Nizoral - antifungal agent for external and internal use.
Release form and composition
- Tablets: flat, round, with beveled edge, white, on one side of the risk and engraved "K 200", on the other - engraved "JANSSEN" (10 pieces in a blister, in a cardboard bundle 1 or 3 blisters);
- Cream for external use 2%: homogeneous, white (15 g each in aluminum tubes, in a carton pack 1 tube);
- Shampoo 2%: red-orange (25 or 60 ml in plastic bottles with a screw-on lid, in a carton pack 1 bottle).
Active ingredient - ketoconazole, its content:
- 1 tablet - 200 mg;
- 1 g of cream - 20 mg;
- 1 g of shampoo - 20 mg.
- Tablets: purified water, colloidal silicon dioxide, polyvidone K90, lactose monohydrate, corn starch, microcrystalline cellulose, magnesium stearate;
- Cream: cetyl alcohol, stearyl alcohol, propylene glycol, polysorbate 60, polysorbate 80, sorbitan stearate, isopropyl myristate, sodium sulfite anhydrous, purified water;
- Shampoo: disodium lauryl sulfosuccinate, macrogol methylene dextrose dioleate, coconut oil diethanolamide fatty acids, sodium lauryl sulfate, imido, collagen hydrolyzate, hydrochloric acid, sodium chloride, sodium hydroxide, water, red charming dye, E129)).
Indications for use
Infections of the skin, mucous membranes and scalp caused by yeast fungi and / or dermatophytes, if previous local treatment was ineffective or local therapy is not applicable due to the significant depth of the lesion or large size of the affected areas, as well as cases of resistance or intolerance to other antifungal systemic drugs actions:
- Licolor versicolor;
- Candidiasis of the mouth and throats;
- Chronic candidiasis of the skin and candidiasis of the mucous membranes;
- Chronic recurrent vaginal candidiasis;
- Folliculitis caused by fungi of the genus Malassezia.
Systemic fungal infections:
Dermatophyte infections of the skin caused by Epidermophyton floccosum, Trichophyton mentagrophytes, Trichophyton rubrum, Microsporum canis:
- Skin candidiasis;
- Seborrheic dermatitis caused by Pityrosporum ovale;
- Groin athlete's disease;
- Tinea versicolor;
- Epidermofitiya hands and feet;
- Ringworm smooth skin.
Prevention and treatment of infections caused by the yeast Malassezia spp. (Pityrosporum spp.):
- Seborrheic dermatitis;
- Local scaly versicolor.
In all dosage forms Nizoral is contraindicated in case of hypersensitivity to the components.
In the form of tablets, the drug should also not be prescribed in the following cases:
- Lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
- Liver diseases (both acute and chronic);
- Children's age up to 3 years;
- The simultaneous use of ergot alkaloids (for example, ergotamine, dihydroergotamine, ergometrine, methylergometrine);
- The simultaneous use of eplerenone, everolimus, irinotecan, nisoldipine;
- Simultaneous use of HMG-CoA reductase inhibitors metabolized through CYP3A4 isoenzymes (simvastatin, lovastatin);
- Simultaneous use of oral forms of triazolam, midazolam;
- Simultaneous use of cytochrome P450 (CYP3A4) 3A4 isoenzyme substrates, such as mizolastin, disopyramide, dofetilide, cisapride, halofantrine, bepridil, astemizole, pimozide, quinidine, terfenadine, sertindol, domperidone, sertindol, quinidine, terfenadine, sertindol, quinidine, sertindol, quinidine, sertindol, quinidine, sertindol, quinidine, sertindol, quinidine, sertindol, quinidine, sertindole, quinidine, sertindole, quinidine, sertindole, quinidine, sertindole, quinidine, sertindole, quinidine, sertindole, quinidine, sertindole, quinidine, sertindole, quinidine, sertindole, quinidine, sertindol, quenidine, sertindol, quenidine
- Hypersensitivity to the drug.
Due to the risk of complications, Nizoral tablets should be used with caution in the following cases:
- Low acidity of the stomach;
- Adrenal insufficiency or borderline states, as well as in patients exposed to significant stress, including during extensive surgical interventions (adrenal gland function should be monitored, since a reduction in the “cortisol response” is possible);
- Alcohol abuse (there is a risk of disulfiram-like reaction);
- The simultaneous use of potentially hepatotoxic drugs;
- The simultaneous use of antacid drugs (between doses should observe at least 2-hour intervals);
- Patients with achlorhydria or receiving drugs that suppress the secretion of hydrochloric acid in the stomach, for example, proton pump inhibitors or H 2 -histamine receptor blockers (in these cases it is recommended to take Nizoral tablets with cola drinks);
- Pregnancy and breastfeeding (the drug can be prescribed only if the expected benefit outweighs the potential risks).
Dosing and Administration
In the form of tablets Nizoral should be taken orally, preferably with meals (to improve absorption).
Adults and children weighing more than 30 kg are prescribed 1 tablet 1 time per day. If no improvement is noted, the dose is increased to 400 mg 1 time per day. For vaginal candidiasis, the recommended dose is 2 tablets 1 time per day.
For children over 3 years old weighing 15-30 kg, the drug is prescribed ½ tablet 1 time per day.
The average duration of treatment depending on the indications:
- Vaginal candidiasis - 7 days;
- Licolor versicolor - 10 days;
- Candidiasis of the skin and oral cavity - 2-3 weeks;
- Skin mycoses caused by dermatophytes - about 4 weeks;
- Fungal lesions of the scalp - 4-8 weeks;
- Histoplasmosis, paracoccidioidomycosis, coccidioidomycosis - about 6 months.
Regardless of the indications, treatment should be continuous, not only clinical parameters, but also laboratory indicators will not indicate the destruction of the pathogen, since an insufficient duration of therapy can lead to a recurrence of an infectious disease. However, it should be borne in mind that it is necessary to cancel the drug and to evaluate the liver function in the laboratory in case of such signs of hepatitis as fatigue, abdominal pain, nausea, dark urine color, vomiting, anorexia, jaundice.
In the form of a cream, the drug should be applied to the affected skin and adjacent areas 1-2 times a day.
The usual duration of treatment:
- Pityriasis versicolor, yeast infections - 2-3 weeks;
- Groin athlete - 2-4 weeks;
- Seborrheic dermatitis - 2-4 weeks;
- Dermatomycosis of smooth skin - 3-4 weeks;
- Epidermofitiya stop - 4-6 weeks.
For maintenance therapy with seborrheic dermatitis cream should be applied 1-2 times a week.
Regardless of the patient's age, shampoo should be applied to the affected areas of the body for 3-5 minutes, then rinsed with water:
- Pityriasis versicolor: treatment - 1 time per day for 5 days, prophylaxis - 1 time per day with a course of 3 days before the onset of summer;
- Seborrheic dermatitis and dandruff: treatment - 2 times a week, a course of 2-4 weeks, prevention - 1 time in 1-2 weeks.
When using tablets Nizoral the following possible side effects:
- Nervous system: headache; hyperexcitability, fatigue, general weakness, anxiety, paresthesia, dizziness, drowsiness, insomnia, reversible increase in intracranial pressure * (for example, swelling of a fontanelle in young children, edema of the optic nerve discs);
- Gastrointestinal: diarrhea, abdominal pain, nausea, vomiting, abnormal liver function, dyspepsia, discoloration of the tongue, dysgeusia, dry mouth, abdominal distension, constipation, jaundice, toxic hepatitis (hypercreatininemia, increased activity of alkaline phosphatases or hepatic transaminases ), severe hepatotoxicity * (including liver failure (including cases of transplantation and death), hepatonecrosis (biopsy), cholestatic hepatitis, liver cirrhosis);
- Endocrine system: gynecomastia, adrenal insufficiency *;
- Sense organs: photophobia;
- Immune system: pseudo-anaphylactic shock, allergic conditions * (including urticaria, anaphylactic reactions, angioedema, anaphylactic shock);
- Metabolism and nutrition: hyperlipidemia, anorexia, increased appetite, alcohol intolerance;
- Musculoskeletal system: myalgia, arthralgia *;
- Reproductive system: menstrual disorders;
- Respiratory system: nosebleeds;
- Cardiovascular system: orthostatic lowering of arterial pressure;
- Urogenital system: azoospermia *, erectile dysfunction *;
- Skin and subcutaneous fat: itching, allergic rash, erythema multiforme, xeroderma, dermatitis, flushing, alopecia, photosensitivity *;
- Laboratory indicators: a decrease in the number of platelets, thrombocytopenia *;
- Other: peripheral edema, fever, chills, temporary decrease in plasma testosterone concentration *.
* - side effects that were observed very rarely in the post-registration period.
When applying Nizoral in the form of a cream, a burning sensation and irritation are possible. In rare cases, the following side effects occur:
- Local skin allergic reactions, incl. contact dermatitis;
- Immune system: urticaria, hypersensitivity;
- Skin and subcutaneous tissue: rash, erythema, pruritus.
When applying shampoo Nizoral possible:
- Immune system: hypersensitivity reactions;
- Body of vision: increased tearing, eye irritation;
- Systemic disorders and local reactions: pustules, pruritus, skin reactions, irritation and erythema at the site of application, hypersensitivity;
- Infections: folliculitis;
- Nervous system: a violation of taste sensitivity;
- Skin and subcutaneous tissue: dry skin, contact dermatitis, impaired hair texture, peeling of the skin, burning sensation, alopecia, acne, skin rash, hair color change *, urticaria *, edema *.
* - side effects that were observed very rarely in the post-registration period.
In the form of tablets, Nizoral should be prescribed only in cases where the expected benefit of therapy outweighs the potential risks, taking into account the presence of other effective antifungal drugs.
Before starting to use the drug, it is necessary to evaluate liver function in order to rule out acute or chronic diseases. In order not to miss the first signs of hepatotoxicity, during treatment should regularly monitor the function of the kidneys and liver, the picture of peripheral blood.
The use of Nizoral in fungal meningitis is impractical because ketoconazole does not penetrate the blood-brain barrier poorly.
If skin diseases were treated with glucocorticosteroids, ketoconazole tablets can be used no earlier than 2 weeks after their cancellation.
Acidic drinks increase the absorbability of ketoconazole.
Nizoral cream is intended solely for external use. Use in ophthalmic practice is prohibited. In the case of previous treatment with local corticosteroids, in order to prevent withdrawal after long-term treatment, it is recommended to continue their use in the morning, and use Nizoral cream in the evening, then gradually remove the steroids within 2-3 weeks.
When using the drug in the form of a shampoo, care should be taken to prevent it from getting into the eyes. If this happens, rinse thoroughly with clean water.
In the case of previous treatment with topical corticosteroids, in order to prevent withdrawal after long-term treatment, it is recommended to continue their use in combination with Nizoral shampoo, then gradually eliminate steroids within 2-3 weeks.
Nizoral does not have a negative effect on the reaction rate and ability to concentrate attention, regardless of the dosage form.
Clinically significant interaction with the simultaneous use of Nizoral in the form of a cream or shampoo with other drugs has not been established.
Drugs that reduce the acidity of gastric juice, reduce the absorption of ketoconazole, taken orally.
The use of ketoconazole is not recommended with microsomal oxidation inducer drugs (such as carbamazepine, rifabutin, isoniazid, phenytoin, nevirapine, rifampicin), since they significantly reduce its bioavailability.
Ritonavir increases the bioavailability of ketoconazal, therefore, the dose of the latter should be reduced.
Ketoconazole may inhibit the metabolism of drugs cleaved by cytochrome P450 CYP3A isoenzymes, as a result of which it is possible to enhance and / or prolong their effects, including side effects.
With the simultaneous appointment of the following drugs, it is necessary to monitor their concentration in the blood plasma, the severity of therapeutic action and side effects (if necessary, the dosage of ketoconazole should be reduced):
- Some immunosuppressive agents: tacrolimus, cyclosporine, sirolimus;
- Blockers of the slow calcium channels of the dihydropyridine series, cleaved by the CYP3A4 isoenzyme, and presumably verapamil;
- Some inhibitors of HMG-CoA reductase, for example, atorvastatin;
- Some anticancer drugs, such as imatinib, docetaxel, busulfan, erlotinib, Vinca roseal alkaloids;
- Some glucocorticosteroids, such as dexamethasone, fluticasone, methylprednisolone, budesonide;
- HIV protease inhibitors such as saquinavir and indinavir;
- Indirect anticoagulants;
- Other medications: buspirone, brotizolam, carbamazepine, alprazolam, cilostazol, alfentanil, ebastine, fentanyl, reboxetine, eletriptan, rifabutin, digoxin, repaglinide, tolterodine, solifenation, sildenafil, quetiapine, quetiapin, cephalophenol, cedeniophen, cedeniophen, cedenophenol, cedeniophene, tsvterodin, solfenil
Ketoconazole increases the concentration of sulfonylureas and increases the risk of hypoglycemia.
In the case of simultaneous use of alcohol, a disulfiram-like reaction may develop, manifested by peripheral edema, headache, rash, nausea, redness.
Terms and conditions of storage
Keep out of reach of children:
- Tablets - 3 years at temperatures up to 30 ºС;
- Cream - 5 years at a temperature of 15-30 ºС;
- Shampoo - 3 years at temperatures up to 25 ºС.