Tìm theo
Methyldopa
Các tên gọi khác (9 ) :
  • (S)-(-)-alpha-Methyldopa
  • 3-Hydroxy-alpha-methyl-L-tyrosine
  • Alpha medopa
  • alpha-Methyl dopa
  • Alphamethyldopa
  • AMD
  • L-alpha-Methyldopa
  • L-Methyl Dopa
  • α-methyl-L-dopa
Thuốc tim mạch
Thuốc Gốc
Small Molecule
CAS: 555-30-6
ATC: C02AB01, C02AB02
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C10H13NO4
PTK: 211.2145
An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H13NO4
Phân tử khối
211.2145
Monoisotopic mass
211.084457909
InChI
InChI=1/C10H13NO4/c1-10(11,9(14)15)5-6-2-3-7(12)8(13)4-6/h2-4,12-13H,5,11H2,1H3,(H,14,15)/t10-/s2
InChI Key
InChIKey=CJCSPKMFHVPWAR-UEQNJFAPNA-N
IUPAC Name
(2S)-2-amino-3-(3,4-dihydroxyphenyl)-2-methylpropanoic acid
Traditional IUPAC Name
methyldopa
SMILES
C[C@](N)(CC1=CC=C(O)C(O)=C1)C(O)=O
Độ tan chảy
300 dec °C
Độ hòa tan
1E+004 mg/L (at 25 °C)
logP
-1.7
logS
-2
pKa (strongest acidic)
1.73
pKa (Strongest Basic)
9.85
PSA
103.78 Å2
Refractivity
53.79 m3·mol-1
Polarizability
20.73 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
5
H Bond Donor Count
4
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Methyldopa is an aromatic-amino-acid decarboxylase inhibitor in animals and in man. Only methyldopa, the L-isomer of alpha-methyldopa, has the ability to inhibit dopa decarboxylase and to deplete animal tissues of norepinephrine. In man the antihypertensive activity appears to be due solely to the L-isomer. About twice the dose of the racemate (DL-alpha-methyldopa) is required for equal antihypertensive effect. Methyldopa has no direct effect on cardiac function and usually does not reduce glomerular filtration rate, renal blood flow, or filtration fraction. Cardiac output usually is maintained without cardiac acceleration. In some patients the heart rate is slowed. Normal or elevated plasma renin activity may decrease in the course of methyldopa therapy. Methyldopa reduces both supine and standing blood pressure. Methyldopa usually produces highly effective lowering of the supine pressure with infrequent symptomatic postural hypotension. Exercise hypotension and diurnal blood pressure variations rarely occur.
Cơ Chế Tác Dụng : An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent. [PubChem] Although the mechanism of action has yet to be conclusively demonstrated, the resultant hypotensive effect is most likely due to the drug's action on the CNS. Methyldopa is converted into the metabolite, alpha-methylnorepinephrine, in the CNS, where it stimulates the central inhibitory alpha-adrenergic receptors, leading to a reduction in sympathetic tone, total peripheral resistance, and blood pressure. Reduction in plasma renin activity, as well as the inhibition of both central and peripheral norepinephrine and serotonine production may also contribute to the drug's antihypertensive effect, although this is not a major mechanism of action. This is done through the inhibition of the decarboxylation of dihydroxyphenylalanine (dopa)—the precursor of norepinephrine—and of 5-hydroxytryptophan (5-HTP)—the precursor of serotonin—in the CNS and in most peripheral tissues.
Dược Động Học :
▧ Absorption :
Absorption from the gastrointestinal tract is variable but averages approximately 50%.
▧ Protein binding :
Low (less than 20%).
▧ Metabolism :
Hepatic, extensively metabolized. The known urinary metabolites are: a-methyldopa mono-0-sulfate; 3-0-methyl-a-methyldopa; 3,4-dihydroxyphenylacetone; a-methyldopamine; 3-0-methyl-a-methyldopamine and their conjugates.
▧ Route of Elimination :
Methyldopa is extensively metabolized. The known urinary metabolites are: α-methyldopa mono-O-sulfate; 3-0-methyl-α-methyldopa; 3,4-dihydroxyphenylacetone; α-methyldopamine; 3-0-methyl-α-methyldopamine and their conjugates. Approximately 70 percent of the drug which is absorbed is excreted in the urine as methyldopa and its mono-O-sulfate conjugate. Methyldopa crosses the placental barrier, appears in cord blood, and appears in breast milk.
▧ Half Life :
The plasma half-life of methyldopa is 105 minutes.
▧ Clearance :
* Renal cl=130 mL/min [healthy]
Độc Tính : The oral LD50 of methyldopa is greater than 1.5 g/kg in both the mouse and the rat. Symptoms of overdose include bloating, constipation, diarrhea, dizziness, extreme drowsiness, gas, light-headedness, nausea, severely low blood pressure, slow heartbeat, vomiting, and weakness.
Chỉ Định : For use in the treatment of hypertension.
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 : Aldomet
  • Công ty :
    Sản phẩm biệt dược : Aldometil
  • Công ty :
    Sản phẩm biệt dược : Aldomin
  • Công ty :
    Sản phẩm biệt dược : Dopamet
  • Công ty :
    Sản phẩm biệt dược : Hypolag
  • Công ty :
    Sản phẩm biệt dược : Medomet
  • Công ty :
    Sản phẩm biệt dược : Medopren
  • Công ty :
    Sản phẩm biệt dược : Novomedopa
  • Công ty :
    Sản phẩm biệt dược : Nu-Medopa
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00968
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07194
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08205
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-0611-01
PharmGKB
http://www.pharmgkb.org/drug/PA450453
Wikipedia
http://en.wikipedia.org/wiki/Methyldopa
RxList
http://www.rxlist.com/cgi/generic2/methyl.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/ald1012.shtml
Drugs.com
http://www.drugs.com/cdi/methyldopa.html
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