Description
INDICATIONS:
Local treatment of vulvovaginal mycosis either accompanied with superinfection with gram positive bacteria or not.
CONTRAINDICATIONS:
- Hypersensibility to one of the product’s components, (or against one of imidazole derivatives).
- Use with latex diaphragm.
WARNINGS:
- In the absence of clinical symptomatic evidence, the observation of candida only on the skin or mucosa is not considered an indication.
- If candidiasis is confirmed, there is a need to search for the ecological factor which stimulates the development of candida.
To avoid relapse, it is necessary to eradicate and suppress the stimulating factors.
- It is desirable to simultaneously treat candidal partners and known pathogens.
PRECAUTIONS:
- In case of local intolerance or allergic reactions, discontinue treatment.
- It is not recommended to use acidic soap (pH is a stimulant of candida multiplication).
DRUG INTERACTIONS:
- Avoid using with latex diaphragm, it may cause rupture.
- Spermicides: the local vaginal treatment is always capable of inactivating the local spermicidal contraceptives.
PREGNANCY & LACTATION:
Pregnancy:
Animal studies have not shown any evidence of teratogenic effect. Since there is no evidence of teratogenic effect in animals, the malformation effect in humans is not expected. An effect due to substances responsible for malformation in humans itself proved to be teratogenic in animals in the course of studies is the same in both species. Clinically, any individual malformation or fetotoxic effect did not appear. However, it is inadequate to use econazole during pregnancy.
In consequence, vaginal econazole should be used during pregnancy only when necessary.
Lactation:
The absorption of econazole nitrate through the vaginal mucosa is week; consequently, lactation is possible during treatment with BENEZOLE ovules.
SIDE EFFECTS:
The more frequent reported side effects in clinical trials are local reactions, such as burning sensation, irritation, pruritus and erythema.
Other rare side effects contain: contact dermatitis and an isolated case of erythematic eruptions or urticaria, the same effects have been also reported after marketing.
PHARMACODYNAMICS:
Anti-infectious and antiseptic in gynecological use (genito-urinary system and sexual hormones).
Econazole nitrate is an imidazole derivative having an antifungal and antibacterial activity.
Its activity has been demonstrated in vitro and tested in patients with mucocutaneous mycosis:
- Candida and other yeasts (agents of vaginal mycosis),
- Gram positive bacteria sometimes inducing superinfection.
In vitro, the attempts of selecting the stump of resistant Candida Albicans against econazole is not considered an evidence of acquired resistance, in vitro, this risk is infinitesimal.
Mechanism of action:
Unlike other antibiotics, it is active in several levels: on membranes (increasing permeability), in cytoplasm (inhibiting the oxidative processes in the level of mitochondria), nuclear (inhibiting RNA synthesis).
The dosage should be adjusted in short term therapy.
PHAMACOKINETICS:
In humans, the absorbance of econazole nitrate is very weak after vaginal administration.
The maximum plasma or serum concentrations of econazole and/or its metabolites are observed after 1 to 2 hours after administration which is approximately 65 ng/ml for each 150 mg ovule.
For each 150 mg ovule, approximately only 5% of the dose of econazole nitrate is absorbed.
In systemic circulation, econazole and/or its metabolites are >98% protein bound. Econazole is strongly metabolized by oxidation, disamination and/or O-disalkylation, and its metabolites are eliminated by renal and fecal excretion.
The excipients form a thin layer of adherent emulsion which allows the penetration of econazole nitrate in all the folds of the vaginal mucosa.
DOSAGE & ADMINISTRATION:
BENEZOLE 150 mg:
- In major cases: insert 1 ovule deeply in the vagina at bedtime, preferably while assuming a supine position, for 3 consecutive days.
- In other cases: in case of resistant or recurrent mycosis due to stimulating factors, a second course of treatment can be prescribed using 3 ovules either immediately after the first course, or after a free interval of 10 days.
BENEZOLE 50 mg:
- In major cases: insert 1 ovule deeply in the vagina at bedtime, preferably while assuming a supine position, for 15 consecutive days.
Practical advice:
- Use neutral or alkaline soap in toilet.
- The treatment should be accompanied with hygiene (underwear should be made of cotton, avoid vaginal douches, avoid using tampons during treatment …) and, to a possible extent, suppression of the stimulating factors.
- Do not interrupt the treatment during amelioration.
- The treatment of the partner should be discussed according to each individual case.
- For the extended vulval or perianal mycotic treatment, it is recommended to use local antifungal treatment.
HOW SUPPLIED:
- BENEZOLE 150: Boxes of 6 ovules.
- BENEZOLE 50: Boxes of 10 ovules.
STORAGE CONDITIONS:
Store at a temperature below 25°C, in a dry place.
