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Carbidopa¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Levodopa¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Ãâó: ±¹¸³µ¶¼º°úÇпø µ¶¼º¹°ÁúÁ¤º¸DB : http://www.nitr.go.kr/nitr/contents/m134200/view.do |
| Mechanism of Action |
Carbidopa¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ 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.
Levodopa¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Striatal dopamine levels in symptomatic Parkinson's disease are decreased by 60 to 80%, striatal dopaminergic neurotransmission may be enhanced by exogenous supplementation of dopamine through administration of dopamine's precursor, levodopa. A small percentage of each levodopa dose crosses the blood-brain barrier and is decarboxylated to dopamine. This newly formed dopamine then is available to stimulate dopaminergic receptors, thus compensating for the depleted supply of endogenous dopamine.
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| Pharmacology |
Carbidopa¿¡ ´ëÇÑ Pharmacology Á¤º¸ Carbidopa, a noncompetitive decarboxylase inhibitor, is used in combination with levodopa for the treatment of Parkinson's disease.
Levodopa¿¡ ´ëÇÑ Pharmacology Á¤º¸ Levodopa (L-dopa) is used to replace dopamine lost in Parkinson's disease because dopamine itself cannot cross the blood-brain barrier where its precursor can. However, L-DOPA is converted to dopamine in the periphery as well as in the CNS, so it is administered with a peripheral DDC (dopamine decarboxylase) inhibitor such as carbidopa, without which 90% is metabolised in the gut wall, and with a COMT inhibitor if possible; this prevents about a 5% loss. The form given therapeutically is therefore a prodrug which avoids decarboxylation in the stomach and periphery, can cross the blood-brain barrier, and once in the brain is converted to the neurotransmitter dopamine by the enzyme aromatic-L-amino-acid decarboxylase.
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| Metabolism |
Carbidopa¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Catechol O-methyltransferase (COMT)Monoamine oxidase type A (MAO-A)Aromatic-L-amino-acid decarboxylase (AADC)Monoamine oxidase type B (MAO-B)
Levodopa¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Monoamine oxidase type A (MAO-A)Monoamine oxidase type B (MAO-B)Aromatic-L-amino-acid decarboxylase (AADC)
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| Protein Binding |
Carbidopa¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 76%
Levodopa¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ High
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| Half-life |
Carbidopa¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 1-2 hours
Levodopa¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 50 to 90 minutes
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| Absorption |
Carbidopa¿¡ ´ëÇÑ Absorption Á¤º¸ 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.
Levodopa¿¡ ´ëÇÑ Absorption Á¤º¸ Levodopa is rapidly absorbed from the proximal small intestine by the large neutral amino acid (LNAA) transport carrier system.
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| Pharmacokinetics |
CarbidopaÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : À§Àå°ü¿¡¼ ½Å¼ÓÇÏÁö¸¸ ºÒ¿ÏÀüÇÏ°Ô Èí¼öµÊ
- ºÐÆ÷ : ³úÇ÷°üÀ庮À» Åë°úÇÏÁö ¸øÇÑ´Ù. µ¿¹° ½ÇÇè¿¡¼ ŹÝÅë°ú, À¯ÁóºÐºñ°¡ °üÂûµÇ¾ú´Ù.
- ¼Ò½Ç : ¹Ìº¯Èü ¹× ´ë»çü·Î ½Å¼ÓÈ÷ ½Å¹è¼³µÊ
LevodopaÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : °æ±¸ : 1-2 ½Ã°£
- ´ë»ç :
- ´ëºÎºÐÀÇ ¾à¹°ÀÌ ¸»ÃÊ decarboxylase¿¡ ÀÇÇØ dopamineÀ¸·Î ÀüȯµÈ´Ù.
- ¼Ò·®ÀÇ levodopa°¡ ³ú·Î µµ´ÞÇÏ¿© Ȱ¼ºÇü dopamineÀ¸·Î decarboxylation µÈ´Ù.
- ¹Ý°¨±â : 1.2-2.3 ½Ã°£
- ¼Ò½Ç : Dopamine, norepinephrine, homovanillic acid·Î¼ ÁÖ·Î ½Å¹è¼³µÊ (80%)
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| Biotransformation |
Carbidopa¿¡ ´ëÇÑ Biotransformation Á¤º¸ Rapidly decarboxylated to dopamine
Levodopa¿¡ ´ëÇÑ Biotransformation Á¤º¸ 95% of an administered oral dose of levodopa is pre-systemically decarboxylated to dopamine by the L-aromatic amino acid decarboxylase (AAAD) enzyme in the stomach, lumen of the intestine, kidney, and liver. Levodopa also may be methoxylated by the hepatic catechol-O-methyltransferase (COMT) enzyme system to 3-O-methyldopa (3-OMD), which cannot be converted to central dopamine.
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| Toxicity |
Carbidopa¿¡ ´ëÇÑ Toxicity Á¤º¸ 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.
Levodopa¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral, mouse: LD50 = 2363 mg/kg; Oral, rabbit: LD50 = 609 mg/kg; Oral, rat: LD50 = 1780 mg/kg.
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| Drug Interactions |
Carbidopa¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
Levodopa¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Carbidopa¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not Available
Levodopa¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not Available
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| Drug Target |
[Drug Target]
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| Description |
Carbidopa¿¡ ´ëÇÑ Description Á¤º¸ 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]
Levodopa¿¡ ´ëÇÑ Description Á¤º¸ The naturally occurring form of dihydroxyphenylalanine and the immediate precursor of dopamine. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to dopamine. It is used for the treatment of parkinsonian disorders and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system. [PubChem]
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| Dosage Form |
Carbidopa¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
Levodopa¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
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| Drug Category |
Carbidopa¿¡ ´ëÇÑ Drug_Category Á¤º¸ AntidyskineticsAntiparkinson AgentsDopamine AgentsEnzyme Inhibitors
Levodopa¿¡ ´ëÇÑ Drug_Category Á¤º¸ AntidyskineticsAntiparkinson AgentsDopamine Agents
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| Smiles String Canonical |
Carbidopa¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(CC1=CC(O)=C(O)C=C1)(NN)C(O)=O
Levodopa¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ NC(CC1=CC(O)=C(O)C=C1)C(O)=O
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| Smiles String Isomeric |
Carbidopa¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ C[C@@](CC1=CC(O)=C(O)C=C1)(NN)C(O)=O
Levodopa¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ N[C@@H](CC1=CC(O)=C(O)C=C1)C(O)=O
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| InChI Identifier |
Carbidopa¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C10H14N2O4/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)/t10-/m0/s1/f/h15H
Levodopa¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C9H11NO4/c10-6(9(13)14)3-5-1-2-7(11)8(12)4-5/h1-2,4,6,11-12H,3,10H2,(H,13,14)/t6-/m0/s1/f/h13H
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| Chemical IUPAC Name |
Carbidopa¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (2S)-3-(3,4-dihydroxyphenyl)-2-hydrazinyl-2-methylpropanoic acid
Levodopa¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoic acid
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| Drug-Induced Toxicity Related Proteins |
LEVODOPA ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Opioid growth factor receptor Drug:levodopa Toxicity:Parkinson's disease (PD). [¹Ù·Î°¡±â] Replated Protein:Parkin Drug:Levodopa Toxicity:dyskinesias. [¹Ù·Î°¡±â] Replated Protein:Catechol O-methyltransferase Drug:levodopa Toxicity:toxicity of levodopa. [¹Ù·Î°¡±â]
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