Usage
Azelastine + Mometasone nasal spray is primarily indicated for the treatment of symptoms associated with seasonal and perennial allergic rhinitis (AR), such as runny nose, sneezing, itching, and nasal congestion. It is also used for the management of nasal polyps in adults. It is classified as an antihistamine and corticosteroid combination.
Azelastine, an antihistamine, works by blocking the action of histamine at H1 receptors, thereby reducing allergy symptoms. Mometasone, a corticosteroid, reduces inflammation in the nasal passages by inhibiting the release of inflammatory mediators.
Alternate Names
While “Azelastine + Mometasone” is the generic name, it’s marketed under various brand names like Dymista (Azelastine and Fluticasone), Ryaltris (Olopatadine and Mometasone), and Montasense Az. Note that Dymista contains Fluticasone, another corticosteroid, instead of Mometasone.
How It Works
Pharmacodynamics: Azelastine competitively inhibits H1 receptors, preventing histamine-mediated vasodilation, capillary permeability, and itching. Mometasone exerts its anti-inflammatory action by binding to glucocorticoid receptors in the cytoplasm, which then translocate to the nucleus and affect gene transcription, suppressing the production of inflammatory cytokines. This results in decreased vascular permeability, mucus secretion, and edema.
Pharmacokinetics: Both drugs are administered intranasally. Azelastine is absorbed into the systemic circulation and metabolized primarily in the liver, with a small portion excreted unchanged in the urine. Mometasone has low systemic absorption due to its high lipophilicity, hence it acts locally. When absorbed systemically, it is metabolized primarily by CYP3A4 enzymes in the liver, with subsequent elimination through renal and fecal routes.
Dosage
Standard Dosage
Adults:
One spray in each nostril twice daily (for 0.1% Azelastine) or two sprays once daily (for 0.15% Azelastine). The maximum daily dose is usually four sprays per nostril for adults.
Children:
- 2 to 5 years: One spray of 0.1% Azelastine in each nostril twice daily.
- 6 to 11 years: One or two sprays of 0.1% Azelastine in each nostril twice daily.
- 12 years and older: Adult dosing.
Special Cases:
- Elderly Patients: No specific dosage adjustment is usually required, but start with a lower dose and titrate based on response and tolerability.
- Patients with Renal Impairment: Dosage adjustments may be needed. Monitor closely for adverse effects.
- Patients with Hepatic Dysfunction: Dosage adjustments may be required. Close monitoring is recommended.
- Patients with Comorbid Conditions: Patients with glaucoma, cataracts, or other ocular conditions should be monitored closely due to the potential for increased intraocular pressure with corticosteroid use.
Clinical Use Cases
The provided sources don’t contain sufficient information on dosage recommendations for specific medical settings such as intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
Dosage modifications might be necessary based on individual patient characteristics, comorbidities, and concurrent medications. Always consult with a specialist for specific cases.
Side Effects
Common Side Effects
Headache, nosebleeds (epistaxis), nasal discomfort, sneezing, runny nose, itchy skin around the nose, cough, dry mouth, throat pain, bitter taste, drowsiness, and tiredness.
Rare but Serious Side Effects
Allergic reactions (rash, itching, swelling), glaucoma, cataracts, adrenal suppression (with prolonged use), and growth suppression (in children with prolonged use).
Long-Term Effects
Potential long-term effects include nasal septal perforation, glaucoma, cataracts, and adrenal suppression.
Adverse Drug Reactions (ADR)
Clinically significant ADRs requiring immediate intervention include severe allergic reactions (anaphylaxis, angioedema), worsening of asthma symptoms, and adrenal crisis.
Contraindications
Hypersensitivity to Azelastine, Mometasone, or any component of the formulation. Untreated local nasal infections (fungal, bacterial, or viral), including active tuberculosis.
Drug Interactions
Azelastine + Mometasone may interact with other antihistamines (e.g., diphenhydramine, cetirizine), muscle relaxants, opioid cough suppressants, and certain antidepressants or anxiolytics, increasing the risk of drowsiness. Alcohol consumption should be limited or avoided.
Pregnancy and Breastfeeding
Use during pregnancy and breastfeeding should only be considered if the potential benefit outweighs the potential risk to the fetus or infant. There are no adequate studies in pregnant or breastfeeding women.
Drug Profile Summary
- Mechanism of Action: Azelastine: H1 receptor antagonist; Mometasone: Corticosteroid (glucocorticoid receptor agonist).
- Side Effects: Common: Headache, nosebleeds, nasal discomfort, bitter taste; Serious: Allergic reactions, glaucoma, cataracts.
- Contraindications: Hypersensitivity, untreated nasal infections.
- Drug Interactions: Other antihistamines, CNS depressants, alcohol.
- Pregnancy & Breastfeeding: Use with caution if benefits outweigh risks.
- Dosage: Adults: 1-2 sprays/nostril twice daily or 2 sprays/nostril once daily; Children: Consult guidelines.
- Monitoring Parameters: Monitor for local nasal side effects, intraocular pressure (especially in patients with glaucoma or cataracts), and growth in children.
Popular Combinations
Azelastine + Fluticasone is a common combination used in clinical practice. However, the rationale for combination therapy is to provide broader coverage of allergy symptoms and inflammation.
Precautions
- General Precautions: Assess for any pre-existing medical conditions, allergies, and drug interactions.
- Specific Populations: Caution in pregnant/breastfeeding women and children. Monitor intraocular pressure in patients with glaucoma or cataracts.
- Lifestyle Considerations: Limit or avoid alcohol. Avoid operating heavy machinery if drowsiness occurs.
FAQs (Frequently Asked Questions)
A: Adults: typically one spray per nostril twice daily (0.1% azelastine) or two sprays once daily (0.15% azelastine). Pediatric dosing varies by age; consult guidelines.
A: Azelastine provides relatively rapid relief of some allergy symptoms, while the full effects of mometasone may take several days to become apparent.
A: Common side effects include headache, nosebleeds, nasal discomfort, bitter taste, and drowsiness.
A: Consult your doctor before use during pregnancy or breastfeeding. Use only if the potential benefits outweigh the risks.
A: Avoid concomitant use with other antihistamines, CNS depressants, and alcohol as these may potentiate drowsiness.
A: Administer the missed dose as soon as you remember, but do not double the dose.
A: Long-term use beyond a few months requires medical supervision due to the potential risk of local and systemic side effects from mometasone.
Q8: Can I use this nasal spray if I have glaucoma?
A: Patients with glaucoma should use Azelastine + Mometasone cautiously and under close monitoring by an ophthalmologist due to the potential for increased intraocular pressure from the corticosteroid component.
A: Both combinations contain an antihistamine (Azelastine) and a corticosteroid. However, they use different corticosteroids (Mometasone vs. Fluticasone). While both are effective, they have slightly different pharmacological profiles and may have different efficacy or tolerability in individual patients.
