Usage
Formoterol + Mometasone is prescribed for the maintenance treatment of asthma in patients 5 years and older not adequately controlled on a long-term asthma control medication (e.g., inhaled corticosteroid) or whose disease severity warrants initiation of treatment with both an inhaled corticosteroid and a long-acting β₂-adrenergic agonist (LABA). It is not indicated for the relief of acute bronchospasm.
It is classified as a combination inhaler medication containing both an inhaled corticosteroid (ICS) (mometasone) and a long-acting beta-agonist (LABA) (formoterol).
Alternate Names
This combination is commonly known as Mometasone/Formoterol. A popular brand name is Dulera. Zenhale is another brand name for this combination.
How It Works
Pharmacodynamics:
- Mometasone: Exerts its anti-inflammatory effects by binding to glucocorticoid receptors in the airways, reducing airway inflammation and hyperresponsiveness.
- Formoterol: Relaxes bronchial smooth muscle by stimulating β₂-adrenergic receptors, leading to bronchodilation and improved airflow.
Pharmacokinetics:
- Mometasone: Low systemic bioavailability (<1%) due to extensive first-pass metabolism. Primarily metabolized by CYP3A4. Excreted mainly in feces. Terminal elimination half-life is approximately 5 hours.
- Formoterol: Rapidly absorbed. Metabolized in the liver via direct glucuronidation and O-demethylation. Excreted primarily in urine. Terminal elimination half-life approximately 10 hours.
Mode of Action:
Mometasone acts by binding to glucocorticoid receptors, modulating gene transcription to suppress inflammatory mediators. Formoterol activates β₂-adrenergic receptors, increasing intracellular cAMP levels and leading to smooth muscle relaxation.
Dosage
Standard Dosage
Adults (≥12 years):
Two inhalations (puffs) twice daily (morning and evening) of either 100 mcg/5 mcg or 200 mcg/5 mcg strength. The maximum dose is 800 mcg mometasone/20 mcg formoterol per day.
Children (5-11 years):
Two inhalations twice daily of the 50 mcg/5 mcg strength. The maximum dose is 200 mcg mometasone/20 mcg formoterol per day.
Children (under 5 years):
Use and dose must be determined by the child’s doctor.
Special Cases:
- Elderly Patients: No specific dosage adjustments, but monitor for potential adverse effects.
- Patients with Renal Impairment: No dosage adjustment data available.
- Patients with Hepatic Dysfunction: Close monitoring is needed, as effects may be increased due to slower removal of the medicine from the body.
- Patients with Comorbid Conditions: Caution advised in patients with cardiovascular disease, diabetes, seizures, thyroid problems, etc.
Clinical Use Cases
Formoterol + Mometasone is not indicated for acute conditions requiring intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. It is for maintenance treatment of asthma.
Dosage Adjustments
Adjust the dosage individually based on the severity of the disease and the patient’s response. Titrate to the lowest effective dose once control is achieved.
Side Effects
Common Side Effects:
Headache, throat irritation, upper respiratory tract infection, hoarseness, oral candidiasis (thrush).
Rare but Serious Side Effects:
Hypersensitivity reactions (e.g., rash, angioedema), paradoxical bronchospasm, adrenal suppression, pneumonia, osteoporosis.
Long-Term Effects:
Growth retardation in children, decreased bone mineral density, cataracts, glaucoma.
Contraindications
- Status asthmaticus or other acute asthma episodes
- Hypersensitivity to mometasone, formoterol, or any component of the formulation.
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole): May increase plasma concentrations of mometasone.
- Beta-blockers: May antagonize the bronchodilating effects of formoterol.
- Other drugs that prolong the QTc interval: May increase the risk of cardiac arrhythmias when used with formoterol.
- MAO inhibitors and tricyclic antidepressants: Caution advised.
Pregnancy and Breastfeeding
- Pregnancy: Use only if the potential benefit justifies the potential risk to the fetus.
- Breastfeeding: Limited data available. Exercise caution.
Drug Profile Summary
- Mechanism of Action: Mometasone: Inhaled corticosteroid, reduces airway inflammation. Formoterol: LABA, bronchodilator.
- Side Effects: Thrush, headache, upper respiratory tract infection, hoarseness. Serious: Adrenal suppression, hypersensitivity reactions.
- Contraindications: Status asthmaticus, hypersensitivity.
- Drug Interactions: Strong CYP3A4 inhibitors, beta-blockers, QTc prolonging drugs.
- Pregnancy & Breastfeeding: Use with caution.
- Dosage: Adults: 2 inhalations BID (100/5 or 200/5 mcg). Children (5-11): 2 inhalations BID (50/5 mcg).
- Monitoring Parameters: Asthma control, growth in children, bone mineral density (long-term use), adverse effects.
Popular Combinations
Formoterol + Mometasone is itself a popular combination. Not typically combined with other controller medications except in severe asthma not controlled with other treatments.
Precautions
- Monitor for oral candidiasis. Rinse mouth after each use.
- Monitor growth in pediatric patients.
- Caution in patients with cardiovascular disease, diabetes, seizures, thyroid disorders.
- Avoid abrupt withdrawal.
FAQs (Frequently Asked Questions)
A: Adults: Two inhalations twice daily (100/5 mcg or 200/5 mcg). Children (5-11 years): Two inhalations twice daily (50/5 mcg).
A: No, it is not a rescue inhaler and should not be used for acute bronchospasm. Patients should use a short-acting beta-agonist (SABA) for acute attacks.
Q3: What are the common side effects?
A: Common side effects include oral candidiasis (thrush), headache, upper respiratory tract infection, and hoarseness.
Q4: What are the potential drug interactions?
A: Strong CYP3A4 inhibitors may increase mometasone levels. Beta-blockers may reduce formoterol’s efficacy. Concomitant use with other QTc-prolonging drugs may increase the risk of arrhythmias.
Q5: Can it be used during pregnancy?
A: Use during pregnancy only if the potential benefit outweighs the potential risk to the fetus.
Q6: What should patients do after each inhalation?
A: Patients should rinse their mouth with water without swallowing to minimize the risk of oral thrush and other local side effects.
Q7: Is there a risk of adrenal suppression with this combination?
A: Yes, there is a potential for adrenal suppression, especially with higher doses. Monitor patients for signs of systemic corticosteroid effects.
A: Growth should be carefully monitored in children, as inhaled corticosteroids can potentially affect growth velocity.
A: Patients with hepatic impairment should be closely monitored for signs of increased drug exposure, as the effects may be increased due to slower removal of the medicine from the body.
A: No dosage adjustment data is available regarding patients with renal impairment. However, It’s important to exercise caution and to adjust dosage based on the individual patients needs, while carefully monitoring for any possible side effects.
