Τόμος 3 (1989) – Τεύχος 1 – Άρθρο 3 – Επιθεώρηση Κλινικής Φαρμακολογίας και Φαρμακοκινητικής-Διεθνής Έκδοση – Volume 3 (1989) – Issue 1 – Article 3 – Epitheorese Klinikes Farmakologias και Farmakokinetikes-International Edition

Title Clinically important drug interactions with theophylline
Author George N. Karachalios

3rd Department of Internal Medicine, Red Cross Hospital, Athens, Greece

Citation Karachalios, G.N.: Clinically important drug interactions with theophylline, Epitheorese Klin. Farmakol. Farmakokinet. 3(1): 22-45 (1989)
Publication Date 1989-07
Full Text Language English
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Keywords Theophilline, drug, liver, biotransformation, demethylation, oxidation, elimination, interaction.
Other Terms review article
Summary Theophilline is a drug widely used as a bronchodilator agent in patients with obstructive lung disease. Theophylline is eliminated mainly by biotransformation in the liver (by demethylation and oxidation); about 10% of administered theophylline is recovered in the urine unchanged. As a result, drugs and other substances affecting liver microsomal enzyme systems may alter theophylline elimination, i.e. the drug is susceptible to enzymatic induction and inhibition. Therefore, drug interactions with theophylline have a great importance. Many drugs (e.g. josamycin, amoxycillin, tetracyfine, antiacids, etc) appear not to significantly affect theophylline clearance. Elimination of theophylline is decreased by some drugs (e.g. erythromycin, cimetidine, oral contraceptives, allopurinol, etc) taken at the same time; these interactions lead to increased theophylline steady-state serum concentrations, so that the dose of theophylline may have to be reduced to avoid possible theophylline toxicity. On the other hand, other drugs (e.g. phenobarbitone, phenytain, carbamazepine, rifampicin, isoniazid, sulphinpyrazone, etc) enhance theophylline elimination, making an increase in the dose of concurrent theophylline advisable. In the two latter cases special care is needed if any of these drugs are stopped in a patient under theophylline treatment. In practice, to minimize the clinical consequences of drug interactions with theophylline, its serum concentrations must be monitored closely. As a result of drug interactions with theophylline, its dosage adjustments may be necessary or alternatively there should be prescribed drugs which do not interact with theophylline.
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