(the off'' i lin)
P / L : Caution - during pregnancy & lactation
|| See TERMINOLOGY & ABBREVIATIONS ||
|Indication(s) & Dosage||
Theophylline is used as a bronchodilator in the symptomatic and prophylactic treatment of asthma and for reversible bronchoconstriction associated with chronic bronchitis and bronchial asthma.
|Administration||May be taken with or without food.
|Overdose||Nausea, vomiting, diarrhoea, agitation, tremor, hypertonicity, hyperventilation, diuresis and repeated vomiting (sometimes haematemesis), cardiac arrhythmias including tachycardia, hypotension, electrolyte disturbances including hypokalaemia, hyperglycaemia, hypophosphataemia, hypercalcaemia, metabolic acidosis, respiratory alkalosis and convulsions. Other reported effects include dementia, toxic psychosis, symptoms of acute pancreatitis, rhabdomyolysis with renal failure and acute compartment syndrome. Empty stomach by lavage if within 2 hr of overdose, with repeated oral doses of activated charcoal and osmotic laxative, especially if modified-release tablets taken. Symptomatic and supportive treatment with monitoring of serum theophylline concentrations. Non-selective Î²blockers to be used in non-asthmatic patient for tachycardia, IV diazepam or a barbiturate to control convulsions, disopyramide may be used in patients with both ventricular arrhythmias and convulsions. In severe cases, general anaesthesia and neuromuscular blockade with ventilation may be needed. Charcoal haemoperfusion or haemodialysis may be helpful especially in CHF or liver disease.|
|Contraindications||Hypersensitivity to xanthine derivatives, porphyria.|
|Special Precautions||Admin IV inj very slowly to avoid direct stimulation of the CNS and CVS. Cardiac failure, hypertension, epilepsy, hyperthyroidism, history of peptic ulcer disease, renal or hepatic dysfunction, glaucoma, DM, severe hypoxaemia, chronic alcoholism, acute febrile illness. On influenza immunization or active influenza infection, COPD and cor pulmonale. Smokers may need higher dose. Pregnancy, lactation, children and elderly.|
|Adverse Drug Reaction(s)||Nausea, vomiting, abdominal pain, diarrhoea, headache, insomnia, dizziness, anxiety, restlessness, tremor, palpitations.
Potentially Fatal: Convulsions, cardiac arrhythmias, hypotension and sudden death after too rapid IV inj.
Theophylline has been reported to interact with a number of drugs. The following increase clearance and it may therefore be necessary to increase dosage to ensure therapeutic effect: barbiturates, carbamazepine, lithium, phenytoin, rifampicin and sulphinpyrazone.
The following reduce clearance and a reduced dosage may therefore be necessary to avoid side-effects: allopurinol, cimetidine, ciprofloxacin, corticosteroids, diltiazem, erythromycin, frusemide, isoprenaline, oral contraceptives, thiabendazole and verapamil. There is some evidence of an interaction between theophylline and influenza vaccine.
Xanthines can potentiate hypokalaemia resulting from beta2 agonist therapy, steroids, diuretics and hypoxia. Particular caution is advised in severe asthma. It is recommended that serum potassium levels are monitored in such situations.
The concomitant use of theophylline and fluvoxamine should usually be avoided. Where this is not possible, patients should have their theophylline dose halved and plasma theophylline should be monitored closely.
Plasma concentrations of theophylline can be reduced by concomitant use of the herbal remedy St John's wort (Hypericum perforatum).
|Food Interaction||St John's wort may increase theophylline levels. Avoiding giving enteral feed for 1 hour before or after theophylline to prevent reduction in theophylline levels.|
|Lab Interference||May cause false positive elevations of serum uric acid (by Bittner or colorimetric method) and increase in urinary catecholamines. Serum theophylline concentrations may be falsely elevated by furosemide, sulfathiazole, phenylbutazone, probenecid, theobromine, caffeine-containing beverages, chocolate and paracetamol if measured by spectrophotometric methods. Theophylline can inhibit the effects of adenosine infusions used in conjunction with radionuclide myocardial imaging, if not withheld 12-24 hr before procedure; reduces the diagnostic accuracy of myocardial imaging using dipyridamole.|
|Pregnancy Category (FDA)||Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.|
|Pharmacology||Mechanism of Action
Theophylline 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., non-bronchodilator prophylactic effects). While the mechanisms of action of theophylline are not known with certainty, studies in animals suggest that bronchodilatation is mediated by the inhibition of two isozymes of phosphodiesterase (PDE III and, to a lesser extent, PDE IV) while non-bronchodilator prophylactic actions are probably mediated through one or more different molecular mechanisms, that do not involve inhibition of PDE III or antagonism of adenosine receptors. Some of the adverse effects associated with theophylline appear to be mediated by inhibition of PDE III (e.g., hypotension, tachycardia, headache, and emesis) and adenosine receptor antagonism (e.g., alterations in cerebral blood flow).
Theophylline increases the force of contraction of diaphragmatic muscles. This action appears to be due to enhancement of calcium uptake through an adenosine-mediated channel.
Theophylline competitively blocks phosphodiesterase which increases cAMP tissue concentrations causing bronchodilatation, diuresis, CNS and cardiac stimulation, and gastric acid secretion.
|ATC Classification||R03DA04 - theophylline; Belongs to the class of other systemic drugs used in the treatment of obstructive airway diseases, xanthines.|
|Brand Name||Manufacturer/Marketer||Composition||Dosage Form||Pack Size & Price|
|Arofil 300||Incepta Pharmaceuticals Limited||Each film coated tablet contains Theophylline BP 300 mg in a sustained release formulation||SR Tablet||10x5's:MRP 117.5 Tk|
|Arofil 400||Incepta Pharmaceuticals Limited||Each film coated tablet contains Theophylline BP 400 mg in a sustained release formulation||SR Tablet||10x5's:MRP 149 Tk|
|ASMACON SR||Pacific Pharmaceuticals Ltd.||Theophylline Anhydrous 400mg||Tablet (sustained release)||50's: 133.50 MRP|
|ASMAIN||Edruc Limited||Theophylline sodium glycinate 120mg/5ml||Syrup||100ml: 25.00 MRP|
|ASMALOC 300 SR||Sharif Pharmaceuticals Ltd.||Theophylline sodium glycinate 300mg||Tablet (sustained release)||50's: 100.00 MRP|
|ASMALOC 400 SR||Sharif Pharmaceuticals Ltd.||Theophylline sodium glycinate 400mg||Tablet (sustained release)||50's: 133.50 MRP|
|CONTIFIL 300||Square Pharmaceuticals Ltd.||Theophylline 300mg||SR Tablet||10x10's: 236.00 MRP|
|CONTIFIL 400||Square Pharmaceuticals Ltd.||Theophylline 400mg||SR Tablet||3x10's: 89.70 MRP|
|CONTINE||Aristopharma Ltd.||Theophylline sodium glycinate 200mg & 300mg||Tablet||100's each: 149.00 & 210.00 MRP|
|CONTINE Syrup||Aristopharma Ltd.||Theophylline sodium glycinate 55mg/5ml||Syrup||100ml: 30.95 MRP|
|CONTINE-400||Aristopharma Ltd.||Theophylline Anhydrous 400mg||Tablet (controlled release)||100's: 267.00 MRP|
|G-THEOPHYLLINE||Gonoshasthaya Pharmaceuticals Ltd||Theophylline sodium glycinate 300mg||Tablet||100's: 82.00 MRP|
|G-THEOPHYLLINE Syrup||Gonoshasthaya Pharmaceuticals Ltd||Theophylline sodium glycinate 120mg/5ml||Syrup||100ml: 15.05 MRP|
|JASOPHYLIN||Jayson Pharmaceuticals Ltd.||Theophylline sodium glycinate 300mg||Tablet||100's: 131.00 MRP|
|JASOPHYLIN Syrup||Jayson Pharmaceuticals Ltd.||Theophylline sodium glycinate 120mg/5ml||Syrup||100ml: 25.10 MRP|
|NEULYN SR||Orion Pharma Ltd.||Theophylline sodium glycinate 400mg||Tablet||100's: 251.00 MRP|
|OD PHYLLINE||Sun Pharmaceutical (Bangladesh) Ltd.||Theophylline Anhydrous 400mg||Tablet (controlled release)||50's: 133.50 MRP|
|THEINULATE TR||The Acme Laboratories Ltd.||Theophylline sodium glycinate 300mg||Capsule (timed release)||100's: 294.00 MRP|
|THENGLATE||The Acme Laboratories Ltd.||Theophylline sodium glycinate 120mg/5ml||Syrup||100ml: 30.95 MRP|
|THENGLATE SR||The Acme Laboratories Ltd.||Theophylline sodium glycinate 250mg & 400mg||Tablet (sustained release)||50's each: 88.00 & 134.00 MRP|
|THEONATE||Doctors Chemical Works Ltd||Theophylline sodium glycinate 300mg||Tablet||100's: 131.00 MRP|
|THEONATE Syrup||Doctors Chemical Works Ltd||Theophylline sodium glycinate 120mg/5ml||Syrup||50ml, 100ml: 15.20 & 25.00 MRP|
|THEOVENT||Drug International Ltd||Theophylline sodium glycinate 300mg||Capsule||100's: 292.00 MRP|
|THEOVENT-SR||Drug International Ltd||Theophylline sodium glycinate 400mg||Tablet (sustained release)||50's: 134.00 MRP|
|UNIKON||IBN SINA Pharmaceutical Industry Ltd.||Theophylline sodium glycinate 120mg/5ml||Syrup||100ml: 26.00 MRP|
|UNIKON SR||IBN SINA Pharmaceutical Industry Ltd.||Theophylline sodium glycinate 400mg||Tablet (sustained release)||100's: 268.00 MRP|
|UNILIN||Opsonin Pharma Limited||Theophylline sodium glycinate 120mg/5ml||Syrup||50ml, 100ml: 15.26& 23.77 MRP|
|UNILIN CR 200||Opsonin Pharma Limited||Theophylline Anhydrous 200mg||Tablet (controlled release)||100's: 154.00 MRP|
|UNILIN CR 300||Opsonin Pharma Limited||Theophylline Anhydrous 300mg||Tablet (controlled release)||100's: 200.00 MRP|
|UNILIN CR 400||Opsonin Pharma Limited||Theophylline Anhydrous 400mg||Tablet (controlled release)||100's: 267.00 MRP|
|| See FDA approved Brand Manufacturer's Prescribing Information |
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