Acyclovir 50 MG Buccal Tablet
DRUG INTERACTIONS
Due to low dose and minimal systemic absorption of SITAVIG, drug interactions are unlikely (7).
OVERDOSAGE
10 Acyclovir absorption and systemic exposure following application of SITAVIG are minimal.
Overdose is therefore unlikely [see Clinical Pharmacology (12.3)].
Symptomatic and supportive care is the basis for management.
DESCRIPTION
11 SECTION SITAVIG (acyclovir) buccal tablet is applied topically to the gum and releases acyclovir as the buccal tablet gradually dissolves [see Clinical Pharmacology (12.3)].
Acyclovir is a synthetic purine nucleoside analogue active against herpes viruses.
The chemical name of acyclovir is 2-amino-1,9-dihydro-9-[(2-hydroxyethoxy)methyl]-6H-purin-6-one; it has a molecular formula of C8H11N5O3 and a molecular weight of 225.
The structural formula is shown in Figure 1.
Acyclovir drug substance is a white or almost white crystalline powder.
SITAVIG contains 50 mg of acyclovir, USP and the following inactive ingredients: hypromellose, USP; milk protein concentrate; sodium lauryl sulfate, NF; magnesium stearate, NF; microcrystalline cellulose, NF; povidone, USP; colloidal silicon dioxide, NF.
Structure
CLINICAL STUDIES
14 Clinical Studies Study in Patients with Recurrent Herpes Labialis (cold sores) The efficacy and safety of SITAVIG was evaluated in a randomized, double-blind, placebo-controlled, patient-initiated, multicenter trial comparing SITAVIG 50 mg administered as a single dose (n = 378) to placebo (n = 397) in patients with recurrent herpes labialis (cold sores).
A total of 376 SITAVIG treated patients and 395 placebo treated patients were included in the Intent to Treat (ITT) efficacy population defined as all patients who took study treatment and who had a start date and time of treatment initiation recorded.
The mean age was 41.0 years (range: 18-80 years) and the majority of patients were female (68.6%), and Caucasian (94.9%).
All patients had at least 4 herpes episodes in the previous year of whom 68.4% had ≥ 5 episodes.
Patients were instructed to initiate treatment within one hour after the onset of prodromal symptoms and before the appearance of any signs of herpes labialis lesions by applying the tablet to the buccal mucosa in the canine fossa.
If the tablet was detached within the first 6 hours, subjects were instructed to reapply a tablet.
The mean and median durations of the recurrent herpes labialis episode (ITT population, n=771) were approximately half a day shorter in patients treated with SITAVIG compared with patients treated with placebo.
HOW SUPPLIED
16 /STORAGE AND HANDLING SITAVIG 50 mg buccal tablets are supplied as off-white tablets containing 50 mg of acyclovir.
SITAVIG tablets have a rounded side and a flat side.
SITAVIG tablets are packaged in blisters (NDC 68712-049-02).
SITAVIG should be stored at 20 to 25°C (68 to 77°F) [see USP controlled room temperature]; excursions between 15 and 30°C (59-86°F) permitted at room temperature.
Protect from moisture, and keep out of reach of children.
GERIATRIC USE
8.5 Geriatric Use Clinical studies of SITAVIG did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects.
DOSAGE FORMS AND STRENGTHS
50 mg buccal tablets (3).
MECHANISM OF ACTION
12.1 Mechanism of Action Acyclovir is an antiviral drug [see Microbiology (12.4)].
INDICATIONS AND USAGE
SITAVIG is indicated for the treatment of recurrent herpes labialis (cold sores) in immunocompetent adults (1).
PEDIATRIC USE
8.4 Pediatric Use Safety and effectiveness of SITAVIG in pediatric patients have not been established.
The ability of pediatric patients to comply with the application instructions has not been evaluated.
Use in younger children is not recommended due to potential risk of choking.
PREGNANCY
8.1 Pregnancy Pregnancy Category B No studies with SITAVIG have been performed in pregnant women.
Systemic exposure of acyclovir following buccal administration of SITAVIG is minimal.
SITAVIG should be used during pregnancy only if the potential benefit outweighs the potential risk to the fetus.
There are no adequate and well-controlled studies of systemic acyclovir in pregnant women.
A prospective epidemiologic registry of acyclovir use during pregnancy between 1984 and 1999 followed 749 pregnancies in women exposed to systemic acyclovir during the first trimester of pregnancy resulting in 756 outcomes.
The occurrence rate of birth defects approximated that found in the general population.
However, the size of the registry was insufficient to evaluate the risk for less common defects or to permit reliable or definitive conclusions regarding the safety of acyclovir in pregnant women and their developing fetuses.
Animal Data Animal reproduction studies have not been conducted with SITAVIG.
Acyclovir was not teratogenic in the mouse, rabbit or rat at exposures greatly in excess of human exposure.
NUSRING MOTHERS
8.3 Nursing Mothers It is not known whether topically applied acyclovir is excreted in breast milk.
Systemic exposure following buccal administration is minimal.
After oral administration of acyclovir, concentrations have been documented in breast milk in 2 women and ranged from 0.6 to 4.1 times the corresponding plasma levels.
These concentrations would potentially expose the nursing infant to a dose of acyclovir up to 0.3 mg/kg/day.
There is no experience with SITAVIG in nursing mothers.
SITAVIG should be administered to a nursing mother with caution.
INFORMATION FOR PATIENTS
Patient Information SITAVIG (SIT-a-vig) (acyclovir) buccal tablets What is SITAVIG? • SITAVIG is a prescription medicine used to treat cold sores (herpes labialis) in adults with normal immune systems.
• It is not known if SITAVIG is safe and effective in children.
Who should not use SITAVIG? Do not use SITAVIG if you are allergic to: • acyclovir or any of the ingredients in SITAVIG.
See the end of this leaflet for a complete list of ingredients in SITAVIG.
• milk protein concentrate Before using SITAVIG, tell your healthcare provider about all of your medical conditions, including if you: • are pregnant or plan to become pregnant.
It is not known if SITAVIG will harm your unborn baby.
• are breastfeeding or plan to breastfeed.
It is not known if SITAVIG passes into your breast milk.
• Tell your healthcare provider about all the medicines you take, including prescription or over-the-counter medicines, vitamins, or herbal supplements.
H ow should I use SITAVIG? See the detailed Instructions for Use for information about how to use SITAVIG.
• Use SITAVIG exactly as your healthcare provider tells you to use it.
• Use SITAVIG within 1 hour after you have the first symptom of a cold sore, such as itching, redness, burning, or tingling, and before a cold sore appears.
• You may eat and drink while using SITAVIG.
• Do not crush, chew, suck, or swallow SITAVIG tablets.
• SITAVIG will slowly dissolve over time while in your mouth and should be left in place.
• Gently rinse your mouth with water to clean your teeth while SITAVIG is in place.
• Drink more liquids if your mouth becomes dry while using SITAVIG.
What should I avoid while using SITAVIG? You should avoid activities that may prevent SITAVIG from sticking to your gum, including: touching or pressing SITAVIG after you apply it, wearing upper dentures, chewing gum, and brushing your teeth during the treatment day.
What are the possible side effects of SITAVIG? The most common side effects of SITAVIG include: headache and pain where SITAVIG is applied.
These are not all the possible side effects of SITAVIG.
Call your doctor for medical advice about side effects.
You may report side effects to FDA at 1-800-FDA-1088.
How should I store SITAVIG? • Store SITAVIG between 68°F to 77°F (20°C to 25°C).
Keep SITAVIG tablets dry.
Keep SITAVIG and all medicines out of the reach of children.
General information about the safe and effective use of SITAVIG Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet.
Do not use SITAVIG for a condition for which it was not prescribed.
Do not give SITAVIG to other people, even if they have the same symptoms that you have.
It may harm them.
You can ask your pharmacist or healthcare provider for information about SITAVIG that is written for health professionals.
What are the ingredients in SITAVIG? Active ingredient: acyclovir Inactive ingredients: hypromellose, milk protein concentrate, sodium lauryl sulfate, magnesium stearate,microcrystalline cellulose, povidone, colloidal silicon dioxide.
Manufactured By: Farméa,10 rue Bouché Thomas, ZAC d’orgemont, 49 000 Angers – France For more information call 1-800-499-4468.
This Patient Information has been approved by the U.S.
Food and DrugAdministration.
Issue: April/2013
DOSAGE AND ADMINISTRATION
Application of one SITAVIG 50 mg buccal tablet as a single dose to the upper gum (canine fossa) region (2.1).
SITAVIG should be applied within one hour after the onset of prodromal symptoms and before the appearance of any signs of herpes labailis.
Do not crush, chew, suck or swallow tablets (2.2)