Fluconazole Stella 150mg medicine for fungal infection (1 blister x 1 tablet)
Dosage form Box of 1 blister x 1 tablet
Specifications Fluconazole
Ingredient
| Composition information | Content |
| Fluconazole | 150mg |
Uses
Indications
Fluconazole Stella 150mg drug is indicated in the following cases:
Fungal infections in adults:
Treatment of fungal infections in children 0 - 17 Tai:
Use fluconazole 50mg/day for up to 28 days of time has been shown to not affect the concentration of testosterone in plasma in men or steroid levels in women in childbearing age. In healthy male volunteers, using fluconazole at a dose of 200 - 400mg/day does not significantly affect clinical effects on endogenous steroid concentrations or on the stimulating response by ACTH. Studies on interactive with antipipine show that the use of single -dose or multiple doses of fluconazole 50mg does not affect the metabolism of this substance.
In vitro sensitivity
fluconazole has antifungal activity for most commonly common Candida species (including C. Albicans, C. Parapsilosis, C. Tropicalis). C. Glabrata shows a wide sensitivity while C. Krusei is resistant to fluconazole. Fluconazole also has in vitro activity for Cryptococcus NeoForans and Cryptococcus Gattii as well as local epidemiological molds Blastomyces dermatiditis, Coccidioides immitis, Histoplasma capsulatum and paracoccioides brasiliensis.
Medicine resistance mechanism
Candida spp. Has developed a number of resistance mechanisms with Azole antifungal drugs. The mushroom strains have developed one or more of this resistance mechanism that is thought to have a minimum minimum inhibitory concentration (mic) for fluconazole, which causes adverse effects in vivo and clinical. There have been reports on superinfection with other Candida species with C. Albicans are often not sensitive to fluconazole (for example, Candida Krusei). Such cases may need an alternative antiviral therapy.
pharmacokinetic
absorption
After drinking, fluconazole is well absorbed, plasma concentrations (and systemic bioavailability) reaches over 90% of the concentration achieved after intravenously. Oral absorption is not affected by the use of food. The peak concentration of plasma in hunger appears in the range of 0.5 - 1.5 hours after drinking. Plasma concentrations are proportional to the dose. In a state of determination, the concentration of drugs is reached 90% on 4 - 5 when using multiple doses x 1 time/day. Using the offensive dose (on 1 day 1) 2 times the usual daily dose causes the drug concentration in plasma to reach approximately 90% in the status of the 2nd day.
Distribution
Volume of ants is approximately equal to the total amount of water in the body. The ability to attach to low plasma proteins (11 - 12%). Fluconazole has been studied with good permeability into all body fluids. Fluconazole concentration in saliva and sputum is equivalent to plasma concentrations. In patients with fungal meningitis, the level of fluconazole in the cerebrospinal fluid reaches approximately 80% of the corresponding concentration in plasma. The concentration of fluconazole on the skin is high, higher than its concentration in serum, achieved in the horny layer, epidermis - dermis and external sweat.
fluconazole is accumulated in the skin's horny layer. At a dose of 50mg x 1 time/day, the concentration of fluconazole after 12 days is 73μg/g and 7 days after stopping the treatment of fluconazole concentration is still 5.8μg/g. With a dose of 150mg x 1 time/week, the concentration of fluconazole in the horn layer on Saturday is 23.4μg/g and 7 days after using the second dose of concentration in the horn layer is still 7.1μg/g. The concentration of fluconazole on the foundation after 4 months of use at a dose of 150mg x 1 time/week is 4.05μg/g at a healthy nail and 1.8μg/g in the disease and can still find fluconazole in the foundation templates 6 months after the end of treatment.
Metabolism
fluconazole is mildly metabolized. With a radioactive dose, only 11% is excreted in the form of unchanged urine. Fluconazole is a moderate inhibitor ISOZE CYP2C9 and CYP3A4. Fluconazole is also a powerful ISOZE CYP2C19 inhibitor.
Elimination
Selling time for plasma is approximately 30 hours. Fluconazole's main elimination sugar is kidney, with approximately 80% of the dose of use appears in a constant form of urine. The clearance of fluconazole is proportional to the clearance of creatinine. There is no evidence that there are its metabolites during circulation. The long -term semi -discharged time in plasma is the basis for a single -dose treatment regimen for vaginal candidiasis for 1 time/day and 1 time/week for other indications.
Dynamic pharmacokinetics in people with renal failure
In patients with severe renal impairment (GFR
Pharmacokinetics during breastfeeding
A pharmacokinetic study in 10 breastfeeding women, who temporarily stop or stop breastfeeding, evaluate fluconazole concentration in plasma and breast milk for 48 hours after the single dose of 150 mg fluconazole. Fluconazole was discovered in breast milk with an average concentration of about 98% compared to the mother's plasma concentrations. The average peak concentration in breast milk is 2.61mg/l achieved at 5.2 hours after the dose. Fluconazole dose is estimated daily for infants from breast milk (assuming the average milk consumption norm is 150ml/kg/day) based on the average peak concentration in milk is 0.39 mg/kg/day, accounting for about 40% of the recommended doses for babies ( Pharmacokinetics in children
Dynamic data is evaluated for 113 children from 5 studies, 2 single -dose study studies, 2 multi -dose studies and 1 study in newborn babies. Data from a study cannot be explained by changes in the way of construction through the research process. There are more data from 1 study using drugs for patients outside clinical trials. After using 2 - 8mg/kg fluconazole for children from 9 months to 15 years old, AUC is about 38μg/m found on every 1mg/kg unit of dose. The average fluconazole waste time in plasma ranges from 15 - 18 hours and the distribution volume is about 880ml/kg after multiple dosage use.
Fluconazole's waste sale time is higher, about 24 hours after a single dose. This is comparable to the semi -exhaust time of fluconazole in plasma after taking a single dose of 3mg/kg intravenously for children from 11 days - 11 months of age. The distribution of this age group is about 950ml/kg. Experience with fluconazole in newborns is limited in pharmacokinetics studies in newborn babies.
The average age at the first dose is 24 hours (about 9 - 36 hours) and the average weight at birth is 0.9kg (about 0.75 - 1.10kg) for 12 infant children lacking in the average pregnancy of about 28 weeks. 7 patients have completed the application, up to 5 times the Fluconazole intravenous infusion at a dose of 6mg/kg is carried out every 72 hours. The average selling time (hour) is 74 (about 44 - 185) on the 1st day of the average time of 53 (about 30 - 131) on 7 and 47 (about 27 - 68) on the 13th. The area under the curve (microgram.h/ml) is 271 (about 173 - 385) on the 1st and increased with an average of 490 (about 292 - 734) on the average of 360 (about 167) on the average of 360 - 566) The distribution volume (ml/kg) is 1183 (about 1070 - 1470) on the 1st day and increased over time to the average of 1184 (about 510 - 2130) on 7 and 1328 (about 1040 - 1680) on the 13th.
Pharmacokinetics in the elderly
Conducting pharmacokinetics research on 22 people ≥ 65 years old, taking a single dose of 50mg fluconazole. Of these, 10 patients take more diuretics. CMAX is 1.54μg/ml and achieved after 1.3 hours. The average AUC is 76.4 ± 20.3μg/h/ml and the last elimination time is 46.2 hours. These pharmacokinetic parameters are higher than the same values on healthy young male volunteers.
Concomitance with diuretics does not significantly change the AUC or CMAX of Fluconazole. Moreover, creatinine clearance (74ml/minute), the percentage of unprocessed drugs found in urine (0 - 24 hours, 22%) and fluconazole clearance through the kidney (0.124ml/min/kg) in the elderly are often lower in young volunteers. Therefore, the pharmacokinetic change of fluconazole in the elderly seems to be related to the characteristics of renal function impairment at this age.
Before taking Fluconazole Stella 150mg medicine for fungal infection (1 blister x 1 tablet)
How to use
Use Fluconazole Stella 150mg oral.
Dosage
Fluconazole Stella 150mg dose should be based on the nature and degree of fungal infection. The treatment of fungal infections requires the use of multi -dose regimen, so it should continue to be treated until clinical parameters or tests show that the active fungal infection has been improved. Inadequate treatment can be used to recur with fungal infections
Cryptococcus fungal infection
Treatment of cryptococcus meningitis
attack dose: 400mg of the first day, the next dose later: 200 - 400mg x 1 time/day.
The normal treatment time is at least 6-8 weeks, in life -threatening cases that can increase to 800mg/day.
Maintain therapy to prevent recurrence of Cryptococcus meningitis in patients with high risk of recurrence: 200mg x 1 time/day.
Duration of treatment: Not determined at a dose of 200mg/day.
Coccidioides Immitis infection
Use 1 tablet, the treatment time is from 11 - 24 months or longer depending on the patient.
Treatment of mucosal candidiasis
Oral Candida infection - Hau
attack dose: 2 tablets on the first day, the next dose then 1 tablet/day.
Treatment time: 7 - 21 days (until the condition of oral Candida - Mind is relieving).
esophagus infection
attack dose: 2 tablets on the first day, the next dose later: 1 tablet/day.
Treatment period of 14 - 30 days (until the contamination of real Candida infection - improvement).
Candida infection
Take 2 capsules/day.
Treatment time: 7 - 21 days.
Treatment time may be longer in patients with serious damaged immune function.
Prevention of recurrence of mucosal candidiasis in HIV -infected patients with a high risk of recurrence
Oral Candida - Mate: 1 tablet/day.
Infection of the esophagus: 1 tablet/day.
Unlimited treatment period for patients with chronic immunosuppressants.
Genital candidiasis infection
Adults
Vaginal candidiasis: 1 tablet, single dose.
Vaginal Candida Rehabilitation and Prevention (recurrence 2-4 times/year): 1 tablet every 3 days, a total of 3 doses (1st, 4th and Saturday) and then use the dose of 1 tablet once a week (for 6 months).
Foreskin inflammation caused by Candida: 1 tablet, single dose.
Youth (12 - 17 years old)
Safety and effectiveness of child genital candidiasis indications have not been set. If you are required to treat genital candidiasis, you should take the same dosage as in adults.
Fungal infections
Fungal fungus, stem fungus, inguinal fungus and candida infection in the skin
Use 1 tablet 1 time/week, treat for 2-4 weeks, leg mushrooms may take up to 6 weeks.
versicide
Use Fluconazole Stella 150mg 2 capsules 1 time/week, time from 1-3 weeks.
Mushrooms
Take 1 capsule 1 time/week. It is necessary to continue treating until the nail is infected with thousands of replacement fungal (new nails have not been developed instead). The re -development of nails and toenails usually takes time from 3 to 6 months and from 6 to 12 months. However, the growth rate may vary a lot depending on the individual and age. For chronic fungal infections for a long time, after successful treatment, the foundation is sometimes deformed.
Candida infection prophylaxis in patients with neutropenia prolonged
Use 2 tablets. It is advisable to start treating a few days before the prediction begins to be neutropenia and continue within 7 days after recovery of neutropenia when the number of neutrophils increases over 1,000 cells/mm3.
Elderly
Adjust the dose based on kidney function.
Patients with renal failure
No dose adjustment when using a single dose. In patients (including children) impaired kidney function using multi-dose fluconazole, the starting dose should be 1-2 tablets based on the recommended daily dose for each specified. After this starting dose, daily (as directed) based on the following table:
50% The dose is based on creatinine clearance.
Patients with liver failure
Restricted data in patients with liver failure, so it is advisable to use Fluconazole carefully in patients with liver function.
Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.
What to do when overdose? In case of serious overdose, blood decomposition should be carried out.
What to do when forgetting 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double dose to compensate for missed dose.
Side Effects
When using Fluconazole Stella 150mg, you may experience unwanted effects (ADR).
Common, ADR> 1/100
Digestive: abdominal pain, vomiting, diarrhea, nausea.
Liver: Increased alanin aminotransferase, increased aspartate aminotransferase, hyperkemop of alkaline phosphatase.
Skin and subcutaneous tissue: rash.
Uncommon, 1/1000 Blood and lymphatic system: Anemia. Mental: Sleep or insomnia. Metabolism and nutrition: Reduce appetite. Neurology: epilepsy, paresthesia, dizziness, loss of taste. ears and mesmerizing: dizziness. Digestive: constipation, indigestion, flatulence, dry mouth. Mile liver: cholestasis, jaundice, increase bilirubin. Skin and subcutaneous tissue: drug rash, urticaria, itching, increased sweating. muscle-joints and connective tissue: muscle pain. Body: fatigue, discomfort, weakness, fever. Rare, 1/10000 ≤ ADR Blood and lymphatic system: granulocytosis, leukopenia, thrombocytopenia, neutropenia. Immune: Anaphylaxis. Metabolism and nutrition: Hyper cholesterol, hyperglyceride, hypotension, hypotension. Neurology: Run. heart: Twisted, long -lasting QT. Liver: Hepatic failure, hepatic necrosis, hepatitis, liver cell damage. Skin and subcutaneous tissue: Poisoned epidermal necrosis, Stevens-Johnson syndrome, acute all-body pustules syndrome, flaking dermatitis, angioedema, face edema, hair loss. Instructions on how to handle ADR: When the side effects of the drug are encountered, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.
Warnings
Before using the drug you need to read the instructions carefully and refer to the information below.
Contraindicated
Fluconazole Stella 150mg drug is contraindicated in the following cases:
Hypersensitivity to fluconazole, Azole antifungal group or any ingredient of the drug.
Caution when using
Ingent disease
Fluconazole is studied to treat first -instant disease in children. Fluconazole has been shown to be not superior to Griseofulvin and the overall success rate is less than 20%. Therefore, Fluconazol 150mg should not be used to treat first impatient disease.
Cryptococcus fungal infection
Evidence of Fluconazole's effectiveness in the treatment of cryptococcus fungal infections in other positions (such as Cryptococcus fungal infections in coordination and skin) is limited, making it difficult to make recommendations on dosage. Deep fungal infections have local epidemics: Evidence of the effectiveness of fluconazole in the treatment of various forms of fungal infections with local epidemics such as paracocioides infections, Sportrichum infection - lymphatic and histoplasma infection is limited, making it difficult to make recommendations on dosage.
Kidney
Should use Fluconazole Stella 150mg cautious in patients with kidney dysfunction.
adrenal failure
Ketoconazole has been known to cause adrenal insufficiency, which can also happen even though rare in Fluconazole. The adrenal failure is related to the simultaneous treatment with Prednisone.
liver - bile
Should use Fluconazole Stella 150mg cautious in patients with liver dysfunction. Fluconazole Stella 150mg is related to a number of serious rare cases of liver toxicity including death, mainly in patients with severe pathology. In cases of liver toxicity related to fluconazole, there is no clear relationship with the total daily dose, treatment time, gender or age of the patient.
Toxicity on the liver due to fluconazole often recovers after stopping treatment. Patients with abnormal liver function tests during treatment with Fluconazole need to be closely monitored to the progression of severe liver damage. Patients need to be notified of symptoms of serious liver effects
Cardiovascular
Some azole, including fluconazole, is associated with extending the QT interval on the electrocardiogram. Fluconazole extends the QT interval through rectifier inhibition of potassium canal (IKR). Extending the QT distance due to other pharmaceutical products (such as amiodarone) can be expanded through the inhibition of Cytochrom P450 (CYP) 3A4. The report after the circulation shows that there are very rare cases of QT interval and torsion in patients using fluconazole. These reports include patients with serious illnesses with many risk factors, such as structural heart disease, electrolyte abnormalities and coordinated with other drugs. Patients who lower potassium and heart failure are at high risk of ventricular arrhythmia and life -threatening torsion. Fluconazole 150mg should be used in patients with potential arrhythmia. Contraindicated with other drugs that extend the QT range and are metabolized through Cytochrom P450 (CYP) 3A4.
halofantrine
halofantrine has been shown to extend the QTC range at the recommended dose and is a substrate of CYP3A4. It is recommended not to simultaneously use fluconazole and halofantrine.
Skin reaction
has appeared (rare) flaky skin reactions, such as Stevens-Johnson syndrome and poisoned epidermal necrosis in patients during the treatment stage with fluconazole. AIDS patients are susceptible to serious skin reactions for many drugs. If the skin rash appears, which is considered to be caused by fluconazole, appear in patients treated with surface fungal infections, need to stop treating this drug. If a skin rash appears in patients with invasive fungal fungal infections or fungal infections, closely monitor and stop fluconazole in the event of a diverse or diverse glossy or rosy lesions.
hypersensitivity
There have been reports on the case of anaphylaxis but rare.
cytochrom p450
Fluconazole is a medium inhibitor CYP2C9 and CYP3A4. Fluconazole is also a strong CYP2C19 inhibitor. It is necessary to monitor patients treated with fluconazole when treated simultaneously with drugs with narrow therapy metabolized through CYP2C9, CYP2C19 and CYP3A4.
terfenadine
Need to monitor carefully when using Fluconazole simultaneously lower doses of 400mg/day with terfenadine.
excipients
fluconazole stella 150mg contains lactose. This drug should not be used for patients with rare genetic problems galactose intolerance, total lactase enzyme deficiency or glucose - galactose. Fluconazole 150mg contains flour. Patients who are allergic to wheat (different from fat diarrhea) should not be used.
The ability to drive and operate machinery
No research on the influence of fluconazole on driving or operating machinery. Patients should be warned of the possibility of dizziness or epilepsy while using fluconazole and should not drive or operate machines if any symptoms occur.
Pregnancy
so far there has been no adequate and strict studies on the use of fluconazole for pregnant women. Fluconazole should only be used for pregnant women when the benefits are greater than the risk of the fetus.
Breastfeeding period
fluconazole is excreted into breast milk with lower concentrations than plasma concentrations. Can maintain breastfeeding after taking the only dose of 150mg. However, it is recommended not to breastfeed after repeated dose or high doses of fluconazole.
Drug interaction
Contraindications
Cisapride: There has been a report on cardiovascular events including torsion in patients using Cisapride and Fluconazole simultaneously. A control study showed that the plasma cisapride levels increased significantly and extended QTC when using Fluconazole 200mg x 1 time/day and Cisapride 20mg x 4 times/day. Contraindicated treatment simultaneously fluconazole and cisapride.
Terfenadine: Because of the appearance of serious arrhythmia due to the extension of QTC in patients using Azole antifungal drugs in combination with Terfenadine, studying drug interaction has been done. Research with the dose of fluconazole 200mg 1 time/day does not detect the extension of QTC. Another study with Fluconazole's dose is 400mg and 800mg/day showing that Fluconazole with dose ≥ 400mg/day significantly increases terfenadine levels in plasma when used simultaneously fluconazole and terfenadine. Contraindications for combination of fluconazole dose ≥ 400mg/day with terfenadine. Strict control should be controlled when indicated in combination of fluconazole at the dose
Astemizole: Concomitance Fluconazole with Astemizole can reduce the clearance of Astemizole. Therefore, increasing the concentration of Astemizole in plasma, which can lead to extending the QT interval and rarely appears twisted. Contraindicated to simultaneously use fluconazole and astemizole.
Pimozide: Although there is no In vitro or in vivo research, simultaneously using fluconazole with pimozide can inhibit the transformation of Pimozide. Increasing pimozide concentration in plasma can extend the QT interval and sometimes the torsion phenomenon appears. Contraindicated to simultaneously use fluconazole and pimozide.
Quinidine: Although there is no in vitro or in vivo research, simultaneously using fluconazole and quinidine can inhibit quinidine metabolism. Using quinidine can extend the QT interval and rarely appear torsion phenomenon. Contraindicated to simultaneously use fluconazole and quinidine.
erythromycin: simultaneously use fluconazole and erythromycin simultaneously capable of increasing the risk of heart toxicity (extending the QT range, causing torsional phenomenon) and thus causing sudden death to the heart. Contraindications to simultaneous use of fluconazole and erythromycin.
Recommendation does not combine
Halofantrine: Fluconazole may increase halofantrine levels in plasma due to CYP3A4 inhibitors. Simultaneous use of fluconazole and halofantrine has the ability to increase the risk of toxicity with the heart (extending the QT range, causing the torsion phenomenon) and thus sudden death to the heart. Need to avoid combining.
Precautions when combining
Amiodarone: Concomitant use of fluconazole with amiodarone may increase the QT range.
Be cautious if you really need to use Fluconazole and Amiodarone simultaneously, especially high doses of fluconazole (800mg).
Combining fluconazole with other drugs below should be cautious and adjustable.
The effect of other drugs on fluconazole
Rifampicin: simultaneously use Fluconazole and Rifampicin to reduce 25% of the area under the curve (AUC) and shorten 20% of fluconazole waste time. In patients with simultaneous use of rifampicin with fluconazole, it is necessary to consider increasing the dose of fluconazole.
Interactive studies show that drinking fluconazole simultaneously with food, cimetidine, antacids or after general irradiation for bone marrow transplantation, Fluconazole absorption is negligible in terms of clinical.
Hydrochlorothiazide: In a pharmacokinetic interaction study, simultaneously indicated Hydrochlorothiazide multi -dose for healthy volunteers using fluconazole to increase the plasma concentration of fluconazole by 40%. This effect does not require the need to change the dosage mode of fluconazole in those who are taking diuretics simultaneously with fluconazole.
The effect of fluconazole on other drugs
Fluconazole is a strong inhibitor of cytochrome P450 (CYP) and is a average inhibitor of 2C9 and 3A4. In addition to the observation interactions and mentioned below, there is also the risk of increasing the concentration of other drugs metabolized by CYP2C9, CYP2C19 and CYP3A4 when used simultaneously with fluconazole. Therefore, it is necessary to be careful when using the above drugs with fluconazole and patients should be closely monitored. The enzyme inhibitory effect of Fluconazole lasts 4-5 days after stopping treatment due to fluconazole with long selling time.
Alfentanil: During the same process with Fluconazole (400mg) and Alfentanil (20μg/kg) intravenously in healthy volunteers, Alfentanil AUC10 doubled, can be through CYP3A4 inhibitors. Alfentanil's dose may be adjusted.
Amitriptyline, Nortriptyline: Fluconazole increases the effects of Amitriptyline and Nortriptyline. 5-Nortriptyline and s-amitriptyline can be measured at the beginning of combined therapy and 1 week later. The dose of Amitriptyline/Nortriptyline should be adjusted if necessary.
Amphotericin B: Concomplified use of fluconazole and amphotericin B for mice with normal infections and immunosuppressive inhibitors shows the following results: The slightly increased antifungal effect in body fungal infections with C. albicans, no interaction with intracranial infections caused by Cryptococcus Neoformans, antifugation between fluconazole and amphoticin Aspergillus fumigatus. Unknown clinical significance of the results obtained in these studies.
Anticoneal drugs: The data after the drug is given to the market, as well as with other antifungal drugs, bleeding events (bruises, nosebleeds, gastrointestinal bleeding, bloody urine and black stools) have been reported and increased prothrombin time in patients using fluconazole simultaneously with Warfarin. During simultaneous treatment of fluconazole and warfarin, the prothrombin time is twice, possibly due to the inhibition of warfarin metabolism through CYP2C9. Prothrombin time in patients who are using anticoagulant drugs or Indanedione should be closely monitored. The dose of anticoagulants may be needed.
Benzodiazepine (short effect), such as Midazolam, Triazolam: After simultaneous use of Midazolam, Fluconazole significantly increases Midazolam concentration and influenced the mental mental. Simultaneous use of Fluconazole 200mg and Midazolam 7.5mg oral Midazolam increases AUC Midazolam and the duration of excretion is 3.7 times and 2.2 times. Fluconazole 200mg/day with simultaneous use with triazolam 0.25mg oral road increases auc triazolam and the selling time is 4.4 times and 2.3 times. The enhanced and prolonged effect of triazolam has been observed when used simultaneously with fluconazole. If it is necessary to treat benzodiazepine simultaneously in patients who are being treated with fluconazole, it is necessary to consider reducing benzodiazepine dose and patients need to be monitored appropriately.
carbamazepine: fluconazole inhibits carbamazepine metabolism and increases carbamazepine levels in serum 30%. There is a risk of increasing carbamazepine toxicity.
Carbamazepine dose adjustment may be necessary to depend on the measurement/efficiency level ratio.
Calcium channel blockers: Some antagonists of calcium channels (Nifedipine, Isradipine, Amlodipine, Verapamil and Felodipine) are metabolized by CYP3A4. Fluconazole may increase the concentration of antagonistic drugs in serum. Recommendations regularly control harmful effects.
Celecoxib: When treating Fluconazole (200mg/day) and Celecoxib (200mg), CMAX of Celecoxib increased by 68% and Celecoxib's AUC increased by 134%. Half of Celecoxib is reduced when used in combination.
cyclophosphamide: simultaneously use cyclophosphamide and fluconazole, increasing bilirubin and creatinine in serum. Consider when using Cyclophosphamide and fluconazole combination due to the risk of increased bilirubin and creatinine levels in serum.
Fentanyl: There has been a case of death toxicity of the death of fentanyl may be due to interaction between fentanyl and fluconazole. Moreover, in healthy volunteers shows that Fluconazole slowed down the elimination of fentanyl significantly. High levels of fentanyl can lead to respiratory inhibition. Patients should be closely monitored on the risk of respiratory inhibition. Necessary can adjust the dose of fentanyl.
HMG-CAA Reductase inhibitors: The risk of muscle disease and muscle pattern increases when using Fluconazole simultaneously and HMG-CAA Reductase inhibitors are metabolized through CYP3A4 such as Atorvastatin and Simvastatin or through CYP2C9 as Fluvastatin. If it is necessary to use combination, patients need to be tested for symptoms of muscle disease and muscle pattern, which needs to control the concentration of Creatine Kinase. HMG-CAA Reductase inhibitors should be stopped if observed with increased creatine kinase levels or doubts or diagnosis of muscle disease/muscle pattern.
olaparib: Average CYP3A4 inhibitors like fluconazole increase the concentration of olaparib in plasma, recommended not to be used simultaneously. If the combination is inevitable, limit the dose of olaparib to 200mg x 2 times/day.
ciclosporin: fluconazole significantly increases the concentration and auc of ciclosporin. In the process of simultaneous use of fluconazole 200mg/day and ciclosporin (2.7mg/kg/day) AUC Ciclosporin increased by 1.8 times. Ciclosporin and fluconazole can be used by reducing the dose of ciclosporin depending on the concentration of ciclosporin.
Everolimus: Although not studied in vivo or in vitro, fluconazole may increase the serum concentration of Everolimus through CYP3A4 inhibitors.
Sirolimus: Fluconazole increases the plasma concentration of syrolimus, this is assumed by Fluconazole inhibiting syrolimus metabolism via CYP3A4 and P-Glycoprotein. Fluconazole can be used with syrolimus depends on the effect/concentration of syrolimus.
tacrolimus: Fluconazole increases the concentration of tacrolimus in serum when used orally up to 5 times due to the inhibition of Tacrolimus metabolism through CYP3A4 in the intestine. There is no change in pharmacokinetics that are observed when using intravenous tacrolimus. Increased tacrolimus concentration is related to kidney toxicity. Reduce oral dose of tacrolimus depends on the concentration of tacrolimus.
Losartan: Fluconazole inhibits the metabolism of Losartan into active metabolites (E-31 74), which plays the main role of Angiotensin II receptor receptor when treated with Losartan. Patients need to be tested continuously.
methadone: fluconazole may increase the concentration of methadone in serum. Methadone dose can be adjusted.
Non -steroid anti -inflammatory drugs (NSAID): Flurbiprofen's CMAX increased by 23% and Flurbiproofen's AUC increased by 81% when using Flurbiprofen simultaneously with fluconazole compared to when using Flurbiprofen alone. Similarly, CMAX of the isomers with pharmacological activity [s-(+)-ibuprofen] increased by 15% and the AUC of the isomers with pharmacological activity [S-(+)-ibuprofen] increased by 82% when using Fluconazole and Ibuprofen Racemic (400 mg) compared to IBuprofen Racemic.
Despite no specific studies, Fluconazole has the ability to increase the concentrations of NSAIDs metabolized by CYP2C9 (e.g. Naproxen, Lornoxicam, Meloxicam, Diclofenac). Recommendations to regularly check the harmful effects and toxicity related to NSAIDs. May need to adjust the dose of NSAIDs.
Phenytoin: Fluconazole inhibits metabolism through the liver of phenytoin. Use simultaneously repeat the dose of 200mg fluconazole and 250mg phenytoin intravenously, resulting in an increase in phenytoin AUC24 75% and 128% cmin. When used in combination with fluconazole and phenytoin, it is necessary to closely monitor the serum concentration of phenytoin to avoid the toxicity of phenytoin.
Prednisone: There is a case of reporting a liver transplant patient treated with Prednisone, an acute adrenal impairment occurs when stopping for 3 months with Fluconazole. The stopping of fluconazole probably increases the activity of CYP3A4, thus leading to an increase in Prednisone metabolism. Patients with long -term treatment with fluconazole and prednisone should be closely monitored about the adrenal insufficiency when stopping Fluconazole.
Rifabutin: Fluconazole increases serum rifabutin levels, leading to 80%increase AUC Rifabutin. There have been reports on cases of grape vein inflammation in patients who have used Fluconazole with rifabutin. In combination therapy, it is necessary to consider the toxic symptoms of rifabutin.
Saquinavir: Fluconazole increases the AUC of Saquinavir approximately 50%, increasing CMAX approximately 55% due to the inhibition of metabolism through Saquinavir by CYP3A4 and P-Glycoprotein inhibitors. Interaction with saquinavir/ritonavir has not been studied and may be more noticeable. Saminavir's dose may be needed.
sulfonylurea: Fluconazole extends the serum semi -serum time of sulfonylurea and oral simultaneous oral (e.g. chlorpropamide, glibenclamide, glipizide, tolbutamide) in healthy volunteers. Recommendations for regular blood glucose monitoring and reduced dose of appropriate sulfonylurea when using Fluconazole simultaneously with sulfonylurea.
Theophyllline: In a place where placebuild control control, using Fluconazole dose of 200mg in 14 days reduces 18% of the average plasma clearance rate of theophylline. Therefore, patients being treated with high doses of theophyllline or patients at high risk of theophyllline poisoning should be monitored for signs of theophyllline poisoning while treating with fluconazole. It is necessary to adjust the treatment regimen appropriately if there are signs of poisoning.
alkaloid coconut: Although not yet studied, fluconazole may increase the plasma concentration of shallow coconut alkaloid alkaloids (e.g. vincistine and vinblastine) and lead to neurotoxic toxicity, which can be explained by the CYP3A4 inhibitors of fluconazole.
Vitamin A: Based on a report in a patient with simultaneous use of Fluconazole with transmper of the Retinoid Acid (acid form of vitamin A), unwanted effects related to the central nervous system are developing fake brain tumors. The phenomenon of fake brain tumor disappears when stopping treatment with fluconazole. Fluconazole can be used with vitamin A but should pay attention to unwanted effects related to the central nervous system.
Voriconazole (CYP2C9 inhibitor, CYP2C19 and CYP3A4): simultaneous use of oral voriconazole (400mg, 2 times a day, then 200mg, 2 times for 2.5 days) and Fluconazole oral (400mg on the first day, then 200mg/day for the next 4 days) for 8 healthy male volunteers to show Healthy CMM and AUC levels Voriconazole is 57% (90% CI: 20%, 107%) and 79% (90% CI: 40%, 128%). The dose reduction has not been studied or the frequency of using voriconazole and fluconazole to eliminate this effect. Need to monitor unwanted effects related to voriconazole if using the next voriconazole after fluconazole.
Zidovudine: Fluconazole increases CMAX and AUC of Zidovudine, 84%and 74%respectively, as fluconazole reduces the clearance of zidovudine oral by 45%. The similar half -of -zidovudine waste time also increased by about 128% when the therapy combined with Fluconazole. Patients using this combination therapy should be monitored the appearance of unwanted effects related to zidovudine. May need to consider reducing zidovudine.
Azithromycin: Researching open, random, 3 -dimensional label on 18 healthy volunteers, assessing the effect of the only 1200mg Azithromycin oral dose on the pharmacokinetics of the only dose of 800mg fluconazole, while assessing the effect of fluconazole on the dynamic of azithromycin. The results showed no significant interaction about pharmacokinetics between fluconazole and azithromycin.
Oral contraceptive pills: 2 pharmacokinetic studies with a combined contraceptive pills are performed when using Fluconazole doses. In the study with the dose of fluconazole 50mg does not see the effects related to hormones, while with the dose of Fluconazole 200mg/day, the area under the curve of Ethinyl Estradiol and Levonorgestrel increases, equivalent to 40% and 24%. Therefore, using Fluconazole doses with the above doses does not seem to affect the effectiveness of oral contraceptive pills.
IVACAFTOR: Concentrated with Ivacaftor, the drug increases the potential of regulating protein transmission through cystic membrane (CFTR), increasing the contact level of IVACaftor 3 times and hydroxymethylivacaftor (M1) is 1.9 times. IVACAFTOR dose should be reduced to 150mg x 1 time/day for patients who use simultaneously with medium CYP3A inhibitors, such as fluconazole and erythromycin.
Storage
Store in closed packaging, dry place. The temperature does not exceed 300C.
Other drugs
- ANTEPSIN 1G/5ML ORAL SUSPENSION / SUCRALFATE 1G/5ML ORAL SUSPENSION
- CLAIRETTE 2000/35 TABLETS
- DUSPATALIN 200MG PROLONGED-RELEASE CAPSULES
- IBUCAPS IBUPROFEN 200MG SOFT GELATIN CAPSULES
- K/L POULTICE (KAOLIN POULTICE BP)
- MIFEGYNE COMBIKIT 600 MG / 400 MICROGRAM TABLETS
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