Tìm theo
Aclidinium
Các tên gọi khác (1) :
  • Aclidinium
muscarinic antagonists, antispasmodics
Thuốc Gốc
Small Molecule
CAS: 727649-81-2
ATC: R03BB05
CTHH: C26H30NO4S2
PTK: 484.651
Aclidinium is an anticholinergic for the long-term management of chronic obstructive pulmonary disease (COPD). It has a much higher propensity to bind to muscarinic receptors than nicotinic receptors. FDA approved on July 24, 2012.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C26H30NO4S2
Phân tử khối
484.651
Monoisotopic mass
484.161624833
InChI
InChI=1S/C26H30NO4S2/c28-25(26(29,23-9-4-17-32-23)24-10-5-18-33-24)31-22-19-27(14-11-20(22)12-15-27)13-6-16-30-21-7-2-1-3-8-21/h1-5,7-10,17-18,20,22,29H,6,11-16,19H2/q+1/t20?,22-,27?/m0/s1
InChI Key
InChIKey=ASMXXROZKSBQIH-VITNCHFBSA-N
IUPAC Name
(3R)-3-{[2-hydroxy-2,2-bis(thiophen-2-yl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azabicyclo[2.2.2]octan-1-ium
Traditional IUPAC Name
(3R)-3-{[2-hydroxy-2,2-bis(thiophen-2-yl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azabicyclo[2.2.2]octan-1-ium
SMILES
OC(C(=O)O[C@H]1C[N+]2(CCCOC3=CC=CC=C3)CCC1CC2)(C1=CC=CS1)C1=CC=CS1
Độ hòa tan
Very slightly soluble
logP
0.45
logS
-5.5
pKa (strongest acidic)
10.35
pKa (Strongest Basic)
-4.8
PSA
55.76 Å2
Refractivity
141.33 m3·mol-1
Polarizability
52.09 Å3
Rotatable Bond Count
10
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
MDDR-Like Rule
true
Dược Lực Học : Aclidinium does not prolong the QTc interval or have significant effects on cardiac rhythm.
Cơ Chế Tác Dụng : Aclidinium is an anticholinergic for the long-term management of chronic obstructive pulmonary disease (COPD). It has a much higher propensity to bind to muscarinic receptors than nicotinic receptors. FDA approved on July 24, 2012. Aclidinium is a long-acting, competitive, and reversible anticholinergic drug that is specific for the acetylcholine muscarinic receptors. It binds to all 5 muscarinic receptor subtypes to a similar affinity. Aclidinium's effects on the airways are mediated through the M3 receptor at the smooth muscle to cause bronchodilation. Prevention of acetylcholine-induced bronchoconstriction effects was dose-dependent and lasted longer than 24 hours.
Dược Động Học :
▧ Absorption :
Bioavailability, healthy subjects = 6%; T max, healthy subjects = 10 minutes; Time to steady state, healthy subjects = 2 days;
▧ Volume of Distribution :
Following IV administration, the volume of distribution is 300 L
▧ Metabolism :
The major route of metabolism of aclidinium bromide is hydrolysis, which occurs both chemically and enzymatically by esterases in the plasma. Aclidinium bromide is rapidly and extensively hydrolyzed to its alcohol and dithienylglycolic acid derivatives, neither of which binds to muscarinic receptors and are pharmacologically inactive.
▧ Route of Elimination :
Intravenously administered radiolabelled aclidinium bromide was administered to healthy volunteers and was extensively metabolized with 1% excreted as unchanged aclidinium. Approximately 54% to 65% of the radioactivity was excreted in urine and 20% to 33% of the dose was excreted in feces. The combined results indicated that almost the entire aclidinium bromide dose was eliminated by hydrolysis. After dry powder inhalation, urinary excretion of aclidinium is about 0.09% of the dose.
▧ Half Life :
Plasma half-life = 2.4 minutes (indicating that aclidinium is very rapidly hydrolyzed in plasma into its two inactive metabolites and has a low chance of causing systemic side effects). Effective half-life = 5-8 hours.
▧ Clearance :
Total clearance, IV dose, young healthy subjects = 170 L/h (inter-individual variability of 36%)
Độc Tính : Most common adverse reactions (≥3% incidence and greater than placebo) are headache, nasopharyngitis and cough.
Chỉ Định : Aclidinium bromide inhalation powder is indicated for the long-term, maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema.
Tương Tác Thuốc :
  • Pramlintide May increase the risk of inhibition of GI motility via pharmacodynamic synergism. Consider alternate therapy.
Liều Lượng & Cách Dùng : Powder - Respiratory (inhalation) - 400 mcg/actuation
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Bretaris Genuair
  • Công ty :
    Sản phẩm biệt dược : Eklira Genuair
  • Sản phẩm biệt dược : Tudorza Pressair
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08897
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08837
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0456-0800-60
Wikipedia
http://en.wikipedia.org/wiki/Aclidinium_bromide
RxList
http://www.rxlist.com/tudorza-pressair-drug.htm
Drugs.com
http://www.drugs.com/tudorza.html
... loading
... loading