What Is Nystatin?

Nystatin is a polyene antibiotic. In 1950, it was discovered that the soil microorganism Streptomyces noursei can secrete an antifungal substance, and thus the first antifungal antibiotic was discovered. Nystatin has a conjugated polyene macrolide structure, can inhibit the activity of fungi and dermatomyces, and has no inhibitory effect on bacteria.

Drug Name: Nystatin

Foreign name: Nystatin
Main indications: Candidiasis enteritis, oral candidiasis

Nystatin Basic Information

Chinese name: nystatin

Chinese alias: nystatin

English name: Nystatin

English alias: Fungicidin Mycostatin; nilstat; Nystain; biofanal; nystatin A1; nystatin A2; nystan; Nyotran; Nystex; stamycin; MORONAL; Nystop

CAS number: 1400-61-9

Molecular formula: C ₄₇ H ₇₅ NO ₁₇

Molecular weight: 926.09500

Exact mass: 925.50300

PSA: 327.45000

LogP: 1.47860

Structural formula:

Physical and chemical properties of nystatin

Appearance and properties: yellow suspended matter

Boiling point: 476ºC at 760mmHg

Flash point: 127.3ºC

Refractive index: 1.503

Storage conditions: -20ºC

Vapor pressure: 1.6E-07mmHg at 25 ° C

Nystatin Safety Information

Customs Code: 2942000000

Danger category code: R11

Safety instructions: S22-S24 / 25

Dangerous goods mark: F; C ^[1]

Nystatin uses

It is mainly used internally for the treatment of fungal infections of the digestive tract or externally for surface skin fungal infections. Such as bovine fungal gastritis, chicken and turkey cystic mycosis, etc., for mastitis caused by Aspergillus, Mucor mold, milk duct perfusion is also effective. For chicken pneumonia caused by Aspergillus fumigatus, spray inhalation is also effective. This product is also used for fungal secondary infections caused by long-term use of broad-spectrum antibiotics.

Nystatin toxicology data

Acute toxicity: LD50 of rat mouth: 10gm / kg; LD50 of mouse mouth: 8gm / kg; LD50 of rat belly: 24305ug / kg; LD50 of mouse abdomen: 4400ug / kg; LD50 of mouse subcutaneous: 120mg / kg; mouse intravenous LD50: 3mg / kg;

Nystatin ecological data

For water that is slightly hazardous, do not allow undiluted or large quantities of products to contact groundwater, waterways or sewage systems. Do not discharge materials into the surrounding environment without government permission.

Nystatin molecular structure data

1. Molar refractive index: 240.33

2. Molar volume (m ^{3 /} mol): 696.1

3. Isometric Zhang Rong (90.2K): 2018.5

4. Surface tension (dyne / cm): 70.6

5. Polarizability (10-24cm ³ ): 95.27

Nystatin calculated chemical data

1. Reference value for calculation of hydrophobic parameters (XlogP): -0.2

2. Number of hydrogen-bonded donors: 12

3. Number of hydrogen bond acceptors: 18

4. Number of rotatable chemical bonds: 3

5. Topological molecular polar surface area (TPSA): 320

6. Number of heavy atoms: 65

7. Surface charge: 0

8. Complexity: 1620

9. Number of isotope atoms: 0

10. Determine the number of atomic stereocenters: 10

11. Uncertain number of atomic stereocenters: 9

12. Determine the number of chemical bond stereocenters: 6

13. Uncertain number of chemical bond stereocenters: 0

14. Number of covalent bond units: 1 ^[2]

Introduction to Nystatin

Nystatin and another important antimycotic antibiotic-amphotericin (Lushanmycin)-conclusion

Nystatin Structure is similar.

Nystatin The medicinal products are mainly nystatin A1, and also contain small amounts of A2 and A3. Character: pale yellow or light brown powder; hygroscopic and grainy. It is unstable in nature, very slightly soluble in water, slightly soluble in ethanol and methanol, and relatively soluble in lipid matrix. It deteriorates when exposed to heat, light, air or humidity. Stable in slightly alkaline media, unstable at pH 9-12. Polyaldehyde nystatin sodium salt is soluble in water.

Nystatin pharmacokinetics

This product does not absorb gastrointestinal tract after oral administration, the blood concentration is very low after giving the usual oral dose.

Nystatin Systemic fungal infections have no therapeutic effect. Almost all doses are excreted from the stool. Topical application is not absorbed by the skin and mucous membranes.

Nystatin uses

It is mainly used internally for the treatment of fungal infections of the digestive tract or externally for surface skin fungal infections.

Structural formula Such as bovine fungal gastritis, chicken and turkey cystic mycosis, etc., for mastitis caused by Aspergillus, Mucor mold, milk duct perfusion is effective. For chicken pneumonia caused by Aspergillus fumigatus, spray inhalation is also effective. This product is also used for fungal secondary infections caused by long-term use of broad-spectrum antibiotics.

Nystatin indications

Oral treatment of gastrointestinal candida enteritis; topical treatment of oral candidiasis and skin mucosal candida infection. Vaginal candidiasis.

Nystatin adverse reactions

[Adverse reactions] Nausea, vomiting, diarrhea can occur after oral administration. Quickly disappears after reduction or withdrawal. May cause allergic contact dermatitis after topical application. Individual patients can cause increased vaginal discharge after vaginal application.

Nystatin dosage

Oral, 2 million to 4 million U / day for adults, divided into 4 times; 50,000 to 100,000 U / time for children, 3 to 4 times per day.

[Digestive tract candidiasis] Oral, 500,000 to 1 million units once for adults, 3 times a day; children take 50,000 to 100,000 units / kg daily, divided into 3 to 4 times.

Nystatin considerations

[Precautions] Those with a history of nystatin allergy are prohibited. Pregnancy class B. Suspensions are not stable at room temperature and should be prepared fresh. Except for Candida enteritis, this product is not suitable for the treatment of other deep fungal diseases. This product has no therapeutic effect on systemic fungal infections. Use with caution in pregnant and lactating women. Not recommended for children under 5 years.

[Side effects: Nausea, vomiting, diarrhea, rash, etc. can be caused after oral administration.

[Dose of western medicine: oral, 500,000 U to 1 million U / day for adults, 3 to 4 times a day; external use, suspension 100,000 U / ml, ointment 100,000 U / g.

Clinical application of nystatin

Nystatin is a polyene antifungal drug with broad-spectrum antifungal effect

Nystatin However, it is not absorbed through the skin and mucous membranes, and the blood concentration after oral administration is extremely low, which is clinically limited to local application and the effect is not ideal. According to the literature, its new formulation not only improves the effect of topical application, but also expands its use.

1Nystatin liposome injection was developed by Aronex and is currently at the end of phase III clinical trials.

Treatment of 109 patients with candida infections, including 91 patients with daily dose of 2mg / kg, and 18 patients with 4mg / kg intravenously, the average course of treatment was 10.6 days. 50 of the 56 evaluable patients were effective. In clinically immunocompromised infected people, 60% of Candida infections that are not sensitive to amphotericin B or fluconazole are sensitive to this product. Intravenous administration can cure 80% of patients.

In the treatment of Aspergillus infection, this product is used to treat 24 patients with invasive aspergillosis that cannot tolerate amphotericin B or ineffective treatment. Intravenous infusion of 4mg / kg daily, 19 of the 19 evaluable patients are effective.

Treatment of Cryptococcus infection In the treatment of Cryptococcal meningitis, the daily effect of 4mg / kg of intravenous administration of this product is similar to that of amphotericin B daily 0.7mg / kg.

Empirical treatment of patients with agranulocytosis and fever 27 patients with recurrent fever agranulocytosis treated with this product for 8 days, of which 10 (37%) achieved satisfactory clinical results.

Adverse reactions

Common adverse reactions include hypokalemia (25%) and impaired renal function (may occur when the daily dose is> 6 mg / kg). Rapid intravenous drip may cause chills, fever, dyspnea, occasional skin rash, and liver damage, but it usually does not affect treatment and does not need to be discontinued.

Each tablet contains nystatin 100,000 U, which is used to treat 120 cases of vulvovaginal candidiasis, aged 20 ~ 50 years old, using this product for 1 week continuously, 2 tablets / d, using 2% ~ 4% sodium bicarbonate before washing For the vulva, dakenin suppository was used as a control, and the total effective rate was 93.3%, which was not significantly different from the dakenin group.

Nystatin glycerol coating agent

Patients with neonatal thrush were male neonates. After 15 days of antibiotic treatment for pneumonia, flaky white milk lumps appeared on the oral mucosa and tongue. Oral nystatin tablets and nystatin aqueous suspension were administered for 15 days. Symptoms are mild and severe. The nystatin was used to coat the affected area with 100,000 U / ml glycerin, 3 times per day, and healed after 2 days without recurrence. Jiang reported that this product was used to treat 69 pediatric patients, with a minimum of 42 days and a maximum of 9 months. The total effective rate was 70%, which was significantly better than the control group using Zhuhuangsan.

Treatment of mycotic stomatitis in this group of 67 cases, 42 males and 25 females, the oldest 76 years old, the youngest 4 years old, clinical manifestations of oral mucosa covered with white false film, severe cases of cheeks, hard palate, gums and tongue Can be covered. Treatment method: first wash the mouth with 2% ~ 4% sodium bicarbonate solution, and then apply nystatin glycerol to the affected area, 3 to 4 times / d, light for 4 to 5 days, and severe for 10 days.

Nystatin paste

For the treatment of mycotic vaginitis, grind nystatin tablets into a fine powder, mix thoroughly with a pediatric skin cream to make a paste, first wash the affected area with 5% sodium bicarbonate solution, and wipe the paste with a cotton swab to coat it with a thickness of 1mm , Once a day, 3 to 7 days can be cured.

Nystatin related drugs

Nystatin tablets

English name NYSTATINTABLETS antifungal. This product is a light yellow tablet.

Pharmacology and toxicology

Polyene antifungal drugs with broad-spectrum antifungal effect and high antibacterial activity against Candida genus, new cryptococcus, aspergillus, mucormyces, microsporum, capsular histoplasma, dermatitis and dermatitis Bacteria are usually also sensitive to this product. This product can be combined with sterols on fungal cell membranes, causing changes in cell membrane permeability, leading to the loss of important cell contents and exerting antifungal effects.

Pharmacokinetics

This product does not absorb gastrointestinal tract after oral administration, the blood concentration is very low after giving the usual oral dose, and has no therapeutic effect on systemic fungal infection. Almost all doses are excreted from the stool. Topical application is not absorbed by the skin and mucous membranes.

Indication

Used orally to treat candidiasis of the digestive tract.

Dosage

Gastrointestinal candidiasis: Orally, pediatrics should be taken 3 to 4 times daily at a weight of 50,000 to 100,000 units / kg; adults will be 500,000 to 1 million units once a day, 3 times a day.

Adverse reactions

Gastrointestinal reactions such as diarrhea, nausea, vomiting, and epigastric pain can occur when a large dose is taken orally, and they quickly disappear after reduction or withdrawal.

Contraindications

Patients who are allergic to this product are prohibited.

Precautions

This product has no therapeutic effect on systemic fungal infections.

Medication for pregnant and lactating women

Use with caution in pregnant and lactating women.

Medication for children Not recommended for children under 5 years.

Nystatin Vaginal Effervescent Tablets

Drug alias: Micotin Mycostatin, preparation specifications vaginal effervescent tablet: 100,000 u.

Indication

Vaginitis and vulvar infections caused by Candida albicans and other Candida.

Dosage

For deep vaginal use, rinse the vulva or sitz bath with 2% ~ 3% soda solution before use. After drying, insert the product with fingers wearing plastic finger wraps, 1 tablet (100,000 u) / time, 1 Times ~ 2 times / day. Symptoms can be alleviated within 24 hours to 72 hours after treatment. Two weeks is a course of treatment and can be repeated if necessary. In order to avoid neonatal fungal stomatitis, pregnant women can use 1 to 2 tablets per day before birth for 3 to 6 weeks.

Precautions

Those who are allergic to this product are prohibited. See antifungal medication. 1. Symptoms did not resolve after 1 course of medication

uterus Consult your physician or pharmacist. 2. This product is for vaginal administration only. Avoid contact with eyes. 3 Pregnant women, lactating women and unmarried women should consult a physician before use. 4 Children must be used under adult supervision. 5. Disable when the characteristics of this product change. 6. Keep this medicine out of the reach of children. Function category This product is a non-prescription drug for gynecological drugs.

Pharmacology and toxicology

This product has a broad-spectrum antifungal effect, is most sensitive to Candida, and also inhibits Cryptococcus and Trichomonas.

Indication

For candidal vulvovaginitis.

Usage and dosage

external use. 1 tablet at a time, 1 or 2 times a day, the course of treatment is generally

Ovary Two weeks. The patient washed his hands and vulva, took a supine position, put on the attached finger cuffs, and sent the tablets deep into the vagina.

Adverse reactions

Occasional allergic reactions, burning and itching.

Taboo

Those who are allergic to this product are prohibited. Disabled during the first 3 months of pregnancy.

Precautions

This product is for vaginal administration only. Avoid contact with eyes. Pregnant women and unmarried women should consult a physician before use. Children must be used under adult supervision. Disable when the characteristics of this product change. Keep this medicine out of the reach of children.

medicine interactions

If you are using other medicines, please consult your physician or pharmacist before using this product.