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

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

Ketoconazole

Ketoconazole: 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. Use in childhood
11. 11. For violations of liver function
12. 12. Drug interactions
13. 13. Analogs
14. 14. Terms and conditions of storage
15. 15. Terms of dispensing from pharmacies
16. 16. Reviews
17. 17. Price in pharmacies

Latin name: Ketoconazole

ATX code: J02AB02 (tablets and capsules), D01AC08 (cream), G01AF11 (suppositories)

Active ingredient: ketoconazole (Ketoconazole)

Manufacturer: VERTEX, JSC (Russia); Pharmaprim (Republic of Moldova); Lekhim-Kharkov CJSC (Ukraine)

Description and photo updated: 2018-26-11

Prices in pharmacies: from 172 rubles.

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Ketoconazole is an antifungal drug.

Release form and composition

Dosage forms:

• tablets: almost white or white with a bevel (10 pcs. in a blister, in a cardboard box 1 or 3 blisters);
• capsules (10 pcs. in a blister, in a cardboard box 2 blisters);
• vaginal suppositories: white or white with a yellow tinge, cylindrical shape with a pointed end, the presence of a funnel-shaped depression or an air rod on the cut is possible (5 pcs. in a blister, in a cardboard box 1 or 2 blisters);
• cream for external use 2%: a homogeneous mass of white or white with a yellow tint (10 g or 15 g each in aluminum tubes, in a cardboard box 1 tube);
• shampoo (150 ml in a bottle, 1 bottle in a cardboard box).

1 tablet contains:

• active substance: ketoconazole - 0.2 g;
• auxiliary components: lactose, corn starch, low molecular weight polyvinylpyrrolidone, colloidal silicon dioxide, magnesium stearate.

In 1 capsule, the content of the active substance - ketoconazole, is 0.2 g.

1 suppository contains:

• active substance: ketoconazole - 0.4 g;
• auxiliary components: butylhydroxyanisole, semi-synthetic glycerides (Suppocir-AM).

1 g of cream contains:

• active substance: ketoconazole - 0.02 g;
• auxiliary components: vaseline oil, emulsifier 61 WL 2659, nipagin, labrafil M 2130 CS, purified water.

The shampoo contains:

• active substance: ketoconazole - 2%;
• auxiliary components: sodium laureth sulfate, cocmidapropyl betaine, sodium laurylethoxysulfosuccinate, cocoglucoside glyceryl oleate, polyquaternium-7, cocamide MEA, PEG (polyethylene glycol) -7 glyceryl cocoate, triethanolamine, laureth-3, sodium chloride, methylenediamine diamine acid, citric acid perfume composition.

Pharmacological properties

Pharmacodynamics

Ketoconazole is a synthetic imidazole derivative, an antifungal agent with a wide spectrum of fungicidal and fungistatic activity. The mechanism of the mycostatic action of the active substance is due to its ability to inhibit the synthesis of ergosterol, phospholipids and triglycerides. This causes a change in the lipid composition of the fungal membrane and a violation of the permeability of the cell wall.

The following microorganisms are sensitive to ketoconazole: dermatophytes [Trichophyton speciales (spp.), Microsporum spp., Epidermophyton floccosum], yeast and yeast-like fungi (Pityrosporum spp., Candida spp., Torulopsis, Cryptococcus spp.), Gram-positive., Streptococcus spp.), Dimorphic fungi and eumycetes.

Pharmacokinetics

After oral administration, ketoconazole is well absorbed. The period to reach the maximum plasma concentration is 1–2 hours.

Plasma protein binding - 99%.

The first phase T _1/2 (half-life) is 2 hours, the second phase is 8 hours.

Within 96 hours, it is excreted in the form of inactive metabolites and 70% of the dose taken unchanged. Through the intestines - 57%, through the kidneys - 13%.

Systemic absorption with external or intravaginal use is negligible.

Indications for use

Pills and capsules

The use of capsules and tablets Ketoconazole is indicated for the treatment and prevention of mycoses caused by microorganisms sensitive to the drug:

• infections of the mucous membranes of the gastrointestinal tract;
• severe lesions of the skin, hair and nails (including dermatophytosis, onychomycosis, versicolor versicolor);
• systemic mycoses: blastomycosis, candidiasis, histoplasmosis, paracoccidioidomycosis, coccidioidomycosis;
• chronic recurrent vaginal candidiasis, with the ineffectiveness of local therapy;
• fungal infectious diseases in debilitated patients, including those with immunodeficiency (for prevention).

Vaginal suppositories

• chronic recurrent and acute vaginal candidiasis;
• prevention of fungal infections of the vagina in case of reduced body resistance, during treatment with drugs (including antibiotics) that cause disruption of the normal microflora of the vagina.

Cream for external use 2%

Topical application of Ketoconazole cream is indicated for the treatment of skin mycoses caused by fungi sensitive to ketoconazole:

• candidiasis of the skin;
• epidermophytosis inguinal;
• dermatomycosis of smooth skin (ringworm);
• epidermophytosis of the feet and hands;
• seborrheic dermatitis caused by Pityrosporum ovale;
• pityriasis versicolor.

Shampoo

The use of Ketoconazole shampoo is indicated for the treatment and prevention of the growth of fungal flora on the scalp, including pityriasis versicolor and dandruff.

Contraindications

Pills

• severe liver dysfunction;
• concomitant therapy with terfenadine, astemizole, triazolam, cisapride, quinidine, simvastatin, lovastatin, pimozide;
• lactation;
• hypersensitivity to the components of the drug.

According to the instructions, Ketoconazole should be taken with caution in case of liver disease, a history of allergic reactions to drugs, adrenal dysfunction, in combination with antacids, if necessary, the simultaneous long-term use of hepatotoxic agents.

The use of Ketoconazole tablets during pregnancy is possible only in special cases when the expected therapeutic effect for the mother outweighs the potential threat to the fetus.

Capsules

• severe liver dysfunction;
• breast-feeding;
• hypersensitivity to macrolides and other components of the drug.

During gestation, the use of capsules is allowed only in cases where the expected therapeutic effect for the mother outweighs the potential threat to the fetus.

Vaginal suppositories

• I trimester of pregnancy;
• age up to 12 years;
• individual intolerance to the components of the drug.

It is recommended to use Ketoconazole with caution in the II and III trimester of pregnancy, during breastfeeding and at the age of 12 to 18 years.

Cream for external use 2%

• violation of the integrity of the skin in the area of the intended application of the cream;
• hypersensitivity to the components of the composition.

Shampoo

Use is contraindicated in case of individual intolerance to the components that make up it.

Instructions for the use of Ketoconazole: method and dosage

Pills and capsules

Ketoconazole tablets and capsules are taken orally with meals.

Recommended dosage:

• dermatomycosis, versicolor versicolor, candidiasis of the skin and oral cavity, onychomycosis, systemic mycoses: adults and children weighing more than 30 kg: 1 pc. (With 200 mg) once a day. If necessary, to achieve a significant clinical effect, the daily dose can be increased to 2 pcs. (400 mg). For children with a body weight of 15-30 kg, the dose is 1/2 pc. (With 100 mg). The duration of the course depends on the diagnosis and can be: dermatomycosis - up to 28 days; versicolor versicolor - 10 days; candidiasis of the skin and oral cavity - 14–21 days, onychomycosis - until clinical and mycological improvement from 180 to 360 days, systemic mycoses - 30–60 days;
• vaginal candidiasis: 2 pcs. per day for 5 days;
• prevention of fungal infections: adults - 2 pcs. per day, children - at the rate of 4-8 mg per 1 kg of the child's weight per day. The duration of the course is prescribed individually, taking into account the clinical situation.

After the symptoms of the disease have completely disappeared, taking the tablets and capsules should be continued for several days.

If after 28 days of using the drug there are no signs of significant improvement in the condition, the diagnosis must be verified.

Vaginal suppositories

Ketoconazole suppositories are intended for intravaginal use.

For the procedure, you should remove the candle from the contour packaging, take a position lying on your back, and insert it deeply into the vagina.

Recommended dosage: 1 pc. 1 per day. The duration of the course is from 3 to 5 days, with chronic candidiasis - 10 days.

Cream for external use 2%

Ketoconazole cream is applied externally, by applying a thin layer of the drug to the infected and adjacent skin area.

The doctor prescribes the duration of the course of treatment individually, taking into account clinical indications.

Recommended dosage:

• dermatomycosis of smooth skin, inguinal epidermophytosis, athlete's foot and hands, candidiasis of the skin, pityriasis versicolor: once a day. Duration of treatment: dermatomycosis of smooth skin - 21-28 days, epidermophytosis inguinal - 14-28 days, epidermophytosis of the hands and feet - 28-42 days, pityriasis versicolor and candidiasis of the skin - 14-21 days;
• seborrheic dermatitis: 1 or 2 times a day for 14–28 days;
• maintenance therapy for inflammation of the sebaceous glands: 1-2 times every 7 days.

After the disappearance of the symptoms of the disease, confirmed by negative results of skin tests for the presence of fungi, the application of the cream must be continued for several days.

Shampoo

Ketoconazole shampoo should be applied liberally to the scalp and left for 5 minutes. Then the hair is thoroughly rinsed with warm water.

Recommended frequency of procedures:

• dandruff treatment: once every three days, course duration - 30 days;
• pityriasis versicolor: 1 time per day for 7 days.

Side effects

Pills

• from the digestive system: rarely - nausea, vomiting; very rarely - a transient increase in the level of liver transaminases, hepatitis;
• from the nervous system: rarely - headache, dizziness, photophobia, reversible increase in intracranial pressure, paresthesia;
• on the part of the reproductive system: rarely (against the background of long-term use of high doses) - menstrual irregularities, inhibition of androgen formation, oligospermia, gynecomastia;
• from the hematopoietic system: rarely - thrombocytopenia.

Capsules

• possible: diarrhea, nausea, vomiting, paresthesia, headache, sleep disturbance, insanity, photophobia, thrombocytopenia, exanthema;
• very rare: fever, hair loss, allergic reactions (urticaria, skin rash), gynecomastia, oligospermia, decreased libido, arthralgia;
• in children in rare cases: nervousness, agitation, insomnia, hyperkinesia, conjunctivitis may appear.

Vaginal suppositories

• allergic reactions: skin rash, urticaria;
• local reactions: itching, irritation and hyperemia of the vaginal mucosa.

Cream for external use 2%

Against the background of the application of the cream, undesirable phenomena can manifest itself as burning, itching, skin irritation, especially at the beginning of treatment.

If a skin rash appears, which is a symptom of a drug allergy, the drug should be discontinued.

Shampoo

After application, the shampoo with ketoconazole is completely washed off with running water, without causing irritation, hypersensitivity and other adverse reactions.

Overdose

Pills and capsules

Symptoms: possible increased manifestation of side effects.

Treatment: immediate gastric lavage. Appointment of symptomatic therapy.

Vaginal suppositories

Due to the low absorption of Ketoconazole with intravaginal use, overdose is unlikely.

Cream for external use 2%

When applied externally, the absorption of the active substance into the systemic circulation practically does not occur, therefore, an overdose of the drug is unlikely.

In case of accidental ingestion of the cream, it is necessary to rinse the stomach. The following shows the conduct of symptomatic therapy.

special instructions

If symptoms of the development of undesirable phenomena appear, the use of the drug should be discontinued and consult your doctor.

If the duration of taking the tablets exceeds 14 days, treatment should be accompanied by regular monitoring of the peripheral blood picture and liver function indicators.

If simultaneous antacid therapy is necessary, Ketoconazole tablets should be taken 2 hours before antacid drugs.

When taking ketoconazole by mouth, alcohol is contraindicated.

Against the background of the use of suppositories in a sexual partner, in rare cases, hyperemia of the penis may occur.

With vaginal candidiasis, simultaneous treatment of both sexual partners is recommended, this will reduce the risk of recurrence of the disease.

Suppositories may impair the reliability of barrier methods of contraception such as latex-containing condoms and vaginal diaphragms.

The cream can only be applied externally, it cannot be used in ophthalmic practice. Do not allow the cream to get into your eyes.

If the use of the cream is prescribed after prolonged external use of glucocorticosteroids, skin irritation may appear. To eliminate it, it is recommended to continue applying the glucocorticosteroid in the morning for 14–21 days, and use ketoconazole in the evening. Then the dose of glucocorticosteroid should be gradually reduced until complete withdrawal. If a potent glucocorticosteroid was used initially, it can be replaced with a less potent glucocorticosteroid.

Influence on the ability to drive vehicles and complex mechanisms

Taking pills and capsules can cause side effects in the patient that affect the speed of psychomotor reactions and concentration of attention, therefore, care should be taken when performing potentially hazardous work, including when driving.

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

Application during pregnancy and lactation

The use of tablets and capsules during pregnancy is possible only in special cases when the expected therapeutic effect for the mother outweighs the potential threat to the fetus.

The use of tablets and capsules during lactation is contraindicated. If it is necessary to take ketoconazole inside, breastfeeding should be discontinued.

The appointment of suppositories is contraindicated in the first trimester of pregnancy. The use of suppositories in the II and III trimester of gestation and during breastfeeding is possible only if, in the opinion of the doctor, the expected benefit from therapy for the mother outweighs the existing risk for the fetus and child.

It is possible to use the cream during pregnancy and lactation due to the low degree of absorption of ketoconazole into the systemic circulation.

Pediatric use

Recommended dosage for tablets and capsules:

• dermatomycosis, tinea versicolor, candidiasis of the skin and oral cavity, onychomycosis, systemic mycoses: children weighing more than 30 kg - 1 pc. (200 mg) once a day, if necessary, the dose can be increased to 2 pcs. Children weighing 15-30 kg - 1/2 pc. (With 100 mg) once a day. Duration of treatment: dermatomycosis - up to 28 days; versicolor versicolor - 10 days; candidiasis of the skin and oral cavity - 14–21 days, onychomycosis - until clinical and mycological improvement from 180 to 360 days, systemic mycoses - 30–60 days;
• prevention of fungal infections: at the rate of 4-8 mg per 1 kg of the child's weight per day. The duration of the course is prescribed individually.

Vaginal suppositories: there is no information on the safety and effectiveness of their use in girls under the age of 12, so their use is contraindicated.

It is recommended to use with caution candles at the age of 12-18 years.

For violations of liver function

The appointment of Ketoconazole tablets and capsules is contraindicated in case of severe liver dysfunction.

Patients with liver disease should be used with caution.

Drug interactions

With the simultaneous use of Ketoconazole in the form of tablets and capsules:

• terfenadine, astemizole, triazolam, cisapride, quinidine, simvastatin, lovastatin, pimozide: drugs the combination of which with ketoconazole is contraindicated;
• antacids, anticholinergics, H2 blockers: contribute to a significant decrease in the absorption of ketoconazole;
• rifampicin, isoniazid, rifabutin, carbamazepine, phenytoin: cause a decrease in the concentration of the drug in the blood plasma;
• cyclosporine, indirect anticoagulants, indinavir, saquinavir, disulfan, vincristine, docetaxel, nifedipine, digoxin, verapamil, carbamazepine, alfentanil, sildenafil, buspirone, alprazolam, the risk of midazolam, an increase in the level of trifabrednizatolone in the blood

With intravaginal and external use of Ketoconazole, there is practically no systemic absorption of the substance, therefore, the interaction of suppositories and cream with other drugs is unlikely.

Analogs

Analogs of Ketoconazole are: tablets - Ketoconazole DS, Fungavis, Funginok, Oronazole, Fungistab, Mycozoral, Nevirapin, Ritonavir, Invirase, Ketazol; capsules - Pradaksa, Krixivan; cream - Dermazole, Nizoral, Ketozoral; ointment - Mikoket, Sebozol, Perhotal; suppositories - Ketoconazole-Altpharm, Livarol, Ketodin; shampoo - Mikanisal, Nizoral, Perkhotal, Nezo-Pharm.

Terms and conditions of storage

Store at temperatures between 15 and 25 ° C; tablets, capsules, suppositories - in a place protected from moisture and light. Keep out of the reach of children.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Tablets and suppositories are available with a prescription, capsules, cream, shampoo - without a prescription.

Reviews of Ketoconazole

Reviews of Ketoconazole in the form of suppositories, cream and shampoo are positive. Patients note the effectiveness of the use of suppositories in the treatment of thrush, good tolerance of the drug. Topical application of ketoconazole for 5 days relieves the feeling of discomfort, itching and other symptoms of fungal disease. Ketoconazole shampoo has a quick effect on dandruff treatment.

In reviews of the cream, patients attribute its availability to the advantages of the drug. But there are reports of the existing risk of recurrence after the complete disappearance of the symptoms of mycosis of the skin.

Few reviews of pills are ambiguous, many of them indicate the frequent development of side effects.

The price of Ketoconazole in pharmacies

The price of Ketoconazole, vaginal suppositories, for a package containing 5 pieces, can range from 233 rubles, for 10 pieces. - from 392 rubles; 1 bottle (150 ml) of shampoo can cost from 187 rubles.

Ketoconazole: prices in online pharmacies

Drug name Price Pharmacy

Shampoo Mirrolla (Mirrolla) against dandruff Ketoconazole 150 ml 172 r Buy

Ketoconazole 400 mg, vaginal suppositories 10 pcs. 189 r Buy

Ketoconazole 400 mg vaginal suppositories 5 pcs. 199 RUB Buy

Ketoconazole (shampoo) 2% medicated shampoo 75 g 1 pc. 249 r Buy

Ketoconazole vaginal suppositories. 400mg 5 pcs. 259 r Buy

Shampoo Mycozoral medicinal Ketoconazole 2% 75 g RUB 300 Buy

Ketoconazole (shampoo) 2% medicated shampoo 150 g 1 pc. 328 RUB Buy

Ketoconazole 400 mg, vaginal suppositories 10 pcs. 329 r Buy

Medicinal shampoo Ketoconazole 2% 150 g 390 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!