NILSTAT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for NILSTAT (NILSTAT).
Nystatin binds to ergosterol in fungal cell membranes, forming pores that disrupt membrane integrity and cause leakage of intracellular contents, leading to fungal cell death.
| Metabolism | Nystatin is not absorbed significantly from the gastrointestinal tract after oral administration; it is excreted unchanged in feces. |
| Excretion | Primarily via feces as unchanged drug; negligible urinary excretion (<1%). |
| Half-life | Not well-defined due to minimal systemic absorption following oral or topical administration; estimated to be <1 hour in systemic circulation if absorbed. |
| Protein binding | Negligible due to poor aqueous solubility; <1% bound to plasma proteins. |
| Volume of Distribution | Not applicable due to minimal systemic absorption; estimated to be <0.1 L/kg if absorbed. |
| Bioavailability | <5% after oral administration due to poor gastrointestinal absorption; topical bioavailability not defined. |
| Onset of Action | Within 24-72 hours for oral candidiasis; immediate for topical application. |
| Duration of Action | 48-72 hours after cessation of therapy; prolonged with continuous administration. |
| Action Class | Cephalosporins: 3 generation |
| Brand Substitutes | Lupitax 500mg Injection, Evacef 500mg Injection, Edicef 500mg Injection, Desatax 500mg Injection, X Ceff 500mg Injection |
Topical: Apply 100,000 units/g cream or ointment to affected area twice daily. Oral suspension: 100,000 units/mL; 4-6 mL swish and swallow four times daily for 14 days. Oral tablets: 500,000 units; 1-2 tablets three times daily.
| Dosage form | SUSPENSION |
| Renal impairment | No dose adjustment required for any level of renal impairment. |
| Liver impairment | No dose adjustment required for any Child-Pugh class (A, B, or C). |
| Pediatric use | Oral suspension: Neonates and infants: 100,000 units (1 mL) four times daily. Children: 100,000-250,000 units (1-2.5 mL) four times daily. Topical: Same as adult, apply twice daily. |
| Geriatric use | No specific dose adjustment; use age-appropriate formulations with caution in patients with swallowing difficulties, but no pharmacokinetic changes necessitate dose modification. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for NILSTAT (NILSTAT).
| Breastfeeding | Nystatin is poorly absorbed from the gastrointestinal tract and not systemically available after topical use. It is not detected in breast milk in clinically relevant amounts. The M/P ratio is not available due to undetectable levels. Considered compatible with breastfeeding. |
| Teratogenic Risk | Topical nystatin is not systemically absorbed and is considered low risk for teratogenicity. No known fetal risks in any trimester when used topically. Oral and vaginal formulations have minimal systemic absorption and are generally considered safe, but data are limited. No association with congenital malformations has been reported. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to nystatin or any component of the formulation.
| Precautions | Hypersensitivity reactions may occur; discontinue if irritation or sensitization develops. Use with caution in patients with severe renal impairment (though systemic absorption is minimal). |
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| Fetal Monitoring | No specific maternal or fetal monitoring is required due to negligible systemic absorption. Routine prenatal care is sufficient. |
| Fertility Effects | No known effects on fertility in males or females based on available data. |