Tìm theo
Midodrine
Các tên gọi khác (7 ) :
  • (+-)-2-amino-N-(beta-Hydroxy-2,5-dimethoxyphenethyl)acetamide
  • 1-(2',5'-Dimethoxyphenyl)-2-glycinamidoethanol
  • 2-Amino-N-(2,5-dimethoxy-beta-hydroxyphenethyl)acetamide
  • DL-N1-(beta-Hydroxy-2,5-dimethoxyphenethyl)glycinamid
  • Midodrin
  • Midodrina
  • Midodrinum
Thuốc tim mạch
Thuốc Gốc
Small Molecule
CAS: 133163-28-7
ATC: C01CA17
ĐG : Actavis Group , http://www.actavis.com
CTHH: C12H18N2O4
PTK: 254.2823
An ethanolamine derivative that is an adrenergic alpha agonist. It is used as a vasoconstrictor agent in the treatment of hypotension. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H18N2O4
Phân tử khối
254.2823
Monoisotopic mass
254.126657074
InChI
InChI=1S/C12H18N2O4/c1-17-8-3-4-11(18-2)9(5-8)10(15)7-14-12(16)6-13/h3-5,10,15H,6-7,13H2,1-2H3,(H,14,16)
InChI Key
InChIKey=PTKSEFOSCHHMPD-UHFFFAOYSA-N
IUPAC Name
2-amino-N-[2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]acetamide
Traditional IUPAC Name
midodrine
SMILES
COC1=CC(C(O)CNC(=O)CN)=C(OC)C=C1
Độ tan chảy
200 to 203°C
Độ hòa tan
Soluble
logP
-0.5
logS
-1.8
pKa (strongest acidic)
13.77
pKa (Strongest Basic)
8.14
PSA
93.81 Å2
Refractivity
66.22 m3·mol-1
Polarizability
26.65 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
pKa
7.8
Dược Lực Học : Midodrine is a prodrug, i.e., the therapeutic effect of orally administered midodrine is due to the major metabolite desglymidodrine formed by deglycination of midodrine. Desglymidodrine diffuses poorly across the blood-brain barrier, and is therefore not associated with effects on the central nervous system. Administration of midodrine results in a rise in standing, sitting, and supine systolic and diastolic blood pressure in patients with orthostatic hypotension of various etiologies. Standing systolic blood pressure is elevated by approximately 15 to 30 mmHg at 1 hour after a 10-mg dose of midodrine, with some effect persisting for 2 to 3 hours. Midodrine has no clinically significant effect on standing or supine pulse rates in patients with autonomic failure.
Cơ Chế Tác Dụng : An ethanolamine derivative that is an adrenergic alpha agonist. It is used as a vasoconstrictor agent in the treatment of hypotension. [PubChem] Midodrine forms an active metabolite, desglymidodrine, that is an alpha1-agonist, and exerts its actions via activation of the alpha-adrenergic receptors of the arteriolar and venous vasculature, producing an increase in vascular tone and elevation of blood pressure. Desglymidodrine does not stimulate cardiac beta-adrenergic receptors.
Dược Động Học :
▧ Absorption :
Rapidly absorbed following oral administration. The absolute bioavailability of midodrine (measured as desglymidodrine) is 93% and is not affected by food.
▧ Metabolism :
Thorough metabolic studies have not been conducted, but it appears that deglycination of midodrine to desglymidodrine takes place in many tissues, and both compounds are metabolized in part by the liver.
▧ Half Life :
The plasma levels of the prodrug peak after about half an hour, and decline with a half-life of approximately 25 minutes, while the metabolite reaches peak blood concentrations about 1 to 2 hours after a dose of midodrine and has a half-life of about 3 to 4 hours.
▧ Clearance :
* Renal cl=385 mL/minute
Độc Tính : Symptoms of overdose could include hypertension, piloerection (goosebumps), a sensation of coldness and urinary retention. The single doses that would be associated with symptoms of overdosage or would be potentially life- threatening are unknown. The oral LD50 is approximately 30 to 50 mg/kg in rats, 675 mg/kg in mice, and 125 to 160 mg/kg in dogs. Desglymidodrine is dialyzable.
Chỉ Định : For the treatment of symptomatic orthostatic hypotension (OH).
Tương Tác Thuốc :
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : ProAmatine
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00211
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4195
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507373
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07890
ChemSpider
http://www.chemspider.com/Chemical-Structure.4050.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0245-0211-11
PharmGKB
http://www.pharmgkb.org/drug/PA164749381
Wikipedia
http://en.wikipedia.org/wiki/Midodrine
RxList
http://www.rxlist.com/cgi/generic3/midodrine.htm
Drugs.com
http://www.drugs.com/cdi/midodrine.html
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