药品详细
Oxtriphylline(胆茶碱)
化学结构式图
中文名
胆茶碱
英文名
Oxtriphylline
分子式
C12H21N5O3
化学名
(2-hydroxyethyl)trimethylazanium; 1,3-dimethyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-7-ide
分子量
Average: 283.3268
Monoisotopic: 283.164439563
Monoisotopic: 283.164439563
CAS号
4499-40-5
ATC分类
R03D 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
Oxtriphylline is the choline salt form of theophylline. Once in the body, theophylline is released and acts as a phosphodiesterase inhibitor, adenosine receptor blocker, and histone deacetylase activator. Its main physiological reponse is to dilate the bronchioles. As such, oxytriphylline is indicated mainly for asthma, bronchospasm, and COPD (i.e. all the same indications as the other theophyllines). It is marketed under the name Choledyl SA, and several forms of oxytriphylline have been discontinued. In the US, oxtriphylline is no longer available.
生产厂家
- Morton grove pharmaceuticals inc
- Parke davis div warner lambert co
- Warner chilcott bermuda ltd
- Watson laboratories inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
药理
| Indication | Used to treat the symptoms of asthma, bronchitis, COPD, and emphysema. |
| Pharmacodynamics | Oxtriphylline is a bronchodilator. Oxtriphylline works in several ways: it relaxes muscles in your lungs and chest to allow more air in, decreases the sensitivity of your lungs to allergens and other substances that cause inflammation, and increases the contractions of your diaphragm to draw more air into the lungs. |
| Mechanism of action | Oxtriphylline is a choline salt of theophylline. After ingestion, theophylline is released from oxytriphylline, and 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. In inflammatory states, theophylline activates histone deacetylase to prevent transcription of inflammatory genes that require the acetylation of histones for transcription to begin. |
| Absorption | After ingestion, theophylline is released from oxytriphylline in the acidic environment of the stomach. |
| Volume of distribution | Theophylline has an apparent volume of distribution of 0.3–0.7 L/kg in children and adults, and the Vd is about twice that of an adult in premature infants. |
| Protein binding | With a serum concentrations of 17 mcg/mL, adults and children have about 56% theophylline bound to plasma protein, and premature infants have about 36%. |
| Metabolism |
Theophylline undergoes hepatic metabolism to 1,3-dimethyluric acid, 1-methyluric acid, and 3-methylxanthine.
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| Route of elimination | The kidneys are the main route of elimination for both theophylline and its metabolites, but some unchanged theophylline is eliminated in the feces. |
| Half life | The serum half life varies greatly between patients and in age. The half life range for a healthy, nonsmoking adult is 3-12.8 hours, for children is 1.5–9.5 hours, and for for premature infants is 15–58 hours. |
| Clearance | Theophylline has an average clearance in children (over 6 months) of 1.45 mL/kg per minute, and in healthy, nonsmoking adults of 0.65 mL/kg per hour. |
| Toxicity | Symptoms of toxicity include abdominal pain (continuing or severe), confusion or change in behavior, convulsions (seizures), dark or bloody vomit, diarrhea, dizziness or lightheadedness, fast and/or irregular heartbeat, nervousness or restlessness (continuing), and trembling (continuing). |
| Affected organisms |
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| Pathways | Not Available |
理化性质
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Acyclovir | Aciclovir may increase the effect and toxicity of oxtriphylline. |
| Adenosine | This xanthine decreases the effect of adenosine |
| Amobarbital | The barbiturate, amobarbital, decreases the effect of oxtriphylline. |
| Aprobarbital | The barbiturate, aprobarbital, decreases the effect of oxtriphylline. |
| Atracurium | Theophylline decreases the effect of muscle relaxant |
| Butabarbital | The barbiturate, butabarbital, decreases the effect of oxtriphylline. |
| Butalbital | The barbiturate, butalbital, decreases the effect of oxtriphylline. |
| Butethal | The barbiturate, butethal, decreases the effect of oxtriphylline. |
| Carbamazepine | Carbamazepine may decrease the serum concentration of oxtriphylline. Oxtriphylline may decrease the serum concentration of carbamazepine. Monitor for changes in the therapeutic effect of both agents if concomitant therapy is initiated, discontinued or dose changed. |
| Carteolol | Antagonism of action and increased effect of theophylline |
| Cimetidine | Cimetidine may increase the serum concentration of oxtriphylline by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of oxtriphylline if cimetidine is initiated, discontinued or dose changed. |
| Ciprofloxacin | Ciprofloxacin may increase the effect of oxtriphylline. |
| Clarithromycin | Clarithromycin may increase the effect and toxicity of oxtriphylline. |
| Dihydroquinidine barbiturate | The barbiturate, dihydroquinidine barbiturate, decreases the effect of oxtriphylline. |
| Disulfiram | Disulfiram may increase the effect and toxicity of oxtriphylline. |
| Doxacurium chloride | Theophylline decreases the effect of muscle relaxant |
| Enoxacin | Enoxacin may increase the effect of oxtriphylline. |
| Erythromycin | The macrolide, erythromycin, may increase the effect and toxicity of the theophylline derivative, oxtriphylline. |
| Ethinyl Estradiol | The contraceptive increases the effect and toxicity of theophylline |
| Ethotoin | Decreased effect of both products |
| Fluvoxamine | Fluvoxamine may increase the therapeutic and adverse effects of oxtriphylline. |
| Fosphenytoin | Decreased effect of both products |
| Grepafloxacin | Grepafloxacin may increase the effect of oxtriphylline. |
| Halothane | Increased risk of cardiac arrhythmia |
| Heptabarbital | The barbiturate, heptabarbital, decreases the effect of oxtriphylline. |
| Hexobarbital | The barbiturate, hexobarbital, decreases the effect of oxtriphylline. |
| Interferon Alfa-2a, Recombinant | Interferon increases the effect and toxicity of theophylline |
| Interferon Alfa-2b, Recombinant | Interferon increases the effect and toxicity of theophylline |
| Interferon alfa-n1 | Interferon increases the effect and toxicity of theophylline |
| Isoniazid | Isoniazid may increase the effect and toxicity of oxtriphylline. |
| Josamycin | The macrolide, josamycin, may increase the effect and toxicity of the theophylline derivative, oxtriphylline. |
| Lithium | Theophylline decreases serum levels of lithium |
| Mephenytoin | Decreased effect of both products |
| Mestranol | The contraceptive increases the effect and toxicity of theophylline |
| Methohexital | The barbiturate, methohexital, decreases the effect of oxtriphylline. |
| Methylphenobarbital | The barbiturate, methylphenobarbital, decreases the effect of oxtriphylline. |
| Metocurine | Theophylline decreases the effect of muscle relaxant |
| Mexiletine | Mexiletine increases the effect and toxicity of theophylline |
| Mivacurium | Theophylline decreases the effect of muscle relaxant |
| Nadolol | Antagonism of action and increased effect of theophylline |
| Norfloxacin | Norfloxacin may increase the effect of oxtriphylline. |
| Pancuronium | Theophylline decreases the effect of muscle relaxant |
| Pefloxacin | Pefloxacin may increase the effect of oxtriphylline. |
| Peginterferon alfa-2a | Interferon increases the effect and toxicity of theophylline |
| Peginterferon alfa-2b | Interferon increases the effect and toxicity of theophylline |
| Penbutolol | Antagonism of action and increased effect of theophylline |
| Pentobarbital | The barbiturate, pentobarbital, decreases the effect of oxtriphylline. |
| Pentoxifylline | Pentoxifylline increases the effect and toxicity of theophylline |
| Phenobarbital | The barbiturate, phenobarbital, decreases the effect of oxtriphylline. |
| Phenytoin | Decreased effect of both products |
| Pindolol | Antagonism of action and increased effect of theophylline |
| Primidone | The barbiturate, primidone, decreases the effect of oxtriphylline. |
| Propafenone | Propafenone increases the effect of theophylline |
| Propranolol | Antagonism of action and increased effect of theophylline |
| Quinidine barbiturate | The barbiturate, quinidine barbiturate, decreases the effect of oxtriphylline. |
| Rifampin | Rifampin may decrease the effect and toxicity of oxtriphylline. |
| Ritonavir | Ritonavir decreases the effect of theophylline |
| Rofecoxib | Rofecoxib increases the effect and toxicity of theophylline |
| Secobarbital | The barbiturate, secobarbital, decreases the effect of oxtriphylline. |
| Sotalol | Antagonism of action and increased effect of theophylline |
| St. John's Wort | St. John's Wort decreases the effect of theophylline |
| Tacrine | Tacrine increases the effect and toxicity of theophylline |
| Talbutal | The barbiturate, talbutal, decreases the effect of oxtriphylline. |
| Terbinafine | Terbinafine increases the effect and toxicity of theophylline |
| Thiabendazole | Thiabendazole increases the effect and toxicity of theophylline |
| Ticlopidine | Ticlopidine increases the effect and toxicity of theophylline |
| Timolol | Antagonism of action and increased effect of theophylline |
| Troleandomycin | The macrolide, troleandomycin, may increase the effect and toxicity of the theophylline derivative, oxtriphylline. |
| Tubocurarine | Theophylline decreases the effect of muscle relaxant |
| Vecuronium | Theophylline decreases the effect of muscle relaxant |
| Verapamil | Verapamil increases the effect of theophylline |
| Zileuton | Zileuton increases the effect and toxicity of theophylline |
食物相互作用
- Avoid high doses of caffeine.
- Take with food to reduce irritation.
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