Nystatin is a polyene antifungal antibiotic obtained from Streptomyces noursei. Structural formula:

C ₄₇ H ₇₅ NO ₁₇                             MW 926.13                       CAS-1400-61-9

MYCOSTATIN® (nystatin lozenges, USP) PASTILLES are round, light to dark gold-colored troches designed to dissolve slowly in the mouth. Each MYCOSTATIN PASTILLE provides 200,000 units nystatin. Inactive ingredients: anise oil, cinnamon oil, gelatin, sucrose, and other ingredients.

Nystatin is both fungistatic and fungicidal in vitro against a wide variety of yeasts and yeast-like fungi. Candida albicans demonstrates no significant resistance to nystatin in vitro on repeated subculture in increasing levels of nystatin; other Candida species become quite resistant. Generally, resistance does not develop in vivo . Nystatin acts by binding to sterols in the cell membrane of susceptible fungi with a resultant change in membrane permeability allowing leakage of intracellular components. Nystatin exhibits no activity against bacteria, protozoa, trichomonads, or viruses.

  Gastrointestinal absorption of nystatin is insignificant. Most orally administered nystatin is passed unchanged in the stool. Significant concentrations of nystatin may appear occasionally in the plasma of patients with renal insufficiency during oral therapy with conventional dosage forms.

Mean nystatin concentrations in excess of those required in vitro to inhibit growth of clinically significant Candida persisted in saliva for approximately two hours after the start of oral dissolution of two MYCOSTATIN PASTILLES (400,000 units nystatin) administered simultaneously to 12 healthy volunteers.

MYCOSTATIN PASTILLES are indicated for the treatment of candidiasis in the oral cavity.

CONTRAINDICATIONS

MYCOSTATIN PASTILLES are contraindicated in those patients with a history of hypersensitivity to any of the components.

PRECAUTIONS

General:    This medication is not to be used for the treatment of systemic mycoses.

In order to achieve maximum effect from the medication, MYCOSTATIN (nystatin lozenges, USP) PASTILLES must be allowed to dissolve slowly in the mouth; therefore, patients for whom the MYCOSTATIN PASTILLE is prescribed, including pediatric patients and the elderly, must be competent to utilize the dosage form as intended.

If irritation or hypersensitivity develops with MYCOSTATIN PASTILLES, treatment should be discontinued and appropriate therapy instituted.

Information for the Patient:   Patients taking this medication should receive the following information and instructions:

1. Use as directed; the medication is not for any disorder other than for which it was prescribed.
2. Allow the MYCOSTATIN PASTILLE to dissolve slowly in the mouth; do not chew or swallow the PASTILLE.
3. The patient should be advised regarding replacement of any missed doses.
4. There should be no interruption or discontinuation of medication until the prescribed course of treatment is completed even though symptomatic relief may occur within a few days.
5. If symptoms of local irritation develop, the physician should be notified promptly.
6. Good oral hygiene, including proper care of dentures, is particularly important for denture wearers.

Laboratory Tests:   If there is a lack of therapeutic response, appropriate microbiological studies (e.g., KOH smears and/or cultures) should be repeated to confirm the diagnosis of candidiasis and rule out other pathogens before instituting another course of therapy.

Carcinogenesis, Mutagenesis, Impairment of Fertility: Studies have not been performed to evaluate carcinogenic or mutagenic potential, or possible impairment of fertility in males or females.

Pregnancy: Teratogenic Effects:   "Category C". Animal reproduction studies have not been conducted with nystatin. It is also not known whether nystatin can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. MYCOSTATIN PASTILLES should be dispensed to a pregnant woman only if clearly needed.

Nursing Mothers:   It is not known whether nystatin is excreted in human milk. Although gastrointestinal absorbtion is insignificant, caution should be exercised when nystatin is prescribed for a nursing woman.

Pediatric Use:   The use of MYCOSTATIN PASTILLES has not been systematically studied in pediatric patients.

ADVERSE REACTIONS

MYCOSTATIN PASTILLES are generally well tolerated by all age groups, even during prolonged use. Rarely, oral irritation or sensitization may occur. Nausea has been reported occasionally during therapy.

Large oral doses of nystatin have occasionally produced diarrhea, gastrointestinal distress, nausea and vomiting. Rash, including urticaria has been reported rarely. Stevens-Johnson syndrome has been reported very rarely.

OVERDOSAGE

Oral doses of nystatin in excess of five million units daily have caused nausea and gastrointestinal upset. There have been no reports of serious toxic effects or superinfections (See CLINICAL PHARMACOLOGY , ).

DOSAGE AND ADMINISTRATION

Pediatric Patients and Adults:   The recommended dose is one or two MYCOSTATIN (nystatin lozenges, USP) PASTILLES (200,000 or 400,000 units nystatin) four or five times daily for as long as 14 days if necessary. The dosage regimen should be continued for at least 48 hours after disappearance of oral symptoms.

Dosage should be discontinued if symptoms persist after the initial 14 day period of treatment (see PRECAUTIONS , Laboratory Tests ).

Administration:   MYCOSTATIN PASTILLES must be allowed to dissolve slowly in the mouth, and should not be chewed or swallowed whole.

HOW SUPPLIED

MYCOSTATIN® (nystatin lozenges, USP) PASTILLES, 200,000 units nystatin each, in packages containing 30 pleasant-tasting PASTILLES ( NDC 0003-0543-20).

ALSO AVAILABLE

MYCOSTATIN® (nystatin, USP) is also available as a ready-to-use oral suspension, oral tablets, vaginal tablets, and topical powder, cream, and ointment (see package inserts accompanying those products for complete information).

Storage   Refrigerate between 2° and 8°C (36° and 46°F).

Manufactured by:

Ernest Jackson & Co., Ltd., Crediton, Devon, England

Distributed by:

Mead Johnson

ONCOLOGY PRODUCTS

A Bristol-Myers Squibb Company

Princeton, NJ 08543

U.S.A.

                                                                         1099698

K1-B001-12-99                            Revised August 1999