Theophylline

Theophylline is a 1, 3-dimethylxanthine. its major source is beverages (tea, cocoa and coffee). Theophylline is used as a bronchodilator. It improves breathing by opening air passages in the lungs. The importance of it in the treatment of asthma as a therapeutic agent is waning as the greater effectiveness of inhaled adrenoceptor agents for acute asthma and of inhaled anti-inflammatory agents for chronic asthma has been established.


Adult Dose
Dose: 300 mg
Single Dose: 300 (300)
Frequency: As recommended.
Route: PO
Instructions: Should be given in divided doses. Frequency may be increased upto 4 times/day if needed.
Neonatal
Paedriatic
Dose: 10 to 12 mg/kg
Single Dose: 11 (11)
Frequency: 12 hourly
Route: Oral
Instructions: SR Dose
Characteristics
. It is of Natural origin and belongs to Alkaloid. It belongs to Phosphodiesterase inhibitor pharmacological group on the basis of mechanism of action and also classified in Bronchodilator pharmacological group.The Molecular Weight of Theophylline is 180.20. It is weakly alkaline drug, 2.94% solution of the drug is isotonic and Its pKa is 8.8.
Contraindications
Theophylline
Effects
Theophylline produces potentially life-threatening effects which include Seizures, Cardiac arrhythmias, Neurotoxicity. which are responsible for the discontinuation of Theophylline therapy.The signs and symptoms that are produced after the acute overdosage of Theophylline include Hypotension, Cardiac arrhythmias, Hypokalemia, Metabolic acidosis, GI hemorrhage, Nausea & vomiting, Rhabdomyolysis.The symptomatic adverse reactions produced by Theophylline are more or less tolerable and if they become severe, they can be treated symptomatically, these include Headache, Irritability, Nausea, Anorexia, Anxiety, Tremors, Insomnia, Nervousness, Depression, Sinus tachycardia.
Indications
Theophylline is primarily indicated in conditions like Acute severe asthma, Apnoea of prematurity, Asthma, Obstructive airway disease, Reversible airways obstruction, and can also be given in adjunctive therapy as an alternative drug of choice in Cheyne stokes respiration.
Interactions
Theophylline is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAcrosoxacinAdenosineTheophylline antagonise anti-arrhythmic effect of adenosine.AlbuterolAn enhanced hypokalemic effect may occur during co administration of salbutamol and theophylline AlcoholAllopurinolAllopurinol possibly increases plasma concentration of theophylline by inhibiting its metabolism results in increased toxicity.MinorClosely monitor for theophylline toxicity.AminoglutethimideAminoglutethimide accelerates the metabolism of theophylline (reduced effects).Amiodarone (HCl)amiodarone cause decrease in metabolism of theophylline leads to theophylline toxicity.Moderatepatients response and tolerance should be monitored.Amlodipine (Besylate)Amlodipine increases plasma concentration of theophylline.AzithromycinAzithromycin possibly increases plasma concentration of Theophylline.BambuterolIncreased risk of hyporkalemia when high doses of Bambuterol given with Theophylline.Bisoprolol (Fumarate)Bisoprolol reduces the CYP450 hepatic metabolism of theophylline and its serum levels may be increased.MajorClosely monitored the increased serum level of theophylline and decreased bronchodilatory effectiveness.CannabisCarbamazepineBoth agents decreases their serum levels due to inhibition of hepatic metabolism.ModerateClose observation for altered effects of both agents is recommended.CarmustineCeliprolol (HCl)Chlortetracycline (HCl)Cimetidine (HCl)Cimetidine (HCl)CinoxacinCiprofloxacinCiprofloxacin enhances the serum level of theophylline by inhibiting its metabolism and by reducing its clearence upto 65% may result in increased risk of toxicity. Concomitant use of theohylline with interavenous ciprofloxacin may results cardiac arrest, seizure,status epilepticus and respiratory failure.MajorConcomitant use should be avoided. Closely monitor the pharmacologic response and serum level of theophylline whenever start, discontinue or change the dose of ciprfloxacin.Patient should notify the symptoms of theophylline toxicity.Clarithromycinthe Cmax of theophylline increase upon repeated dose of clarithmycin Monitoring of Theophylline concentration during concomitant administration is recommendedClopidogrelDeflazacortDemeclocycline (HCl)Diltiazem (HCl)Diltiazem inhibit the CYP450 3A4 hepatic metabolism of Theophylline results in increased serum level of theophylline.ModerateClinical monitoring of response and tolerance is recommended. Report should be given if observe any sign of theophylline toxicity.DoxapramEnoxacinEphedrineCoadministration may increases the side effects of theophylline because of synergistic pharmacological effects.MinorClosely monitor the patient for side effects of theophylline.ErythromycinSerum concentration of theophylline is icreased by erythromycin due to CYP450 3A4 inhibition result in seizures in pediatric patient. Clearance of theophylline is reduced 83% by oral erythromycinModeratePatient response and serum theophylline levels should be monitor if erythromycin given with theophylline.Fluconazoletheophylline decrease mean plasma concentration of fluconazolelook for sign and symptoms of theophylline toxicityFluticasone PropionateFluvoxamine (Maleate)FosphenytoinGallopamilHalothaneInfluenza VaccineInterferon AlphaInterferon AlphaInterferon Alpha 2aIpriflavoneIsoproterenolKetoconazoleCo-administration decreases serum theophylline concentration by decreased absorption.MinorDose adjustment is necessary. Altered efficacy of theophylline should be monitored.LansoprazoleLevobunolol (HCl)LevofloxacinLevofloxacin decrease the clearance of theophylline and caffeine.LithiumMethotrexateMethotrexate reduces oral theophylline clearance.ModerateClose monitoring of theophylline serum level and signs of toxicity.MexiletineMinocycline (HCl)ModafinilConcomitant use may decrease the efficacy of modafinil.Moricizine (HCl)Nebivolol (HCl)Concurrent use may decrease the extent of absorption of Nebivolol (HCl).NelfinavirNevirapineNicotineEspecially inform your doctor if you are using this combination.NifedipineNorfloxacinObidoxime (Cl)OfloxacinOmeprazoleOmeprazole may inhibit the absorption of theophyllineOrciprenaline (Sulphate)OxpentifyllineOxpentifylline increases the effect and toxicity of theophylline.Pancuronium (Br)Peginterferon Alfa-2a (rbe)Should not be used concurrently without doctors prescription.PenbutololPharmacological effect of these agents are opposite. Penbutolol cause bronchoconstriction while theophylline cause bronchodilation.Penbutolol also decreases the metabolism of theophylline thus increases its serum level result in increased toxicity.MajorThis combination is considered contraindicated. If necessary to take this combination so closely monitor the patient for increased serum level of theophylline.PentoxifyllinePhenytoin (Na)Pipemidic AcidPralidoximePropafenone (HCl)Propranolol (HCl)PropylthiouracilTheophylline clearance may decrease when hyperthyroid patients on a stable theophylline regimen become euthyroid.A reduced dose of theophylline may be needed.ProtirelinQuazepamMay partially antagonize some of the effects of benzodiazepines. Monitor for decreased response; may require higher doses for sedation.Quinalbarbitone (Na)RifampicinRifampicinRiluzoleTheophylline could decrease the rate of riluzole elimination.Riociguatcause hypotensioncontraindicatedRitonavirRofecoxibRofecoxib 12.5, 25, and 50 mg administered once daily for 7 days increased plasma theophylline concentrations by 38 to 60%.RoflumilastRoflumilast when co administer with theophylline reult in 8% incerase in the roflumilast PDE4 Inhibitory effect.SalmeterolConcurrent use may potentiate the risk of adverse effects.SparfloxacinSt.Johns Wort ExtractSerum theophylline levels were decreased with concomitant ingestion of St. Johns wort.StilboestrolSucralfateSulphinpyrazoneSulphinpyrazoneSulphinpyrazone increases the clearence of theophylline by 22% by increasing metabolism and decreasing its renal clearence.MinorClosely monitor the serum level of theophylline. Patient should report the worsening of respiratory symptoms to physician.Tacrine (HCl)TerbutalineTetracycline (HCl)ThiabendazoleThiabendazoleTiclopidine (HCl)Tocainide (HCl)TriamcinoloneVecuronium (Br)Verapamil (HCl)Vidarabine (Monohydrate)VORICONAZOLEVoriconazole may increase the serum concentration of theophylline by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects ZafirlukastZileuton These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Interfere with Bittner Method for Serum Uric Acid Measurement
Risks
Drug should not be given to Pregnant Mothers, Cardiac / Hypertensive Patients, patients suffering from Kidney dysfunction, patients suffering from Liver Malfunction, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Tab, Syrup Store in a well closed container, Below 40°C. Protect from Sunlight and Moisture.
Warnings
Theophylline should be used with caution in patients with severe cardiac, kidney or liver disease, hyperthyroidism, congestive heart failure (CHF), peptic ulcer. It should be used with caution in neonates and elderly persons.
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