doses and children below 2 years should be given half of the adult dose.
Symptoms: Elevations in BUN and serum creatinine, subsequent renal failure, anuria, agitation, coma, lethargy, seizures.
Management: Consider use of haemodialysis until renal function is restored.
Interaction with other Medicine
Probenecid reduces Aciclovir excretion and so increases plasma concentration and risk of toxicity.
Store at 15°C to 25°C. Protected from light and moisture. Keep the medicine out of the reach of children.