Full Prescribing Info
Miconazole nitrate.
Each suppository also contains the following excipients: Witepol and polysorbate 80.
Pharmacology: Pharmacodynamics: Micotran contains miconazole nitrate, an imidazole derivative antifungal drug. Miconazole nitrate has a broad spectrum of activity and is particularly effective against pathogenic fungi and yeasts including Candida albicans. In addition, it is effective against gram-positive bacteria.
Miconazole nitrate shows its effect during ergosterol synthesis present on cell cytoplasmic membrane. Miconazole nitrate changes permeability of mycotic cell Candida species in vitro and inhibits the glucose consumption of the cell.
Pharmacokinetics: Absorption: Miconazole persists in the vagina for up to 72 hrs after a single dose. Systemic absorption of miconazole after intravaginal administration is limited, with a bioavailability of 1-2% following intravaginal administration of a 1.2 g dose. Plasma concentrations of miconazole are measurable within 2 hrs of administration in some subjects, with maximal levels seen 12-24 hrs after administration. Plasma concentrations decline slowly, thereafter and were still measurable in most subjects 96 hrs post-dose. Absorption of miconazole nitrate by the intravaginal route is very low (approximately 1.4% of dose).
Distribution: Following the insertion of vaginal suppository containing miconazole nitrate 1.2 g in a single dose, the average maximum serum concentration is 10.4 mcg/L, and the elimination half-life (t½) is 56.8 hrs. The average serum concentration-time curve has been calculated to be 967 mcg/L/hr. Protein-binding ratio is between 90% and 93%.
Biotransformation: It is metabolized in liver microsomally. There are no active metabolites. The major metabolite formed by oxidative-N-dealkylation is 2,4-diclorophenile-1 H imidazole ethanol and secondary metabolite is oxidative 2,4-dicloromandelic acid by O-dealkylation.
Elimination: Half-life is 24 hrs. Less than 1% is excreted in the urine. Approximately 50%, is usually excreted with feces as unchanged drug.
Single-dose treatment of vulvovaginal candidiasis. It should be used in the treatment of fungal infections of vagina especially originating from Candida, and fungal infections coexistent with Gram (+) bacteria (Staphylococcus, Streptococcus, and Micrococcus bacteria causing secondary infections) particularly.
Dosage/Direction for Use
One (1) suppository should be inserted high into the vagina only for 1 night before sleeping. It should not be used without consulting a physician. The application may be repeated after 3 days if it is thought to be necessary by the physician.
Elderly >65 years: Same dose for adults is administered.
Renal and Hepatic Impairment: Dose adjustment is not required in patients with renal and hepatic failure.
Administration: The suppository should be inserted high into the vagina in a resting position.
The suppository should not be ingested or taken by any other route.
If accidental ingestion of large quantities of Micotran occurs, an appropriate method of gastric lavage should be applied. There is no specific antidote; symptomatic treatment is applied. Burning sensation in the mouth and throat, anorexia, nausea, vomiting, headache and diarrhea may be determined as a result of overdose.
Patients who had shown hypersensitivity to miconazole nitrate or any of the excipients of Micotran.
Use in children: Micotran should not be used in children <12 years.
Special Precautions
It is not recommended during menstruation period.
Since Micotran is only effective against candidal vulvovaginitis, detection material should be investigated microscopically with potassium hydroxide and/or candidal vulvovaginitis diagnosis should be proven by culture. Micotran should not be used in virgins and young girls who are not sexually mature. The suppository should not be used with contraceptive diaphragms and condoms since the suppository base may react with the rubber. Diaphragms or condoms can be used after 3 days following the insertion of the suppository. Other vaginal products (eg, tampon, douche or spermicide) should not be used during the treatment.
Effects on the Ability to Drive or Operate Machinery: Effect on the ability to drive and use of machines is unknown.
Use In Pregnancy & Lactation
Pregnancy Category C.
Since the effects of miconazole nitrate on fetus and newborn growth are not clearly known, women of childbearing potential who will use Micotran should avoid pregnancy with a proper birth control method. There is no sufficient data regarding the use of Micotran in pregnant women. Oral miconazole nitrate application to rats leaded to prolonged gestation but not observed in rabbits. At high doses, toxic effects on fetus and embryo in rats and rabbits, and dystocia in rats are observed. These effects were not observed in intravaginal application. Potential risk is unknown in humans.
There is insufficient data regarding the use of Micotran in the 1st trimester of pregnancy. Therefore, Micotran should not be used in the 1st trimester of pregnancy. In the 2nd and 3rd trimesters, benefit/risk ratio should be evaluated by a physician, should not be used unless it is necessary. It is not certain whether it is hazardous or not in lactation period.
Adverse Reactions
Following the insertion of the suppository, vaginitis symptoms eg vaginal burning and itching may increase in some of the patients (2-6%). Additionally, pelvic cramps (2%), headache (1.3%) and very rarely urticarial, skin rash may be observed.
The frequency of adverse events listed in the following is defined using the following convention: Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000); very rare (<1/10,000), not known (cannot be estimated from the available data).
Immune System Disorders: Not Known: Hypersensitivity reactions, angioedema.
Nervous System Disorders: Common: Headache.
Gastrointestinal Disorders: Not Known: Abdominal cramp.
Skin and Subcutaneous Tissue Disorders: Uncommon: Urticaria, skin rash. Not Known: Itching.
General Disorders and Administration Site Conditions: Very Common: Burning, itching. Not Known: Vaginal irritation, pelvic cramps.
Inform physician whenever an unexpected effect is observed.
Drug Interactions
Drug interactions related to miconazole is less likely to occur during the use of Micotran, but it should be considered that the following interactions can be seen due to concomitant use with the following drugs:
Acenocoumarol, Anisindione, Dicumarol, Phenindione, Phenprocoumon, Warfarin: Increase in bleeding risk.
Astemizole, Cisaprid and Terfenadine: Metronidazole inhibits the metabolism of these drugs and increases the plasma concentrations.
Cyclosporine: Increase in cyclosporine risk (renal dysfunction, cholestasis, paresthesia).
Fentanyl: Increase or long taking effects of opioid (central nervous system depression, respiratory depression).
Phenytoin and Phosphenytoin: Increase in phenytoin toxicity risk (ataxia, hyperreflexia, nystagmus, tremor).
Glimepiride: Hypoglycemia.
Carbamazepine: Reduction in carbamazepine metabolism.
Oxybutinin: Due to inhibition of oxybutinin metabolism, exposure to oxybutinin and increase in plasma concentration (dry mouth, constipation, headache).
Oxycodone: Increase in oxycodone plasma concentration and reduction in clearance.
Pimozide: Increase in cardiotoxicity risk (QT prolongation, Torsades de pointes, cardiac arrest).
Tolterodine: Increase in tolterodine bioavalaibility in people with weak cyctochrome P450 2D6 activity.
Trimetrexate: Increase in trimetrexate toxicity (bone marrow suppression, renal and hepatic dysfunction and gastrointestinal ulceration).
Special Populations: Possibility of increase anticoagulant effect due to interact of absorbed Miconazole nitrate in low levels with warfarin and oral anticoagulants (acenocoumarol, dicumarol, phenindione).
No interaction study has been conducted in pediatric population.
Store at temperature not exceeding 25°C.
ATC Classification
G01AF04 - miconazole ; Belongs to the class of imidazole derivative antiinfectives. Used in the treatment of gynecological infections.
Vag supp (whitish, torpedo-shaped) 1.2 g x 1's.
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