The drug "Penotran Forte" is a medicine with antibacterial, antiprotozoal and antifungal properties for topical application. It is used in gynecology.
Also on sale you can find "Neo-Penotran Forte L". The composition of the medication contains lidocaine.
The composition and form of production
This medicine is produced in the form of vaginal suppositories with a rounded end, they are usually white. This medication has two active components: metronidazole and miconazole nitrate. One candle "Penotran Forte" contains 750 milligrams of metronidazole and 200 miconazole. The auxiliary ingredients are vitepsol and lidocaine. In each package, one blister is sold, in which there are seven candles.
Pharmacological effects
So, the considered drug "Penotran Forte" is a medicine with antibacterial, antiprotozoal and antifungal properties. It contains metronidazole, which has an antibacterial and antiprotozoal effect, and, in addition, miconazole, which is endowed with an antifungal effect.
The substance metronidazole is active against anaerobic bacteria and streptococcus. Miconazole nitrate has a wide range of effects. In particular, it is active against pathogenic fungi, including candida, and is also dangerous for gram-positive bacteria. The effect of miconazole is the synthesis of ergosterol in the cytoplasmic membranes. Miconazole changes the permeability of candida fungal cells, inhibiting glucose uptake.
Metronidazole, which is a derivative of the substance nitroimidazole, is considered an antiprotozoal and, at the same time, antibacterial agent that is effective against various infections caused by protozoa and anaerobic bacteria, including streptococci.
Miconazole along with metronidazole does not have synergistic or antagonistic properties when taken concurrently. Lidocaine stabilizes neural membranes and inhibits ion fluxes, which are necessary for the conduction and occurrence of impulses, thereby exerting a local anesthetic effect.
Pharmacokinetics
The absorption of miconazole nitrate as part of the intravaginal administration of Penotran Forte suppositories is very small and amounts to approximately one and a half percent of the dose. Miconazole nitrate can be determined in plasma within a few days (usually three) after intravaginal administration.
The bioavailability of metronidazole as part of intravaginal administration is twenty percent compared with oral administration. Equilibrium concentrations of metronidazole in blood plasma are from 1.1 to 5 micrograms per milliliter after daily intravaginal administration of suppositories for three days. Metronidazole is usually metabolized in the liver through an oxidation process. The main metabolites of metronidazole (acetic acid compounds) are released via the kidneys. The biological activity of metabolites is thirty percent of the biological effects of metronidazole. After oral or intravenous use of metronidazole, sixty to eighty percent of the dose is excreted by the kidneys (approximately twenty percent leave the body in unchanged form as metabolites).
As indicated by the instructions for use with Neo Penotran Forte candles, exposure to lidocaine begins after five minutes. Lidocaine, as a rule, is absorbed as a surface application to damaged skin and mucous membranes, this substance is metabolized very quickly (the metabolic process is carried out in the liver). Metabolites along with the drug in an unchanged form leave the body through the kidneys. After intravaginal daily administration of these suppositories for three days, lidocaine is absorbed in the very minimum amount, and its plasma level itself is from 0.03 to 1 microgram per milliliter.
Indications
In what cases is it advisable to use Neo Penotran Forte candles?
The presented therapeutic suppositories, as a rule, are prescribed to patients for use in the following diagnoses:
- The presence of vaginal candidiasis in a patient.
- The development of bacterial vaginosis.
- The occurrence of Trichomonas vaginitis.
- The appearance of vaginitis caused by a mixed infection.
Contraindications
But in the framework of the use of Penotran Forte suppositories, it is required to adhere to certain contraindications, they are as follows:
- The initial trimester of pregnancy.
- The patient has porphyria or epilepsy.
- The occurrence of severe violations of the liver.
- It is forbidden to use this drug for patients under the age of eighteen years due to a lack of information on the use in this age category.
- These candles are not suitable for use by virgins.
- The patient's sensitivity to the active ingredients of the drug or their derivatives.
Dosage
According to the instructions for the use of Neo Penotran Forte suppositories, the presented medicinal product is administered intravaginally, one at night for a week. With recurrent vaginitis resistant to other types of treatment, this remedy should be used for two weeks. Vaginal suppositories should be inserted deep into the vagina using the disposable fingertips contained in the package. For patients who are over sixty-five years old, dosage regimen adjustment is not required.
What else does the instructions for use with Penotran Forte tell us?
Side effects
In rare examples, reactions of excessive sensitivity (in the form of a skin rash) can be observed in combination with side effects such as abdominal pain along with vaginal itching, burning and irritation of the vagina.
Miconazole nitrate, like other antifungal agents based on imidazole derivatives introduced into the vagina, can cause irritation (usually this happens in six percent of cases). Due to the presence of inflammation of the vaginal mucosa during the development of vaginitis, irritation may intensify after the first suppository is inserted or by the third day of therapy. But such complications disappear very quickly during the continuation of treatment. If severe irritation occurs, therapy should be discontinued.
Systemic adverse reactions can occur very rarely, since with vaginal absorption, the amount of metronidazole in the blood plasma is very low. Adverse reactions that are associated with the systemic process of absorption of metronidazole include:
- The appearance of hypersensitivity (which is very rare).
- The occurrence of leukopenia, ataxia, changes in the psyche (in the form of anxiety and mood lability).
- Seizures, diarrhea, dizziness, and headache.
- Loss of appetite, along with nausea, vomiting, abdominal pain or cramping, a change in taste and constipation.
- Dry mouth in combination with a metallic taste is possible.
- Sometimes there is increased fatigue.
Overdose
There is no information about the overdose of “Penotran Forte” in humans as part of the intravaginal use of metronidazole. True, when these suppositories are introduced into the vagina, metronidazole is absorbed in an amount sufficient to cause a systemic effect. Symptoms of an overdose of metronidazole usually include the following manifestations:
- The occurrence of nausea, vomiting, and abdominal pain.
- The appearance of diarrhea and generalized itching.
- The presence of a metallic taste in the mouth.
- The appearance of motor disorders along with dizziness, paresthesia, convulsions and peripheral neuropathy.
- The development of leukopenia and dark urine.
It is worth noting that the symptoms of an overdose of metronidazole nitrate have not been identified. In case of ingestion of too much of the drug in question, gastric lavage can be performed if necessary. Improvement in the condition after this is achieved in individuals who have ingested up to 12 grams of metronidazole. The antidote for the drug does not exist. Doctors recommend symptomatic and supportive therapy in case of an overdose.
Drug interaction
Next, we consider the main nuances of the interaction of Neo-Penotran Forte L with other medicines and substances:
- The interaction of metronidazole with ethanol can cause a disulfiram-like reaction.
- With the simultaneous use of these suppositories with oral anticoagulants, an increase in anticoagulant effects is noted.
- With the combined use of these suppositories with phenytoin, a decrease in the concentration of metronidazole is noted with a simultaneous increase in the content of phenytoin.
- With simultaneous use with Phenobarbital, a decrease in the concentration of metronidazole is noted.
- When combined with Disulfiram, side effects from the nervous system are likely (usually psychotic reactions are observed in this case).
- With the simultaneous use of the presented candles with "Cimetidine" in the blood, the concentration of metronidazole increases, and, in addition, the risks of developing neurological adverse reactions increase.
- When using this medicine with lithium, an increase in the toxicity of the latter is observed.
- When combined with Astemizole and Terfenadine, miconazole and metronidazole, the metabolism of these substances is suppressed, and their plasma concentration also increases.
special instructions
Preclinical studies indicate the absence of any specific risk for the patient, based on the results of standard analyzes of pharmacology, safety, toxicity, genotoxicity, multiple dosages, carcinogenic potential and danger to the reproductive system. It is very important to avoid drinking alcohol during treatment or at least for two days after completing the course due to the possible development of disulfiram-like reactions.
In accordance with the instructions for use with Penotran Forte suppositories, caution should be exercised while using these suppositories with condoms and contraceptive diaphragms due to possible damage to the rubber base suppositories. For patients suffering from trichomonas vaginitis, simultaneous treatment of a sexual partner is required. The patient should be informed that the suppositories can not be swallowed or used in any other way.
It is possible to change the result as part of the determination of glucose, the level of the liver enzyme, procainamide and theophylline in the blood. The drug in question does not affect the patient’s ability to drive a car and operate machinery.
Instructions for use with Neo Penotran Forte must be strictly observed.
During pregnancy
Metronidazole along with lidocaine is classified as category B, and miconazole, in turn, is associated with category C. At the end of the initial trimester, Penotran Forte suppositories can be used under the supervision of a doctor in cases where the expected effectiveness exceeds the risks to the bearing fetus.
Breastfeeding should be stopped when using these suppositories, because metronidazole is able to penetrate into breast milk. Feeding can be continued twenty-four to forty-eight hours after the end of treatment. To date, it is still not established and it is not known whether lidocaine penetrates the composition of breast milk. Therefore, nursing women should take it with caution.
The use of "Neo Penotran Forte" in violation of the liver
It is worth noting that this medicine is strictly contraindicated in the presence of severe liver failure in the patient. In case of serious impairment of the functions of this organ, the clearance of metronidazole may worsen. Metronidazole can cause symptoms of encephalopathy due to its increased level in the blood plasma, and because of this it should be used with caution in patients suffering from hepatic encephalopathy.
In patients who suffer from hepatic encephalopathy, the daily dosage of metronidazole should be reduced to 1/3. In patients with impaired liver function, the half-life of lidocaine may increase two or more times.
This is confirmed by the instruction for candles "Penotran Forte."
In case of impaired renal function
In the presence of renal failure, the dosage of metronidazole should be necessarily reduced. Deterioration of renal function does not affect the pharmacokinetics of lidocaine, but can provoke the accumulation of metabolites.
Application in children and elderly
Patients who are under the age of eighteen years, due to insufficient information on the use of these candles in this age category should not be treated by them. For patients who are over sixty-five years of age, a dosage regimen adjustment is usually not required.
Storage conditions
The presented medicinal product is dispensed, as a rule, according to a medical prescription. According to the instructions, Penotran Forte should be stored in an inaccessible room (away from children) at a temperature that should not exceed twenty degrees. These suppositories are not stored in the refrigerator, and their shelf life is two years. Next, we find out what patients think about the use of these suppositories for treatment.
Reviews about Penotran Fort
About a medical tool on the Internet, you can read different reviews. Basically, patients respond well to this remedy and say that it effectively helps if patients have vaginal candidiasis, bacterial vaginosis or trichomonas vaginitis.
In addition, in the comments it is reported that this drug often helps women with the appearance of vaginitis caused by mixed infections.
Dissatisfaction with this medicine is associated with the manifestation of some side effects, the comments mostly mention diarrhea, dizziness and headache. It is also reported that sometimes, with the use of Penotran Forte for treatment, itching occurs in some women after the administration of suppositories.