| Chemical Composition & Mechanisms of action |
Each Micoprogel Vaginal Pessary Contains:
Metronidazole 500 mg
Miconazole Nitrate 100 mg
Mechanisms of action:
- Miconazole nitrate which is a synthetic imidazole antifungal agent has a wide spectrum of activity and is particularly effective against pathogenic fungi, including Candida albicans. In addition, Miconazole nitrate is effective against gram-positive bacteria. Miconazole nitrate shows its effect by ergosterol synthesis in the cytoplasmic membrane. Miconazole nitrate changes permeability of the mycotic cell of Candida sepcies. and inhibits glucose utilization in vitro.
- Metronidazole, a 5-nitroimidazole derivative, is an antiprotozoal and antibacterial agent effective against several infections caused by anaerobic bacteria and protozoa e.g., Trichomonasvaginalis, Gardnerellavaginalis and anaerobic bacteria including anaerobic Streptococci.
Miconazole and Metronidazole have no synergistic or antagonistic effect when administered concomitantly.
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| Pharmacokinetics |
Absorption of miconazole nitrate through the intravaginal route is very low. Bioavailability of metronidazole by this route is 20% compared to the oral route. Miconazole nitrate could not be detected in plasma after vaginal application.
Metronidazole is metabolized in the liver by oxidation. The half-life of metronidazole is 6-11 hours.
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| Indications |
Vaginal Pessaries are used for:
Treatment of vaginal candidias is caused by Candida albicans, bacterial vaginitis caused by anaerobic bacteria and Gardnerella vaginalis, trichomonal vaginitis caused by Trichomonas vaginalis and mixed vaginal infections.
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| Contraindications |
Known hypersensitivity to any active ingredients or derivatives of this drug and during the 1st trimester of pregnancy. Patients with serious liver function disorders, epilepsy and porphyria.
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| Precautions |
Patients should be warned not to take alcohol during the therapy and for at least 2 days after the end of a course of treatment because of the possibility of disulfiram-like reactions. High doses and long-term systemic use may cause peripheral neuropathy and convulsion.
The base contained in the vaginal Pessaries formulation may interact with certain rubber or latex products e.g., those used in vaginal contraceptive diaphragms or condoms, therefore concurrent use is not recommended.
Sexual partners of patients with Trichomonas vaginalis should be treated at the same time.
Metronidazole dose must be reduced in renal failure. In serious liver function failures, Metronidazole clearance may be impaired. Metronidazole may increase encephalopathy symptoms due to increased plasma levels and therefore should be used carefully in hepatic encephalopathy patients. The daily dose of Metronidazole must be reduced to 1/3 in patients with hepatic encephalopathy.
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| Side Effects |
- Vaginal Disorders: Vaginal irritation (burning, itching). Owing to the inflammation of the vaginal mucosa in vaginitis. These complaints disappear quickly when the treatment continues. If there is severe irritation, treatment should be discontinued.
- Gastrointestinal Disorders: Abdominal pain, metallic taste, constipation, dry mouth, seldom diarrhea, lack of appetite, vomiting, nausea, tiredness.
- Nervous System Disorders: Headache, dizziness, mental changes, ataxia, convulsion, peripheral neuropathy after overdose or long period of usage.
- Skin Disorders: Hypersensitivity reactions.
- Blood Disorders: Leucopenia.
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| Drug Interactions |
Due to Metronidazole absorption, interactions may be seen if used concomitantly with any of the following drugs:
- Alcohol intolerance (disulfiram-like reaction).
- Oral Anticoagulants: Increase in the anticoagulant effect.
- Phenytoin: Increase in phenytoin blood levels, decrease in Metronidazole blood levels.
- Phenobarbital: Decrease in Metronidazole blood levels.
- Cimetidine: Metronidazole blood levels and the risk of neurologic side effects may increase.
- Disulfiram :Some effects (psychotic reactions) related to the central nervous system may occur.
- Lithium :Increase in Lithium toxicity can be observed.
- Interference with blood levels of liver enzymes, glucose, theophylline, andprocainamide have been observed.
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| Use in pregnancy & lactation |
Pregnancy:
Pregnancy Category B for Metronidazole and pregnancy category C for Miconazole. After the 1st trimester of pregnancy, This drug may be used in cases considered essential by a physician, but should be used under control.
Breastfeeding :
Breastfeeding should be discontinued since Metronidazole appears in the mother milk. It can be started again 24-48 hrs after the end of treatment.
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| Dosage |
Micoprogel :
It should applied in lying position.
Unless advised otherwise by a physician, insert 1 Pessary at night for 14 days. Or 1 pessary at night and 1 pessary in the morning for 7 days.
In recurrent cases, or when vaginitis has resisted other treatments, 1 Pessary should be inserted at night and in the morning for 14 days.
For elderly patients (over 65 years): As for younger adults.
Children : Not recommended for children.
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| Overdosage |
Symptoms: Due to Metronidazole : Nausea, vomiting, abdominal pain, diarrhea, pruritus, metallic taste, ataxia, vertigo, paresthesia, convulsion, leukopenia and darkening of urine.
Due to Miconazole Nitrate: Nausea, vomiting, anorexia, headache and diarrhea, sore throat and mouth. |
| Treatment |
| If accidental ingestion of large quantities of this drug occurs, an appropriate method of gastric emptying may be considered if necessary. There exist no specific antidote, symptomatic treatment can be applied. Cure can be provided in persons who ingested a dose of Metronidazole 12g. |
| Presentation |
| Micoprogel : Carton box contains 14 vaginal pessaries with a leaflet. |
| Storage |
Micoprogel – fort : Store at temperature below 25 °C.
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