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9) ÇǺΠ: µÎµå·¯±â, ¼ÒÆ÷Áø, ½ºÆ¼ºì½º-Á¸½¼ÁõÈıºÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù. ÈçÇÏ°Ô ¹ßÇÑ ¶Ç´Â ÈçÇÏÁö ¾Ê°Ô ÇǺιÝÀÀ(¿¹, °£Áö·¯¿ò, ¹ßÁø, µÎµå·¯±â)ÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù.
10) ÀÇÁ¸¼º : ÀÌ ¾àÀº ¸ôÇÉÇü(¥ì-¾ÆÆí) ¾à¹°ÀÇ Á¤½ÅÀû¡¤½ÅüÀû ÀÇÁ¸¼ºÀ» ÀÏÀ¸Å°¸ç ÀÌ ¾àÀÇ ³²¿ë ¹× ÀÇÁ¸¼º »ç·Ê°¡ º¸°íµÇ¾úÀ¸¹Ç·Î ¾ÆÆí ÀÇÁ¸¼º ȯÀÚ¿¡´Â Åõ¿©ÇÏÁö ¾Ê´Â´Ù. ÀÇÁ¸ º´·ÂÀÌ Àְųª ¸¸¼ºÀûÀ¸·Î ´Ù¸¥ ¾ÆÆí·ù¸¦ »ç¿ëÇϴ ȯÀÚ¿¡¼ ½ÅüÀû ÀÇÁ¸¼ºÀÌ Àç¹ßÇÒ ¼ö ÀÖ´Ù. ¾à¹° ³²¿ë °æÇâÀÌ Àִ ȯÀÚ, ¾à¹° ÀÇÁ¸º´·ÂÀÌ Àִ ȯÀÚ, ¸¸¼ºÀûÀ¸·Î ¾ÆÆí·ù¸¦ »ç¿ëÇϴ ȯÀÚ¿¡´Â Åõ¿©ÇÏÁö ¾Ê´Â °ÍÀÌ ¹Ù¶÷Á÷ÇÏ´Ù.
11) Á¤½ÅÁúȯ : µå¹°°Ô ȯ°¢, Âø¶õ, ¼ö¸éÀå¾Ö, ºÒ¾È°ú ¾Ç¸ùÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù. Æ®¶ó¸¶µ¹ Åõ¿© ÈÄ Á¤½ÅÀû ÀÌ»ó¹ÝÀÀÀÌ ÀϾ ¼ö ÀÖÀ¸¸ç ±× Á¤µµ¿Í Ư¡Àº °³Àο¡ µû¶ó ´Ù¸£´Ù. (°³ÀÎÀÇ ¼º°Ý°ú Ä¡·á±â°£¿¡ ÀÇÁ¸ÀûÀÓ). ÀÌ·¯ÇÑ ¹ÝÀÀ¿¡´Â ±âºÐº¯È(ÁÖ·Î ´ÙÇà°¨, ÈçÇÏÁö ¾Ê°Ô ºÒÄè°¨), Ȱµ¿º¯È(ÁÖ·Î ¾ïÁ¦, ÈçÇÏÁö ¾Ê°Ô Áõ°¡), ÀÎÁö¿Í °¨°¢´É·Â º¯È(¿¹, °áÁ¤Çൿ, ÀνÄÀÌ»ó)°¡ Æ÷ÇԵǸç ÀÇÁ¸¼ºÀÌ ³ªÅ¸³¯ ¼öµµ ÀÖ´Ù.
12) °£´ãÁó ÀÌ»ó : ¸î ¸î »ç·Ê¿¡¼ Æ®¶ó¸¶µ¹ÀÇ Ä¡·á ±â°£ µ¿¾È °£È¿¼Ò ¼öÄ¡ »ó½ÂÀÌ º¸°íµÇ¾ú´Ù.
13) ´ë»ç ¹× ¿µ¾ç°è ÀÌ»ó : ÀúÇ÷´çÁõÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸³ª ºóµµ´Â ¾Ë·ÁÁöÁö ¾Ê¾Ò´Ù.
14) ±âŸ : ÈçÇÏÁö ¾Ê°Ô ¹ß¿, ¿°¨, ¿ÀÇÑ, ³Ã°¨, µÎµå·¯±â, ¹ßÁø, ½Ã°¢Àå¾Ö, ¹Ì°¢Àå¾Ö, üÁß°¨¼Ò, ÁÖ»çºÎÀ§ÀÇ Àڱذ¨(ÁÖ»çÁ¦¿¡ ÇÑÇÔ)ÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù. ÈçÇÏ°Ô ÇǷΰ¡ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¸ç µå¹°°Ô °ú¹ÎÁõ (¿¹, È£Èí°ï¶õ, ±â°üÁö°æ·Ã, õ¸í, Ç÷°ü½Å°æºÎÁ¾)°ú ¾Æ³ªÇʶô½Ã½º ¹ÝÀÀ, ¾ÆÆíÅõ¿© Áß´Ü ½Ã¿Í À¯»çÇÑ ±Ý´Ü Áõ»óÀÌ ´ÙÀ½°ú °°ÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù : ÈïºÐ, ºÒ¾È, ½Å°æ°ú¹Î, ºÒ¸é, ¿îµ¿°ú´Ù, ÁøÀü ¹× À§Àå°ü Áõ»ó. ºóµµ°¡ ¾Ë·ÁÁöÁö ¾ÊÀº ½Å»ý¾Æ ¾à¹°±Ý´ÜÁõÈıº, ¾à¹°³»¼ºÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù.
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1) ÀÌ ¾à°ú º¥Á¶µð¾ÆÁ¦ÇÉ°è ¾à¹° ¹× º¥Á¶µð¾ÆÁ¦ÇÉ À¯»ç ¾à¹°°ú °°Àº ÁøÁ¤Á¦, ´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.
MAO ¾ïÁ¦Á¦¸¦ Åõ¿© ÁßÀ̰ųª Åõ¿©Áß´ÜÈÄ 14ÀÏ À̳»ÀÇ È¯ÀÚ´Â ÀÌ ¾à°ú º´¿ëÅõ¿©ÇÏÁö ¾Ê´Â´Ù.
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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¦(¿¹, 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 ; Âø¶õ, ÈïºÐ, ºó¸Æ, ÁøÀü, È¥¼ö, ¹ß¿, ¹ßÇÑ, ¿îµ¿½ÇÁ¶, °ú´Ù¹Ý»ç, °£´ë¼º±Ù°æ·ÃÁõ, ¼³»ç, ÀÚ¹ßÀû °£´ë¼º °æ·Ã, ºÒ¾ÈÀ̳ª ¹ßÇÑÀ» µ¿¹ÝÇÑ À¯µµÀû ¶Ç´Â ¾È±¸ÀÇ °£´ë¼º °æ·Ã, ±äÀå Ç×Áø ¹× ¹ß¿À» ¼ö¹ÝÇÏ´Â À¯µµÀû ¶Ç´Â ¾È±¸ÀÇ °£´ë¼º °æ·Ã.
¼¼·ÎÅä´Ñ ÁõÈıºÀº ÇØ´ç ¾à¹°ÀÇ Åõ¾àÁß´Ü ÀÌÈÄ ÀϹÝÀûÀ¸·Î ºü¸£°Ô Áõ»óÀÌ °³¼±µÇ¸ç, Áõ»óÀÇ Æ¯Â¡°ú Áߵ¿¡ µû¶ó Ä¡·á¸¦ °áÁ¤ÇØ¾ß ÇÑ´Ù.
11) ¸®³×Á¹¸®µå : ºñ¼±Åüº MAO ¾ïÁ¦Á¦¿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. |
| Related FDA Approved Drug |
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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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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
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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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The database contains the following fields: The generic name of each chemical For module A10 (liver enzyme composite module): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method) Number of endpoints at which each compound is marginally active (M) Number of endpoints at which each compound is active (A) For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method) Number of ADR reports for each compound, given as <4 or ¡Ã4 Reporting Index value for each compound, except where no shipping units were available (NSU) Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period. TRAMADOL[GGT Increase][Composite Activity](Score) I(Marginal) 0(Active) 0[Alkaline Phosphatase Increase](Activity Score) I(Number of Rpts) <4(Index value) 0.1[SGOT Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.5[SGPT Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.8[LDH Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.6[GGT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0.2
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