Mometasone + Formoterol

Inhalation/Respiratory
Asthma

As primary treatment of status asthmaticus, acute episodes of asthma, and during rapidly deteriorating or potentially worsening episode of asthma.

Patient w/ severe asthma, risk factors for decreased BMD, CV disease (e.g. arrhythmia, coronary insufficiency, HTN, recent MI), DM, GI disease (e.g. diverticulitis, peptic ulcer, ulcerative colitis), myasthenia gravis, cataract/glaucoma, pheochromocytoma, seizure disorders, hypokalaemia, thyroid disease, bacterial (e.g. active or quiescent pulmonary TB), fungal, parasitic, and viral (e.g. chickenpox, measles, ocular herpes simplex) infections. Hepatic impairment. Childn. Pregnancy and lactation.

Significant: Adrenal suppression, hypercorticism, immunosuppression, Kaposi sarcoma, oral candidiasis, psychiatric disturbances, decreased BMD, BP and heart rate elevation, CNS stimulation/excitation, risk of arrhythmias (e.g. AF, ventricular extrasystoles, tachyarrhythmia), ECG changes (e.g. flat T wave, prolonged QT interval, depressed ST segment), increased intra-ocular pressure, glaucoma, cataract, hypokalaemia, myasthenia gravis exacerbation, ketoacidosis aggravation, hyperglycaemia, risk of perforation. Rarely, vasculitis, hypersensitivity reactions (e.g. allergic dermatitis, angioedema, bronchospasm, arthralgia, flushing, rash, anaphylaxis, urticaria).
Nervous: Headache, tremor.
Resp: Nasopharyngitis, voice disorder, sinusitis.
Potentially Fatal: Asthma exacerbation, paradoxical bronchospasm.

Inhalation/Respiratory: C

Rinse mouth thoroughly every after inhalation. Avoid abrupt withdrawal.

Monitor FEV₁, peak flow meter and/or other pulmonary function tests, BP, heart rate, serum glucose, serum K, BMD, and eye exam (chronic users). Monitor signs of asthma deterioration, growth in paediatric patients, symptom relief, HPA axis suppression, CNS stimulation.

Symptoms: Hypercorticism, angina, HTN or hypotension, tachycardia, arrhythmias, nervousness, headache, tremor, seizures, muscle cramps, dry mouth, palpitation, nausea, dizziness, fatigue, malaise, hypokalaemia, hyperglycaemia, insomnia, metabolic acidosis, cardiac arrest. Management: Symptomatic and supportive treatment.

Mometasone: Increased plasma concentration w/ strong CYP3A4 inhibitors (e.g. ketoconazole, ritonavir, cobicistat-containing products).
Formoterol: Enhanced hypokalaemic effect w/ xanthine derivatives, or non-potassium sparing diuretics. May prolong QTc-interval and increase the risk of ventricular arrhythmias when used w/ quinidine, terfenadine, astemizole, macrolides, disopyramide, procainamide, phenothiazines, MAOIs, and TCA. Decreased therapeutic effect w/ β-adrenergic blockers. Increased risk of arrhythmias w/ halogenated hydrocarbons.

Description: Mometasone is a synthetic nonfluorinated glucocorticoid. It prevents or reduce inflammation by controlling the rate of protein synthesis, depressing the migration of polymorphonuclear leukocytes/fibroblasts, and reversing capillary permeability and lysosomal stabilization at the cellular level.
Formoterol is a long-acting selective β₂ adrenoceptor agonist. It relaxes bronchial smooth muscles by stimulation of adenyl cyclase, thereby increasing cyclic-3’- 5’-adenosine monophosphate (cAMP) levels.
Duration: Formoterol: Up to 12 hr.
Pharmacokinetics:
Absorption: Mometasone: Rapidly absorbed. Absolute bioavailability: Approx 14%. Time to peak plasma concentration: 0.5-4 hr.
Formoterol: Rapidly absorbed. Time to peak plasma concentration: 0.17-1.97 hr.
Distribution: Mometasone: Volume of distribution: 152 L. Plasma protein binding: 98-99%.
Formoterol: Plasma protein binding: 61-64% (34% primarily to albumin).
Metabolism: Mometasone: Undergoes hepatic metabolism by CYP3A4 enzyme to 6-β hydroxymometasone furoate.
Formoterol: Metabolised via glucuronidation and O-demethylation.
Excretion: Mometasone: Mainly via faeces (74%); urine (8%, lesser extent). Terminal elimination half-life: Approx 5 hr.
Formoterol: Mainly via urine (approx 10% as unchanged drug). Terminal elimination half-life: Approx 10 hr.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 441335, Mometasone. https://pubchem.ncbi.nlm.nih.gov/compound/Mometasone. Accessed Oct. 26, 2022.

Source: National Center for Biotechnology Information. PubChem Database. Arformoterol, CID=3083544, https://pubchem.ncbi.nlm.nih.gov/compound/Arformoterol (accessed on Jan. 21, 2020)

Store between 20-25°C.

Antiasthmatic & COPD Preparations

R03AK09 - formoterol and mometasone ; Belongs to the class of adrenergics in combination with corticosteroids or other drugs, excluding anticholinergics. Used in the treatment of obstructive airway diseases.

Anon. Mometasone and Formoterol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/09/2017.

Buckingham R (ed). Formoterol Fumarate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/09/2017.

Buckingham R (ed). Mometasone Furoate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/09/2017.

Dulera Inhalation Aerosol (Merck Sharp & Dohme Corp.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 07/09/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Mometasone Furoate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 07/09/2017.