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1) ÀÌ ¾à°ú º¥Á¶µð¾ÆÁ¦ÇÉ°è ¾à¹°, ´Ù¸¥ ¸¶¾à¼º ÁøÅëÁ¦, Àü½Å¸¶ÃëÁ¦, Æä³ëƼ¾ÆÁø°è ¾à¹°, ½Å°æ¾ÈÁ¤Á¦, ¼ö¸éÁ¦, »ïȯ°è Ç׿ì¿ïÁ¦, ½Å°æ±ÙÀ°Â÷´ÜÁ¦, ¶Ç´Â ¾ËÄÚ¿ÃÀ» Æ÷ÇÔÇÑ ´Ù¸¥ ÁßÃ߽Űæ¾ïÁ¦Á¦¸¦ º´¿ëÅõ¿©Çϸé Ãß°¡ÀûÀÎ ÁßÃ߽Űæ¾ïÁ¦ÀÛ¿ëÀÌ À¯¹ßµÇ°í, È£Èí¾ïÁ¦, ÀúÇ÷¾Ð, ±íÀº ÁøÁ¤, ¶Ç´Â È¥¼ö, »ç¸Á°ú °°Àº ÁßÃ߽Űæ¾ïÁ¦ÀÛ¿ëÀÌ Áõ°¡µÉ ¼ö ÀÖ´Ù. µû¶ó¼ ÀÌ·¯ÇÑ ¾à¹°°ú º´¿ëÅõ¿©ÇÏ´Â °æ¿ì¿¡´Â 2°¡Áö ¾à¹° Áß Çϳª, ¶Ç´Â µÑ ´Ù ¿ë·®À» °¨·®ÇØ¾ß ÇÑ´Ù.
ÀÌ ¾à°ú ÁßÃ߽Űæ¾ïÁ¦Á¦ÀÇ º´¿ëÀÌ ÇÊ¿äÇÑ °æ¿ì¿¡´Â ÃÖÀúÀ¯È¿¿ë·®À¸·Î ÃִܱⰣµ¿¾È ó¹æÇÏ¿©¾ß Çϰí È£Èí¾ïÁ¦¿Í ÁøÁ¤ÀÇ Â¡ÈÄ¿Í Áõ»ó¿¡ ´ëÇÏ¿© ¸é¹ÐÇÏ°Ô ÃßÀû°üÂûÇÏ¿©¾ß ÇÑ´Ù.
Æ®¶ó¸¶µ¹Àº MAO ÀúÇØÁ¦¿Í º´¿ëÅõ¿©Çؼ´Â ¾ÈµÈ´Ù. ¸¶¾à ÆäƼµò(pethidine)À» Åõ¿©Çϱâ Àü 14ÀÏ À̳»¿¡ MAOÀúÇØÁ¦¸¦ Åõ¿©ÇÑ È¯ÀÚ¿¡°Ô¼ ÁßÃ߽Űæ°è, È£Èí±â, ½ÉÇ÷°ü±â´É¿¡ ´ëÇØ »ý¸íÀ» À§ÇùÇÏ´Â ¾à¹°»óÈ£ÀÛ¿ëÀÌ °üÂûµÇ¾ú´Ù. Æ®¶ó¸¶µ¹ÀÇ Ä¡·á±â°£µ¿¾È MAO ÀúÇØÁ¦¿ÍÀÇ µ¿ÀÏÇÑ ¾à¹°»óÈ£ÀÛ¿ëÀÇ °¡´É¼ºÀ» ¹èÁ¦ÇÒ ¼ö ¾ø´Ù.
2) Ä«¸£¹Ù¸¶Á¦ÇÉ(È¿¼Ò À¯µµÁ¦)°úÀÇ µ¿½Ã ¶Ç´Â Àü Åõ¿©´Â Æ®¶ó¸¶µ¹ÀÇ ÁøÅëÈ¿°ú¸¦ °¨¼Ò½Ã۰í ÀÛ¿ë½Ã°£À» ÁÙÀÏ ¼ö ÀÖ´Ù.
3) Äí¸¶¸°°è Ç×ÀÀ°íÁ¦´Â ±¹Á¦Á¤»óȺñÀ²(INR)À» Áõ°¡½ÃŰ¹Ç·Î Äí¸¶¸°°è Ç×ÀÀ°íÁ¦¸¦ Åõ¿© ÁßÀΠȯÀÚ¿¡°Ô Æ®¶ó¸¶µ¹ÀÇ Åõ¿©¸¦ ½ÃÀÛÇÒ ¶§¿¡´Â ÁÖÀǰ¡ ÇÊ¿äÇÏ´Ù.
4) Äû´Ïµò°ú º´¿ë½Ã »óÈ£ ÀÌ»ó¹ÝÀÀÀÌ Áõ°¡µÉ ¼ö ÀÖÀ¸¹Ç·Î ½ÅÁßÈ÷ Åõ¿©ÇÑ´Ù.
5) µð°î½Å°ú º´¿ë½Ã µð°î½Å Áßµ¶ÀÌ ³ªÅ¸³µ´Ù´Â º¸°í°¡ ÀÖÀ¸¹Ç·Î ½ÅÁßÈ÷ Åõ¿©ÇÑ´Ù.
6) ¿Í¸£ÆÄ¸°°ú º´¿ëÅõ¿©½Ã ÇÁ·ÎÆ®·Òºó ½Ã°£ÀÇ ¿¬Àå µî ¿Í¸£ÆÄ¸°ÀÇ È¿°ú¿¡ ¿µÇâÀ» ³ªÅ¸³Â´Ù´Â º¸°í°¡ ÀÖ´Ù.
7) ¾à¹°µ¿·ÂÇнÃÇè °á°ú ½Ã¸ÞƼµò(È¿¼Ò ¾ïÁ¦Á¦)°úÀÇ º´¿ë ¶Ç´Â ÀüÅõ¿©·Î ÀÎÇÑ ÀÓ»óÀû »óÈ£ÀÛ¿ëÀÌ ¹ß»ýÇÒ °¡´É¼ºÀº °ÅÀÇ ¾ø´Ù.
8) Æ®¶ó¸¶µ¹°ú °°Àº ¼ø¼ö È¿´É¾àÀÇ ÁøÅëÈ¿°ú´Â ÀÌ·ÐÀûÀ¸·Î È¥ÇÕ È¿´É/±æÇ×Á¦(¿¹, ºÎÇÁ·¹³ë¸£ÇÉ, ³¯ºÎÇÉ, ÆæÅ¸Á¶½Å)°ú º´¿ëÅõ¿© ÇÒ °æ¿ì °¨¼ÒÇÒ ¼ö ÀÖÀ¸¹Ç·Î ±ÇÀåµÇÁö ¾Ê´Â´Ù.
9) Æ®¶ó¸¶µ¹Àº °æ·ÃÀ» À¯¹ßÇÒ ¼ö ÀÖÀ¸¸ç, ¼±ÅÃÀûÀÎ ¼¼·ÎÅä´Ñ ÀçÈí¼ö ¾ïÁ¦Á¦(SSRI), »ïȯ°è Ç׿ì¿ïÁ¦(TCA), Ç×Á¤½Åº´¾à¹°, ¹ßÀÛ¿ªÄ¡¸¦ ³·Ãß´Â ¾à¹°(ºÎÇÁ·ÎÇÇ¿Â, ¹Ì¸£Å¸ÀÚÇÉ, Åׯ®¶óÇÏÀ̵å·Îijªºñ³î µî)ÀÇ °æ·Ã À¯¹ß °¡´É¼ºÀ» ³ôÀδÙ.
10) ¼±ÅÃÀû ¼¼·ÎÅä´Ñ ÀçÈí¼ö ¾ïÁ¦Á¦(SSRI), ¼¼·ÎÅä´Ñ-³ë¸£¿¡Çdz×ÇÁ¸° ÀçÈí¼ö ¾ïÁ¦Á¦(SNRI), MAO¾ïÁ¦Á¦, »ïȯ°è Ç׿ì¿ïÁ¦(TCA), ¹Ì¸£Å¸ÀÚÇÉ, °ñ°Ý±ÙÀÌ¿ÏÁ¦(½ÃŬ·Îº¥ÀÚÇÁ¸°, ¸ÞŹ»ì·Ð)°ú °°Àº ¼¼·ÎÅä´Ñ Ç×Áø ¾à¹°°ú Æ®¶ó¸¶µ¹ÀÇ º´¿ë Åõ¿© ½Ã ¼¼·ÎÅä´Ñ ÁõÈıºÀÌ º¸°íµÇ¾ú´Ù. ¼¼·ÎÅä´Ñ ÁõÈıºÀÇ Áõ»óÀÇ ¿¹´Â ´ÙÀ½°ú °°´Ù ; ÀÚ¹ßÀû °£´ë¼º °æ·Ã, ºÒ¾ÈÀ̳ª ¹ßÇÑÀ» µ¿¹ÝÇÑ À¯µµÀû ¶Ç´Â ¾È±¸ÀÇ °£´ë¼º °æ·Ã, ¶³¸²°ú ¹Ý»çÇ×Áø, ±äÀå Ç×Áø ¹× ¹ß¿À» ¼ö¹ÝÇÏ´Â À¯µµÀû ¶Ç´Â ¾È±¸ÀÇ °£´ë¼º °æ·Ã.
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11) ¸®³×Á¹¸®µå : ºñ¼±Åüº MAO ÀúÇØÁ¦¿Í º´¿ëÅõ¿©½Ã ¼¼·ÎÅä´Ñ ÁõÈıºÀÇ ¹ß»ý À§ÇèÀÌ Áõ°¡ÇÒ ¼ö ÀÖ´Ù. (¼³»ç, ºó¸Æ, ¹ßÇÑ, ÁøÀü, Âø¶õ ¹× È¥¼ö)
12) ÄÉÅäÄÚ³ªÁ¹°ú ¿¡¸®½º·Î¸¶À̽Űú °°Àº »çÀÌÅäÅ©·ÒP3A4¸¦ ÀúÇØÇÏ´Â °ÍÀ¸·Î ¾Ë·ÁÁø ¾à¹°Àº Æ®¶ó¸¶µ¹ ´ë»ç(N-Å»¸ÞÄ¥È)¿Í Ȱ¼º O-Å»¸ÞÄ¥ÈµÈ ´ë»çüÀÇ ´ë»ç¸¦ ÀúÇØÇÒ ¼ö ÀÖ´Ù. ÀÌ·¯ÇÑ »óÈ£ÀÛ¿ëÀÇ ÀÓ»óÀû Á߿伺Àº ¿¬±¸µÇÁö ¾Ê¾Ò´Ù.
13) Á¦ÇÑµÈ ¼öÀÇ ¿¬±¸¿¡ ÀÇÇϸé 5-HT3 ±æÇ×Á¦ÀÎ Ç×±¸ÅäÁ¦ ¿Â´Ü¼¼Æ®·ÐÀ» ¼ö¼ú ÀüÈÄ¿¡ Åõ¿©ÇÑ È¯Àڵ鿡 ´ëÇÏ¿© ¼ö¼ú ÈÄ ÅëÁõÀ¸·Î ÀÎÇÑ Æ®¶ó¸¶µ¹ Åõ¿©°¡ Áõ°¡Çß´Ù.
14) 50mg/ml, 100mg/2ml ÁÖ»çÁ¦´Â µðŬ·ÎÆä³«, Àεµ¸ÞŸ½Å, Æä´ÒºÎŸÁ¸, µð¾ÆÁ¦ÆÊ, Ç÷ç´ÏÆ®¶óÁ¦ÆÊ, ¹Ì´ÙÁ¹¶÷, ´ÏÆ®·Î±Û¸®¼¼¸° ÁÖ»çÁ¦¿Í ¹èÇÕÀ» ±Ý±âÇÑ´Ù. (ÁÖ»çÁ¦¿¡ ÇÑÇÔ) |
| Related FDA Approved Drug |
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8806481001800 |
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Tramadol / N02AX02
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Æû¸ñ±âÁØÄÚµå: 198801776 /´ëÇ¥ÄÚµå: 8806481001800/Ç¥ÁØÄÚµå: 8806481001848
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Æû¸ñ±âÁØÄÚµå: 198801776 /´ëÇ¥ÄÚµå: 8806481001800/Ç¥ÁØÄÚµå: 8806481001855
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| Mechanism of Action |
Tramadol¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Tramadol and its O-desmethyl metabolite (M1) are selective, weak OP3-receptor agonists. Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. The analgesic properties of Tramadol can be attributed to norepinephrine and serotonin reuptake blockade in the CNS, which inhibits pain transmission in the spinal cord. The (+) enantiomer has higher affinity for the OP3 receptor and preferentially inhibits serotonin uptake and enhances serotonin release. The (-) enantiomer preferentially inhibits norepinephrine reuptake by stimulating alpha(2)-adrenergic receptors.
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| Pharmacology |
Tramadol¿¡ ´ëÇÑ Pharmacology Á¤º¸ Tramadol, a centrally-acting analgesic, exists as a racemic mixture of the trans isomer, with important differences in binding, activity, and metabolism associated with the two enantiomers. Although Tramadol is a synthetic analog of codeine, it has a significantly lower affinity for opioid receptors than codeine. Tramadol is used to treat postoperative, dental, cancer, and acute musculosketetal pain and as an adjuvant to NSAID therapy in patients with osteoarthritis.
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| Metabolism |
Tramadol¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2D6 (CYP2D6)
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| Protein Binding |
Tramadol¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 20%
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| Half-life |
Tramadol¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 23 +/- 10 minutes
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| Absorption |
Tramadol¿¡ ´ëÇÑ Absorption Á¤º¸ Racemic tramadol is rapidly and almost completely absorbed after oral administration. The mean absolute bioavailability of a 100 mg oral dose is approximately 75%.The mean peak plasma concentration of racemic tramadol and M1 occurs at two and three hours, respectively, after administration in healthy adults.
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| Pharmacokinetics |
Tramadol HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÁøÅëÈ¿°ú ¹ßÇö½Ã°£ : 1½Ã°£ À̳»
- ÃÖ´ëÈ¿°ú ¹ßÇö½Ã°£ : 2-3 ½Ã°£
- Èí¼ö : °æ±¸ : ½Å¼ÓÇÏ°í °ÅÀÇ ¿ÏÀüÇÏ°Ô Èí¼öµÊ
- ºÐÆ÷ : ºÐÆ÷¿ëÀû : 2.6-2.9 L/kg
- ´ë»ç : °£¿¡¼ ¸¹Àº ¾çÀÌ ´ë»çµÇ¸ç, Ȱ¼ºÇü ´ë»çü (M1)´Â CYP 2D6¿¡ ÀÇÇØ »ý¼ºµÊ
- ¹Ý°¨±â : 6-7 ½Ã°£
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : ¾à 2½Ã°£
- ¼Ò½Ç : ´ë»çü(60%)¿Í ¹Ìº¯Èü(30%)·Î ½Å¹è¼³µÊ
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| Biotransformation |
Tramadol¿¡ ´ëÇÑ Biotransformation Á¤º¸ The major metabolic pathways appear to be N- and O- demethylation and glucuronidation or sulfation in the liver. One metabolite (O-desmethyltramadol, denoted M1) is pharmacologically active in animal models.
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| Toxicity |
Tramadol¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=350mg/kg (orally in mice)
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| Drug Interactions |
Tramadol¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Tramadol¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 2D6
Beta Blockers:
S-metoprolol
propafenone
timolol
Antidepressants:
amitriptyline
clomipramine
desipramine
imipramine
paroxetine
Antipsychotics:
haloperidol
risperidone
thioridazine
aripiprazole
codeine
dextromethorphan
duloxetine
flecainide
mexiletine
ondansetron
tamoxifen
**tramadol**
venlafaxine
INHIBITORS
CYP 2D6
amiodarone
buproprion
chlorpheniramine
cimetidine
clomipramine
duloxetine
fluoxetine
haloperidol
methadone
mibefradil
paroxetine
quinidine
ritonavir
INDUCERS
CYP 2D6
N/A
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| Drug Target |
[Drug Target]
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| Description |
Tramadol¿¡ ´ëÇÑ Description Á¤º¸ A narcotic analgesic proposed for severe pain. It may be habituating. [PubChem]
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| Drug Category |
Tramadol¿¡ ´ëÇÑ Drug_Category Á¤º¸ AnalgesicsAnalgesics, OpioidNarcotics
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| Smiles String Canonical |
Tramadol¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=CC=CC(=C1)C1(O)CCCCC1CN(C)C
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| Smiles String Isomeric |
Tramadol¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=CC=CC(=C1)[C@@]1(O)CCCC[C@@H]1CN(C)C
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| InChI Identifier |
Tramadol¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C16H25NO2/c1-17(2)12-14-7-4-5-10-16(14,18)13-8-6-9-15(11-13)19-3/h6,8-9,11,14,18H,4-5,7,10,12H2,1-3H3/t14-,16+/m1/s1
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| Chemical IUPAC Name |
Tramadol¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (1R,2R)-2-(dimethylaminomethyl)-1-(3-methoxyphenyl)cyclohexan-1-ol
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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