Meconazol
Meconazol Uses, Dosage, Side Effects, Food Interaction and all others data.
Meconazol topical cream is a broad-spectrum antimycotic which offers a high antifungal activity against dermatophytes, yeasts and other phyco-Asco and Adelomycetes, with a potent antibacterial activity against Gram-positive bacilli and cocci. Meconazol topical cream proved to be markedly effective in secondary infected mycoses, which under other treatments were resistant or reappeared. Meconazol topical cream does not stain skin or clothes.
The active ingredient, Meconazol, is a synthetic imidazole anti-fungal agent with a broad spectrum of activity against pathogenic fungi (including yeast and dermatophytes) and gram-positive bacteria (Staphylococcus and Streptococcus spp). It may act by interfering with the permeability of the fungal cell membranes. When administered orally, Meconazol is incompletely absorbed from the gastrointestinal tract, peak plasma levels of about 1 µg per ml have been achieved after a dose of 1 gm per day. Meconazol is inactivated in the body and 10-20% of an oral dose is excreted in the urine, mainly as metabolites, within 6 days. About 50% of an oral dose may be excreted unchanged in the faeces.
Meconazol is an azole antifungal that functions primarily through inhibition of a specific demethylase within the CYP450 complex. As miconazole is typically applied topically and is minimally absorbed into the systemic circulation following application, the majority of patient reactions are limited to hypersensitivity and cases of anaphylaxis. Patients using intravaginal miconazole products are advised not to rely on contraceptives to prevent pregnancy and sexually transmitted infections, as well as not to use tampons concurrently.
| Trade Name | Meconazol |
| Availability | Prescription only |
| Generic | Miconazole |
| Miconazole Other Names | Miconazol, Miconazole, Miconazolum |
| Related Drugs | fluconazole, nystatin, clotrimazole, Diflucan, itraconazole, amphotericin b |
| Type | |
| Formula | C18H14Cl4N2O |
| Weight | Average: 416.129 Monoisotopic: 413.986023908 |
| Protein binding | In vitro data suggests that miconazole binds human serum albumin, however, the clinical significance of this observation is unclear. |
| Groups | Approved, Investigational, Vet approved |
| Therapeutic Class | Topical Antifungal preparations |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Meconazol Topical Cream has an antibacterial effect on Gram-positive bacteria, it may be used in mycoses secondarily infected with such bacteria. Skin and nail infections due to dermatophytes, yeasts and other fungi such as: Tinea capitis, corporis, manuum, pedis, barbae, cruris, unguium or onychomycosis. Pityriasis versicolor, candidiasis of skin and nails, stomatitis angularis, otitis externa.
Meconazol Oral treatment and prevention of fungal infections of the oropharynx and gastrointestinal tract, and of super infections due to Gram-positive bacteria.
Meconazol is also used to associated treatment for these conditions: Acne Vulgaris, Dermatophytosis, Dermatophytosis of nail, Diaper Dermatitis, Excessive sweating and body odor, Fungal skin infection, Gastrointestinal candidiasis, Infection Mixed, Infections, Fungal of the Skin Folds, Nail candida, Oropharyngeal Candidiasis, Pityriasis versicolor, Ringworm, Seborrheic Dermatitis, Skin candida, Tinea Capitis, Tinea Corporis, Tinea Cruris, Tinea Pedis, Vaginal Candidiasis, Cutaneous candidiasis
How Meconazol works
Meconazol is an azole antifungal used to treat a variety of conditions, including those caused by Candida overgrowth. Unique among the azoles, miconazole is thought to act through three main mechanisms. The primary mechanism of action is through inhibition of the CYP450 14α-lanosterol demethylase enzyme, which results in altered ergosterol production and impaired cell membrane composition and permeability, which in turn leads to cation, phosphate, and low molecular weight protein leakage.
In addition, miconazole inhibits fungal peroxidase and catalase while not affecting NADH oxidase activity, leading to increased production of reactive oxygen species (ROS). Increased intracellular ROS leads to downstream pleiotropic effects and eventual apoptosis.
Lastly, likely as a result of lanosterol demethylation inhibition, miconazole causes a rise in intracellular levels of farnesol. This molecule participates in quorum sensing in Candida, preventing the transition from yeast to mycelial forms and thereby the formation of biofilms, which are more resistant to antibiotics. In addition, farnesol is an inhibitor of drug efflux ABC transporters, namely Candida CaCdr1p and CaCdr2p, which may additionally contribute to increased effectiveness of azole drugs.
Dosage
Meconazol dosage
For oral administration: Dosage is based on 15 mg/kg/day.
- Adults: 1-2 tea-spoonfuls of gel four times daily
- Children aged 6 years and over: One tea-spoonful of gel four times daily
- Children aged 2-6 years: One tea-spoonful of gel twice daily
- Infants under 2 years: Half tea-spoonful of gel twice daily.
For localised lesions of the mouth:
A small amount of gel may be applied directly to the affected area with a clean finger. For topical treatment of the oropharynx, the gel should be kept in the mouth for as long as possible. Treatment should be continued for up to 2 days after the symptoms have cleared.
For oral candidasis, dental prostheses:
Should be removed at night and brushed with the gel.
The dosage is same for all the ages.
For skin infections: Apply some cream to the lesions twice daily and rub it well with finger until it has fully penetrated the skin. All lesions usually disappear after 2 to 5 weeks. Prolong treatment for some 10 days to prevent relapse.
For nail infections: Clip infected nail as shortly as possible. Apply some cream once daily to the infected nail and rub with your finger, cover nail with a non-perforated occlusive plastic bandage.
Also after loosening of the infected nail (from 2-3 weeks onwards) uniterrupted treatment should be continued until the growth of a new nail has set in and definite cure can be observed (usually after seven months or more).
Side Effects
Topical application of Meconazol Nitrate has almost no side effect.
For oral gel: Occasionally, nausea and vomiting have been reported, and with long term treatment, diarrhoea. In rare instances, allergic reactions have been reported. There are isolated reports of hepatitis, for which the causal relationship with Meconazol has not been established.
Toxicity
Meconazol overdose has not been reported. Patients experiencing an overdose are at an increased risk of severe adverse effects such as headache, skin irritation, diarrhea, nausea, vomiting, abdominal pain, and dysgeusia. Symptomatic and supportive measures are recommended.
Meconazol has an oral LD50 of 500 mg/kg in rats.
Precaution
If the concomitant use of Meconazol and anticoagulants is envisaged, the anticoagulant effect should be carefully monitored and titrated. It is advisable to monitor Meconazol and phenytoin levels, if they are used concomitantly. Particularly in infants and young children, caution is required to ensure that the gel does not obstruct the throat. Hence, the gel should not be applied to the back of the throat and the full dose should be divided into smaller portions. Observe the patient for possible choking.
Interaction
Meconazol can inhibit the metabolism of drugs metabolised by the Cytochrome P450-3A and -2C9 families. This can result in an increase or prolongation of their effects, including side effects. Meconazol Oral Gel should not be used during treatment with the following drugs: terfenadine, astemizole,mizolastine, cisapride, triazolam, oral midazolam, dofetilide, quinidine, pimozide, CYP3A4 metabolised HMG-CoA reductase inhibitors such as simvastatin and lovastatin.
Food Interaction
No interactions found.Meconazol Cholesterol interaction
[Minor] Elevations in cholesterol and triglyceride levels may occur in patients receiving intravenous miconazole and are attributed to the drug vehicle, Cremophor EL (polyethoxylated castor oil).
These increases are reversible upon discontinuation of miconazole therapy.
Clinicians should be cognizant of these effects when interpreting lab results of hyperlipidemic patients during treatment with miconazole.
Meconazol Drug Interaction
Moderate: fluconazole, alprazolamUnknown: ibuprofen, lorazepam, amoxicillin / clavulanate, diphenhydramine, omega-3 polyunsaturated fatty acids, fluticasone nasal, metoprolol, polyethylene glycol 3350, acetaminophen, bifidobacterium infantis / lactobacillus acidophilus, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, ranitidine, ondansetron, sertraline, cetirizine
Meconazol Disease Interaction
Volume of Distribution
A 1200 mg miconazole vaginal suppository resulted in a calculated apparent volume of distribution of 95 546 L while a 100 mg vaginal cream yielded an apparent volume of distribution of 10 911L.
Elimination Route
Meconazol given to healthy volunteers as a single 50 mg oral tablet produced a mean Cmax of 15.1 ± 16.2 mcg/mL, a mean AUC0-24 of 55.2 ± 35.1 mcg*h/mL, and a median Tmax of 7 hours (range 2.0-24.1). In these patients measurable plasma concentrations ranged from 0.5 to 0.83 mcg/mL.
Topical miconazole is absorbed poorly into the systemic circulation. In pediatric patients aged 1-21 months given multiple topical applications of miconazole ointment for seven days, the plasma miconazole concentration was less than 0.5 ng/mL in 88% of the patients, with the remaining patients having a concentration of 0.57 and 0.58 ng/mL, respectively. Similarly, patients. administered with a vaginal 1200 mg ovule had a mean Cmax of 10.71 ng/mL, mean Tmax of 18.4 hours, and mean AUC0-96 of 477.3 ng*h/mL.
Half Life
Meconazol has a terminal half-life of 24 hours.
Elimination Route
Meconazol is excreted through both urine and feces; less than 1% of unchanged miconazole is recovered in urine.
Pregnancy & Breastfeeding use
In animals, Meconazol has shown no teratogenic effects but is foetotoxic at high oral doses. The significance of this to man is unknown. However, as with other imidazoles, Meconazol Oral Gel should be avoided in pregnant women if possible. The potential hazards should be balanced against the possible benefits. It is not known whether Meconazol is excreted in human milk. Caution should be exercised when prescribing Meconazol Oral Gel to nursing mothers.
Only small amounts of Meconazol cream are absorbed following local administration. However as with other imidazoles, Meconazol nitrate should be used with caution during pregnancy.
Contraindication
Meconazol is contraindicated in patients with known hypersensitivity to the active drug.
Acute Overdose
In general, Meconazol is not highly toxic. In the event of accidental overdosage, vomiting and diarrhoea may occur.
Storage Condition
Store away from direct heat. Keep out of reach of children.
Innovators Monograph
You find simplified version here Meconazol
Meconazol contains Miconazole see full prescribing information from innovator Meconazol Monograph, Meconazol MSDS, Meconazol FDA label
FAQ
What is Meconazol used for?
Meconazol is an antifungal medication used to treat ring worm, pityriasis versicolor, and yeast infections of the skin or vagina. It is used for ring worm of the body, groin (jock itch), and feet (athlete's foot). It is applied to the skin or vagina as a cream or ointment.
How safe is Meconazol?
Meconazol topical is for use only on the skin. Meconazol may be harmful if swallowed. If someone has overdosed and has serious symptoms such as passing out or trouble breathing.
How does Meconazol work?
Meconazol works by stopping the growth of yeast (fungus) that causes the infection.
What are the common side effects of Meconazol?
Common side effects of Meconazol are include:
Burning, stinging, swelling, irritation, redness, pimple-like bumps, tenderness, or flaking of the treated skin may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.
Is Meconazol safe during pregnancy?
Yes, you can use during pregnancy.
Is Meconazol safe during breastfeeding?
There are currently no studies looking at Meconazol use during breastfeeding. However, because only small amounts of the medication could pass into breastmilk Meconazol is used on the skin or in the vagina, breastfeeding is not expected to be a concern.
Can I take alcohol with Meconazol?
You should not drink alcohol if you are feeling sick or uncomfortable while fighting off a fungal infection because alcohol can have adverse effects that may make you feel worse. Alcohol, as with some other foods and beverages, can affect your body's yeast infection.
What happens after taking Meconazol?
Headache, vaginal/urethral burning/itching/pain, or lower abdominal cramps may occur.
How long does it take Meconazol to start working?
You should begin to feel better during the first three days of treatment with Meconazol.
How often can I take Meconazol?
The cream is used twice a day for up to 7 days, on the skin around the outside of the vagina. Follow the directions on the package or as directed by your doctor carefully, and ask your doctor or pharmacist to explain any part you do not understand.
How long can I use Meconazol for?
Do not use for more than 4 weeks without advice.
Who should not take Meconazol?
You should not take Meconazol If you have any of the following health problems, consult your doctor or pharmacist before using this medication: diabetes, immune system problems , frequent vaginal yeast infections.
What happens if I stop Meconazol early?
No you should continue until treatment is finished. Vaginal yeast infections respond best to 7-day treatments and tend to come back if medicine is stopped early.
What happens if I miss a dose?
Apply the missed dose as soon as you remember. However, if it is almost time for the next dose, skip the dose you missed and apply only the next regularly scheduled dose. Do not use a double dose of this medication.
What happens if I overdose?
An overdose of Meconazol vaginal is unlikely. If you do suspect that a much larger than normal dose has been used or that Meconazol vaginal has been ingested, contact an emergency room or a poison control center.
How well does Meconazol work?
Meconazol topical has an average rating of 3.0 out of 10 from a total of 4,019 ratings on Drugs.com. 15% of reviewers reported a positive effect, while 72% reported a negative effect.
When should I use Meconazol?
Use the medication usually once daily at bedtime for 1 to 7 nights depending on the product used, or as directed by your doctor.
Can Meconazol affect my liver?
Cause liver damage or failure, especially when combined with alcohol or certain medicines.
Can Meconazol affects my heart ?
Meconazol should be given with caution to patients with underlying heart disease.
