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Fluconazole capsule

Product description
Approved date: March 16, 2007
 
Date of revision: October 1, 2010
 
         October 01, 2012
 
         November 30, 2015
 
Fluconazole capsule instructions
 
 Please read the instructions carefully and use them under the guidance of a physician.
 
【Drug Name】
Common name: Fluconazole capsule
English name: Fluconazole Capsules
Pinyin: Fukangzuo Jiaonang
 
[Ingredients] The main component of this product is fluconazole. Its chemical name is: α-(2,4-difluorophenyl)-α-(1H-1,2,4-triazol-1-ylmethyl)-1H-1,2,4-triazole- 1-based ethanol.
Its chemical structure is:
 
 
 
Molecular formula: C13H12F2N6O
 
Molecular weight: 306.28
 
【Properties】 This product is a capsule, and the content is white or off-white powder.
 
[Indications] This product is mainly used for patients with severe conditions in the following indications:
    1. Candidiasis: for the treatment of oropharyngeal and esophageal candidiasis; disseminated candidiasis, including peritonitis, pneumonia, urinary tract infections; Candida vulvovaginitis. Can also be used in patients with bone marrow transplantation to prevent the occurrence of Candida infection when receiving cytotoxic drugs or radiation therapy.
    2. Cryptococcosis: used to treat new cryptococcosis outside the meninges; when treating cryptococcal meningitis, this product can be used as a maintenance therapy for amphotericin B combined with fluorocytosine.
    3. Coccidioidomycosis.
    4. This product can also be used as a substitute for itraconazole for the treatment of blastomycosis and histoplasmosis.
 
【Specification】 100mg
 
[Usage and dosage] Oral. Adults (1) Disseminated candidiasis: The first dose is 0.4g (4 capsules), the next dose is 0.2g (2 capsules), once a day for 4 weeks, and the symptoms are relieved for at least 2 weeks.
 
(2) Esophageal candidiasis: the first dose of 0.2g (2 capsules), the next dose of 0.1g (1 capsule), once a day, for at least 3 weeks, the symptoms lasted for at least 2 weeks. Depending on the treatment response, the dose can also be increased to 0.4g (4 capsules) once a day.
 
(3) Oropharynx candidiasis: the first dose of 0.2g (2 capsules), the next dose of 0.1g (1 capsule), once a day, for at least 2 weeks.
 
(4) Candida vulvovaginitis: single dose, 0.15g (1.5 capsules).
 
(5) Prevention of candidiasis: There are indications for preventive medication 0.2 to 0.4 g (2 to 4 capsules), once a day.
 
If renal insufficiency is only required to be administered once, no dose adjustment is required; when multiple administrations are required, the first dose should be given on the first and second days, and thereafter the dose should be adjusted according to the creatinine clearance rate, as described in the following table. :
 
Creatinine clearance (ml/min)
 
Dosage
 
>50
 
Conventional dose
 
11~50
 
Half of the regular dose
 
Patient undergoing routine dialysis
 
Once every dialysis
 
Pediatric treatment programs have not yet been established. It has been reported that the starting dose is 3-6 mg/kg per day, once a day, and a small number of pediatric patients born between 2 weeks and 14 years old are treated. The result is safe.
【Adverse reactions】
    1. Common digestive tract reactions, manifested as nausea, vomiting, abdominal pain or diarrhea.
    2. Allergic reaction: can be expressed as a rash, occasionally severe exfoliative dermatitis (often accompanied by liver damage), exudative polymorphous erythema.
    3. Hepatotoxicity: Mild transient serum aminotransferase may occur during treatment, and hepatotoxic symptoms may occur, especially in patients with severe underlying diseases such as AIDS and cancer.
    4. Visible dizziness, headache.
    5. In some patients, especially those with severe underlying diseases (such as AIDS and cancer), renal dysfunction may occur.
    6. Occasionally, hematological changes such as transient neutropenia and thrombocytopenia in peripheral blood may occur, especially in patients with severe underlying diseases such as AIDS and cancer.
[Contraindications] It is forbidden to have a history of allergies to this product or other azole drugs.
【Precautions】
    1. This product can cross-allergic reactions with other azole drugs, so this product is banned for anyone who is allergic to azole drugs.
    2. Since this product is mainly excreted from the kidney, renal function should be checked regularly during treatment. For patients with renal dysfunction, need to reduce the application.
    3. The long-term prophylaxis of this product in immunodeficiency patients has led to an increase in the resistance of Helicobacter and other azole antifungal drugs such as fluconazole, so it is necessary to grasp the indications to avoid the use of preventive drugs.
    4. Mild transient serum aminotransferase may occur during treatment, and hepatotoxic symptoms may occur. Therefore, the liver function should be checked regularly before and during treatment. If the liver function is persistently abnormal, or the clinical symptoms of hepatotoxicity occur, the product should be stopped immediately.
    5. This product can be used in combination with hepatotoxic drugs. If you need to take this product for more than two weeks or receive multiple times the usual dose, the incidence of hepatotoxicity can be increased. Therefore, it should be closely observed. Every two weeks before treatment and during treatment. Perform a liver function test.
    6. The application of this product should be based on the site of infection and individual treatment response. General treatment should continue until the clinical manifestations of fungal infections and laboratory tests indicate that the fungal infection has disappeared. AIDS patients with cryptococcal meningitis or recurrent oropharyngeal candidiasis need to use this product for long-term maintenance to prevent recurrence.
    7. In patients who have undergone bone marrow transplantation, if the severe neutropenia has occurred in advance, the product should be used prophylactically until the neutrophil count rises to 1×109/L or more and 7 days later.
    8. For patients with impaired renal function, the dosage can be adjusted according to the above scheme (see [Usage and Dosage]); hemodialysis patients can give this product a daily amount after each dialysis, because 3-hour hemodialysis can reduce the blood concentration of this product. About 50%.
[Pregnant women and lactating women]
     1. In animal experiments, high doses of this product can cause changes in abortion, stillbirth, rib deformity, cleft palate in young animals. Although no such condition is found in humans, pregnant women should still be banned.
     2. There is no data on the concentration of this product in breast milk, so lactating women should suspend breastfeeding when using or taking this product with caution.
[Children's medication] This product has insufficient research data on the impact of children. Although a small number of children born between 2 weeks and 14 years old have no adverse reactions with 3-6 mg/kg (by weight) daily dose, children are still not suitable for application.
[Geriatric Use]
    Elderly patients with no renal dysfunction do not need to adjust the dose. Elderly patients with impaired renal function should adjust the dose according to creatinine clearance rate (see [Usage and Dosage] for details).
【medicine interactions】
    1. When this product is combined with isoniazid or rifampin, it can affect the blood concentration of this product.
    2. When combined with sulfonylurea hypoglycemic agents such as tolbutamide, chlorobutazone and glipizide, the blood drug concentration of such drugs may increase, which may lead to hypoglycemia. Therefore, blood glucose should be monitored. And reduce the dose of sulfonylurea hypoglycemic agents.
    3. When the high dose of this product and cyclosporine are combined, the blood concentration of cyclosporine can be increased, and the risk of toxicity is increased. Therefore, it is necessary to be cautious in monitoring the blood concentration of cyclosporine and adjusting the dose. application.
    4. This product is combined with hydrochlorothiazide to increase the blood concentration of this product.
    5. When this product is combined with theophylline, the plasma concentration of theophylline can be increased by about 13%, which can lead to toxicity, so it is necessary to monitor the plasma concentration of theophylline.
    6. When combined with warfarin and other coumarin anticoagulants, this product can enhance the anticoagulant effect of dicoumarin anticoagulants and prolong prothrombin time. Therefore, the prothrombin time should be monitored and used with caution. .
    7. When this product is combined with phenytoin, the blood concentration of phenytoin can be increased, so the blood concentration of phenytoin should be monitored.
 
8. When combined with short-acting benzodiazepines such as midazolam, this product can cause a significant increase in the plasma concentration of midazolam and a psychomotor effect. This effect is more pronounced in oral administration than in intravenous injection. If the patient is required to receive both fluconazole and benzodiazepines, consideration should be given to reducing the dose of benzodiazepines and appropriate observation of the patient.
 
9. This product may cause adverse cardiac reactions, including torsade de pointes, in conjunction with cisapride. Patients receiving fluconazole treatment are prohibited from taking cisapride.
 
10. When taken with tacrolimus, it can cause an increase in the blood concentration of tacrolimus, which may cause nephrotoxicity. Patients taking fluconazole and tacrolimus should be closely monitored.
 
11. When the product is administered at a dose of 400 mg or higher per day with terfenadine, the plasma concentration of terfenadine is significantly increased. Fluconazole 400 mg or higher is contraindicated with terfenadine. When fluconazole is administered at a dose of less than 400 mg per day and taken concurrently with terfenadine, the plasma concentration of terfenadine should be closely monitored.
 
12. When this product is taken together with zidovudine, the blood concentration of the latter can be increased, and the occurrence of adverse reactions associated with zidovudine should be observed.
 
13. This product can cause elevated serum concentrations of these drugs when taken with aspirin or other drugs metabolized by the cytochrome P-450 system. In the absence of clear information, when taking with fluconazole, these drugs should be used with caution and the patient should be closely observed.
 
Doctors should be aware of other drug interactions that have not been studied but may occur.
 
【Drug overdose】
 
There have been reports of overdose of fluconazole. A 42-year-old patient with HIV infection, after taking 8200 mg of fluconazole, experienced hallucinations and excitability. The patient returned to normal within 48 hours of being admitted to the hospital.
 
For patients with overdose, symptomatic treatment (supportive therapy) can be used only.
 
Fluconazole is mostly excreted in the urine, and forced diuresis may increase its clearance rate. Treatment with hemodialysis for 3 hours reduced the plasma concentration of fluconazole by approximately 50%.
【Pharmacology and Toxicology】
    Pharmacological action
    This product is a pyrrole antifungal. The antifungal spectrum is wider. Oral and intravenous injection of fungal infections in humans and various animals, such as Candida infections (including systemic candidiasis in normal or immunocompromised humans and animals), cryptococcal infections (including intracranial infections), Malassezia, Microsporum, Trichophyton, Epidermidis, dermatitis buds, Coccidioides (including intracranial infection) and capsular histoplasma, Fischer-colored bacteria, Kasper Branching spores and the like are effective. The mechanism of action of this product is mainly to selectively interfere with the activity of fungal cytochrome P-450, thereby inhibiting the biosynthesis of ergosterol on the fungal cell membrane.
 
    Toxic effect
    Teratogenic effects: rats with oral fluconazole 20mg / kg, can slightly delay the delivery process, but does not affect its fertility. Perinatal results in rats showed that some animals developed dystocia and delayed labor when they received 20 mg/kg and 40 mg/kg. The main manifestation is a slight increase in the number of stillbirths and a decrease in the number of surviving newborn rats. The effect of high-dose fluconazole on the delivery of rats may be related to the specific reduction of estrogen levels in the species. This change in hormone levels has not been observed in women receiving fluconazole.
 
Mutagenicity: Ames test, mouse lymphoma L5178Y cell line test, animal bone marrow micronucleus test, human lymphocyte chromosome test results were negative.
 
Carcinogenicity: The mice and rats were studied. The mice and rats were given oral fluconazole at a dose of 2.5, 5 or 10 mg/kg body weight/day (about 2-7 times the recommended dose of the human body). Month, suggesting that fluconazole has no carcinogenic effects. However, male rats received doses of 5 mg/kg and 10 mg/kg, and continuous administration for 24 months showed an increase in the incidence of hepatocellular adenomas.
 
[Pharmacokinetics] Oral absorption is good, and is not affected by food, antacids, H2 receptor blockers. Oral administration of this product can absorb about 90% of the dose. A single oral dose of 100 mg, the average peak plasma concentration (Cmax) is 4.5 ~ 8 mg / L. The apparent volume of distribution (Vd) is close to the total amount of liquid in the body. The plasma protein binding rate of this product is low (11%~12%), and it is widely distributed in skin, blister fluid, peritoneal fluid, sputum and other tissue fluids. The concentration of urine and skin is about 10 times that of blood. The blister skin is about 2 times; saliva, sputum, blister fluid, and nails are close to the blood drug concentration; when the meninges are inflamed, the concentration of the product in the cerebrospinal fluid can reach 54% to 85% of the blood drug concentration. A small amount of this product is metabolized in the liver. It is mainly excreted from the kidney, and it is discharged from the urine in the original form, accounting for more than 80% of the dose. The half-life of blood elimination (t1/2) was 27 to 37 hours, which was significantly prolonged when renal function was reduced. Hemodialysis or peritoneal dialysis can partially remove this product.
 
Pharmacokinetics in children
 
The reported pharmacokinetic parameters for children are as follows:
 
The age of the child being studied
 
dose
 
(mg/kg body weight)
 
half life
 
(hour)
 
Area under the curve
 
(AUC, micrograms • hour/mg)
 
11 days - 11 months
 
Single dose intravenous injection
 
3 mg / kg body weight
 
twenty three
 
110.1
 
9 months - 13 years old
 
Single dose oral
 
2 mg / kg body weight
 
25
 
94.7
 
9 months - 13 years old
 
Single dose oral
 
8 mg / kg body weight
 
19.5
 
362.5
 
5-15 years old
 
Multiple dose intravenous injection
 
2 mg / kg body weight
 
17.4*
 
1.3
 
5-15 years old
 
Multiple dose intravenous injection
 
3 mg / kg body weight
 
15.5
 
41.6
 
5-15 years old
 
Multiple dose intravenous injection
 
4 mg / kg body weight
 
15.2*
 
1.9
 
5-15 years old
 
Multiple dose intravenous injection
 
8 mg / kg body weight
 
17.6*
 
1.7
 
*Show the results of the last day of the test
[Storage] Sealed and stored in a dry place (10 ~ 30 ° C).
[Packing] Aluminum-plastic packaging, 6 capsules per box; 12 capsules per box.
[Validity Period] 24 months
[Executive Standards] "Chinese Pharmacopoeia" 2015 Edition 2
 
[Approval No.] National Drug Standard H20059399
【manufacturer】
 
Company Name: Guangdong Pi Di Pharmaceutical Co., Ltd.
 
    Production address: No. 66, Pidi Avenue, Yueshan Town, Kaiping City, Guangdong Province
 
    Postal code: 529331
 
Phone number: (0750) 2789348 2783621
 
400-8899-328 (National Service Phone)
 
    Fax number: (0750) 2789348
 
Website: http://www.pdpharm.com
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