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Orphenadrine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Orphenadrine binds to both histamine H1 receptors and NMDA receptors. It restores the motor disturbances induced by neuroleptics, in particular the hyperkinesia. The dopamine deficiency in the striatum increases the stimulating effects of the cholinergic system. This stimulation is counteracted by the anticholinergic effect of orphenadrine. It may have a relaxing effect on skeletal muscle spasms and it has a mood elevating effect.
|
| Pharmacology |
Orphenadrine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Orphenadrine is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute painful musculoskeletal conditions. Orphenadrine is an anticholinergic with a predominantly central effect and only a weak peripheral effect. In addition, it has mild antihistaminic and local anaesthetic properties. Parkinson's syndrome is the consequence of a disturbed balance between cholinergic and dopaminergic neurotransmission in the basal ganglia caused by a decrease in dopamine. Orphenadrine restores the physiological equilibrium and has a favourable effect on the rigidity and tremor of Parkinson's disease and Parkinsonian syndromes. The effect is somewhat less on bradykinesia.
|
| Metabolism |
Orphenadrine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2B6 (CYP2B6)Cytochrome P450 2E1 (CYP2E1)
|
| Protein Binding |
Orphenadrine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 95%
|
| Half-life |
Orphenadrine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 13-20 hours
|
| Absorption |
Orphenadrine¿¡ ´ëÇÑ Absorption Á¤º¸ Orphenadrine is almost completely absorbed in the gastrointestinal tract.
|
| Pharmacokinetics |
Orphenadrine CitrateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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|
| Biotransformation |
Orphenadrine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Biotransformation occurs mainly in the liver. Pharmacologically active metabolites are N-demethyl orphenadrine and N,N-didemethyl orphenadrine.
|
| Toxicity |
Orphenadrine¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral, mouse LD50 = 100 mg/kg; oral, rat LD50 = 255 mg/kg
|
| Drug Interactions |
Orphenadrine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Docetaxel The agent increases the serum levels and toxicity of docetaxelDonepezil Possible antagonism of actionGalantamine Possible antagonism of actionRivastigmine Possible antagonism of action
|
CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
|
| Food Interaction |
Orphenadrine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals. Avoid alcohol.
|
| Drug Target |
[Drug Target]
|
| Description |
Orphenadrine¿¡ ´ëÇÑ Description Á¤º¸ A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm. [PubChem]
|
| Dosage Form |
÷°¡Á¦1 º¥Áú¾ËÄÚ¿Ã (ÁÖ»çÁ¦¿¡ ÇÑÇÔ.) ¡Û °æ°í
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|
| Drug Category |
Orphenadrine¿¡ ´ëÇÑ Drug_Category Á¤º¸ AntidyskineticsAntiparkinson AgentsMuscarinic AntagonistsMuscle Relaxants, CentralParasympatholyticsSkeletal Muscle Relaxants
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| Smiles String Canonical |
Orphenadrine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN(C)CCOC(C1=CC=CC=C1)C1=CC=CC=C1C
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| Smiles String Isomeric |
Orphenadrine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN(C)CCO[C@@H](C1=CC=CC=C1)C1=CC=CC=C1C
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| InChI Identifier |
Orphenadrine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C18H23NO/c1-15-9-7-8-12-17(15)18(20-14-13-19(2)3)16-10-5-4-6-11-16/h4-12,18H,13-14H2,1-3H3
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| Chemical IUPAC Name |
Orphenadrine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ N,N-dimethyl-2-[(2-methylphenyl)-phenylmethoxy]ethanamine
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Á¤º¸ÀÇ Á¤È®¼ºÀ» À§ÇØ ³ë·ÂÇϰí ÀÖÀ¸³ª ÆíÁý»óÀÇ ¿À·ù, Çã°¡»çÇ× º¯°æ, Ãß°¡ÀûÀÎ Çмú¿¬±¸ ¶Ç´Â Àӻ󿬱¸ ¹ßÇ¥ µîÀ¸·Î ÀÎÇØ ¹ß»ýÇÏ´Â ¹®Á¦¿¡ ´ëÇØ µå·°ÀÎÆ÷´Â
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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