Miconazole

Miconazole is an antimycotic (antifungal) agent used to treat various fungal infections of the skin and mucous membranes. This drug is used in the form of cream, gel, spray, ointment or vaginal tablets, depending on the localization of the infection. Miconazole is effective against a wide range of fungi, including Candida yeast-like fungi that cause candidiasis (thrush), as well as other types of fungi that can cause dermatomycosis (infections of the skin, hair or nails).

The mechanism of action of miconazole is to disrupt the synthesis of ergosterol, an important component of the cell membrane of fungi. This leads to membrane damage and, ultimately, to the death of the fungal cell.

Vaginal forms of miconazole are often used to treat vaginal candidiasis. Ointments and creams may be used to treat skin infections such as athlete's foot, jock itch, and ringworm. Miconazole may also be useful in treating dandruff and seborrheic dermatitis if they are caused by fungi that are sensitive to it.

Before using miconazole, it is important to consult your doctor to make sure the treatment is appropriate for your case and to avoid possible side effects or interactions with other medications.

Indications Miconazole

The indications for the use of miconazole depend on its form. Here are the main indications for the use of different forms of miconazole:

1. External forms (creams, ointments, solutions for external application):

   • Fungal infections of the skin, such as dermatophytosis (trichophytosis, microsporidia, epidermophytosis) and candidiasis (including mycoses of the feet and interdigital spaces).
   • Fungal nail infections (onychomycosis).
   • Fungal infections of the mucous membrane.

2. Vaginal forms (creams and suppositories):

   • Vaginal fungal infections (vaginal candidiasis, or thrush).
   • Prevention of recurrence of vaginal candidiasis.

3. Oral forms:

   • Treatment of systemic fungal infections such as coccidiomycosis, histoplasmosis, cryptococcosis and others when the use of oral antimycotics is considered appropriate.

Release form

Miconazole is a medication that usually comes in several forms for different uses. Here are some of the most common forms of miconazole:

1. Cream: Usually used to treat different types of fungal skin infections, including dermatomycosis (fungal skin infections), candidiasis (yeast infections), and others. The cream is usually applied in a thin layer to the affected areas of the skin.
2. Ointment: Similar to cream, miconazole ointment is also used to treat fungal skin infections. However, it may have a thicker consistency and may be used in a thicker layer.
3. Solution: Miconazole may also come in the form of a solution, which is commonly used to treat fungal nail infections.
4. Vaginal suppositories: This form of miconazole is used to treat vaginal fungal infections such as vaginal candidiasis.
5. Tablets or capsules: Sometimes miconazole may be available in tablet or capsule form for oral administration for systemic fungal infections when the infection spreads to internal organs.

Pharmacodynamics

The mechanism of action of miconazole is based on its ability to inhibit the synthesis of ergosterol, which is a key component of fungal cell membranes. It acts as follows:

1. Inhibition of the enzyme 14α-demethylase: Miconazole inhibits the enzyme 14α-demethylase, which is involved in the conversion of lanosterol to ergosterol, an important structural component of fungal cell membranes. This interferes with the formation of ergosterol, resulting in a disruption of the structure and function of the fungal cell membrane.
2. Cell membrane damage: As a result of inhibition of ergosterol synthesis and accumulation of other metabolic products, miconazole causes damage to the cell membrane of the fungus. This leads to leakage of cellular contents and death of the fungal cell.
3. Antifungal effect: All these mechanisms together provide the antifungal effect of miconazole, which allows it to effectively fight fungal infections.

Active against various types of fungi.

1. Candida albicans: This type of fungus is the most common cause of vaginal candidiasis (yeast infection).
2. Trichophyton spp.: These fungi often cause dermatophytoses such as athlete's foot (mycosis of the foot), dermatophytosis (skin infections), and others.
3. Epidermophyton spp.: They also cause dermatophytosis, including infections of the nails, skin, and hair.
4. Microsporum spp.: This genus of fungus causes dermatophytoses.
5. Cryptococcus neoformans: It is a fungus that causes cryptococcosis, an infection that most commonly affects the lungs and central nervous system.
6. Malassezia spp.: These fungi can cause a variety of dermatologic problems, including seborrheic dermatitis.
7. Histoplasma spp.: These are fungi that cause histoplasmosis, an infection that is most commonly associated with the respiratory system.
8. Mold fungi: Miconazole may also be effective against various types of mold fungi, including Aspergillus spp. And others.

Miconazole may also be active against other types of fungi, depending on the specific form of infection and the sensitivity of the microorganism to the drug.

Pharmacokinetics

1. Absorption: Miconazole is usually applied topically as a cream, ointment, lotion or solution. After topical application, small amounts of miconazole may be absorbed through the skin or mucous membranes. After oral administration of miconazole, its bioavailability is about 1-10%.
2. Metabolism: The drug undergoes extensive metabolism in the liver with formation of various metabolites. The main metabolite is 4-desmethyl-miconazole, which also has antifungal activity.
3. Distribution: The drug is widely distributed in the body, including skin, nails, mucous membranes and other tissues.
4. Excretion: Miconazole and its metabolites are mainly excreted in the urine.
5. Uptake: The eliminationhalf-life of miconazole from the body varies and is approximately 20-50 hours.
6. Pharmacokinetics in hepatic and renal dysfunction: In case of hepatic dysfunction, metabolism of miconazole may be reduced, which may lead to an increase in its concentration in the body. However, there are no sufficient data on the pharmacokinetics of the drug in severe hepatic or renal dysfunction.

Dosing and administration

1. Local application (cream, ointment, lotion, solution):

   • Damaged skin areas or mucous membranes should be clean and dry before applying miconazole.
   • Cream or ointment should be applied in a thin layer to the affected areas of the skin or mucous membranes and gently rubbed. The procedure is repeated 1-2 times a day for 2-4 weeks, depending on the doctor's recommendations and the type of infection.
   • The lotion or solution may also be applied according to the instructions for use.

2. Taking oral forms (tablets, capsules):

   • Dosage and regimen of oral miconazole depends on the type of infection, severity of the disease and doctor's recommendations.
   • The usual initial recommended dose is 200 mg (1 tablet or capsule) once daily for 1 to 4 weeks.
   • For some infections and in severe cases, the dosage may be increased to 400 mg daily or short courses at higher doses may be used.

3. Treatment of fungal nail infections:

   • Miconazole can be used in the form of a cream, ointment, or solution for application to affected nails.
   • Treatment for nail infections usually lasts longer than for skin infections and can last several months until full recovery.

Use Miconazole during pregnancy

The use of miconazole during pregnancy should only be done under the supervision of a doctor and after careful discussion of the benefits of treatment and the potential risks to the mother and fetus. Here are some considerations:

1. Safety in pregnancy: The available data on the safety of miconazole during pregnancy are limited, especially regarding systemic use. However, some studies suggest that topical use of miconazole, such as vaginal suppositories for the treatment of vaginal candidiasis, may be safe during pregnancy.
2. Potential risks: There may be potential risks to fetal development when miconazole is used during pregnancy. These risks may be associated with toxic effects of the drug on the fetus or its development.
3. Alternative treatments: If possible, your doctor may recommend alternative treatments that may be safer during pregnancy. However, the decision whether to use miconazole or another antimycotic depends on the severity of the infection and the general condition of the pregnant woman.
4. Consultation with your doctor: It is important to discuss all potential risks and benefits of treatment with your healthcare professional to make an informed decision about using miconazole during pregnancy.

Contraindications

1. General contraindications:

   • Known allergy to miconazole or other azole antimycotics.
   • Known allergic reaction to any other components of the drug.

2. External forms (creams, ointments, solutions for external application):

   • There are usually not many contraindications to external forms of miconazole, but if you have open wounds, ulcers, or other severe skin damage, you should consult your doctor before using miconazole.

3. Vaginal forms (creams and suppositories):

   • First trimester of pregnancy. In some cases, the doctor may prescribe miconazole in the second and third trimesters only if the potential benefit of treatment exceeds the potential risk to the fetus.
   • Repeated or misdiagnosed vaginal fungal infections unless confirmed by laboratory tests. If necessary, a differential diagnosis should be performed to rule out other infections or conditions.

4. Oral forms:

   • Contraindications to oral forms of miconazole may include severe liver dysfunction, renal impairment, cardiac arrhythmias, and pregnancy and breastfeeding if the potential benefit of treatment does not outweigh the potential risks to the mother and fetus (or child).

Side effects Miconazole

1. Local irritations: These include redness, itching, burning or irritation at the site of miconazole application. These symptoms are usually mild and temporary.
2. Allergic reactions: Rarely, allergic reactions such as skin rash, swelling, or difficulty breathing may develop. If signs of allergy occur, discontinue use immediately and consult a physician.
3. Dry or flaky skin: Some people may experience dry or flaky skin at the site of miconazole application.
4. Emergence of new infections: In rare cases, miconazole may reduce the natural defense mechanisms of the skin or mucous membranes, which may lead to the development of new infections.
5. Taste change: When miconazole is used as sublingual tablets, some people may experience a change in taste.
6. Rare systemic side effects: In individual cases, systemic side effects such as headache, nausea, vomiting, diarrhea, or hypersensitivity to light may occur with systemic administration (e.g., ingestion).

Overdose

Miconazole overdose is unlikely when applied topically (e.g. Creams, ointments, vaginal suppositories) due to limited absorption through the skin or mucous membranes. However, if miconazole is swallowed or administered in large quantities, systemic effects may result.

Symptoms of miconazole overdose may include:

1. Nausea and vomiting: This may be the first sign of overdose when miconazole is administered orally.
2. Dizziness and headache: The occurrence of these symptoms may indicate a possible overdose.
3. Allergic reactions: Including skin rash, itching, swelling of the face, lips or tongue, difficulty breathing.
4. Other systemic effects: Including changes in liver function, blood pressure, etc.

In case of suspected miconazole overdose, it is important to seek immediate medical attention. Treatment of miconazole overdose may include symptomatic support and measures to remove the drug from the body, if necessary.

Interactions with other drugs

Miconazole may interact with other medicines, which may alter their effectiveness or increase the risk of side effects. Below are some of the main interactions of miconazole with other medicines:

1. Antifungal drugs: Miconazole may enhance the effects of other antifungal drugs, which may lead to increased toxicity or side effects.
2. Anticoagulants (e.g. Warfarin): Miconazole may increase the risk of bleeding when used concomitantly with anticoagulants.
3. Cyclosporine: Miconazole may increase blood levels of cyclosporine, which may lead to toxicity.
4. Tacrolimus: Miconazole use may increase tacrolimus levels in the blood, which may also lead to toxicity.
5. Midazolam and other benzodiazepines: Miconazole may increase blood levels of midazolam and other benzodiazepines, which may lead to an increase in their sedative effect.
6. Cycloserine: Miconazole may increase blood levels of cycloserine, which may lead to toxicity.
7. Phenytoin and carbamazepine: Miconazole may decrease the blood levels of phenytoin and carbamazepine, which may reduce their effectiveness.

Storage conditions

The storage conditions for miconazole may vary slightly depending on its form of release (e.g. Cream, ointment, sublingual tablets, etc.). Usually, the manufacturer provides storage instructions on the package or in accompanying information. Here are general recommendations for storing miconazole:

1. Temperature: Most often, miconazole should be stored at room temperature, which is usually between 15 and 25 degrees Celsius. Overheating of the drug or storage at low temperatures is not recommended.
2. Light: Many forms of miconazole (e.g. Creams and ointments) should be protected from direct sunlight. Exposure to sunlight may adversely affect the stability of the drug.
3. Humidity: Store miconazole in a dry place. Avoid storage in humid conditions as this may cause deterioration of the drug.
4. Packaging: Keep miconazole in its original packaging or container to protect it from outside exposure and maintain its effectiveness.
5. Children and animals: Keep miconazole out of the reach of children and animals to avoid accidental use.
6. Avoid extreme conditions: Do not store miconazole in places with excessively high or low temperatures, such as the freezer or bathroom.
7. Expiration date: Observe the expiration date of miconazole as stated on the package or in the accompanying information. After the expiry date, the medicine may lose its effectiveness and safety.