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Mechanism of Action
Theophylline¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Theophylline relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and allergen. Theophylline competitively inhibits type III and type IV phosphodiesterase (PDE), the enzyme responsible for breaking down cyclic AMP in smooth muscle cells, possibly resulting in bronchodilation. Theophylline also binds to the adenosine A2B receptor and blocks adenosine mediated bronchoconstriction.
Pharmacology
Theophylline¿¡ ´ëÇÑ Pharmacology Á¤º¸ Theophylline, an xanthine derivative chemically similar to caffeine and theobromine, is used to treat asthma and bronchospasm. Theophylline has two distinct actions in the airways of patients with reversible (asthmatic) obstruction; smooth muscle relaxation (i.e., bronchodilation) and suppression of the response of the airways to stimuli (i.e., non-bronchodilator prophylactic effects).
Protein Binding
Theophylline¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 40%, primarily to albumin.
Half-life
Theophylline¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 8 hours
Absorption
Theophylline¿¡ ´ëÇÑ Absorption Á¤º¸ Theophylline is rapidly and completely absorbed after oral administration in solution or immediate-release solid oral dosage form.
Pharmacokinetics
TheophyllineÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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Oxtriphyline(64% theophylline) : Á¦Çü¿¡ µû¶ó 75-100%±îÁö º¯ÇÑ´Ù.
Theophylline : Á¦Çü¿¡ µû¶ó 100%±îÁö Èí¼öµÊ
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Vd = 0.45L/kg
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´ë»ç : °£¿¡¼ demethylation, oxidation
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Biotransformation
Theophylline¿¡ ´ëÇÑ Biotransformation Á¤º¸ 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.
Toxicity
Theophylline¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include seizures, arrhythmias, and GI effects.
Drug Interactions
Theophylline¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
CYP450 Drug Interaction
[CYP450 TableÁ÷Á¢Á¶È¸] Theophylline¿¡ ´ëÇÑ P450 table SUBSTRATES
CYP 1A2
clozapine
cyclobenzaprine
imipramine
mexiletine
naproxen
riluzole
tacrine
**theophylline**
INHIBITORS
CYP 1A2
cimetidine
fluoroquinolones
fluvoxamine
ticlopidine
INDUCERS
CYP 1A2
tobacco
Description
Theophylline¿¡ ´ëÇÑ Description Á¤º¸ A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3&
Drug Category
Theophylline¿¡ ´ëÇÑ Drug_Category Á¤º¸ Bronchodilator AgentsPhosphodiesterase InhibitorsRespiratory Smooth Muscle RelaxantsVasodilator Agents
Smiles String Canonical
Theophylline¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN1C(=O)N(C)C2=C(NC=N2)C1=O
Smiles String Isomeric
Theophylline¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN1C(=O)N(C)C2=C(NC=N2)C1=O
InChI Identifier
Theophylline¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C7H8N4O2/c1-10-5-4(8-3-9-5)6(12)11(2)7(10)13/h3H,1-2H3,(H,8,9)/f/h8H
Chemical IUPAC Name
Theophylline¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 1,3-dimethyl-7H-purine-2,6-dione
Drug-Induced Toxicity Related Proteins
THEOPHYLLINE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸Replated Protein :Renin Drug :theophylline Toxicity :low blood pressure . [¹Ù·Î°¡±â] Replated Protein :Acid sphingomyelinase-like phosphodiesteraseDrug :Theophylline Toxicity :emetic side effect. [¹Ù·Î°¡±â] Replated Protein :Alanine aminotransferaseDrug :theophylline Toxicity :metabolic acidosis. [¹Ù·Î°¡±â]
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