Version May 2024
Herpes, genital:
Note: The CDC discourages topical antiviral therapy for genital herpes infection due to minimal clinical benefit (Ref).
Topical ointment: Apply a 1/2-inch ribbon of ointment per 4-inch square surface area 6 times daily (every ~3 hours) for 7 days. Initiate as early as possible following onset of signs and symptoms.
Herpes labialis (cold sores), recurrent:
Topical cream: Apply 5 times daily for 4 days.
Buccal tablet: Apply one 50 mg tablet as a single dose to the upper gum region (canine fossa).
Herpes simplex virus, mucocutaneous (non-life-threatening, immunocompromised): Topical ointment: Apply a 1/2-inch ribbon of ointment per 4-inch square surface area 6 times daily (every ~3 hours) for 7 days. Initiate as early as possible following onset of signs and symptoms.
There are no dosage adjustments provided in the manufacturer's labeling. However, dosage adjustment is unlikely due to low systemic absorption.
There are no dosage adjustments provided in the manufacturer's labeling. However, dosage adjustment is unlikely due to low systemic absorption.
Refer to adult dosing.
(For additional information see "Acyclovir (topical): Pediatric drug information")
Herpes labialis (cold sores): Topical cream: Children ≥12 years and Adolescents: Apply 5 times/day for 4 days
There are no dosage adjustments provided in the manufacturer’s labeling; however, dosage adjustment is unlikely due to low systemic absorption.
There are no dosage adjustments provided in the manufacturer’s labeling; however, dosage adjustment is unlikely due to low systemic absorption.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%: Dermatologic: Local pain (ointment 30%; mild; includes transient burning and stinging)
1% to 10%:
Central nervous system: Lethargy (buccal tablet 1%)
Dermatologic: Erythema (buccal tablet 1%), skin rash (buccal tablet 1%)
Gastrointestinal: Aphthous stomatitis (buccal tablet 1%), gingival pain (buccal tablet 1%)
Local: Application site reaction (cream 5%; including dry lips, desquamation, dryness of skin, cracked lips, burning skin, pruritus, flakiness of skin, and stinging on skin); application site irritation (buccal tablet 1%)
<1%, postmarketing, and/or case reports: Anaphylaxis, angioedema, contact dermatitis, eczema, localized edema, local pruritus, pruritus
Hypersensitivity to acyclovir, valacyclovir, or any component of the formulation
Buccal tablet: Additional contraindications: Hypersensitivity to milk protein concentrate
Concerns related to adverse effects:
• Dermatologic toxicity: Cream may be irritating and cause contact sensitization. The sensitizing ingredient has not been identified.
Disease-related concerns:
• Appropriate use: Genital herpes: 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. There are no data to support the use of acyclovir ointment to prevent transmission of infection to other persons or prevent recurrent infections if no signs or symptoms are present.
• Appropriate use: Herpes labialis: Treatment should begin with the first signs or symptoms.
Special populations:
• Immunocompromised patients: Buccal tablet, cream: Use and safety has not been studied; use with caution.
Dosage form specific issues:
• Buccal tablet: Apply to the area of the upper gum above the incisor tooth on the same side as the symptoms; do not apply to the inside of the lip or cheek.
• Cream: For external use only to the lips and face; do not apply to eye or inside the mouth or nose, or to any mucous membranes.
• Ingredient precaution: Some products may contain milk protein concentrate.
• Ointment: For cutaneous use only; do not use in the eye.
Some dosage forms may contain propylene glycol; in neonates large amounts of propylene glycol delivered orally, intravenously (eg, >3,000 mg/day), or topically have been associated with potentially fatal toxicities which can include metabolic acidosis, seizures, renal failure, and CNS depression; toxicities have also been reported in children and adults including hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Shehab 2009).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Cream, External:
Zovirax: 5% (5 g) [contains cetostearyl alcohol, propylene glycol]
Generic: 5% (5 g)
Ointment, External:
Zovirax: 5% (30 g)
Generic: 5% (5 g, 15 g, 30 g)
Tablet, Buccal:
Sitavig: 50 mg [contains milk protein concentrate]
May be product dependent
Cream (Acyclovir External)
5% (per gram): $40.00 - $192.50
Cream (Zovirax External)
5% (per gram): $48.00
Ointment (Acyclovir External)
5% (per gram): $2.00 - $26.59
Ointment (Zovirax External)
5% (per gram): $6.00
Tablets (Sitavig Buccal)
50 mg (per each): $572.45
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Cream, External:
Zovirax: 5% (5 g) [contains cetostearyl alcohol, propylene glycol]
Ointment, External:
Zovirax: 5% (4 g, 30 g)
Generic: 5% (4 g, 5 g, 15 g, 30 g)
Oral: Buccal tablet: Apply within 1 hour after onset of prodromal symptoms and before appearance of any signs of lesions. Apply tablet with a dry finger immediately after removing it from packaging blister. Place tablets to the upper gum just above the incisor tooth (canine fossa) on the same side of the mouth as the prodromal symptoms and hold in place with slight pressure over the upper lip for 30 seconds to ensure adhesion. The rounded side of the tablet should be placed on the upper gum (for comfort purposes, does not affect efficacy). Do not crush, chew, suck, or swallow. If tablet falls off within the first 6 hours, reposition the same tablet immediately or apply a new tablet. If tablet is swallowed within the first 6 hours, drink a glass of water and apply a new tablet. If tablet falls out or is swallowed after the first 6 hours, do not reapply. Patients may eat and drink normally while tablet is in place. Avoid gum chewing, brushing teeth, wearing an upper denture or touching/pressing the tablet after placement. Rinse mouth gently if teeth need to be cleaned while the tablet is in place. Drink plenty of liquids in case of dry mouth.
Topical: Cream or ointment: Apply as early as possible following the onset of prodromal symptoms or when lesions appear.
Cream: Not for use on the genitals. Ensure the face and/or lips are clean and dry. Not for use in the eye, mouth or mucous membranes. Wash hands with soap and water prior to application and after application. Apply sufficient amount to adequately cover all lesions, including the outer margin. Avoid unnecessary rubbing of the affected area. Do not apply other topical products to the affected area during therapy.
Ointment: Not for use in the eye. Apply sufficient amount to adequately cover all lesions. Apply using a finger cot or rubber glove to avoid transmission to other parts of the body or to other persons.
Buccal tablet: Apply within 1 hour after onset of prodromal symptoms and before appearance of any signs of lesions. Apply tablet with a dry finger immediately after removing it from packaging. Place tablets to the upper gum just above the incisor tooth (canine fossa) on the same side of the mouth as the prodromal symptoms and hold in place with slight pressure over the upper lip for 30 seconds to ensure adhesion. The rounded side of the tablet should be placed on the upper gum (for comfort purposes, does not affect efficacy). Do not crush, chew, suck, or swallow. If tablet falls off within the first 6 hours, reposition the same tablet immediately or apply a new tablet. If tablet is swallowed within the first 6 hours, drink a glass of water and apply a new tablet. If tablet falls out or is swallowed after the first 6 hours, do not reapply. Patients may eat and drink normally while tablet is in place. Avoid gum chewing, brushing teeth, wearing an upper denture or touching/pressing the tablet after placement. Rinse mouth gently if teeth need to be cleaned while the tablet is in place. Drink plenty of liquids in case of dry mouth.
Topical: Cream or ointment: Apply as early as possible following the onset of prodromal symptoms or when lesions appear.
Cream: Not for use on the genitals. Ensure the face and/or lips are clean and dry. Not for use in the eye, mouth, or mucous membranes. Wash hands with soap and water prior to application and after application. Apply an amount to sufficiently cover the affected area, including the outer margin. Avoid unnecessary rubbing of the affected area. Do not apply other topical products to the affected area during therapy.
Ointment: Use a fingercot or rubber glove when applying ointment to prevent autoinoculation of other body sites or transmission of infection to other persons. Not for use in the eye.
Herpes virus:
Buccal tablet: Treatment of recurrent herpes labialis (cold sores) in immunocompetent adults
Cream: Treatment of recurrent herpes labialis (cold sores) in immunocompetent children ≥12 years of age, adolescents, and adults
Ointment: Management of initial genital herpes and in limited non-life-threatening mucocutaneous herpes simplex virus infections in immunocompromised patients. Note: The CDC discourages topical antiviral therapy for genital herpes infection due to minimal clinical benefit (CDC [Workowski 2021]).
Acyclovir may be confused with ganciclovir, Retrovir, valacyclovir
Zovirax may be confused with Doribax, Valtrex Zithromax, Zostrix, Zyloprim, Zyvox
Opthavir [Mexico] may be confused with Optivar brand name for azelastine [US]
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Talimogene Laherparepvec: Antiherpetic Antivirals may diminish the therapeutic effect of Talimogene Laherparepvec. Risk C: Monitor therapy
When administered orally, acyclovir crosses the placenta. The amount of acyclovir available systemically following topical application of the cream, buccal tablet, or ointment is significantly less in comparison to oral doses.
Refer to the Acyclovir (Systemic) monograph for additional information.
When administered orally, acyclovir is present in breast milk.
The amount of acyclovir available systemically following topical application of the cream, buccal tablet, or ointment is significantly less in comparison to oral doses. 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 the benefits of treatment to the mother. Patients with herpetic lesions near or on the breast should avoid breastfeeding.
Refer to the Acyclovir (Systemic) monograph for additional information.
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.
Absorption: Minimal
Buccal tablet: Single dose application of buccal tablets containing 50 mg to the buccal mucosa provided mean maximum salivary concentrations 8 hours after tablet application. Plasma concentrations were delayed (undetectable at 5 hours) and subsequently below antiviral activity concentration (0.018 to 0.055 mcg/mL).
Cream: Plasma concentrations following topical application of the cream were below the limit of detection in 5/6 male volunteers (<0.01 μM) and 0.014 μM in one subject.
Ointment: Following application of the ointment to patients with varicella-zoster infection, acyclovir plasma concentrations were <0.01 to 0.28 mcg/mL in patients with normal renal function and <0.01 to 0.78 mcg/mL in a patient with renal impairment.
Excretion: Urine (Buccal tablet: Primarily renally excreted unchanged; Cream: 0.04% of the daily dose; Ointment: <0.02% to 9.4% of the daily dose)
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