Embedded Files
Pharmacologic Category
Dosing: Adult
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)
HSV, mucocutaneous (non-life-threatening, immunocompromised): Topical ointment: 1/2” ribbon of ointment for a 4” square surface area every 3 hours (6 times daily) for 7 days
* See Dosage and Administration in AHFS Essentials for additional information.
Dosing: Geriatric
Refer to adult dosing.
Dosing: Renal Impairment: Adult
There are no dosage adjustments provided in the manufacturer’s labeling. However, dosage adjustment is unlikely due to low systemic absorption.
Dosing: Hepatic Impairment: Adult
There are no dosage adjustments provided in the manufacturer’s labeling. However, dosage adjustment is unlikely due to low systemic absorption.
Dosing: Pediatric
Herpes labialis (cold sores): Topical cream: Children ≥12 years and Adolescents: Apply 5 times/day for 4 days
Dosing: Renal Impairment: Pediatric
There are no dosage adjustments provided in the manufacturer’s labeling; however, dosage adjustment is unlikely due to low systemic absorption.
Dosing: Hepatic Impairment: Pediatric
There are no dosage adjustments provided in the manufacturer’s labeling; however, dosage adjustment is unlikely due to low systemic absorption.
Use: Labeled Indications
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 limited non-life-threatening mucocutaneous herpes simplex virus infections in immunocompromised patients
* See Uses in AHFS Essentials for additional information.
Use: Unsupported: Adult
Herpes, genital
Although included as an FDA-approved use in the manufacturer's prescribing information for management of initial genital herpes, the Centers for Disease Control and Prevention (CDC) discourages topical antiviral therapy for genital herpes infection due to minimal clinical benefit (CDC [Workowski 2015]).
Administration: 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.
Administration: 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.
Administration: Pediatric
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.
Storage/Stability
Buccal tablet: Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F). Protect from moisture.
Cream: Store at or below 25°C (77°F); excursions permitted between 15°C and 30°C (59°F and 86°F).
Ointment: Store at controlled room temperature of 20°C to 25°C (68°F to 77°F) in a dry place.
Medication Patient Education with HCAHPS Considerations
What is this drug used for?
• It is used to treat cold sores.
• It is used to treat genital warts.
• It is used to treat herpes infections.
Frequently reported side effects of this drug
• Burning
• Stinging
• Dry skin
• Itching
• Dry lips
• Application site pain
• Headache
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
• Severe application site irritation
• Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.
Medication Safety Issues
Sound-alike/look-alike issues:
International issues:
Contraindications
Hypersensitivity to acyclovir, valacyclovir, or any component of the formulation
Buccal tablet: Additional contraindications: Hypersensitivity to milk protein concentrate
Warnings/Precautions
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.
* See Cautions in AHFS Essentials for additional information.
Geriatric Considerations
No specific information concerning elderly patients.
Warnings: Additional Pediatric Considerations
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).
Pregnancy Considerations
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 details.
Breast-Feeding Considerations
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 continue or discontinue breastfeeding during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. Women with herpetic lesions near or on the breast should avoid breastfeeding.
Refer to the Acyclovir (Systemic) monograph for details.
Briggs' Drugs in Pregnancy & Lactation
Adverse Reactions
>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
* See Cautions in AHFS Essentials for additional information.
Allergy and Idiosyncratic Reactions
Metabolism/Transport Effects
None known.
Drug Interactions Open Interactions
Talimogene Laherparepvec: Antiherpetic Antivirals may diminish the therapeutic effect of Talimogene Laherparepvec. Risk C: Monitor therapy
Dosage Forms: US
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]
Dosage Forms: Canada
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Cream, External:
Zovirax: 5% (5 g)
Ointment, External:
Zovirax: 5% (4 g, 15 g, 30 g)
Generic: 5% (4 g, 5 g, 15 g, 30 g)
Anatomic Therapeutic Chemical (ATC) Classification
- D06BB03
Generic Available (US)
May be product dependent
Pricing: US
Cream (Acyclovir External)
5% (per gram): $182.37 - $192.50
Cream (Zovirax External)
5% (per gram): $202.63
Ointment (Acyclovir External)
5% (per gram): $6.80 - $26.59
Ointment (Zovirax External)
5% (per gram): $58.52
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.
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.
Pharmacodynamics/Kinetics
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)
Dental Use
Treatment of initial and prophylaxis of recurrent mucosal and cutaneous herpes simplex (HSV-1 and HSV-2) infections in immunocompromised patients
* See Uses in AHFS Essentials for additional information.
Local Anesthetic/Vasoconstrictor Precautions
No information available to require special precautions
Dental Health Professional Considerations
Although some conflicting data, dental treatment may be a risk factor for asymptomatic viral shedding of herpes simplex virus type-1 (HSV-1) into human saliva in patients with previous exposure to the virus (Hyland 2007).
It is recommended to reappoint the patient if an active lesion is present. If the lesion is already "crusted" over, treatment will not induce spread of the virus but treatment is aimed at patient comfort during the procedure relating to the wound healing on their lip.
Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Topical (Zovirax cream): Dry/cracked lips and dry/flaky skin were reported in fewer than 1 in 100 patients in clinical studies.
Effects on Bleeding
No information available to require special precautions
Dental Usual Dosing
Herpes labialis (cold sores): Children ≥12 years and Adults: Topical: Cream: Apply 5 times/day for 4 days
Mucocutaneous HSV: Adults: Nonlife-threatening, immunocompromised: Topical: Ointment: 1/2” ribbon of ointment for a 4” square surface area every 3 hours (6 times/day) for 7 days
Index Terms
Aciclovir; ACV; Acycloguanosine
FDA Approval Date
May 29, 1982
References
American Academy of Pediatrics Committee on Drugs. "Inactive" ingredients in pharmaceutical products: update (subject review). Pediatrics. 1997;99(2):268-278.[PubMed 9024461]
Hyland PL, Coulter WA, Abu-Ruman I, et al. Asymptomatic shedding of HSV-1 in patients undergoing oral surgical procedures and attending for noninvasive treatment. Oral Dis. 2007;13(4):414-418.[PubMed 17577329]
Shehab N, Lewis CL, Streetman DD, Donn SM. Exposure to the pharmaceutical excipients benzyl alcohol and propylene glycol among critically ill neonates. Pediatr Crit Care Med. 2009;10(2):256-259.[PubMed 19188870]
Sitavig (acyclovir) [prescribing information]. Charleston, SC: EPI Health LLC; December 2019.
Workowski KA, Bolan GA; Centers for Disease Control and Prevention (CDC). Sexually transmitted diseases treatment guidelines, 2015. MMWR Recomm Rep. 2015;64(RR-03):1-137.[PubMed 26042815]
Zovirax cream (acyclovir) [prescribing information]. Bridgewater, NJ: Valeant Pharmaceuticals; April 2018.
Zovirax ointment (acyclovir) [prescribing information]. Bridgewater, NJ: Alembic Pharmaceuticals; May 2018.
Brand Names: International
A.C.V. (TH); Acevirex (RO); Acic (AE, CY, EE, IE, KW, LV, QA); Acic Creme (DE); Aciclidan (DK); Aciclor (VE); Aciclosina (PT); Acifar (ID); Aciherpin (PH); Acirax (LK, VN); Acivir (CH, ET, IN, LV, QA); Acivirex (GT, HN, NI, SV); Activir (FR); Acycla (PH); Acyclostad (EG); Acyvir (EC); Agerp (UA); Anti (SE); Antix (NO); Astad (HK); Avir (VE); Avorax (SG); Cicloferon (CR, DO, GT, PA, SV); Cicloviral (CO); Civar (ET, LB, QA); Clinovir (ID, TH); Clovir (KW, SA, TW); Covelay (PH); Covir Cream (TH); Cusi Viral (KW); Cycloherp (HK, JO); Cyclostad (PH); Cyclovax (HK, TR); Cyclovir (IN); Danovir (ID); Declovir (ET, HK); Deherp (TW); Dravyr (SG); Ecuvir (EC); Entir (TH); Entir Cream (HK); Eurovir (PY); Expit (UY); Ezopen Creme (BR); Herpavir (JO); Herpecid (KR); Herpesin (CZ); Herpevir (FR); Herpex (IN); Herpizing (ET); Imavir (AE); Immunovir (MT); Licovir (ID); Lisovyr Cream (AR); Lisovyr Crema (CL); Lovire (ZA); Lovrak (JO, KW, QA); Marvir (TH); Matrovir (ID); Medovir (MY); Novirax (QA); Oppvir (TW); Poviral (AR); Qualiclovir (HK); Remex (FR); Soviclor (CR, DO, GT, HN, NI, PA, SV); Ultravir (BD); Univir (ET); Vicorax (TW); Viramed (ZW); Viratak (ZW); Viratop (BE); Virest (LK); Virex (CO); Virless (SG); Virolox (HR); Virzin (DE); Vitir (HK); Vivir (KR); Zeven (MY); Zevin (TH); Zoral (HK, MY, SG); Zorax (SG); Zorax Cream (MY); Zovir (DK, IS); Zovirax (AE, AR, AU, BB, BE, BH, BM, BR, BS, CH, CL, CN, CY, CZ, EC, EE, EG, ES, FI, FR, GB, GY, HK, HR, ID, IE, IL, IS, JM, JO, KR, KW, LB, LK, LT, LU, LV, MT, MY, NL, NO, NZ, PE, PR, PT, PY, QA, RO, SA, SE, SK, TH, TR, TT, TW, UY, VN, ZA, ZW); Zovirax Intensive (PL)
Last Updated 4/17/20
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