Fluconazole Polfarmex: composition and pharmaceutical form
Fluconazole Polfarmex comes as tablets containing 50 mg, 100 mg or 150 mg of fluconazole. The tablets are swallowed whole, independently of food.
The different strengths correspond to different tasks: 150 mg is most often a single dose or a weekly dose, while 50 and 100 mg are the strengths for daily courses. Fluconazole also exists as a solution for intravenous administration and, for children who cannot swallow a tablet, a syrup is made; when switching from intravenous administration to oral and back the dose does not need to be changed.
How Fluconazole Polfarmex works
Fluconazole is a synthetic antifungal medicine from the third-generation azole group. It disrupts the biosynthesis of ergosterol, because of which the permeability of the fungal cell membrane changes, the coordination of chitin synthesis is upset and the fungal cell dies.
From the gastrointestinal tract the medicine is absorbed quickly and independently of food, and the maximum plasma concentration is reached after 1–2 hours. In saliva, in joint and peritoneal fluid and in vaginal secretions the concentration is close to that in plasma — this explains why the medicine works in infections of the most varied sites. Fluconazole is eliminated mainly with the urine, and its half-life is about 30 hours. At doses of 50 to 400 mg a day it does not affect the level of testosterone and cortisol in men or of oestradiol in women.
Indications
In adults the medicine is prescribed in cryptococcal meningitis, coccidioidomycosis, invasive candidiasis, candidiasis of the mucous membranes — of the pharynx, of the oesophagus — in candiduria and chronic candidiasis of the skin and mucous membranes, and in chronic atrophic candidal stomatitis associated with wearing dentures, when oral hygiene and local treatment are not enough. It is also used in acute and recurrent vaginal candidiasis and candidal balanitis, when local treatment is insufficient, in dermatomycoses — of the feet, the trunk, the legs — in pityriasis versicolor and candidiasis of the skin, and also in onychomycosis, if other medicines are judged unsuitable.
A separate group of indications is prevention: of recurrences of cryptococcal meningitis in patients at high risk, of recurrences of candidiasis of the mucosa of the mouth, pharynx and oesophagus in people with HIV, of recurrences of vaginal candidiasis with four or more episodes a year, and of fungal infections in patients with prolonged neutropenia. Children and adolescents aged 3 to 17 are prescribed the medicine in candidiasis of the mucous membranes, invasive candidiasis and cryptococcal meningitis, and also to prevent candidiasis when immunity is weakened. Treatment can be started before the culture results are received, but once they are in, therapy is adjusted.
Method of use and dosage
The dose is chosen according to the type and severity of the fungal infection. If repeated dosing is required, treatment is continued until the clinical and microbiological signs of active infection have gone: too short a course leads to a recurrence.
| Indication | Scheme for adults |
|---|---|
| Cryptococcal meningitis | 400 mg on the first day, then 200–400 mg a day, usually 6–8 weeks; in a life-threatening infection up to 800 mg a day |
| Prevention of recurrence of cryptococcal meningitis | 200 mg a day long-term |
| Coccidioidomycosis | 200–400 mg a day, from 11 to 24 months and longer |
| Invasive candidiasis | 800 mg on the first day, then 400 mg a day; in candidaemia — 2 weeks after the first negative culture |
| Candidiasis of the mouth and pharynx | 200–400 mg on the first day, then 100–200 mg a day, 7–21 days |
| Candidiasis of the oesophagus | 200–400 mg on the first day, then 100–200 mg a day, 14–30 days |
| Acute vaginal candidiasis, candidal balanitis | A single dose of 150 mg |
| Recurrent vaginal candidiasis | 150 mg on days 1, 4 and 7, then 150 mg once a week for 6 months |
| Dermatomycoses of the feet, trunk and legs, candidiasis of the skin | 150 mg once a week or 50 mg a day, 2–4 weeks (in athlete's foot up to 6 weeks) |
| Onychomycosis | 150 mg once a week until the healthy nail has fully grown out: 3–6 months on the hands and 6–12 months on the feet |
Special groups of patients
In elderly patients the dose is adjusted according to kidney function. With a single dose it does not need changing, and with repeated dosing one starts with a loading dose of 50–400 mg depending on the indication, after which, with a creatinine clearance above 50 ml/min the full recommended dose is given, with a clearance of 50 ml/min or below without dialysis half the dose is given, and patients on regular dialysis are given the full dose after every session. In pityriasis versicolor another regimen is also possible: 300–400 mg once a week for 1–3 weeks. Prevention in patients with neutropenia is started a few days before it is expected to develop and continued for 7 days after the neutrophil count has risen above 1000 per mm³.
Contraindications
The medicine is contraindicated in hypersensitivity to its components.
In addition, use in pregnancy is permissible only when, in the doctor's opinion, the benefit to the mother outweighs the potential risk to the foetus, and during breastfeeding its use is not recommended. Separate attention is required by the combination with a number of medicines — their list is given below.
Special warnings and precautions
Particular caution is needed in patients in a severe general condition — for example with AIDS or an oncological disease. In them disturbances of liver and kidney function arise more often, as do haematological and biochemical abnormalities.
In such cases it is recommended to monitor the activity of the aminotransferases and of alkaline phosphatase, the bilirubin level and also the parameters of kidney function — the serum concentration of creatinine and of urea nitrogen. Monitoring is especially important in patients with renal failure, since fluconazole is eliminated predominantly by the kidneys in unchanged form.
Drug interactions
Fluconazole inhibits the metabolism of oral glucose-lowering medicines and enhances their action: this concerns tolbutamide, glibenclamide, glipizide and other sulfonylurea derivatives. It also enhances the action of anticoagulants and raises the concentration of phenytoin and theophylline and, in large doses, of ciclosporin in the plasma as well.
An increase in the concentration of terfenadine, astemizole and cisapride is possible. The influence works in the opposite direction too: rifampicin speeds up the metabolism of fluconazole and reduces its efficacy, while hydrochlorothiazide, on the contrary, raises the plasma concentration of fluconazole. All these combinations require medical assessment and sometimes an adjustment of the doses.
Pregnancy and breastfeeding
During pregnancy the medicine may be used only if, in the doctor's opinion, the benefit to the mother outweighs the potential risk to the foetus. This means that the routine treatment of uncomplicated fungal infections is postponed for the duration of the pregnancy or replaced with local preparations, and the decision is taken by the doctor.
During breastfeeding the use of fluconazole is not recommended. If treatment is nevertheless necessary, the question of continuing to feed is settled individually with the doctor.
Adverse effects
The most frequent are nausea, headache, rash, vomiting, abdominal pain, diarrhoea and a transient rise in the activity of the liver enzymes.
- in isolated cases — severe disorders of the liver: hepatitis, cholestatic jaundice, fulminant liver failure with a fatal outcome;
- fatal liver failure was seen above all in patients with AIDS or oncological diseases, and also with the concomitant use of other potentially hepatotoxic medicines — rifampicin, phenytoin, isoniazid, valproic acid and glucose-lowering sulfonylurea derivatives;
- very rare — anaphylactic reactions;
- isolated reports — fever, oedema, oliguria, a fall in blood pressure, muscle pain, epileptic seizures;
- isolated reports — exfoliative diseases of the skin;
- isolated reports — changes in the blood picture: leucopenia and thrombocytopenia;
- isolated reports — changes in the lipid profile: hypertriglyceridaemia and hypercholesterolaemia, and also hypokalaemia.
In women who took a single 150 mg dose, headache and dizziness, nausea, abdominal pain, diarrhoea, dyspepsia and disturbances of taste were noted. All these reactions were mild or moderate.
Overdose
Treatment of an overdose is symptomatic, with support of the vital functions. In justified cases gastric lavage is carried out.
Fluconazole is well removed by haemodialysis: a three-hour session reduces the plasma concentration of the medicine by about 50%. If an overdose is suspected, medical help must be sought at once.
How to get a prescription for Fluconazole Polfarmex online
Fluconazole is dispensed on prescription: the dose and the length of the course differ greatly depending on which infection is involved — from one tablet in acute vaginal candidiasis to several months of treatment in onychomycosis.
During the online consultation the doctor will establish the nature and site of the infection, any concomitant illnesses and the medicines being taken and, if there are no contraindications, will issue an electronic prescription — the medicine can be collected from a pharmacy using its code.
