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Acyclovir (ophthalmic): Drug information

Acyclovir (ophthalmic): Drug information
(For additional information see "Acyclovir (ophthalmic): Patient drug information" and see "Acyclovir (ophthalmic): Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Pharmacologic Category
  • Antiviral Agent, Ophthalmic
Dosing: Adult
Herpetic keratitis

Herpetic keratitis: Ophthalmic: Apply a ½-inch ribbon of ointment in the lower cul-de-sac of the affected eye(s) 5 times daily (approximately every 3 hours while awake) until the corneal ulcer heals, then apply a ½-inch ribbon 3 times daily for 7 days.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling. However, dosage adjustment unlikely due to low systemic absorption.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling. However, dosage adjustment unlikely due to low systemic absorption.

Dosing: Older Adult

Refer to adult dosing.

Dosing: Pediatric

(For additional information see "Acyclovir (ophthalmic): Pediatric drug information")

Herpes simplex keratitis

Herpes simplex keratitis: Children ≥2 years and Adolescents: Ophthalmic: Apply a 1 cm ribbon in the lower eyelid of affected eye(s) 5 times a day (~every 3 hours while awake) until corneal ulcer heals, then apply a 1 cm ribbon 3 times daily for 7 more days

Dosing: Kidney Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling; however, dosage adjustment unlikely due to low systemic absorption.

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling; however, dosage adjustment unlikely due to low systemic absorption.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

1% to 10%: Ophthalmic: Eye pain, follicular conjunctivitis, punctate keratitis, stinging of eyes

<1%, postmarketing, and/or case reports: Angioedema, blepharitis, type I hypersensitivity reaction, urticaria

Contraindications

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

Warnings/Precautions

Special populations:

• Contact lens wearers: Contact lenses should not be worn during the course of therapy or in any patient with signs/symptoms of herpetic keratitis.

Other warnings/precautions:

• Appropriate use: For topical ophthalmic use only. Consult a health care professional if pain, redness, itching, or inflammation becomes aggravated.

Product Availability

Avaclyr: FDA approved April 2019; anticipated availability is currently unknown.

Administration: Adult

Ophthalmic: For topical ophthalmic use only; avoid touching tip of applicator to eye(s) or other surfaces. After application close the eye(s) for 1 to 2 minutes; excess ointment may be wiped away. Contact lenses should not be worn during therapy or with signs/symptoms of herpetic keratitis.

Administration: Pediatric

Ophthalmic: For ophthalmic application only; avoid touching tip of applicator to eye or other surfaces. Apply to inside of lower eyelid; instruct patient to close eye(s) for 1 to 2 minutes following application. Patients should avoid wearing contact lenses during the course of therapy or with signs/symptoms of herpetic keratitis.

Use: Labeled Indications

Herpetic keratitis: Treatment of acute herpetic keratitis (dendritic ulcers) in patients with herpes simplex (HSV-1 and HSV-2) virus

Metabolism/Transport Effects

None known.

Drug Interactions

There are no known significant interactions.

Pregnancy Considerations

Acyclovir has not been detected in the blood following ophthalmic administration; limited systemic absorption would limit potential exposure to the fetus. Results from a pregnancy registry, established in 1984 and closed in 1999, did not find an increase in the number of birth defects with exposure to systemic acyclovir when compared to those expected in the general population.

Breastfeeding Considerations

Acyclovir is present in breast milk following oral administration; exposure following ophthalmic administration is unknown. However, acyclovir has not been detected in the blood following ophthalmic use; limited systemic absorption would limit potential exposure via breast milk.

According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother. Systemic use of acyclovir is considered compatible with breastfeeding (WHO 2002).

Mechanism of Action

Acyclovir 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.

Pharmacokinetics (Adult Data Unless Noted)

Absorption: Not detected in blood by existing bioanalytical methods

Excretion: Trace quantities are detectable in the urine but are not therapeutically relevant

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (QA) Qatar: Imavir | Zovirax
  1. Avaclyr (acyclovir) [prescribing information]. Locust Valley, NY: Fera Pharmaceuticals LLC; July 2021.
  2. World Health Organization (WHO). Breastfeeding and maternal medication, recommendations for drugs in the eleventh WHO model list of essential drugs. http://www.who.int/maternal_child_adolescent/documents/55732/en. Published 2002.
Topic 120876 Version 27.0

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