Acyclovir intravenous infusion is indicated for the treatment of-
- Acute clinical manifestations of Herpes simplex virus in immunocompromised patients
- Severe primary or non-primary herpes genitalis in immune-competent patients
- Varicella-zoster viral infection in immunocompromised patients
- Herpes zoster (shingles) in immune-competent patients who show very severe acute local or systemic manifestations of the disease
- Herpes simplex encephalitis
Acyclovir exerts its antiviral eects on the Herpes simplex virus and Varicella zoster virus by interfering with DNA synthesis and inhibiting viral replication. In cells infected with herpes, the antiviral activity of Acyclovir appears to depend principally on the intracellular conversion of the drug to Acyclovir Triphosphate. Acyclovir is converted to Acyclovir Monophosphate principally via virus-coded thymidine kinase, the monophosphate is phosphorylated to diphosphate via cellular guanylate kinase then via other cellular enzymes to the Triphosphate, which is that the pharmacologically active sort of the drug.
Dosage & Administration:
- Herpes simplex infection: For normal or immunocompromised immune status: 5 mg/kg every 8 hours
- Very severe Herpes zoster infection (shingles): For normal immune status: 5 mg/kg every 8 hours
- Varicella-zoster infection: For immunocompromised immune status: 10 mg/kg every 8 hours
- Herpes simplex encephalitis: For normal or immunocompromised immune status: 10 mg/kg every 8 hours
- Each dose should be administered by slow intravenous infusion over a one-hour period.
Administration :
It is recommended that Acyclovir IV Injection for Intravenous Infusion should be administered for five to seven days within the treatment of most infections and for a minimum of ten days within the treatment of Herpes simplex encephalitis.
Acyclovir IV Injection after reconstitution could also be injected directly into a vein over one hour by a controlled-rate infusion pump or be further diluted for administration by infusion. For intravenous infusion, each vial of Acyclovir IV Injection should be reconstituted then, wholly or partially consistent with the dosage required, added to and mixed with a minimum of 50 mL-100 ml infusion solution. A maximum of 250 mg & 500 mg of Acyclovir could also be added to 50 ml & 100 ml infusion solution respectively. After the addition of Acyclovir IV Injection to an infusion solution, the mixture should be shaken to make sure thorough mixing. Acyclovir IV Injection when diluted in accordance with the above schedule will give an Acyclovir concentration not greater than 0.5% w/v.
Acyclovir IV Injection is understood to be compatible with the subsequent infusion fluids and stable for up to 12 hours at temperature (below 25°C) when diluted to a degree not greater than 0.5% w/v Acyclovir.
- 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
- Sodium Chloride (0.45% w/v) and Glucose (2.5% w/v) Intravenous Infusion
- Compound Sodium Lactate Intravenous Infusion BP (Hartmann's Solution)
Acyclovir IV Injection for Intravenous Infusion contains no preservative. Reconstitution and dilution should therefore be administered immediately before use and any unused solution should be discarded. the answer shouldn't be refrigerated.
Interaction:
Co-administration of probenecid with Acyclovir has been shown to extend the mean Acyclovir half-life and therefore the area under the concentration-time curve. Urinary excretion and renal clearance were correspondingly reduced. In patients over 60 years aged concurrent use of diuretics increases plasma levels of Acyclovir very significantly.
Contraindications:
Acyclovir IV Injection is contraindicated in patients known to be hypersensitive to Acyclovir or Valacyclovir.
Side Effects:
Some infrequent adverse reactions are lethargy, obtundation, tremors, confusion, hallucinations, agitation, somnolence, psychosis, convulsions and coma, phlebitis, nausea, vomiting, reversible increases in liver-related enzymes, pruritus, urticaria, rashes, increases in blood urea and creatinine. Local inflammatory reactions may occur if Acyclovir IV Infusion is inadvertently infused into extracellular tissues.
Pregnancy & Lactation:
Pregnancy category B. There are no adequate and well-controlled studies concerning the security of Acyclovir in pregnant women. It shouldn't be used during pregnancy unless the advantages to the patient clearly outweigh the potential risks to the fetus. Acyclovir should only be administered to nursing mothers if the advantages to the mother outweigh the potential risks to the baby. there's no experience of the effect of Acyclovir on human fertility.
Precautions & Warnings:
Acyclovir IV injection is meant for intravenous infusion only and will not be used through the other route. Reconstituted Acyclovir IV Infusion features a pH of roughly 11.0 and will not be administered orally. Acyclovir IV injection as infusion must tend over a period of a minimum of one hour so as to avoid renal tubular damage. It shouldn't be administered as a bolus injection. Acyclovir IV infusion must be amid adequate hydration. Since maximum urine concentration occurs within the primary few hours following infusion, particular attention should tend to determine sufficient urine ‑ow during that period. Concomitant use of other nephrotoxic drugs, pre-existing renal disease, and dehydration increase the danger of further renal impairment by Acyclovir. As Acyclovir has been related to reversible encephalopathic changes, it should be used with caution in patients with neurological abnormalities, significant hypoxia, or serious renal, hepatic, or electrolyte abnormalities.
Use in Special Populations:
Pediatric use: The dose of Acyclovir IV injection in children aged 1-12 years should be calculated on the idea of the body area. Children during this age bracket with Herpes simplex infections (except Herpes simplex encephalitis) or Varicella zoster infections should tend Acyclovir IV Infusion in doses of 250 mg/m2 (equivalent to five mg/kg in adults). Immunocompromised children during this age bracket with Varicella zoster viral infection or with Herpes simplex encephalitis should tend Acyclovir IV Infusion in doses of 500 mg/m2 (equivalent to 10 mg/kg in adults). Children with impaired renal function require an appropriately modified dose, consistent with the degree of impairment.
Geriatric use: No data are available on this age bracket. However, as creatinine clearance is usually low within the elderly, special attention should tend to dosage reduction.
In patients with renal impairment:
Acyclovir should be administered with caution since the drug is excreted through the kidneys. the subsequent modifications in dosage are suggested:
- CrCl: 25-50 ml/min: 5 or 10 mg/kg every 12 hours
- CrCl: 10-25 ml/min: 5 or 10 mg/kg every 24 hours
- CrCl: 0-10 ml/min: 2.5 or 5 mg/kg every 24 hours and after dialysis.
Overdose:
Overdosage of intravenous Acyclovir has resulted in elevations of serum creatinine, blood urea nitrogen, and subsequent kidney failure. Neurological effects including confusion, hallucinations, agitation, seizures, and coma are described in association with overdosage. Adequate hydration is important to scale back the likelihood of crystal formation within the urine. Hemodialysis significantly enhances the removal of Acyclovir from the blood and should, therefore, be considered an option within the management of an overdose of Acyclovir.
Duration of Treatment :
It is recommended that Acyclovir IV Injection for Intravenous Infusion should be administered for five to seven days within the treatment of most infections and for a minimum of ten days within the treatment of Herpes simplex encephalitis.
Reconstitution :
Each 250 mg vial of Acyclovir IV Injection should be reconstituted by the addition of 10 ml of either Water for Injection or common salt Intravenous Infusion (0.9% w/v). This provides an answer containing 25 mg Acyclovir per ml.
Each 500 mg vial of Acyclovir IV Injection should be reconstituted by the addition of 10 ml of either Water for Injection or common salt Intravenous Infusion (0.9% w/v). This provides an answer containing 50 mg Acyclovir per ml.
Storage:
Store at 15°C to 25°C. shielded from light and moisture. Keep the drugs out of the reach of youngsters.
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