The drug "Mikosist" application instructions defines as an antifungal agent. The active ingredient in the drug is fluconazole, a selective inhibitor of the synthesis of sterols in fungal cells. It inhibits the cytochrome P450 system in the human body, does not show androgenic activity, is effective against pathogens of mycosis.
Pharmacokinetics
After oral administration or intravenous administration, the Mikosist medication (instructions indicate this) penetrates well into body fluids and tissues. In sputum, peritoneal and articular fluid, saliva, breast milk, the concentration of the drug is similar to that achieved in blood plasma. The fluconazole content in cerebrospinal fluid in patients with fungal meningitis is eighty percent of the plasma concentration, which, in turn, is directly proportional to the dose taken. With a single daily application, a 90 percent equilibrium concentration is reached by the fourth to fifth day. If you take a dose twice the usual dose on the first day, you can already reach 90 percent equilibrium cumulation by the second day. Eleven to twelve percent of fluconazole binds to plasma proteins. No metabolites are found in peripheral blood. Pharmacokinetics significantly depends on the work of the kidneys, because the drug is excreted from the body mainly by them, and about eighty percent - unchanged. Within three hours after hemodialysis, the concentration of the active substance in the plasma is halved.
Indications for appointment
It is recommended to use the Mikosist medication for thrush, including generalized, disseminated, genital, with other forms of invasive candida infection, candidaemia, as well as in the presence of factors conducive to the appearance of thrush. In addition, the use of the drug for people with candidiasis of the mucous membranes is shown: pharynx; the oral cavity, including atrophic candidiasis resulting from wearing dentures; esophagus. The medicine "Mikosist" application instruction advises to prescribe to patients suffering from cryptococcal meningitis or sepsis, cryptococcosis, cryptococcal infection of the skin or lungs. It is also used to prevent relapse of these pathologies in patients with AIDS and in other cases of immunodeficiency. The medication is used to prevent fungal infections in people with malignant tumors predisposed to radiation damage or chemotherapy. Also, the drug "Mikosist" is used in the treatment of mycoses of the inguinal region and trunk, deep endemic mycoses, including paracoccidioidomycosis, coccidioidomycosis, histoplasmosis in patients with normal immunity.
Dosage form, packaging, composition
Mikosist has two dosage forms: capsules and a solution for infusion. Capsules are produced containing 50, 100 and 150 milligrams of fluconazole. All of them are hard gelatinous, with an opaque white body, and differ only in the color of the caps: capsules containing 50 milligrams of the active ingredient, the cap is light blue, 100 milligrams is turquoise, 150 milligrams is blue. The content is a powdery dense mass or a white (almost white) powder. The auxiliary ingredients are magnesium stearate, anhydrous lactose, colloidal silicon dioxide, talc, titanium dioxide, corn starch, gelatin, indigo carmine. Capsules containing 50 and 100 milligrams of fluconazole are marketed in packs of one, two, four blisters, seven in each. And those that contain 150 milligrams of the active substance - one or two pieces.
The infusion solution is in the form of a clear, slightly colored or colorless liquid. One milliliter contains two milligrams of the active substance. Minor components are water for injection and sodium chloride. The solution is dispensed in glass bottles with a volume of one hundred milliliters, placed in cardboard packs. One pack includes one bottle.
How to take "Mikosist"? Dosage
The usual dose of fluconazole for cryptococcal infections is 400 milligrams on the first day of treatment, and 200-400 milligrams on the following days. The duration of therapy depends on the clinical efficacy confirmed by the mycological study , often it does not exceed six to eight weeks. In case of cryptococcal meningitis , the Mikosist medicine is recommended for use within ten to twelve weeks after a negative result of a study of the cerebrospinal fluid was obtained. After the end of the course of primary treatment, AIDS patients are prescribed for the prevention of relapses of cryptococcal meningitis for a long period taking Mikosist at a dose of at least two hundred milligrams per day.
With disseminated candidiasis, candidaemia, and other invasive candidiasis infections, as a rule, four hundred milligrams of the drug are taken on the first day, and two hundred milligrams daily on the following days. In case of severe systemic thrush, the dose can be increased to eight hundred milligrams per day. Treatment should be continued for at least another two weeks after the symptoms are resolved and negative blood culture is obtained. With oropharyngeal candidiasis, including in patients with impaired immunity, the dosage of the drug per day is fifty to one hundred milligrams, it should be taken within seven to fourteen days. With atrophic candidiasis arising from the wearing of dentures, fifty milligrams of the drug is usually prescribed per day in combination with antiseptic agents. Treatment is continued for two weeks. For other candidal infections (candiduria, esophagitis, candidiasis of the mucous membranes and skin), the daily dose of the medication is fifty to one hundred milligrams, the course of treatment is fourteen to thirty days.
In order to eliminate vaginal candidiasis, the drug "Mikosist" instructions for use show taking once in an amount of 150 milligrams. You can drink one capsule (150 mg) for four to twelve months once a month to reduce the frequency of relapses. Often with candidiasis, suppositories are prescribed in addition to the Mikosist drug, for example, Terzhinan, Klion-D, Ginezol. Depending on the degree of risk of a fungal infection, for the prevention of candidiasis, the daily recommended dose of the medication can vary from fifty to four hundred milligrams.
In the case of deep endemic mycosis, it may be necessary to take the drug in a dosage of two hundred - four hundred milligrams per day for two years. The duration of therapy depends on individual characteristics and the clinical picture: with coccidioidomycosis, it can be from eleven to twenty four months, with paracoccidioidomycosis - from two to seventeen months, with histoplasmosis - from three to seventeen months.
Application rules
The drug should be administered intravenously, at a rate of not more than twenty milliliters per minute. There is no need to change the daily dosage when transferring a patient from intravenous administration to oral medication. The solution for infusion is compatible with a twenty percent glucose solution; Hartman and Ringer solutions; solutions of sodium bicarbonate, potassium chloride in glucose, sodium chloride (0.9%). Fluconazole can be infused using ordinary transfusion kits using one of these solutions.
Side effects
Most patients who took the drug "Mikosist" leave good reviews about it. The drug really effectively eliminates fungal infections, but it can cause negative effects. So, from the digestive system there is a risk of nausea, flatulence, impaired liver function, problems with taste sensations, diarrhea. Also, some people mention the occurrence of headaches, cramps, dizziness. They say that such phenomena arose soon after taking the "Mikosist" medication. The reviews of other patients contain information about the development of allergy in the form of erythema, skin rash, angioedema, urticaria against the background of therapy. Other possible side effects include alopecia, ventricular fibrillation, impaired renal function, hypertriglyceridemia, hypercholesterolemia and hypokalemia.
Contraindications
In the form of capsules, medication should not be prescribed to children up to six months of age (for newborns, the use of medication in the form of a solution for infusion is allowed). The use of the Mikosist drug is contraindicated for lactating women (pregnant women should be prescribed with caution), as well as for people who are highly sensitive to the ingredients included in the composition. With increased caution, it is necessary to use the drug in patients with renal / hepatic insufficiency, with intolerance to acetylsalicylic acid.
Overdose
Cases of overdose of the drug "Mikosist." Reviews of people who took the medicine in excessive doses indicate the development of diarrhea, nausea, and vomiting. In severe cases, the appearance of seizures, paranoid behavior, hallucinations. A person with symptoms of an overdose must be taken to a hospital, where he will undergo gastric lavage, hemodialysis, forced diuresis, and symptomatic therapy.
Mikosist or Fluconazole: which is better?
This question is often asked by patients. In fact, both drugs act the same way, we can say that they are identical. The only difference is that the Mikosist medicine is produced by the Hungarian pharmaceutical company Gedeon Richter, while Fluconazole is a domestic drug. Of course, this directly affects the cost of medicines. Choosing what to buy - “Mikosist” or “Fluconazole” - many prefer the medicine that is cheaper. Indeed, the price difference is significant. So, for a package of Mikosista (one capsule containing 150 milligrams of fluconazole) you have to pay an average of 295 rubles, while the same package of Fluconazole will cost only 8-20 rubles. The average price of a 100-ml bottle of Mikosist infusion solution is 311 rubles.
As for the pharmacological properties of the two drugs, they are almost identical, the difference can be seen only in the absorption rate: according to available data, the maximum concentration in the body of “Fluconazole” is reached 1-2 hours after application, and “Mikosista” - after 0.5 -1,5 hour. However, not all patients report the same two drugs. Some do not see any difference between the two, the second believe that the quality depends on the price, which means which medication is more expensive is better. You can often find reviews in which women say that after taking Fluconazole, the thrush returned, but Mikosist allowed her to get rid of it for a long time. In any case, the choice is yours.
Analogs
In addition to Fluconazole, there are other medications that can replace the Mikosist drug. Analogues of a medicinal product having the same substance as an active ingredient are represented quite widely. In the form of capsules for the treatment of thrush and other fungal infections, you can use the drugs "Diflucan", "Flucostat", "Mikomaks" and others. Effective is the drug "Mikoflukan" (tablets). "Mikosist" differs from all the analogues mentioned above in such indicators as bioavailability, half-life, absorption rate.
Drug interaction
It is necessary to carefully monitor the prothrombin time in patients receiving, along with fluconazole, the indirect anticoagulants of the coumarin group, since there is a risk of an increase in PTV. When taken simultaneously with sulfonylurea derivatives, the Mikosist drug can increase their half-life, therefore, the possibility of hypoglycemia should be taken into account. In the case of the combined use of fluconazole and phenytoin, the concentration of the latter can increase to a clinically significant degree, as a result of which, if necessary, the combined dose should be reduced. With the simultaneous administration of Mikosist and rifampicin, a decrease in the concentration of fluconazole will be observed, therefore, the dose of Mikosist must be increased. The combined use of the drug with azole derivatives in combination with terenadine is contraindicated, since a serious, life-threatening arrhythmia can develop. If you take the medicine "Mikosist" together with cisapride, unwanted reactions from the heart, including ventricular tachycardia , may occur . With the simultaneous use of fluconazole and theophylline, the average clearance rate from the blood plasma of the latter decreases, which means that the likelihood of its toxic effects and overdose increases.
special instructions
Continue treatment with Mikosist until clinical and hematological remission appears. Premature termination of therapy is fraught with relapse. As already mentioned, patients with renal failure should use the medication as carefully as possible, since it is excreted mainly by the kidneys. Dosage for long-term treatment should be given, taking into account QC. Sometimes the use of fluconazole entails toxic effects on the liver, so it is necessary to monitor the functioning of this organ. If signs of damage are detected, the drug should be discontinued.
Patients with the use of the Mikosist drug have been noted rare cases of the appearance of exfoliative skin reactions, such as toxic epidermal necrolysis and Stevens-Johnson syndrome. Patients with malignant neoplasms and AIDS are more prone to severe skin reactions when using drugs containing fluconazole. If a rash appears during treatment of superficial fungal infection, the medicine should be discontinued. If a rash occurs in people with an invasive or systemic fungal infection, the doctor should strengthen the observation and discontinue the drug if erythema multiforme or bullous lesions develop. During treatment with the Mikosist medication (reviews confirm this), dizziness may occur, so patients need to be very careful when working with equipment and driving vehicles.