Mometasone + Formoterol


Concise Prescribing Info
Indications/Uses
Asthma.
Dosage/Direction for Use
Adult : Inhalation Each actuation of metered-dose inhaler releases fluticasone (mcg)/formoterol (mcg): 50/5, 100/5 or 200/5: 2 puffs bid.
Dosage Details
Inhalation/Respiratory
Asthma
Adult: Available preparations:
Metered dose inhaler releasing mometasone 50 mcg and formoterol 5 mcg per actuation
Metered dose inhaler releasing mometasone 100 mcg and formoterol 5 mcg per actuation
Metered dose inhaler releasing mometasone 200 mcg and formoterol 5 mcg per actuation
2 puffs bid. Dose is titrated to the lowest effective dose and may be shifted to higher strength for adequate control of symptoms. Max 800 mcg/20 mcg.
Child: ≥12 yr Same as adult dose.
Contraindications
As primary treatment of status asthmaticus, acute episodes of asthma, and during rapidly deteriorating or potentially worsening episode of asthma.
Special Precautions
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.
Adverse Reactions
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
Patient Counseling Information
Rinse mouth thoroughly every after inhalation. Avoid abrupt withdrawal.
MonitoringParameters
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.
Overdosage
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.
Drug Interactions
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.
Action
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.
Chemical Structure

Chemical Structure Image
Mometasone

Source: National Center for Biotechnology Information. PubChem Database. Mometasone, CID=441335, https://pubchem.ncbi.nlm.nih.gov/compound/Mometasone (accessed on Jan. 23, 2020)


Chemical Structure Image
Formoterol

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

Storage
Store between 20-25°C.
ATC Classification
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.
References
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.

Disclaimer: This information is independently developed by MIMS based on Mometasone + Formoterol from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in