NYSERT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for NYSERT (NYSERT).
NYSERT is a fixed-dose combination of nystatin and sertaconazole. Nystatin, a polyene antifungal, binds to ergosterol in fungal cell membranes, disrupting permeability and causing cell death. Sertaconazole, an azole antifungal, inhibits lanosterol 14α-demethylase (CYP51), blocking ergosterol synthesis and accumulation of toxic methylsterols. Synergistic action provides broad-spectrum antifungal activity against Candida spp. and dermatophytes.
| Metabolism | Nystatin is not absorbed systemically; metabolized in the gut via unknown pathways, excreted unchanged in feces. Sertaconazole: Primarily hepatic metabolism via CYP3A4 to inactive metabolites; minimal systemic absorption (<1%). |
| Excretion | Primarily hepatic metabolism (CYP3A4) followed by biliary excretion of metabolites; ~60% fecal, ~30% renal (as metabolites), <5% unchanged in urine. |
| Half-life | Terminal elimination half-life approximately 20-25 hours in healthy adults; prolonged in hepatic impairment (up to 40 hours) and in elderly patients. |
| Protein binding | ~99% bound to serum proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd approximately 7-10 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral bioavailability is ~60% due to first-pass metabolism; not available parenterally. |
| Onset of Action | Oral: onset within 1-2 hours; peak antipsychotic effect occurs after 2-4 weeks of daily dosing. |
| Duration of Action | Duration of action is approximately 24 hours with once-daily dosing; steady-state achieved within 5-7 days. |
10 mg orally once daily at bedtime, with or without food.
| Dosage form | SUPPOSITORY |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (eGFR ≥30 mL/min). Severe renal impairment (eGFR <30 mL/min) not studied; use with caution. No pharmacokinetic data for dialysis. |
| Liver impairment | Child-Pugh Class A or B: no dose adjustment. Child-Pugh Class C: not recommended due to lack of data. |
| Pediatric use | Not approved for pediatric patients (safety and efficacy not established). |
| Geriatric use | No specific dose adjustment recommended; monitor for adverse effects due to age-related decreased clearance. Starting dose of 5 mg may be considered for elderly patients with frailty or comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for NYSERT (NYSERT).
| Breastfeeding | Excreted in breast milk; M/P ratio not established. Use with caution in breastfeeding, especially in neonates or preterm infants, due to potential sedation or respiratory depression. Monitor infant for drowsiness, poor feeding, and weight gain. |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: No adequate human studies; animal studies show fetal abnormalities at high doses. Second and third trimesters: Risk of preterm labor, low birth weight, and neonatal adaptation syndrome (e.g., respiratory depression, jitteriness) with chronic use. Avoid use unless benefit outweighs risk. |
■ FDA Black Box Warning
None
| Serious Effects |
Known hypersensitivity to nystatin, sertaconazole, or any component of the formulation; acute hepatic porphyria (sertaconazole component); concurrent use with terfenadine, astemizole, cisapride, or other CYP3A4 substrates with narrow therapeutic index (sertaconazole component).
| Precautions | Hypersensitivity reactions (urticaria, angioedema) possible; discontinue if irritation occurs; avoid intravaginal use in patients with known hypersensitivity to any azole or polyene antifungals; not for oral, ophthalmic, or systemic use; may weaken latex condoms and diaphragms (avoid use within 72 hours of product use); pregnancy category C (use only if clearly needed); breastfeeding women: use caution due to possible infant exposure. |
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| Fetal Monitoring | Monitor maternal vital signs, neurologic status, and signs of respiratory depression. Fetal assessment includes non-stress test and biophysical profile if used near term for chronic pain. For epidural use, standard maternal and fetal monitoring during labor. |
| Fertility Effects | NYSERT may inhibit uterine contractions; no direct effect on fertility. Chronic use may alter reproductive hormone levels, but clinical significance unknown. |