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药品详细

Carbidopa(卡比多巴)

化学结构式图
中文名
卡比多巴
英文名
Carbidopa
分子式
C10H16N2O5
化学名
(2S)-3-(3,4-dihydroxyphenyl)-2-hydrazinyl-2-methylpropanoic acid hydrate
分子量
Average: 244.2444
Monoisotopic: 244.105921632
CAS号
28860-95-9
ATC分类
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

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]

生产厂家
  • Aton pharma inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Vickers S, Stuart EK, Bianchine JR, Hucker HB, Jaffe ME, Rhodes RE, Vandenheuvel WJ: Metabolism of carbidopa (1-(-)-alpha-hydrazino-3,4-dihydroxy-alpha-methylhydrocinnamic acid monohydrate), an aromatic amino acid decarboxylase inhibitor, in the rat, rhesus monkey, and man. Drug Metab Dispos. 1974 Jan-Feb;2(1):9-22. Pubmed
  2. Vickers S, Stuart EK, Hucker HB: Further studies on the metabolism of carbidopa, (minus)-L-alpha-hydrazino-3,4-dihydroxy-alpha-methylbenzenepropanoic acid monohydrate, in the human, Rhesus monkey, dog, and rat. J Med Chem. 1975 Feb;18(2):134-8. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes Not Available
Substructures Not Available
适应症
药理
Indication For treatment of the symptoms of idiopathic Parkinson's disease (paralysis agitans), post-encephalitic parkinsonism
Pharmacodynamics Carbidopa, a noncompetitive decarboxylase inhibitor, is used in combination with levodopa for the treatment of Parkinson's disease.
Mechanism of action 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.
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.
Volume of distribution Not Available
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]

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Carbidopa
    		3,4-Dihydroxyphenylacetone Details
    Carbidopa
      		3-(3-hydroxyphenyl)-2-methyllactic acid Details
      Carbidopa
        		3-(3-hydroxyphenyl)-2-methylpropionic acid Details
        Carbidopa
          		3-(3,4-dihydroxyphenyl)-2-methylpropionic acid Details
          Carbidopa
            		3-(4-hydroxy-3-methoxyphenyl)-2-methyllactic acid Details
            Carbidopa
              		3-(4-hydroxy-3-methoxyphenyl)-2-methylpropionic acid Details
              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
              Clearance Not Available
              Toxicity 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.
              Affected organisms
              • Humans and other mammals
              Pathways Not Available
              理化性质
              Properties
              State solid
              Experimental Properties
              Property Value Source
              melting point 208 °C PhysProp
              water solubility 3.8 mg/L Not Available
              logP -1.9 Not Available
              Predicted Properties
              Property Value Source
              logP -1.2 ChemAxon
              pKa (strongest acidic) 3.59 ChemAxon
              pKa (strongest basic) 5.65 ChemAxon
              physiological charge -1 ChemAxon
              hydrogen acceptor count 6 ChemAxon
              hydrogen donor count 5 ChemAxon
              polar surface area 115.81 ChemAxon
              rotatable bond count 4 ChemAxon
              refractivity 68.77 ChemAxon
              polarizability 21.81 ChemAxon
              药物相互作用
              食物相互作用
              Not Available

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