Metacortil
Metacortil Uses, Dosage, Side Effects, Food Interaction and all others data.
Metacortil is a corticosteroid drug that can be used for the treatment of asthma, rhinitis, and certain skin conditions. It has a glucocorticoid receptor binding affinity 22 times stronger than dexamethasone and higher than many other corticosteroids as well. Metacortil is formulated as a dry powder inhaler, nasal spray, and ointment for its different indications.
Mometasone is a synthetic corticosteroid with an affinity for glucocorticoid receptors 22 times higher than that of dexamethasone. Metacortil also has a lower affinity to mineralocorticoid receptors than natural corticosteroids, making it more selective in its action. Metacortil diffuses across cell membranes to activate pathways responsible for reducing inflammation.
| Trade Name | Metacortil |
| Generic | Mometasone furoate |
| Mometasone furoate Other Names | Mometasone furoate |
| Type | Cream |
| Formula | C27H30Cl2O6 |
| Weight | Average: 521.429 Monoisotopic: 520.141944106 |
| Protein binding | 98% to 99% (in vitro concentration of 5 to 500ng/mL). |
| Groups | Approved, Investigational, Vet approved |
| Therapeutic Class | |
| Manufacturer | Macleods Pharmaceuticals |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Metacortil is a corticosteroid used to treat asthma, allergic rhinitis, nasal congestion, nasal polyps, dermatitis, and pruritus.
There are 3 formulations of mometasone furoate with various indications. The inhaler is indicated for prophylaxis of asthma in patients ≥4 years. The nasal spray is indicated for treating nasal symptoms of allergic rhinitis in patients ≥2 years, treating symptoms of nasal congestion from seasonal allergic rhinitis in patients ≥2 years, treating nasal polyps in patients ≥18 years, and prophylaxis of seasonal allergic rhinitis in patients ≥12 years. The ointment is indicated for symptomatic treatment of dermatitis and pruritis in patients ≥2 years.
Metacortil is also used to associated treatment for these conditions: Allergic Rhinitis (AR), Asthma, Dermatitis, Dermatitis, Eczematous caused by superficial Fungal skin infection, Moderate to Severe Plaque Psoriasis, Polyps, Nasal, Pruritus, Psoriasis, Psoriasis, Moderate to Severe, Seasonal Allergies, Skin Diseases, Eczematous, Skin Infections
How Metacortil works
In asthma, mometasone is believed to inhibit mast cells, eosinophils, basophils, and lymphocytes. There is also evidence of inhibition of histamine, leukotrienes, and cytokines.
Corticosteroids diffuse across cell membranes into the cytosol of cells where they bind to glucocorticoid receptors to produce their activity. Metacortil has a particularly high receptor affinity compare to other corticosteroids, 22 times higher than that of dexamethasone. Metacortil binding to a glucocorticoid receptor causes conformational changes in the receptor, separation from chaperones, and the receptor moves to the nucleus. Once at the nucleus, receptors dimerize and bind to a DNA sequence known as the glucocorticoid response element which either increases expression of anti-inflammatory molecules or inhibits expression of pro-inflammatory molecules (such as interleukins 4 and 5). Metacortil also reduces inflammation by blocking transcription factors such as activator-protein-1 and nuclear factor kappa B (NF-kappaB).
Toxicity
Overdose with a mometasone furoate inhaler may occur with chronic overuse. Symptoms of chronic overuse may present as hypercorticism and adrenal suppression, and patients may not require any more treatment than monitoring.
In animal studies of pregnancy, some fetal toxic effects were seen at or above the maximum recommended human dose, though rodents are more sensitive to these effects than humans. The benefits and risks of use should be considered in pregnant patients
It is unknown if mometasone furoate is excreted in breast milk but other corticosteroids are and therefore caution should be exercised when administering to nursing mothers.
Safety and effectiveness in pediatric populations has been established through clinical trials, though there may be a reduction in expected growth of about 1cm per year depending on the dose and duration of treatment. Pediatric patients should be titrated to the lowest effective dose for mometasone furoate inhalers.
A trial of geriatric patients showed no difference in safety or efficacy compared to younger patients, however patients of an even greater age may still be more sensitive to mometasone furoate.
The use of a mometasone furoate inhaler in moderate or severe hepatic impairment rarely leads to detectable plasma concentrations though caution may be prudent with increasing degrees of severity.
The effects of mometasone furoate in renal impairment, and across gender and race have not been studied.
Food Interaction
No interactions found.Volume of Distribution
Steady state volume of distribution of 152L.
Elimination Route
["\"Official drug label\" href=\"#label-reference","Label<\/a> but studies of repeat doses of inhaled corticosteroids suggest a bioavailability of 11%. The 0.1% ointment may have a bioavailability of 0.7%.<\/p>\n"]Half Life
The terminal half life of an inhaled dose is approximately 5 hours though it has been reported as 5.8 hours by other sources.
Clearance
The clearance rate of mometasone furoate is not readily available, though it may be close to 90L/h.
Elimination Route
For an inhaled dose, approximately 74% is excreted in the feces and 8% is excreted in the urine.
Innovators Monograph
You find simplified version here Metacortil
FAQ
What is Metacortil used for?
Metacortil used to treat certain skin conditions, hay fever, and asthma. Specifically it is used to prevent rather than treat asthma attacks. Metacortil skin treatments are used to treat itching, swollen and irritated skin. Metacortil can help with different types of eczema and psoriasis.
How safe is Metacortil?
Generally Metacortil is not recommended for the sensitive skin on your face. Only use it on your face if your doctor says it's safe. Metacortil skin treatments will not help with conditions such as acne or rosacea. Only use Metacortil on large areas of your body or for long periods of time if your doctor says it's safe.
How does Metacortil work?
Metacortil works by activating natural substances in the skin to reduce swelling, redness, and itching.
Is Metacortil safe during pregnancy?
Metacortil should be used in pregnant women only if the potential benefit justifies the potential risk to the mother or the foetus.
Is Metacortil safe during breastfeeding?
Metacortil nasal implants have been studied during breastfeeding. Although not measured, the amounts of inhaled and nasal corticosteroids absorbed into the maternal bloodstream and excreted into breastmilk are probably too small to affect a breastfed infant.
Can I drink alcohol with Metacortil?
Yes, you can drink alcohol with Metacortil.
How long does Metacortil take to work?
Metacortil nasal spray demonstrated a clinically significant onset of action within 12 hours after the first dose in some patients with seasonal allergic rhinitis; however, full benefit of treatment may not be achieved in the first 48 hours.
When is the best time to use Metacortil spray?
If you are using Metacortil nasal spray to treat nasal polyps, it is usually sprayed in each nostril once or twice daily. Use Metacortil at around the same times every day.
How quickly does Metacortil work?
Metacortil nasal spray demonstrated a clinically significant onset of action within 12 hours after the first dose in some patients with seasonal allergic rhinitis; however, full benefit of treatment may not be achieved in the first 48 hours.
How often can I take Metacortil?
For allergic rhinitis the usual dose is 1 or 2 sprays into each nostril once a day. Do not use more than 2 sprays per nostril in 24 hours. For nasal polyps the usual dose is 1 or 2 sprays into each nostril once or twice a day.
Can I overdose on Metacortil ?
An overdose of Metacortil nasal is not expected to produce life threatening symptoms. Long term use of high doses can lead to thinning skin, easy bruising, changes in body fat, increased acne or facial hair, menstrual problems, impotence, or loss of interest in sex.
How long should I use Metacortil ?
You may need to use Metacortil for 1 or 2 weeks, or sometimes for longer.
Does Metacortil cause weight gain?
Metacortil can causes weight gain also with other side effects.
Can I stop taking Metacortil ?
You can usually use it for up to 3 months, but tell your doctor if you feel no better after using it for 14 days. If you are prescribed mometasone, your doctor may advise you to use it for longer.
Who should not take Metacortil?
Metacortil nasal spray is not approved to treat allergy symptoms in anyone younger than 2 years old, or to prevent allergy symptoms in anyone younger than 12 years old. Metacortil nasal implant is not approved for use by anyone younger than 18 years old.
What happens if I miss a dose?
Use the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not use two doses at one time.
Can Metacortil raise blood pressure?
It causes hypoxia and concomitant sympathetic system activation, which may also lead to increased blood pressure levels in these patients.
Can Metacortil affect my heart?
Metacortil can also abnormally stimulate the heart and blood vessels throughout the body.
