Tìm theo
Hyoscyamine
Các tên gọi khác (18 ) :
  • (-)-Atropine
  • (-)-Hyoscyamine
  • (−)-atropine
  • (−)-hyoscyamine
  • (S)-(-)-Hyoscyamine
  • (S)-(−)-hyoscyamine
  • (S)-atropine
  • [3(S)-Endo]-alpha-(hydroxymethyl)benzeneacetic acid 8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester
  • Daturin
  • Daturine
  • Duboisine
  • Hyoscyamin
  • Hyoscyamine
  • Hyoscyaminum
  • L-Hyoscyamine
  • L-Tropine Tropate
  • Tropine-L-tropate
  • Tropine, (-)-tropate
Thuốc chống loạn nhịp
Thuốc Gốc
Small Molecule
CAS: 101-31-5
ATC: A03BA03
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C17H23NO3
PTK: 289.3694
Hyoscyamine is a chemical compound, a tropane alkaloid it is the levo-isomer to atropine. It is a secondary metabolite of some plants, particularly henbane (Hyoscamus niger.) Hyoscyamine is used to provide symptomatic relief to various gastrointestinal disorders including spasms, peptic ulcers, irritable bowel syndrome, pancreatitis, colic and cystitis. It has also been used to relieve some heart problems, control some of the symptoms of Parkinson's disease, as well as for control of respiratory secretions in end of life care.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H23NO3
Phân tử khối
289.3694
Monoisotopic mass
289.167793607
InChI
InChI=1S/C17H23NO3/c1-18-13-7-8-14(18)10-15(9-13)21-17(20)16(11-19)12-5-3-2-4-6-12/h2-6,13-16,19H,7-11H2,1H3/t13-,14+,15+,16-/m1/s1
InChI Key
InChIKey=RKUNBYITZUJHSG-FXUDXRNXSA-N
IUPAC Name
(1R,3S,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl (2S)-3-hydroxy-2-phenylpropanoate
Traditional IUPAC Name
hyoscyamine
SMILES
CN1[C@H]2CC[C@@H]1C[C@@H](C2)OC(=O)[C@H](CO)C1=CC=CC=C1
Độ tan chảy
108.5 °C
Độ hòa tan
3560 mg/L (at 20 °C)
logP
1.8
logS
-1.91
pKa (strongest acidic)
15.15
pKa (Strongest Basic)
9.39
PSA
49.77 Å2
Refractivity
80.82 m3·mol-1
Polarizability
31.74 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
11.7
Dược Lực Học : L-Hyoscyamine, the active optical isomer of atropine (dl-hyoscyamine), is a tertiary amine anticholinergic gastrointestinal agent.
Cơ Chế Tác Dụng : Hyoscyamine is a chemical compound, a tropane alkaloid it is the levo-isomer to atropine. It is a secondary metabolite of some plants, particularly henbane (Hyoscamus niger.) Hyoscyamine is used to provide symptomatic relief to various gastrointestinal disorders including spasms, peptic ulcers, irritable bowel syndrome, pancreatitis, colic and cystitis. It has also been used to relieve some heart problems, control some of the symptoms of Parkinson's disease, as well as for control of respiratory secretions in end of life care. Hyoscyamine competes favorably with acetylcholine for binding at muscarinic receptors in the salivary, bronchial, and sweat glands as well as in the eye, heart, and gastrointestinal tract. The actions of hyoscyamine result in a reduction in salivary, bronchial, gastric and sweat gland secretions, mydriasis, cycloplegia, change in heart rate, contraction of the bladder detrusor muscle and of the gastrointestinal smooth muscle, and decreased gastrointestinal motility.
Dược Động Học :
▧ Absorption :
Absorbed totally and completely by sublingual administration as well as oral administration.
▧ Protein binding :
50%
▧ Metabolism :
Hepatic
▧ Half Life :
2-3.5 hours
Độc Tính : Symptoms of overdose include headache, nausea, vomiting, blurred vision, dilated pupils, hot dry skin, dizziness, dryness of the mouth, difficulty in swallowing, and CNS stimulation. LD50=mg/kg(orally in rat)
Chỉ Định : For treatment of bladder spasms, peptic ulcer disease, diverticulitis, colic, irritable bowel syndrome, cystitis, and pancreatitis. Also used to treat certain heart conditions, to control the symptoms of Parkinson's disease and rhinitis.
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, Hyoscyamine, 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 Hyoscyamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Hyoscyamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trospium Trospium and Hyoscyamine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Solution / drops - Oral
Tablet - Oral
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