acyclovir ophthalmic (Rx)

2-10%

Eye pain (stinging)

Punctuate keratitis

Follicular conjunctivitis

Frequency Not Defined

Blepharitis

Hypersensitivity reactions (eg, angioedema, urticaria)

Contraindications

Hypersensitivity to acyclovir or valacyclovir

Cautions

For ophthalmic use only

Patients should not wear contact lenses if they have signs or symptoms of herpetic keratitis or during the course of therapy

Product is sterile when packaged; patients should be advised to not allow the tip of the container to touch any surface; this may contaminate the ointment; if pain develops, or redness, itching, or inflammation becomes aggravated, patient should consult a physician

Pregnancy

A prospective epidemiologic registry of acyclovir use from 1984-1999 reported birth defects in women exposed to systemic acyclovir during the first trimester of pregnancy

Likewise, oral and SC administration of acyclovir to pregnant mice, rats, and rabbits during organogenesis did not produce teratogenicity at clinically relevant doses

Lactation

Acyclovir concentrations reported in breast milk following oral administration of acyclovir

There is no information regarding presence of acyclovir in human milk following ocular administration, effects on the breastfed infant, or effects on milk production

Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Synthetic purine nucleoside analogue is converted by the viral encoded thymidine kinase into acyclovir monophosphate, a nucleotide analogue then further converted to acyclovir triphosphate by other cellular enzymes

Acyclovir triphosphate inhibits DNA synthesis and viral replication by competing with nucleotides for viral DNA polymerase and being incorporated into viral DNA

Ophthalmic Administration

Advise patients to wash hands well and pull down lower lid of the affected eye to form a pocket

Apply 1-cm (1/2 inch) ribbon of ointment in the pocket formed by the lower lid (the lower cul-de-sac)

After application, advise patient to close their eye for 1-2 minutes Wipe any excess ointment away

Storage

Store at 20-25°C (68-77°F)