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2. °¹ÚÀå¾Ö : ÀÌ ¾àÀ¸·Î¼ Ãʱ⠿뷮Àº 50 mgÀ» 1ÁÖ ÀÌ»ó Åõ¿©ÇÑ´Ù. ±× ÀÌÈÄ¿¡ 1ÀÏ 100¢¦200 mgÀÇ À¯È¿¿ë·®¿¡ µµ´ÞÇÒ ¶§±îÁö ¿ë·®À» Á¡Â÷ Áõ·®Çϸç, 1ÀÏ ÃÖ´ë 300 mg±îÁö 2¢¦3ȸ·Î ³ª´©¾î º¹¿ëÇÒ ¼ö ÀÖ´Ù. ÀûÀýÇÑ Ä¡·áÈ¿°ú¸¦ ¾òÀº °æ¿ì 10ÁÖ ÈÄ¿¡µµ Ä¡·á¸¦ °è¼ÓÇÒ ¼ö ÀÖÀ¸¸ç À̶§ÀÇ ¿ë·®Àº ȯÀÚÀÇ ¹ÝÀÀÀ» °í·ÁÇÏ¿© ÃÖ¼ÒÀ¯È¿·®À¸·Î ÇÑ´Ù. Ä¡·á¿¡ ´ëÇÑ ÇÊ¿ä´Â Á¤±âÀûÀ¸·Î Æò°¡µÇ¾î¾ß ÇÑ´Ù. ¾à¹°Ä¡·á¿¡ Àß ¹ÝÀÀÇϴ ȯÀÚÀÇ °æ¿ì Çൿġ·á¸¦ µ¿½Ã¿¡ ÇÏ´Â °ÍÀ» °í·ÁÇÒ ¼ö ÀÖ´Ù.
3. Á¤½ÅÁúȯ Ä¡·á¸¦ Çϱâ À§ÇÑ MAOÀúÇØÁ¦ Àüȯ °ü·Ã
Á¤½ÅÁúȯ Ä¡·á¸¦ À§ÇÑ MAOÀúÇØÁ¦ Åõ¾àÀ» Áß´ÜÇÏ°í µ¿ Á¦Á¦ Ä¡·á¸¦ ½ÃÀÛÇÒ °æ¿ì Àû¾îµµ 14ÀÏ ÀÌ»ó °£°ÝÀ» µÎ¾î¾ß ÇÑ´Ù. ¹Ý´ë·Î, Á¤½ÅÁúȯ Ä¡·á¸¦ À§ÇØ MAOÀúÇØÁ¦ Åõ¿©¸¦ ½ÃÀÛÇÏ·Á¸é µ¿ Á¦Á¦ Åõ¾à Áß´Ü ÈÄ Àû¾îµµ 14ÀÏÀÌ °æ°úÇØ¾ß ÇÑ´Ù.
4. ¸®³×Á¹¸®µå ¶Ç´Â ¸ÞÄ¥·»ºí·ç¿Í °°Àº ´Ù¸¥ MAOÀúÇØÁ¦
¸®³×Á¹¸®µå ¶Ç´Â Á¤¸ÆÁÖ»ç¿ë ¸ÞÄ¥·»ºí·ç Á¦Á¦¸¦ Åõ¿©¹Þ´Â ȯÀÚ´Â ¼¼·ÎÅä´Ñ ÁõÈıº À§Ç輺 Áõ°¡ ¶§¹®¿¡ µ¿ Á¦Á¦ Åõ¿©¸¦ ½ÃÀÛÇØ¼´Â ¾ÈµÈ´Ù. ÀÔ¿øÀ» Æ÷ÇÔÇÑ, ´Ù¸¥ ÁßÀçÀû½Ã¼úµé, ´õ ±ä±ÞÇÑ Á¤½ÅÁúȯÀû »óÅ ġ·á¸¦ ÇÊ¿ä·Î Çϴ ȯÀÚÀÇ °æ¿ì´Â Åõ¿©¸¦ °í·ÁÇØ¾ß ÇÑ´Ù.
ÀÌ¹Ì µ¿ Á¦Á¦¸¦ Åõ¿©¹Þ´Â ȯÀÚ¿¡°Ô ¸®³×Á¹¸®µå ¶Ç´Â Á¤¸ÆÁÖ»ç¿ë ¸ÞÄ¥·»ºí·ç Á¦Á¦¸¦ ±ä±ÞÈ÷ Åõ¿©ÇÒ Çʿ䰡 ÀÖÀ» ¼ö ÀÖÀ¸¸ç, ¸®³×Á¹¸®µå³ª Á¤¸ÆÁÖ»ç¿ë ¸ÞÄ¥·»ºí·ç Á¦Á¦¿¡ ´ëÇÑ ´ëü¾à¹°ÀÌ ¾ø°í ƯÁ¤È¯ÀÚ¿¡¼ ¸®³×Á¹¸®µå ¶Ç´Â Á¤¸ÆÁÖ»ç¿ë ¸ÞÄ¥·»ºí·ç Á¦Á¦ Ä¡·áÀÇ À¯ÀͼºÀÌ ¼¼·ÎÅä´Ñ ÁõÈıº À§Ç輺À» »óȸÇÑ´Ù°í ÆÇ´ÜµÇ´Â °æ¿ì µ¿ Á¦Á¦¸¦ Áï½Ã Áß´ÜÇÏ°í ¸®³×Á¹¸®µå ¶Ç´Â Á¤¸ÆÁÖ»ç¿ë ¸ÞÄ¥·»ºí·ç Á¦Á¦¸¦ Åõ¿©ÇÒ ¼ö ÀÖ´Ù. ȯÀÚ´Â ¸®³×Á¹¸®µå ¶Ç´Â Á¤¸ÆÁÖ»ç¿ë ¸ÞÄ¥·»ºí·ç Á¦Á¦¸¦ Åõ¿©ÇÑ Áö 2ÁÖ ¶Ç´Â ¸¶Áö¸· Åõ¿© ÈÄ 24½Ã°£ Áß ¸ÕÀú ¿À´Â ½ÃÁ¡¿¡¼ ¼¼·ÎÅä´Ñ ÁõÈıº Áõ»óÀ» ¸ð´ÏÅ͸µÇØ¾ß ÇÑ´Ù. ¸®³×Á¹¸®µå ¶Ç´Â Á¤¸ÆÁÖ»ç¿ë ¸ÞÄ¥·»ºí·ç Á¦Á¦ ¸¶Áö¸· Åõ¿©·ÎºÎÅÍ 24½Ã°£ ÈÄ µ¿ Á¦Á¦ Ä¡·á¸¦ ´Ù½Ã ½ÃÀÛÇÒ ¼ö ÀÖ´Ù.
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1) MAO ¾ïÁ¦Á¦¸¦ Åõ¿© ÁßÀΠȯÀÚ
: Á¤½ÅÁúȯ Ä¡·á¸¦ À§ÇØ ÀÌ ¾à°ú MAO ÀúÇØÁ¦¸¦ º´¿ëÅõ¿©Çϰųª ÀÌ ¾à Åõ¿© Áß´Ü ÈÄ 14ÀÏ À̳»¿¡ MAOÀúÇØÁ¦¸¦ Åõ¿©ÇÏ´Â °ÍÀº ¼¼·ÎÅä´Ñ ÁõÈıº À§Ç輺À» Áõ°¡½Ã۱⠶§¹®¿¡ ±Ý±âÀÌ´Ù. Á¤½ÅÁúȯ Ä¡·á¸¦ À§ÇØ MAO ÀúÇØÁ¦ Åõ¿© Áß´Ü ÈÄ 14ÀÏ À̳»¿¡ ÀÌ ¾àÀ» Åõ¿©ÇÏ´Â °Í ¶ÇÇÑ ±Ý±âÀÌ´Ù. (¿ë¹ý¤ý¿ë·® Ç× ¹× 5. ÀϹÝÀûÁÖÀÇ Ç× ÂüÁ¶)
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2) ÀÌ ¾à ¶Ç´Â ÀÌ ¾àÀÇ ±¸¼º¼ººÐ¿¡ °ú¹Î¹ÝÀÀ ȯÀÚ
3) Ƽ¿À¸®´ÙÁø, ¸Þ¼Ò¸®´ÙÁø, ÇǸðÁöµå, ƼÀڴϵò¿°»ê¿°, Å׸£Æä³ªµò, ¾Æ½ºÅ×¹ÌÁ¹ ¶Ç´Â ½Ã»çÇÁ¸®µå¸¦ Åõ¿© ÁßÀΠȯÀÚ
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1) °£Àå¾Ö ȯÀÚ(ÀÌ ¾àÀÇ AUCÁõ°¡µÇ¾î ¹Ý°¨±â°¡ ¿¬ÀåµÈ´Ù. Àú¿ë·®À¸·Î Ä¡·á¸¦ ½ÃÀÛÇϰí ÁÖÀÇ ±í°Ô ¸ð´ÏÅ͸µÇÏ¿©¾ß ÇÑ´Ù.)
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5) Á¶Áõ ¶Ç´Â ±× º´·ÂÀÌ Àִ ȯÀÚ(Á¶Áõ »óÅ¿¡ Àִ ȯÀÚ´Â ÀÌ ¾àÀÇ Åõ¿©¸¦ ÁßÁöÇØ¾ß ÇÑ´Ù.)
6) ³úÀÇ ±âÁúÀûÀå¾Ö ¶Ç´Â Á¤½ÅÁúȯÀÇ ¿äÀÎÀÌ Àִ ȯÀÚ(Á¤½ÅÁõ»óÀ» ¾ÇȽÃų ¼ö ÀÖ´Ù.)
7) Ãæµ¿¼ºÀÌ ³ôÀº º´Á¸Àå¾Ö ȯÀÚ(Á¤½ÅÁõ»óÀ» ¾ÇȽÃų ¼ö ÀÖ´Ù.)
8) ½ÉÀåÁúȯ ȯÀÚ(¹æ½ÇÂ÷´Ü, ½É½Çºó¹Ú µîÀÌ ³ªÅ¸³µ´Ù´Â º¸°í°¡ ÀÖ´Ù.)
9) ÃâÇ÷¼ºÁúȯ º´·Â ¶Ç´Â ÃâÇ÷¼º¿äÀÎÀÌ Àִ ȯÀÚ(ÃâÇ÷°æÇâÀÌ Áõ´ëµÉ ¼ö ÀÖ´Ù.)
10) °í·ÉÀÚ
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(12) °ñ°Ý±Ù ¹× °áÇÕÁ¶Á÷ : ¶§¶§·Î °üÀýÅë, ±ÙÀ°Åë
(13) ÀÏ¹Ý Àå¾Ö ¹× Åõ¿©ºÎÀ§ : ¾à¹°±Ý´ÜÁõÈıº(½Å»ý¾Æ ¾à¹°±Ý´ÜÁõÈıº Æ÷ÇÔ), ÀÚÁÖ ¹«·Â, ±Çۨ
(14) °æ·Ã, Çê¼Ò¸®, È¥¶õ, ȯ°¢, ¸Á»ó, ÀǽÄÀå¾Ö, ¼îÅ©, ¾Æ³ªÇʶô½Ã½º Áõ»ó, ¼¼·ÎÅä´ÑÁõÈıº(Âø¶õ, ¹ß¿, ÁøÀü, ¹ßÇÑ µîÀÌ ¹ßÇö)ÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î °üÂûÀ» ÃæºÐÈ÷ Çϰí ÀÌ»óÀÌ ÀÎÁ¤µÇ´Â °æ¿ì Åõ¾àÀ» ÁßÁöÇϰí ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù.
(15) Ç×Á¤½Å¾à(Ç×Á¤½Åº´¾à, Ç׿ì¿ï¾à µî)ÀÇ º´¿ëÀ¸·Î ½Å°æÀÌ¿ÏÁ¦¾Ç¼ºÁõÈıºÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î, ¿îµ¿¸¶ºñ, ÁßÁõÀÇ ±ÙÀ°°Á÷, »ïÅ´°ï¶õ, ºó¸Æ, Ç÷¾Ðº¯È, ¹ßÇÑ µîÀÌ ³ªÅ¸³ª°í ÀÌ·¯ÇÑ Áõ»ó°ú ÇÔ²² ¹ß¿ÀÌ ³ªÅ¸³ª´Â °æ¿ì Åõ¿©¸¦ ÁßÁöÇÏ°í ½Åü³Ã°¢, ¼öºÐº¸±Þ µî Àü½ÅÀû °ü¸®¿Í ÇÔ²² ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù. ÀÌ Áõ»óÀÇ ¹ßÇö½Ã¿¡´Â ¹éÇ÷±¸ Áõ°¡, Ç÷û CPKÀÇ »ó½ÂÀÌ ÀÚÁÖ ³ªÅ¸³ª°í ¹Ì¿À±Û·Îºó´¢ÁõÀ» µ¿¹ÝÇÑ ½Å±â´ÉÀúÇϰ¡ ³ªÅ¸³¯ ¼ö ÀÖ´Ù. ¶ÇÇÑ °í¿ÀÌ Áö¼ÓµÇ°í ÀǽÄÀå¾Ö, È£Èí°ï¶õ, ¼øÈ¯ÇãÅ»°ú Å»¼öÁõ»ó, ±Þ¼º ½ÅºÎÀüÀ¸·Î ¹ßÀüÇØ¼ »ç¸ÁÇß´Ù´Â º¸°í°¡ ÀÖ´Ù.
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1) ÀÌ ¾àÀº °£¾à¹°´ë»çÈ¿¼Ò Áß CYP1A2 ¹× CYP2C19ÀÇ °ÇÑ ÀúÇØÁ¦À̰í, CYP2C9, CYP2D6 ¹× CYP3A4´Â ³·Àº Á¤µµ·Î ÀúÇØÇÑ´Ù. ÀÌ ¾àÀº ÀÌ·¯ÇÑ CYPÈ¿¼Ò¿¡ ÀÇÇØ ´ë»çµÇ´Â ¾à¹°ÀÇ ºÐÇØ¸¦ ´ÊÃâ ¼ö ÀÖ´Ù. Ŭ·ÎÇǵµ±×·¼°ú °°Àº Àü±¸¾à¹°(prodrug)ÀÇ °æ¿ì´Â ÀÌ ¾à°ú º´¿ëÅõ¿© ½Ã Ȱ¼º´ë»çüÀÇ Ç÷Áß³óµµ°¡ ³·¾ÆÁú ¼ö ÀÖ´Ù. Ŭ·ÎÇǵµ±×·¼°ú ÀÌ ¾àÀ» º´¿ëÇÏ´Â °ÍÀº ±ÇÀåµÇÁö ¾Ê´Â´Ù. Àü±¸¾à¹°À» º´¿ëÇÒ °æ¿ì¿¡´Â ÀÌ ¾àÀ» ³·Àº ¿ë·®À¸·Î ½ÃÀÛÇϰųª ÀûÁ¤Çϵµ·Ï ÇÑ´Ù. ÇÊ¿ä ½Ã º´¿ëÅõ¿© µÈ ¾à¹°ÀÇ Ç÷Áß³óµµ, ¾à¹°È¿°ú, ÀÌ»ó¹ÝÀÀÀ» ¸ð´ÏÅ͸µÇϰí, Åõ¿©¿ë·®À» ÁÙ¿©¾ß ÇÑ´Ù. ÀÌ ¾àÀ¸·Î Ä¡·á°³½Ã ¶Ç´Â Á¾·á½Ã¿¡ ÀÓ»óÀûÀ¸·Î Áß´ëÇÑ »óÈ£ÀÛ¿ëÀÇ °¡´É¼ºÀÌ ÀÖ´Â Çù¼ÒÇÑ Ä¡·á°è¼ö¸¦ °¡Áø ¾à¹°(¿¹ : ¿Í¸£ÆÄ¸°, Æä´ÏÅäÀÎ, Å׿ÀÇʸ°, Ä«¸£¹Ù¸¶Á¦ÇÉ, Ŭ·ÎÀÚÇÉ)À» º´¿ëÇÒ °æ¿ì ¿ë·®À» Á¶ÀýÇÒ Çʿ䰡 ÀÖ´Ù. ÀÌ ¾àÀ» µð°î½ÅÀ̳ª ¾ÆÅ׳î·Ñ°ú º´¿ëÇÒ °æ¿ì »óÈ£ÀÛ¿ëÀº °üÂûµÇÁö ¾Ê¾Ò´Ù.
2) º´¿ë±Ý±â ¾à¹°
(1) MAO ¾ïÁ¦Á¦ : ¿ë¹ý¤ý¿ë·® Ç×, »ç¿ë»óÀÇÁÖÀÇ»çÇ× Áß 2. ´ÙÀ½ ȯÀÚ¿¡´Â Åõ¿©ÇÏÁö ¸» °Í Ç× ¹× 5 .ÀϹÝÀûÁÖÀÇ Ç×À» ÂüÁ¶ÇÑ´Ù.
(2) Ƽ¿À¸®´ÙÁø, ÇǸðÁöµå : º´¿ëÀ¸·Î Ƽ¿À¸®´ÙÁø, ÇǸðÁöµåÀÇ Ç÷Áß³óµµ°¡ »ó½Â ¶Ç´Â ¹Ý°¨±â°¡ ¿¬ÀåµÇ¾î QT¿¬Àå, ½É½Ç¼ººÎÁ¤¸Æ(torsases de pointes¸¦ Æ÷ÇÔ) µîÀÇ ½ÉÇ÷°ü°èÀÇ ÀÌ»ó¹ÝÀÀÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù.
(3) ƼÀڴϵò¿°»ê¿° : º´¿ëÀ¸·Î ƼÀڴϵò¿°»ê¿°ÀÇ Ç÷Áß³óµµ°¡ »ó½Â ¶Ç´Â ¹Ý°¨±â°¡ ¿¬ÀåµÇ¾î ÇöÀúÇÑ Ç÷¾ÐÀúÇÏ µîÀÇ ÀÌ»ó¹ÝÀÀÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù.
(4) ½Ã»çÇÁ¸®µå : º´¿ëÀ¸·Î ½Ã»çÇÁ¸®µåÀÇ Ç÷Áß³óµµ »ó½Â °¡´É¼ºÀÌ ÀÖ¾î QT¿¬Àå, ½É½Ç¼ººÎÁ¤¸Æ µîÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù.
3) º´¿ëÁÖÀÇ ¾à¹°
(1) ¸®Æ¬ : ½ÉÇÑ ¿ì¿ïÁõ ȯÀÚ¿¡ ÀÌ ¾àÀ» ¸®Æ¬°ú Á¶ÇÕÇÏ¿© »ç¿ëÇÒ °æ¿ì ¸®Æ¬À¸·Î ÀÎÇÏ¿© ÀÌ ¾àÀÇ ÀÌ»ó¹ÝÀÀÀ» °È½Ãų ¼ö ÀÖ´Ù. ÀÌ ¾àÀ» ´Ù¸¥ ¼¼·ÎÅä´Ñ¾à°ú ÇÔ²² »ç¿ëÇϸé, ¼¼·ÎÅä´Ñ È¿°ú¸¦ Áõ°¡½Ãų ¼ö ÀÖ´Ù.
(2) L-Æ®¸³ÅäÆÇÀ» ÇÔÀ¯ÇÏ´Â Á¦Á¦ : ¼¼·ÎÅä´ÑÁõÈıºÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù.
(3) ¼¼·ÎÅä´Ñ¼º ¾à¹° : ¿ë¹ý¤ý¿ë·® Ç×, »ç¿ë»óÀÇÁÖÀÇ»çÇ× Áß 2. ´ÙÀ½ ȯÀÚ¿¡´Â Åõ¿©ÇÏÁö ¸» °Í Ç× ¹× 5 .ÀϹÝÀûÁÖÀÇ Ç×À» ÂüÁ¶ÇÑ´Ù.
(4) Ç×Àü°£Á¦, »ïȯ°è Ç׿ì¿ï¾à, º¥Á¶µð¾ÆÁ¦ÇÉ°è ¾à¹°, ¿Ã¶õÀÚÇÉ, ¸ß½Ç·¹Æ¾¿°»ê¿° : ÀÌ·¯ÇÑ ¾à¹°ÀÇ Ç÷Á߳󵵸¦ »ó½Â½Ãų ¼ö ÀÖÀ¸¹Ç·Î, º´¿ë½Ã ÀÌ·¯ÇÑ ¾à¹°À» °¨·®ÇÏ´Â µî ÁÖÀÇÇÏ¿© Åõ¿©ÇÑ´Ù.
(5) º£Å¸-Â÷´Ü¾à(ÇÁ·ÎÇÁ¶ó³ë³î¿°»ê¿°) : ÇÁ·ÎÇÁ¶ó³ë³îÀÇ Ç÷Áß³óµµ »ó½ÂÀ¸·Î »ý°¢µÇ´Â ¼¸Æ, ÀúÇ÷¾Ð µîÀÌ º¸°íµÇ°í ÀÖÀ¸¹Ç·Î ÁÖÀÇÇÏ¿© Åõ¿©ÇÑ´Ù.
(6) ÀÜÆ¾°è ±â°üÁöÈ®ÀåÁ¦(Å׿ÀÇʸ° µî) : Å׿ÀÇʸ°ÀÇ Ã»¼ÒÀ²À» 1/3·Î ÀúÇÏÇÏ´Â °æ¿ì°¡ ÀÖÀ¸¹Ç·Î, Å׿ÀÇʸ°ÀÇ ¿ë·®À» 1/3·Î °¨·®ÇÏ´Â µî ÁÖÀÇÇÏ¿© Åõ¿©ÇÑ´Ù. º´¿ëÇÏ´Â °æ¿ì ¾îÁö·¯¿ò, Á¹À½, ºÎÁ¤¸Æ µîÀÌ ³ªÅ¸³µ´Ù´Â º¸°í°¡ ÀÖ´Ù.
(7) ½ÃŬ·Î½ºÆ÷¸° : ½ÃŬ·Î½ºÆ÷¸°ÀÇ Ç÷Áß³óµµ »ó½ÂÀÌ º¸°íµÇ¾úÀ¸¹Ç·Î ÁÖÀÇÇÏ¿© Åõ¿©ÇÑ´Ù.
(8) Äí¸¶¸°°è Ç×Ç÷¾×ÀÀ°íÁ¦(¿Í¸£ÆÄ¸°Ä®·ý) : ¿Í¸£ÆÄ¸°ÀÇ Ç÷Áß³óµ¶ »ó½ÂÇÏ¿´´Ù´Â º¸°í°¡ ÀÖÀ¸¹Ç·Î ÇÁ·ÎÆ®·Òºó½Ã°£À» ÃøÁ¤ÇÏ°í ¿Í¸£ÆÄ¸°ÀÇ ¿ë·®À» Á¶ÀýÇÏ´Â µî ÁÖÀÇÇÏ¿© Åõ¿©ÇÑ´Ù.
(9) ÃâÇ÷°æÇâÀÌ Áõ°µÇ´Â ¾à¹°(Ç×Á¤½Åº´¾à, Æä³ëƼ¾ÆÁø°è ¾à¹°, »ïȯ°è Ç׿ì¿ï¾à, ¾Æ½ºÇǸ° µî NSAID·ù, ¿Í¸£ÆÄ¸° µî) : ÇǺÎÀÇ ÀÌ»óÃâÇ÷(±¸»óÃâÇ÷, ÀÚ¹Ý µî), ÃâÇ÷Áõ»ó(À§ÀåÃâÇ÷ µî)ÀÌ º¸°íµÇ¾úÀ¸¹Ç·Î ÁÖÀÇÇÏ¿© Åõ¿©ÇÑ´Ù.
(10) ¾ËÄÚ¿Ã : ÀÌ ¾à º¹¿ëÁß ¾ËÄÚ¿Ã º¹¿ëÀº ÇÇÇØ¾ß ÇÑ´Ù.
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| Pharmacology |
Fluvoxamine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Fluvoxamine is one of a class of antidepressants known as selective serotonin reuptake inhibitors (SSRIs). It is used to treat the depression associated with mood disorders. It is also used on occassion in the treatment of body dysmorphic disorder and anxiety. The antidepressant, antiobsessive-compulsive, and antibulimic actions of Fluvoxamine are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin. In vitro studies show that Fluvoxamine is a potent and selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake. Fluvoxamine has no significant affinity for adrenergic (alpha1, alpha2, beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors; antagonism of such receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs. The chronic administration of Fluvoxamine was found to downregulate brain norepinephrine receptors, as has been observed with other drugs effective in the treatment of major depressive disorder. Fluvoxamine does not inhibit monoamine oxidase.
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| Metabolism |
Fluvoxamine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)Cytochrome P450 2D6 (CYP2D6)Monoamine oxidase type A (MAO-A)Cytochrome P450 2C9 (CYP2C9)Cytochrome P450 2C19 (CYP2C19)Cytochrome P450 1A1 (CYP1A1)
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| Protein Binding |
Fluvoxamine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ ~77-80% (plasma protein)
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| Half-life |
Fluvoxamine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 15.6 hours
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| Absorption |
Fluvoxamine¿¡ ´ëÇÑ Absorption Á¤º¸ Well absorbed, bioavailability of fluvoxamine maleate is 53%.
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| Biotransformation |
Fluvoxamine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic
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| Toxicity |
Fluvoxamine¿¡ ´ëÇÑ Toxicity Á¤º¸ Side effects include anorexia, constipation, dry mouth, headache, nausea, nervousness, skin rash, sleep problems, somnolence, liver toxicity, mania, increase urination, seizures, sweating increase, tremors, or Tourette's syndrome.
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| Drug Interactions |
Fluvoxamine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Almotriptan Increased risk of CNS adverse effectsEletriptan Increased risk of CNS adverse effectsFrovatriptan Increased risk of CNS adverse effectsNaratriptan Increased risk of CNS adverse effectsRizatriptan Increased risk of CNS adverse effectsSumatriptan Increased risk of CNS adverse effectsZolmitriptan Increased risk of CNS adverse effectsAminophylline Increases the effect and toxicity of theophyllineDyphylline Increases the effect and toxicity of theophyllineOxtriphylline Increases the effect and toxicity of theophyllineTheophylline Increases the effect and toxicity of theophyllineAmitriptyline Fluvoxamine increases the effect and toxicity of tricyclicsAmoxapine Fluvoxamine increases the effect and toxicity of tricyclicsClomipramine Fluvoxamine increases the effect and toxicity of tricyclicsDesipramine Fluvoxamine increases the effect and toxicity of tricyclicsDoxepin Fluvoxamine increases the effect and toxicity of tricyclicsImipramine Fluvoxamine increases the effect and toxicity of tricyclicsNortriptyline Fluvoxamine increases the effect and toxicity of tricyclicsProtriptyline Fluvoxamine increases the effect and toxicity of tricyclicsTrimipramine Fluvoxamine increases the effect and toxicity of tricyclicsAmphetamine Risk of serotoninergic syndromeBenzphetamine Risk of serotoninergic syndromeDextroamphetamine Risk of serotoninergic syndromeDexfenfluramine Risk of serotoninergic syndromeDiethylpropion Risk of serotoninergic syndromeFenfluramine Risk of serotoninergic syndromeMazindol Risk of serotoninergic syndromeMethamphetamine Risk of serotoninergic syndromePhendimetrazine Risk of serotoninergic syndromePhentermine Risk of serotoninergic syndromePhenylpropanolamine Risk of serotoninergic syndromeSibutramine Risk of serotoninergic syndromeAnisindione Fluvoxamine increases the effect of the anticoagulantAcenocoumarol Fluvoxamine increases the effect of the anticoagulantDicumarol Fluvoxamine increases the effect of the anticoagulantWarfarin Fluvoxamine increases the effect of the anticoagulantAstemizole Increased risk of cardiotoxicity and arrhythmiasMesoridazine Increased risk of cardiotoxicity and arrhythmiasTerfenadine Increased risk of cardiotoxicity and arrhythmiasThioridazine Increased risk of cardiotoxicity and arrhythmiasCarbamazepine Fluvoxamine increases the effect of carbamazepineCilostazol Fluvoxamine increases the effect of cilostazolClozapine The antidepressant increases the effect of clozapineDihydroergotamine Possible ergotism and severe ischemia with this combinationErgotamine Possible ergotism and severe ischemia with this combinationDuloxetine Fluvoxamine increases the effect and toxicity of duloxetineEthotoin Increases the effect of hydantoinFosphenytoin Increases the effect of hydantoinMephenytoin Increases the effect of hydantoinPhenytoin Increases the effect of hydantoinIsocarboxazid Possible severe adverse reaction with this combinationPhenelzine Possible severe adverse reaction with this combinationTranylcypromine Possible severe adverse reaction with this combinationRasagiline Possible severe adverse reaction with this combinationSelegiline Possible severe adverse reaction with this combinationLinezolid Combination associated with possible serotoninergic syndromeLithium The SSRI increases serum levels of lithiumMethadone Fluvoxamine increases the effect and toxicity of methadoneMexiletine Increases the effect and toxicity of mexiletineMirtazapine Increases the effect adn toxicity of mirtazapineMoclobemide Increased incidence of adverse effects with this associationOlanzapine Fluvoxamine increases the effect and toxicity of olanzapineOxycodone Increased risk of serotonin syndromeTramadol Increased risk of serotonin syndromeRamelteon Fluvoxamine increases the levels/toxicity of ramelteonRopinirole Increases the effect and toxicity of ropiniroleRopivacaine Increases the effect and toxicity of ropivacaineSt. John's Wort St. John's Wort increases the effect and toxicity of the SSRITacrine Fluvoxamine increases the effect of tacrineTizanidine Fluvoxamine increases the effect/toxicity of tizanidine
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Fluvoxamine¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 1A2
clozapine
cyclobenzaprine
imipramine
mexiletine
naproxen
riluzole
tacrine
theophylline
INHIBITORS
CYP 1A2
cimetidine
fluoroquinolones
**fluvoxamine**
ticlopidine
INDUCERS
CYP 1A2
tobacco
SUBSTRATES
CYP 3A4/3A5/3A7
Macrolide antibiotics:
clarithromycin
erythromycin
NOT azithromycin
telithromycin
Anti-arrhythmics:
quinidine
Benzodiazepines:
alprazolam
diazepam
midazolam
triazolam
Immune Modulators:
cyclosporine
tacrolimus (FK506)
HIV Protease Inhibitors:
indinavir
ritonavir
saquinavir
Prokinetic:
cisapride
Antihistamines:
astemizole
chlorpheniramine
Calcium Channel Blockers:
amlodipine
diltiazem
felodipine
nifedipine
nisoldipine
nitrendipine
verapamil
HMG CoA Reductase Inhibitors:
atorvastatin
cerivastatin
lovastatin
NOT pravastatin
simvastatin
aripiprazole
buspirone
gleevec
haloperidol (in part)
methadone
pimozide
quinine
NOT rosuvastatin
sildenafil
tamoxifen
trazodone
vincristine
INHIBITORS
CYP 3A4/3A5/3A7
HIV Protease Inhibitors:
indinavir
nelfinavir
ritonavir
amiodarone
NOT azithromycin
cimetidine
clarithromycin
diltiazem
erythromycin
**fluvoxamine**
grapefruit juice
itraconazole
ketoconazole
mibefradil
nefazodone
troleandomycin
verapamil
INDUCERS
CYP 3A4/3A5/3A7
carbamazepine
phenobarbital
phenytoin
rifabutin
rifampin
St. John's wort
troglitazone
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| Food Interaction |
Fluvoxamine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid high doses of caffeine.Take without regard to meals.Avoid alcohol.Grapefruit and grapefruit juice should be avoided throughout treatment as grapefruit can significantly increase serum levels of this product.
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| Drug Target |
[Drug Target]
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| Description |
Fluvoxamine¿¡ ´ëÇÑ Description Á¤º¸ Fluvoxamine (brand name as Luvox®, Faverin®, Fevarin® and Dumyrox®) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor. Though it is in the same class as other SSRI drugs, it is most often used to treat obsessive-compulsive disorder.Fluvoxamine has been in use in clinical practice since 1983 and has a clinical trial database comprised of approximately 35,000 patients. It was launched in the US in December 1994 and in Japan in June 1999. As of the end of 1995, more than 10 million patients worldwide have been treated with fluvoxamine.
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| Drug Category |
Fluvoxamine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-anxiety AgentsAntidepressive AgentsAntidepressive Agents, Second-GenerationSelective Serotonin Reuptake Inhibitors (SSRIs)Serotonin Uptake Inhibitors
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| Smiles String Canonical |
Fluvoxamine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COCCCCC(=NOCCN)C1=CC=C(C=C1)C(F)(F)F
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| Smiles String Isomeric |
Fluvoxamine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COCCCC\C(C1=CC=C(C=C1)C(F)(F)F)=N/OCCN
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| InChI Identifier |
Fluvoxamine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C15H21F3N2O2/c1-21-10-3-2-4-14(20-22-11-9-19)12-5-7-13(8-6-12)15(16,17)18/h5-8H,2-4,9-11,19H2,1H3
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| Chemical IUPAC Name |
Fluvoxamine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-[[5-methoxy-1-[4-(trifluoromethyl)phenyl]pentylidene]amino]oxyethanamine
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| Drug-Induced Toxicity Related Proteins |
FLUVOXAMINE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:CYP2D6 Drug:Fluvoxamine Toxicity:Toxicity and inefficacy. [¹Ù·Î°¡±â] MALEATE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Intercellular adhesion molecule 1 Drug:maleate Toxicity:hepatic injury. [¹Ù·Î°¡±â]
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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. FLUVOXAMINE[GGT Increase][Composite Activity](Score) A(Marginal) 0(Active) 2[Alkaline Phosphatase Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 2.7[SGOT Increase](Activity Score) A(Number of Rpts) ¡Ã4(Index value) 8.9[SGPT Increase](Activity Score) A(Number of Rpts) ¡Ã4(Index value) 8.9[LDH Increase](Activity Score) I(Number of Rpts) <4(Index value) 2.1[GGT Increase](Activity Score) I(Number of Rpts) <4(Index value) 1.4
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