PDR MEMBER LOGIN:
  • PDR Search

    Required field
  • Advertisement
  • CLASSES

    Combinations of Corticosteroids with Antivirals
    Topical Antivirals

    DEA CLASS

    Rx

    DESCRIPTION

    Topical antiviral and steroid combination agent for herpes labialis (cold sores).

    COMMON BRAND NAMES

    Xerese

    HOW SUPPLIED

    Xerese Topical Cream: 5-1%

    DOSAGE & INDICATIONS

    For the early treatment of recurrent herpes labialis (cold sores) to reduce the likelihood of ulcerative cold sores and to shorten the lesion healing time.
    Topical dosage
    Adults, Adolescents, and Children >= 6 years

    Apply topically to orofacial affected area 5 times per day for 5 days as early as possible after the first signs and symptoms of herpes labialis occur (during the prodrome or when lesions appear).

    MAXIMUM DOSAGE

    Adults

    Apply 5x/day.

    Geriatric

    Apply 5x/day.

    Adolescents

    Apply 5x/day.

    Children

    >= 6 years: Apply 5x/day.
    < 6 years: Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    Neonates

    Safety and efficacy have not been established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

    Renal Impairment

    Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

    ADMINISTRATION

    Topical Administration
    Cream/Ointment/Lotion Formulations

    Apply acyclovir; hydrocortisone cream topically to cold sore lesions.
    Apply a quantity sufficient to cover the affected area, including the outer margin.
    Avoid unnecessary rubbing of the affected area to avoid aggravating or transferring the infection.
    Do not apply the topical cream to the eye, inside the mouth or nose, or on the genitals.
    Use a finger cot or rubber glove when applying to avoid transmission of the virus to other sites or persons.
    Wash hands thoroughly after administration.
    Do not cover cold sore with an occlusive dressing or bandage.
    Do not use other skin products (make-up, sun screen, lip balm) or other skin medications on the cold sore or around the cold sore.
    Do not bathe, shower, or swim, within 30 minutes of applying acyclovir; hydrocortisone.

    STORAGE

    Xerese:
    - Do not freeze
    - Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees F

    CONTRAINDICATIONS / PRECAUTIONS

    General Information

    NOTE: This monograph discusses the use of the acyclovir; hydrocortisone topical combination product. Clinicians may wish to consult the individual monographs of acyclovir or hydrocortisone for more information about each specific agent.

    Fungal infection

    Acyclovir; hydrocortisone is for herpes labialis infections. Other orofacial lesions, including those caused by a bacterial or fungal infection, may be difficult to distinguish from cold sores. Patients should seek medical advice when a potential cold sore fails to heal within 2 weeks to determine if another infectious process is taking place.

    Ophthalmic administration

    Acyclovir; hydrocortisone is intended for cutaneous herpes labialis use only. Avoid ophthalmic administration, administration inside the mouth or nose, or administration to the genitals.

    Immunosuppression

    Acyclovir; hydrocortisone has been studied in immunocompromised patients; however, data are insufficient to support its use in patients with immunosuppression. Immunocompromised patients should consult a physician regarding the treatment of herpes labialis. In clinical trials of immunocompromised patients, the mean healing time for cold sores was similar between the acyclovir; hydrocortisone group (6.6 days) and the 5% topical acyclovir group (6.9 days).

    Children, infants, neonates

    The safety and effectiveness of acyclovir; hydrocortisone in neonates, infants, and children less than 6 years of age have not been established.

    Geriatric

    In clinical studies of acyclovir; hydrocortisone, there were insufficient patients greater than 65 years of age to make any conclusions regarding safety and efficacy. However, the available data suggest that results were similar between geriatric patients and younger patients.

    Pregnancy

    Acyclovir; hydrocortisone is classified as FDA pregnancy category B. There are no adequate and well-controlled studies of systemic acyclovir in pregnant women. A prospective epidemiologic registry of systemic acyclovir use in the first trimester of pregnancy showed similar birth defect rates as compared to the general population; however, the size of the registry (n=749) was insufficient to evaluate the risk for less common birth defects or to allow for reliable conclusions regarding the safety of systemic acyclovir in pregnant women. Corticosteroids, such as hydrocortisone, are considered teratogenic in laboratory animals when administered systemically and potent corticosteroids have been shown to be teratogenic in laboratory animals after dermal application. Systemic exposure of acyclovir and hydrocortisone after topical administration for herpes labialis is expected to be minimal; however, caution is warranted if used in pregnant women.

    Breast-feeding

    The manufacturer advises caution when administering acyclovir; hydrocortisone to women who are breast-feeding as it is not known whether topically applied acyclovir or hydrocortisone is excreted in breast milk. However, systemic exposure after topical administration of acyclovir; hydrocortisone when used to treat cold sores is expected to be minimal. Instruct nursing mothers to avoid topical application to the breast. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    ADVERSE REACTIONS

    Moderate

    erythema / Early / 0-1.0
    contact dermatitis / Delayed / Incidence not known

    Mild

    xerosis / Delayed / 0-1.0
    skin irritation / Early / Incidence not known

    DRUG INTERACTIONS

    There are no drug interactions associated with Acyclovir; Hydrocortisone products.

    PREGNANCY AND LACTATION

    Pregnancy

    Acyclovir; hydrocortisone is classified as FDA pregnancy category B. There are no adequate and well-controlled studies of systemic acyclovir in pregnant women. A prospective epidemiologic registry of systemic acyclovir use in the first trimester of pregnancy showed similar birth defect rates as compared to the general population; however, the size of the registry (n=749) was insufficient to evaluate the risk for less common birth defects or to allow for reliable conclusions regarding the safety of systemic acyclovir in pregnant women. Corticosteroids, such as hydrocortisone, are considered teratogenic in laboratory animals when administered systemically and potent corticosteroids have been shown to be teratogenic in laboratory animals after dermal application. Systemic exposure of acyclovir and hydrocortisone after topical administration for herpes labialis is expected to be minimal; however, caution is warranted if used in pregnant women.

    The manufacturer advises caution when administering acyclovir; hydrocortisone to women who are breast-feeding as it is not known whether topically applied acyclovir or hydrocortisone is excreted in breast milk. However, systemic exposure after topical administration of acyclovir; hydrocortisone when used to treat cold sores is expected to be minimal. Instruct nursing mothers to avoid topical application to the breast. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    MECHANISM OF ACTION

    Acyclovir: Acyclovir has inhibitory activity against herpes simplex virus 1 (HSV-1) and herpes simples virus 2 (HSV-2) in vitro and in vivo. Acyclovir selectively binds the thymidine kinase (TK) enzyme to inhibit viral DNA synthesis. The viral TK enzyme converts acyclovir into acyclovir monophosphate (a nucleotide analogue), which is further converted into acyclovir diphosphate and then acyclovir triphosphate. Acyclovir triphosphate competitively inhibits and inactivates viral DNA polymerase. It is also incorporated into and terminates the viral DNA chain. Viral resistance can result from qualitative and quantitative changes in the viral TK enzyme and/or viral DNA polymerase. HSV isolates with reduced acyclovir susceptibility have been recovered from immunocompromised patients. Viral resistance should be considered in patients who show poor clinical response during therapy.
    Hydrocortisone: Hydrocortisone is the main glucocorticoid secreted by the adrenal cortex. When used topically, hydrocortisone exhibits anti-inflammatory properties that help suppress the clinical manifestations associated with the herpes infection outbreak.

    PHARMACOKINETICS

    Acyclovir; hydrocortisone is administered topically.
    Acyclovir: Minimal absorption of acyclovir is expected after topical application of acyclovir; hydrocortisone. If acyclovir does reach systemic circulation, it would be expected to undergo metabolism and excretion similar to systemically administered acyclovir. After systemic administration, infected viral cells transform acyclovir to its active triphosphate, and a small proportion may be metabolized extracellularly. Renal elimination via glomerular filtration and tubular secretion of unchanged drug is the major route of elimination accounting for 62—91% of the dose. The elimination half-life of acyclovir is 2.5—3.3 hours.
    Hydrocortisone: If hydrocortisone is absorbed through the skin, it binds to plasma proteins. Hydrocortisone is metabolized primarily in the liver and then excreted by the kidneys.

    Topical Route

    Acyclovir: Acyclovir; hydrocortisone plasma concentrations have not been measured after topical administration on cold sores; however, when applied as a single ingredient topically, systemic absorption is minimal with no drug detected in the blood or urine.
    Hydrocortisone: Acyclovir; hydrocortisone plasma concentrations have not been measured after topical administration on cold sores. However, many factors determine the extent of percutaneous absorption of topical corticosteroids, including the vehicle used, the integrity of the epidermal barrier, and the use of occlusive dressings. Topical corticosteroids can be absorbed from normal, intact skin and can have systemic side effects depending on the potency of the steroid and the size of the surface area to which the steroid is applied. Inflammation and other diseases of the skin that disrupt the skin barrier can increase percutaneous absorption.