The drug "Fluconazole" is an antifungal drug from the category of triazole derivatives. The drug is produced by the Russian pharmaceutical company CJSC VERTEX, which is located in St. Petersburg. Reviews of "Fluconazole" from "Vertex" will be presented below.
Composition and dosage form
The drug is available in the form of capsules, the active substance is fluconazole at a dosage of 50 mg or 150 mg. Fluconazole does not have a tablet form of release.
As auxiliary substances in the production are used: polyvinylpyrrolidone (povidone), corn starch, colloidal silicon dioxide (aerosil), sodium lauryl sulfate, lactose, calcium stearate. For capsules at a dosage of 50 mg, gelatin, titanium dioxide, azorubine dye, yellow dye - sunset are used, and for Fluconazole, produced at a dosage of 150 mg from Vertex, titanium dioxide and gelatin are used. Gelatin hard capsules - with a white body, orange cap, theircontents - compacted mass or powder of white or yellowish hue.
Pharmacological properties
As we are informed by the instructions for use, "Fluconazole" from "Vertex" is a class of triazole antifungal drugs. It is a potent selective inhibitor of the fungal cell enzyme 14-α-demethylase. This medicine prevents the transformation of lanosterol into ergosterol, the main element of fungal cell membranes.
Not everyone knows why Fluconazole tablets help. The drug 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 paracoccidioides are less sensitive to fluconazole than to other azoles.
Indications for prescription
The drug "Fluconazole" from the company "Vertex" is prescribed for the treatment of the following pathologies:
- cryptococcosis, including cryptococcal 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 candidiasisinvasive infections (infections of the endocardium, peritoneum, eyes, urinary and respiratory organs);
- mucosal candidiasis, e.g., pharynx and oral cavity (including atrophic candidiasis of the oral mucosa due to wearing prostheses), bronchopulmonary non-invasive candidiasis, candiduria, cutaneous candidiasis;
- prevention of recurrent oropharyngeal candidiasis in people with AIDS;
- mycosis of the skin (groin, body, feet);
- onychomycosis, pityriasis versicolor;
- skin candidiasis;
- genital candidiasis: chronic and acute vaginal candidiasis of recurrent 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 patients with oncological neoplasms who are predisposed to fungal infections due to radiation therapy or treatment with cytostatics;
- candidal balanitis;
- deep endemic mycoses, including histoplasmosis and coccidioidomycosis.
Contraindications
Fluconazole (Vertex) tablets are contraindicated in the following conditions:
- high sensitivity to fluconazole, other components of the drug or azole compounds;
- 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 drugs that prolong the Q-T interval and increase the risk of developingchanges in heart rate;
- lactation;
- under 3 years old.
This must be considered before appointment.
Careful reception
The drug is prescribed with caution in case of liver failure, kidney failure, with the appearance of a rash while taking the drug in patients with systemic / invasive fungal infections or with a superficial infection. Caution should also be observed when taking fluconazole and terfenadine at the above dose, since this can cause potentially proarrhythmogenic conditions in people with risk factors (electrolyte imbalance, organic heart pathologies, simultaneous use of medications that cause arrhythmia). Reviews of Fluconazole from Vertex should be read in advance.
During pregnancy and lactation
The use of the drug during pregnancy is not advisable, except for 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 drug is taken orally, the daily dosage depends on the severity and nature of the fungal disease.
For cryptococcal infections and cryptococcal meningitis, 400 mg is prescribed on the first day, after which treatment is continued at a dose of 200 mg per day for 10-12 weeks.
For disseminated candidiasis, candidemia and other candidal invasive infections, the dosage is400 mg on the first day, and after that - 200 mg for at least 2 weeks.
For oropharyngeal candidiasis, the drug is prescribed at 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 other localization of candidiasis, except for genital (esophagitis, non-invasive bronchopulmonary lesions, candiduria, fungal lesions 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?
For vaginal candidiasis, the drug is taken once at a dose of 150 mg, for skin mycoses - 150 mg per week 1 time, for pityriasis versicolor - 300 mg once a week. "Fluconazole" from nail fungus is used 150 mg 1 time per week. With deep endemic mycosis, the drug is prescribed at a dosage of 200-400 mg per day for 2 years.
For the prevention of candidiasis, the recommended dose of fluconazole is 50-400 mg once a day. For patients with expected severe or long-lasting neutropenia, the optimal dose is 400 mg 1 time per day.
Side effects
According to reviews, "Fluconazole Vertex" can cause such side effects:
- Digestive system: taste changes, decreased appetite, dyspepsia, diarrhea, bloating, abdominal pain, increased activityliver enzymes and changes in its functional parameters (hyperbilirubinemia, jaundice, hepatocellular necrosis, increased activity of aspartic aminotransferase, alanine aminotransferase and alkaline phosphatase, hepatitis), including fatal.
- CNS: headache, dizziness, convulsions.
- Hematopoietic organs: neutropenia, agranulocytosis, hematological disorders (thrombocytopenia and leukopenia).
- Cardiovascular: ECG QT prolongation, ventricular flutter/flicker.
- Allergic reactions: exudative erythema multiforme, skin rashes, epidermal toxic necrolysis, bronchial asthma, anaphylactoid reactions.
- Other: altered renal function, hypercholesterolemia, hypokalemia, baldness, hypertriglyceridemia.
Drug Interactions
A single dose of medication 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 drugs, the following reactions are possible:
- With terfenadine, astemizole and cisapride: Increased plasma concentrations of these drugs, which can prolong the QT interval and lead to serious cardiac arrhythmias. Fluconazole in the liver inhibits enzymes of the P450 system, reducing the metabolism of these drugs.
- With the combined use of fluconazole and warfarin, the prothrombin time is prolonged, therefore, with this combination of substances, control of thisindicator.
- Fluconazole prolongs the half-life of hypoglycemic oral agents (sulfonylurea derivatives).
- When taken simultaneously with hydrochlorothiazide, the concentration of fluconazole in the blood increases.
- Rifampicin accelerates the metabolism of fluconazole.
- In kidney transplant patients, the drug may increase plasma levels of ciclosporin. With this in mind, monitoring of ciclosporin concentrations is recommended.
- Fluconazole increases plasma levels of theophylline, midazolam and indinavir.
- This drug enhances the pharmacological properties of rifabutin and phenytoin to a significant extent.
- Drug increases tacrolimus levels, resulting in risk of nephrotoxicity.
Reviews about "Fluconazole Vertex"
Today, almost every person knows the drug "Fluconazole" due to its effectiveness and frequent prescription by doctors. The medicine from the company "Vertex" is considered the best among all others, and this is confirmed by numerous reviews from patients.
Patients who took the capsules note that this medication successfully and quickly copes with various forms of fungal diseases. The most common of them are fungal lesions of the mucous membranes, including thrush in women, oral candidiasis, etc. Fluconazole is widely used for nail and foot fungus, and in this case the drug also showed high efficiency.
Negative reviews about the drug due toa large number of side effects that develop on the background of its reception. As the most frequent reactions, people note headaches, dyspeptic disorders, excessive drowsiness and dizziness. Often, patients experienced digestive disorders in the form of flatulence and constipation.
