Fluconazole

I got SARS, throat and general condition. It looks like the immune system has gone down.

After taking antibiotics, the thrush worsened. She began to put pimafucin suppositories and drank fluconazole. I developed symptoms of poisoning - weakness, nausea, loose stools, loss of appetite. Will I use fluconazole again in a row?

After taking fluconazole, the middle and index fingers swelled and itch. It is not clear why! Why only these fingers, and not all?

Good evening. fluconazole saw from thrush is a real d ... mo better not to drink it at all, side effects from this medicine, my lip was swollen, and so it’s just impossible to put into words even two fingers on my right hand, it itches a lot and swollen that I can’t bend my fingers.
So before you drink, think about whether it's worth it!!

Good day. After using Fluconazole, after 3 days, I had itching of the skin all over my body. On the 4th or 5th day, she turned to a dermatologist, she prescribed me a hot injection for 5 days, she said it would pass within a month, but alas, after a hot injection, these red reddenings darkened and turned brown (((didn’t know what to do, turned to another dermatologist, she wrote out 10 days of a hot injection, but there were no changes. Since then) More than 1 year has passed and I still can’t get rid of it, because I’m a girl, this is a huge problem for me, and it’s just a disaster. I don’t even know what to do and whom to turn to, for a year I have been suffering with this problem, I tried whitening, but the results are 0%.

Hello! after fluconozol, my face was very swollen and covered with red spots. After that, I'm afraid to take even nystatin.

Hello! I suffer from thrush all the time, recently I was treated with antibiotics for another disease and it immediately worsened. I drank fluconazole at night. I suffered all night, a feeling of anxiety, discomfort .... In the morning I woke up all "rumpled" with swelling on my face. Lips swollen so that it was difficult to talk (((

A few months ago I had a mini-abortion. The deadline was then five weeks. After that, for two days it was a little smeared, and after the discharge they intensified and became brown. Four weeks did not pass. They prescribed me hormones, herbs, fluconazole and a couple more drugs, in addition to this and suppositories with indomethacin. Didn't work for 4 weeks. After that, I drank some more herbs and the cycle seemed to normalize. As for fluconazole, I can say that it helped.

86386-73-4

Characteristics of the substance Fluconazole

An antifungal agent from the group of triazole derivatives.

White or almost crystalline powder white color, odorless, with a characteristic taste, sparingly soluble in water and isopropyl alcohol, sparingly soluble in ethanol and chloroform, soluble in acetone and easily soluble in methanol (isoosmotic infusion solution). Molecular weight 306.3.

Pharmacology

pharmachologic effect- antifungal.

Pharmacodynamics

Capsules, solution for infusion

Fluconazole is a triazole antifungal drug that is a powerful selective inhibitor of sterol synthesis in fungal cells.

Fluconazole has been shown to be active under conditions in vitro and in clinical infections against most of the following organisms: Candida albicans, Candida glabrata(many strains are moderately sensitive), Candida parapsilosis, Candida tropicalis, Cryptococcus neoformans.

Fluconazole has been shown to be active under conditions in vitro against the following microorganisms: Candida dubliniensis, Candida guilliermondii, Candida kefyr, Candida lusitaniae; however, the clinical significance of this is unknown.

When administered orally and intravenously, fluconazole is active in various models of fungal infections in animals. The activity of fluconazole in opportunistic mycoses, incl. caused Candida spp.(including generalized candidiasis in immunosuppressed animals), Cryptococcus neoformans(including intracranial infections), Microsporum spp. And Trychophyton sp..

The activity of fluconazole has also been established in models of endemic mycoses, including infections caused by Blastomyces dermatitidis, Coccidioides immitis(including intracranial infections) and Histoplasma capsulatum in animals with normal and suppressed immunity.

Fluconazole has a high specificity for fungal enzymes dependent on the cytochrome P450 system. Therapy with fluconazole at a dose of 50 mg / day for up to 28 days does not affect the concentration of testosterone in blood plasma in men or the concentration of steroids in blood plasma in women of childbearing age. Fluconazole at a dose of 200-400 mg / day does not have a clinically significant effect on the concentration of endogenous steroids and their response to ACTH stimulation in healthy male volunteers.

Mechanisms of development of resistance to fluconazole. Fluconazole resistance can develop in the following cases: a qualitative or quantitative change in the enzyme that is the target of fluconazole (lanosteryl-14-α-demethylase), a decrease in access to the target of fluconazole, or a combination of these mechanisms.

Point mutations in the ERG11 gene encoding the target enzyme lead to a modification of the target and a decrease in affinity for azoles. An increase in the expression of the ERG11 gene leads to the production of high concentrations of the target enzyme, which creates a need to increase the concentration of fluconazole in the intracellular fluid to suppress all enzyme molecules in the cell.

The second significant mechanism of resistance is the active removal of fluconazole from the intracellular space through the activation of two types of transporters involved in the active removal (efflux) of drugs from the fungal cell. These transporters include the main messenger encoded by multidrug resistance genes. (MDR), and the superfamily of the ATP-binding transporter cassette encoded by fungal resistance genes Candida to azole antimycotics (CDR).

Gene overexpression MDR leads to resistance to fluconazole, while at the same time gene overexpression CDR can lead to resistance to various azoles.

Resistance to candida glabrata usually mediated by gene overexpression CDR leading to resistance to many azoles. For those strains in which the minimum inhibitory concentration is defined as intermediate (16-32 μg / ml), it is recommended to use the maximum dose of fluconazole.

Candida krusei should be considered as resistant to fluconazole. The mechanism of resistance is associated with reduced sensitivity of the target enzyme to the inhibitory effect of fluconazole.

Pharmacokinetics

Capsules, solution for infusion

The pharmacokinetics of fluconazole is similar when administered intravenously and orally. After oral administration, fluconazole is well absorbed, its plasma concentration (and overall bioavailability) exceed 90% of those when administered intravenously. Simultaneous food intake does not affect the absorption of fluconazole. Plasma concentration is proportional to the dose, and T max in plasma is 0.5-1.5 hours after taking fluconazole on an empty stomach, and T 1/2 is about 30 hours. 90% C ss is achieved by the 4-5th day after the start of therapy (with multiple doses of the drug 1 time per day). When taken orally, Tmax is 4 hours.

The use of a loading dose (on the 1st day), 2 times the usual daily dose, makes it possible to achieve 90% C ss by the 2nd day of therapy. V d approaches the total water content in the body. Plasma protein binding is low (11-12%).

Fluconazole penetrates well into all body fluids. The concentration of the agent in saliva and sputum is similar to its concentration in blood plasma. In patients with fungal meningitis, fluconazole concentrations in cerebrospinal fluid make up about 80% of its plasma concentrations.

In the stratum corneum, epidermis, dermis and sweat fluid, high concentrations are achieved that exceed serum levels. Fluconazole accumulates in the stratum corneum. When taken at a dose of 50 mg 1 time per day, the concentration of fluconazole in the stratum corneum after 12 days is 73 mcg / g, and after 7 days after stopping treatment - only 5.8 mcg / g. When used at a dose of 150 mg once a week, the concentration of fluconazole in the stratum corneum on the 7th day is 23.4 mcg / g, and 7 days after the second dose - 7.1 mcg / g.

The concentration of fluconazole in the nail plate after 4 months of use at a dose of 150 mg once a week is 4.05 mcg / g in healthy and 1.8 mcg / g in the affected nail plates, 6 months after completion of therapy, fluconazole is still determined in the nail plates.

The drug is excreted mainly by the kidneys, approximately 80% of the administered dose is found in the urine unchanged. Fluconazole clearance is proportional to creatinine clearance. No circulating metabolites were found.

Long-term T 1/2 from blood plasma allows you to take fluconazole once for vaginal candidiasis and 1 time per day or 1 time per week for other indications.

Pharmacokinetics in selected groups of patients

Capsules solution for infusions

Children. Below are the obtained values of T 1/2 (hours) and AUC (µg·h/ml) depending on the age and dose of fluconazole.

9 months-13 years: once orally 2 mg / kg - 25 hours and 94.7 μg h / ml.

9 months-13 years: once orally 8 mg / kg - 19.5 hours and 362.5 μg h / ml.

Average age 7 years: repeatedly orally 3 mg / kg - 15.5 hours and 41.6 μg h / ml.

11 days-11 months: once in / in 3 mg / kg - 23 hours and 110.1 μg h / ml.

5-15 years: repeatedly in / in 2 mg / kg - 17.4 * h and 67.4 * μg h / ml.

5-15 years: repeatedly in / in 4 mg / kg - 15.2 * h and 139.1 * μg h / ml.

5-15 years: repeatedly in / in 8 mg / kg - 17.6 * h and 196.7 * μg h / ml.

* The indicator noted on the last day.

Premature infants (approximately 28 weeks of development) received fluconazole IV at a dose of 6 mg/kg every 3rd day up to a maximum of 5 doses while the infants remained in the intensive care unit. The average T 1/2 was 74 hours (within 44-185 hours) on the 1st day, with a decrease on the 7th day to an average of 53 hours (within 30-131 hours) and on the 13th day to an average of 47 hours (within 27-68 hours).

The AUC value was 271 µg h/mL (range 173-385 µg h/mL) on day 1, then increased to 490 µg h/mL (range 292-734 µg h/mL) on day 7 and decreased to a mean of 360 µg h/mL (range 167-566 µg h/m k) by the 13th day.

V d was 1183 ml/kg (range 1070-1470 ml/kg) on day 1, then increased to an average of 1184 ml/kg (range 510-2130 ml/kg) on day 7 and to 1328 ml/kg (range 1040-1680 ml/kg) on day 13.

Capsules, solution for infusion

Elderly age. With a single dose of fluconazole at a dose of 50 mg orally in elderly patients 65 years of age and older (some of whom were simultaneously taking diuretics), T max in blood plasma was 1.3 hours after administration and C max - 1.54 μg / ml, the average values of AUC - (76.4 ± 20.3) μg h / ml, and the average T 1/2 - 46.2 hours. macological parameters are higher than in young patients, which is probably due to the reduced renal function characteristic of elderly patients. The simultaneous use of diuretics did not cause a pronounced change in AUC and Cmax in plasma. Cl creatinine (74 ml / min), the percentage of fluconazole excreted by the kidneys unchanged (0-24 h, 22%), and renal clearance of fluconazole (0.124 ml / min / kg) in elderly patients is lower than in young patients.

The use of the substance Fluconazole

Capsules

Treatment of diseases in adults: cryptococcal meningitis; coccidioidomycosis; invasive candidiasis; mucous candidiasis, incl. oropharyngeal candidiasis, esophageal candidiasis, candiduria and chronic mucocutaneous candidiasis; chronic atrophic candidiasis oral cavity(associated with wearing dentures) when oral hygiene or topical treatment is not enough; vaginal candidiasis, acute or recurrent when topical therapy is not applicable; candidal balanitis, when topical therapy is not applicable; dermatomycosis, incl. dermatophytosis of the feet, dermatophytosis of the trunk, inguinal dermatophytosis, multi-colored and cutaneous candidal lichen, when systemic treatment is indicated; dermatophytosis of the nails (onychomycosis), when treatment with other drugs is unacceptable.

Disease prevention in adults: relapse of cryptococcal meningitis in patients at high risk of relapse; recurrence of oropharyngeal candidiasis and esophageal candidiasis in HIV-infected patients with a high risk of relapse; reduction in the frequency of recurrence of vaginal candidiasis (4 or more episodes per year); candidal infections in patients with prolonged neutropenia (such as patients with hemoblastoses undergoing chemotherapy or patients undergoing hematopoietic stem cell transplantation).

Treatment of diseases in children: mucous candidiasis (oropharyngeal candidiasis and esophageal candidiasis); invasive candidiasis; cryptococcal meningitis and prevention of candidal infections in immunocompromised patients. Fluconazole can be used as maintenance therapy to prevent recurrence of cryptococcal meningitis in children at high risk of relapse.

Solution for infusion

Cryptococcosis, including cryptococcal meningitis and infections of other localization (for example, lungs, skin), incl. in patients with a normal immune response and AIDS patients, recipients of transplanted organs and patients with other forms of immunodeficiency, maintenance therapy to prevent recurrence of cryptococcosis in AIDS patients; generalized candidiasis, including candidemia, disseminated candidiasis and other forms of invasive candidal infection, such as infections of the peritoneum, endocardium, eyes, respiratory and urinary tract, incl. in patients with malignant tumors in intensive care units and receiving cytotoxic and immunosuppressive drugs, as well as in patients with other factors predisposing to the development of candidiasis; candidiasis of the mucous membranes, including mucous membranes of the oral cavity and pharynx, esophagus, non-invasive broncho-pulmonary infections, candiduria, mucocutaneous and chronic atrophic candidiasis of the oral cavity (associated with wearing dentures), incl. in patients with normal and suppressed immune function, prevention of recurrence of oropharyngeal candidiasis in patients with AIDS; prevention of fungal infections in patients with malignancies who are predisposed to such infections as a result of cytotoxic chemotherapy, or radiotherapy; mycoses of the skin, including mycoses of the feet, body, inguinal region, pityriasis versicolor, onychomycosis and skin candidal infections; deep endemic mycoses in patients with normal immunity, coccidioidomycosis.

Contraindications

Capsules, solution for infusion

Hypersensitivity to fluconazole, azole compounds with a structure similar to fluconazole; taking terfenadine during repeated use of fluconazole at a dose of 400 mg / day or more (see "Interaction"); simultaneous use with drugs that prolong the QT interval and are metabolized using the CYP3A4 isoenzyme, such as cisapride, astemizole, erythromycin, pimozide and quinidine (see "Interaction").

Application restrictions

Capsules, solution for infusion

Impaired liver function; impaired renal function; the appearance of a skin rash during the use of fluconazole in patients with superficial fungal infection and invasive / systemic fungal infections; simultaneous use of terfenadine and fluconazole at a dose of less than 400 mg / day; potentially proarrhythmic conditions in patients with multiple risk factors (organic heart disease, electrolyte imbalance and concomitant therapy that contributes to the development of such disorders).

Use during pregnancy and lactation

Capsules, solution for infusion

Adequate and well-controlled studies on the use of fluconazole in pregnant women have not been conducted.

Several cases of multiple congenital malformations have been described in newborns whose mothers received high-dose fluconazole therapy (400-800 mg / day) for most or all of the first trimester. The following developmental disorders were noted: brachycephaly, impaired development of the facial part of the skull, impaired formation of the cranial vault, cleft palate, curvature of the femur, thinning and lengthening of the ribs, arthrogryposis and congenital heart defects. Currently, there is no evidence of an association of the listed congenital anomalies with the use of low doses of fluconazole (150 mg once for the treatment of vulvovaginal candidiasis) in the first trimester of pregnancy. The use of fluconazole during pregnancy should be avoided except in cases of severe and potentially life threatening fungal infections when the expected benefit of treatment outweighs the possible risk to the fetus.

Women of childbearing age should use contraception.

Fluconazole is found in breast milk at concentrations close to plasma, so its use in women during breastfeeding is not recommended.

side effects of fluconazole

Capsules, solution for infusion

Fluconazole is generally well tolerated.

In clinical and post-marketing * studies on the use of fluconasol, the following adverse reactions were noted.

From the blood and lymphatic system*: leukopenia, including neutropenia and agranulocytosis, thrombocytopenia, anemia.

From the immune system*: anaphylaxis (including angioedema, swelling of the face, urticaria, pruritus).

From the side of metabolism and nutrition *: increase in the concentration of cholesterol and triglycerides in blood plasma, hypokalemia.

From the side nervous system: headache, dizziness*, convulsions*, taste change*, paresthesia, insomnia, drowsiness, tremor.

From the gastrointestinal tract: abdominal pain, diarrhea, flatulence, nausea, dyspepsia*, vomiting*, dryness of the oral mucosa, constipation.

From the side of the liver and biliary tract: hepatotoxicity, in some cases fatal, increased plasma bilirubin concentration, serum ALT, ACT, alkaline phosphatase, liver dysfunction *, hepatitis *, hepatocellular necrosis *, jaundice *, cholestasis, hepatocellular damage.

From the skin and subcutaneous tissues: skin rash, alopecia*, exfoliative skin lesions* including Stevens-Johnson syndrome and toxic epidermal necrolysis, acute generalized exanthematous pustulosis.

From the side of the heart*: prolongation of the QT interval on the ECG, ventricular tachycardia of the "pirouette" type (see "Precautions").

From the side of the musculoskeletal and connective tissue: myalgia.

General disorders and disorders at the injection site: weakness, asthenia, fatigue, fever, excessive sweating, vertigo.

In some patients, especially those with serious illnesses such as AIDS or cancer, changes in blood counts, kidney and liver function were observed during treatment with fluconazole and similar drugs (see "Precautions"), but the clinical significance of these changes and their relationship to treatment has not been established.

Interaction

Capsules, solution for infusion

Single or multiple use of fluconazole at a dose of 50 mg does not affect the metabolism of phenazone when they are used simultaneously.

Simultaneous use of fluconazole with the following drugs is contraindicated

Cisapride: with the simultaneous use of fluconazole and cisapride, adverse reactions from the heart are possible, incl. ventricular tachycardia of the "pirouette" type. The use of fluconazole at a dose of 200 mg 1 time per day and cisapride at a dose of 20 mg 4 times a day leads to a pronounced increase in plasma concentrations of cisapride and prolongation of the QT interval on the ECG. The simultaneous use of cisapride and fluconazole is contraindicated.

Terfenadine: with the simultaneous use of azole antifungal drugs and terfenadine, serious arrhythmias may occur as a result of prolongation of the QT interval on the ECG. When using fluconazole at a dose of 200 mg / day, the QT interval prolongation on the ECG was not established, however, the use of fluconazole at doses of 400 mg / day and above causes a significant increase in the concentration of terfenadine in blood plasma. The simultaneous use of fluconazole in doses of 400 mg / day or more with terfenadine is contraindicated (see "Contraindications"). Treatment with fluconazole at doses less than 400 mg / day simultaneously with terfenadine should be carried out under close supervision.

Astemizol: the simultaneous use of fluconazole with astemizole or other drugs, the metabolism of which is carried out by the cytochrome P450 system, may be accompanied by an increase in the serum concentrations of these agents. Elevated plasma concentrations of astemizole can lead to a prolongation of the QT interval on the ECG and, in some cases, to the development of ventricular tachycardia of the "pirouette" type. The simultaneous use of astemizole and fluconazole is contraindicated.

Pimozide: in vitro or in vivo, the simultaneous use of fluconazole and pimozide can lead to inhibition of the metabolism of pimozide. In turn, an increase in plasma concentrations of pimozide can lead to a prolongation of the QT interval on the ECG and, in some cases, to the development of ventricular tachycardia of the "pirouette" type. The simultaneous use of pimozide and fluconazole is contraindicated.

Quinidine: despite the fact that no relevant studies have been conducted in vitro or in vivo, the simultaneous use of fluconazole and quinidine can also lead to inhibition of the metabolism of quinidine. The use of quinidine is associated with prolongation of the QT interval on the ECG and, in some cases, with the development of ventricular tachycardia of the "pirouette" type. The simultaneous use of quinidine and fluconazole is contraindicated.

Erythromycin: the simultaneous use of fluconazole and erythromycin potentially leads to an increased risk of developing cardiotoxicity (prolongation of the QT interval on the ECG, ventricular tachycardia of the "pirouette" type) and, as a result, sudden cardiac death. The simultaneous use of fluconazole and erythromycin is contraindicated.

Caution should be exercised and possibly dose adjustments should be made when the following drugs are co-administered with fluconazole

Simultaneously taken drugs that affect fluconazole. Hydrochlorothiazide: repeated use of hydrochlorothiazide simultaneously with fluconazole leads to an increase in the concentration of fluconazole in blood plasma by 40%. The effect of this degree of severity does not require a change in the dosing regimen of fluconazole in patients receiving diuretics at the same time, but the doctor should take this into account.

Rifampicin: the simultaneous use of fluconazole and rifampicin leads to a decrease in the AUC value and the duration of T 1/2 of fluconazole by 25 and 20%, respectively. In patients concomitantly taking rifampicin, it is necessary to consider the advisability of increasing the dose of fluconazole.

Simultaneously taken drugs, which are affected by fluconazole. Fluconazole is a strong isoenzyme inhibitor CYP2C9 And CYP2C19 and a moderate inhibitor of the CYP3A4 isoenzyme. In addition, in addition to the effects listed below, there is a risk of increasing plasma concentrations of other drugs metabolized by isoenzymes CYP2C9, CYP2C19 and CYP3A4 when used concomitantly with fluconazole. In this regard, care should be taken with the simultaneous use of the listed drugs, and if necessary, such combinations, patients should be under close medical supervision. It should be borne in mind that the inhibitory effect of fluconazole persists for 4-5 days after its withdrawal due to the long half-life.

Alfentanil: there is a decrease in clearance and V d , lengthening T 1/2 alfentanil. This may be due to the inhibition of the CYP3A4 isoenzyme by fluconazole. Dose adjustment of alfentanil may be required.

Amitriptyline, nortriptyline: increase in effect. Plasma concentrations of 5-nortriptyline and/or S-amitriptyline can be measured at the start of combination therapy with fluconazole and one week after initiation. If necessary, the dose of amitriptyline/nortriptyline should be adjusted.

Amphotericin B: in studies on mice (including those with immunosuppression), the following results were noted - a small additive antifungal effect in systemic infection caused by candida albicans, lack of interaction in intracranial infection caused by Cryptococcus neoformans, and antagonism in systemic infection caused by Aspergillus fumigatus. The clinical significance of these results is unclear.

Anticoagulants: like other antifungal drugs (azole derivatives), fluconazole, when used simultaneously with warfarin, increases PT (by 12%), and therefore the development of bleeding (hematomas, nasal and gastrointestinal bleeding, hematuria, melena) is possible. In patients receiving coumarin anticoagulants, it is necessary to constantly monitor PV during therapy and for 8 weeks after simultaneous use. The advisability of adjusting the warfarin dose should also be assessed.

Azithromycin: with simultaneous use of oral fluconazole in a single dose of 800 mg with azithromycin in a single dose of 1200 mg, a pronounced pharmacokinetic interaction between both drugs was not established.

Benzodiazepines ( short action): after ingestion of midazolam, fluconazole significantly increases the concentration of midazolam in the blood plasma and psychotropic effects, and this effect is more pronounced after oral administration of fluconazole than when it is administered intravenously. If concomitant benzodiazepine therapy is required, patients taking fluconazole should be monitored to assess the appropriateness of an appropriate dose reduction of the benzodiazepine.

With the simultaneous use of a single dose of triazolam, fluconazole increases triazolam AUC by approximately 50%, C max by 25-32% and T 1/2 by 25-50% due to inhibition of triazolam metabolism. Dose adjustment of triazolam may be necessary.

Carbamazepine: fluconazole inhibits the metabolism of carbamazepine and increases the serum concentration of carbamazepine by 30%. The risk of carbamazepine toxicity must be considered. The need to adjust the dose of carbamazepine depending on the plasma concentration/effect should be assessed.

Nevirapine: co-administration of fluconazole and nevirapine increases the exposure of nevirapine by approximately 100% compared with control data for the separate use of nevirapine. Due to the risk of increased release of nevirapine with concomitant use of drugs, some precautions and careful monitoring of patients are necessary.

BKK: some CCBs (nifedipine, isradipine, amlodipine, verapamil and felodipine) are metabolized by the CYP3A4 isoenzyme. Fluconazole increases the systemic exposure to CCB. It is recommended to control the development of side effects.

Cyclosporine: in patients with a transplanted kidney, the use of fluconazole at a dose of 200 mg / day leads to a slow increase in the concentration of cyclosporine in the blood plasma. However, with repeated use of fluconazole at a dose of 100 mg / day, the change in the concentration of cyclosporine in blood plasma in recipients bone marrow was not observed. With the simultaneous use of fluconazole and cyclosporine, it is recommended to control the concentration of cyclosporine in the blood plasma.

Cyclophosphamide: with the simultaneous use of cyclophosphamide and fluconazole, an increase in serum concentrations of bilirubin and creatinine is noted. This combination is acceptable taking into account the risk of increasing the concentrations of bilirubin and creatinine in the blood plasma.

Fentanyl: there is a report of one fatal outcome, possibly associated with the simultaneous use of fentanyl and fluconazole. It is assumed that the violations are associated with fentanyl intoxication. Fluconazole has been shown to significantly prolong the elimination time of fentanyl. It should be borne in mind that an increase in the concentration of fentanyl in the blood plasma can lead to respiratory depression.

Halofantrine: fluconazole may increase plasma concentrations of halofantrine due to inhibition of the CYP3A4 isoenzyme. With simultaneous use with fluconazole, as with other drugs of the azole series, it is possible to develop arrhythmias - ventricular tachycardia of the "pirouette" type. Therefore, co-administration is not recommended.

HMG-CoA reductase inhibitors: with simultaneous use of fluconazole with HMG-CoA reductase inhibitors metabolized by the CYP3A4 isoenzyme (such as atorvastatin and simvastatin) or isoenzyme CYP2D6(such as fluvastatin), the risk of myopathy and rhabdomyolysis is increased. If simultaneous therapy with these drugs is necessary, patients should be observed in order to identify symptoms of myopathy and rhabdomyolysis. It is necessary to control the concentration of CPK in the blood plasma. In the event of a significant increase in the concentration of CPK in the blood plasma, or the development of myopathy or rhabdomyolysis is diagnosed or suspected, therapy with HMG-CoA reductase inhibitors should be discontinued.

Losartan: fluconazole inhibits the metabolism of losartan to its active metabolite (E-3174), which is responsible for most of the effects associated with angiotensin II receptor antagonism. Regular blood pressure monitoring is required.

Methadone: fluconazole may increase the plasma concentration of methadone. You may need to adjust your methadone dose.

NSAIDs: With max and AUC of flurbiprofen in blood plasma increased by 23 and 81%, respectively. Similarly: Cmax and AUC of the pharmacologically active isomer (S-(+)-ibuprofen) increased by 15% and 82%, respectively, when fluconazole was co-administered with racemic ibuprofen (400 mg).

With the simultaneous use of fluconazole at a dose of 200 mg / day and celecoxib at a dose of 200 mg, C max and AUC of celecoxib in blood plasma increased by 68 and 134%, respectively. In this combination, it is possible to reduce the dose of celecoxib by half.

Despite the lack of targeted studies, fluconazole may increase the systemic exposure of other NSAIDs metabolized by the isoenzyme CYP2C9(eg naproxen, lornoxicam, meloxicam, diclofenac). You may need to adjust the dose of NSAIDs.

With the simultaneous use of NSAIDs and fluconazole, patients should be under close medical supervision in order to identify and control adverse events and manifestations of toxicity associated with NSAIDs.

Oral contraceptives: with the simultaneous use of a combined oral contraceptive with fluconazole at a dose of 50 mg, a significant effect on the concentration of hormones in the blood plasma has not been established, whereas with daily use of 200 mg of fluconazole, the AUC of ethinylestradiol and levonorgestrel in the blood plasma increases by 40 and 24%, respectively, and with the use of 300 mg of fluconazole once a week, the AUC of ethinylestradiol la and norethindrone in plasma increased by 24 and 13%, respectively. Thus, repeated use of fluconazole at the indicated doses is unlikely to affect the effectiveness of the combined oral contraceptive.

Phenytoin: the simultaneous use of fluconazole and phenytoin may be accompanied by a clinically significant increase in the concentration of phenytoin in the blood plasma. If it is necessary to use both drugs simultaneously, the concentration of phenytoin in the blood plasma should be monitored and its dose adjusted accordingly in order to ensure a therapeutic concentration in the blood serum.

Prednisone: there is a report on the development of acute adrenal insufficiency in a patient after liver transplantation against the background of fluconazole withdrawal after a three-month course of therapy. Presumably, the cessation of fluconazole therapy caused an increase in the activity of the CYP3A4 isoenzyme, which led to an acceleration of the metabolism of prednisone. Patients receiving combination therapy with prednisone and fluconazole should be under close medical supervision when fluconazole is discontinued in order to assess the state of the adrenal cortex.

Rifabutin: the simultaneous use of fluconazole and rifabutin can lead to an increase in serum concentrations of the latter up to 80%. With the simultaneous use of fluconazole and rifabutin, cases of uveitis have been described. Patients receiving rifabutin and fluconazole concomitantly should be closely monitored.

Saquinavir: Saquinavir plasma AUC is increased by approximately 50%, C max by 55%, saquinavir clearance is reduced by approximately 50% due to inhibition of hepatic metabolism by the CYP3A4 isoenzyme and inhibition of P-gp. Dose adjustment of saquinavir may be necessary.

Sirolimus: an increase in the concentration of sirolimus in the blood plasma, presumably due to inhibition of the metabolism of sirolimus by the isoenzyme CYP3A4 and P-gp. This combination can be used with appropriate dose adjustment of sirolimus depending on the effect/concentration.

Sulfonylureas derivatives: fluconazole leads to an elongation of T 1/2 of sulfonylurea derivatives (chlorpropamide, glibenclamide, glipizide and tolbutamide) for oral administration. Patients with diabetes you can prescribe the simultaneous use of fluconazole and sulfonylurea derivatives for oral administration, but the possibility of developing hypoglycemia should be taken into account, in addition, regular monitoring of blood glucose is necessary and, if necessary, dose adjustment of sulfonylurea derivatives.

Tacrolimus: the simultaneous use of fluconazole and tacrolimus (orally) leads to an increase in serum concentrations of the latter up to 5 times due to inhibition of the metabolism of tacrolimus, which occurs in the intestine through the CYP3A4 isoenzyme. Significant changes in the pharmacokinetics of drugs were not observed with the use of tacrolimus in / in. Cases of nephrotoxicity have been described. Patients receiving concomitant oral tacrolimus and fluconazole should be closely monitored. The dose of tacrolimus should be adjusted depending on the degree of increase in its concentration in blood plasma.

Theophylline: when used simultaneously with fluconazole at a dose of 200 mg for 14 days, the average plasma clearance rate of theophylline is reduced by 18%. When prescribing fluconazole to patients taking high doses of theophylline, or to patients with an increased risk of developing the toxic effects of theophylline, the appearance of symptoms of theophylline overdose should be monitored and, if necessary, therapy should be adjusted accordingly.

Tofacitinib: exposure to tofacitinib increases with its simultaneous use with drugs that are both moderate inhibitors of the CYP3A4 isoenzyme and strong inhibitors of the isoenzyme CYP2C19(eg fluconazole). Dose adjustment of tofacitinib may be necessary.

Vinca alkaloids: despite the lack of targeted studies, it is assumed that fluconazole can increase the concentration of vinca alkaloids (for example, vincristine and vinblastine) in blood plasma, and thus. lead to neurotoxicity, which may be associated with inhibition of the CYP3A4 isoenzyme.

Vitamin A: there is a report of one case of the development of adverse reactions from the side of the central nervous system in the form of a pseudotumor of the brain with the simultaneous use of all-trans retinoic acid and fluconazole, which disappeared after fluconazole was discontinued. The use of this combination is possible, but one should be aware of the possibility of adverse reactions from the central nervous system.

Zidovudine: when used simultaneously with fluconazole, there is an increase in Cmax and AUC of zidovudine in plasma by 84 and 74%, respectively. This effect is probably due to a slowdown in the metabolism of the latter to its main metabolite. Before and after therapy with fluconazole at a dose of 200 mg / day for 15 days in patients with AIDS and AIDS-associated complex, a significant increase in plasma AUC of zidovudine (20%) was found.

Patients receiving this combination should be monitored for side effects of zidovudine.

Voriconazole (isoenzyme inhibitor CYP2C9, CYP2C19 and CYP3A4): the simultaneous use of voriconazole (400 mg 2 times a day on the first day, then 200 mg 2 times a day for 2.5 days) and fluconazole (400 mg on the first day, then 200 mg / day for 4 days) leads to an increase in Cmax and AUC of voriconazole in plasma by 57 and 79%, respectively. This effect persists with a decrease in the dose and / or a decrease in the frequency of taking any of the drugs. Co-administration of voriconazole and fluconazole is not recommended.

Interaction studies with fluconazole (oral) when taken with food, cimetidine, antacids, and after total body irradiation in preparation for bone marrow transplantation have shown that these factors do not have a clinically significant effect on the absorption of fluconazole.

These interactions have been established with repeated use of fluconazole, interactions with drugs as a result of a single dose of fluconazole are unknown.

Physicians should be aware that the interaction with other drugs has not been specifically studied, but it is possible.

Solution for infusion

Fluconazole in the form of a solution for infusion is compatible with the following solutions: 20% dextrose solution, Ringer's solution, Hartman's solution, potassium chloride solution in dextrose, 4.2% sodium bicarbonate solution, aminofusine, 0.9% sodium chloride solution.

Alcohol and fluconazole are two substances that have a toxic effect on the liver. Yes, and other systems and organs can suffer from such a combination. Or, in extreme cases, treatment of the fungus with fluconazole will not work if alcohol is consumed during this period. So, experimenting with your own health is not worth it. To prove it, read this article.

The effect of fluconazole on the liver The effect of fluconazole and alcohol on brain cells The role of alcohol in the treatment of fungus

Fluconazole is an effective medical antifungal drug that has wide range actions. The work of the agent is directly related to the destruction of biologically active substances necessary for the construction of membranes in the cells of the fungus. Consequently, if there are not enough of these substances, then the vital activity of fungi is disrupted and their cells die.
Fluconazole, like other active medications may be the cause of many side effects. Central to this list is the detrimental effect on liver cells (hepatotoxic effects).

It is noteworthy that the liver suffers from the toxic effect to the greatest extent when there is some kind of disturbance in the functioning of this organ. A healthy liver practically does not feel negative consequences.

Unfortunately, few of the patients are aware of the presence of one or another liver ailment. The reason for this is the absence of symptoms that are noticeable only in advanced cases. The doctor, prescribing an antifungal agent, is obliged to make the patient check the functioning of the liver. In reality, such a procedure is not often done, so the hepatotoxic effect of fluconazole cannot be ruled out.
Violation of liver function, during treatment with this drug, manifests itself in the following form:

Changes in laboratory data (increase in bilirubin in the blood, excessive activity of liver enzymes). The skin and sclera become yellowish. Hepatitis. Necrosis of hepatic cells. All side effects can last both for a short time and have serious consequences, causing irreversible changes in the organ.

The prescription for the drug states that it is forbidden to use other drugs or hepatotoxic substances while taking fluconazole. Of course, alcohol is no exception, since it directly has a toxic effect on liver cells (hepatocytes), destroying and replacing them with fat cells or connective tissue cells. With minor liver ailments, the medicine may not affect in any way, but its combination with alcohol will cause irreparable harm to the organ.

The effect of fluconazole and alcohol on brain cells

Fluconazole can also adversely affect neurons (brain cells). This side effect is rare and manifests itself in the form of:

convulsions; loss of working capacity; fatigue; dizziness; headache.

In case of an overdose, hallucinations and delusions occur.
Alcohol affects brain cells in the same way as it affects hepatocytes. And the combination of alcohol intake with fluconazole treatment will increase the neurotoxic effect several times. Moreover, the induced state is difficult to predict.

The antifungal drug also affects the circulatory system. All this is reflected in the activity of the heart, causing even ventricular flutter and atrial fibrillation.

Alcoholic drinks, especially strong ones, simply expand at first. blood vessels, and then they are sharply narrowed.

Not for nothing that chronic alcoholics have an increase in blood pressure. All this puts a heavy load on the heart and entails various violations of its functions. The combination of alcohol and fluconazole can cause a severe arrhythmia attack.

Ethyl alcohol or alcohol when taken orally is characterized by rapid absorption into the blood and a significant effect on cell metabolism. It breaks everyone's work active substances, important in metabolic processes. And this, in turn, leads to a leveling of the action of fluconazole and a decrease in its effect. Fluconazole is effective drug in the fight against fungal infections. But at the same time, it has a number of side effects, including a detrimental effect on brain and liver cells. To avoid irreversible consequences, drinking alcohol is prohibited during treatment with fluconazole. This is also indicated in the instructions for use of the drug and you should not skip these lines, motivating that fluconazole does not belong to “strong” drugs!

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Fluconazole is a fairly serious antifungal drug that has a number of possible side effects, contraindications and drug interactions. Refers to prescription drugs, i.e. can only be prescribed by a doctor, taking into account individual characteristics patient and disease.

The severity of side effects does not depend on the route of administration of the drug, but on the dose per kg of body weight per day.

It is well absorbed from the intestines (bioavailability over 90%), food intake does not affect absorption. The maximum concentration in the blood appears within an hour after ingestion. Penetrates into all tissues, including the brain. Excreted by the kidneys (mainly). Partially affects hormonal background in men.

High doses of fluconazole negatively affect weight gain in rabbits, increase the frequency of miscarriages. This applies to dosages similar to 20 times the human therapeutic dose. With adequate weight of animal quantities of administered fluconazole, no negative effects on the part of the fetus or mother were identified. The existing negative effects when prescribing high doses are attributed to the moderate effect of the drug on the hormonal background.

Pregnancy

Fluconazole is indicated for pregnant women only for severe infections that threaten the life of the mother and / or fetus. Only the attending physician can take responsibility, with a clear comparison of the risks and the intended effect. There are no direct studies of the use of fluconazole in pregnant and lactating women.

There is evidence of developmental abnormalities in children whose mothers were treated with sufficiently high doses of the drug (for severe fungal diseases), although a direct connection between these facts has not been proven. According to FDA standards, the risk of exposure to the fetus is rated as C, i.e. conjectural.

During maternal therapy breast-feeding should be terminated, because fluconazole is found in breast milk in the same concentrations as in the blood (as already mentioned, it penetrates perfectly into all liquids).

Side effects of the remedy

In the United States, a fairly serious study was conducted on 448 patients who took fluconazole at a standard therapeutic dosage, i.e. 150 mg once for the treatment of vaginal candidiasis (thrush). Every fourth person on the background of taking the drug experienced the following side effects:

13% headache; 7% nausea; 6% abdominal pain; 3% diarrhea; 1% dyspepsia; 1% dizziness; 1% violation of taste perception.

The rest felt some poorly differentiated negative sensations. In rare cases, fluconazole causes a pronounced allergic reaction.

In a larger study (4048 patients), a complication rate was observed when fluconazole was combined with other drugs and diseases. Worst of all, fluconazole was combined with cytostatics in patients with HIV. The main side effects were the same as in the first group of subjects.

Sometimes fluconazole causes serious complications from the liver, up to death. When the drug is discontinued, the symptoms of liver damage subside. For this reason, with long-term treatment with fluconazole, the doctor should periodically prescribe liver tests (AST, ALT, etc.).

In severe cases, the hepatotoxic effect manifests itself in the form of hepatitis, impaired bile outflow (cholestasis), and acute liver failure. All these sad outcomes were observed mainly in patients with HIV, malignant neoplasms, and severe forms of tuberculosis.

Perhaps this is due to the parallel use of heavy specific antibiotics: isoniazid, rifampicin, phenytoin, pyrazinamide.

A side effect differs from a side effect in that the relationship of what happened with the intake of a particular drug has not been proven. Nevertheless, manufacturing companies are required to record everything that happens to the patient (control group) during treatment, and include this in the instructions:

convulsions; Skin rash, Stevenas-Johnson syndrome, toxic injury skin (epidermal necrolysis); Exfoliative dermatitis in patients with AIDS and malignant tumors; Violation of the composition of the cellular elements of the blood: leukopenia (decrease in the number of leukocytes), thrombocytopenia (decrease in the number of platelets);

Cholesterol increase

Violation of fat metabolism: increased cholesterol (hypercholesterolemia), triglycerides;

Decreased potassium levels.

The studies were conducted in the USA and Europe, they included 577 children from one day old to 17 years old inclusive. The dosage for all was 15 mg/kg body weight/day for an extended period. In total, side effects were detected in 13% of cases:

5.4% vomiting; 2.8% abdominal pain; 2.3% nausea; 2.1% diarrhea.

In 2.3%, treatment was discontinued due to severe side effects.

The drug may be harmful in the following conditions

Overdose and first aid

The main symptoms: diarrhea, nausea up to vomiting, there may be convulsions.

Skin rashes

Treatment: gastric lavage with parallel administration of diuretics. Hospitalization is required. The admitted patient is sent for a three-hour hemodialysis (allows you to reduce the concentration of the drug by almost 50%), otherwise the doctors act according to the circumstances, depending on the type of interaction. As a rule, this situation occurs in elderly patients with a large number of concomitant appointments.

There is information about one patient who, with an overdose of fluconazole, gave a clinic of paranoid delusions and hallucinations. Given that this was a 42-year-old HIV patient (drug addict), such side effects can not be classified as typical for an overdose.

If you or your loved ones have been prescribed fluconazole for a long course, try to eliminate the risk of drug interactions, listen carefully to the recommendations of your doctor, and do not drink alcohol during this period. Particular attention should be paid to elderly relatives who take many different drugs at the same time, since this significantly increases the risk of side effects while taking fluconazole.

Physician-therapist of the city polyclinic. Eight years ago she graduated from the Tver State Medical University with honors.

Antifungal agent Fluconazole is a synthetic antimycotic, belongs to the group of triazole derivatives. The action of the drug is based on the inhibition of fungal cytochrome P450 enzymes.

In humans, fluconazole inhibits the CYP2C9 enzyme of cytochrome P450, which is involved in the metabolism of anticoagulants, drugs that reduce blood clotting and prevent the formation of blood clots.

Fluconazole does not suppress the main group of cytochrome P450-dependent enzymes in humans, which makes it safer for the liver than antifungal agents of other classes.

The antimycotic Fluconazole is used in the treatment of a wide range of fungal diseases, it is used in the treatment of:

candidiasis - skin, genitals, oral cavity, lungs; microsporia; trichophytosis; blastomycosis.

An antifungal agent is prescribed for antibiotic treatment, chemotherapy, organ transplantation to prevent fungal diseases.

The drug is available in tablets, capsules, powders for injection. When taking capsules, the maximum concentration in the blood is created after 1.5 hours. The time during which the concentration of Fluconazole in the blood plasma decreases by 2 times is 30 hours.

The antimycotic easily penetrates into all body fluids and is maintained at a therapeutic dose throughout the day. The drug is found in saliva, breast milk, cerebrospinal fluid, sputum, vaginal secretions, sweat fluid.

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The drug is excreted from the body by the kidneys, the duration of the half-life depends on their functional state. With renal failure, the excretion of the drug slows down.

The absolute contraindication of antimycotics is allergy to the drug, breastfeeding, age up to 4 years. With caution appoint it to the elderly, people suffering from renal failure, liver disease, during pregnancy.

A relative contraindication is the simultaneous use of drugs with a hepatotoxic effect and alcohol. In this case, when prescribing a medicine, the possible benefit or harm that it can have on human health is evaluated.

The most pronounced side effects are observed from the side digestive tract. Taking an antifungal causes:

pain in the stomach; nausea, vomiting; taste perversion, lack of appetite; jaundice, hepatonecrosis.

Fluconazole causes disturbances in the functions of the nervous system. Long-term treatment with this antifungal agent can cause dizziness, fatigue, convulsions, and in case of an overdose, hallucinations, behavioral changes.

Dangerous changes occur with an adverse reaction of the body to Fluconazole from the heart. There are changes in the cardiogram (prolongation of the Q-T interval), atrial fibrillation. Less commonly, there is a decrease in potassium in the blood, damage to the hematopoietic system, kidneys.

On the video information about the drug Fluconazole:

The danger of the compatibility of Fluconazole and ethyl alcohol lies in their effect on the liver and heart. Simultaneous administration of the drug and ethanol can cause severe allergic reactions - anaphylactic shock, angioedema.

In addition, if you take alcohol together with Fluconazole, there may be disturbances in the function of the organs of balance with the development of true vertigo, a disease in which dizziness can last for several hours.

Alcohol, like an antimycotic, adversely affects the electrocardiogram (ECG). These toxic compounds, when used together, amend the ECG, threatening sudden death.

One of the possible side effects of taking fluconazole is the lengthening of the Q-T interval on the ECG. Alcohol, especially with prolonged abuse, causes a similar ECG change.

The cardiotoxic effect of fluconazole and ethanol is manifested by dizziness, loss of consciousness. The asymptomatic course of this disorder is especially dangerous. With a latent, asymptomatic form of the course of the interval lengthening syndrome Q-T risk sudden death increases.

Both alcohol and Fluconazole have a toxic effect on the liver, cause an increase in the blood levels of bilirubin, a breakdown product of red blood cells.

Impaired liver function is accompanied by:

yellowing skin, white of the eye; darkening of urine, feces; irritability, weakness; drowsiness, fainting.

Like alcohol, fluconazole can increase the level of the liver enzyme alkaline phosphatase, causing nausea, abdominal pain, and fever.

The use of antifungals and alcohol affects the liver in a similar way:

activates the enzymes alanine aminotransferase, aspartate aminotransferase; increases the risk of liver failure.

The most likely consequence of the simultaneous interaction of fluconazole and alcohol is hepatonecrosis of the liver. Moreover, alcohol itself will change the effect of the drug on the body.

The most dangerous changes in cardiac activity for health are:

violation of the rhythm of the heartbeat; ischemia of the heart; heart attack.

Most dangerous consequences taking a drug and a large dose of alcohol - cirrhosis of the liver, sudden death due to cardiac arrest.

Doctors note that even small doses of alcohol should not be drunk when taking antimycotics. The substances are not compatible with each other. But is it possible to drink alcohol 30 hours after Fluconazole, at the end of the half-life of the drug?

In this case, it must be remembered that the half-life corresponds to a halving of the therapeutic concentration, and not to the complete elimination of the drug from the body.

With liver failure, in old age, this antimycotic remains in the body for a long time, which is taken into account when prescribing the dosage - it is reduced in this case by 2 times.

A certain amount of Fluconazole is present in the blood plasma even after 30 hours. And with concomitant kidney diseases, the half-life interval itself may increase.

So how long can you drink alcohol? In order for the body to be completely cleared of Fluconazole, 3 days or more must pass if the patient has kidney disease. The trace content of this antimycotic can be detected within 5 days.

You can drink alcohol after fluconazole no earlier than 3 days later. It is advisable to extend this period to 5 days to enable the liver and kidneys to completely rid the body of the presence of antimycotics.

Category:

Or, in extreme cases, treatment of the fungus with fluconazole will not work if alcohol is consumed during this period. So, experimenting with your own health is not worth it. To prove it, read this article.

Effects of fluconazole on the liver

Fluconazole is an effective medical antifungal drug that has a wide spectrum of action. The work of the agent is directly related to the destruction of biologically active substances necessary for the construction of membranes in the cells of the fungus. Consequently, if there are not enough of these substances, then the vital activity of fungi is disrupted and their cells die.

Fluconazole, like other active drugs, can cause many side effects. Central to this list is the detrimental effect on liver cells (hepatotoxic effects).

It is noteworthy that the liver suffers from the toxic effect to the greatest extent when there is some kind of disturbance in the functioning of this organ. A healthy liver practically does not feel negative consequences.

Violation of liver function, during treatment with this drug, manifests itself in the following form:

Changes in laboratory data (increase in bilirubin in the blood, excessive activity of liver enzymes).
The skin and sclera become yellowish.
Hepatitis.
Necrosis of hepatic cells.
All side effects can last either for a short time or have serious consequences, causing irreversible changes in the organ.

Double damage to the liver

The effect of fluconazole and alcohol on brain cells

Fluconazole can also adversely affect neurons (brain cells). This side effect is rare and manifests itself in the form of:

In case of an overdose, hallucinations and delusions occur.

Alcohol affects brain cells in the same way as it affects hepatocytes. And the combination of alcohol intake with fluconazole treatment will increase the neurotoxic effect several times. Moreover, the induced state is difficult to predict.

Harm to other organs and tissues

The antifungal drug also affects the circulatory system. All this is reflected in the activity of the heart, causing even ventricular flutter and atrial fibrillation.

Alcoholic drinks, especially strong ones, at first simply expand the blood vessels, and then narrow them sharply.

The role of alcohol in the treatment of fungus

Ethyl alcohol or alcohol when taken orally is characterized by rapid absorption into the blood and a significant effect on cell metabolism. This disrupts the work of all active substances important in metabolic processes. And this, in turn, leads to a leveling of the action of fluconazole and a decrease in its effect. Fluconazole is an effective drug in the fight against fungal infections. But at the same time, it has a number of side effects, including a detrimental effect on brain and liver cells. To avoid irreversible consequences, drinking alcohol is prohibited during treatment with fluconazole. This is also indicated in the instructions for use of the drug and you should not skip these lines, motivating that fluconazole does not belong to “strong” drugs!

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If the disease has a recurrent form (if thrush manifests itself more than once every three months), then it is necessary to take one hundred milligrams of fluconazole once every seven days for a sufficiently long time. This will prevent the return of the disease. But more precisely, the duration of the course of treatment can only be prescribed by the attending physician on the basis of periodic tests that will need to be taken during the treatment process.

This drug is not used in the treatment of persons under the age of sixteen.

The work of organs that produce blood can also be disrupted. This is expressed in thrombocytopenia, leukopenia, agranulocytosis, neutropenia.

Often, drug treatment causes allergic manifestations, such as urticaria, very rarely different types exudative erythema, Lyell's syndrome, in isolated cases, anaphylactic manifestations.

An overdose of the drug should not be allowed. This can provoke visions and paranoid states. In case of an overdose, you need to do a gastric lavage, as well as drink a diuretic. For three hours, hemodialysis can also help.

Fluconazole should not be used without the advice of a physician or other physician.

For the treatment of oral candidiasis caused by dentures, fifty milligrams should be taken once a day for two weeks in combination with other drugs.

For the treatment of balanitis provoked by Candida, take one hundred and fifty milligrams of fluconazole orally once.

In the process of taking the drug, you should periodically take a blood test, as well as special samples that reflect the functioning of the liver and kidneys. If the samples show signs of deterioration in this work, you should immediately stop using the medicine.

If urticaria appears during use against the background of suppressed immunity, you need to constantly be under the supervision of a doctor. Since if the rash worsens, the drug should be stopped in order to avoid the appearance of Layell's syndrome or Steven-Johnson's syndrome.

Fluconazole is used to prevent cryptococcal complications in people with AIDS.

It is used for candidiasis of the mucous membranes of the mouth, digestive organs, pharynx, bronchi, candiduria, as well as for candidiasis provoked by the use of dentures.

Effective in genital candidiasis: balanitis and vaginal candidiasis in acute form, as well as in recurrent form.

It is used in the treatment of fungal infections of the feet, groin, onychomycosis, skin diseases provoked by candida, pityriasis versicolor, as well as endemic mycoses of deep penetration (sporotrichosis, coccidioidomycosis, histoplasmosis) that develop in patients who do not suffer from impaired immune response.

Sometimes children of the first year of life suffer candiduria. The methods of treatment of this disease in children of the first year of life until today included the intravenous use of certain drugs, as well as surgical intervention and irrigation of the urinary organs. These methods of treatment are very difficult to carry out in a child at a similar age, and for their implementation it is necessary for the baby to be in the hospital for quite a long time.

A month later from the start of treatment, the kids passed the tests, in which candida were not detected. At the same time, no severe side effects of the drug were found in any baby. Scientists are planning a number of studies of the drug with the participation of infants.

One capsule contains fifty, one hundred, one hundred and fifty and two hundred milligrams active substance.

Up to ninety percent of the drug is not processed by the body, but absorbed into the blood and all biologically active fluids. Approximately twelve percent of the drug interacts with blood proteins. It is prescribed for systemic fungal infections. It is not recommended to use in the treatment of babies under the age of six.

Indications for use of all fluconazole analogues are the same. Side effects and contraindications also do not differ.

Fluconazole tablets are intended for the treatment of fungal infections that affect the entire body.

The dosage of the drug depends on the severity of the disease. A drug is also prescribed to prevent the development of fungal infections in case of a violation of the immune system (for example, with AIDS, after treatment oncological diseases immunosuppressive drugs). The duration of the course of taking fluconazole tablets is prescribed only by the attending physician. In addition, you should not independently prolong the course of treatment or increase the dose, as severe consequences associated with an overdose are possible.

In a carton pack one blister containing ten tablets. They can only be used for four years from the date of issue. And you need to store in a dark place, away from a heat source, at room temperature. The first aid kit should not be directly accessible to babies.

In pharmacies, the drug is sold only on the special prescription of a doctor.

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I want to know about 4-5 weeks of pregnancy, I took fluconazole daily.

How is fluconazole used for stomatitis in a child?

How to use fluconazole for thrush in a child?

Hello! I am 21 years old. My husband and I have been planning a child for a long time. And here it is.

How should I take fluconazole: before or after food?

About 2 days ago, strange symptoms appeared in the urethra.

The doctor prescribed me and my husband flucanose 150 mg once. We drank one.

Hello! A 5-year-old child, weight 18 kg, diagnosed with lacunar tonsillitis, was vaccinated.

I am 29 years old. During pregnancy, thrush appeared. cured .. gave birth.

Good afternoon Whether it is possible to accept this preparation Diflucan (Flukanozol) opening.

Side effects of fluconazole

The side effects of fluconazole range from mild to severe. The most common are mild side effects such as headache and abdominal pain. Serious side effects may include cramps, fever, and blistering of the skin. An allergic reaction is the most severe potential side effect of fluconazole and requires immediate medical attention.

Fluconazole is an antibiotic. It is prescribed for fungal infections and is used to treat infections throughout the body, including the mouth, lungs, bladder and blood. Fluconazole is sold trade name Diflucan ® (Diflucan ®).

The most common side effects of fluconazole are among the mildest. Such side effects include headache, abdominal pain, heartburn and diarrhea. Some patients experience bad taste in the mouth or experience different taste sensations while eating food. Other side effects include dizziness, itching, and vomiting. These problems usually go away gradually, and if they persist or become more serious, you should tell your doctor.

Some of the more severe side effects of fluconazole include flu-like symptoms, seizures, fever, and chills.

Patients may also experience loss of appetite, pain in the right upper abdomen, and nausea. Fluconazole can cause severe fatigue, weakness, or lack of energy in some people. This drug can also cause dark urine or pale or brown stools.

Other serious side effects of fluconazole affect the skin. These side effects include blistering, peeling skin, rashes, and easy bruising or bleeding. Patients who experience any of these side effects of this drug should tell their doctor as soon as possible. Allergic reactions, which may include swelling above the neck, hives, or difficulty breathing, require immediate medical attention.

Fluconazole is taken either in liquid or tablet form, usually once a day, although the dose may depend on the type of infection requiring treatment.

You should not take the drug in doses exceeding those prescribed by your doctor. If an overdose occurs, the most common symptoms are an intense fear of harming other people and hallucinations, in particular auditory hallucinations and seeing objects that do not exist.

There are several diseases that should be reported to the doctor before starting treatment with fluconazole, as they can make taking this drug too risky. Such conditions include any heart rhythm disorder, liver or kidney disease, and a family or personal history of long QT syndrome, a rare hereditary disease hearts. It is also important to report alcohol abuse, acquired immunodeficiency syndrome (AIDS) and any type of cancer.

say fluconazole pills are very harmful. they seem to either affect the kidneys or the liver better than diflucan, mycomax, etc.

All the drugs you mentioned contain the same active ingredient fluconazole. Accordingly, choose what you can afford and the most convenient form for you. In my opinion, local effects (candles) are more effective for vaginal candidiasis ...

Flucostat is also a drug of fluconazole. .

It is also necessary to take into account the dosage of the drug, sometimes analogues are produced with a higher dosage ...

The easiest way is to buy something that is cheaper (choose from analogues or buy a generic) in vaginal suppositories. .

The difference between a generic and analogues is only in the form of release, monetary policy and production technology, but in any case, the original product must meet quality standards. So there isn't much of a difference.

In listed by you operating in-in one: flukonazol. But it is Diflucan and Mycomax that are imported. Toxic effect is reduced to a minimum.

Fluconazole costs 60 rubles, and flucostat, diflucan, etc., more than 200.

When "Fluconazole" can harm: side effects and contraindications

Fluconazole is a rather serious antifungal drug that has a number of possible side effects, contraindications and drug interactions. Refers to prescription drugs, i.e. can only be prescribed by a doctor, taking into account the individual characteristics of the patient and the disease.

The severity of side effects does not depend on the route of administration of the drug, but on the dose per kg of body weight per day.

Pharmacokinetic properties of fluconazole

Studies of the effect of the drug on pregnant women

High doses of fluconazole negatively affect weight gain in rabbits, increase the frequency of miscarriages. This applies to dosages similar to 20 times the human therapeutic dose. With adequate weight of animal quantities of administered fluconazole, no negative effects on the part of the fetus or mother were identified. The existing negative effects when prescribing high doses are attributed to the moderate effect of the drug on the hormonal background.

Fluconazole is indicated for pregnant women only for severe infections that threaten the life of the mother and / or fetus. Only the attending physician can take responsibility, with a clear comparison of the risks and the intended effect. There are no direct studies of the use of fluconazole in pregnant and lactating women.

During therapy of the mother, breastfeeding should be discontinued, because. fluconazole is found in breast milk in the same concentrations as in the blood (as already mentioned, it penetrates perfectly into all liquids).

Direct contraindications to the appointment

Individual intolerance to the active substance or components of the dosage form;
Simultaneous appointment with terfenadine;
Combination with quinidine, cisapride, astemizole.

Side effects of the remedy

13% headache;
7% nausea;
6% abdominal pain;
3% diarrhea;
1% dyspepsia;
1% dizziness;
1% violation of taste perception.

The rest felt some poorly differentiated negative sensations. In rare cases, fluconazole causes a pronounced allergic reaction.

Effect of fluconazole on the liver (hepatotoxicity)

Perhaps this is due to the parallel use of heavy specific antibiotics: isoniazid, rifampicin, phenytoin, pyrazinamide.

Side effects sometimes observed while taking the drug

convulsions;
Skin rashes, Stevenas-Johnson syndrome, toxic skin lesions (epidermal necrolysis);
Exfoliative dermatitis in patients with AIDS and malignant tumors;
Violation of the composition of the cellular elements of the blood: leukopenia (decrease in the number of leukocytes), thrombocytopenia (decrease in the number of platelets);
Cholesterol increase

Violation of fat metabolism: increased cholesterol (hypercholesterolemia), triglycerides;

Side effects from taking fluconazole in children

In 2.3%, treatment was discontinued due to severe side effects.

Instructions for use of Fluconazole tablets - composition, indications, side effects, analogues and price

Doctors prescribe Fluconazole tablets for manifestations of fungal diseases: tonsillitis, lichen, infections related to gynecology, mycoses and other ailments. When using the medication, you must carefully follow the instructions for use, follow the dosage, familiarize yourself with the contraindications in order to avoid the occurrence of unwanted side effects.

fluconazole tablets

The drug for fighting fungi can be purchased in the form of tablets, capsules and solution. Fluconazole pills help to cope with the pathogenic influence of microorganisms, to prevent fungal infections. Tablets have several dosage options, which makes them more convenient to take. You can buy medicine if necessary without a doctor's prescription.

Compound

The drug is released in the form of tablets having a convex shape, white or yellowish color. The composition of each pill can be considered in the table:

Fluconazole (150, 100, 50 mg)

colloidal silicon dioxide

Pharmacological properties

The instructions for use say that Fluconazole is an inhibitor of the specific synthesis of sterols in fungal cells. Medicine belongs to the class of triazole compounds. The active substance is active against microorganisms of the Candida species, pathogens of endemic mycoses, cryptococci. A specific effect of the drug on fungal enzymes dependent on cytochrome P450 was revealed. The drug inhibits the transformation of fungal cells into ergosterol lanosterol.

What is fluconazole for?

The active substance fluconazole is effective against a number of fungal diseases. Tablets have the following indications for use:

fungal meningitis caused by microorganisms of the genus Cryptococcus;
vaginal candidiasis in acute or recurrent form;
mycoses of the skin (groin, feet, torso);
fungal nail infections;
candidal balanitis;
oral candidiasis;
mucous candidiasis (oropharyngeal, mucocutaneous, esophageal fungus, candiduria);
invasive candidiasis;
multi-colored lichen;
prevention of fungal infections in patients with malignant neoplasms undergoing radiation or chemotherapy;
skin candidiasis;
prevention of infection caused by cryptococci in AIDS patients.

Method of application and dosage

Fluconazole tablets should be swallowed whole with a small amount of water. A suitable dosage is calculated based on the type of fungus, the severity of the infection. Instructions for use indicate the following conditions:

Patients with candidemia and disseminated candidiasis are shown 400 mg on the first day, then the dose is reduced to 200 mg. For the treatment of children's generalized candidiasis, a daily intake of 6-12 mg of the drug per 1 kg of the child's weight is prescribed.
Therapy of the oropharyngeal form of candidiasis is carried out for 1-12 weeks. It is shown to take daily from 50 to 100 mg of the drug.
Patients with atrophic candidiasis of the oral mucosa should drink 50 mg / day. Treatment is carried out days.
For the prevention of oropharyngeal candidiasis in patients with immunodeficiency, it is necessary to use 150 mg of Fluconazole weekly.
With cryptococcal meningitis and other infections caused by this pathogen, pomg is prescribed daily. The duration of therapy is 1.5-2 months.
infectious skin diseases treated with a weekly dose of the drug at a dose of 150 mg. The course is 2-4 weeks, with foot fungus, its period for men and women can be extended to 1.5 months.
Patients with pityriasis versicolor are shown 300 mg / week. The therapy lasts 14 days.
Reception schedule for nail fungus: 150 mg / week. Treatment must be completed when a healthy plate completely replaces the affected one.
Therapy of vaginal candidiasis involves a single use of a tablet, a dosage of 150 mg. For prevention chronic thrush it is required to drink a similar dose of the drug at intervals of 1 time / month.

special instructions

Treatment with fluconazole tablets is allowed to start in the absence of laboratory tests. It is necessary to continue therapy until the appearance of clinical and hematological remission. If treatment is stopped prematurely, relapses may occur. The active substance of the drug is excreted by the kidneys, therefore, when used in patients with insufficiency, it is recommended to take precautions.

There are rare cases when the use of the drug led to toxic changes in the liver. In patients with serious comorbidities, a lethal outcome was observed. In most cases, the hepatotoxic effect is reversible, its symptoms disappear after discontinuation of the drug. If an allergic rash occurs in patients with HIV, it is necessary to urgently stop taking Fluconazole. If rashes appear in patients with invasive or systemic fungal infections, observation is necessary, drug withdrawal with the development of erythema multiforme, bullous changes.

Patients suffering from diseases of the liver, heart, kidneys should consult a doctor before using Fluconazole. Before treating thrush with a single dose of medication, a woman should be warned that the symptoms of the disease are reduced in the first 24 hours. The full therapeutic effect occurs in a few days. If during this time the symptoms of thrush have not disappeared, an appeal to a gynecologist is required.

During pregnancy

Controlled studies on the use of fluconazole tablets in pregnant women have not been conducted. There is a description of several cases when, when using high doses of the drug by the mother in the first trimester of gestation, developmental disorders were detected in the fetus. The following Negative consequences: failures in the formation of the skull in the front part, curvature of the bones of the thighs, congenital heart defects, brachycephaly, cleft palate, arthrogryposis. Data on anomalies in the development of the child with the use of low doses of Fluconazole is not registered.

The drug is not prescribed during pregnancy, except in cases where the fungal infection is life-threatening, difficult to tolerate, and also if the benefit of the drug to the mother outweighs the risk to the fetus. The appointment of the drug during lactation is contraindicated, since its concentration in breast milk is similar to the content of the active substance in the blood plasma. Under such conditions, the child may experience unwanted side effects.

Interaction with drugs

Fluconazole is able to react with some medications. Simultaneous use with other drugs can cause the following consequences:

Sharing with Cisapride is contraindicated, since the risk of developing ventricular tachysystolic arrhythmia is high.
Taking the antibiotic Erythromycin together with fluconazole leads to cardiotoxicity, sudden cardiac death.
The combination with Warfarin increases the prothrombin time of the antifungal drug.
The likelihood of hypoglycemia increases with the interaction of the active substance of the tablets and sulfonylurea derivatives.
Increase the concentration of fluconazole in the blood can be its repeated combined use with hydrochlorothiazide.
When interacting with Rifampicin, the physician should consider the possibility of increasing the dose of antifungal tablets, since the duration of the half-life of the active substance decreases.
Simultaneous administration of Fluconazole with Terfenadine, Astemizol, Pimozide, Quinidine is contraindicated due to the risk of tachysystolic ventricular arrhythmia.
If the drug is combined with Cyclosporine, it is recommended to control the content of the latter in the patient's blood.
Fluconazole with prolonged use can provoke a decrease in the clearance rate of Theophylline, so it is necessary to monitor the appearance of possible symptoms of an overdose.
The combination of an antifungal drug and Zidovudine increases the side effects of the latter.

Fluconazole

The use of fluconazole

Antifungal drug. Effectively suppresses the vital activity of many types of fungi, including those with malignant neoplasms. Released according to the recipe.

Diseases for which fluconazole is used

Generalized candidiasis.
Cryptococcosis. Including as part of maintenance therapy in the treatment of AIDS.
Mucosal candidiasis.
Prevention of fungal infections in malignant neoplasms.
Genital candidiasis. Treatment and prevention to reduce the risk of relapse.
Deep endemic mycosis, paracoccidioidomycosis, coccidioidomycosis, histoplasmosis, sporotrichosis.
Skin fungal infections.

Varieties of fluconazole

side effects of fluconazole

Nervous system. Convulsions, dizziness, headache.
Digestive system. Nausea, vomiting, pain in the stomach, dyspepsia, flatulence, diarrhea, digestive disorders.
Skin covers. Hyperemia, rash, toxic epidermal necrolysis, alopecia, Stevens-Johnson syndrome.
The cardiovascular system. Paroxysmal ventricular tachycardia, prolongation of the QT interval.
Hematopoietic system. Granulocytosis, neutropenia, leukopenia, thrombocytopenia.
Liver and gallbladder. Liver failure, toxic liver damage, hepatocellular necrosis, hepatitis, jaundice, increased levels of aspartate aminotransferase, alkaline phosphatase, alanine aminotransferase, bilirubin.
Others. Hypertriglyceridemia, hypercholesterolemia, taste deterioration, hypokalemia.

Fluconazole contraindications

Age up to 5 years (for injections - up to 16 years).
Increased sensitivity.
Pregnancy, lactation.
Simultaneous reception of terfenadine (with a dosage of fluconazole more than 400 mg / day) and cisapride.

Taking with extra care:

Violation of the digestibility of lactose.
Simultaneous reception of terfenadine (at a dosage of fluconazole more than 400 mg / day, the combination with terfenadine is contraindicated).
Elevated levels of liver enzymes.
Renal failure.

fluconazole during pregnancy

During pregnancy, taking the drug is permissible only if the benefit from it outweighs the potential harm to the fetus. Fluconazole passes into breast milk. If necessary, treatment during lactation is recommended to refuse breastfeeding.

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The severity of side effects does not depend on the route of administration of the drug, but on the dose per kg of body weight per day.

Pharmacokinetic properties of fluconazole

Studies of the effect of the drug on pregnant women

Direct contraindications to the appointment

Individual intolerance to the active substance or components of the dosage form;
Simultaneous appointment with terfenadine;
Combination with quinidine, cisapride, astemizole.

Side effects of the remedy

13% headache;
7% nausea;
6% abdominal pain;
3% diarrhea;
1% dyspepsia;
1% dizziness;
1% violation of taste perception.

The rest felt some poorly differentiated negative sensations. In rare cases, fluconazole causes a pronounced allergic reaction.

Effect of fluconazole on the liver (hepatotoxicity)

Perhaps this is due to the parallel use of heavy specific antibiotics: isoniazid, rifampicin, phenytoin, pyrazinamide.

Side effects sometimes observed while taking the drug

Side effects from taking fluconazole in children

5.4% vomiting;
2.8% abdominal pain;
2.3% nausea;
2.1% diarrhea.

In 2.3%, treatment was discontinued due to severe side effects.

Interaction with other drugs

Increases the half-life of sugar-lowering tablets (based on sulfonylurea), which can lead to hypoglycemia. Those. with diabetes insipidus of the elderly - hypoglycemic drugs act much more strongly;
Slows down the elimination of theophylline and zidovudine, saquinavir, increases the concentration of sirolimus, which may require an additional dose titer of these substances;
Increases the concentration of cytostatics, which is important for patients with transplanted internal organs;
In combination with anticoagulants (Clexane, rivaroxaban, warfarin), it can provoke various types of bleeding. If, while taking fluconazole, a sign of any bleeding is detected, the drug is immediately canceled;
When combined with hydrochlorothiazide, which is part of many drugs for pressure (Enap-N, etc.), the concentration of fluconazole increases sharply (one and a half times), which must be taken into account, since the risks of side effects also increase, incl. renal failure;
Increases drug toxicity NSAID groups- diclofenac, meloxicam, naproxen, etc. Given that all of these drugs are routine (and many are OTC), the patient should exercise increased caution when using NSAIDs during treatment with fluconazole;
May cause heart rhythm disturbances when combined with quinidine, cisapride, astemizole and other antifungal agents;
May cause renal failure when co-administered with tacrolimus;
When combined with midazolam, it can cause mental abnormalities;
Enhances the effect of amitriptyline.

The drug may be harmful in the following conditions

Overdose and first aid

The main symptoms: diarrhea, nausea up to vomiting, there may be convulsions.

There is information about one patient who, with an overdose of fluconazole, gave a clinic of paranoid delusions and hallucinations. Given that this was a 42-year-old HIV patient (drug addict), such side effects can not be classified as typical for an overdose.

Video about the consequences of six months of fluconazole therapy

Physician-therapist of the city polyclinic. Eight years ago she graduated from the Tver State Medical University with honors. Rate this article: Share with friends!

Source: med-look.ru