Tìm theo
Ergoloid mesylate
Các tên gọi khác (17 ) :
  • co-dergocrine mesilate
  • co-dergocrine mesylate
  • co-dergocrine methanesulfonate
  • codergocrine mesilate
  • codergocrine mesylate
  • codergocrine methanesulfonate
  • Dihydroergotoxine Mesilate
  • Dihydroergotoxine Mesylate
  • dihydroergotoxine methanesulfonate
  • Dihydroergotoxine Methanesulfonate
  • dihydroergotoxine methanesulfonates
  • dihydroergotoxine monomethanesulfonate
  • dihydrogenated ergot alkaloids
  • Ergoloid Mesylates
  • ergoloid methanesulfonate
  • ergoloid methanesulfonates
  • hydrogenated ergot alkaloids
nootropic agents, vasodilator agents, adrenergic alpha antagonists
Thuốc Gốc
Small Molecule
CAS: 8067-24-1
ATC: C04AE01
ĐG : Gallipot , http://www.gallipot.com
CTHH: C30H41N5O8S
PTK: 631.74
Ergoloid mesylate is a dihydrogenated ergot (Claviceps purpurea) derivative alkaloid used as a vasodilator agent. Ergoloid Mesylate is the only vasodilator that has shown mild benefits in the treatment of vascular dementia. Ergoloid Mesylate is a mixture of three different ergotamantriones: dihydroergocornine, dihydroergocristine, and dihydroergocryptine. It has been proposed to be a neuroprotective agent. The mechanism of its therapeutic actions is not clear.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C30H41N5O8S
Phân tử khối
631.74
Monoisotopic mass
631.267584003
InChI
InChI=1S/C29H37N5O5.CH4O3S/c1-15(2)28(27(37)34-16(3)26(36)33-10-6-9-23(33)29(34,38)39-28)31-25(35)18-11-20-19-7-5-8-21-24(19)17(13-30-21)12-22(20)32(4)14-18;1-5(2,3)4/h5,7-8,13,15-16,18,20,22-23,30,38H,6,9-12,14H2,1-4H3,(H,31,35);1H3,(H,2,3,4)/t16-,18+,20+,22+,23-,28+,29-;/m0./s1
InChI Key
InChIKey=FQHMMOGHDWAXDI-WUQHHHCFSA-N
IUPAC Name
(2R,4R,7R)-N-[(1S,2S,4R,7S)-2-hydroxy-7-methyl-5,8-dioxo-4-(propan-2-yl)-3-oxa-6,9-diazatricyclo[7.3.0.0^{2,6}]dodecan-4-yl]-6-methyl-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(16),9,12,14-tetraene-4-carboxamide; methanesulfonic acid
Traditional IUPAC Name
(2R,4R,7R)-N-[(1S,2S,4R,7S)-2-hydroxy-4-isopropyl-7-methyl-5,8-dioxo-3-oxa-6,9-diazatricyclo[7.3.0.0^{2,6}]dodecan-4-yl]-6-methyl-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(16),9,12,14-tetraene-4-carboxamide; methanesulfonic acid
SMILES
CS(O)(=O)=O.[H][C@@]12CCCN1C(=O)[C@H](C)N1C(=O)[C@](NC(=O)[C@H]3CN(C)[C@]4([H])CC5=CNC6=CC=CC(=C56)[C@@]4([H])C3)(O[C@@]21O)C(C)C
logP
2.8
pKa (strongest acidic)
9.71
pKa (Strongest Basic)
8.39
PSA
118.21 Å2
Refractivity
143.66 m3·mol-1
Polarizability
57.99 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
6
H Bond Donor Count
3
Physiological Charge
1
Number of Rings
7
Bioavailability
1
Dược Lực Học : Ergoloid Mesylate may increase cerebral metabolism and blood flow. The role of this medication in the therapy of dementia is controversial. A recent controlled study in patients with Alzheimer's disease found that there was no advantage to the use of ergoloid mesylates compared to placebo, suggesting that ergoloid mesylates may lower scores on some cognitive and behavioral rating scales. Further study is needed to determine the risk-benefit profile of ergoloid mesylates in the treatment of dementia.
Cơ Chế Tác Dụng : Ergoloid mesylate is a dihydrogenated ergot (Claviceps purpurea) derivative alkaloid used as a vasodilator agent. Ergoloid Mesylate is the only vasodilator that has shown mild benefits in the treatment of vascular dementia. Ergoloid Mesylate is a mixture of three different ergotamantriones: dihydroergocornine, dihydroergocristine, and dihydroergocryptine. It has been proposed to be a neuroprotective agent. The mechanism of its therapeutic actions is not clear. Ergoloid mesylates act centrally, decreasing vascular tone and slowing the heart rate, and acts peripherally to block alpha-receptors. One other possible mechanism is the effect of ergoloid mesylates on neuronal cell metabolism, resulting in improved oxygen uptake and cerebral metabolism, thereby normalizing depressed neurotransmitter levels.
Dược Động Học :
▧ Absorption :
Rapidly but incompletely (approximately 25%) absorbed from the gastrointestinal tract. Approximately 50% of the absorbed dose is eliminated by first-pass metabolism.
▧ Protein binding :
98-99%
▧ Metabolism :
Hepatic.
▧ Half Life :
3.5 hours
Độc Tính : Symptoms of overdose include dyspnea, hypotension or hypertension, rapid weak pulse, delirium, nausea, vomiting, and bradycardia.
Chỉ Định : For use as an adjunct therapy for patients with dementia.
Tương Tác Thuốc :
  • Desvenlafaxine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Telithromycin Telithromycin may reduce clearance of Ergoloid mesylates. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Ergoloid mesylates if Telithromycin is initiated, discontinued or dose changed.
  • Tipranavir Tipranavir may increase the plasma concentration of Ergoloid mesylates. Concomitant therapy should be avoided.
  • Tramadol Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Tranylcypromine Increased risk of serotonin syndrome. Use caution during concomitant therapy and monitor for symptoms of serotonin syndrome.
  • Trazodone Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Trimipramine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Venlafaxine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of ergoloid mesylates by decreasing their metabolism. Concomitant therapy is contraindicated.
  • Zolmitriptan Concomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, ergoloid mesylate, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Alkergot
  • Công ty :
    Sản phẩm biệt dược : Gerimal
  • Công ty :
    Sản phẩm biệt dược : Hydergine
  • Công ty :
    Sản phẩm biệt dược : Hydergine LC
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01049
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C14055
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02268
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0078-0101-05
PharmGKB
http://www.pharmgkb.org/drug/PA164752439
Wikipedia
http://en.wikipedia.org/wiki/Ergoloid
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