New Release: Alpha testing version has been released.

Nystatin

D07C - Corticosteroids, combinations with antibiotics ATC A07AA02 Unknown approved 1964 Oral Topical

JFDA label: Rianest Oral Suspension

Mechanism of Action

Sequestering Agent of Ergosterol — Ergosterol sequestering agent

TargetActionGene / class
Ergosterol efficacy SEQUESTERING AGENT

Indications

Approved

  • Candidiasis — candidiasis
  • Infections — infection

Off-label

  • Bacteremia
  • Burns
  • Candidiasis, Oral
  • Graft vs Host Disease
  • HIV Infections
  • Leukemia
  • Lymphoma
  • Multiple Myeloma
  • Myelodysplastic Syndromes
  • Myeloproliferative Disorders
  • Pneumonia
  • Stomatitis
  • Stomatitis, Denture
  • Tobacco Use Disorder
  • Vaginosis, Bacterial

Class profile

antifungalClassPolyene
targetMoleculeErgosterol (membrane disruption)
isFungicidal1
spectrumCandidaS (topical/oral)
spectrumAspergillusNot used systemically
spectrumCryptococcusNot used systemically
spectrumDermatophytesLimited
resistanceMechanismsErgosterol deficiency mutations (clinical resistance rare with topical use)
sourcePappas2016/Lass-Florl2011

Contraindications

Source: openFDA

  • The preparation is contraindicated in patients with a history of hypersensitivity to any of its components. Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Skin and subcutaneous tissue disorders (3)

Not Known Eczema · Itching · Rash

General disorders and administration site conditions (1)

Not Known Burning

Dosing

Source: openFDA

2 mL (200,000 units) four times daily (in infants and young children, use dropper to place one-half of dose in each side of mouth and avoid feeding for 5 to 10 minutes). NOTE: Limited clinical studies in premature and low birth weight infants indicate that 1 mL four times daily is effective. CHILDREN AND ADULTS: 4 to 6 mL (400,000 to 600,000 units) four times daily (one-half of dose in each side of mouth). The preparation should be retained in the mouth as long as possible before swallowing. Continue treatment for at least 48 hours after perioral symptoms have disappeared and cultures demonstrate eradication of Candida albicans .

Pregnancy & Lactation

Pregnancy

Lactation

Caution Hale L3

Nystatin is less effective than other topical agents for the treatment of thrush.

Monitoring

EfficacyFungal culture and species identification; minimum inhibitory concentration (MIC) where available; clinical response (temperature, imaging for invasive fungal disease)
ToxicityLFTs (hepatotoxicity — azoles in particular); renal function; ECG for QT prolongation (azoles); drug levels if available (itraconazole, voriconazole)
Clinical pearlVoriconazole levels are highly variable due to CYP2C19 polymorphism — TDM recommended (target trough 2–5 mg/L). Check for drug interactions with CYP3A4 substrates.
CounselingReport visual disturbances (voriconazole), jaundice, or rash. Take azoles with food or as directed to optimise absorption.

Chemistry & Properties

2D structure
FormulaC47H75NO17
Molecular weight926.1 g/mol
IUPAC name(1S,15S,16R,17R,18S,19E,21E,25E,27E,29E,31E)-33-[(2S,3S,4S,5S,6R)-4-amino-3,5-dihydroxy-6-methyloxan-2-yl]oxy-1,3,4,7,9,11,17,37-octahydroxy-15,16,18-trimethyl-13-oxo-14,39-dioxabicyclo[33.3.1]nonatriaconta-19,21,25,27,29,31-hexaene-36-carboxylic acid
CAS1400-61-9
PubChem CID6433272
InChIKeyVQOXZBDYSJBXMA-RKEBNKJGSA-N
logP-0.2 (XLogP -0.2)
Polar surface area320.0 Ų
H-bond acceptors / donors18 / 12
SMILESCC1C=CC=CCCC=CC=CC=CC=CC(CC2C(C(CC(O2)(CC(C(CCC(CC(CC(CC(=O)OC(C(C1O)C)C)O)O)O)O)O)O)O)C(=O)O)OC3C(C(C(C(O3)C)O)N)O

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability70.0%
Half-life4.191 h
Volume of distribution0.268 L/kg
Protein binding59.6%
BBB penetrantNo

Enzyme interactions

EnzymeRoleDetail
CYP2C8Inhibitor

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)OATP2B1 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (16)

BrandForm / strengthPackAgentCitizen (JOD)
Nystaform Oint Ointment 1 g, 3 g, 1 g 20 g tube AL-Faiasel Drug Store 0.930
Nystatin Oral Suspension Suspension 100000 IU 30 ml AL EIMAN DRUG STORE CO LLC 1.030
kenacin cream Cream 100000 IU, 0.1 %, 0.025 %, 0.25 % 15 g tube pack varies MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN 1.370
kenacin oint Ointment 100000 IU, 0.1 %, 0.025 %, 0.25 % 15 g tube pack varies MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN 1.370
Panderm Cream Cream 10.000000 IU/100 g, 0.025 g/100 g, 0.25 g/100 g, 0.1 g/100 g 15 g tube pack varies Professional Drug Store 1.420
Kenaphil Cream Cream 0.326 g/tube, 0.00375 g/tube, 0.055161 g/tube, 0.015 g/tube 15 g tube PHILADELPHIA PHAEMACEUTICALS.COMP/JORDAN 1.510
Mycophil Ointment Ointment 100000 IU/g 30 g tube PHILADELPHIA PHAEMACEUTICALS.COMP/JORDAN 1.650
Rianest Oral Suspension Suspension 100.000 IU/ml 30 ml Khoury Drug Store 1.830
Mycophil Susp. Suspension 500000 Unit/5 ml 30 ml PHILADELPHIA PHAEMACEUTICALS.COMP/JORDAN 1.840
Mycosat oral suspention Injection 100000 IU/ml 30 ml pack varies Amman Pharmaceutical Industries Co 1.930
Panderm Cream Cream 10.000000 IU/100 g, 0.025 g/100 g, 0.25 g/100 g, 0.1 g/100 g 30 g tube pack varies Professional Drug Store 2.480
Polygynax 6 Vag. Cap. Capsule 100000 IU, 35, 000 IU, 35, 000 IU 6 cap Quality Drug Store 2.700
Mycophil Susp. Suspension 500000 Units/5 ml 60 ml PHILADELPHIA PHAEMACEUTICALS.COMP/JORDAN 3.500
Mycosat oral suspention Injection 100000 IU/ml 60 ml pack varies Amman Pharmaceutical Industries Co 3.500
Topsym polyvalent oint. Ointment 100.000 IU 15 g tube Nabulsi Drug Store 4.520
Polygynax 12 Ovules Ovule 100000 IU, 35000 IU, 35000 IU 12 Quality Drug Store 4.710