Nizoral - Instructions For Use, Price, Shampoo, Cream, Tablets

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Nizoral

Nizoral: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Drug interactions
11. 11. Analogs
12. 12. Terms and conditions of storage
13. 13. Terms of dispensing from pharmacies
14. 14. Reviews
15. 15. Price in pharmacies

Latin name: Nizoral

ATX code: D01AC08

Active ingredient: ketoconazole (ketoconazole)

Manufacturer: Janssen Pharmaceutica (Belgium), Janssen-Cilag, S. p. A. (Italy)

Description and photo update: 2019-19-08

Prices in pharmacies: from 400 rubles.

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Nizoral is an antifungal drug.

Release form and composition

Dosage forms of Nizoral:

• Tablets: white, round, flat, with a beveled edge, engraved with "JANSSEN" on one side, "K 200" on the other, and a dividing line (10 pcs. In blisters, in a cardboard box 1 or 3 blisters);
• Cream for external use 2%: uniform structure of white color (15 g each in aluminum tubes, in a cardboard box 1 tube);
• Shampoo 2%: red-orange liquid (25 ml or 60 ml each in high-density polyethylene bottles with a screw cap, 1 bottle in a cardboard box).

The active ingredient of Nizoral is ketoconazole:

• 1 tablet - 200 mg;
• 1 g cream - 20 mg;
• 1 g of shampoo - 20 mg.

Auxiliary components:

• Tablets: lactose monohydrate, corn starch, magnesium stearate, polyvidone K90, colloidal silicon dioxide, microcrystalline cellulose, purified water (removed during production);
• Cream: stearyl alcohol, propylene glycol, cetyl alcohol, polysorbate 60, sorbitan stearate, isopropyl myristate, polysorbate 80, sodium sulfite anhydrous, purified water;
• Shampoo: disodium lauryl sulfosuccinate, sodium lauryl sulfate, collagen hydrolyzate, hydrochloric acid, macrogol methyldextrose dioleate, diethanolamide of coconut oil fatty acids, sodium chloride, sodium hydroxide, imidourea, charming red dye (E129), fragrance, water.

Pharmacological properties

Pharmacodynamics

Ketoconazole is a synthetic imidazole dioxolan derivative characterized by mycostatic or fungicidal action against higher fungi (eumycetam), dermatophytes (Microsporum spp., Epidermophyton floccosum, Trichophyton spp.), Dimorphic fungi and yeast (Cryptococcus). Sporothrix schenckii, Aspergillus spp., Some varieties of Dematiaceae, Mucor spp. Are less sensitive to the action of ketoconazole. and other phycomycetes, excluding Entomophthorales.

Ketoconazole slows down the biosynthesis of ergosterol in fungi and promotes changes in the composition of other lipid components in membranes. The results of clinical studies and the study of interactions with other drugs confirm that when taking Nizoral in the form of tablets at a dosage of 200 mg 2 times a day for 3-7 days, a slight lengthening of the QT interval was sometimes observed. The average maximum increase in the QT interval to 6-12 msec was recorded 1-4 hours after taking the drug, when the level of ketoconazole in the blood plasma reached its peak values. However, such an increase in the QT interval has no particular clinical significance.

When Nizoral is prescribed in a therapeutic dose of 200 mg 1 time per day, a transient decrease in the concentration of testosterone in plasma may be observed. This indicator returns to its original value within 24 hours after the intake of ketoconazole. During a long course of therapy using this dosage, the testosterone content usually differs slightly from the control value.

When healthy volunteers took ketoconazole at a daily dose of 400 mg or more, a decrease in the "cortisol response" to ACTH stimulation was noted.

Nizoral shampoo helps to quickly eliminate itching and flaking, which are often symptoms of pityriasis versicolor, dandruff, and seborrheic dermatitis.

The drug in the form of a cream quickly acts on itching associated with yeast and dermatophyte infections, and a decrease in the severity of symptoms is noted even before the first signs of recovery appear.

Pharmacokinetics

Ketoconazole is a weak dibasic compound that absorbs and dissolves in an acidic environment. On average, its maximum plasma concentration is approximately 3.5 μg / ml and is determined 1-2 hours after a single oral intake with meals 200 mg Nizoral in the form of tablets. The maximum bioavailability of ketoconazole is achieved when it is combined with food intake.

Absorption ketoconazole decreases in patients with reduced acidity of gastric juice, which, for example, take antisecretory agents (proton pump inhibitors, antagonists, H ₂ receptor) or antacids (aluminum hydroxide), and in patients with achlorhydria specific disease provoked. In such patients, the absorption of the active substance Nizoral when taking tablets before meals increases when the drug is combined with drinks that contain acid (for example, non-diet cola).

With the preliminary administration of the proton pump inhibitor omeprazole, the bioavailability of ketoconazole, taken once in a dose of 200 mg, decreased to 17% compared to its bioavailability when taken on an empty stomach. When Nizoral is combined with acidic drinks and the preliminary administration of omeprazole, the bioavailability of ketoconazole is 65% of its bioavailability when taken before meals without the introduction of concomitant drugs into the body.

The degree of binding of ketoconazole to plasma proteins in vitro (mainly to the albumin fraction) is 99%. The substance is widely distributed throughout the tissues, but only a small amount penetrates into the cerebrospinal fluid.

After absorption from the gastrointestinal tract, ketoconazole is involved in metabolic processes in the liver, forming inactive metabolites in large quantities. In vitro studies confirm that the CYP3A4 isoenzyme is involved in the metabolism of the drug. The main metabolic processes characteristic of ketoconazole are aromatic hydroxylation, oxidative O-dealkylation, and oxidation and cleavage of the piperazine and imidazole rings. Ketoconazole is not an inducer of its own metabolism.

Ketoconazole is excreted from plasma in two phases: during the first 10 hours, the half-life is 2 hours, and then - 8 hours. Approximately 13% of the dose is excreted through the kidneys, with about 2–4% unchanged. Ketoconazole is excreted mainly in the bile in the gastrointestinal tract, after which approximately 57% of the dose is excreted through the intestines.

In patients with hepatic or renal insufficiency, the pharmacokinetic parameters of ketoconazole generally differ slightly from those in healthy individuals. There are limited clinical data on the pharmacokinetic characteristics of ketoconazole in tablet form in children.

After local application of Nizoral in the form of a shampoo to the scalp, the concentration of the active substance is not determined in the blood plasma, however, it is determined after local application of the drug to the whole body and is 11.2‒33.3 ng / ml. The risk that such concentrations can provoke any drug interactions is minimal, but there may be an increase in allergic reactions.

After topical application of Nizoral in the form of a cream to the skin, the concentration of ketoconazole was not determined in the blood plasma of adult patients.

In a study involving 19 children suffering from seborrheic dermatitis, approximately 40 g of the cream was applied daily to the surface of the skin covering more than 40% of body weight. At the same time, plasma concentrations of ketoconazole were found in 5 children and ranged from 32 to 133 ng / ml. With repeated use in children of Nizoral in the form of a cream in large quantities (more than 3 g), there is a certain risk of drug interactions (for example, inhibition of the metabolism of drugs, in the metabolic processes of which enzymes of the CYP3A4 system are involved, in particular cisapride). Allergic reactions may also increase.

Indications for use

Pills

The use of Nizoral in the form of tablets is indicated for the treatment of infectious diseases of the skin, mucous membranes, scalp caused by yeasts and / or dermatophytes.

Nizoral tablets are prescribed in the absence of a clinical effect from previously conducted local therapy, the impossibility of using the cream due to the large size of the lesion area or its significant depth in patients with intolerance or resistance to therapy with other antifungal agents for systemic use, for the following diseases / conditions:

• Dermatophytosis;
• Versicolor versicolor;
• Folliculitis caused by fungi of the genus Malassezia;
• Candidiasis of the skin, mouth and pharynx;
• Chronic candidiasis of the mucous membranes;
• Recurrent form of chronic vaginal candidiasis.

In addition, Nizoral tablets are prescribed for the treatment of systemic fungal infections: coccidioidosis, paracoccidioidosis, blastomycosis, histoplasmosis.

With fungal meningitis, the use is impractical due to poor penetration through the blood-brain barrier.

Cream for external use 2%

The use of Nizoral cream is indicated for the treatment of fungal skin infections caused by Trichophyton mentagrophytes, Trichophyton rubrum, Epidermophyton floccosum and Microsporum canis:

• Pityriasis versicolor;
• Dermatomycosis of smooth skin;
• Epidermophytosis of the feet and hands;
• Inguinal epidermophytosis;
• Skin candidiasis;
• Seborrheic dermatitis with Pityrosporum ovale.

Shampoo 2%

The use of Nizoral shampoo is indicated for the prevention and treatment of local pityriasis versicolor, seborrheic dermatitis and dandruff.

Contraindications

According to the instructions, Nizoral in all forms of release is contraindicated for use in case of hypersensitivity to its components.

Contraindications to the use of tablets:

• Acute or chronic liver disease
• Simultaneous use of cytochrome P450 with substrates of the CYP3A4 isoenzyme: disopyramide, bepridil, astemizole, cisapride, halofantrine, dofetilide, mizolastine, levacetylmethadol (levomethadil), pimozide, quinidine, sertinidolomine, and terfenadine, which can lead to an increase in domoperine arrhythmias of the "pirouette" type;
• Concomitant therapy with HMG-CoA reductase inhibitors metabolized through CYP3A4 isoenzymes, including lovastatin, simvastatin;
• Combination with oral midazolam and triazolam;
• Use in combination with eplerenone, everolimus, nisoldipine, irinotecan;
• Simultaneous use with methylergometrine, ergometrine, dihydroergotamine, ergotamine and other ergot alkaloids;
• Glucose-galactose malabsorption syndrome, lactose intolerance, lactase deficiency;
• Age up to 3 years;
• Breastfeeding period.

Nizoral tablets are prescribed with caution with low stomach acidity (absorption of the drug worsens); concomitant use of antacids (including aluminum hydroxide), they should be taken only 2 hours after Nizoral; for patients with achlorhydria or taking drugs that suppress the secretion of hydrochloric acid in the stomach (proton pump inhibitors, blockers of H2-histamine receptors), it is advisable to take the drug with drinks containing cola; with adrenal insufficiency and with borderline conditions, including after extensive surgical intervention; with alcohol abuse; liver failure (risk of hepatotoxicity); concomitant use of potentially hepatotoxic drugs.

During pregnancy, tablets and shampoo can be prescribed in exceptional cases if the intended benefits of therapy to the mother outweigh the potential risk to the fetus.

During the period of breastfeeding, Nizoral shampoo should be used with caution, after consulting a doctor.

Instructions for use Nizoral: method and dosage

Pills

Nizoral tablets are taken orally with meals.

Recommended dosage for systemic infections and for the treatment of lesions of the mucous membranes, skin, scalp caused by yeast and / or dermatophytes:

• Patients weighing more than 30 kg: 1 tablet once a day, in the absence of a clinical effect, it is recommended to increase a single dose to 2 tablets; with vaginal candidiasis - 2 tablets 1 time per day;
• Children older than 3 years old with a body weight of 15-30 kg: ¹ / ₂ tablet 1 time per day.

Average duration of therapy depending on the disease:

• Skin mycoses caused by dermatophytes - about 4 weeks;
• Vaginal candidiasis - 1 week;
• Oral cavity and skin candidiasis - 2-3 weeks;
• Versicolor versicolor - 1.5 weeks;
• Fungal lesions of the scalp - 1-2 months;
• Histoplasmosis, paracoccidioidomycosis, coccidioidomycosis - 6 months.

Continuous use of Nizoral should be carried out until the eradication of the pathogen, confirmed by laboratory tests.

If symptoms of hepatitis appear (fatigue, nausea, vomiting, anorexia, jaundice, abdominal pain, dark urine), it is necessary to discontinue the drug and assess liver function.

Cream for external use 2%

Nizoral cream should be applied to the skin affected by the fungus, capturing the adjacent healthy areas, once a day.

Average course duration, depending on the disease:

• Dermatomycosis of smooth skin - 3-4 weeks;
• Pityriasis versicolor - 2-3 weeks;
• Epidermophytosis inguinal - 2-4 weeks;
• Yeast infections - 2-3 weeks;
• Epidermophytosis of the feet - 4-6 weeks.

With seborrheic dermatitis, the cream is recommended to be applied, depending on the severity of the lesion, 1 or 2 times a day until all symptoms of the disease completely disappear (usually 2-4 weeks).

To prevent relapse, contaminated surfaces should be lubricated 1-2 times a week as maintenance therapy. If, after using Nizoral for 4 weeks, the clinical effect does not occur, you should consult a doctor to clarify the diagnosis.

Shampoo 2%

Shampoo is applied externally, applying to problem areas of the scalp and skin for 3-5 minutes and rinsing thoroughly with water.

Dosing regimen of Nizoral when used for medicinal purposes:

• Pityriasis versicolor: 1 time per day for 5 days;
• Dandruff and seborrheic dermatitis: 2 times a week, the course of therapy is 2-4 weeks.

Dosing regimen of Nizoral when used for prophylactic purposes:

• Pityriasis versicolor: it is recommended to carry out a one-time course before the summer season - once a day for 3 days;
• Seborrheic dermatitis and dandruff: once every 1-2 weeks.

The mode of application of the shampoo has no age restrictions.

Side effects

Open clinical studies of the use of Nizoral tablets in patients with superficial and deep mycoses noted the following side effects (often - more than 1%, infrequently - with a frequency of less than 1%):

• Gastrointestinal tract: often - abdominal pain, nausea, diarrhea, liver functional disorder; infrequently - dry mouth, vomiting, constipation, dyspepsia, bloating, dysgeusia, toxic hepatitis (hypercreatininemia, increased activity of liver enzymes, alkaline phosphatases), discoloration of the tongue, jaundice;
• Nervous system: often - headache; infrequently - general weakness, dizziness, drowsiness, paresthesia, insomnia, anxiety, increased excitability, fatigue;
• Cardiovascular system: infrequently - orthostatic decrease in blood pressure;
• Endocrine system: infrequently - gynecomastia;
• Nutrition and metabolism: infrequently - increased appetite, alcohol intolerance, hyperlipidemia, anorexia;
• Sense organs: infrequently - photophobia;
• Immune system: infrequently - pseudo-anaphylactic shock;
• Respiratory system: infrequently - epistaxis;
• Musculoskeletal system: infrequently - myalgia;
• Reproductive system: infrequently - menstrual irregularities;
• Dermatological reactions: infrequently - itching, rash, dermatitis, allergic rash, alopecia, erythema multiforme, xeroderma, hot flushes, erythema;
• Laboratory indicators: infrequently - a decrease in the level of platelets;
• General indicators: infrequently - fever, chills, peripheral edema.

In addition, the use of Nizoral tablets in the post-registration period caused the following undesirable actions:

• Immune system: very rarely - urticaria, angioedema, anaphylactic shock, anaphylactic reactions and other allergic conditions;
• Nervous system: very rarely - a reversible increase in intracranial pressure in the form of edema of the optic discs, in children - swelling of the fontanelle and other signs;
• Endocrine system: very rarely - adrenal insufficiency;
• Musculoskeletal system: very rarely - arthralgia;
• Gastrointestinal tract: very rarely - a severe form of hepatotoxicity (liver failure, cholestatic hepatitis, liver cirrhosis, hepatonecrosis (biopsy), including cases of death and transplantation);
• Genitourinary system: very rarely - erectile dysfunction, azoospermia against the background of exceeding the recommended doses;
• Dermatological reactions: very rarely - photosensitivity;
• Laboratory indicators: very rarely - thrombocytopenia;
• Others: possibly - a decrease in the level of testosterone in the blood plasma (restored 24 hours after ingestion).

When applied, Nizoral cream can cause a burning sensation and skin irritation, rarely - local allergic reactions (in the form of contact dermatitis).

Side effects identified during post-marketing research include:

• Immune system: very rarely - urticaria, hypersensitivity;
• Skin and subcutaneous tissues: very rarely - itching, rash, erythema.

Shampooing can cause infrequent adverse reactions:

• Systemic and local disorders: pruritus, erythema, irritation at the site of application, pustules, hypersensitivity, skin reactions;
• Organ of vision: increased lacrimation, eye irritation;
• Immune system: hypersensitivity reactions;
• Nervous system: violation of taste sensations;
• Invasions and infections: folliculitis;
• Dermatological reactions: dry skin, skin rash, burning sensation, peeling of the skin, acne, contact dermatitis, alopecia, violation of hair texture; very rarely - urticaria, edema, change in hair color.

Overdose

When taking Nizoral in the form of tablets, the most common symptoms of an overdose include nausea (27.2%), increased fatigue, including lethargy and drowsiness (14.2%), vomiting (12.6%), abdominal pain (12%)), anorexia (including weight loss) and loss of appetite (7.4%), hyperemia, including excessive sweating (6.3%), edema (5.7%), gynecomastia (4.8%), skin rashes, including dermatitis, purpura, eczema (3.3%), diarrhea (2.2%), headache (2%), dysgeusia (1.3%), alopecia (1.1%).

A specific antidote to ketoconazole has not been found. In case of an overdose within the first hour after taking Nizoral, activated charcoal should be taken orally. Careful monitoring of the patient's condition is also recommended. If necessary, symptomatic therapy is prescribed and gastric lavage is performed.

When Nizoral is used in the form of a shampoo, there are practically no reports of overdose cases, since it is intended exclusively for external use. In case of accidental ingestion, there is no need for special events. To avoid aspiration, vomiting and gastric lavage are contraindicated.

Applying Nizoral in the form of a cream in large quantities can lead to a burning sensation, swelling and erythema, which are temporary and disappear after the completion of the course of treatment. In case of accidental oral administration, symptomatic and supportive therapy is prescribed.

special instructions

Taking into account the risk of hepatotoxicity, Nizoral tablets should be used only if the benefits of therapy exceed the potential threat, given the availability of other types of effective antifungal agents.

Treatment with tablets should be started after a preliminary assessment of liver function, excluding acute or chronic pathologies. Oral use of Nizoral should be accompanied by regular monitoring of the peripheral blood picture, the functional state of the kidneys and liver, since it is important not to miss the first signs of hepatotoxicity that may occur in patients without obvious risk factors. The resulting total dose of ketoconazole poses a threat to the development of severe hepatotoxicity. The patient should be informed that in case of nausea, vomiting, anorexia, weakness, darkening of urine, abdominal pain and jaundice, it is necessary to stop using the tablets and immediately consult a doctor.

Patients with increased activity of hepatic enzymes or postponed toxic liver damage while taking other drugs Nizoral can be prescribed only in the most acute cases, ensuring control of the level of liver enzymes.

With a daily dose of 2 tablets or more, a decrease in the cortisol response to stimulation of adrenocorticotropic hormone is possible, therefore, adrenal function should be monitored in adrenal insufficiency or borderline conditions in patients experiencing significant stress effects (intensive care conditions, extensive surgical interventions, etc.), as well as in patients with a long course of treatment with suspected adrenocortical insufficiency.

With a decrease in the acidity of gastric juice, the absorption of ketoconazole worsens.

Nizoral can be prescribed no earlier than 2 weeks after the cancellation of previous glucocorticosteroid therapy.

Acidic drinks increase the absorption of ketoconazole.

The use of Nizoral does not affect the patient's ability to drive vehicles and mechanisms.

The cream should be applied only externally; use in ophthalmology is contraindicated.

In order to prevent the development of a withdrawal syndrome after long-term therapy with local corticosteroids, it is recommended to stop using them gradually, continuing use for 2-3 weeks. When combined with a cream, topical corticosteroids should be used only in the morning during the withdrawal period and the cream in the evening.

Application during pregnancy and lactation

At the moment, there is limited information about the use of Nizoral in the form of tablets during pregnancy. Animal studies support the reproductive toxicity of ketoconazole. The degree of possible risk to humans is unknown. In this regard, the tablets should not be used in pregnant women, except in cases where the potential benefits of treatment for the mother significantly outweigh the possible risks to the fetus.

Ketoconazole is determined in breast milk, therefore its appointment during lactation is contraindicated.

Studies of the use of Nizoral in the form of shampoo and cream in pregnant and lactating women have not been conducted, therefore, there is no reliable information on the safety of using these forms of the drug during pregnancy and lactation.

Drug interactions

When prescribing Nizoral in the form of tablets, the doctor must determine the possibility of combining the drug with other drugs.

Clinically significant interaction with the simultaneous use of cream and shampoo with other drugs has not been established.

Analogs

Analogs of Nizoral are: Ketoconazole, Ketoconazole DS, Mycozoral, Sebozol, Mikoket, Mikanisal, Dermazole, Ketodin, Ketozoral, Zalain, Onbet, Kandibene, Kanesten, Fungisan, Funginok, Perhotal, Kenazbers, Orazolt.

Terms and conditions of storage

Keep out of reach of children at temperature:

• Tablets: up to 30 ° C, dry;
• Cream: 15-30 ° C;
• Shampoo: up to 25 ° C.

Shelf life: tablets, shampoo - 3 years, cream - 5 years.

Terms of dispensing from pharmacies

The tablets are prescription, cream and shampoo are available without a prescription.

Reviews about Nizoral

According to reviews, Nizoral in the form of tablets is rarely used due to the hepatotoxicity of this dosage form, therefore, reports of taking the drug are rare, which does not allow us to fully assess its effectiveness. Doctors prescribe pills only in individual cases due to the need for constant monitoring of liver function throughout the course of therapy and the availability of safer analogues.

Nizoral in the form of a shampoo is actively used by patients with pityriasis versicolor and other pathological conditions, but it is mainly prescribed for the treatment of dandruff. Reviews of Nizoral are different, however, patients rarely report the ineffectiveness of the drug or the development of adverse reactions. In this case, often after the end of the course of treatment, dandruff may reappear.

Many patients claim that Nizoral in the form of a cream helps well with fungal skin diseases, but with fungal nail infections, the result is worse. Cases of ineffectiveness of this dosage form or the development of serious side effects are quite rare.

Price for Nizoral in pharmacies

The price of Nizoral in the form of a cream for external use is 412-534 rubles. You can buy shampoo 2% for 561-765 rubles (for a 60 ml bottle) or for 790-988 rubles (for a 120 ml bottle). At the moment, the tablet form is not available for sale.

Nizoral: prices in online pharmacies

Drug name Price Pharmacy

Nizoral 2% cream for external use 15 g 1 pc. RUB 400 Buy

Nizoral cream for external use 2%, tube 15 g 474 r Buy

Nizoral shampoo 2% shampoo 60 ml 1 pc. 543 r Buy

Reviews Nizoral (shampoo) 543 r Buy

Nizoral shampoo 20mg / g 60 ml 558 r Buy

Nizoral shampoo 2% shampoo 120 ml 1 pc. 696 r Buy

Reviews Nizoral (shampoo) 696 r Buy

Nizoral shampoo 20mg / g 120 ml 715 RUB Buy

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Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!