The drug "Fluconazole" is an antifungal medication from the category of triazole derivatives. The drug is produced by the Russian pharmaceutical company VERTEX CJSC, which is located in St. Petersburg. Vertex reviews of Fluconazole will be presented below.
Composition and dosage form
The medication is available in the form of capsules, the active substance is fluconazole in a dosage of 50 mg or 150 mg. Fluconazole does not have a tablet form of release.
The following are used as auxiliary substances in the production: polyvinylpyrrolidone (povidone), corn starch, colloidal silicon dioxide (aerosil), sodium lauryl sulfate, lactose, calcium stearate. For capsules in a dosage of 50 mg, gelatin, titanium dioxide, dye azorubin, yellow dye for sunset are used, and for Flutonazole from Vertex, 150 mg, titanium dioxide and gelatin are used. Hard gelatin capsules - with a white body, an orange cap, their contents are a compacted mass or powder of a white or yellowish tint.
Pharmacological properties
According to the instructions for use, “Fluconazole” from Vertex represents a class of triazole antifungal drugs. It is a potent selective inhibitor of the fungal cell enzyme 14-α-demethylase. This medical tool prevents the processes of transformation of lanosterol into ergosterol - the main element of the cell membranes of fungi.
Not everyone knows why Fluconazole tablets help. The medication has increased activity in opportunistic mycoses, in particular, provoked by Candida spp. (Candida tropicalis, Candida albicans), Microsporum spp., Cryptococcus neoformans, Trichophyton spp. In addition, the activity of the main component was tested on models of endemic mycoses, including infections caused by Blastomyces dermatidis, Coccidioides immitis and Histoplasma capsulatum. However, histoplasmas, blastomycetes, sporotrix and paracoccidioid are less sensitive to fluconazole than to other azoles.
Indications for appointment
The medicine "Fluconazole" from the company "Vertex" is prescribed for the treatment of the following pathologies:
- cryptococcosis, including cryptococcal type meningitis and other localizations of this infection (skin, lungs) both in patients with a normal immune system response and with various types of immunosuppression (AIDS, organ transplantation);
- generalized candidiasis, including candidaemia, disseminated candidiasis and other forms of candidal invasive infections (infections of the endocardium, peritoneum, eyes, urinary and respiratory organs);
- candidiasis of the mucous membranes, for example, pharynx and oral cavity (including atrophic candidiasis of the oral mucosa due to wearing prostheses), non-invasive candidiasis bronchopulmonary candidiasis, cutaneous candidiasis;
- prevention of recurrent oropharyngeal candidiasis in people with AIDS;
- mycosis of the skin (inguinal region, body, feet);
- onychomycosis, pityriasis versicolor;
- candidiasis of the skin;
- genital candidiasis: chronic and acute vaginal candidiasis of a relapsing type, as well as prophylactic use to reduce the frequency of relapses of this disease (3 or more times a year);
- prevention of fungal diseases in cancer patients with a predisposition to fungal infections due to radiation therapy or treatment with cytostatics;
- candida balanitis;
- deep endemic mycoses, including histoplasmosis and coccidiomycosis.
Contraindications
Tablets "Fluconazole" ("Vertex") are contraindicated in such conditions:
- high sensitivity to fluconazole, other components of the drug or azole compounds;
- the combined use of terfenadine and this drug (against the background of constant use of fluconazole at a dosage of 400 mg or more per day), astemizole or cisapride and other medicines that extend the QT interval and increase the risk of heart rate changes;
- lactation period;
- age up to 3 years.
This must be considered before the appointment.
Careful reception
The medication is prescribed with caution in case of liver, kidney, or rash on the background of taking the drug in patients with systemic / invasive fungal infections or with superficial infection. Caution should also be observed when taking fluconazole and terfenadine in the above dose, since this can cause potentially proarrhythmogenic conditions in people with risk factors (electrolyte imbalance, organic heart pathologies, while taking medications that cause arrhythmia). Vertex reviews of Fluconazole should be reviewed in advance.
During pregnancy and lactation
The use of the drug during pregnancy is impractical, with the exception of life-threatening types of fungal infections.
The active element of the drug is found in breast milk at the same level as in the blood, so its use during lactation is undesirable.
Instructions for use
The medication is taken orally, the daily dosage depends on the severity and nature of the fungal disease.
With cryptococcal infections and cryptococcal meningitis, 400 mg is prescribed on the first day, after which treatment continues at a dose of 200 mg per day for 10-12 weeks.
With disseminated candidiasis, candidaemia, and other candida invasive infections, the dosage is 400 mg on the first day, and then 200 mg for at least 2 weeks.
With oropharyngeal candidiasis, the medication is prescribed 50-100 mg once a day, up to 14 days.
With atrophic candidiasis - 50 mg per day, 1 time, 2 weeks in combination with local antiseptics.
With a different localization of candidiasis, in addition to genital (esophagitis, non-invasive bronchopulmonary lesion, candiduria, fungal infection of the skin and mucous membranes), the effective dose is 50-100 mg per day, 30 days. In severe forms of these diseases, the dosage is increased.
How is Fluconazole used for thrush in women?
With vaginal candidiasis, the medicine is taken once at a dose of 150 mg, with mycosis of the skin - 150 mg per week, 1 time, with pityriasis versicolor - 300 mg once a week. "Fluconazole" from nail fungus is used at 150 mg once a week. With deep endemic mycosis, the medication is prescribed in a dosage of 200-400 mg per day for 2 years.
For the prevention of candidiasis, the recommended dose of fluconazole will be 50-400 mg once a day. For patients with expected severe or persistent neutropenia, the optimal dose is 400 mg once a day.
Side effects
According to reviews, Fluconazole Vertex can cause these side effects:
- From the digestive system: taste change, decreased appetite, dyspepsia, diarrhea, bloating, abdominal pain, increased activity of liver enzymes and a change in its functional parameters (hyperbilirubinemia, jaundice, hepatocellular necrosis, increased activity of aspartic aminotransferase, alanine aminotransferase, alkaline phosphatase, hepatic and alkaline phosphatase) including fatal.
- CNS: headache, dizziness, cramps.
- Hematopoietic organs: neutropenia, agranulocytosis, hematological disorders (thrombocytopenia and leukopenia).
- Cardiovascular system: prolongation of the Q — T interval on the ECG, flutter / ventricular fibrillation.
- Allergic reactions: exudative erythema multiforme, skin rashes, epidermal toxic necrolysis, bronchial asthma, anaphylactoid reactions.
- Other: changes in the functional characteristics of the kidneys, hypercholesterolemia, hypokalemia, baldness, hypertriglyceridemia.
Drug interaction
A single dose of the drug in the treatment of vaginal candidiasis (thrush) is not accompanied by significant interactions. However, when using higher dosages of the drug in conjunction with other medicines, the following reactions are possible:
- With terfenadine, astemizole and cisapride: an increase in the concentration of these medicines in the plasma, which can become a factor in lengthening the QT interval and lead to serious heart rhythm disturbances. Fluconazole in the liver suppresses the enzymes of the P450 system, reducing the metabolism of these drugs.
- With the combined use of fluconazole and warfarin, the prothrombin time lengthens, therefore, with this combination of substances, control of this indicator is necessary.
- Fluconazole prolongs the half-life of hypoglycemic oral agents (sulfonylureas).
- With simultaneous administration with hydrochlorothiazide, the concentration of fluconazole in the blood increases.
- Rifampicin accelerates the processes of fluconazole metabolism.
- In patients after kidney transplantation, the drug may increase plasma cyclosporine levels. With this in mind, monitoring of cyclosporin concentration is recommended.
- Fluconazole increases the level of theophylline, midazolam and indinavir in plasma.
- This drug enhances the pharmacological properties of rifabutin and phenytoin to a significant extent.
- The medication increases the level of tacrolimus, as a result of which there is a risk of nephrotoxicity.
Reviews on "Fluconazole Vertex"
Today, almost every person knows the drug "Fluconazole" due to its effectiveness and frequent prescription by doctors. The medicine from the Vertex company is considered the best among all others, and this is confirmed by numerous reviews from patients.
Patients who took capsules note that this medication successfully and quickly copes with various forms of fungal diseases. The most common of these are fungal infections of the mucous membranes, including thrush in women, oral candidiasis, etc. Fluconazole from nail and foot fungus is widely used, and in this case the drug also showed high efficiency.
Negative reviews about the drug are due to a large number of side effects that develop while taking it. As the most frequent reactions, people note headaches, dyspeptic disorders, excessive drowsiness and dizziness. Often, patients had digestive disorders in the form of flatulence and constipation.