药品详细

Aminophylline(氨茶碱)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

氨茶碱

英文名

Aminophylline

分子式

C₁₆H₂₄N₁₀O₄

化学名

bis(1,3-dimethyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione); ethane-1,2-diamine

分子量

Average: 420.4264
Monoisotopic: 420.198199306

CAS号

317-34-0

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

Aminophylline is a drug combination that contains theophylline and ethylenediamine in a 2:1 ratio. Once in the body, theophylline is released and acts as a phosphodiesterase inhibitor, adenosine receptor blocker, and histone deacetylase activator. Similar to other theophyllines, aminophylline is indicated for the treatment of lung diseases such as asthma, chronic bronchitis, and COPD. The majority of aminophylline medications are discontinued and the remaining medications on the market are in short supply.

生产厂家

Abraxis pharmaceutical products
Actavis mid atlantic llc
Ascot hosp pharmaceuticals inc div travenol laboratories inc
Barr laboratories inc
Duramed pharmaceuticals inc sub barr laboratories inc
Elkins sinn div ah robins co inc
Fisons corp
G and w laboratories inc
Gd searle llc
Halsey drug co inc
Hospira inc
Impax laboratories inc
International medication system
International medication systems ltd
King pharmaceuticals inc
Kv pharmaceutical co
Lannett co inc
Luitpold pharmaceuticals inc
Morton grove pharmaceuticals inc
Pal pak inc
Panray corp sub ormont drug and chemical co inc
Pharma serve inc sub torigian laboratories
Pharmaceutical research assoc inc
Purepac pharmaceutical co
Roxane laboratories inc
Sandoz inc
Smith and nephew solopak div smith and nephew
Tablicaps inc
Teva parenteral medicines inc
Vale chemical co inc
Valeant pharmaceuticals international
Vangard laboratories inc div midway medical co
Vintage pharmaceuticals inc
Watson laboratories inc
West ward pharmaceutical corp

封装厂家

Amend
C.O. Truxton Inc.
Cardinal Health
Carlisle Laboratories Inc.
Dispensing Solutions
G & W Labs
General Injectables and Vaccines Inc.
Hospira Inc.
Kaiser Foundation Hospital
Lake Erie Medical and Surgical Supply
Major Pharmaceuticals
Murfreesboro Pharmaceutical Nursing Supply
PCA LLC
Pharmedix
Prescript Pharmaceuticals
West-Ward Pharmaceuticals

参考

Synthesis Reference	Not Available
General Reference	Not Available

剂型

规格

化合物类型

Type	small molecule

Classes

Xanthines

Substructures

Aliphatic and Aryl Amines
Xanthines
Pyrimidines and Derivatives
Imidazoles
Heterocyclic compounds
Aromatic compounds
Purines and Purine Derivatives
Cyanamides

适应症

药理

Indication	For the treatment of bronchospasm due to asthma, emphysema and chronic bronchitis.
Pharmacodynamics	Aminophylline is the ethylenediamine salt of theophylline. Theophylline stimulates the CNS, skeletal muscles, and cardiac muscle. It relaxes certain smooth muscles in the bronchi, produces diuresis, and causes an increase in gastric secretion.
Mechanism of action	Aminophylline is the ethylenediamine salt of theophylline. After ingestion, theophylline is released from aminophylline, 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	Not Available
Volume of distribution	0.3 to 0.7 L/kg
Protein binding	60%
Metabolism	Not Available
Route of elimination	Not Available
Half life	7-9 hours
Clearance	0.29 mL/kg/min [postnatal age 3-15 days] 0.64 mL/kg/min [postnatal age 25-57 days] 1.7 mL/kg/min [ 1-4 years] 1.6 mL/kg/min [4-12 years] 0.9 mL/kg/min [13-15 years] 1.4 mL/kg/min [16-17 years] 0.65 mL/kg/min [Adults (16-60 years), non-smoking asthmatics] 0.41 mL/kg/min [Elderly (>60 years). liver, and renal function] 0.33 mL/kg/min [Acute pulmonary edema] 0.54 mL/kg/min [COPD→60 years, stable non-smoker >1 year] 0.48 mL/kg/min [COPD with cor pulmonale] 1.25 mL/kg/min [Cystic fibrosis (14-28 years)] 0.31 mL/kg/min [Liver disease -cholestasis] 0.35 mL/kg/min [cirrhosis] 0.65 mL/kg/min [acute hepatitis] 0.47 mL/kg/min [Sepsis with multi-organ failure] 0.38 mL/kg/min [hypothyroid] 0.8 mL/kg/min [hyperthyroid]
Toxicity	Not Available
Affected organisms	Humans and other mammals
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
water solubility	2E+005 mg/L	MERCK INDEX (1996)
logP	-3.03	Not Available

Predicted Properties

Property	Value	Source
logP	-0.77	ChemAxon
pKa (strongest acidic)	7.82	ChemAxon
pKa (strongest basic)	-0.78	ChemAxon
physiological charge	0	ChemAxon
hydrogen acceptor count	3	ChemAxon
hydrogen donor count	1	ChemAxon
polar surface area	69.3	ChemAxon
rotatable bond count	1	ChemAxon
refractivity	44.93	ChemAxon
polarizability	16.86	ChemAxon

药物相互作用

Drug	Interaction
Acyclovir	Acyclovir increases the effect and toxicity of theophylline
Adenosine	This xanthine decreases the effect of adenosine
Amobarbital	The barbiturate, amobarbital, decreases the effect of aminophylline.
Aprobarbital	The barbiturate, aprobarbital, decreases the effect of aminophylline.
Atracurium	Theophylline decreases the effect of muscle relaxant
Bromazepam	Aminophylline may decrease the therapeutic effect of bromazepam. Monitor for changes in the therapeutic effects of bromazepam if aminophylline is initiated, discontinued or dose changed.
Butabarbital	The barbiturate, butabarbital, decreases the effect of aminophylline.
Butalbital	The barbiturate, butalbital, decreases the effect of aminophylline.
Butethal	The barbiturate, butethal, decreases the effect of aminophylline.
Carbamazepine	Carbamazepine may decrease the serum concentration of aminophylline. Aminophylline 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 aminophylline by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of aminophylline if cimetidine is initiated, discontinued or dose changed.
Ciprofloxacin	Ciprofloxacin may increase the effect of aminophylline.
Clarithromycin	Clarithromycin may increase the effect amd toxicity of aminophylline.
Dihydroquinidine barbiturate	The barbiturate, dihydroquinidine barbiturate, decreases the effect of aminophylline.
Disulfiram	Disulfiram may increase the effect and toxicity of aminophylline.
Doxacurium chloride	Theophylline decreases the effect of muscle relaxant
Enoxacin	Enoxacin may increase the effect of aminophylline.
Erythromycin	The macrolide, erythromycin, may increase the effect and toxicity of the theophylline derivative, aminophylline.
Ethinyl Estradiol	The contraceptive increases the effect and toxicity of theophylline
Ethotoin	Decreased effect of both products
Fluvoxamine	Fluvoxamine may increase the effect and toxicity of aminophylline.
Fosphenytoin	Decreased effect of both products
Grepafloxacin	Grepafloxacin may increase the effect of aminophylline.
Halothane	Increased risk of cardiac arrhythmia
Heptabarbital	The barbiturate, heptabarbital, decreases the effect of aminophylline.
Hexobarbital	The barbiturate, hexobarbital, decreases the effect of aminophylline.
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, aminophylline.
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 aminophylline.
Methylphenobarbital	The barbiturate, methylphenobarbital, decreases the effect of aminophylline.
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 aminophylline.
Pancuronium	Theophylline decreases the effect of muscle relaxant
Pefloxacin	Pefloxacin may increase the effect of aminophylline.
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 aminophylline.
Pentoxifylline	Pentoxifylline may increase the effect and toxicity of aminophylline.
Phenobarbital	The barbiturate, phenobarbital, decreases the effect of aminophylline.
Phenytoin	Decreased effect of both products
Pindolol	Antagonism of action and increased effect of theophylline
Primidone	The barbiturate, primidone, decreases the effect of aminophylline.
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 aminophylline.
Regadenoson	Reduces duration of >2-fold increase in peak flow velocity. No effect on heart rate increase.
Rifampin	Rifampin decreases the effect of theophylline
Ritonavir	Ritonavir decreases the effect of theophylline
Rofecoxib	Rofecoxib increases the effect and toxicity of theophylline
Secobarbital	The barbiturate, secobarbital, decreases the effect of aminophylline.
Sotalol	Antagonism of action and increased effect of theophylline
St. John's Wort	St. John's Wort decreases the effect of theophylline
Tacrine	Tacrine may reduce the elimination rate of Aminophylline. Monitor for changes in the therapeutic and toxic effects of theophylline if Tacrine is initiated, discontinued or if the dose is changed.
Talbutal	The barbiturate, talbutal, decreases the effect of aminophylline.
Temazepam	Aminophylline may decrease the efficacy of Temazepam. Monitor for changes in the therapeutic effect of Temazepam if Aminophylline is initiated, discontinued or dose changed.
Terbinafine	Terbinafine increases the effect and toxicity of theophylline
Thiabendazole	The strong CYP1A2 inhibitor, Thiabendazole, may increase the effects and toxicity of Aminophylline by decreasing Aminophylline metabolism and clearance. Monitor for changes in the therapeutic and adverse effects of Aminophylline if Thiabendazole is initiated, discontinued or dose changed.
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 theophylline derivative, aminophylline.
Tubocurarine	Theophylline decreases the effect of muscle relaxant
Vecuronium	Theophylline decreases the effect of muscle relaxant
Verapamil	Verapamil increases the effect of theophylline
Zafirlukast	Zafirlukast serum concentrations may be decreased by the theophylline derivative Aminophylline.
Zileuton	Zileuton increases the effect and toxicity of theophylline

食物相互作用

Limit caffeine intake.
Take with food.
Vitamin B6 needs increased, supplement recommended.

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