Dyphylline

Các tên gọi khác (17 ) :

(+-)-7-(2,3-Dihydroxypropyl)theophylline
(+-)-Diprophylline
(+-)-Dyphylline
(±)-diprophylline
(±)-dyphylline
(1,2-Dihydroxy-3-propyl)thiophyllin
1,3-Dimethyl-7-(2,3-dihydroxypropyl)xanthine
7-(2,3-Dihydroxypropyl)-1,3-dimethylxanthine
7-(2,3-Dihydroxypropyl)-3,7-dihydro-1,3-dimethyl-1H-purine-2,6-dione
7-(2,3-Dihydroxypropyl)theophylline
7-(beta,gamma-Dihydroxypropyl)theophylline
7-(β,γ-dihydroxypropyl)theophylline
Dihydroxypropyl theopylin
Diprofilina
Diprophylline
Diprophyllinum
Dyphylline

phosphodiesterase inhibitors, bronchodilator agents, vasodilator agents, muscle relaxants respiratory

Thuốc Gốc

Small Molecule

CAS: 479-18-5

ATC: R03DA01

ĐG : Breckenridge Pharmaceuticals , http://www.bpirx.com

CTHH: C₁₀H₁₄N₄O₄

PTK: 254.2426

A theophylline derivative with broncho- and vasodilator properties. It is used in the treatment of asthma, cardiac dyspnea, and bronchitis. [PubChem]

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₁₀H₁₄N₄O₄

Phân tử khối

254.2426

Monoisotopic mass

254.101504956

InChI

InChI=1S/C10H14N4O4/c1-12-8-7(9(17)13(2)10(12)18)14(5-11-8)3-6(16)4-15/h5-6,15-16H,3-4H2,1-2H3

InChI Key

InChIKey=KSCFJBIXMNOVSH-UHFFFAOYSA-N

IUPAC Name

7-(2,3-dihydroxypropyl)-1,3-dimethyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione

Traditional IUPAC Name

dyphylline

SMILES

CN1C2=C(N(CC(O)CO)C=N2)C(=O)N(C)C1=O

Độ tan chảy

155-157

Độ hòa tan

3.33E+005 mg/L (at 25 °C)

logP

-1.9

logS

-0.17

pKa (strongest acidic)

13.91

pKa (Strongest Basic)

-0.97

PSA

98.9 Å²

Refractivity

62.09 m³·mol^-1

Polarizability

24.65 Å³

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

Rule of Five

true

Dược Lực Học : Dyphylline, a xanthine derivative, is a bronchodilator used for relief of acute bronchial asthma and for reversible bronchospasm associated with chronic bronchitis and emphysema. Dyphylline is a xanthine derivative with pharmacologic actions similar to theophylline and other members of this class of drugs. Its primary action is that of bronchodilation, but it also exhibits peripheral vasodilatory and other smooth muscle relaxant activity to a lesser degree.

Cơ Chế Tác Dụng : A theophylline derivative with broncho- and vasodilator properties. It is used in the treatment of asthma, cardiac dyspnea, and bronchitis. [PubChem] The bronchodilatory action of dyphylline, as with other xanthines, is thought to be mediated through competitive inhibition of phosphodiesterase with a resulting increase in cyclic AMP producing relaxation of bronchial smooth muscle as well as antagonism of adenosine receptors.

Dược Động Học :

▧ Protein binding :
84%
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Dyphylline exerts its bronchodilatory effects directly and, unlike theophylline, is excreted unchanged by the kidneys without being metabolized by the liver. Approximately 88% of a single oral dose can be recovered from the urine unchanged.
▧ Half Life :
2 hours (range 1.8 - 2.1 hours)

Độc Tính : LD₅₀=1954 mg/kg (orally in mice)

Chỉ Định : For relief of acute bronchial asthma and for reversible bronchospasm associated with chronic bronchitis and emphysema.

Tương Tác Thuốc :

Aciclovir Acyclovir increases the effect and toxicity of dyphylline.
Adenosine This xanthine decreases the effect of adenosine
Bromazepam Dyphylline may decrease the therapeutic effect of bromazepam. Monitor for changes in the therapeutic effects of bromazepam if dyphylline is initiated, discontinued or dose changed.
Carbamazepine Carbamazepine may decrease the serum concentration of diphylline. Diphylline 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.
Cimetidine Increases the effect of theophylline
Ciprofloxacin Ciprofloxacin may increase the effect of dyphylline.
Clarithromycin Increases the effect and toxicity of theophylline
Disulfiram Increases the effect and toxicity of theophylline
Erythromycin The macrolide, erythromycin, may increase the effect and toxicity of the theophylline derivative, dyphylline.
Ethinyl Estradiol The contraceptive increases the effect and toxicity of theophylline
Fluvoxamine Increases the effect and toxicity of theophylline
Fosphenytoin Decreased effect of both products
Grepafloxacin Grepafloxacin may increase the effect of dyphylline.
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 Increases the effect and toxicity of theophylline
Lithium Theophylline decreases serum levels of lithium
Mexiletine Mexiletine increases the effect and toxicity of theophylline
Nadolol Antagonism of action and increased effect of theophylline
Norfloxacin Norfloxacin may increase the effect of dyphylline.
Peginterferon alfa-2a Interferon increases the effect and toxicity of theophylline
Peginterferon alfa-2b Interferon increases the effect and toxicity of theophylline
Pentoxifylline Pentoxifylline increases the effect and toxicity of theophylline
Phenobarbital The barbiturate, phenobarbital, decreases the effect of dyphylline.
Phenytoin Decreased effect of both products
Pindolol Antagonism of action and increased effect of theophylline
Primidone The barbiturate, primidone, decreases the effect of dyphylline.
Propafenone Propafenone increases the effect of theophylline
Propranolol Antagonism of action and increased effect of theophylline
Rifampicin Rifampin decreases the effect of theophylline
Temazepam Dyphylline may decrease the efficacy of Temazepam. Monitor for changes in the therapeutic effect of Temazepam if Dyphylline is initiated, discontinued or dose changed.
Terbinafine Terbinafine 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

Liều Lượng & Cách Dùng : Tablet - Oral

Dữ Kiện Thương Mại

Giá thị trường

Biệt dược thương mại : Lufyllin 200 mg tablet

Giá bán buôn : USD >3.15

Đơn vị tính : tablet
Biệt dược thương mại : Lufyllin-400 tablet

Giá bán buôn : USD >4.62

Đơn vị tính : tablet
Biệt dược thương mại : Afinitor 5 mg tablet

Giá bán buôn : USD >234.75

Đơn vị tính : tablet
Biệt dược thương mại : Afinitor 10 mg tablet

Giá bán buôn : USD >247.58

Đơn vị tính : tablet
Biệt dược thương mại : Dyphylline gg tablet

Giá bán buôn : USD >0.69

Đơn vị tính : tablet
Biệt dược thương mại : Dyphylline gg es tablet

Giá bán buôn : USD >0.78

Đơn vị tính : tablet

Nhà Sản Xuất

Công ty : Nippon Shinyaku

Sản phẩm biệt dược : Corphyllin
Công ty : Savage

Sản phẩm biệt dược : Dilor
Công ty : Mallinckrodt

Sản phẩm biệt dược : Lufyllin

Đóng gói

Công ty : Breckenridge Pharmaceuticals

Website : http://www.bpirx.com
Công ty : Great Southern Laboratories

Website : http://greatsouthernlabs.com
Công ty : Lunsco Inc.
Công ty : Meda AB

Website : http://www.meda.se
Công ty : Novartis AG

Website : http://www.novartis.com
Công ty : Savage Labs

Website : http://www.savagelabs.com

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB00651

PubChem Compound

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3182

PubChem Substance

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504443

KEGG Compound

http://www.genome.jp/dbget-bin/www_bget?cpd:C07819

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D00691

ChemSpider

http://www.chemspider.com/Chemical-Structure.3070.html

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0037-0521-92

PharmGKB

http://www.pharmgkb.org/drug/PA164748027

RxList

http://www.rxlist.com/cgi/generic2/dyphylline.htm

Drugs.com

http://www.drugs.com/cdi/dyphylline.html

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