Tìm theo
Aminophylline
Các tên gọi khác (3) :
  • Aminophyllin
  • Somophyllin
  • Theophylline ethylenediamine
Thuốc tác dụng trên đường hô hấp
Thuốc Gốc
Small Molecule
CAS: 317-34-0
ĐG : Amend
CTHH: C16H24N10O4
PTK: 420.4264
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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H24N10O4
Phân tử khối
420.4264
Monoisotopic mass
420.198199306
InChI
InChI=1S/2C7H8N4O2.C2H8N2/c2*1-10-5-4(8-3-9-5)6(12)11(2)7(10)13;3-1-2-4/h2*3H,1-2H3,(H,8,9);1-4H2
InChI Key
InChIKey=FQPFAHBPWDRTLU-UHFFFAOYSA-N
IUPAC Name
bis(1,3-dimethyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione); ethane-1,2-diamine
Traditional IUPAC Name
ethylenediamine; bis(theophylline)
SMILES
NCCN.CN1C2=C(NC=N2)C(=O)N(C)C1=O.CN1C2=C(NC=N2)C(=O)N(C)C1=O
Độ hòa tan
2E+005 mg/L
logP
-3.03
pKa (strongest acidic)
7.82
pKa (Strongest Basic)
-0.78
PSA
69.3 Å2
Refractivity
44.93 m3·mol-1
Polarizability
16.86 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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. 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.
Dược Động Học :

▧ Volume of Distribution :
* 0.3 to 0.7 L/kg
▧ Protein binding :
60%
▧ 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]
Chỉ Định : For the treatment of bronchospasm due to asthma, emphysema and chronic bronchitis.
Tương Tác Thuốc :
  • Aciclovir 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.
  • Rifampicin 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
Liều Lượng & Cách Dùng : Solution - Intravenous
Tablet - Oral
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Minomal
  • Công ty :
    Sản phẩm biệt dược : Phyllocontin
  • Công ty :
    Sản phẩm biệt dược : Somophyllin
  • Công ty :
    Sản phẩm biệt dược : Truphylline
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01223
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=9433
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508784
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00227
ChemSpider
http://www.chemspider.com/Chemical-Structure.9062.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0517-3810-25
PharmGKB
http://www.pharmgkb.org/drug/PA164781029
Wikipedia
http://en.wikipedia.org/wiki/Aminophylline
Drugs.com
http://www.drugs.com/cdi/aminophylline.html
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