Usage
Mometasone is a synthetic corticosteroid prescribed for the treatment of various inflammatory and pruritic conditions. Its primary uses include:
- Allergic Rhinitis: Relieves symptoms of seasonal and perennial allergic rhinitis (hay fever), including nasal congestion, sneezing, runny nose, and itching.
- Nasal Polyps: Reduces inflammation and shrinks nasal polyps in adults.
- Asthma: Used as a prophylactic treatment for persistent asthma in adults and children. (inhalation route)
- Inflammatory Skin Conditions: Relieves inflammation and itching associated with corticosteroid-responsive dermatoses such as eczema and psoriasis. (topical formulations)
Pharmacological Classification: Corticosteroid (glucocorticoid)
Mechanism of Action: Mometasone exerts its anti-inflammatory effects by binding to glucocorticoid receptors in the cytoplasm of target cells. This complex then translocates to the nucleus, where it modulates gene expression, resulting in decreased production of inflammatory mediators (e.g., cytokines, prostaglandins, leukotrienes) and reduced inflammatory cell infiltration.
Alternate Names
- Mometasone furoate (International Nonproprietary Name - INN)
Brand Names:
- Nasonex
- Asmanex
- Elocon (topical formulations)
How It Works
Pharmacodynamics: Mometasone binds to glucocorticoid receptors, leading to decreased inflammation, reduced vascular permeability, and suppressed immune responses.
Pharmacokinetics:
- Absorption: Mometasone is minimally absorbed systemically after intranasal or inhalation administration. Topical absorption varies depending on the formulation and application site.
- Metabolism: Primarily metabolized in the liver via CYP3A4 enzymes.
- Elimination: Excreted primarily in feces with a small amount in urine.
Mode of Action: Mometasone exerts its effects through receptor binding to glucocorticoid receptors, inhibiting inflammatory gene expression and reducing the production of inflammatory mediators.
Receptor binding: Glucocorticoid receptor
Elimination pathways: Primarily hepatic metabolism followed by fecal excretion.
Dosage
Standard Dosage
Adults:
- Allergic Rhinitis/Nasal Polyps (Nasal Spray): 2 sprays (50 mcg/spray) in each nostril once daily. May increase to 2 sprays twice daily for nasal polyps if symptoms are not controlled. Maintenance dose: 1 spray in each nostril daily.
- Asthma (Inhalation): Dosage varies depending on the severity of asthma and previous corticosteroid use. Refer to specific product information for detailed guidance.
Children:
- Allergic Rhinitis (Nasal Spray): Children 2-11 years: 1 spray (50 mcg/spray) in each nostril once daily. Children under 2 years: Dosage should be determined by a physician.
- Asthma (Inhalation): Dosage varies depending on age and severity of asthma. Refer to specific product information.
Special Cases:
- Elderly Patients: No specific dose adjustments are typically required, but monitor for potential systemic effects with prolonged use.
- Patients with Renal Impairment: No dose adjustment is generally needed.
- Patients with Hepatic Dysfunction: Use with caution in patients with severe hepatic impairment, as mometasone is metabolized in the liver.
- Patients with Comorbid Conditions: Consider potential drug interactions and monitor for adverse effects in patients with diabetes, cardiovascular disease, or other relevant conditions.
Clinical Use Cases
Mometasone is not typically used in clinical settings such as intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its primary indications are for the long-term management of allergic rhinitis, nasal polyps, and asthma.
Dosage Adjustments
Dose adjustments may be necessary based on individual patient response and the presence of hepatic impairment.
Side Effects
Common Side Effects:
- Headache
- Nosebleeds
- Sore throat
- Nasal irritation
- Upper respiratory tract infection
Rare but Serious Side Effects:
- Vision changes (cataracts, glaucoma)
- Growth suppression (in children with prolonged use)
- Immunosuppression
- Adrenal suppression (with prolonged high doses)
- Allergic reactions (rash, itching, swelling)
Long-Term Effects:
- Increased risk of infections
- Osteoporosis (with prolonged high doses)
- Thinning of skin (with topical use)
Adverse Drug Reactions (ADR):
Contraindications
- Hypersensitivity to mometasone furoate.
- Active untreated nasal infections.
- Recent nasal surgery or trauma (until healed).
Drug Interactions
- CYP3A4 Inhibitors: Ketoconazole, itraconazole, erythromycin, clarithromycin may increase mometasone levels.
- Other Corticosteroids: Concomitant use of other corticosteroids may increase the risk of systemic side effects.
- Ritonavir: May increase mometasone levels.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: C (US FDA). Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
- Breastfeeding: Mometasone is present in breast milk in low amounts. Use with caution while breastfeeding and monitor the infant for potential adverse effects.
Drug Profile Summary
- Mechanism of Action: Binds to glucocorticoid receptors, reducing inflammation.
- Side Effects: Headache, nosebleeds, sore throat, nasal irritation.
- Contraindications: Hypersensitivity, active nasal infections.
- Drug Interactions: CYP3A4 inhibitors, other corticosteroids, ritonavir.
- Pregnancy & Breastfeeding: Use with caution.
- Dosage: Varies based on indication and age; consult product information.
- Monitoring Parameters: Growth (in children), intraocular pressure, bone density (with long-term high-dose use).
Popular Combinations
Mometasone is sometimes used in combination with other medications, such as antihistamines or decongestants, for the treatment of allergic rhinitis. However, specific recommendations for combinations should be based on individual patient needs and clinical judgment.
Precautions
- General Precautions: Monitor for local and systemic adverse effects, especially with long-term use.
- Specific Populations: Use with caution in pregnant or breastfeeding women, children, and patients with hepatic impairment.
- Lifestyle Considerations: No specific lifestyle considerations.
FAQs (Frequently Asked Questions)
A: The dosage varies depending on the condition being treated, the patient’s age, and the formulation of mometasone used. Consult the relevant prescribing information or package insert for specific dosage recommendations.
A: Common side effects include headache, nosebleeds, sore throat, and nasal irritation.
A: Mometasone should be used during pregnancy or breastfeeding only if the potential benefit outweighs the potential risk to the fetus or infant. Consult with a physician before use.
A: Mometasone reduces inflammation in the nasal passages, relieving symptoms such as congestion, sneezing, and runny nose.
A: Contraindications include hypersensitivity to mometasone and active untreated nasal infections.
A: Patients should report any side effects to their physician, who can determine whether dose adjustment or discontinuation of the medication is necessary.
A: Yes, inhaled mometasone is used as a controller medication for the long-term management of asthma.
A: While some patients may experience relief within 12 hours, the full benefit may not be apparent for up to 48 hours or longer, especially with nasal formulations. For asthma, full therapeutic effect may take one to two weeks.
A: Yes, mometasone can interact with certain medications, such as CYP3A4 inhibitors (e.g., ketoconazole, erythromycin), ritonavir and other corticosteroids. It is important to inform your physician of all medications you are taking.
