Usage
Azelastine + Fluticasone Furoate nasal spray is prescribed for the relief of symptoms of seasonal allergic rhinitis (hay fever) in adults and children 6 years of age and older. It is a combination drug belonging to the pharmacological classifications of antihistamines (azelastine) and corticosteroids (fluticasone furoate). The azelastine component works by blocking histamine H1 receptors, thus reducing the effects of histamine, a chemical mediator responsible for allergic symptoms. Fluticasone furoate, a corticosteroid, exerts its action by reducing inflammation in the nasal passages.
Alternate Names
This combination medication is commonly marketed under the brand name Dymista. Other brand names may exist internationally. There are no widely used alternate generic names.
How It Works
Pharmacodynamics: Azelastine, an antihistamine, competitively binds to histamine H1 receptors, preventing histamine from binding and triggering the cascade of events leading to allergic symptoms such as sneezing, rhinorrhea, and nasal congestion. Fluticasone furoate, a synthetic trifluorinated corticosteroid, exhibits potent anti-inflammatory activity by binding to glucocorticoid receptors, resulting in decreased production and release of inflammatory mediators.
Pharmacokinetics:
- Azelastine: After intranasal administration, azelastine is absorbed systemically with a bioavailability of approximately 40%. Peak plasma concentrations are reached in about 30 minutes to 1 hour. It is extensively metabolized in the liver, primarily by CYP enzymes, and eliminated through renal and fecal routes.
- Fluticasone furoate: Fluticasone furoate also displays low systemic bioavailability after intranasal administration (around 1% at therapeutic doses). It undergoes extensive first-pass metabolism in the liver, primarily via CYP3A4, and is excreted primarily in the feces.
Mode of Action: Azelastine acts by antagonizing H1 receptors, inhibiting the effects of histamine on smooth muscle contraction, vascular permeability, and mucus secretion. Fluticasone furoate, by binding to glucocorticoid receptors, modulates gene expression to suppress the production of various inflammatory mediators, including cytokines, chemokines, and adhesion molecules.
Elimination: Azelastine is eliminated mainly through hepatic metabolism followed by renal and fecal excretion. Fluticasone furoate undergoes extensive hepatic metabolism and is primarily eliminated through biliary excretion in feces, with a small fraction excreted in urine.
Dosage
Standard Dosage
Adults: One spray in each nostril twice daily (morning and evening).
Children (6 years and older): One spray in each nostril twice daily.
Special Cases:
- Elderly Patients: No specific dosage adjustment is generally recommended. However, dose titration should be considered based on individual response and tolerance.
- Patients with Renal Impairment: While not explicitly contraindicated, caution is advised. Monitor for potential increased systemic exposure to azelastine.
- Patients with Hepatic Dysfunction: Caution is recommended, especially in severe hepatic impairment, due to potential increased systemic exposure to fluticasone furoate. Close monitoring for corticosteroid-related adverse effects is advised.
- Patients with Comorbid Conditions: Dosage adjustments may be necessary based on specific comorbidities and concomitant medications. Consult relevant guidelines and consider individual patient characteristics.
Clinical Use Cases
The use of azelastine + fluticasone furoate is primarily indicated for seasonal allergic rhinitis. Its use in other clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations is not established.
Dosage Adjustments
No specific dosage adjustments are indicated based solely on age, renal function (except in severe cases), or hepatic function (except in severe cases). However, individual dose titration may be needed based on patient response and tolerance. For patients with severe hepatic or renal impairment, consider monitoring for potential increased adverse effects and adjust the dose accordingly.
Side Effects
Common Side Effects
- Headache
- Epistaxis (nosebleed)
- Dysgeusia (altered taste)
- Nasal irritation
- Cough
- Pharyngitis (sore throat)
Rare but Serious Side Effects
- Allergic reactions (anaphylaxis, angioedema)
- Adrenal suppression (with prolonged or high-dose use)
- Growth retardation (in children with prolonged use)
- Glaucoma, cataracts (with prolonged use)
- Immunosuppression
- Nasal septal perforation (rare)
Long-Term Effects
- Adrenal insufficiency
- Osteoporosis
- Growth retardation in children
- Cataracts
- Glaucoma
Adverse Drug Reactions (ADR)
Clinically significant ADRs requiring immediate intervention include allergic reactions (e.g., anaphylaxis, angioedema), severe or persistent epistaxis, signs of adrenal insufficiency, or evidence of infection.
Contraindications
- Hypersensitivity to azelastine, fluticasone furoate, or any of the excipients in the formulation.
- Active, untreated localized nasal infection (e.g., bacterial, fungal, or viral)
Drug Interactions
- Ritonavir: Avoid concomitant use due to potential for increased systemic corticosteroid exposure.
- Other strong CYP3A4 inhibitors: Use with caution due to potential increased systemic corticosteroid effects.
- CNS depressants (alcohol, sedatives, opioids): Additive effects may occur; advise caution.
Pregnancy and Breastfeeding
- Pregnancy: Azelastine + Fluticasone Furoate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Data regarding the safety of this combination in pregnancy are limited.
- Breastfeeding: Fluticasone propionate is present in human milk, but azelastine information is lacking. It is unknown if this combination drug is excreted in human milk; caution is advised.
Drug Profile Summary
- Mechanism of Action: Azelastine: H1 receptor antagonist; Fluticasone furoate: Glucocorticoid receptor agonist.
- Side Effects: Common: Headache, epistaxis, dysgeusia. Serious: Adrenal suppression, growth retardation, glaucoma/cataracts.
- Contraindications: Hypersensitivity, untreated localized nasal infection.
- Drug Interactions: Ritonavir, strong CYP3A4 inhibitors, CNS depressants.
- Pregnancy & Breastfeeding: Use with caution; limited data available.
- Dosage: Adults and children ≥ 6 years: 1 spray in each nostril twice daily.
- Monitoring Parameters: Nasal examination, growth in children, ophthalmic exam (long-term use).
Popular Combinations
Azelastine + Fluticasone Furoate is itself a combination product. Combining it with other medications for allergic rhinitis is usually not necessary. However, if symptoms persist, additional medications may be added as directed by a physician.
Precautions
- General Precautions: Evaluate for any contraindications or potential drug interactions before initiating therapy. Assess for pre-existing nasal conditions.
- Specific Populations: Use with caution in pregnancy and during breastfeeding. Monitor children for growth retardation with prolonged use.
- Lifestyle Considerations: Advise patients to avoid alcohol and other CNS depressants due to potential additive effects. Caution against operating machinery or driving until the effects on alertness are known.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Azelastine + Fluticasone Furoate?
A: The standard recommended dosage for adults and children 6 years and older is one spray in each nostril twice daily.
Q2: Can pregnant women use this medication?
A: Use during pregnancy should only be considered if the potential benefit outweighs the potential risk to the fetus. Consult a physician for appropriate guidance.
Q3: How should I prime the nasal spray bottle before first use?
A: Shake the bottle gently. Prime the pump by spraying into the air several times (usually 6-8) or until a fine mist appears.
Q4: What if I miss a dose?
A: Administer the missed dose as soon as remembered. If it is close to the time for the next dose, skip the missed dose and continue with the regular dosing schedule.
Q5: What are the most important drug interactions to be aware of?
A: Concurrent use with ritonavir or other strong CYP3A4 inhibitors should be avoided or carefully monitored. Additive effects may occur with CNS depressants.
Q6: Can I use this nasal spray if I have glaucoma?
A: While not strictly contraindicated, caution is warranted. Corticosteroids can increase intraocular pressure. Monitor closely for any changes in vision. Consult an ophthalmologist if needed.
Q7: What should I do if I accidentally spray the medication in my eyes?
A: Immediately flush the eyes with water for at least 10 minutes. Seek medical advice if irritation persists.
Q8: How long can I use Azelastine + Fluticasone Furoate nasal spray?
A: This medication can be used for extended periods, as directed by a physician. Regular follow-up is essential to monitor for potential long-term side effects.
Q9: Are there any age restrictions for using this medication?
A: It is not recommended for children under 6 years of age, as safety and efficacy have not been established in this age group.
Q10: Can I use this medication while breastfeeding?
A: It is unknown if azelastine is excreted in human milk. Fluticasone propionate is present in human milk. Exercise caution when administering this combination to breastfeeding women, and monitor the infant for potential side effects. Consult a physician.
