Tìm theo
Carbidopa
Các tên gọi khác (12 ) :
  • (-)-L-alpha-Hydrazino-3,4-dihydroxy-alpha-methylhydrocinnamic acid monohydrate
  • (2S)-3-(3,4-Dihydroxyphenyl)-2-hydrazinyl-2-methylpropanoic acid hydrate
  • (2S)-3-(3,4-Dihydroxyphenyl)-2-hydrazinyl-2-methylpropanoic acid monohydrate
  • (AlphaS)-alpha-hydrazino-3,4-dihydroxy-alpha-methylbenzenepropanoic acid monohydrate
  • (S)-(-)-Carbidopa hydrate
  • (S)-(−)-carbidopa hydrate
  • (S)-carbidopa hydrate
  • carbidopa hydrate
  • Carbidopa monohydrate
  • Carbidopum
  • Carbidopum monohydricum
  • L-alpha-(3,4-Dihydroxybenzyl)-alpha-hydrazinopropionic acid monohydrate
enzyme inhibitors, dopamine agents, antiparkinson agents, antidyskinetics
Thuốc Gốc
Small Molecule
CAS: 28860-95-9
ĐG : Aton Pharma Inc. , http://www.atonrx.com
CTHH: C10H16N2O5
PTK: 244.2444
An inhibitor of DOPA decarboxylase, preventing conversion of levodopa to dopamine. It is used in parkinson disease to reduce peripheral adverse effects of levodopa. It has no antiparkinson actions by itself. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H16N2O5
Phân tử khối
244.2444
Monoisotopic mass
244.105921632
InChI
InChI=1S/C10H14N2O4.H2O/c1-10(12-11,9(15)16)5-6-2-3-7(13)8(14)4-6;/h2-4,12-14H,5,11H2,1H3,(H,15,16);1H2/t10-;/m0./s1
InChI Key
InChIKey=QTAOMKOIBXZKND-PPHPATTJSA-N
IUPAC Name
(2S)-3-(3,4-dihydroxyphenyl)-2-hydrazinyl-2-methylpropanoic acid hydrate
Traditional IUPAC Name
carbidopa hydrate
SMILES
O.C[[email protected]@](CC1=CC(O)=C(O)C=C1)(NN)C(O)=O
Độ tan chảy
208 °C
Độ hòa tan
3.8 mg/L
logP
-1.9
pKa (strongest acidic)
3.59
pKa (Strongest Basic)
5.65
PSA
115.81 Å2
Refractivity
68.77 m3·mol-1
Polarizability
21.81 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
6
H Bond Donor Count
5
Physiological Charge
-1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Carbidopa, a noncompetitive decarboxylase inhibitor, is used in combination with levodopa for the treatment of Parkinson's disease.
Cơ Chế Tác Dụng : An inhibitor of DOPA decarboxylase, preventing conversion of levodopa to dopamine. It is used in parkinson disease to reduce peripheral adverse effects of levodopa. It has no antiparkinson actions by itself. [PubChem] When mixed with levodopa, carbidopa inhibits the peripheral conversion of levodopa to dopamine and the decarboxylation of oxitriptan to serotonin by aromatic L-amino acid decarboxylase. This results in increased amount of levodopa and oxitriptan available for transport to the CNS. Carbidopa also inhibits the metabolism of levodopa in the GI tract, thus, increasing the bioavailability of levodopa.
Dược Động Học :
▧ Absorption :
Rapidly decarboxylated to dopamine in extracerebral tissues so that only a small portion of a given dose is transported unchanged to the central nervous system.
▧ Protein binding :
76%
▧ Metabolism :
The loss of the hydrazine functional group (probably as molecular nitrogen) represents the major metabolic pathway for carbidopa. There are several metabolites of carbidopa metabolism including 3-(3,4-dihydroxyphenyl)-2-methylpropionic acid, 3-(4-hydroxy-3-methoxyphenyl)-2-methylpropionic acid, 3-(3-hydroxyphenyl)-2-methylpropionic acid, 3-(4-hydroxy-3-methoxyphenyl)-2-methyllactic acid, 3-(3-hydroxyphenyl)-2-methyllactic acid, and 3,4-dihydroxyphenylacetone (1,2). [PMID: 4150141]
▧ Route of Elimination :
In clinical pharmacologic studies, simultaneous administration of separate tablets of carbidopa and levodopa produced greater urinary excretion of levodopa in proportion to the excretion of dopamine when compared to the two drugs administered at separate times.
▧ Half Life :
1-2 hours
Độc Tính : Symptoms of a carbidopa toxicity include muscle spasms or weakness, spasms of the eyelid, nausea, vomiting, diarrhea, an irregular heartbeat, confusion, agitation, hallucinations, and unconsciousness.
Chỉ Định : For treatment of the symptoms of idiopathic Parkinson's disease (paralysis agitans), post-encephalitic parkinsonism
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Lodosyn 25 mg tablet
    Giá bán buôn : USD >2.53
    Đơn vị tính : tablet
  • Biệt dược thương mại : Carbidopa powder
    Giá bán buôn : USD >27.54
    Đơn vị tính : g
Nhà Sản Xuất
  • Công ty : Aton
    Sản phẩm biệt dược : Lodosyn
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