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Aminophylline

RESPIRATORY SYSTEM

ANTIASTHMATIC - [ RESPIRATORY SYSTEM ]

Aminophylline is a 2:1 complex of theophylline and ethylenediamine. It has two distinct actions in the airways of patients with reversible obstruction; smooth muscle relaxation (i.e., bronchodilation) and suppression of the response of the airways to stimuli (i.e., nonbronchodilator prophylactic effects). It is available for pareneteral as well as oral use. (1)

Intravenous: As an adjunct to inhaled beta-2 selective agonists and systemically administered corticosteroids for the treatment of acute exacerbations of the symptoms and reversible airflow obstruction associated with asthma and other chronic lung diseases, e.g., emphysema and chronic bronchitis. Oral: Treatment of the symptoms and reversible airflow obstruction associated with chronic asthma and other chronic lung diseases, e.g., emphysema and chronic bronchitis. (2,3)

Hypersensitivity to any of the components of the medication (2,3)

Convulsions Hypokalemia Dizziness Headache Palpitation Tachycardia Diarrhoea Anxiety Urinary retention Restlessness Tremors Abdominal pain Exfoliative dermatitis Erythema (2,3,4)

Cimetidine, erythromycin, fluoroquinolones, fluvoxamine, St. John’s wort, fluconazole, ketoconazole, acyclovir, diltiazem, verapamil, interferon alpha, zafirlukast: Inhibit the metabolism and increase the plasma concentration of theophylline Carbamazepine, rifampin, ritonavir, barbiturates: Enhance the metabolism Quinidine: Increased risk of convulsions Benzodiazepine: Effects reduced by theophylline Corticosteroids, beta 2 sympathomimetics: Increased risk of hypokalemia Doxapram: Increased CNS stimulation Zafirlukast: Decrease in the plasma concentration of zafirlukast Sucralfate: Interferes with the absorption of theophylline (2,3,5)

Hepatic insufficiency: Careful attention to dose reduction and frequent monitoring of serum theophylline concentrations are required in patients with reduced hepatic function Congestive heart failure: Careful attention to dose reduction and frequent monitoring of serum theophylline concentrations are required in patients with CHF (2,3)

Parenteral/Oral Adult- 250-500 mg orally or by slow i.v injection. Loading dose- 5 mg/kg. Maintainance dose- 0.5 mg/kg/h. Child- (6 months – 9 years) 1 mg/kg/h. (10 – 16 years) 800 µg/kg/h (4)

1. Barnes PJ. Pulmonary Pharmacology. In: Brunton L, Chabner B, Knollmann B eds. Goodman & Gilman’s The Pharmacological basis of Therapeutics. 12th ed. USA: McGraw Hill; 2011: 1031-66. 2. Aminophylline injection, solution. [Online] [Cited 2013 Sept 27]. Available from: URL: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=9a663ef3-881f-48bd-2689-3713b24545c2#nlm34068-7 3. Aminophylline tablet. [Online] [Cited 2013 Sept 27]. Available from: URL: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=4bc5d8ca-58de-4683-a27a-3e216b20e82b#nlm34071-1 4. National Formulary of India. 4th ed. Government of India, Ministry of Health and Family Welfare. India: Indian Pharmacopoeia Commission; 2011. 5. British Medical Association and the Royal Pharmaceutical Society of Great Britain British National Formulary Issue 61. BMJ Publishing Group: UK; 2011.