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Æä´ÏÅäÀÎÀº »çÀÌÅäÅ©·Ò P450 3A4 È¿¼Ò°èÀÇ ÀÛ¿ëÀ» À¯µµÇÑ´Ù. ÀÌ ¾à°ú Æä´ÏÅäÀÎÀ» º´¿ëÇÒ °æ¿ì ÀÌ ¾àÀÇ »ý¹°ÇÐÀû ÀÌ¿ë·üÀÌ °¨¼ÒÇÏ¿© ÀÌ ¾àÀÇ È¿´ÉÀÌ °¨¾àµÈ´Ù. µÎ ¾à¹°À» º´¿ëÅõ¿© ÇÒ °æ¿ì ÀÌ ¾à¿¡ ´ëÇÑ ÀÓ»óÀû Ä¡·á¹ÝÀÀÀ» °üÂûÇÏ¿©¾ßÇϸç ÇÊ¿äÇÑ °æ¿ì ÀÌ ¾àÀÇ ¿ë·®Áõ°¡¸¦ °í·ÁÇØ¾ß ÇÑ´Ù. ÀÌ ¾à°ú Æä´ÏÅäÀÎÀ» º´¿ë Åõ¿©ÇÏ´Â µ¿¾È ÀÌ ¾àÀÇ ¿ë·®À» Áõ°¡½ÃÄ×´Ù¸é Æä´ÏÅäÀÎÀÇ Åõ¿©¸¦ Áß´ÜÇßÀ» °æ¿ì ÀÌ ¾àÀÇ ¿ë·®°¨¼Òµµ °í·ÁÇØ¾ß ÇÑ´Ù.
4) ½Ã¸ÞƼµòÀº »çÀÌÅäÅ©·Ò P450 3A4¸¦ ¾ïÁ¦½Ã۱⠶§¹®¿¡ ÀÌ ¾àÀÇ Ç÷Á߳󵵸¦ Áõ°¡½Ã۸ç Ç×°íÇ÷¾ÐÈ¿°ú¸¦ Áõ°½Ãų ¼ö ÀÖ´Ù.
5) ¸®ÆÊÇǽŰúÀÇ º´¿ë¿¡ ÀÇÇØ ÀÌ ¾àÀÇ ÀÛ¿ëÀÌ °¨¾àµÉ ¼ö ÀÖÀ¸¹Ç·Î º´¿ëÅõ¿©ÇÏÁö´Â ¾Ê´Â´Ù(¸®ÆÊÇǽÅÀº »çÀÌÅäÅ©·Ò P450 3A4°èÀÇ È¿¼ÒÀÛ¿ëÀ» °ÇÏ°Ô À¯µµÇÑ´Ù. µû¶ó¼ ¸®ÆÊÇǽÅÀ» ÀÌ ¾à°ú º´¿ëÇÒ °æ¿ì ÀÌ ¾àÀÇ »ý¹°ÇÐÀûÀÌ¿ë·üÀÌ ¶Ñ·ÇÇÏ°Ô °¨¼ÒÇÏ¿© ÀÌ ¾àÀÇ À¯È¿¼ºÀÌ °¨¼ÒµÈ´Ù.)
6) ÀÌ ¾àÀº Áú»ê¿°Á¦Á¦¿Í º´¿ëÅõ¿©ÇÒ ¼ö ÀÖÀ¸³ª ÀÌ·¯ÇÑ º´¿ë¿¡ ´ëÇÑ Çù½ÉÁõ¿¡¼ÀÇ À¯È¿¼ºÀº È®¸³µÇ¾î ÀÖÁö ¾Ê´Ù.
7) Äí¸¶¸°°è Ç×ÀÀ°íÁ¦¿Í º´¿ëÅõ¿©½Ã µå¹°°Ô ÇÁ·ÎÆ®·Òºó½Ã°£À» ¿¬Àå½ÃÄ×´Ù´Â º¸°í°¡ ÀÖÀ¸³ª ÀÌ·¯ÇÑ °ü·Ã¼ºÀº ºÒÈ®½ÇÇÏ´Ù.
8) Äû´Ïµò°ú º´¿ëÅõ¿©½Ã Äû´ÏµòÀÇ Ç÷Áß ³óµµ°¡ °¨¼Ò ¶Ç´Â ÀÌ ¾à Åõ¾à ÁßÁö ÈÄ ÀϺΠȯÀÚ¿¡¼ ¸íÈ®ÇÑ Äû´ÏµòÀÇ Ç÷Áß³óµµ Áõ°¡°¡ °üÂûµÇ¾ú´Ù. µû¶ó¼ ÀÌ ¾àÀ» Ãß°¡ÀûÀ¸·Î Åõ¿©Çϰųª Åõ¾àÀ» ÁßÁöÇÒ °æ¿ì Äû´ÏµòÀÇ Ç÷Áß ³óµµ¸¦ ¸ð´ÏÅÍÇϰí ÇÊ¿ä½Ã Äû´ÏµòÀÇ Åõ¿©·® Á¶ÀýÀÌ ±ÇÀåµÈ´Ù. µÎ °¡Áö ¾à¹°À» º´¿ëÅõ¿©ÇÏ¿´À» ¶§ ÀÌ ¾àÀÇ Ç÷Áß ³óµµ°¡ Áõ°¡ÇÑ´Ù´Â º¸°í°¡ ÀÖÀ¸³ª ÀÌ ¾àÀÇ ¾à¹°µ¿ÅÂÇÐÀû ¼ºÁúÀÌ º¯ÇÏÁö ¾Ê´Â´Ù´Â º¸°íµµ ÀÖ´Ù. µû¶ó¼ ÀÌ ¾àÀ» Åõ¿©ÇÏ´Â Áß¿¡ Äû´ÏµòÀ» Åõ¿©ÇÒ °æ¿ì Ç÷¾ÐÀ» ÃæºÐÈ÷ ¸ð´ÏÅÍÇØ¾ß ÇÑ´Ù. ÇÊ¿äÇÑ °æ¿ì ÀÌ ¾àÀÇ Åõ¿©·®À» °¨¼Ò½ÃÄÑ¾ß ÇÑ´Ù.
9) Åõº¸Äí¶ó¸°°ú °°Àº ±ÙÀ°ÀÌ¿ÏÁ¦¿Í º´¿ëÅõ¿©½Ã Åõº¸Äí¶ó¸°ÀÇ È¿°ú¸¦ Áõ°½ÃŲ´Ù´Â º¸°í°¡ ÀÖ´Ù
10) ½Ã»çÇÁ¸®µå¿ÍÀÇ º´¿ë¿¡ ÀÇÇØ ÀÌ ¾àÀÇ Ç÷Áß ³óµµ°¡ »ó½ÂÇß´Ù´Â º¸°í°¡ ÀÖ´Ù. µÎ°¡Áö ¾à¹°À» º´¿ëÅõ¿©ÇÏ´Â °æ¿ì Ç÷¾ÐÀº ¸ð´ÏÅÍÇØ¾ß Çϸç ÇÊ¿ä½Ã ÀÌ ¾àÀÇ Åõ¿©·®À» °¨¼Ò½ÃŲ´Ù.
11) °í¿ë·®ÀÇ ÆæÅ¸´Ò ¸¶ÃëÁ¦¸¦ Åõ¿©¹ÞÀº ´ÙÀ½ ÀÌ ¾àÀ» º¹¿ëÇÑ È¯ÀÚ¿¡¼ ½ÉÇÑ ÀúÇ÷¾ÐÀÌ º¸°íµÈ Àû ÀÖ´Ù.
12) Äû´©ÇÁ¸®½ºÆ¾/´ÞÆ÷ÇÁ¸®½ºÆ¾°ú ÀÌ ¾àÀ» º´¿ëÅõ¿©ÇÏ´Â °æ¿ì ÀÌ ¾àÀÇ Ç÷Áß³óµµ°¡ Áõ°¡ÇÒ ¼ö ÀÖ´Ù. µÎ ¾à¹°À» º´¿ëÅõ¿©ÇÏ´Â °æ¿ì, Ç÷¾ÐÀ» °üÂûÇÏ¿©¾ß Çϸç ÇÊ¿äÇÒ °æ¿ì ÀÌ ¾àÀÇ ¿ë·®À» ÁÙ¿©¾ß ÇÑ´Ù.
13) ÀÚ¸ùÁ꽺´Â »çÀÌÅäÅ©·Ò P450 3A4¸¦ ¾ïÁ¦ÇÑ´Ù. µû¶ó¼, ÀÌ ¾àÀ» ÀÚ¸ùÁ꽺¿Í ÇÔ²² Åõ¿©Çϸé ÃÊȸÅë°ú´ë»ç°¡ °¨¼ÒµÇ¾î ÀÌ ¾àÀÇ Ç÷Áß ³óµµ°¡ Áõ°¡ÇÑ´Ù. Áï, Ç÷¾Ð°ÇÏÈ¿°ú°¡ Áõ°µÉ ¼ö ÀÖ´Ù. µû¶ó¼ ÀÚ¸ùÁ꽺¸¦ ÀÏ»óÀûÀ¸·Î º¹¿ëÇÏ´Â °æ¿ì Ç÷¾Ð°ÇÏÈ¿°ú´Â ÀÚ¸ùÁ꽺¸¦ ¸¶Áö¸·À¸·Î ¼·ÃëÇÑ ÈÄ 3ÀÏÀÌ»ó Áö¼ÓµÉ ¼ö ÀÖ´Ù.
14) ¥â-Â÷´ÜÁ¦¿Í ´ÏÆäµðÇÉ º´¿ëÅõ¿© ½Ã ´ÏÆäµðÇÉ Åõ¿©½ÃÀÛÈÄ µå¹°°Ô ½ÉºÎÀüÀÌ ¹ß»ýµÉ ¼ö ÀÖ°í, ´ëµ¿¸Æ ÇùÂøÁõÀ» °¡Áø ȯÀÚÀÇ °æ¿ì ´ëµ¿¸Æ È帧ÀÇ ÀÏÁ¤ÇÑ ¹æÇØ·Î ÀÎÇØ ´ÏÆäµðÇÉÀÇ ºÎÇϰ¨¼Ò È¿°ú°¡ Àû°Ô ³ªÅ¸³ª ´õ À§ÇèÇÒ ¼ö ÀÖ´Ù. ´ëºÎºÐÀÇ Çù½ÉÁõ ȯÀÚ¿¡ ´ëÇÑ ´ÏÆäµðÇÉÀÇ ÀúÇ÷¾ÐÀÛ¿ëÀº ¾àÇϰí, Àß ¼øÀÀµÇÁö¸¸ ¸î¸îÀÇ È¯ÀÚ¿¡¼ ½ÉÇÑ ÀúÇ÷¾ÐÀÌ ³ªÅ¸³ ÀûÀÌ ÀÖ´Ù. ÀÌ·¯ÇÑ ¹ÝÀÀÀº º¸Åë óÀ½ Åõ¿©ÇÒ ¶§, ¶Ç´Â °è¼Ó »ó¿ë·® ÀÌ»óÀ» Åõ¿©ÇÒ ¶§, ¥â-Â÷´ÜÁ¦¿Í º´¿ëÅõ¿©ÇÒ ¶§ ³ªÅ¸³µ¾ú´Ù.
15) ÀÌ·ÐÀûÀ¸·Î °¡´ÉÇÑ »óÈ£ÀÛ¿ë
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´Ü, ¾ÆÁö½º·Î¸¶À̽ÅÀº ±¸Á¶ÀûÀ¸·Î ¸¶Å©·Î¶óÀ̵å°è Ç×»ýÁ¦¿Í °ü·ÃÀÌ ÀÖÁö¸¸ CYP3A4À» ÀúÇØÇÏÁö ¾Ê´Â´Ù.
(2) Ç÷ç¿Á¼¼Æ¾ : ÀÌ ¾à°ú Ç÷ç¿Á¼¼Æ¾°£ÀÇ ¾à¹°»óÈ£ÀÛ¿ë °¡´É¼º¿¡ °üÇÑ Àӻ󿬱¸´Â ¾ø´Ù. Ç÷ç¿Á¼¼Æ¾Àº in vitro¿¡¼ »çÀÌÅäÅ©·Ò P450 3A4¸¦ ÅëÇÑ ÀÌ ¾àÀÇ ´ë»ç¸¦ ¾ïÁ¦ÇÏ´Â °ÍÀ¸·Î ³ªÅ¸³µ´Ù. ±×·¯¹Ç·Î µÎ ¾à¹°À» º´¿ëÅõ¿©ÇÏ´Â °æ¿ì ÀÌ ¾àÀÇ Ç÷Áß ³óµµ°¡ Áõ°¡ÇÏ´Â °ÍÀ» ¹èÁ¦ÇÒ ¼ö ¾ø´Ù. Ç÷ç¿Á¼¼Æ¾°ú ÀÌ ¾àÀ» ÇÔ²² Åõ¿©ÇÒ ¶§, Ç÷¾ÐÀ» °üÂûÇÏ¿©¾ß Çϸç ÇÊ¿äÇÒ °æ¿ì ÀÌ ¾àÀÇ Åõ¿©·®À» ÁÙ¿©¾ß ÇÑ´Ù.
(3) Ç× HIV ´Ü¹éºÐÇØÈ¿¼Ò ¾ïÁ¦Á¦(¿¹, ¾ÏÇÁ·¹³ª¹ö, Àε𳪹ö, ³ÚÇdzª¹ö, ¸®Å䳪¹ö, »çÄû³ª¹ö : ÀÌ ¾à°ú Ç× HIV ´Ü¹éºÐÇØÈ¿¼Ò ¾ïÁ¦Á¦ÀÎ ¾ÏÇÁ·¹³ª¹ö, Àε𳪹ö, ³ÚÇdzª¹ö, ¸®Å䳪¹ö, »çÄû³ª¹ö°£ÀÇ ¾à¹°»óÈ£ÀÛ¿ë °¡´É¼º¿¡ °üÇÑ Àӻ󿬱¸´Â ¾ø´Ù. ÀÌµé °è¿ÀÇ ¾à¹°Àº »çÀÌÅäÅ©·Ò P450 3A4¸¦ ¾ïÁ¦ÇÏ´Â °ÍÀ¸·Î ¾Ë·ÁÁ® ÀÖ´Ù. ¶ÇÇÑ ÀÌµé °è¿ÀÇ ¾à¹°Àº in vitro¿¡¼ »çÀÌÅäÅ©·Ò P450 3A4¸¦ ÅëÇÑ ÀÌ ¾àÀÇ ´ë»ç¸¦ ¾ïÁ¦ÇÏ´Â °ÍÀ¸·Î ³ªÅ¸³µ´Ù. ÀÌ ¾à°ú ÀÌµé °è¿ÀÇ ¾à¹°À» º´¿ëÅõ¿©ÇÒ ¶§ ÃÊȸÅë°ú´ë»ç°¡ °¨¼ÒÇϰí ÀÌ·Î ÀÎÇØ ¾à¹°Á¦°Å°¡ °¨¼ÒÇÏ¿© ÀÌ ¾àÀÇ Ç÷Áß ³óµµ°¡ Áõ°¡ÇÏ´Â °ÍÀ» ¹èÁ¦ÇÒ ¼ö ¾ø´Ù. µÎ ¾à¹°À» ÇÔ²² Åõ¿©ÇÏ´Â °æ¿ì, Ç÷¾ÐÀ» °üÂûÇÏ¿©¾ß Çϸç ÇÊ¿äÇÒ °æ¿ì ÀÌ ¾àÀÇ Åõ¿©·®À» ÁÙ¿©¾ß ÇÑ´Ù.
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(5) ³×ÆÄÁ¶µ· : ÀÌ ¾à°ú ³×ÆÄÁ¶µ·°£ÀÇ ¾à¹°»óÈ£ÀÛ¿ë °¡´É¼º¿¡ °üÇÑ Àӻ󿬱¸´Â ¾ø´Ù. ³×ÆÄÁ¶µ·Àº »çÀÌÅäÅ©·Ò P450 3A4¸¦ ÅëÇÑ ´Ù¸¥ ¾à¹°ÀÇ ´ë»ç¸¦ ¾ïÁ¦ÇÏ´Â °ÍÀ¸·Î ¾Ë·ÁÁ® ÀÖ´Ù. ±×·¯¹Ç·Î, µÎ ¾à¹°À» º´¿ëÅõ¿©ÇÏ´Â °æ¿ì, ÀÌ ¾àÀÇ Ç÷Áß ³óµµ°¡ Áõ°¡ÇÏ´Â °ÍÀ» ¹èÁ¦ÇÒ ¼ö ¾ø´Ù. ³×ÆÄÁ¶µ·°ú ÀÌ ¾àÀ» ÇÔ²² Åõ¿©ÇÒ ¶§, Ç÷¾ÐÀ» °üÂûÇÏ¿©¾ß Çϸç ÇÊ¿äÇÒ °æ¿ì ÀÌ ¾àÀÇ Åõ¿©·®À» ÁÙ¿©¾ß ÇÑ´Ù.
(6) Ÿũ·Î¸®¹«½º´Â »çÀÌÅäÅ©·Ò P450 3A4¸¦ ÅëÇØ ´ë»çµÇ´Â °ÍÀ¸·Î ³ªÅ¸³µ´Ù. ÃÖ±Ù¿¡ ¹ßÇ¥µÈ ÀÚ·á¿¡ µû¸£¸é °æ¿ì¿¡ µû¶ó ÀÌ ¾àÀ» º´¿ëÅõ¿©Çϴ Ÿũ·Î¸®¹«½ºÀÇ ¿ë·®À» ÁÙ¿©¾ß Çß´Ù. µÎ ¾à¹°À» º´¿ëÅõ¿©ÇÏ´Â °æ¿ì, Ÿũ·Î¸®¹«½ºÀÇ Ç÷Á߳󵵸¦ °üÂûÇØ¾ß Çϸç ÇÊ¿äÇÒ °æ¿ì Ÿũ·Î¸®¹«½ºÀÇ ¿ë·®À» ÁÙ¿©¾ß ÇÑ´Ù.
(7) Ä«¸£¹Ù¸¶Á¦ÇÉ : ÀÌ ¾à°ú Ä«¸£¹Ù¸¶Á¦Çɰ£ÀÇ »óÈ£ÀÛ¿ë °¡´É¼º¿¡ °üÇÑ ¿¬±¸´Â ¾ø¾ú´Ù. Ä«¸£¸¶Á¦ÇÉÀÌ È¿¼ÒÀ¯µµÀÛ¿ë¿¡ ÀÇÇØ ±¸Á¶ÀûÀ¸·Î À¯»çÇÑ Ä®½·Ã¤³ÎÂ÷´ÜÁ¦ÀÎ ´Ï¸ðµðÇÉÀÇ Ç÷Á߳󵵸¦ ³·Ãß´Â °ÍÀ¸·Î ³ªÅ¸³µ±â ¶§¹®¿¡ ÀÌ ¾àÀÇ Ç÷Áß³óµµ°¡ °¨¼ÒÇϰí ÀÌ·Î ÀÎÇØ È¿°ú°¡ °¨¼ÒÇÏ´Â °ÍÀ» ¹èÁ¦ÇÒ ¼ö ¾ø´Ù.
(8) Æä³ë¹ÙºñÅæ : ÀÌ ¾à°ú Æä³ë¹ÙºñÅæ°£ÀÇ »óÈ£ÀÛ¿ë °¡´É¼º¿¡ °üÇÑ ¿¬±¸´Â ¾ø¾ú´Ù. Æä³ë¹ÙºñÅæÀÌ È¿¼ÒÀ¯µµÀÛ¿ë¿¡ ÀÇÇØ ±¸Á¶ÀûÀ¸·Î À¯»çÇÑ Ä®½·Ã¤³ÎÂ÷´ÜÁ¦ÀÎ ´Ï¸ðµðÇÉÀÇ Ç÷Á߳󵵸¦ ³·Ãß´Â °ÍÀ¸·Î ³ªÅ¸³µ±â ¶§¹®¿¡ ÀÌ ¾àÀÇ Ç÷Áß³óµµ°¡ °¨¼ÒÇϰí ÀÌ·Î ÀÎÇØ È¿°ú°¡ °¨¼ÒÇÏ´Â °ÍÀ» ¹èÁ¦ÇÒ ¼ö ¾ø´Ù.
(9) ¹ßÇÁ·ÎÀλê : ÀÌ ¾à°ú ¹ßÇÁ·ÎÀλ갣ÀÇ »óÈ£ÀÛ¿ë °¡´É¼º¿¡ °üÇÑ ¿¬±¸´Â ¾ø¾ú´Ù. ¹ßÇÁ·ÎÀλêÀÌ È¿¼ÒÀúÇØÀÛ¿ë¿¡ ÀÇÇØ ±¸Á¶ÀûÀ¸·Î À¯»çÇÑ Ä®½·Ã¤³ÎÂ÷´ÜÁ¦ÀÎ ´Ï¸ðµðÇÉÀÇ Ç÷Á߳󵵸¦ Áõ°¡½ÃŰ´Â °ÍÀ¸·Î ³ªÅ¸³µ±â ¶§¹®¿¡ ÀÌ ¾àÀÇ Ç÷Áß³óµµ°¡ Áõ°¡Çϰí ÀÌ·Î ÀÎÇØ È¿°ú°¡ Áõ°¡ÇÏ´Â °ÍÀ» ¹èÁ¦ÇÒ ¼ö ¾ø´Ù.
16) »óÈ£ÀÛ¿ëÀÌ ¾ø´Â ¾à¹°
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º¹¾àÀ̹ÌÁö´Â ¸ðµç º¹¾àÁöµµ »çÇ×À» Ç¥½ÃÇѰÍÀº ¾Æ´Ï¸ç, Ãß°¡ÀûÀ¸·Î ¾÷µ¥ÀÌÆ®µÇ°Å³ª ¼öÁ¤µÉ ¼ö ÀÖ½À´Ï´Ù. |
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º¹¾àÀ̹ÌÁöÀÇ Ç¥½Ã¿©ºÎ´Â ½ÇÁ¦ ¾à¹°º¹¿ë½Ã Á߿䵵¿¡ µû¸¥°ÍÀº ¾Æ´Ï¸ç ´Ü¼øÈ÷ Çã°¡Á¤º¸»ó Ű¿öµå¸¦ ±âÁØÀ¸·Î µî·ÏµÇ¾ú½À´Ï´Ù. |
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³»¿ë |
| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
º´¿ë±Ý±â :
[rifampicin]
[»óÈ£ÀÛ¿ë/º´¿ë±Ý±â°Ë»ö]
¿¬·É´ë±Ý±â :
°í½ÃµÈ ¿¬·É±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
[¿¬·É´ë±Ý±â»ó¼¼°Ë»ö]
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| Mechanism of Action |
Nifedipine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Nifedipine inhibits the influx of extracellular calcium through myocardial and vascular membrane pores by physically plugging the channel. The decrease in intracellular calcium inhibits the contractile processes of smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
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| Pharmacology |
Nifedipine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Nifedipine, the prototype of the dihydropyridine class of calcium-channel antagonists, is similar to other dihydropyridines including amlodipine, felodipine, isradipine, and nicardipine. Nifedipine is used to treat Prinzmetal's angina, hypertension, and other vascular disorders such as Raynaud's phenomenon. By blocking the calcium channels, Nifedipine inhibits the spasm of the coronary artery and dilates the systemic arteries, results in a increase of myocardial oxygen supply and a decrease in systemic blood pressure.
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| Metabolism |
Nifedipine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)Cytochrome P450 2E1 (CYP2E1)Cytochrome P450 2D6 (CYP2D6)
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| Protein Binding |
Nifedipine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 92-98%
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| Half-life |
Nifedipine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2 hours
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| Absorption |
Nifedipine¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly and fully absorbed following oral administration.
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| Pharmacokinetics |
NifedipineÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ë¹ßÇö½Ã°£
- °æ±¸ 20ºÐ À̳»
- ¼³ÇÏÁ¤ 1-5ºÐ À̳»
- ´Ü¹é°áÇÕ : 92-98% (³óµµÀÇÁ¸Àû)
- ´ë»ç : °£¿¡¼ ºñȰ¼º´ë»çü·Î ´ë»çµÊ
- »ýü³»ÀÌ¿ëÀ²
- ݼ¿Á¦ 45-75%
- ¼¹æÇüÁ¦Á¦ 65-86%
- ¹Ý°¨±â
- Á¤»ó ¼ºÀÎÀº 2-5½Ã°£
- °£°æÈ°¡ ÀÖ´Â ¼ºÀÎÀº 7½Ã°£
- ¼Ò½Ç : ´¢¸¦ ÅëÇØ ¹è¼³
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| Biotransformation |
Nifedipine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic.
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| Toxicity |
Nifedipine¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include dizziness, drowsiness, nausea, severe drop in blood pressure, slurred speech, and weakness. LD50=494 mg/kg (orally in mice); LD50=1022 mg/kg (orally in rats)
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| Drug Interactions |
Nifedipine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Amobarbital The barbiturate decreases the effect of the calcium channel blockerAprobarbital The barbiturate decreases the effect of the calcium channel blockerButabarbital The barbiturate decreases the effect of the calcium channel blockerButalbital The barbiturate decreases the effect of the calcium channel blockerButethal The barbiturate decreases the effect of the calcium channel blockerCimetidine Cimetidine increases the effect of the calcium channel blockerCisapride Cisapride increases the effect and toxicity of nifedipineCyclosporine Increased risk of gingivitisGinseng Ginseng increases the effect and toxicity of nifedipineHeptabarbital The barbiturate decreases the effect of the calcium channel blockerHexobarbital The barbiturate decreases the effect of the calcium channel blockerImatinib Imatinib increases the effect and toxicity of nifedipineMelatonin Melatonin can possibly decrease the effect of nifedipineMethohexital The barbiturate decreases the effect of the calcium channel blockerMethylphenobarbital The barbiturate decreases the effect of the calcium channel blockerPentobarbital The barbiturate decreases the effect of the calcium channel blockerPhenobarbital The barbiturate decreases the effect of the calcium channel blockerPrimidone The barbiturate decreases the effect of the calcium channel blockerSecobarbital The barbiturate decreases the effect of the calcium channel blockerTalbutal The barbiturate decreases the effect of the calcium channel blockerRifampin Rifampin decreases the effect of the calcium channel blockerQuinidine Decreased quinidine effect, increased nifedipine effectQuinidine barbiturate Decreased quinidine effect, increased nifedipine effectDihydroquinidine barbiturate Decreased quinidine effect, increased nifedipine effectQuinupristin Synercid increases the effect of ziprasidoneTacrolimus Nifedipine increases serum levels of tacrolimusSt. John's Wort St. John's Wort decreases the effect of nifedipine
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Nifedipine¿¡ ´ëÇÑ P450 table
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 |
Nifedipine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Avoid taking with grapefruit juice.Avoid natural licorice.Take with low fat meal.
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| Drug Target |
[Drug Target]
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| Description |
Nifedipine¿¡ ´ëÇÑ Description Á¤º¸ A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. [PubChem]
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| Drug Category |
Nifedipine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Calcium Channel BlockersDihydropyridinesTocolytic AgentsVasodilator Agents
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| Smiles String Canonical |
Nifedipine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC(=O)C1=C(C)NC(C)=C(C1C1=CC=CC=C1[N+]([O-])=O)C(=O)OC
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| Smiles String Isomeric |
Nifedipine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC(=O)C1=C(C)NC(C)=C(C1C1=CC=CC=C1[N+]([O-])=O)C(=O)OC
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| InChI Identifier |
Nifedipine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C17H18N2O6/c1-9-13(16(20)24-3)15(14(10(2)18-9)17(21)25-4)11-7-5-6-8-12(11)19(22)23/h5-8,15,18H,1-4H3
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| Chemical IUPAC Name |
Nifedipine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
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| Drug-Induced Toxicity Related Proteins |
NIFEDIPINE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Adenosylhomocysteinase Drug:nifedipine Toxicity:side effects. [¹Ù·Î°¡±â]
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| ÃֽŹ®Çå°ËÅä |
Sex Differences in Blood Pressure Response toAntihypertensive Therapy in Chinese Patients with Hypertension
BACKGROUND: Ç×°íÇ÷¾ÐÁ¦¿¡ ´ëÇÑ ¼ºº°°£ ¹ÝÀÀ¼ºÀÇ Â÷ÀÌ¿¡ ´ëÇØ¼´ÂÀß ¾Ë·ÁÁ® ÀÖÁö ¾Ê´Ù.
OBJECTIVE: Community-basedprospective clinical trial·Î Ç×°íÇ÷¾ÐÁ¦¿¡ ´ëÇÑ ¼ºº°°£ ¹ÝÀÀ¼º Â÷À̰¡ ÀÖ´ÂÁö¸¦ È®ÀÎÇϱâ À§ÇÏ¿© ÀÌ ¿¬±¸¸¦ ½ÃÇàÇÏ¿´´Ù.
METHODS: Áß±¹³»ÀÇ 7°³ÀÇ Áö¿ª¿¡¼ ÀÌÀü¿¡ °íÇ÷¾Ð Ä¡·á¸¦ ¹ÞÁö ¾Ê¾Ò´ø 4075¼¼ ȯÀÚ 3535¸í(¿©¼º:2326¸í)À» ¸ðÁýÇÏ¿´´Ù. ȯÀڵ鿡°Ô atenolol, hydrochlorothiazide (HCTZ), captopril, sustained-releasednifedipine Áß¿¡ 1°³ÀÇ ¾à¹°À» ¹«ÀÛÀ§ ¹èÁ¤ÇÏ¿©8ÁÖµ¿¾È ½ÃÇèÀ» ÁøÇàÇÏ¿´´Ù. ÀÌÈÄ ³²¼º°ú ¿©¼º »çÀÌÀÇ Æò±Õ Ç÷¾Ð °¨¼ÒÁ¤µµ, Ç÷¾ÐÀÌ Á¶ÀýµÇ´Â ºñÀ², ÀÌ»ó¹ÝÀÀÀÇ ¹ß»ý·üÀ» ºñ±³ÇÏ¿´´Ù.
RESULTS: ¿©¼ºÀÇ HCTZ¿¡ ´ëÇÑ ¹ÝÀÀ¼ºÀº À̿ϱâÇ÷¾Ð¿¡À־²¼ºº¸´Ù´õÁÁ¾Ò°í(1.8mmHg ´õ°¨¼Ò, p < 0.05) ³²¼ºº¸´Ù 57%ÀÌ»ó ´õ ¸ñÇ¥ÇÑÀ̿ϱâÇ÷¾Ð¿¡µµ´ÞÇÏ¿´´Ù(p < 0.05). Atenolol group¿¡¼´Â ¿©¼ºÀÌ ³²¼ºº¸´Ù Æò±Õ¼öÃà±â Ç÷¾ÐÀÌ 3.9 mmHgÀÌ»ó ´õ °¨¼ÒÇÏ¿´°í(p <0.05), ¿©¼ºÀÌ ³²¼ºº¸´Ù 65%ÀÌ»ó ´õ ¸ñÇ¥ÇÑ ¼öÃà±â Ç÷¾Ð¿¡ µµ´ÞÇÏ¿´À¸¸ç 57% ÀÌ»ó ´õ ¸ñÇ¥ÇÑ À̿ϱâÇ÷¾Ð¿¡µµ´ÞÇϱ⽬¿ü´Ù(p < 0.05).Nifedipine°ú captopril group¿¡¼ ¾à¹°°ú °ü·ÃµÈ ÀÌ»ó¹ÝÀÀÀÌ ¼ºº°°ú °ü·ÃÇÏ¿©À¯ÀǼº ÀÖ´Â Â÷À̸¦ º¸¿´Áö¸¸ (Nifedipine-15.8% in women vs 9.8% in men; p =0.017, captopril- 14.3% in women vs 8.4% in men; p = 0.005) HCTZ°ú atenolol group¿¡¼´Â À¯ÀǼº ÀÖ´Â Â÷À̸¦ º¸ÀÌÁö ¾Ê¾Ò´Ù.
CONCLUSIONS: ¿©¼ºÀÌ HCTZ¿Í atenolol¿¡ ´ëÇØ ´õ ÁÁÀº Ç÷¾Ð ¹ÝÀÀ¼ºÀ» ³ªÅ¸³»°í sustained-release nifedipine°ú captopril¿¡´ëÇØ ³²¼ºº¸´Ù ´õ ¸¹Àº ÀÌ»ó¹ÝÀÀÀ» ³ªÅ¸³»¾ú´Ù. À̰ÍÀº Ç×°íÇ÷¾ÐÁ¦¸¦ ¼±ÅÃÇϴµ¥ ÀÖ¾î¼ ¼ºº°À» °í·ÁÇÒ ¼öÀÖ´Ù´Â °ÍÀ» ÀǹÌÇÑ´Ù.
Ann Pharmacother2008;42:1772-81
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º» ¼öÁ¤ÀÏ Á¤º¸´Â Çã°¡Á¤º¸ ÀÌ¿ÜÀÇ ±âŸÁ¤º¸ ¼öÁ¤ÀÏÀ» ÀǹÌÇϹǷÎ, Çã°¡Á¤º¸¼öÁ¤ÀÏÀº º»¹®¿¡ Ç¥±âµÈ ³¯Â¥¸¦ ÂüÁ¶ÇϽñ⠹ٶø´Ï´Ù.
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»ó¼¼Á¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×À» Åä´ë·Î ÀÛ¼ºµÇ¾úÀ¸¸ç ¿ä¾àÁ¤º¸´Â »ó¼¼Á¤º¸ ¹× ±âŸ¹®ÇåÀ» ±â¹ÝÀ¸·Î µå·°ÀÎÆ÷¿¡¼ ÆíÁýÇÑ ³»¿ëÀÔ´Ï´Ù. Á¦Ç°Çã°¡»çÇ×ÀÇ ¸ñÂ÷¿Í ´Ù¼Ò »óÀÌÇÒ ¼ö ÀÖ½À´Ï´Ù. |
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µå·°ÀÎÆ÷ ÀǾàÇмúÁ¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×, Çмú¹®Çå, Á¦¾àȸ»ç Á¦°øÁ¤º¸ µîÀ» ±Ù°Å·Î ÀÛ¼ºµÈ Âü°í Á¤º¸ÀÔ´Ï´Ù.
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
Ã¥ÀÓÀ» ÁöÁö ¾Ê½À´Ï´Ù. ÀÚ¼¼ÇÑ ³»¿ëÀº ¡°Ã¥ÀÓÀÇ ÇÑ°è ¹× ¹ýÀû°íÁö¡±¸¦ ÂüÁ¶ÇØ ÁֽʽÿÀ.
¹Ýµå½Ã Á¦Á¶¡¤¼öÀÔ»ç, ÆÇ¸Å»ç, ÀÇ»ç, ¾à»ç¿¡°Ô ÃÖÁ¾ÀûÀ¸·Î È®ÀÎÇϽñ⠹ٶø´Ï´Ù.
ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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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. NIFEDIPINE[GGT Increase][Composite Activity](Score) I(Marginal) 0(Active) 0[Alkaline Phosphatase Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.3[SGOT Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.6[SGPT Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.4[LDH Increase](Activity Score) I(Number of Rpts) <4(Index value) 0.1[GGT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0
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