CLASSES
Gynecological Antifungals
Polyene Antifungals
Topical Dermatological Antifungals
DESCRIPTION
Topical polyene antifungal antibiotic.
Used in the treatment of oropharyngeal, cutaneous, mucocutaneous, and vulvovaginal candidiasis; not useful for systemic fungal infections.
Adverse events tend to be minimal due to limited systemic absorption.
COMMON BRAND NAMES
Bio-Statin, Mycostatin, Nyamyc, Nyata, Nystex, Nystop, Pedi-Dri, Pediaderm AF
HOW SUPPLIED
Bio-Statin/Nystatin Oral Cap: 500000U, 1000000U
Mycostatin/Nyamyc/Nyata/Nystatin/Nystop/Pedi-Dri Topical Pwd: 1g, 100000U
Mycostatin/Nystatin Oral Tab: 500000U
Mycostatin/Nystatin/Nystex Oral Susp: 1mL, 5mL, 100000U, 500000U
Mycostatin/Nystatin/Nystex/Pediaderm AF Topical Cream: 1g, 100000U
Nystatin/Nystex Topical Ointment: 1g, 100000U
DOSAGE & INDICATIONS
For the treatment of candidiasis, including gastrointestinal candidiasis and cutaneous and mucocutaneous candidiasis, including candidal diaper dermatitis.
For the treatment of gastrointestinal candidiasis.
Oral dosage (tablets)
Adults
500,000 to 1,000,000 units PO 3 times daily for at least 48 hours after clinical cure to prevent relapse.
For the treatment of cutaneous and mucocutaneous candidiasis, including candidal diaper dermatitis.
Topical dosage (cream or ointment)
Adults
Apply to affected area(s) twice daily until healing is complete.
Infants, Children, and Adolescents
Apply to affected area(s) twice daily until healing is complete.
Neonates
Apply to affected area(s) twice daily until healing is complete.
Topical dosage (topical powder)
Adults
Apply to affected area(s) 2 to 3 times daily until healing is complete. For infections of the feet, also dust powder in footwear. Topical powder is recommended over creams and ointments for very moist lesions.
Infants, Children, and Adolescents
Apply to affected area(s) 2 to 3 times daily until healing is complete. For infections of the feet, also dust powder in footwear. Topical powder is recommended over creams and ointments for very moist lesions.
Neonates
Apply to affected area(s) 2 to 3 times daily until healing is complete. For infections of the feet, also dust powder in footwear. Topical powder is recommended over creams and ointments for very moist lesions.
For the treatment of oropharyngeal candidiasis (thrush).
Oral dosage (suspension)
Adults
400,000 to 600,000 units (4 to 6 mL) PO 4 times daily for 7 to 14 days; divide dose so that one-half of each dose is placed in each side of the mouth. The FDA-approved duration is for at least 48 hours after clinical cure.
Children and Adolescents
400,000 to 600,000 units (4 to 6 mL) PO 4 times daily for 7 to 14 days; divide dose so that one-half of each dose is placed in each side of the mouth. The FDA-approved duration is for at least 48 hours after clinical cure.
Infants
200,000 units (2 mL) PO 4 times daily for 7 to 14 days; divide dose so that one-half of each dose is placed in each side of the mouth. Avoid feeding for 5 to 10 minutes. The FDA-approved duration is for at least 48 hours after clinical cure.
Neonates
200,000 units (2 mL) PO 4 times daily for 7 to 14 days; divide dose so that one-half of each dose is placed in each side of the mouth. Avoid feeding for 5 to 10 minutes. The FDA-approved duration is for at least 48 hours after clinical cure.
Premature Neonates
100,000 units (1 mL) PO 4 times daily for at least 48 hours after clinical cure based on limited data in premature and low birth weight neonates; divide each dose so that one-half of each dose is placed in each side of the mouth. Avoid feeding for 5 to 10 minutes.
For candidiasis prophylaxis† in high-risk premature neonates.
Oral dosage
Premature Neonates
100,000 units (1 mL) 3 times daily for 6 weeks is recommended by guidelines as an alternative therapy in premature neonates weighing less than 1500 g in cases where resistance or availability preclude the use of fluconazole. 100,000 units (1 mL) 3 to 4 times daily has reduced invasive candidiasis in studies of high-risk patients. Doses were either administered as half the dose placed in each side of the mouth or instilled into the stomach via oro/nasogastric tube. One study coated the mouth with 0.5 mL of nystatin and then gave the rest via orogastric tube. Duration of prophylaxis has varied. Avoid feeding for 5 to 10 minutes after a dose.
†Indicates off-label use
MAXIMUM DOSAGE
Adults
2.4 million units/day PO; maximum dosage information is not available for topical powder, cream, or ointment.
Geriatric
2.4 million units/day PO; maximum dosage information is not available for topical powder, cream, or ointment.
Adolescents
2.4 million units/day PO; maximum dosage information is not available for topical powder, cream, or ointment.
Children
2.4 million units/day PO; maximum dosage information is not available for topical powder, cream, or ointment.
Infants
800,000 units/day PO; maximum dosage information is not available for topical powder, cream, or ointment.
Neonates
Neonates: 800,000 units/day PO; maximum dosage information is not available for topical powder, cream, or ointment.
Premature Neonates: 400,000 units/day PO; maximum dosage information is not available for topical powder, cream, or ointment.
DOSING CONSIDERATIONS
Hepatic Impairment
No dosage adjustment needed.
Renal Impairment
No dosage adjustment needed.
ADMINISTRATION
Oral Administration
Oral Liquid Formulations
For topical, oral administration, use nystatin suspension as a swish and swallow. If using the powder for suspension, prepare only a single dose at a time because it does not contain preservatives.
Shake the suspension liquid well prior to each adminstration.
Use the provided dropper or a calibrated oral syringe for accurate dose measurement.
Administer one half of the dose in each side of the mouth.
The suspension should be retained in the mouth for as long as possible (e.g., several minutes) before swallowing.
Topical Administration
Topical preparations should not be applied to the eye.
Cream/Ointment/Lotion Formulations
Rub ointment or cream gently into the skin of the affected area.
Other Topical Formulations
Topical Powder
For the treatment of candidal infection of the feet, the powder should be dusted in shoes and socks, as well as on the feet.
Intravaginal Administration
Use vaginal applicators supplied by the manufacturer.
Instruct patient on proper administration.
STORAGE
Generic:
- Protect from freezing
- Protect from light
- Store at controlled room temperature (between 68 and 77 degrees F)
Bio-Statin :
- Refrigerate (between 36 and 46 degrees F)
Mycostatin:
- Protect from direct sunlight
- Protect from freezing
- Protect from heat
- Protect from light
- Store at controlled room temperature (between 68 and 77 degrees F)
Nyamyc:
- Avoid excessive heat (above 104 degrees F)
- Store at controlled room temperature (between 68 and 77 degrees F)
Nyata:
- Avoid excessive heat (above 104 degrees F)
- Store at controlled room temperature (between 68 and 77 degrees F)
Nystex:
- Protect from direct sunlight
- Protect from freezing
- Protect from heat
- Protect from light
- Store at controlled room temperature (between 68 and 77 degrees F)
Nystop:
- Avoid excessive heat (above 104 degrees F)
- Store at controlled room temperature (between 68 and 77 degrees F)
Pediaderm AF:
- Keep from freezing
- Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees F
Pedi-Dri:
- Avoid excessive heat (above 104 degrees F)
- Store at controlled room temperature (between 68 and 77 degrees F)
CONTRAINDICATIONS / PRECAUTIONS
Paraben hypersensitivity
Some formulations of nystatin, such as the nystatin oral suspension and the topical cream, contain methylparaben and propylparaben. These products should be used with caution in patients with paraben hypersensitivity.
Pregnancy
Animal reproduction studies have not been conducted with any oral or topical nystatin preparation. It also is not known whether these preparations can cause fetal harm when used during human pregnancy or can affect reproductive capacity. However, gastrointestinal absorption of oral nystatin is insignificant and systemic absorption is minimal. Topical nystatin products are not absorbed from intact skin or mucous membranes. Nystatin should be used during pregnancy only when clearly needed.
Breast-feeding
It is unknown whether oral nystatin is excreted in human milk. However, gastrointestinal absorption of oral nystatin is insignificant; therefore, minimal serum and milk concentrations would be expected. Topical nystatin products are not absorbed from intact skin or mucous membranes. 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 ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.
Diabetes mellitus
Because nystatin suspension contains significant amounts of sucrose, it should be used cautiously in patients with diabetes mellitus.
ADVERSE REACTIONS
Severe
Stevens-Johnson syndrome / Delayed / 0-0.1
eczema vaccinatum / Delayed / 0-0.1
bronchospasm / Rapid / Incidence not known
angioedema / Rapid / Incidence not known
Moderate
hyperglycemia / Delayed / Incidence not known
sinus tachycardia / Rapid / Incidence not known
Mild
diarrhea / Early / 1.0-10.0
vomiting / Early / 1.0-10.0
dyspepsia / Early / 1.0-10.0
nausea / Early / 1.0-10.0
urticaria / Rapid / 0-1.0
skin irritation / Early / 0-1.0
rash / Early / 0-1.0
pruritus / Rapid / 0-0.1
myalgia / Early / Incidence not known
DRUG INTERACTIONS
Econazole: (Moderate) The combination of econazole and nystatin represents duplication of therapy whenever the drugs are used by similar routes and are usually avoided.
Ketoconazole: (Moderate) The combination of ketoconazole and nystatin represents duplication of therapy whenever the drugs are used by similar routes and are usually avoided.
Miconazole: (Moderate) The combination of miconazole and nystatin represents duplication of therapy whenever the drugs are used by similar routes and are usually avoided.
Miconazole; Petrolatum; Zinc Oxide: (Moderate) The combination of miconazole and nystatin represents duplication of therapy whenever the drugs are used by similar routes and are usually avoided.
Oxiconazole: (Moderate) The combination of oxiconazole and nystatin represents duplication of therapy whenever the drugs are used by similar routes and are usually avoided.
Sertaconazole: (Moderate) The combination of sertaconazole and nystatin represent duplication of therapy whenever the drugs are used by similar route, and is usually avoided.
Sulconazole: (Moderate) The combination of sulconazole and nystatin represents duplication of therapy whenever the drugs are used by similar routes and are usually avoided.
PREGNANCY AND LACTATION
Pregnancy
Animal reproduction studies have not been conducted with any oral or topical nystatin preparation. It also is not known whether these preparations can cause fetal harm when used during human pregnancy or can affect reproductive capacity. However, gastrointestinal absorption of oral nystatin is insignificant and systemic absorption is minimal. Topical nystatin products are not absorbed from intact skin or mucous membranes. Nystatin should be used during pregnancy only when clearly needed.
It is unknown whether oral nystatin is excreted in human milk. However, gastrointestinal absorption of oral nystatin is insignificant; therefore, minimal serum and milk concentrations would be expected. Topical nystatin products are not absorbed from intact skin or mucous membranes. 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 ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.
MECHANISM OF ACTION
Nystatin is a polyene antifungal that binds to sterols in the cell membranes of both fungal and human cells. Nystatin is usually fungistatic in vivo but may have fungicidal activity at high concentrations or against extremely susceptible organisms. Nystatin has greater affinity for ergosterol, the sterol found in fungal cell membranes, than for cholesterol, the sterol found in human cell membranes; however, nystatin is too toxic to be used systemically. As a result of this binding, membrane integrity of both fungal cells and human cells is impaired, causing the loss of intracellular potassium and other cellular contents. Because bacteria do not contain sterols in their cell membranes, nystatin is ineffective against this class of organisms. Nystatin is also ineffective against protozoa, trichomonads, and viruses.
PHARMACOKINETICS
Nystatin is administered orally, topically, and intravaginally.
Oral Route
Although nystatin is used orally, it is poorly absorbed from the GI tract. After oral administration, nystatin is almost entirely excreted in feces as unchanged drug.
Topical Route
Nystatin is not absorbed from intact skin or mucous membranes.