mph Bangladesh


Theophylline

(the off'' i lin)

PCaution when used during lactation / LCaution when used during lactation : Caution - during pregnancy & lactation

Molecule Info

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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.

Oral route
Acute bronchospasm
Adult: As conventional tablet: 5 mg/kg every 6-8 hr.
Child: As conventional tablet: 5 mg/kg every 4-6 hr.

Chronic bronchospasm
Adult: As conventional dosage form: 300-1000 mg in divided doses, every 6-8 hr daily. As modified-release preparations: 175-500 mg every 12 hr. Rate of absorption of modified released preparations varies for different brands.
Child: <2 yr: Not recommended; 2-6 yr: ¼ the adult dose; 20-35 kg (about 6-12 yr old): ½ the adult dose. Rate of absorption of modified released preparations varies for different brands.

Apnoea in infants
Child: Initial dose in neonates: <24 days: 1 mg/kg every 12 hr; >24 days: 1.5 mg/kg every 12 hr. Full-term infants: initial daily dosage calculated based on formula, given in 3-4 divided doses: daily dose (mg/kg) = (0.2 X age in wk) + 5.0. If loading dose is needed, 5 mg/kg (or in those already on theophylline, 1 mg/kg for each 2 mcg/ml increase in serum-theophylline concentration).

Intravenous

Severe bronchospasm
Adult: Patients who are not taking theophylline or other xanthine medication: 4-5 mg/kg as loading dose by IV infusion over 20-30 minutes followed by maintenance: 0.4 mg/kg/hr. 
Child: Patients who are not taking theophylline or other xanthine medication: 4-5 mg/kg as loading dose by IV infusion over 20-30 minutes, followed by maintenance dose: 1-9 yr: 0.8 mg/kg/hr; >9 yr: 0.6-0.7 mg/kg/hr.

Special Populations: Reduce dose in patients with cor pulmonale, heart failure, liver disease and in the elderly. Increase maintenance dose for smokers.

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 βblockers 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.
Drug Interactions

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.
Absorption: Rapid and completely absorbed following oral and rectal (enemas) administration, slow after rectal (suppositories) and IM administration. Food delays rate but not extent of absorption. Peak serum concentrations: 1-2 hr (liquid, capsules or uncoated tablets); 4 hr (modified-release preparations).
Distribution: Rapidly distributed throughout extracellular fluids and body tissues. Crosses the placenta and enters breast milk. Protein binding: 40%.
Metabolism: Hepatic metabolism via cytochrome P450 isoenzyme CYP1A2, CYP2E1 and CYP3A3. Serum half-life: 6-12 hr (healthy, non-smoking asthmatic adult); 1-5 hr (children); 4-5 hr (cigarette smokers); 10-45 hr (neonates and premature infants).
Excretion: Via urine as metabolites and unchanged drug; small amount via faeces as unchanged drug.

ATC Classification R03DA04 - theophylline; Belongs to the class of other systemic drugs used in the treatment of obstructive airway diseases, xanthines.

Brand/Product Info


Total Products : 30                              
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
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