Tìm theo
Glycopyrrolate
Các tên gọi khác (6 ) :
  • AHR-504
  • Glycopyrrolate
  • Glycopyrronium bromide
  • Nodapton
  • Robinul
  • Tarodyn
muscarinic antagonists, adjuvants anesthesia, cholinergic antagonists
Thuốc Gốc
Small Molecule
CAS: 596-51-0
ATC: A03AB02
ĐG : American Regent , http://www.americanregent.com
CTHH: C19H28NO3
PTK: 318.4305
Glycopyrrolate is a synthetic anticholinergic agent with a quaternary ammonium structure. A muscarinic competitive antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H28NO3
Phân tử khối
318.4305
Monoisotopic mass
318.206918767
InChI
InChI=1S/C19H28NO3/c1-20(2)13-12-17(14-20)23-18(21)19(22,16-10-6-7-11-16)15-8-4-3-5-9-15/h3-5,8-9,16-17,22H,6-7,10-14H2,1-2H3/q+1
InChI Key
InChIKey=ANGKOCUUWGHLCE-UHFFFAOYSA-N
IUPAC Name
3-[(2-cyclopentyl-2-hydroxy-2-phenylacetyl)oxy]-1,1-dimethylpyrrolidin-1-ium
Traditional IUPAC Name
3-[(2-cyclopentyl-2-hydroxy-2-phenylacetyl)oxy]-1,1-dimethylpyrrolidin-1-ium
SMILES
C[N+]1(C)CCC(C1)OC(=O)C(O)(C1CCCC1)C1=CC=CC=C1
Độ tan chảy
193-194.5
Độ hòa tan
9.44e-04 g/l
logP
-0.99
logS
-5.6
pKa (strongest acidic)
11.53
pKa (Strongest Basic)
-4.3
PSA
46.53 Å2
Refractivity
101.08 m3·mol-1
Polarizability
35.88 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Dược Lực Học : Glycopyrrolate decreases acid secretion in the stomach. Hence it can be used for treating ulcers in the stomach and small intestine, in combination with other medications. In anesthesia, glycopyrrolate injection serves as a preoperative antimuscarinic operation that reduces salivary, tracheobronchial, and pharyngeal secretions, as well as decreases the acidity of gastric secretions blocks cardiac vagal inhibitory reflexes during intubation
Cơ Chế Tác Dụng : Glycopyrrolate is a synthetic anticholinergic agent with a quaternary ammonium structure. A muscarinic competitive antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics. [PubChem] Glycopyrrolate binds competitively to the muscarinic acetylcholine receptor. Like other anticholinergic (antimuscarinic) agents, it inhibits the action of acetylcholine on structures innervated by postganglionic cholinergic nerves and on smooth muscles that respond to acetylcholine but lack cholinergic innervation. These peripheral cholinergic receptors are present in the autonomic effector cells of smooth muscle, cardiac muscle, the sinoatrial node, the atrioventricular node, exocrine glands and, to a limited degree, in the autonomic ganglia. Thus, it diminishes the volume and free acidity of gastric secretions and controls excessive pharyngeal, tracheal, and bronchial secretions.
Dược Động Học :
▧ Absorption :
Rapidly absorbed (1-2 minutes) after intravenous injection
▧ Half Life :
0.6-1.2 hours
Độc Tính : Side effects include dry mouth, difficult urinating, heachaches, diarrhea and constipation. The medication also induces drowsiness or blurred vision. LD50=709 mg/kg (rat, oral).
Chỉ Định : For use as a preoperative antimuscarinic to reduce salivary, tracheobronchial, and pharyngeal secretions, to reduce the volume and free acidity of gastric secretions and to block cardiac vagal inhibitory reflexes during induction of anesthesia and intubation.
Tương Tác Thuốc :
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia
  • Rivastigmine Possible antagonism of action
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Glycopyrrolate, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
  • Trimethobenzamide Trimethobenzamide and Glycopyrrolate, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Glycopyrrolate, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trospium Trospium and Glycopyrrolate, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Liquid - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Gray
    Sản phẩm biệt dược : Acpan
  • Công ty :
    Sản phẩm biệt dược : Cuvposa
  • Công ty :
    Sản phẩm biệt dược : Glycate
  • Công ty :
    Sản phẩm biệt dược : Nodapton
  • Công ty :
    Sản phẩm biệt dược : Robanul
  • Công ty :
    Sản phẩm biệt dược : Robinal
  • Công ty : Goldshield
    Sản phẩm biệt dược : Robinul
  • Công ty : Shionogi
    Sản phẩm biệt dược : Robinul Forte
  • Công ty : Lundbeck
    Sản phẩm biệt dược : Tarodyl
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00986
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3494
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509133
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00540
ChemSpider
http://www.chemspider.com/Chemical-Structure.3374.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0143-1250-01
PharmGKB
http://www.pharmgkb.org/drug/PA164754882
Wikipedia
http://en.wikipedia.org/wiki/Glycopyrrolate
RxList
http://www.rxlist.com/cgi/generic3/glycopyrrolate.htm
Drugs.com
http://www.drugs.com/cdi/glycopyrrolate.html
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