Neo-penotran forte l vaginal candles №7

Composition

1 suppository contains:

• Active substance
  • Metronidazole (micronized) - 750.0 mg.
  • Miconazole nitrate (micronized) - 200.0 mg.
  • Lidocaine - 100.0 mg.

Excipients

Witepsol - 1436.75 mg.

In a plastic blister 7 suppositories. In carton packaging 1 blister.

Indications and usage

• Vaginal candidiasis caused by Candida albicans.
• Bacterial vaginitis caused by anaerobic bacteria and Gardnerella vaginalis.
• Trichomonas vaginitis caused by Trichomonas vaginalis.
• Mixed vaginal infections.

The absorption of miconazole nitrate with intravaginal use is very small (approximately 1.4% of the dose). Miconazole nitrate can be determined in plasma for three days after the intravaginal administration of the suppositories Neo-Penotran Forte-L.

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  • Suction and distribution

The bioavailability of Metronidazole with intravaginal administration is 20% compared with oral administration. The equilibrium plasma concentration of metronidazole is 1.1-5.0 mcg / ml after daily intravaginal administration of the suppositories Neo-Penotran Forte-L for three days.

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  • Metabolism and excretion

Metronidazole is metabolized by the liver through oxidation. The main metabolites of metronidazole are hydroxy derivatives and acetic acid compounds are excreted by the kidneys. The biological activity of hydroxy metabolites is 30% of the biological activity of metronidazole. The half-life of metronidazole is 6-11 hours. After oral or intravenous administration of metronidazole, 60-80% of the dose is eliminated by the kidneys (about 20% - unchanged, and in the form of metabolites).

Lidocaine

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  • Suction and distribution

The action begins in 3-5 minutes. Lidocaine is absorbed by superficial application to damaged skin and mucous membranes and is rapidly metabolized in the liver.

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  • Metabolism and excretion

Metabolites and drug in unchanged form (10% of the administered dose) are eliminated through the kidneys. After daily intravaginal administration of the suppositories Neo-Penotran Forte-L for three days, lidocaine is absorbed in a minimum amount, and its plasma levels are 0.04–1 μg / ml.

Clinical Pharmacology

Suppositories Neo-Penotran Forte-L contain miconazole, which has antifungal effects, metronidazole, which has antibacterial and antitrihomonadnoe effects, as well as lidocaine, which gives a local anesthetic effect.

• Miconazole

It is a synthetic imidazole derivative, has antifungal activity and has a wide spectrum of action. Especially effective against pathogenic fungi, including Candida albicans.In addition, miconazole is effective against gram-positive bacteria. The action of miconazole is the synthesis of ergosterol in the cytoplasmic membrane. Miconazole alters the permeability of the mycotic cells of Candida species, and inhibits glucose consumption in vitro.

• Metronidazole

A derivative of 5-nitroimidazole, it 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, including anaerobic streptococci. Miconazole and metronidazole do not have a synergistic or antagonistic effect while taking.

• Lidocaine

Stabilizes the neural membrane, inhibiting ion fluxes necessary for the occurrence and conduction of impulses, thereby providing a local anesthetic effect.

Pregnancy and Breastfeeding

• Pregnancy

Metronidazole and lidocaine belong to category B, miconazole - to category C. After the first trimester, Neo-Penotran Forte-L can be used under the supervision of a physician in cases where the intended benefit outweighs the potential risk to the fetus.

• Lactation

Breastfeeding should be discontinued, as metronidazole passes into breast milk. Feeding can be resumed within 24-48 hours after the end of treatment. It is not known whether lidocaine penetrates into breast milk.A nursing woman should take lidocaine with caution.

Contraindications

• Hypersensitivity to the drug.
• First trimester of pregnancy.
• Porphyria.
• Epilepsy.
• Severe abnormal liver function.

• 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.

• Systemic side effects

The frequency of systemic side effects is very low, because with the vaginal application of metronidazole contained in the vaginal suppositories of Neo-Penotran Forte-L, the concentration of metronidazole in plasma is very low (2-12% compared with oral administration).

• maybe

Miconazole nitrate, like all other antifungal agents based on imidazole derivatives that are inserted into the vagina, can irritate the vagina (burning, itching) (2-6%). Such symptoms can be eliminated by the local anesthetic effect of lidocaine. In case of severe irritation, treatment should be discontinued.

• In extremely rare cases

The side effects caused by the systemic use of metronidazole include hypersensitivity reactions (rarely), leukopenia, ataxia, psycho-emotional disorders, peripheral neuropathy in overdose and prolonged use, convulsions; diarrhea (rare), constipation, dizziness, headache, loss of appetite, nausea,vomiting, pain or cramping in the abdominal cavity, change in taste (rarely), dry mouth, metallic or unpleasant taste, increased fatigue.

These side effects occur in extremely rare cases, since blood levels of metronidazole with intravaginal use are very low.

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

Alcohol: disulfiram-like reactions.

Peroral anticoagulants: increased anticoagulant effect.

Phenytoin: an increase in the level of phenytoin and a decrease in the level of metronidazole in the blood.

Phenobarbital: a decrease in blood levels of metronidazole.

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

Cimetidine: may increase the level of metronidazole in the blood and, consequently, increase the risk of neurological side effects.

Lithium: lithium toxicity may increase.

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

There is an effect on blood levels of liver enzymes, glucose (as measured by the hexokinase method), theophylline, and procainamide.

Overdosage

• Symptoms of an overdose of metronidazole: nausea, vomiting, abdominal pain, diarrhea, itching, metallic taste in the mouth, Ataxia, Paresthesia convulsions, leukopenia, dark urine.
• Symptoms in case of overdose of miconazole nitrate: nausea, vomiting, dryness in the larynx and mouth, Anorexia headache, diarrhea.
• Treatment: in case of accidental ingestion of a large dose of the drug, if necessary, you can do a gastric lavage. No special antidote; applied symptomatic treatment. Treatment should be prescribed to individuals taking a dose of 12 g of metronidazole.

Unless otherwise recommended by the doctor, 1 suppository is administered deep into the vagina overnight for 7 days.

Suppositories should be inserted in the supine position deep in the vagina using the enclosed disposable fingertips.

• With recurrent disease or vaginitis resistant to other treatment

It is recommended to extend the course of treatment to 14 days.

Not recommended for use in children and virgins.

Alcohol intake should be avoided during treatment and, at least, within 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 convulsions.

Care should be taken 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.

• With renal failure

The dose of metronidazole should be reduced.

• With abnormal liver function

In severe hepatic impairment, clearance of metronidazole may be impaired. Metronadizol can cause symptoms of encephalopathy due to elevated plasma levels and therefore should be used with caution in patients with hepatic encephalopathy. In patients with hepatic encephalopathy, the daily dose of metronidazole should be reduced to 1/3. In patients with reduced liver function, the half-life of lidocaine may increase by two or more times.

• Decreased kidney function

It does not affect the pharmacokinetics of lidocaine, but may cause accumulation of metabolites.

• Influence on ability to driving of the car and control of mechanisms Suppositories Neo-Penotran Forte-L do not affect the ability to drive and work with mechanisms.

• Store at a temperature not higher than 25 ° С. Do not store in the refrigerator.