Adult: As metered-dose aerosol or dry powd inhaler delivering budesonide 80 mcg or 160 mcg and formoterol 4.5 mcg/actuation: 2 inhalations bid. As metered-dose dry powd inhaler delivering budesonide 320 mcg and formoterol 9 mcg/actuation: Maintenance therapy: 1 inhalation bid, increase if necessary, up to 2 inhalations bid. Child: ≥ 12 yr: Same as adult dose.
Adult: As metered-dose aerosol or dry powd inhaler delivering budesonide 160 mcg and formoterol 4.5 mcg/actuation: 2 inhalations bid. As metered-dose dry powd inhaler delivering budesonide 320 mcg and formoterol 9 mcg/actuation: 1 inhalation bid.
Contraindications
As primary treatment of status asthmaticus, acute episodes of asthma or COPD requiring intensive measures, and potentially worsening or rapidly deteriorating asthma or COPD.
Special Precautions
Patients w/ asthma that is adequately controlled on low- or medium-dose inhaled corticosteroids; bacterial (e.g. active or quiescent pulmonary TB), fungal, parasitic, and viral (e.g. chickenpox, measles, ocular herpes simplex) infection, hypokalaemia, thyrotoxicosis, cataract/glaucoma, phaeochromocytoma, DM, CV disorders (e.g. arrhythmia, heart failure, hypertrophic obstructive cardiomyopathy, idiopathic subvalvular aortic stenosis, severe HTN, aneurysm), osteoporosis, seizures. Hepatic impairment. Pregnancy and lactation.
Perform FEV1, peak flow meter and/or other pulmonary function tests. Monitor signs of asthma or COPD deterioration, growth in paediatric patients, and symptom relief.
Drug Interactions
Increased plasma concentration of budesonide when used w/ CYP3A4 inhibitors (e.g. ketoconazole, clarithromycin, nefazodone, HIV protease inhibitors). Decreased effect of formoterol if concomitantly used w/ β-adrenergic blockers. May prolong QTc-interval and increase the risk of ventricular arrhythmias when used w/ quinidine, disopyramide, procainamide, phenothiazines, antihistamines, MAOIs, and TCAs. May precipitate hypertensive reactions w/ furazolidone, procarbazine and MAOIs. May increase risk of arrhythmias w/ anaesthesia (w/ halogenated hydrocarbons) and digitalis (if patient has hypokalaemia).
Action
Description: Budesonide is a corticosteroid that exhibits potent glucocorticoid and weak mineralocorticoid activities. It controls the rate of protein synthesis, depresses the migration of polymorphonuclear leukocytes/fibroblasts, and reverses capillary permeability and cellular lysosomal stabilisation to control inflammation. 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. Onset: Asthma: 15 min. Pharmacokinetics: Absorption: Rapidly absorbed. Budesonide: Time to peak plasma concentration: 30 min. Bioavailability: Approx 49%. Formoterol: Time to peak plasma concentration: W/in 10 min. Bioavailability: Approx 61%. Distribution: Budesonide: Volume of distribution: 3 L/kg. Plasma protein binding: Approx 90%. Formoterol: Volume of distribution: approx 4 L/kg. Plasma protein binding: Approx 50%. Metabolism: Budesonide: Undergoes extensive first-pass metabolism in the liver by CYP3A4 enyme to major metabolites 6-β-hydroxybudesonide and 16-α-hydroxyprednisolone. Formoterol: Metabolised via glucuronidation and O-demethylation to active O-demethylated and deformylated metabolites. Excretion: Budesonide: Via urine (mainly as conjugated form). Terminal elimination half-life: 2-4 hr. Formoterol: Via urine (8-13% as unchanged drug). Terminal elimination half-life: 17 hr.
Chemical Structure
Budesonide Source: National Center for Biotechnology Information. PubChem Database. Budesonide, CID=5281004, https://pubchem.ncbi.nlm.nih.gov/compound/Budesonide (accessed on Jan. 22, 2020)
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)
R03AK07 - formoterol and budesonide ; 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. Budesonide and Formoterol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 15/09/2016.Buckingham R (ed). Budesonide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/09/2016.Buckingham R (ed). Formoterol Fumarate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/09/2016.Joint Formulary Committee. Budesonide with Formoterol. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/09/2016.McEvoy GK, Snow EK, Miller J et al (eds). Budesonide. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 15/09/2016.McEvoy GK, Snow EK, Miller J et al (eds). Formoterol Fumarate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 15/09/2016.Symbicort Aerosol (AstraZeneca LP). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 15/09/2016.
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