Tìm theo
Pilocarpine
Các tên gọi khác (3) :
  • (3S-cis)-3-Ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-2(3H)-furanone
  • (3S,4R)-3-Ethyldihydro-4-((1-methyl-1H-imidazol-5-yl)methyl)-2(3H)-furanone
  • Pilocarpine
cholinergic agents
Thuốc Gốc
Small Molecule
CAS: 54-71-7
ATC: N07AX01, S01EB01
ĐG : Actavis Group , http://www.actavis.com
CTHH: C11H16N2O2
PTK: 208.2569
A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
208.2569
Monoisotopic mass
208.121177766
InChI
InChI=1S/C11H16N2O2/c1-3-10-8(6-15-11(10)14)4-9-5-12-7-13(9)2/h5,7-8,10H,3-4,6H2,1-2H3/t8-,10-/m0/s1
InChI Key
InChIKey=QCHFTSOMWOSFHM-WPRPVWTQSA-N
IUPAC Name
(3S,4R)-3-ethyl-4-[(1-methyl-1H-imidazol-5-yl)methyl]oxolan-2-one
Traditional IUPAC Name
pilocarpine
SMILES
CC[[email protected]]1[[email protected]@H](CC2=CN=CN2C)COC1=O
Độ tan chảy
204-205 °C
Độ hòa tan
1E+006 mg/L (at 25 °C)
logP
1.1
logS
-2
pKa (Strongest Basic)
6.61
PSA
44.12 Å2
Refractivity
56.53 m3·mol-1
Polarizability
22.34 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
6.78
Dược Lực Học : Pilocarpine is a choline ester miotic and a positively charged quaternary ammonium compound. Pilocarpine, in appropriate dosage, can increase secretion by the exocrine glands. The sweat, salivary, lacrimal, gastric, pancreatic, and intestinal glands and the mucous cells of the respiratory tract may be stimulated. When applied topically to the eye as a single dose it causes miosis, spasm of accommodation, and may cause a transitory rise in intraocular pressure followed by a more persistent fall. Dose-related smooth muscle stimulation of the intestinal tract may cause increased tone, increased motility, spasm, and tenesmus. Bronchial smooth muscle tone may increase. The tone and motility of urinary tract, gallbladder, and biliary duct smooth muscle may be enhanced. Pilocarpine may have paradoxical effects on the cardiovascular system. The expected effect of a muscarinic agonist is vasodepression, but administration of pilocarpine may produce hypertension after a brief episode of hypotension. Bradycardia and tachycardia have both been reported with use of pilocarpine.
Cơ Chế Tác Dụng : A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma. [PubChem] Pilocarpine is a cholinergic parasympathomimetic agent. It increase secretion by the exocrine glands, and produces contraction of the iris sphincter muscle and ciliary muscle (when given topically to the eyes) by mainly stimulating muscarinic receptors.
Dược Động Học :
▧ Absorption :
There was a decrease in the rate of absorption of pilocarpine from SALAGEN Tablets when taken with a high fat meal by 12 healthy male volunteers
▧ Metabolism :
Possibly occurs at the neuronal synapses and in the plasma
▧ Half Life :
0.76 hours
Chỉ Định : For the treatment of radiation-induced dry mouth (xerostomia) and symptoms of dry mouth in patients with Sjögrens syndrome.
Tương Tác Thuốc :
  • Tacrine The acetylcholinesterase inhibitor, Tacrine, may increase the adverse/toxic effects of Pilocarpine, a cholinergic agonist. Monitor for increased cholinergic effects and toxicity.
Liều Lượng & Cách Dùng : Gel - Ophthalmic
Liquid - Ophthalmic
Liquid - Oral
Solution - Ophthalmic
Solution / drops - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Diocarpine
  • Công ty :
    Sản phẩm biệt dược : Miocarpine
  • Công ty :
    Sản phẩm biệt dược : Pilostat
  • Công ty :
    Sản phẩm biệt dược : Pilovisc
  • Công ty :
    Sản phẩm biệt dược : Salagen
  • Công ty :
    Sản phẩm biệt dược : Timpilo
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