Theophylline
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| Trade names | Theolair, Slo-Bid |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a681006 |
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| Routes of administration |
By mouth, IV, rectal |
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| Pharmacokinetic data | |
| Bioavailability | 100% (IV) |
| Protein binding | 40% (primarily to albumin) |
| Metabolism | Hepatic to 1-methyluric acid |
| Biological half-life | 5–8 hours |
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| ECHA InfoCard | 100.000.350 |
| Chemical and physical data | |
| Formula | C7H8N4O2 |
| Molar mass | 180.164 g/mol |
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Theophylline, also known as 1,3-dimethylxanthine, is a methylxanthine drug used in therapy for respiratory diseases such as chronic obstructive pulmonary disease (COPD) and asthma under a variety of brand names. As a member of the xanthine family, it bears structural and pharmacological similarity to theobromine and caffeine. A small amount of theophylline is one of the products of caffeine metabolic processing in the liver.
The main actions of theophylline involve:
The main therapeutic uses of theophylline are aimed at:
A clinical study reported in 2008 that theophylline was helpful in improving the sense of smell in study subjects with anosmia.
The use of theophylline is complicated by its interaction with various drugs and by the fact that it has a narrow therapeutic index; its use must be monitored by direct measurement of serum theophylline levels to avoid toxicity. It can also cause nausea, diarrhea, increase in heart rate, abnormal heart rhythms, and CNS excitation (headaches, insomnia, irritability, dizziness and lightheadedness). Seizures can also occur in severe cases of toxicity, and are considered to be a neurological emergency. Its toxicity is increased by erythromycin, cimetidine, and fluoroquinolones, such as ciprofloxacin. It can reach toxic levels when taken with fatty meals, an effect called dose dumping. Theophylline toxicity can be treated with beta blockers. In addition to seizures, tachyarrhythmias are a major concern.
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Wikipedia