Simplovir(Aciclovir)

Therapeutic Group: Anti Viral

Presentation

Simplovir 200 tablet: Each tablet contains Aciclovir BP 200 mg.

Simplovir 400 tablet: Each tablet contains Aciclovir BP 400 mg.

Simplovir 250 IV: Each vial contains lyophilized powder of Aciclovir Sodium equivalent to Aciclovir BP 250 mg.

Simplovir 500 IV: Each vial contains lyophilized powder of Aciclovir Sodium equivalent to Aciclovir BP 500 mg.

Simplovir 1 gm IV: Each vial contains lyophilized powder of Aciclovir Sodium equivalent to Aciclovir BP 1 gm.

Description

Simplovir is the brand name of Aciclovir, 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.

Indications

• Herpes Zoster

• Genital Herpes

• Chickenpox

• Herpes Simplex Infections

• Herpes Simplex Encephalitis

Dosage & Administration

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.

Simplovir Tablet
• 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.
• Chickenpox:
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.

Simplovir IV
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
Hartmann\\\'s Solution

Side Effects

Rash, gastro-intestinal disturbances, rises in bilirubin and liver-related enzymes, increase in blood urea and creatinine, decreases in hematological indices, headache, neurological reactions, fatigue.

Precautions

Aciclovir should be administered with caution in patient with renal impairment and doses should be adjusted according to creatinine clearance.

Use in Pregnancy & Lactation

Pregnancy category B & caution should be exercised when it is administered to a lactating mother.

Drug Interaction

Probenecid reduces Aciclovir excretion and so increases plasma concentration and risk of toxicity.

Storage

Keep in a cool & dry place away from light. Keep drugs out of the reach of children.

Commercial Pack

Simplovir 200 mg tablet: Each box contains 3 blister strips of 10 tablets.
Simplovir 400 mg tablet: Each box contains 2 blister strips of 10 tablets.
Simplovir 250 IV: Each box contains 1 vial of 250 mg Aciclovir lyophilized powder, 1 bottle of 50 ml of 0.9% Sodium Chloride solution, 1 disposable syringe & 1 infusion set.