Aciclovir: Effective Antiviral Treatment for Herpes Infections
Aciclovir
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Aciclovir is a nucleoside analogue antiviral medication that has been a cornerstone in the management of herpesvirus infections for decades. As a selective inhibitor of viral DNA polymerase, it interferes with viral replication without significantly affecting normal cellular processes. This medication is available in multiple formulations—including oral tablets, topical cream, and intravenous solutions—to address a spectrum of clinical presentations, from localized outbreaks to severe systemic infections. Its well-established efficacy and favorable safety profile make it a first-line choice for both treatment and prophylaxis in immunocompetent and immunocompromised patients.
Features
- Active ingredient: Aciclovir (chemically known as 9-[(2-hydroxyethoxy)methyl]guanine)
- Available formulations: 200mg, 400mg, and 800mg oral tablets; 5% topical cream; intravenous infusion
- Mechanism: Selective inhibition of viral DNA polymerase via competitive incorporation as a guanosine analogue
- High bioavailability in its intravenous form; oral bioavailability approximately 10–20%
- Rapid conversion to active triphosphate form in virus-infected cells
- Low protein binding (9–33%) and primarily renal excretion
Benefits
- Reduces duration and severity of symptomatic outbreaks in herpes simplex virus (HSV) infections
- Decreases frequency of recurrent episodes when used as suppressive therapy
- Lowers risk of viral transmission to partners in genital herpes management
- Prevents visceral dissemination in immunocompromised patients
- Minimizes postherpetic neuralgia risk in herpes zoster treatment
- Well-tolerated with minimal cellular toxicity due to selective activation in infected cells
Common use
Aciclovir is primarily indicated for infections caused by herpes simplex viruses (HSV-1 and HSV-2) and varicella-zoster virus (VZV). This includes treatment of initial and recurrent genital herpes, herpes labialis (cold sores), herpes zoster (shingles), and chickenpox. In immunocompromised patients, it is used both therapeutically and prophylactically to prevent reactivation. Off-label uses include prevention of cytomegalovirus (CMV) reactivation in transplant recipients and management of herpes simplex encephalitis, though higher intravenous doses are typically required for CNS penetration.
Dosage and direction
Dosage varies significantly based on indication, patient immune status, and formulation:
Oral tablets:
- Genital herpes (initial): 200mg 5 times daily for 10 days
- Genital herpes (recurrent): 200mg 5 times daily for 5 days
- Suppressive therapy: 400mg twice daily or 200mg 3–4 times daily
- Herpes zoster: 800mg 5 times daily for 7–10 days
- Chickenpox (children >2 years and adults): 20mg/kg (max 800mg) 4 times daily for 5 days
Intravenous:
- HSV encephalitis: 10mg/kg every 8 hours for 14–21 days
- HSV in immunocompromised: 5mg/kg every 8 hours for 7 days
- Must be infused over at least 1 hour to prevent renal tubular damage
Topical:
- Apply to affected area 5 times daily for 4 days (initiate at earliest symptom recognition)
Dosage adjustment required for renal impairment (CrCl <50 mL/min). Maintain adequate hydration during treatment.
Precautions
Hydration status must be monitored during intravenous administration due to risk of crystalline nephropathy. Use with caution in elderly patients and those with pre-existing renal impairment or dehydration. Neurological monitoring is advised in patients with neurological disorders or those receiving concurrent nephrotoxic drugs. Topical application should avoid mucous membranes and eyes. Pregnancy Category B: adequate human studies lacking, but registry data show no increased teratogenic risk. Excreted in breast milk—consider risk/benefit during lactation.
Contraindications
Hypersensitivity to aciclovir or valaciclovir. Concurrent administration with other nephrotoxic agents in patients with renal impairment should be avoided unless benefits outweigh risks. Intravenous administration is contraindicated in patients with profound dehydration or pre-existing crystalline nephropathy.
Possible side effect
Generally well-tolerated. Most common adverse effects:
- Oral: Nausea (2–5%), diarrhea (2–3%), headache (1–2%)
- IV: Inflammation at injection site (9%), transient renal function elevation (5–10%)
- Topical: Local burning/stinging (30%), pruritus (4%)
- Rare: Neurological symptoms (agitation, confusion, tremor—particularly in renal impairment or rapid IV infusion)
- Very rare: Hematological abnormalities (leukopenia, thrombocytopenia), hepatitis, anaphylaxis
Drug interaction
Probenecid reduces renal clearance of aciclovir, increasing AUC by approximately 40%. Concurrent use with other nephrotoxic drugs (aminoglycosides, cyclosporine, IV pentamidine) may enhance renal toxicity. Zidovudine may cause increased drowsiness. No significant interactions with oral contraceptives or warfarin documented.
Missed dose
If a dose is missed, take as soon as remembered unless close to next scheduled dose. Do not double doses. Maintaining consistent dosing intervals is important for antiviral efficacy, particularly during acute treatment phases.
Overdose
Symptoms may include neurological manifestations (agitation, coma, seizures) and renal impairment. Management includes supportive care and hemodialysis (significantly enhances elimination—60% reduction in half-life). Maintain adequate hydration and renal function monitoring.
Storage
Store at room temperature (15–30°C) in original container. Protect from moisture. Do not freeze oral formulations. Intravenous solution should be used within 12 hours of reconstitution. Keep all medications out of reach of children.
Disclaimer
This information is for educational purposes and does not replace professional medical advice. Dosage and treatment decisions must be made by a qualified healthcare provider based on individual patient characteristics. Not all uses described may be approved in your country—check local prescribing information.
Reviews
Clinical studies demonstrate efficacy across populations:
- Meta-analysis of 12 trials: Aciclovir reduced healing time in recurrent genital herpes by 1.5 days (95% CI: 1.0–2.0)
- Cochrane Review: Suppressive therapy reduced recurrence frequency by 80% compared to placebo
- IV aciclovir reduced mortality from HSV encephalitis from 70% to 28% in landmark trial Long-term safety data show well-tolerated profile with >40 years of clinical use