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Acyclovir (topical)

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Acyclovir (topical)
Copyright 1978-2011 Lexicomp, Inc. All rights reserved.

Brand Names: U.S.

  • Zovirax®
Brand Names: Canada

  • Zovirax®
Pharmacologic Category

  • Antiviral Agent, Topical
Dosing: AdultGenital HSV: Topical: Immunocompromised: Ointment: Initial episode: 1/2” ribbon of ointment for a 4” square surface area every 3 hours (6 times/day) for 7 days

Herpes labialis (cold sores): Topical: Apply 5 times/day for 4 days

Mucocutaneous HSV: Topical: Ointment: Non-life-threatening, immunocompromised: 1/2” ribbon of ointment for a 4” square surface area every 3 hours (6 times/day) for 7 days

Dosing: PediatricHerpes labialis (cold sores): Topical: Children ≥12 years: Refer to adult dosing.

Dosing: GeriatricRefer to adult dosing.

Dosage Forms: U.S.Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Cream, topical:

Zovirax®: 5% (2 g, 5 g)

Ointment, topical:

Zovirax®: 5% (15 g, 30 g)

Generic Equivalent Available: U.S.No

AdministrationTopical: Not for use in the eye. Apply using a finger cot or rubber glove to avoid transmission to other parts of the body or to other persons.

UseTreatment of herpes labialis (cold sores), mucocutaneous HSV in immunocompromised patients

Medication Safety Issues

Sound-alike/look-alike issues:

Acyclovir may be confused with ganciclovir, Retrovir®, valacyclovir

Zovirax® may be confused with Doribax®, Valtrex®, Zithromax®, Zostrix®, Zyloprim®, Zyvox®

International issues:

Opthavir [Mexico] may be confused with Optivar brand name for azelastine [U.S.]

Adverse Reactions Significant>10%: Dermatologic: Mild pain, burning, or stinging (ointment 30%)

1% to 10%: Dermatologic: Pruritus (ointment 4%), itching

ContraindicationsHypersensitivity to acyclovir, valacyclovir, or any component of the formulation

Warnings/PrecautionsDisease-related concerns:

• Genital herpes: Appropriate use: Physical contact should be avoided when lesions are present; transmission may also occur in the absence of symptoms. Treatment should begin with the first signs or symptoms.

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• Herpes labialis: Appropriate use: For external use only to the lips and face; do not apply to eye or inside the mouth or nose. Treatment should begin with the first signs or symptoms.

Special populations:

• Immunocompromised patients: Use with caution in immunocompromised patients.

Pregnancy ImplicationsTeratogenic effects were not observed in animal studies. When administered orally, acyclovir crosses the placenta. Refer to the Acyclovir, Systemic monograph for details. The amount of acyclovir available systemically following topical application of the cream or ointment is significantly less in comparison to oral doses.

Breast-Feeding ConsiderationsWhen administered orally, acyclovir enters breast milk. Refer to the Acyclovir, Systemic monograph for details. The amount of acyclovir available systemically following topical application of the cream or ointment is significantly less in comparison to oral doses. Nursing mothers with herpetic lesions near or on the breast should avoid breast-feeding.

Pricing: U.S. (www.drugstore.com)Cream (Zovirax)

5% (2): $95.99

5% (5): $180.94

International Brand Names

  • Acic (EE);
  • Acic Creme (DE);
  • Aciclidan (DK);
  • Aciclomed (BE);
  • Aciclor (VE);
  • Aciclosina (PT);
  • Aciherpin (PH);
  • Acilax Cream (HK);
  • Acivir (CH, IL, IN);
  • Acivirex (GT, HN, NI, SV);
  • Activir (FR);
  • Acyvir (EC);
  • Anti (SE);
  • Antix (NO);
  • Avir (VE);
  • Cicloferon (CR, DO, GT, PA, SV);
  • Cicloviral (CO);
  • Clinovir (ID);
  • Clovir (TW);
  • Covelay (PH);
  • Cycloherp (HK);
  • Cyclomed (IL);
  • Cyclostad (PH);
  • Cyclovax (HK);
  • Cyclovir (IN);
  • Declovir (HK);
  • Deherp (TW);
  • Dravyr (SG);
  • Ecuvir (EC);
  • Erlivirax (SG);
  • Eurovir (PY);
  • Expit (UY);
  • Ezopen Creme (BR);
  • Herpesin (CZ);
  • Herpevir (FR);
  • Herpex (IN);
  • Lisovyr Cream (AR);
  • Lisovyr Crema (CN);
  • Lovir (NZ);
  • Lovire (ZA);
  • Marvir (TH);
  • Medovir (MY);
  • Oppvir (TW);
  • Poviral (AR);
  • Qualiclovir (HK);
  • Remex (FR);
  • Vicorax (TW);
  • Viratop (BE);
  • Virex (CO);
  • Virless (SG);
  • Virogon (TH);
  • Virzin (DE);
  • Vivir (KP);
  • Zeven (MY);
  • Zevin (TH);
  • Zoral (HK, MY, SG);
  • Zorax (SG);
  • Zovir (DK);
  • Zovirax (AR, AU, BB, BE, BM, BR, BS, CH, CL, CN, CZ, EC, EE, FI, FR, GB, GY, HK, ID, IE, IL, JM, KP, MY, NL, NO, NZ, PE, PH, PR, PT, PY, SE, TH, TT, TW, UY, ZA)
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Mechanism of ActionAcyclovir is converted to acyclovir monophosphate by virus-specific thymidine kinase then further converted to acyclovir triphosphate by other cellular enzymes. Acyclovir triphosphate inhibits DNA synthesis and viral replication by competing with deoxyguanosine triphosphate for viral DNA polymerase and being incorporated into viral DNA.

Pharmacodynamics/KineticsAbsorption: Plasma concentrations following topical application of the cream were below the limit of detection in 5/6 male volunteers (<0.01μM) and 0.014 μM in one subject. Following application of the ointment to patients with varicella-zoster infection, acyclovir plasma concentrations were <0.01-0.28 mcg/mL in patients with normal renal function and <0.01-0.78 mcg/mL in a patient with renal impairment.

Excretion: Urine (0.04% of the daily dose following topical application of the cream; <0.02% to 9.4% of the daily dose following topical application of the ointmen

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