Mikomaks

Микомакс Drug photo

The description is actual on 09.06.2016

  • Latin name: Mycomax
  • ATH code: J02AC01
  • Active ingredient: Flukonazol (Fluconazole)
  • Producer: Zentiva k.s (Czech Republic), Fresenius Kabi Austria (Austria)

Structure

One capsule can include 50 mg 100 mg or 150 mg of a flukonazol. In addition: monohydrate of lactose, prezhelatinirovanny starch, colloid silicon dioxide, lauryl sodium sulfate, magnesium stearate.

One milliliter of infusion solution includes 2 mg of a flukonazol. In addition: sodium chloride, injection water.

Release form

Mikomaks it is made in the form of tablets on 50 mg and 100 mg No. 7 in the blister and on 150 mg No. 1 or No. 3 in the blister, and also in the form of injection solution on 100 ml No. 1.

Pharmacological action

Anti-mycotic (antifungal).

Pharmacodynamics and pharmacokinetics

Drug of Mikomaks, with active ingredient flukonazoly, is the representative of a class of the anti-mycotic atriazolny remedies possessing the powerful selection inhibiting impact on the ergosterol synthesis happening in membranes of a cell of micromycetes (mushrooms). The antifungal mechanism of action of a flukonazol is based on its ability to specifically suppress activity of the isofermental fungal R-450 system.

Efficiency of drug is observed concerning opportunistic mycoses, including the mycoses provoked by mushrooms: sorts Candida (Candida spp.), including their generalized forms which are shown against an immunosuppression; sorts of cryptococci (Cryptococcus neoformans), inclusive with intracranial infections; sorts of trikhofiton (Trichophyton spp.) and sorts Microsporum (Microsporum spp). Also efficiency of a flukonazol is noted concerning the endemic mycoses caused by mushrooms: sorts of koktsidioid (Coccidiodes immitis), including intracranial infections; sorts of a blastomyces (Blastomyces dermatilidis) and a sort gistoplazm (Histoplasma capsulalum), including their manifestation at an immunosuppression.

There are messages on episodes of emergence of the superinfection caused by the sort mushrooms Candida which are not belonging to a type of Candida albicans (vulval candidiasis, the milkwoman) who often show natural resistance to action of a flukonazol (in particular Candida krusei). In such cases purpose of alternative antifungal medical drugs can be required.

Flukonazol is characterized by high specificity in relation to isoenzymes of the P450 system of a mushroom and the minimum influence on these isoenzymes in a human body. So single and repeated use of 50 mg of a flukonazol does not exert impact on an antipyrine metabolism. Daily daily reception of 50 mg of a flukonazol for 28 days did not lead to change of plasma level of testosterone at men or sexual gomon at the women who are in childbearing age. Use of a flukonazol in a daily dose of 200-400 mg was not followed by clinically significant change of level of endogenous steroids and essentially influenced hormonal reaction of healthy men to introduction of AKTG.

At oral administration rather fast and full-fledged absorbability of a flukonazol in a gastrointestinal tract is observed. Bioavailability is at the level of 90%. Plasma Cmax, at internal reception of 150 mg of a flukonazol on an empty stomach, makes 90% in comparison with this indicator noted at in introduction of a similar dose. In parallel the eaten food does not exert impact on drug absorption. TCmax varies within 30-90 minutes.

At internal and in use in all biological liquids of a human body high concentration of a flukonazol is fixed. In a phlegm and saliva its level corresponds to plasma contents. Plasma concentration of a flukonazol dozozavisimy. At patients with fungal meningitis in cerebrospinal fluid the level of a flukonazol reaching 80% of its plasma concentration is noted. Css at the level of 90% is reached after 4-5 days at daily one-time reception of a flukonazol.

In case of use in the first day of therapy of a shock dose of a flukonazol (is twice higher than usual), Css at the level of 90% is noted already on second day. Vd approaches cumulative water level in a human body. Communication with plasma proteins is carried out for 11-12%.

In sweat, a corneous layer, a derma and epidermis flukonazol is in the concentration exceeding plasma values. At a single dose of 150 mg of a flukonazol a week, its concentration in a corneous skin layer made 23,4 mkg/g, and at repeated reception of a similar dose in 7 days already of 7,1 mkg/g. After carrying out 4-month therapy with a single dose in a week of a flukonazol in a dose of 150 mg, its concentration in healthy nails made 4,05 mkg/g, and in the infected nails of 1,8 mkg/g. In half a year after drug withdrawal concentration in nails of a flukonazol still gave in to definition.

T1/2 is equal to about 30 hours. Removal of a flukonazol is generally carried out by kidneys (approximately for 80% in not changed form). The clearance of a flukonazol corresponds to clearance of creatinine. Drug metabolism products in peripheral blood are not revealed.

Indications to use

Tablets and infusion solution of Mikomaks are shown to appointment at:

  • generalized candidiases, including the disseminated candidiasis, a kandidemiya and other invasive candidosis infections of fabrics/bodies (an endocardium, a spleen, a peritoneum, urinary ways, eyes, a liver, respiratory tracts and so forth), including at patients with the diagnosed malignant tumors, an immunosuppression and other states contributing to developing of candidiases;
  • cryptococcoses, including pulmonary and skin forms of this infection, and also the cryptococcal meningitis including observed at an immunosuppression (an organ transplantation, AIDS);
  • candidiases of a mucous gullet, mouth/throat, kandiduriya, bronchopulmonary noninvasive candidiases, skin candidiases, including patients with an immunosuppression and prevention at patients with AIDS of recurrence of oropharyngeal candidiasis;
  • candidosis balanitis;
  • vaginal candidiases in a chronic recurrent form and an acute form, and also for them preventively recurrence of this mycotic infection;
  • passing by patients with malignant new growths beam or chemotherapy with use of tsitostatik owing to which the risk of emergence of fungal infections increases (for the purpose of prevention);
  • skin mycoses, including mycoses of a body, inguinal area and feet;
  • skin candidiases;
  • onychomycosis and chromophytosis;
  • local deep mycoses, including histoplasmosis, koktsidiomikoz, a sporotrichosis and parakoktsidiomikoz at patients with normal immunity.

Contraindications

Mikomaks it is contraindicated to use at:

  • personal hypersensitivity to a flukonazol, structurally similar azolny connections or other auxiliary ingredients of tablets or infusion solution;
  • pregnancies;
  • the combined reception of a terfenadin (for dosages over 400 mg of a flukonazol at 24 o'clock), and also a tsizaprida and an astemizola (because of possible increase in a QT interval and developing of ventricular tachycardias);
  • feeding by a breast;
  • any hereditary intolerance of sugars;
  • to the body weight of the patient to 40 kilograms, generally at children's age (for tablets on 100 mg and 150 mg).

It is careful it is necessary to appoint Mikomaks at:

  • liver failure;
  • the combined reception of a terfenadin (for dosages less than 400 mg of a flukonazol at 24 o'clock);
  • renal failure (correction of the dosing mode is necessary);
  • proaritmogenny pathologies at patients with numerous risk factors (disorder of water and electrolytic balance, organic pathologies of heart, parallel reception of the medical drugs causing arrhythmias);
  • the carried-out therapy using oral hypoglycemic remedies, sulfonilmochevina derivatives (only under control of level of glucose in blood sometimes with correction of hypoglycemic therapy, because of possible development of a hypoglycemia).

Side effects

Sometimes at Mikomaks's use observed:

Mikomaks, application instruction (Way and dosage)

The application instruction of Mikomaks assumes oral administration of tablets drug and in/in administration of solution in the form of infusions (with solvent with a speed no more than 20 mg a minute). Transfer of the patient from one dosage form on another does not demand modification of the dosing mode.

For adult patients

At treatment of cryptococcal meningitis and other cryptococcal infections, in the first days, as a rule, appoint 400 mg of Mikomaks then practice single use of 200-400 mg at 24 o'clock. Duration of therapy is influenced by the clinical performance of drug confirmed with the conducted mycologic researches. Cryptococcal meningitis will usually respond to treatment for at least 6-8 weeks. For prevention at patients with AIDS of recurrence of cryptococcal meningitis, after the termination of primary therapeutic course, appoint 200 mg of Mikomaks in the 24th hour for an appreciable length of time.

At candidiases of a mouth/throat single daily use of 100 mg of a flukonazol for 7-14 days is shown. Patients with the expressed decrease in immunity can demand carrying out longer course of treatment.

For therapy of the disseminated candidiasis, a kandidemiya and other invasive candidiases usually appoint 400 mg of Mikomaks then pass to use 200 mg at 24 o'clock in the first days. At unsatisfactory clinical performance allow increase of a daily dose to 400 mg. In case of candidosis infections life-threatening it is possible to increase a single daily dose to 800 mg. Duration of treatment is defined according to observed clinical performance.

At candidiases of other localizations (except genital candidiasis), including skin candidiasis, bronchopulmonary noninvasive defeats, an esophagitis, a kandiduriya, candidiasis of mucous membranes and so forth, daily use of 100 mg of a flukonazol within 14-30 days will be reasonable.

Prevention with AIDS of possible recurrence of oropharyngeal candidiasis demands weekly use of 150 mg of Mikomaks from patients, after the termination of full primary course of therapy.

Vaginal candidiasis (milkwoman) will respond to treatment once accepted Mikomaks's dose of 150 mg. For reduction in the frequency of recurrence it is necessary to accept a similar dose of drug once in a month (as an alternative it is possible to use the candles containing flukonazol). Duration of therapy is established in an individual order and, as a rule, varies within 4-12 months. Treatment of some women can demand more frequent use of drug or additional purpose of candles with flukonazoly.

At therapy of a candidosis balanitis most often rather single application of 150 mg of Mikomaks.

Prevention of candidiasis, considering a risk degree of forming of a fungal infection, it is carried out in single doses of 50-400 mg. At high risk of developing of a generalized infection, for example, at patients with the long or expressed neutropenia expected, recommend to use a dose of 400 mg which is appointed several days prior to the expected neutropenia. At increase in quantity of neutrophils more than on 1000/mm3 continue Mikomaks's reception for 7 more days.

At skin mycoses, including mycoses of a body, inguinal area and feet the recommended week single dose equals 150 mg, applied within 2-4 weeks. Some mycoses of feet can demand carrying out more prolonged treatment (about 6 weeks).

Therapy of an onychomycosis is carried out using a single week dose of 150 mg. Treatment is continued up to full replacement of the infected nail by healthy. As a rule, this process, in connection with specific features and age, takes from 3rd to 6 months, and sometimes and up to 12 months (at therapy of a nail of a thumb of a leg). After full replacement of a nail plate its deformed form can remain.

At treatment of a chromophytosis, the single week dose is usually equal to 300 mg, accepted for 2 weeks. To some patients of rather single-step reception of 300-400 mg of Mikomaks, thrice reception of 300 mg can be necessary for others. As alternative practice use of the therapeutic scheme borrowing 2-4 weeks with reception of 50 mg of Mikomaks at 24 o'clock.

At local deep mycoses long therapy (to 2 years) using 200-400 mg of Mikomaks at 24 o'clock is carried out. Treatment duration individual for each patient can also vary: 3-17 months for treatment of histoplasmosis; 2-17 months for therapy of a parakoktsidiomikoz; 1-16 months for treatment of a sporotrichosis; 11-24 months for therapy of a koktsidiomikoz.

For children

Duration of use of Mikomaks in pediatrics also depends on mycologic and clinical performance. Children should not appoint the daily dosages of drug exceeding those at adult patients at treatment of similar infections. At children's age of a dosage of Mikomaks expect kilogram of weight of the child and recommend to accept 1 time at 24 o'clock.

When carrying out therapy of candidiasis mucous appoint every day 3 mg/kg. In the first days of treatment, for achievement of fast equilibrium concentration, recommend to use a shock dosage of a flukonazol of 6 mg/kg.

At treatment of cryptococcal mycosis and generalized candidiasis, depending on observed disease severity, recommend to accept 6-12 mg/kg a day.

Prevention of children's mycotic infections at reduced immunity, with risk of their emergence, connected with a neutropenia which can develop as a result of carrying out chemotherapy with use of tsitostatik or radiation therapy, is carried out in a daily dosage of 3-12 mg/kg (being coordinated with duration and expressiveness of the induced neutropenia).

For elderly patients

Elderly patients with normal renal function do not need correction of dosages of Mikomaks.

For patients with insufficiency of kidneys

Single use of Mikomaks by patients of all age categories at KK more than 50 ml/min. does not demand changes of its dosing. Course therapy of patients of all age categories with the broken renal function is carried out with initial use of a shock dose within 50-400 mg (depending on an observed mycotic infection). Further, at KK of 11-50 ml/min. appoint a dose of a flukonazol, a component of 50% of the recommended dosage of drug applied to therapy of this or that fungal infection. Purpose of the usual doses of Mikomaks applied after holding each session of a dialysis is shown to the patients who is regularly undergoing procedure of a hemodialysis.

Overdose

At overdose by Mikomaks developing of hallucinations and paranoid manifestations is possible.

The symptomatic treatment including cleaning of a gastrointestinal tract and carrying out an artificial diuresis is shown. At 3-hour procedure of a hemodialysis of their blood plasma about 50% of a flukonazol are removed.

Interaction

The combined use of indirect anticoagulants, coumarinic derivatives (for example, Warfarin) can provoke increase in a prothrombin time that demands continuous tracking of this indicator.

Parallel use of some azoles with terfenadiny, because of increase at a QT interval ECG, led to emergence of serious cordial violations of a rhythm, inclusive with piruetny tachycardia. The conducted researches of a flukonazol did not reveal increase in a QT interval at its reception in a daily dose of 200 mg. Reception of a flukonazol in dosing borders of 400-800 mg led to significant increase of serumal maintenance of a terfenadin. In this regard, the combined use of a terfenadin and flukonazol in dosages less than 400 mg demands attentive supervision, and higher than 400 mg are contraindicated in drug doses.

At combined use of a flukonazol and astemizol, as well as the other remedies which are metabolized P450 cytochrome isoenzymes increase in their serumal concentration in this connection, such combination of drugs demands continuous supervision over their plasma contents and timely correction of dosages at change of that is not excluded.

The hydrochlorothiazide is capable to increase the plasma level of a flukonazol for 40%, nevertheless such combination of drugs does not need change of dosages of Mikomaks.

At the combined Mikomaks's use with the oral hypoglycemic medical drugs derivative of a sulfonilmochevina (glipizid, Glibenclamidum, Tolbutamidum and so forth), increase in their plasma contents and T1/2 was observed. For this reason at such combination of medical drugs it is necessary to consider probability of forming of a hypoglycemia and to watch carefully glucose level in blood. In certain cases change of the dosing mode of the accepted hypoglycemic drug can be necessary.

Flukonazol increases plasma level jointly of the accepted midazolam that can become an origin of psychotic manifestations. The effect of this interaction is more expressed in case of oral administration of midazolam, in comparison with in/in administration of this drug, and can demand decrease in its dosages.

Parallel purpose of a flukonazol and Phenytoinum led to clinically significant increase of serumal contents of the last. At joint purpose of these drugs it is necessary to trace plasma concentration of Phenytoinum and to timely adjust its dosing mode.

The combined reception of Rifampicin reduces the plasma maintenance of a flukonazol by 25% and reduces its T1/2 approximately by 20% that demands increase of dosages of Mikomaks.

Joint reception of a flukonazol and Rifabutin leads to increase in serumal level of a rifabutin that can be the cause of development of a uveitis. In this regard the combined use of these remedies demands continuous supervision.

There are messages on development of the negative cordial phenomena (inclusive with piruetny tachycardia) provoked by a concomitant use of a flukonazol and a tsizaprid. The conducted controlled researches showed reliable increase of serumal maintenance of a tsizaprid and increase in a QT interval at single daily dose of 200 mg of a flukonazol and parallel quadruple daily reception of 20 mg of a tsizaprid. Owing to such effect of interaction of these medicines their concomitant use is contraindicated.

Patients with the transplanted kidney have a combined reception of Cyclosporine and a daily dose of a flukonazol of 200 mg led to slight increase of plasma content of cyclosporine. At the same time at the patients with the replaced marrow accepting flukonazol in a daily dosage of 100 mg, the serumal level of cyclosporine did not change. For this reason, in case of need single-step use of Mikomaks and cyclosporine, it is necessary to trace plasma concentration of the last constantly.

Flukonazol can increase the serumal level of Theophylline. Use of 200 mg of Mikomaks for 14 days led to reduction of average values of serumal clearance of theophylline by 18%. In this regard, the patients receiving theophylline in high dosages as well as patients with probability of forming of teofillinovy intoxication, demand continuous supervision for timely detection of symptomatology of overdose by theophylline.

High dosages of a flukonazol (it is higher than 400 mg) clinically significantly increase the plasma maintenance of a zidovudine, because of decrease in its transformation to the main metabolite that can lead to aggravation of by-effects of a zidovudine. At use by the patient of such combination of drugs regular control of its state regarding forming of the negative by-effects connected with a zidovudine is necessary.

Use of a flukonazol promotes increase in serumal concentration of Takrolimus that can lead to the clinical phenomena of its toxicity (a hyperglycemia, nephrotoxicity, a hyperpotassemia). In this case decrease in dosages jointly of the accepted takrolimus can be required.

Parallel reception of 50 mg of a flukonazol and oral contraceptives did not reveal significant changes of serumal concentration of levonorgestrel and ethinylestradiol. At reception of 200 mg of drug noted increase for 24% of AUC levonorgestrel and for 40% of AUC ethinylestradiol. Thereof significant impact of a flukonazol on contraceptive efficiency of oral contraceptives is not expected.

The conducted researches of interaction of Mikomaks did not reveal significant decrease in absorption of a flukonazol at parallel meal, use of Cimetidinum or carrying out radiation of all body before transplantation of marrow.

The attending physician appointing Mikomaks has to take possible development of its other interactions as researches of a combination of Mikomaks to other medical drugs were not conducted into account.

Terms of sale

Tablets of Mikomaks can be got without recipe of the doctor, and infusion solution at presentation of that.

Storage conditions

Temperature of storage of tablets should not exceed 25 °C and to be within 10-25 °C for infusion solution.

Period of validity

Both dosage forms of Mikomaks are subject to storage for 3 years.

Special instructions

All above-stated indications to use of medical drug of Mikomaks demand continuation of therapy with its use up to approach of the full remission confirmed with clinical laboratory indicators. Premature phase-out of Mikomaks often leads to recurrence. At all stage of the carried-out treatment it is necessary to control functionality of kidneys/liver of the patient and to trace his hematologic indicators.

In rare instances when carrying out therapy flukonazoly observed changes of a liver of toxic character, capable to lead to a lethal outcome. Such changes mainly noted at patients with the serious accompanying pathologies. The found hepatotoxic effects of a flukonazol significantly did not depend on use of a cumulative daily dose, duration of therapy, age and a sex of the patient. As a rule, the hepatotoxic action of drug was reversible with disappearance of signs after the end of treatment. At emergence against Mikomaks's use of any disturbance of hepatic/renal function it is necessary to interrupt the carried-out therapy.

Patients with AIDS are more subject to forming of heavy skin manifestations at use of various remedies. In cases of development of rash in the patient with the superficial mycotic infection associated using Mikomaks, the carried-out therapy should be stopped. At detection of rash at patients with system invasive mycoses it is necessary to watch attentively its development and to cancel Mikomaks at detection of violent manifestations or a mnogoformny erythema.

The doctor needs to remember probable development against Mikomaks's use increases in a QT interval and the piruetny ventricular tachycardia which is occasionally noted during therapy by drugs of a flukonazol. This effect was in most cases observed at patients with heavy cardiac pathologies and numerous risk factors, including disturbances of a salt metabolism, a myopathy and parallel reception of the remedies influencing a cordial rhythm.

Infusional Mikomaks should be mixed with the following solutions: glucose (20%); Ringera; Chloride Potassium in glucose; Hartman; bicarbonate sodium (4,2%), chloride Sodium (0,9%).

Analogs

Mikomaks's analogs are provided by drugs:

Zdravzona

  • Mikomaks 150 mg No. 3 of a kapsulyzentiv
  • Mikomaks 150 mg No. 1 of a kapsulazentiv
  • Mikomaks 2mg/ml solution for infusions 100mlzentiva

Drugstore of IFC

  • Mikomaks kaps 150 mg No. 3, Zentiva A.S.Chekhiya
  • Mikomaks kaps 150 mg No. 1, Zentiva A.S.Chekhiya
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Apteka24

  • Mikomaks capsules 150 mg No. 3lechiva (Czech Republic)
  • Mikomaks capsules 150 mg No. 1lechiva (Czech Republic)

Paniapteka

  • Mikomaks kaps. 150 mg No. 1zentiva International a.o.
  • Mikomaks kaps. 150 mg No. 1zentiva International a.o.

BIOSPHERE

  • Mikomaks 150 mg No. 1 kaps. Zentiva of ampere-second. (Czech Republic)
  • Mikomaks 200 mg 100 ml solution for inf.fl. Frezenius Kabi Austria Gmbh, Austria for Zentiva of ampere-second. (Czech Republic)
  • Mikomaks 100 mg No. 7 kaps. Zentiva of ampere-second. (Czech Republic)
  • Mikomaks 150 mg No. 3 kaps. Zentiva of ampere-second. (Czech Republic)
  • Mikomaks 5 mg/ml 100 ml siropleciva a.s. (Czech Republic)
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Section: Antifungal
in more detail

Education: Graduated from the Vinnytsia national medical university of N. I. Pirogov, pharmaceutical faculty, the higher pharmaceutical education – the specialty "Pharmacist".

Experience: Work in Koneks and Bios-Media pharmacy chains as "Druggist". Work as "Pharmacist" in Avicenna pharmacy chain of the city of Vinnytsia.

PAY ATTENTION! Information on drugs on the website is help generalizing, collected from public sources and can form the basis for making decision on use of medicines it is not aware of treatment. Before use of medicine of Mikomaks surely consult with the attending physician.