Drug Interaction:
Formoterol Other adrenergic agonists - cause additive adrenergic stimulation Tricyclic antidepressants, MAO inhibitors-may increase cardiovascular effects Corticisteroids, diuretics, theophylline may potentiate hypokalemia. Dofetilide, quinidine, procainamide, pimozide, moxifloxacin, sparfloxacin, gatifloxacin, solatol, mesoridazine , thioridazine may increase QTc intervals. Budenoside The metabolism of budesonide is primarily mediated by CYP3A4, a subfamily of cytochrome P450, inhibitors of this enzyme, eg. ketoconazole may therefore increase systemic exposure to budesonide Budesonide and formoterol have not been observed to interact with any other drug used in the treatment of asthma.
Adverse Reaction:
Budesonide Depression, glucocorticoid effects, behavioural disturbances, immediate and delayed hypersensitivity recations. Formoterol Angina pectoris, hyperglycaemia. cardiac arrhythmias in the form of atrial fibrillation, supraventricular tachycardia and extrasystoles have been reported for beta- agonists Others- Headache, palpitations, tremor, canida infections in the oropharynx, mild irritation in the throat, coughing and hoarseness. Rare tachycardia,.
Contra-Indications:
Budenoside:
Hypersensitivity Formoterol Hypersenstivity within 2 weeks of MAO inhibitor use. Special precautions: It is recommended that the dose is tapered when the treatment is discontinued. Sytemic effects may occur with inhaled corticosteroid, particularly at high doses prescribed for long periods. Possible systemic effects include adrenal suppression, growth retardation in children and adolescence, decrease in bone mineral density, cataract and glaucoma The benefits of inhaled budesonide therapy would normally minimize the need for oral steroids, but patients transferring from oral steroids may remain at risk of impaired adrenal reserve for a considerable time To minimise the risk of oropharyngeal canida infection, the patient should be instructed to rinse the mouth with water after each dosing occasion. Caution to be taken when given to pregnant women. The lowest effective dose of budesonide to maintain adequate asthma control should be used. Care should be taken when given to lactating women..
Dosages/ Overdosage Etc:
Asthma Individualised according to disease severity. Adults- 1-2 inhalitions twice daily
Pharmacology/ Pharmacokinetics:
Pharmacology:
It contains budesonide and formoterol, which have different modes of action and together improve asthma symptoms and reduction of asthma exacerbations Budesinide is a potent glucocorticosteroid that when inhaled reduces the number of inflammatory cells such as eosinophils, lymphocytes and mast cells and helps restore airway epithelial integrity. These effects result from the inhibition of transcription of several cytokines that are expressed in asthma. Budesonide inhibits phopholipase A2 activity. and thus reduces the formation of postaglandins and leukotrienes in the airway. Formetrol is a very potent adrenonoreceptor agonist. Its affinity for the beta-adrenoreceptor is significantly greater than that for the beta-adrenoreceptor. It has a high intrinsic activity and a rapid onset of action due to its lipid solubility, most of the formetrol is taken up into the plasma bilayer from where it diffuses slowly to stimulate adenylate cyclase and increases the intracellular concentration of cyclic AMP in airway smooth muscle. The bronchodilating effect is rapid within 1-3 minutes after inhalation and has a duration of 12 hours after a single dose.
Pharmacokinetics:
Budesonide- Maximum plasma concentration is reached within 30inutes after inhalation. The systemic bioavilability is 49% of the delivered dose. The metabolites are excreted in urine as such or in conjugated form. Formoterol Maximum plasma concentration is reached within 10 minutes after inhalation. Systemic availability is about 61% of the delivered dose. Eliminated by liver followed by renal excretion.
Pregnancy and lactation:
Caution to be taken when given to preganat women. The lowest effective dose of budesonide to maintain adequate asthma control should be used. Care should be taken when given to lactating women..