Ketoconazole tablets

Ketoconazole is a synthetic imidazole dioxane derivative that has antibacterial and bactericidal activity against dermatophytes, yeasts (Candida, Malassezia, Torulopsis and Cryptococcus), dimorphic fungi and some molds. Ketoconazole is less sensitive to Aspergillus, Sporothrix Schenckii, some dark-colored fungi and Mucor, but is an exception to Entomophthora. Ketoconazole exerts its antibacterial effect by inhibiting the biosynthesis of fungal ergosterol and changing the composition of other lipid compounds in the cell membrane. Clinical pharmacology and drug interaction research data show that oral ketoconazole twice a day, 200 mg each time, for 3-7 days, will cause a slight prolongation of the QT interval: when the plasma concentration of ketoconazole reaches its peak (approximately 1-4 hours after taking the drug), the average maximum prolongation is 6-12 milliseconds, but this slight prolongation of the QT interval is not clinically significant.

Ketoconazole.

This product is white to slightly reddish tablets.

1. Systemic fungal infections, such as systemic candidiasis, paracoccidioidomycosis, histoplasmosis, coccidioidomycosis and blastomycosis. 2. Infections of the skin, hair and nails caused by dermatophytes and/or yeasts (tinea dermatophytes, onychomycosis, candidal perionychia, tinea versicolor, pityriasis dryis, Malassezia folliculitis, chronic skin and mucosal candidiasis, etc.). This product can be used for treatment when local treatment is ineffective or when topical treatment is not suitable due to factors such as the site, area and depth of infection. 3. Gastrointestinal yeast infections. 4. Chronic and recurrent vaginal candidiasis that is ineffective with local treatment. 5. It can also be used for the prevention and treatment of patients who are prone to opportunistic fungal infections due to reduced immune function (hereditary and caused by diseases or drugs). This product has poor penetration into the central nervous system and is not suitable for the treatment of fungal meningitis.

This product must be used under the guidance of a doctor. This product should be taken with meals to achieve maximum absorption. 1. Adults: Skin, gastrointestinal and deep infections: Oral, 0.2g (1 tablet) once a day. If necessary, it can be increased to 0.4g (2 tablets) once a day, or 0.2g (1 tablet) once a day, twice a day. Vaginal candidiasis: Oral, 0.4g (2 tablets) once a day. 2. Children: Children weighing 15-30 kg, 0.1g (half a tablet) once a day, or as directed by a doctor. Children weighing more than 30 kg, the same amount as adults. 3. Preventive treatment of immunodeficient patients: Adults: 0.4g (2 tablets) a day. Children (weighing more than 15 kg): 0.1g to 0.2g (4-8mg per kilogram of body weight) once a day. 4. The usual course of treatment for this product is as follows: vaginal candidiasis: 5 consecutive days; skin infections caused by dermatophytes: about 4 weeks; tinea versicolor: 10 days; oral and skin candidiasis caused by Candida: 2-3 weeks; hair infection: 1-2 months; nail infection: 6-12 months, depending on the growth rate of the nail, and it is necessary to wait until the diseased nail grows out completely; systemic candidiasis: 1-2 months; paracoccidioidomycosis, histoplasmosis, coccidioidomycosis: the appropriate course of treatment is 3-6 months. In general, the course of treatment for this product should last at least 1 week after the symptoms disappear and the fungal examination turns negative.

According to the following convention: very common (1/10); common (1/100, 1/10); uncommon (1/1,000; 1/100); rare (1/10,000; 1/1,000); very rare (1/10,000), including individual cases, the adverse reactions are ranked by incidence: In the clinical trials of this product, the main adverse reactions are: 1. Gastrointestinal tract, hepatobiliary system: common reactions are nausea, vomiting, abdominal pain; rare reactions are diarrhea, dyspepsia, reversible liver enzyme elevation; 2. Skin and subcutaneous tissue: common reactions are itching; rash and hair loss are rare; 3. Nervous system: rare headache, dizziness, photophobia; rare sensory abnormalities; 4. Reproductive system and breast: rare reversible male breast enlargement (on daily basis)

According to the following convention: very common (1/10); common (1/100,1/10); uncommon (1/1,000;1/100); rare (1/10,000;1/1,000); very rare (1/10,000), including individual cases, the adverse reactions are ranked by incidence: In the clinical trials of this product, the main adverse reactions are: 1. Gastrointestinal tract, hepatobiliary system: common reactions include nausea, vomiting, and abdominal pain; rare reactions include diarrhea, dyspepsia, and reversible liver enzyme elevation; 2. Skin and subcutaneous tissue: common reactions are itching; rash and hair loss are rare; 3. Nervous system: rare headache, dizziness, and photophobia; rare sensory abnormalities; 4. Reproductive system and breast: rare reversible male breast enlargement (at a daily dose of 0.2g or 0.4g, higher than the recommended dose); rare impotence; 5. Blood and lymphatic system: rare thrombocytopenia. According to post-marketing experience, the following adverse reactions have also been reported: 1. Immune system: extremely rare allergic reactions, including individual cases of anaphylactic shock; 2. Nervous system: extremely rare reversible intracranial pressure increase (such as papilledema, prominent fontanelle in infants); 3. Hepatobiliary system: extremely rare severe hepatotoxicity (including jaundice, hepatitis, liver necrosis confirmed by biopsy), including liver failure leading to liver transplantation or death; 4. Skin and subcutaneous tissue: extremely rare urticaria; 5. Reproductive system and breast: extremely rare menstrual abnormalities, decreased sperm (higher than the recommended dose at a daily dose of 0.2g or 0.4g), male breast enlargement; when taking a dose of 0.2g once a day, a transient decrease in plasma testosterone concentration may occur, but the plasma testosterone concentration will return to normal within 24 hours after taking the drug. When treated for a long time at this dose, the testosterone amount is not significantly different from the control group. This product is contraindicated in the following situations: 1. Patients with known allergy to ketoconazole or any of the ingredients of this product; 2. Patients with acute or chronic liver disease; 3. Since the co-administration of this product with drugs metabolized by CYP3A4 may increase the plasma concentration of these drugs, which may lead to QT interval prolongation and individual occurrence of torsades de pointes, this product is contraindicated for co-administration with the following drugs: terfenadine, astemizole, mizolastine, cisapride, dofetilide, quinidine, pimozide; 4. Since the co-administration of domperidone may lead to QT interval prolongation, this product is contraindicated for co-administration with domperidone; 5. It is contraindicated for co-administration with triazolam and midazolam oral preparations; 6. It is contraindicated for co-administration with HMG-CoA reductase inhibitors metabolized by CYP3A4 enzymes, such as simvastatin and lovastatin.

Precautions for children: There is limited data on the use of this product for children weighing less than 15kg, so it is not recommended for children. Precautions for pregnancy and lactation: There is no research data on pregnant women, so this product should not be used during pregnancy unless the possible benefits outweigh the potential risks to the fetus. This product can be excreted in breast milk, so breastfeeding should be stopped when breastfeeding women take this product. Precautions for the elderly: Use with caution in elderly patients.

1. Drugs that affect ketoconazole metabolism Enzyme-inducing drugs, such as rifampicin, rifabutin, carbamazepine, isoniazid and phenytoin, will significantly reduce the bioavailability of ketoconazole and reduce its efficacy. Drugs that affect gastric acid: See [Precautions]. Ritonavir will increase the bioavailability of ketoconazole, so when the two are used together, the dosage of ketoconazole should be reduced as appropriate. 2. Drugs affected by ketoconazole Some drugs are metabolized by liver P450 enzymes, especially CYP3A4 enzymes. Ketoconazole can inhibit the metabolism of these drugs, resulting in enhanced and/or prolonged effects (including side effects) of these drugs. For example: (1) When using ketoconazole, the following drugs are prohibited from being used in combination: Since the combination of this product with drugs metabolized by CYP3A4 may increase the plasma concentration of these drugs, which may lead to QT interval prolongation and the occurrence of torsades de pointes in some cases, this product is prohibited from being used in combination with the following drugs: terfenadine, astemizole, mizolastine, cisapride, dofetilide, quinidine, pimozide; Since the combination with domperidone may cause QT interval prolongation, this product is prohibited from being used in combination with domperidone; It is prohibited to be used in combination with triazolam and midazolam oral preparations; (2) If used in combination with ketoconazole, the dose should be reduced as appropriate, and the plasma concentration, action or side effect of the drug should be monitored: oral anticoagulants HIV protease inhibitors, such as indinavir and saquinavir; some anti-tumor drugs, such as vinblastine, busulfan, and docetaxel; calcium channel blockers metabolized by CYP3A4, such as dihydropyridines and verapamil (possibly); some immunosuppressants: cyclosporine, tacrolimus, and rapamycin; others: digoxin, carbamazepine, buspirone, alfentanil, sildenafil, alprazolam, brotizolam, intravenous midazolam, rifabutin, methylprednisolone, trimetrexate, ibastine, and reboxetine; 3. Occasionally, there have been case reports of this product having a disulfiram-like reaction, manifested as facial flushing, rash, peripheral edema, nausea, and headache, which can completely disappear within a few hours.

Store in a dry place at 15-30℃.

0.2 g

60 months.