Neo - penotran forte L vaginal suppositories, No. 7

vaginal candidiasis caused by Candida albicans ;

bacterial vaginitis caused by anaerobic bacteria and Gardnerella vaginalis ;

Trichomonas vaginitis caused by Trichomonas vaginalis ;

mixed vaginal infections.

Intravaginally. Suppositories should be inserted in the supine position, deep into the vagina.

Unless otherwise recommended by a doctor, 1 supp. injected deep into the vagina at night for 7 days.

In case of recurrent disease or vaginitis resistant to other treatment, it is recommended to extend the course of treatment up to 14 days.

Vaginal suppositories 1 supp.

active substances:

metronidazole (micronized) 750 mg

miconazole nitrate (micronized) - 200 mg

lidocaine - 100 mg

excipients: witepsol - 1436.75 mg

hypersensitivity to the components of the drug;

I trimester of pregnancy;

porphyria;

epilepsy;

severe liver dysfunction.

Composition:

Vaginal suppositories 1 supp.

active substances:

metronidazole (micronized) 750 mg

miconazole nitrate (micronized) - 200 mg

lidocaine - 100 mg

excipients: witepsol - 1436.75 mg

Description of the dosage form

Vaginal suppositories in the form of a flat body with a rounded end, from white to slightly yellowish.

pharmachologic effect

Pharmacological action - local anesthetic, antifungal, antiprotozoal, antimicrobial .

Pharmacodynamics

Suppositories Neo-PenotranЃ Forte L contain miconazole, which has an antifungal effect, metronidazole, which has an antibacterial and antichomonas effect, and lidocaine, which has a local anesthetic effect.

Miconazole, a synthetic imidazole derivative, has antifungal activity and a broad spectrum of action. It is especially effective against pathogenic fungi including Candida albicans . In addition, miconazole is effective against gram-positive bacteria. Miconazole works by synthesizing ergosterol in the cytoplasmic membrane. Miconazole alters the permeability of mycotic cells of Candida species and inhibits in vitro glucose uptake .

Metronidazole, a derivative of 5-nitroimidazole, is an antiprotozoal and antibacterial agent effective against several infections caused by anaerobic bacteria and protozoa such as Trichomonas vaginalis, Gardnerella vaginalis and anaerobic bacteria, incl. anaerobic streptococci. Miconazole and metronidazole do not have a synergistic or antagonistic effect when taken simultaneously.

Lidocaine stabilizes the neural membrane by inhibiting the ionic fluxes required for the emergence and conduction of impulses, thereby providing a local anesthetic effect.

Pharmacokinetics

Miconazole nitrate: the absorption of miconazole nitrate with intravaginal administration is very low (approximately 1.4% of the dose). Miconazole nitrate can be determined in plasma within 3 days after intravaginal administration of Neo-PenotranЃ Forte L. suppositories.

Metronidazole: The bioavailability of metronidazole with intravaginal administration is 20% compared to oral administration. Css of metronidazole in plasma is 1.1Ц5 ?g / ml after daily intravaginal administration of Neo-PenotranЃ Forte L suppositories for 3 days. Metronidazole is metabolized in the liver by oxidation. The main metabolites of metronidazole - hydroxy derivatives and acetic acid compounds - are excreted by the kidneys. The biological activity of hydroxymetabolites is 30% of the biological activity of metronidazole. T1 / 2 of metronidazole is 6-11 hours. After oral or intravenous administration of metronidazole 60-80% of the dose is excreted by the kidneys (about 20% - unchanged and in the form of metabolites).

Lidocaine: the action begins in 3-5 minutes. Lidocaine is absorbed when applied superficially to damaged skin and mucous membranes and is rapidly metabolized in the liver. The metabolites and the drug in unchanged form (10% of the administered dose) are excreted through the kidneys. After daily intravaginal administration of suppositories Neo-PenotranЃ Forte L for 3 days, lidocaine is absorbed in a minimal amount, and its plasma levels are 0.04Ц1 ?g / ml.

Indications of the drug

vaginal candidiasis caused by Candida albicans ;

bacterial vaginitis caused by anaerobic bacteria and Gardnerella vaginalis ;

Trichomonas vaginitis caused by Trichomonas vaginalis ;

mixed vaginal infections.

Contraindications

hypersensitivity to the components of the drug;

I trimester of pregnancy;

porphyria;

epilepsy;

severe liver dysfunction.

Application during pregnancy and lactation

Metronidazole and lidocaine - category B, miconazole - category C.

After the first trimester of pregnancy, Neo-PenotranЃ Forte L can be used under medical supervision in cases where the intended benefit outweighs the potential risk to the fetus.

Breastfeeding should be discontinued as metronidazole passes into breast milk. Feeding can be resumed 24Ц48 hours after the end of treatment. It is not known whether lidocaine passes into breast milk. Lidocaine should be used with caution in a nursing woman.

Side effects

In rare cases, hypersensitivity reactions (skin rashes) and side effects such as abdominal pain, headache, vaginal itching, burning and irritation of the vagina are observed.

The incidence of systemic side effects is very low, since with the vaginal use of metronidazole contained in Neo-PenotranЃ Forte L vaginal suppositories, the plasma metronidazole concentration is very low (2Ц12% compared to oral administration). Miconazole nitrate, like all other antifungal agents based on imidazole derivatives that are injected into the vagina, can irritate the vagina (burning, itching - 2Ц6%). Such symptoms can be eliminated by the local anesthetic action of lidocaine. In case of severe irritation, treatment should be discontinued.

Side effects caused by systemic use of metronidazole include hypersensitivity reactions (rarely), leukopenia, ataxia, psychoemotional disorders, peripheral neuropathy in case of overdose and prolonged use, convulsions; diarrhea (rare), constipation, dizziness, headache, loss of appetite, nausea, vomiting, abdominal pain or cramps, change in taste (rare), dry mouth, metallic or unpleasant taste, fatigue. These side effects occur in extremely rare cases, since the blood levels of metronidazole with intravaginal use are very low.

Interaction

As a result of the absorption of metronidazole, the following interactions may occur.

Alcohol: disulfiram-like reactions.

Oral anticoagulants: enhancement of the anticoagulant effect.

Phenytoin: Increased phenytoin levels and decreased blood levels of metronidazole.

Phenobarbital: a decrease in the level of metronidazole in the blood.

Disulfiram: possible changes in the central nervous system (for example, mental reactions).

Cimetidine: it is possible to increase the level of metronidazole in the blood and, therefore, to increase the risk of neurological side effects.

Lithium: Potentially increased toxicity of lithium.

Astemizole and terfenadine: metronidazole and miconazole inhibit the metabolism of these compounds and increase their plasma concentration.

There is an effect on the level in the blood of liver enzymes, glucose (when determined by the hexokinase method), theophylline and procainamide.

Method of administration and dosage

Intravaginally. Suppositories should be inserted in the supine position, deep into the vagina.

Unless otherwise recommended by a doctor, 1 supp. injected deep into the vagina at night for 7 days.

In case of recurrent disease or vaginitis resistant to other treatment, it is recommended to extend the course of treatment up to 14 days.

Overdose

Symptoms: in case of an overdose of metronidazole - nausea, vomiting, abdominal pain, diarrhea, itching, metallic taste in the mouth, ataxia, paresthesia, convulsions, leukopenia, dark urine; with an overdose of miconazole nitrate - nausea, vomiting, dryness in the larynx and mouth, anorexia, headache, diarrhea.

Treatment: prescribed to persons who have taken a dose of 12 g of metronidazole. In case of accidental ingestion of a large dose of the drug, gastric lavage can be performed if necessary; symptomatic treatment is carried out. There is no specific antidote.

special instructions

Not recommended for use in children and virgins.

It is necessary to avoid alcohol intake during treatment and at least for 24-48 hours after the end of the course due to possible disulfiram-like reactions. Large doses and long-term systematic use of the drug can cause peripheral neuropathy and seizures. Caution should be exercised when using suppositories simultaneously with contraceptive diaphragms and condoms due to the possible interaction of rubber with the suppository base.

In patients with a diagnosis of Trichomonas vaginitis, simultaneous treatment of the sexual partner is necessary.

In renal failure, the dose of metronidazole should be reduced. With serious violations of liver function, the clearance of metronidazole may be impaired. Metronidazole can cause symptoms of encephalopathy due to elevated plasma levels and should therefore be used with caution in patients with hepatic encephalopathy (the daily dose of metronidazole should be reduced to 1/3).

In patients with reduced liver function, the T1 / 2 of lidocaine may increase by 2 or more times. Decreased renal function does not affect the pharmacokinetics of lidocaine, but may cause accumulation of metabolites.

Preclinical safety data. Preclinical studies of safety, pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, reproductive toxicity have not identified a potential risk to humans.

Influence on the ability to drive a car and control complex mechanisms. Neo-PenotranЃ Forte L suppositories do not affect the ability to drive and operate machinery.

Release form

Vaginal suppositories. 7 supp. in a plastic blister. 1 blister is placed in a cardboard box.

Conditions of dispensing from pharmacies

On prescription.

Storage conditions

At a temperature not exceeding 25 ? C.

Keep out of the reach of children.

Shelf life

3 years.

Do not use after the expiration date printed on the package.