mometasone/intranasal

Action and Spectrum

Mechanism of action

The mechanism of action of mometasone intranasal involves its ability to bind to glucocorticoid receptors in target cells, resulting in the inhibition of inflammatory mediators such as cytokines and chemokines, as well as the suppression of immune system activity. This results in a reduction of inflammation and swelling in the nasal passages, improving breathing and relieving allergic rhinitis symptoms

Spectrum

The spectrum of activity of mometasone intranasal is broad, as it effectively treats a wide range of nasal symptoms caused by allergies. It is indicated for treating seasonal and perennial allergic rhinitis in adults and children aged two years. Mometasone intranasal can help reduce symptoms such as nasal congestion, sneezing, itching, and runny nose associated with allergic rhinitis. It is also effective in treating nasal polyps, non-cancerous growths in the nasal passages that can cause nasal obstruction, loss of smell, and other symptoms

Drug Interaction

Adverse Reaction

Frequency defined:

>10%

Pharyngitis

Viral infection

Headache

Cough

Epistaxis

1-10%

Dyspnea

Dysmenorrhea

Myalgia

Otitis Media

Diarrhea

Vomiting

Musculoskeletal pain

Conjunctivitis

Flu-like syndrome

<1%

Angioedema

Nasal candidiasis

Nasal septum perforation

Anaphylaxis

Growth suppression

Taste disturbance

Nasal burning and irritation

Post-marketing reports

Immunosuppression and risk of infections

Glaucoma and cataracts

Hypercortism and adrenal suppression

Impaired wound healing

Ulcerations

Black Box Warning

Contraindication / Caution

Contraindications

• Hypersensitivity can be a concern in the context of nasal surgery, trauma, or septum ulcers because the nasal tissues may be more sensitive and reactive to certain substances.
• After recent nasal surgery or trauma, the nasal tissues may be inflamed and more prone to hypersensitivity reactions.
• Nasal septum ulcers can make the nasal tissues more sensitive and prone to hypersensitivity reactions.

Caution

• Avoiding use in patients with recent nasal surgery or trauma, as this may increase the risk of side effects or delayed healing
• Using with caution in patients with active or quiescent tuberculosis, fungal or bacterial infections of the respiratory tract, or herpes simplex infection of the eye or the respiratory tract
• Monitoring patients for signs of systemic corticosteroid effects, such as adrenal suppression, when using mometasone intranasal for prolonged periods
• Monitoring patients with a history of nasal septum perforation or nasal ulcers, as mometasone intranasal may delay healing of these conditions
• Using caution in patients with a history of glaucoma or cataracts, as mometasone intranasal may increase intraocular pressure
• Avoid use in patients allergic to mometasone or any of its components

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available

Lactation: Excretion of the drug in human breast milk is unknown

Pregnancy category:

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology

mometasone intranasal is a synthetic glucocorticoid with anti-inflammatory and immunomodulatory properties. It is a prodrug rapidly metabolized to the active form, mometasone furoate; upon intranasal administration,

it has a high affinity for glucocorticoid receptors located in the cytoplasm of cells throughout the body. Once mometasone furoate binds to these receptors, it can translocate to the nucleus and regulate the expression of genes involved in inflammation and immune response. Specifically, mometasone furoate can inhibit the transcription of pro-inflammatory genes, such as cytokines and chemokines, and enhance the transcription of anti-inflammatory genes, such as lipocortin’s. This leads to a reduction in inflammation and immune response, resulting in improved symptoms of allergic rhinitis

Pharmacodynamics

mometasone furoate can inhibit the transcription of pro-inflammatory genes, such as cytokines and chemokines, and enhance the transcription of anti-inflammatory genes, such as lipocortin’s. This leads to a reduction in inflammation and immune response, resulting in improved symptoms of allergic rhinitis

Pharmacokinetics

Absorption

mometasone furoate, the active ingredient in mometasone intranasal, has a low bioavailability of approximately 0.1-0.5% due to extensive first-pass metabolism in the liver. Most of the medication is swallowed and eliminated in the faeces after administration, with minimal systemic absorption

Distribution

mometasone furoate is highly protein-bound, with approximately 98-99% binding to plasma proteins

Metabolism

mometasone furoate is primarily metabolized by the liver via the cytochrome P450 enzyme CYP3A4. The metabolites are primarily excreted in the feces

Elimination/Excretion

The half-life of mometasone furoate after intranasal administration is approximately 5.8 hours. The medication is primarily eliminated in the feces, with a small amount excreted in the urine

Adminstartion

Administration

Intranasal administration

• Only for intranasal usage
• Shake vigorously before using.
• Blow nose gently to clear nostrils
• While keeping the bottle upright and tilting the head forward slightly, close one nostril and put the nasal applicator into the other nostril carefully.
• Avoid spraying the nasal septum directly (the wall between the two nostrils)
• Untaken dosage
• If a dose is missed, take it as soon as you recall, but do not exceed the recommended dosage

Storage

• Storage at 77°F (25°C), with excursions allowed to 15–30°C (59-86F)
• Obstruct the light
• Avoid exposing the product to extended direct light once it has been taken from the cardboard packaging.

Patient Information Leaflet

Patient information leaflet

Generic Name: mometasone, intranasal

Why do we use mometasone, intranasal?

mometasone intranasal is a medication used to treat allergic rhinitis symptoms such as nasal congestion, sneezing, itching, and runny nose. It is a corticosteroid that works by reducing inflammation in the nasal passages

Here are some of the uses of mometasone intranasal:

• Allergic rhinitis: It is commonly used to treat seasonal or perennial allergic rhinitis symptoms. It helps reduce inflammation and swelling in the nasal passages, which helps relieve symptoms
• Nasal polyps: It is also used to treat nasal polyps, which are non-cancerous growths in the nasal passages that can cause difficulty breathing and a decreased sense of smell
• Sinusitis: It can be used as a treatment plan for sinusitis, an inflammation of the sinuses that can cause facial pain, headache, and nasal congestion
• Non-allergic rhinitis: It may also be used to treat non-allergic rhinitis, which is inflammation of the nasal passages not related to an allergy