Definition
A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLYL CYCLASES and cyclic AMP.
Constit. of tea leaves (Camellia thea) and maté (Ilex paraguariensis) Theophylline, also known as dimethylxanthine, is a methylxanthine drug used in therapy for respiratory diseases such as COPD and asthma under a variety of brand names. As a member of the xanthine family, it bears structural and pharmacological similarity to caffeine. It is naturally found in tea and in cocoa beans. (Wikipedia)
Liquorice or licorice is the root of Glycyrrhiza glabra from which a somewhat sweet flavor can be extracted. The liquorice plant is a legume that is native to southern Europe and parts of Asia. It is not botanically related to anise, star anise, or fennel, which are sources of similar flavouring compounds. It is a herbaceous perennial, growing to 1 m in height, with pinnate leaves about 7?15 cm (3?6 in) long, with 9?17 leaflets. The flowers are 0.8?1.2 cm (??½ in) long, purple to pale whitish blue, produced in a loose inflorescence. The fruit is an oblong pod, 2?3 cm (1 in) long, containing several seeds. The roots are stoloniferous.
Description
A methylxanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Mechanistically, theophylline acts as a phosphodiesterase inhibitor, adenosine receptor blocker, and histone deacetylase activator. Theophylline is marketed under several brand names such as Uniphyl and Theochron, and it is indicated mainly for asthma, bronchospasm, and COPD.
Theophylline is Found in These Foods
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Theophylline Health Effects
- Allergenic
- (+)-inotropic
- Anti apneic
- Anti asthmatic
- Anti bradyarrhythmic
- Anti bronchitic
- Anti cellulitic
- Antidote
- Anti emphysemic
- Anti neuralgic
- Anti rhinitic
- Anti spasmodic
- Anti viral
- Arteriodilator
- Bronchodilator
- CAMP inhibitor
- Cardiovascular
- CGMP inhibitor
- CGMP-phosphodiesterase inhibitor
- Choleretic
- Central nervous system stimulant
- Diuretic
- Fetotoxic
- Herbicide
- Hypertensive
- Hyperuricemic
- Hypoglycemic
- Myocardiotonic
- Pesticide
- Prostaglandin secretor
- Stimulant
- Tachycardic
- Teratogenic
- Vasodilator
- CAMP-phosphodiesterase inhibitor
- Myorelaxant
General Information
- Metabolism: Hepatic. Biotransformation takes place through demethylation to 1-methylxanthine and 3-methylxanthine and hydroxylation to 1,3-dimethyluric acid. 1-methylxanthine is further hydroxylated, by xanthine oxidase, to 1-methyluric acid. About 6% of a theophylline dose is N-methylated to caffeine. Caffeine and 3-methylxanthine are the only theophylline metabolites with pharmacologic activity. Route of Elimination: Theophylline does not undergo any appreciable pre-systemic elimination, distributes freely into fat-free tissues and is extensively metabolized in the liver. Renal excretion of unchanged theophylline in neonates amounts to about 50% of the dose, compared to about 10% in children older than three months and in adults. Half Life: 8 hours
- Uses/Sources: For the treatment of the symptoms and reversible airflow obstruction associated with chronic asthma and other chronic lung diseases, such as emphysema and chronic bronchitis.
- Symptoms: Symptoms of overdose include seizures, arrhythmias, and GI effects.
- Route of Exposure: Theophylline is rapidly and completely absorbed after oral administration in solution or immediate-release solid oral dosage form.
Mechanism of Action
| Target Name | Mechanism of Action | References |
|---|---|---|
|
Adenosine receptor A1 cAMP-specific 3',5'-cyclic phosphodiesterase 4B Adenosine receptor A2a cAMP-specific 3',5'-cyclic phosphodiesterase 4A cGMP-specific 3',5'-cyclic phosphodiesterase Histone deacetylase 2 Adenosine receptor A2b cGMP-inhibited 3',5'-cyclic phosphodiesterase A Transcription factor E2F1 |
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