Neo-Penotran forte L, supp vagina. No. 7 (Embil Pharmaceutical CO LTD, Türkiye)
Compound.
| active substances: | |
| Metronidazole (micronized) | 750 mg |
| miconazole nitrate (micronized) | 200 mg |
| lidocaine | 100 mg |
| excipients: vitepsol - 1436.75 mg |
Description of the dosage form.
Vaginal suppositories are flat-shaped with a rounded end, white to slightly yellowish in color.
Pharmachologic effect. Antiprotozoal, antimicrobial, antifungal, local anesthetic.
Pharmacodynamics.
Neo-Penotran® Forte L suppositories contain miconazole, which has an antifungal effect, metronidazole, which has an antibacterial and antitrichomoniacal effect, as well as lidocaine, which has a local anesthetic effect.
Miconazole,
which is a synthetic derivative of imidazole, has antifungal activity and has a wide spectrum of action.
Particularly 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 cell of Candida species
and inhibits glucose uptake
in vitro
.
Metronidazole,
which is a 5-nitroimidazole derivative, 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 together.
Lidocaine
stabilizes the neuronal membrane, inhibiting the ionic currents necessary for the occurrence and conduction of impulses, thereby providing a local anesthetic effect.
Pharmacokinetics.
Miconazole nitrate:
The absorption of miconazole nitrate when administered intravaginally is very small (approximately 1.4% of the dose). Miconazole nitrate can be detected in plasma for 3 days after intravaginal administration of Neo-Penotran® Forte L suppositories.
Metronidazole:
the bioavailability of metronidazole when administered intravaginally is 20% compared to oral administration. Css of metronidazole in plasma is 1.1–5 μg/ml after daily intravaginal administration of Neo-Penotran® 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 within 3–5 minutes. Lidocaine is absorbed when applied superficially to damaged skin and mucous membranes and is quickly metabolized in the liver. Metabolites and the drug in unchanged form (10% of the administered dose) are excreted through the kidneys. After daily intravaginal administration of Neo-Penotran® Forte L suppositories for 3 days, lidocaine is absorbed in minimal quantities, and its plasma levels are 0.04–1 mcg/ml.
Indications.
● 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.
Use during pregnancy and breastfeeding.
Metronidazole and lidocaine are category B, miconazole is category C.
After the first trimester of pregnancy, Neo-Penotran® Forte L can be used under medical supervision in cases where the expected benefit outweighs the potential risk to the fetus.
Breastfeeding should be stopped because... Metronidazole passes into breast milk. Feeding can be resumed 24–48 hours after the end of treatment. It is not known whether lidocaine passes into breast milk. A nursing woman should use lidocaine with caution.
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 have been observed.
The incidence of systemic side effects is very low, since with vaginal use of metronidazole contained in Neo-Penotran® Forte L vaginal suppositories, the concentration of metronidazole in plasma is very low (2-12% compared to oral administration). Miconazole nitrate, like all other antifungal agents based on imidazole derivatives that are introduced into the vagina, can cause vaginal irritation (burning, itching - 2-6%). Such symptoms can be relieved by the local anesthetic effect 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, psycho-emotional disorders, peripheral neuropathy in overdose and long-term use, convulsions; diarrhea (rare), constipation, dizziness, headache, loss of appetite, nausea, vomiting, abdominal pain or cramps, changes in taste (rare), dry mouth, metallic or unpleasant taste, increased fatigue. These side effects occur in extremely rare cases, since blood levels of metronidazole when used intravaginally are very low.
Interaction.
The following interactions may occur as a result of metronidazole absorption.
Alcohol:
disulfiram-like reactions.
Oral anticoagulants:
enhancing the anticoagulation effect.
Phenytoin:
increased levels of phenytoin and decreased levels of metronidazole in the blood.
Phenobarbital:
decrease in the level of metronidazole in the blood.
Disulfiram:
changes in the central nervous system (for example, mental reactions) are possible.
Cimetidine:
it is possible to increase the level of metronidazole in the blood and, therefore, increase the risk of neurological side effects.
Lithium:
possible increase in lithium toxicity.
Astemizole and terfenadine:
Metronidazole and miconazole inhibit the metabolism of these compounds and increase their plasma concentrations.
There is an effect on the blood levels of liver enzymes, glucose (when determined by the hexokinase method), theophylline and procainamide.
Method of administration and dose.
Intravaginally.
Suppositories should be inserted in a lying position, deep into the vagina.
Unless otherwise recommended by your doctor, 1 supp. inserted deep into the vagina at night for 7 days.
For recurrent disease or vaginitis resistant to other treatment, it is recommended to extend the course of treatment to 14 days.
Overdose.
Symptoms:
in case of metronidazole overdose - nausea, vomiting, abdominal pain, diarrhea, itching, metallic taste in the mouth, ataxia, paresthesia, convulsions, leukopenia, darkening of urine; with an overdose of miconazole nitrate - nausea, vomiting, dryness in the larynx and mouth, anorexia, headache, diarrhea.
Treatment:
is 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 done if necessary; symptomatic treatment is carried out. There is no special antidote.
Special instructions.
Use in children and virgins is not recommended.
Alcohol intake should be avoided during treatment and for at least 24–48 hours after completion 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 diagnosed with trichomonas vaginitis, simultaneous treatment of the sexual partner is necessary.
In case of renal failure, the dose of metronidazole should be reduced. In cases of severe liver dysfunction, the clearance of metronidazole may be impaired. Metronidazole may cause symptoms of encephalopathy due to elevated plasma levels and should therefore be used with caution in patients with hepatic encephalopathy (daily dose of metronidazole should be reduced to 1/3).
In patients with reduced liver function, 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, and reproductive toxicity have shown no potential risk to humans.
Influence on the ability to drive a car and control complex mechanisms.
Neo-Penotran® Forte L suppositories do not affect the ability to drive a car or operate machinery.
Release form.
Vaginal suppositories.
7 sup. in a plastic blister. 1 blister is placed in a cardboard box.
Manufacturer.
Embil Pharmaceutical Co. Ltd., Türkiye. Merkez Mahallesi Birakhane Juice. No. 28 Sisli 34381, Istanbul, Türkiye.
You can obtain additional information about the drug, as well as send your complaints and information about adverse events to the following address in Russia: Raifarm LLC, 127006, Moscow, st. Malaya Dmitrovka, 4, of. 8.
Tel., fax.
Conditions for dispensing from pharmacies.
On prescription.
Neo-Penotran forte-L supp vag 100 mg+750 mg+200 mg x7
ATX code: G01AF20 (Combinations of imidazole derivatives) Active substances metronidazole Rec.INN WHO registered miconazole Rec.INN WHO registered lidocaine Rec.INN WHO registered Dosage form NEO-PENOTRAN® FORTE L vaginal suppositories. 100 mg+750 mg+200 mg: 7 pcs. included with fingertips reg. No.: LP-000486 from 03/01/11 - Valid Release form, composition and packaging Vaginal suppositories in the form of a flat body with a rounded end, from white to slightly yellowish in color.
1 sup. metronidazole micronized 750 mg miconazole nitrate micronized 200 mg lidocaine 100 mg
Excipients: vitepsol S55 1436.75 mg.
7 pcs. — plastic blisters (1) complete with fingertips — cardboard packs.
Clinical-pharmacological group: Drug with antibacterial, antiprotozoal and antifungal action for topical use in gynecology Pharmaco-therapeutic group: Antimicrobial combined agent (antimicrobial and antiprotozoal agent + antifungal agent)
Indications: vaginal candidiasis caused by Candida albicans,
- bacterial vaginitis caused by anaerobic bacteria and Gardnerella vaginalis, trichomonas vaginitis caused by Trichomonas vaginalis,
- mixed vaginal infections.
ICD-10 codes ICD-10 code Indication A59 Trichomoniasis B37.3 Candidiasis of the vulva and vagina N76 Other inflammatory diseases of the vagina and vulva
Dosage regimen Unless otherwise recommended by your doctor, 1 suppository is inserted deep into the vagina at night for 7 days.
For recurrent disease or vaginitis resistant to other treatment, it is recommended to extend the course of treatment to 14 days.
Suppositories should be inserted in a lying position deep into the vagina using the disposable finger tips provided.
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 vaginal use of metronidazole contained in Neo-Penotran Forte-L vaginal suppositories, the concentration of metronidazole in plasma is very low (2-12% compared to oral administration).
Miconazole nitrate, like all other antifungal agents based on imidazole derivatives that are introduced into the vagina, can cause vaginal irritation (burning, itching) (2-6%). Such symptoms can be relieved by the local anesthetic effect 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 overdose and long-term use, convulsions, diarrhea (rarely), constipation, dizziness, headache, loss of appetite, nausea , vomiting, abdominal pain or cramps, changes in taste (rare), dry mouth, metallic or unpleasant taste, increased fatigue. These side effects occur in extremely rare cases, since blood levels of metronidazole when used intravaginally are very low.
Contraindications for use: first trimester of pregnancy,
- porphyria,
- epilepsy,
- severe liver dysfunction,
- hypersensitivity to the components of the drug.
Use during pregnancy and breastfeeding Metronidazole and lidocaine belong to category B, miconazole to category C. After the first trimester of pregnancy, Neo-Penotran Forte-L can be used under medical supervision in cases where the expected benefit outweighs the potential risk to the fetus.
Breastfeeding should be stopped because... Metronidazole passes into breast milk. Feeding can be resumed 24-48 hours after the end of treatment. It is not known whether lidocaine passes into breast milk. A nursing woman should take lidocaine with caution.
Use for liver dysfunction Contraindicated in severe liver failure.
In cases of severe liver dysfunction, the clearance of metronidazole may be impaired.
Metronidazole may cause symptoms of encephalopathy due to elevated plasma levels and should therefore be used with caution in patients with hepatic encephalopathy.
In patients suffering from 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 twofold or more.
Use for impaired renal function In case of renal failure, the dose of metronidazole should be reduced.
Decreased renal function does not affect the pharmacokinetics of lidocaine, but may cause accumulation of metabolites.
Use in children Not recommended for use in children Special instructions Not recommended for use in children and virgins.
It is necessary to avoid drinking alcohol during treatment and for at least 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 diagnosed with trichomonas vaginitis, simultaneous treatment of the sexual partner is necessary.
In case of renal failure, the dose of metronidazole should be reduced.
In cases of severe liver dysfunction, the clearance of metronidazole may be impaired.
Metronidazole may cause symptoms of encephalopathy due to elevated plasma levels and should therefore be used with caution in patients with hepatic encephalopathy.
In patients suffering from 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 twofold or more.
Decreased renal function does not affect the pharmacokinetics of lidocaine, but may cause accumulation of metabolites.
Impact on the ability to drive vehicles and operate machinery
Neo-Penotran Forte-L suppositories do not affect the ability to drive a car or operate machinery.
Preclinical safety data
Preclinical studies of safety, pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, and reproductive toxicity have shown no potential risk to humans.
Overdose Symptoms: nausea, vomiting, abdominal pain, diarrhea, itching, metallic taste in the mouth, ataxia, paresthesia, convulsions, leukopenia, darkening of urine. Symptoms of an overdose of miconazole nitrate are nausea, vomiting, dry larynx and mouth, anorexia, headache, diarrhea.
Treatment: in case of accidental ingestion of a large dose of the drug, gastric lavage can be done if necessary. There is no special antidote; symptomatic treatment is used. Treatment should be prescribed to persons who have taken a dose of 12 g of metronidazole.
Drug interactions As a result of absorption of metronidazole, the following interactions may occur:
Alcohol: disulfiram-like reactions.
Oral anticoagulants: enhanced anticoagulation effect.
Phenytoin: increased levels of phenytoin and decreased levels of metronidazole in the blood.
Phenobarbital: decreased levels of metronidazole in the blood.
Disulfiram: changes in the central nervous system (for example, mental reactions) are possible.
Cimetidine: There may be an increase in metronidazole blood levels and therefore an increased risk of neurological side effects. Lithium: Possible increased toxicity of lithium.
Astemizole and terfenadine: Metronidazole and miconazole inhibit the metabolism of these compounds and increase their plasma concentrations.
There is an effect on the blood levels of liver enzymes, glucose (when determined by the hexokinase method), theophylline and procainamide.
Conditions for dispensing from pharmacies The drug is dispensed with a prescription. Conditions and periods of storage Store the drug at a temperature not exceeding 25°C. Do not store in the refrigerator. Store in original packaging.
Keep out of the reach of children.
Shelf life: 2 years. Do not use after the expiration date
