Adult: Dosage is individualised based on the severity of the disease and adjusted according to patient response and tolerance. Titrate to the lowest effective dose once control is achieved. Treatment guidelines must be considered. Metered-dose inhaler: Mometasone 100 mcg and formoterol 5 mcg per actuation Mometasone 200 mcg and formoterol 5 mcg per actuation
In patients not adequately controlled on a long-term asthma-control medication (e.g. inhaled corticosteroid [ICS]) or whose disease warrants initiation of treatment with both an ICS and long-acting β2-adrenergic agonist (LABA): 2 inhalations bid. Max: 2 inhalations of 200 mcg/5 mcg bid. Child: Metered-dose inhaler: Mometasone 50 mcg and formoterol 5 mcg per actuation 5-<12 years 2 inhalations bid. Max: 200 mcg/20 mcg daily.
Mometasone 100 mcg and formoterol 5 mcg per actuation Mometasone 200 mcg and formoterol 5 mcg per actuation ≥12 years Same as adult dose.
Chống chỉ định
Status asthmaticus or other acute episodes of asthma.
Thận trọng
Patient with CV disease (e.g. arrhythmia, coronary insufficiency, hypertension, acute MI); major risk factor for decreased bone mineral content (e.g. prolonged immobilisation, family history of osteoporosis, postmenopausal status, tobacco use, poor nutrition), diabetes mellitus, gastrointestinal disease (e.g. diverticulitis, peptic ulcer, ulcerative colitis), myasthenia gravis, cataracts, glaucoma, aneurysm, phaeochromocytoma, seizure disorders, hypokalaemia, thyroid disease, active or quiescent TB infection of the respiratory tract, untreated systemic fungal, bacterial, viral or parasitic infections; ocular herpes simplex. Avoid exposure to chickenpox or measles. Not indicated for the relief of acute bronchospasm. Avoid abrupt withdrawal. Hepatic impairment. Children and elderly. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Adrenal suppression (e.g. hypercortisolism, HPA axis suppression); hypersensitivity reactions (e.g. urticaria, flushing, allergic dermatitis); Kaposi sarcoma, oral candidiasis, psychiatric disturbances (e.g. depression, euphoria, insomnia, mood swings, personality changes), decreased BMD, elevated blood pressure or heart rate, CNS stimulation or excitation; increased risk of arrhythmias and ECG changes (e.g. flattening of the T wave, prolonged QTc interval, ST segment depression), increased IOP, glaucoma, cataracts, hypokalaemia, increased serum glucose, aggravated ketoacidosis; growth velocity reduction in children. Cardiac disorders: Angina pectoris. Eye disorders: Blurred vision. Nervous system disorders: Headache. Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, sinusitis. Potentially Fatal: Rarely, paradoxical bronchospasm.
Mometasone: Increased plasma concentration with strong CYP3A4 inhibitors (e.g. atazanavir, clarithromycin, cobicistat-containing drugs, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin).
Formoterol: Enhanced hypokalaemic effect with xanthine derivatives. May increase the risk of hypokalaemia and ECG changes with loop or thiazide diuretics. Effects on the CV system may be potentiated with concomitant use or within 2 weeks of discontinuation of MAOIs or TCAs. May have diminished or antagonised therapeutic effect with β-blockers. Concomitant use with other sympathomimetic agents may potentiate the adverse effects of formoterol.
Tác dụng
Description: Mechanism of Action: Mometasone is a synthetic glucocorticoid which has a potent anti-inflammatory activity. It is believed to have a wide range of inhibitory effects on multiple cell types (e.g. mast cells, eosinophils, neutrophils, macrophages, lymphocytes) and mediators (e.g. histamine, eicosanoids, leukotrienes, cytokines) involved in inflammation and asthmatic response.
Formoterol, a synthetic sympathomimetic amine, is a long-acting selective β2-adrenergic receptor agonist. It relaxes bronchial smooth muscles by stimulating adenyl cyclase, thereby increasing the levels of cyclic adenosine monophosphate (cAMP). Duration: Formoterol: Up to 12 hours. Pharmacokinetics: Absorption: Mometasone: Bioavailability: <1%. Time to peak plasma concentration: 0.5-2.5 hours.
Formoterol: Rapidly absorbed. Distribution: Mometasone: Volume of distribution: 152 L. Plasma protein binding: 98-99%.
Formoterol: Plasma protein binding: 61-64%. Metabolism: Mometasone: Extensively metabolised in the liver by CYP3A4 isoenzyme into 6 β-hydroxymometasone furoate.
Formoterol: Metabolised in the liver via direct glucuronidation and O-demethylation. Excretion: Mometasone: Mainly via faeces (approx 74%); urine (8%). Terminal elimination half-life: Approx 5 hours.
Formoterol: Via urine (15-18% as direct glucuronide metabolites, 2-10% as unchanged drug). Terminal elimination half-life: Approx 10 hours.
Đặc tính
Mometasone Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 441335, Mometasone. https://pubchem.ncbi.nlm.nih.gov/compound/Mometasone. Accessed Dec. 20, 2023.
Formoterol Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3410, Formoterol. https://pubchem.ncbi.nlm.nih.gov/compound/Formoterol. Accessed Dec. 20, 2023.
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.
Tài liệu tham khảo
Anon. Formoterol Fumarate. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/06/2023.Anon. Formoterol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/06/2023.Anon. Mometasone (Oral Inhalation). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/06/2023.Anon. Mometasone and Formoterol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/06/2023.Anon. Mometasone Furoate. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/06/2023.Buckingham R (ed). Formoterol Fumarate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/12/2023.Buckingham R (ed). Mometasone Furoate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/12/2023.Dulera Aerosol (Organon LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/06/2023.Formoterol; Mometasone. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 04/06/2023.
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