Acyclovir
Also known as: Acyloguanosine, Aciclovir, Aciclovier
Acyclovir is antiviral agent. Acyclovir is a synthetic purine nucleoside analog with an acyclic side chain. Acyclovir is clinically active aganist herpes simplex virus 1 and 2, varicella zoster virus, Epstein-Barr virus and cytomegalovirus. Acyclovir is not used for cure of herpes, but it relieves the pain and makes the infection clear faster. Acyclovir is given prophylactically to seropositive patients before bone marrow and after heart transplant to protect such individuals during post transplant immunosuppressive treatment.
Primary Characteristics
Acyclovir is also known as Acyloguanosine, Aciclovir, Aciclovier.
It is of Synthetic origin and belongs to Guanine.
It belongs to DNA polymerase inhibitor pharmacological group on the basis of mechanism of action. It is also classified under Antiviral Agents .
Molecular Weight: 225 · pKa: 2.27, 9.25 · Solubility in Water: 1 in 400 · Solubility in Alcohol: < 1 in 5000 · Non-proprietary name: Acyclovir.
Pharmacokinetics
Absorption: Acyclovir has an oral bioavailability is 17% (±4%).
Distribution: Acyclovir has a volume of distribution is 22.5-10 litre. plasma protein binding is 9-24%.
Elimination: it is metabolised via 20%, plasma half-life is 3.32 ± 0.32 hr, renal excretion is 80%.
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Indications
Acyclovir is primarily indicated in conditions like Cytomegalovirus infection prophylaxis, Encephalitis, Herpes simplex, Herpes simplex (in immunocompromised patients), Herpes simplex infection of mucous membrane, Herpes simplex infection prophylaxis, Herpes simplex keratitis, Prophylaxis of herpes simplex, Severe initial genital herpes, Simplex encephalitis, Treatment of herpes simplex, Varicella and herpes zoster, Varicella zoster infections, Varicella-zoster, Varicella-zoster (chickenpox-shingles), Viral conjunctivitis.
Acyclovir is also indicated for secondary conditions like Herpes simplex (prevention of recurrence), Prevention of recurrence of herpes simplex, Treatment of herpes simplex (immunocompromised patients).
Contraindications
Acyclovir is contraindicated in conditions like Hypersensitivity.
Dosage
Acyclovir's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 3 % | 3 % | Every 4h | Ophthalmic | As Required |
| 200 mg | 200 mg | Every 4h | PO | For heapes simplex prophylenis. |
| 300 mg | 300 mg | Every 4h | PO | For heapes simplex prophylexis in the immunocompromised patient |
| 400 mg | 400 mg | Every 2h | PO | For heapes simplex prophylenis. |
| 200 mg | 200 mg | Every 4.8h | PO,IV | For 5 Days. Doses and duration vary according to indication. |
| Paediatric Dosage (20kg) | ||||
| 10 – 20 mg/kg | — | Every 3h | IV Infusion | For months to 12 years. |
| 0 – 20 mg/Kg | — | Every 4h | PO | For herpes simplex for vericella for 5 days. |
| 0 – 200 mg | — | Every 4h | PO | For Children under 2 years for vericella |
| 100 – 100 mg | — | Every 4.8h | PO | For children under 2 years of age. |
| 5 % | 5 % | Every 4.8h | Topical | As Required |
| Neonatal Dosage (3kg) | ||||
| 0 – 20 mg/Kg | — | Every 3h | For herpes simplex for 14 days and 21 days if CNS involvement. (For neonate and infant the age of upto 3 months) | |
| 12.5 mg/kg | 12.5 mg/kg | Every 8h | Infusion | Over 1 hr. |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Acyclovir in overdosage may give rise to further complications which include Acute renal failure , Encephalopathy , Renal tubular obstruction, Rises in blood urea and creatinine , Seizures .
Acyclovir produces potentially life-threatening effects which include Coma. Careful monitoring is needed with proper medical management.
Acyclovir is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Agitation , Anorexia , Confusion, Contact dermatitis, Crystalluria , Elevation of liver enzymes, Erythema, Hallucination , Headache, Itching, Lethargy, Malaise, Nausea, Reaction at injection site, Severe local inflammatory reactions , Skin rashes, Stinging on application, Transient burning, Tremors, Vomiting .
Warnings / Precautions
Available Brands
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Single Ingredient
Storage Conditions
Drug Classification
- 1.6.5.1 — Herpes and cytomegalovirus infection
- 2.13.2.2 — Antivirals, topical
- 3.21.1.2 — Antivirals