Ŭ·¡¸®½Ãµå°ÇÁ¶½Ã·´250mg/5mL(Ŭ·¡¸®½º·Î¸¶À̽Å) (100mL)  KLARICID SYR.[Clarithromycin]  
                    
                 
               
              
                
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644200543  \0 ¿ø/100(1)mL/º´(2018.03.01) (ÇöÀç¾à°¡) \149 ¿ø/100(1)mL/º´(2017.02.01) (º¯°æÀü¾à°¡) 
                         
                        
						     
						     
                         
                      
                     
                       
                     
                     
                    
                       ATCÄÚµå 
                      Clarithromycin  / J01FA09 
                     
                    
                    
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Å©·¹¾ÆÆ¼´Ñû¼ÒÀ²ÀÌ 30mL/min/1.73m2 ÀÌÇÏÀÎ ½ÅºÎÀü ȯÀÚÀÇ °æ¿ì¿¡´Â ¿ë·®À» Àý¹ÝÀ¸·Î ÁÙ¿©¾ß ÇÑ´Ù. ÀÌ·± ȯÀÚ¿¡°Ô´Â 14ÀÏ ÀÌ»ó Åõ¿©ÇÏÁö ¾Ê´Â´Ù.
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Àû·®ÀÇ ¹°À» ³Ö°í Àß Èçµé¾î ¿ëÇØ½ÃŲ´Ù. Á¶Á¦µÈ ÀÌ ¾àÀÇ ³óµµ´Â 250mg/5mLÀÌ´Ù.
 
  
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   2,500mg/50mL
   
   27mL
   
   50mL
   
   250mg/5mL
   
   
  
   3,500mg/70mL
   
   37mL
   
   70mL
   
   250mg/5mL
   
   
  
   5,000mg/100mL
   
   53mL
   
   100mL
   
   250mg/5mL
   
   
  
   7,000mg/140mL
   
   74mL
   
   140mL
   
   250mg/5mL
   
   
 
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13) ÀúÄ®·ýÇ÷Áõ ȯÀÚ
14) ÀÌ ¾àÀº À¯´çÀ» ÇÔÀ¯Çϰí ÀÖÀ¸¹Ç·Î, °¥¶ôÅä¿À½º ºÒ³»¼º(galactose intolerance), Lapp À¯´çºÐÇØÈ¿¼Ò °áÇÌÁõ(Lapp lactase deficiency) ¶Ç´Â Æ÷µµ´ç-°¥¶ôÅä¿À½º Èí¼öÀå¾Ö(glucose-galctose malabsorption) µîÀÇ À¯ÀüÀûÀÎ ¹®Á¦°¡ Àִ ȯÀÚ¿¡°Ô´Â Åõ¿©ÇÏ¸é ¾È µÈ´Ù. (¼¹æÁ¤¿¡ ÇÑÇÔ)
 
   
  
  
  
  
   
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4) È£Èí±â°è : ¹ß¿, ±âħ, È£Èí°ï¶õ, ÈäºÎ X¼± ÀÌ»ó, È£»ê±¸ Áõ°¡ µîÀ» ¼ö¹ÝÇϴ ȣ»ê±¸¼º ÆóħÀ±․°£Áú¼ºÆó·Å µîÀÌ »ý±æ ¼ö ÀÖÀ¸¹Ç·Î ÀÌ¿Í °°Àº Áõ»óÀÌ ¹ß»ýÇϸé Åõ¿©¸¦ ÁßÁöÇϰí ÄÚ¸£Æ¼ÄÚÀ̵åÀÇ Åõ¿© µî ÀûÀýÇÑ Ã³Ä¡¸¦ ½Ç½ÃÇÑ´Ù. ¸¸¼º ±â°üÁö¿° ¹× ±Þ¼º »ó¾Çµ¿¿°ÀÇ ±Þ¼º¾Çȵµ °üÂûµÇ¾ú´Ù.
5) Ç÷¾×°è : ¶§¶§·Î È£»ê±¸ Áõ°¡, Ç÷¼ÒÆÇ °¨¼Ò, ¹üÇ÷±¸ °¨¼Ò, ¿ëÇ÷¼º ºóÇ÷, ¹éÇ÷±¸ °¨¼Ò, ¹«°ú¸³±¸Áõ µîÀÌ ³ªÅ¸³ª±âµµ ÇϹǷΠÁ¤±âÀûÀ¸·Î °Ë»çÇÏ¿© ÃæºÐÈ÷ °üÂûÀ» Çϰí, ÀÌ»ó¹ÝÀÀÀÌ ³ªÅ¸³ª¸é Åõ¿©¸¦ ÁßÁöÇÏ´Â µî, ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù.
6) ÁßÃ߽Űæ°è : ¾îÁö·¯¿ò, ¿ì¿ï, ¹Ì°¢¼Ò½Ç, Èİ¢»ó½Ç, ºÒ¾È, µå¹°°Ô ºÒ¸é, ¾Ç¸ù, À̸í, Âø¶õ, Áö³²·ÂÀå¾Ö, ȯ°¢, Á¤½Åº´, ÀÌÀÎÁõ, °æ·Ã(°Á÷°£´ë¼º, °£´ë¼º±Ù°æ·ÃÁõ, ÀǽļҽǹßÀÛ µî), ¶³¸², ¸¶ºñ°¨ µî Àϰú¼º ÁßÃ߽Űæ°è ÀÌ»ó¹ÝÀÀÀÌ ³ªÅ¸³µ´Ù´Â º¸°í°¡ ÀÖÀ¸³ª ÀÌ ¾à°úÀÇ °ü·Ã¿©ºÎ´Â ¹àÇôÁöÁö ¾Ê¾Ò´Ù. Çൿº¯È, Á¶ÁõÇൿÀÌ ³ªÅ¸³µÀ¸³ª ¾à¹°Åõ¿©¸¦ Áß´ÜÇÏ¸é ¼Ò½ÇµÈ´Ù. ¿©·¯ °¡Áö ÀÌ»ó¹ÝÀÀÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î °üÂûÀ» ÃæºÐÈ÷ Çϰí ÀÌ»ó¹ÝÀÀÀÌ ³ªÅ¸³ª´Â °æ¿ì¿¡´Â Åõ¿©¸¦ ÁßÁöÇϰí ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù.
7) ÇǺΠ: ½ºÆ¼ºì½¼-Á¸½¼ÁõÈıº, µ¶¼ºÇ¥ÇDZ«»ç¿ëÇØ µîÀÌ ¹ß°ßµÇ±âµµ ÇϹǷΠÀß °üÂûÇϰí ÀÌ»ó¹ÝÀÀÀÌ ³ªÅ¸³ª´Â °æ¿ì¿¡´Â Åõ¿©¸¦ ÁßÁöÇÏ°í ºÎ½ÅÇÇÁúÈ£¸£¸óÁ¦ÀÇ Åõ¿© µî ÀûÀýÇÑ Ã³Ä¡¸¦ ½Ç½ÃÇÑ´Ù. ¾Ë·¹¸£±â¼º Àڹݺ´ÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î °üÂûÀ» ÃæºÐÈ÷ Çϰí ÀÌ»ó¹ÝÀÀÀÌ ³ªÅ¸³ª´Â °æ¿ì¿¡´Â Åõ¿©¸¦ ÁßÁöÇϰí ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù. ½ÃÆÇ ÈÄ °æÇè Áß ¡®È£»ê±¸Áõ°¡¿Í Àü½Å¼º Áõ»óÀ» µ¿¹ÝÇÑ ¾à¹° ¹ßÁø(DRESS ; drug rash with eosinophilla and systemic symptoms)'ÀÌ ³ªÅ¸³µ´Ù
8) °£Àå : ´Ù¸¥ ¸¶Å©·Î¶óÀ̵å°è Ç×»ý¹°Áú°ú ¸¶Âù°¡Áö·Î µå¹°°Ô Ȳ´ÞÀ» µ¿¹ÝÇϰųª ¶Ç´Â µ¿¹ÝÇÏÁö ¾Ê´Â °£¼¼Æ÷¼º ¶Ç´Â ´ãÁó¿ïü¼º °£¿°, °£È¿¼ÒÄ¡ÀÇ Áõ°¡¸¦ Æ÷ÇÔÇÑ °£±â´É Àå¾Ö°¡ ³ªÅ¸³µ´Ù´Â º¸°í°¡ ÀÖ´Ù. ÀÌ·¯ÇÑ °£±â´ÉÀå¾Ö´Â ÁßÁõÀÏ ¼ö ÀÖÀ¸¸ç, ´ëü·Î °¡¿ªÀûÀÌ´Ù. ¸î¸î °æ¿ì, »ç¸Á(fatal outcome)À» µ¿¹ÝÇÑ °£ºÎÀüÀÌ º¸°íµÈ ¹Ù ÀÖÀ¸¸ç, ÀÌ´Â ´ëü·Î ÁßÁõÀÇ ±âÀúÁúȯ ¹×/¶Ç´Â º´¿ëÅõ¿©µÈ ¾àÁ¦¿Í °ü·ÃÀÌ ÀÖ¾ú´Ù. Àü°Ý¼º°£¿°, AST, ALT, ¥ã-GTP, LDH, ALP »ó½Â, ÃÑ ºô¸®·çºó Áõ°¡ µîÀ» µ¿¹ÝÇÑ °£±â´ÉÀå¾Ö, Ȳ´Þ, °£ºÎÀüÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î °üÂûÀ» ÃæºÐÈ÷ Çϰí, ½Ä¿åºÎÁø, Ȳ´Þ, ÁøÇÑ»öÀÇ ´¢, °¡·Á¿òÁõ, ¶Ç´Â º¹ºÎ¾ÐÅë µî°ú °°Àº °£¿°ÀÇ Áõ»ó°ú ¡Èİ¡ ³ªÅ¸³¯ °æ¿ì Åõ¿©¸¦ ÁßÁöÇϰí ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù.
9) ½ÅÀå : µå¹°°Ô Ç÷ûũ·¹¾ÆÆ¼´Ñ »ó½ÂÀÌ ÀϾ´Ù´Â º¸°í°¡ ÀÖÀ¸³ª, ÀÌ ¾à°úÀÇ °ü·Ã ¿©ºÎ´Â ¹àÇôÁöÁö ¾Ê¾Ò´Ù. µå¹°°Ô º¹¿ë·®ÀÌ ¸¹À» ¶§ BUNÀÌ »ó½ÂÇÑ´Ù´Â º¸°í°¡ ÀÖ´Ù. °£Áú¼º ½Å¿°, ½ÅºÎÀü, ÃéÀå¿° µîÀÌ º¸°íµÇ¾ú´Ù. ±ÙÀ°Åë, ¹«·Â°¨, CPK »ó½Â, Ç÷Áß ¹× ¿äÁß ¹Ì¿À±Û·Îºó »ó½ÂÀ» Ư¡À¸·Î Çϴ Ⱦ¹®±ÙÀ¶ÇØÁõÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î °üÂûÀ» ÃæºÐÈ÷ ½Ç½ÃÇϰí ÀÌ»ó¹ÝÀÀÀÌ ³ªÅ¸³ª´Â °æ¿ì¿¡´Â Åõ¿©¸¦ ÁßÁöÇϰí ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÏ´Â µî Ⱦ¹®±ÙÀ¶ÇØÁõ¿¡ ÀÇÇÑ ±Þ¼º ½ÅºÎÀüÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î ÁÖÀÇÇÑ´Ù. ÇÌ´¢ µîÀÇ Áõ»óÀ̳ª Ç÷ûũ·¹¾ÆÆ¼´ÑÄ¡ »ó½Â µî ½Å±â´É ÀúÇϰ¡ ³ªÅ¸³ª´Â °æ¿ì¿¡´Â Åõ¿©¸¦ ÁßÁöÇϰí ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù.
10) ±Õ±³´ëÁõ : µå¹°°Ô ¼³¿°, ±¸³»¿°, ±¸°Äµð´ÙÁõÀÌ ³ªÅ¸³µ´Ù´Â º¸°í°¡ ÀÖ´Ù.
11) ¼øÈ¯±â°è : ´Ù¸¥ ¸¶Å©·Î¶óÀ̵å°è¿Í °°ÀÌ QT¿¬Àå, ½É½Ç¼ººó¸Æ, Torsades de pointes°¡ µå¹°°Ô º¸°íµÇ¾ú´Ù.
12) ±âŸ : µå¹°°Ô ±Çۨ, µÎÅë, ¹Ì°¢µµÂø, °¡¿ªÀûÀΠû°¢»ó½Ç, À̻󰨰¢Áõ, °üÀýÅë, ±ÙÀ°Åë, Èİ¢Àå¾Ö°¡ ³ªÅ¸³µ´Ù´Â º¸°í°¡ ÀÖ´Ù. À̸í, û°¢Àå¾ÖÀÎ °æ¿ì ÀϹÝÀûÀ¸·Î Åõ¿©¸¦ Áß´ÜÇÏ¸é °¨¼ÒµÉ ¼ö ÀÖÀ¸³ª Åõ¿© ¿¬Àå±â°£ µ¿¾È 1ÀÏ 1g ÀÌ»ó Åõ¿© ½Ã ´Ù½Ã ³ªÅ¸³¯ ¼ö ÀÖ´Ù. °æ±¸ÀúÇ÷´ç¾à¹° ¶Ç´Â Àν¶¸°À» Åõ¿© ¹Þ´Â ȯÀÚ¿¡°Ô¼ µå¹°°Ô ÀúÇ÷´çÁõÀÌ ³ªÅ¸³µ´Ù´Â º¸°í°¡ ÀÖ´Ù. ½ÃÆÇ ÈÄ °æÇè Áß È¾¹®±ÙÀ¶ÇØÁõÀÌ º¸°íµÇ¾ú´Ù. ÀϺΠȾ¹®±ÙÀ¶ÇØÁõÀÇ º¸°í¿¡¼, Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀº ½ºÅ¸Æ¾°è, ÇǺ극ÀÌÆ®°è, ÄÝŰ½Å, ¶Ç´Â ¾Ë·ÎǪ¸®³î°ú º´¿ëÅõ¿© µÇ¾ú¾ú´Ù.
13) ÄÝŰ½Å°ú º´¿ëÅõ¿©½Ã, ƯÈ÷ °í·ÉÀÚ¿Í ÀϺΠ½ÅºÎÀüȯÀÚ¿¡°Ô ÄÝŰ½Å µ¶¼ºÀÌ ³ªÅ¸³µ´Ù´Â ½ÃÆÇ ÈÄ º¸°í°¡ ÀÖ¾ú´Ù. À̵é ȯÀÚ Áß ÀϺο¡¼´Â »ç¸Á»ç·Êµµ º¸°íµÇ¾ú´Ù. ÀÌ ¾à°ú ÄÝŰ½ÅÀº º´¿ëÅõ¿© ÇÏÁö ¾Ê´Â´Ù.
14) ÇÑÁ¤µÈ Àοø¼öÀÇ ¼Ò¾Æ AIDSȯÀÚÀÇ ¸¶ÀÌÄÚ¹ÚÅ׸®¾Æ °¨¿°Áõ¿¡ ÀÌ ¾àÀ» Åõ¿©ÇÏ¿´À»¶§ ȯÀÚÀÇ º´¹ß »óÅ¿¡ ±âÀÎÇÑ ÀÌ»ó¹ÝÀÀÀ» Á¦¿ÜÇÑ °¡Àå ÈçÇÏ°Ô º¸°íµÈ ÀÌ»ó¹ÝÀÀÀº À̸í, ³Ã», ±¸Åä, ±¸¿ª, º¹Åë, Àڹݼº ¹ßÁø, ÃéÀå¿° ¹× ¾Æ¹Ð¶ó¾ÆÁ¦ Áõ°¡À̾ú´Ù. ƯÁ¤ °Ë»ç¿¡¼ ½É°¢ÇÏ°Ô ºñÁ¤»óÀûÀÎ ¼öÁØ (»óÇÑ ¶ÇÇÑ ÇÏÇÑÄ¡)ÀÇ °Ë»çÄ¡¸¦ ºÐ¼®ÇÏ¿´À»¶§ ÀÌ ¾à <15mg/kg/ÀÏÀ» Åõ¿©ÇÑ 1¸íÀÇ ¼Ò¾Æ AIDSȯÀÚ¿¡¼ ½É°¢ÇÏ°Ô ºñÁ¤»óÀûÀÎ(»ó½ÂµÈ) ÃѺô¸®·çºóÄ¡¸¦ ³ªÅ¸³ÂÀ¸¸ç ÀÌ ¾à 15 ÀÌ»ó <25mg/kg/ÀÏÀ» Åõ¿©ÇÑ È¯ÀÚ¿¡¼ °¢°¢ 1¸í¾¿ ½É°¢ÇÏ°Ô ºñÁ¤»óÀûÀÎ SGPT, BUN ¹× ½É°¢ÇÏ°Ô °¨¼ÒµÈ Ç÷¼ÒÆÇ¼ö¸¦ ³ªÅ¸³Â´Ù. ÀÌ ¾à ÃÖ°í¿ë·® (¡Â25mg/kg/ÀÏ)À» Åõ¿©ÇÑ È¯ÀÚ¿¡¼ ½É°¢ÇÏ°Ô ºñÁ¤»óÀûÀÎ ¼öÄ¡´Â º¸°íµÇÁö ¾Ê¾Ò´Ù(°ÇÁ¶½Ã·´Á¦¿¡ ÇÑÇÔ).
15) ¸é¿ª±â´ÉÀÌ ÀúÇÏµÈ È¯ÀÚ¿¡¼ ƯÁ¤ °Ë»ç¿¡¼ ½É°¢ÇÏ°Ô ºñÁ¤»óÀûÀÎ ¼öÁØ(»óÇÑ ¶ÇÇÑ ÇÏÇÑÄ¡)ÀÇ °Ë»çÄ¡¸¦ ºÐ¼®ÇÏ¿´À» ¶§ 1ÀÏ ¾à 1000mgÀ» Åõ¿©ÇÑ È¯ÀÚÀÇ ¾à 2-3%¿¡¼ AST ¹× ALT°¡ ½É°¢ÇÏ°Ô ºñÁ¤»óÀûÀÎ ¼öÁØÀ¸·Î »ó½ÂÇÏ°í ¹éÇ÷±¸¿Í Ç÷¼ÒÆÇ¼ö°¡ ºñÁ¤»óÀûÀ¸·Î ³·¾Ò´Ù. ¶ÇÇÑ ´õ ÀûÀº ¼öÀÇ È¯ÀÚ¿¡¼ BUNÀÌ »ó½ÂÇÏ¿´´Ù (ÀϹÝÁ¤Á¦¿¡ ÇÑÇÔ).
16) Ŭ·¡¸®Æ®·Î¸¶À̽Űú °ü·ÃÀÌ ÀÖÀ» ¼ö ÀÖ´Ù°í ÆÇ´ÜµÇ´Â ÀÌ»ó¹ÝÀÀÀ» Àü½ÅÁ¶Á÷ºÐ·ù¿Í ´ÙÀ½°ú °°Àº ºóµµºÐ·ù¿¡ µû¶ó ¾Æ·¡ Ç¥·Î ³ªÅ¸³»¾ú´Ù: ¸Å¿ì ÈçÈ÷(¡Ã 1/10), ÈçÈ÷(¡Ã 1/100~< 1/10), µå¹°°Ô(¡Ã 1/1000~1/100), ±×¸®°í not known(½ÃÆÇÈÄÁ¶»ç¿¡¼ ³ªÅ¸³ ÀÌ»ó¹ÝÀÀÀ¸·Î µ¥ÀÌÅͷκÎÅÍ ÃßÁ¤ÇÒ ¼ö ¾øÀ½). °¢ Ä¿¡¼ ÀÌ»ó¹ÝÀÀÀº Áß´ëÇÔÀÌ Æò°¡°¡´ÉÇÒ °æ¿ì Áß´ëÇÔÀÌ Å« ¼ø¼ºÎÅÍ ±âÀçÇÏ¿´´Ù.
 
  
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Æ®¸®¾ÆÁ¹¶÷°ú ¾ËÇÁ¶óÁ¹¶÷À» Æ÷ÇÔÇÑ, CYP3A·Î ´ë»çµÇ´Â ´Ù¸¥ º¥Á¶µð¾ÆÁ¦ÇÉ·ùµé¿¡µµ °°Àº ÁÖÀÇ»çÇ×ÀÌ Àû¿ëµÈ´Ù. CYP3A¿¡ ÀÇÇØ ´ë»çµÇÁö ¾Ê´Â º¥Á¶µð¾ÆÁ¦ÇÉ·ùµé (Å׸¶Á¦ÆÊ, ´ÏÆ®¶óÁ¦ÆÊ, ·Î¶óÁ¦ÆÊ)¿¡´Â, Ŭ·¡¸®Æ®·Î¸¶À̽ŰúÀÇ »óÈ£ÀÛ¿ëÀº ÀÓ»óÀûÀ¸·Î Áß¿äÇÏÁö ¾Ê´Ù.
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½ÃÆÇ ÈÄ Á¶»ç¿¡¼ µð¼ÒÇǶó¹Ìµå¿Í º´¿ëÅõ¿© ÇÏ´Â °æ¿ì ÀúÇ÷´çÁõÀÌ ¹ß»ýÇß´Ù´Â º¸°í°¡ ÀÖ¾ú´Ù. µû¶ó¼ Åõ¿© Áß Ç÷´çÀ» ¸ð´ÏÅ͸µ ÇÏ¿©¾ß ÇÑ´Ù.
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5) µð°î½ÅÀº À¯Ãâ¿î¹ÝÀÚ(efflux transporter)ÀÎ P-glycoprotein(Pgp)ÀÇ ±âÁú·Î ¿©°ÜÁø´Ù. Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀº PgpÀ» ÀúÇØÇÏ´Â °ÍÀ¸·Î ¾Ë·ÁÁ®ÀÖ´Ù. Ŭ·¡¸®Æ®·Î¸¶À̽Űú µð°î½ÅÀ» º´¿ë Åõ¿©ÇßÀ» ¶§, Ŭ·¡¸®Æ®·Î¸¶À̽ſ¡ ÀÇÇÑ PgpÀÇ ÀúÇØ´Â µð°î½Å ¼öÄ¡ÀÇ »ó½ÂÀ» ¾ß±âÇÑ´Ù.
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6) HIV °¨¿° ¼ºÀΠȯÀÚ¿¡°Ô ÀÌ ¾à°ú ÁöµµºÎµòÀ» °æ±¸·Î º´¿ëÅõ¿©ÇÏ´Â °æ¿ì¿¡´Â ÁöµµºÎµòÀÇ Èí¼ö¸¦ ¹æÇØÇÏ¿© ÁöµµºÎµò ³óµµ Ç×Á¤»óŸ¦ ÀúÇϽÃŲ´Ù. ÀÌ ¾à°ú ÁöµµºÎµò ¶Ç´Â µðµ¥¿Á½ÃÀ̳ë½ÅÀ» º´¿ëÅõ¿©ÇÑ ¼Ò¾Æ HIV ȯÀÚ¿¡¼´Â ÀÌ·¯ÇÑ »óÈ£ÀÛ¿ëÀÌ °üÂûµÇÁö ¾Ê¾Ò´Ù. ¼ºÀÎ HIV ȯÀÚ¿¡¼´Â µð´Ù³ë½ÅÀÇ ¾àµ¿Çп¡ ´ëÇØ Åë°èÀûÀ¸·Î À¯ÀÇÇÑ ¿µÇâÀº ¾ø¾ú´Ù.(°ÇÁ¶½Ã·´Á¦¿¡ ÇÑÇÔ)
7) HIV °¨¿° ¼ºÀΠȯÀÚ¿¡°Ô ÀÌ ¾à°ú ÁöµµºÎµòÀ» °æ±¸·Î º´¿ëÅõ¿©ÇÏ´Â °æ¿ì¿¡´Â ÁöµµºÎµòÀÇ Èí¼ö¸¦ ¹æÇØÇÏ¿© ÁöµµºÎµò ³óµµ Ç×Á¤»óŸ¦ ÀúÇϽÃŲ´Ù. ÀÌ ¾àÀº µ¿½Ã Åõ¿©ÇÑ °æ±¸ ÁöµµºÎµòÀÇ Èí¼ö¸¦ ¹æÇØÇÏ´Â °ÍÀ¸·Î ³ªÅ¸³µÀ¸¸ç ÀÌ ¾à°ú ÁöµµºÎµòÀÇ Åõ¿© °£°ÝÀ» µÎ¸é ÀÌ »óÈ£ÀÛ¿ëÀ» ´ëºÎºÐ ÇÇÇÒ ¼ö ÀÖ´Ù. ÀÌ ¾à°ú ÁöµµºÎµò ¶Ç´Â µðµ¥¿Á½ÃÀ̳ë½ÅÀ» º´¿ëÅõ¿©ÇÑ ¼Ò¾Æ HIV ȯÀÚ¿¡¼´Â ÀÌ·¯ÇÑ »óÈ£ÀÛ¿ëÀÌ °üÂûµÇÁö ¾Ê¾Ò´Ù. ¼ºÀÎ HIV ȯÀÚ¿¡¼´Â µð´Ù³ë½ÅÀÇ ¾àµ¿Çп¡ ´ëÇØ Åë°èÀûÀ¸·Î À¯ÀÇÇÑ ¿µÇâÀº ¾ø¾ú´Ù.(¼¹æÁ¤ ¹× ÀϹÝÁ¤Á¦¿¡ ÇÑÇÔ)
8) ¶õ¼ÒÇÁ¶óÁ¹°ú º´¿ëÅõ¿©ÇÏ´Â °æ¿ì¿¡´Â Ç÷û ³óµµ°¡ °æ¹ÌÇÏ°Ô »ó½ÂÇÑ´Ù´Â º¸°í°¡ ÇÑ °ÇÀÌ ÀÖ¾úÀ¸³ª, ¿ë·® Á¶Àý µî¿¡ ´ëÇÑ °á°ú¸¦ µÞ¹ÞħÇÒ¸¸ÇÑ ÀÚ·á´Â ¾ø´Ù. °Ç°ÇÑ ¼ºÀο¡ ´ëÇØ 8½Ã°£¸¶´Ù Ŭ·¡¸®Æ®·Î¸¶À̽Š500mg°ú 1ÀÏ 1ȸ ¿À¸ÞÇÁ¶óÁ¹ 40mgÀ» º´¿ëÅõ¿© ÇÏ¿´À» ¶§ Ç×Á¤»óÅ ¿À¸ÞÇÁ¶óÁ¹ÀÇ Cmax, AUC0-24¿Í T1/2ÀÌ °¢°¢ 30%, 89%, 34% Áõ°¡Çß´Ù. Æò±Õ 24½Ã°£ ³» À§Àå pH°¡ ¿À¸ÞÇÁ¶óÁ¹ ´Üµ¶Åõ¿© ½Ã´Â 5.2À̰í ÀÌ ¾à°ú º´¿ë Åõ¿©ÇßÀ» ¶§´Â 5.7À̾ú´Ù.
9) ¸®ÆÄºÎƾ ¶Ç´Â ¸®ÆÊÇɰú º´¿ëÅõ¿©ÇÏ´Â °æ¿ì Ŭ·¡¸®Æ®·Î¸¶À̽г󵵰¡ °¨¼ÒµÈ´Ù. Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀº ¸®ÆÄºÎƾÀÇ Ç÷û ¹× Á¶Á÷ ³» ³óµµ¸¦ Áõ°¡½ÃÄÑ µ¶¼ºÀ» Áõ°¡½Ãų ¼ö ÀÖ°í, Æ÷µµ¸·¿°ÀÇ À§Ç輺À» Áõ°¡¸¦ ÃÊ·¡ÇÏ¿´´Ù.
10) ¸®Å䳪ºñ¸£¿Í º´¿ëÅõ¿©ÇÏ´Â °æ¿ì¿¡´Â Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ ´ë»ç¸¦ ÇöÀúÈ÷ ¹æÇØÇÑ´Ù´Â ¾à¹°µ¿·ÂÇÐ ¿¬±¸º¸°í°¡ ÀÖ´Ù. Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ Ä¡·á¿µ¿ªÀÌ ³Ð±â ¶§¹®¿¡ ½Å±â´ÉÀÌ Á¤»óÀΠȯÀÚ¿¡ ´ëÇÏ¿©´Â ¿ë·®°¨¼Ò°¡ ÇÊ¿äÇÏÁö ¾ÊÀ¸³ª ½ÅºÎÀü ȯÀÚ´Â ´ÙÀ½°ú °°ÀÌ ¿ë·®Á¶ÀýÀÌ ÇÊ¿äÇÏ´Ù. Áï Å©·¹¾ÆÆ¼´Ñû¼ÒÀ²ÀÌ 30¢¦60mL/minÀΠȯÀÚ´Â ¿ë·®À» 50% ÁÙ¿©¼ »ç¿ëÇϰí, Å©·¹¾ÆÆ¼´Ñû¼ÒÀ²ÀÌ 30mL/min ÀÌÇÏÀΠȯÀÚ´Â 75% ÁÙ¿©¼ »ç¿ëÇÑ´Ù. ¸®Å䳪ºñ¸£¿Í º´¿ëÅõ¿© ½Ã Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ ¿ë·®ÀÌ 1g/ÀÏÀ» ÃʰúÇÏÁö ¾Ê´Â´Ù. Àε𳪺ñ¸£¿Í º´¿ëÅõ¿© ½Ã¿¡´Â ´ë»ç»óÈ£ÀÛ¿ëÀÌ ³ªÅ¸³´Ù´Â º¸°í°¡ ÀÖ´Ù. ±×·¯³ª ½Å±â´ÉÀÌ Á¤»óÀΠȯÀÚ¿¡ ´ëÇØ¼´Â ¿ë·®Á¶ÀýÀÌ ÇÊ¿äÇÏÁö ¾Ê´Ù. (°ÇÁ¶½Ã·´Á¦ ¹× ÀϹÝÁ¤Á¦¿¡ ÇÑÇÔ)
11) ¸®Å䳪ºñ¸£¿Í º´¿ëÅõ¿©ÇÏ´Â °æ¿ì¿¡´Â Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ ´ë»ç¸¦ ÇöÀúÈ÷ ¹æÇØÇÑ´Ù´Â ¾à¹°µ¿·ÂÇÐ ¿¬±¸º¸°í°¡ ÀÖ´Ù. Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ Ä¡·á¿µ¿ªÀÌ ³Ð±â ¶§¹®¿¡ ½Å±â´ÉÀÌ Á¤»óÀΠȯÀÚ¿¡ ´ëÇÏ¿©´Â ¿ë·®°¨¼Ò°¡ ÇÊ¿äÇÏÁö ¾ÊÀ¸³ª ½ÅºÎÀü ȯÀÚ´Â ´ÙÀ½°ú °°ÀÌ ¿ë·®Á¶ÀýÀÌ ÇÊ¿äÇÏ´Ù. Áï Å©·¹¾ÆÆ¼´Ñû¼ÒÀ²ÀÌ 30¢¦60mL/minÀΠȯÀÚ´Â ¿ë·®À» 50% ÁÙ¿©¼ ÃÖ´ë¿ë·®ÀÎ 1ÀÏ Å¬·¡¸®Æ®·Î¸¶À̽м¹æÇü Á¤Á¦ 1Á¤À» »ç¿ëÇϰí, Å©·¹¾ÆÆ¼´Ñû¼ÒÀ²ÀÌ 30mL/min ÀÌÇÏÀΠȯÀڴ Ŭ·¡¸®Æ®·Î¸¶À̽м¹æÇü Á¤Á¦´Â ¿ë·®°¨¼Ò°¡ ºÒ°¡´ÉÇϱ⠶§¹®¿¡ »ç¿ëÇÏÁö ¾ÊÀ¸¸ç Ŭ·¡¸®Æ®·Î¸¶À̽мӹæÇü Á¤Á¦¸¦ »ç¿ëÇÑ´Ù. ¸®Å䳪ºñ¸£¿Í º´¿ëÅõ¿© ½Ã Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ ¿ë·®ÀÌ 1g/ÀÏÀ» ÃʰúÇÏÁö ¾Ê´Â´Ù. Àε𳪺ñ¸£¿Í º´¿ëÅõ¿© ½Ã¿¡´Â ´ë»ç»óÈ£ÀÛ¿ëÀÌ ³ªÅ¸³´Ù´Â º¸°í°¡ ÀÖ´Ù. ±×·¯³ª ½Å±â´ÉÀÌ Á¤»óÀΠȯÀÚ¿¡ ´ëÇØ¼´Â ¿ë·®Á¶ÀýÀÌ ÇÊ¿äÇÏÁö ¾Ê´Ù(¼¹æÁ¤¿¡ ÇÑÇÔ).
½ÅºÎÀü ȯÀÚ¿¡¼ ¸®Å䳪ºñ¸£¸¦ ´Ù¸¥ HIV ÇÁ·ÎÅ×¾ÆÁ¦ ¾ïÁ¦Á¦(¾ÆÅ¸ÀÚ³ªºñ¸£, »çÄû³ªºñ¸£ Æ÷ÇÔ)¿¡ ´ëÇÑ ¾àµ¿ÇÐ °ÈÁ¦(pharmacokinetic enhancer)·Î¼ »ç¿ëÇÒ °æ¿ì, À¯»çÇÑ ¿ë·®Á¶Á¤À» °í·ÁÇÏ¿©¾ß ÇÑ´Ù.
12) Ÿũ·Î¸®¹«½º¿Í º´¿ëÅõ¿©ÇÏ´Â °æ¿ì¿¡´Â Ÿũ·Î¸®¹«½ºÀÇ Ç÷Àå³óµµ¸¦ Áõ°¡½ÃÄѼ µ¶¼ºÀ» Áõ°¡½Ãų ¼ö ÀÖ´Ù.
13) ¾Æ¸ñ½Ã½Ç¸° ¹×(¶Ç´Â) ¿À¸ÞÇÁ¶óÁ¹°ú º´¿ëÅõ¿©ÇÏ´Â °æ¿ì¿¡´Â °¢ ¾à¹°¿¡ ´ëÇÑ »ç¿ë»óÀÇ ÁÖÀÇ»çÇ×, ¾à¹°»óÈ£ÀÛ¿ë µîÀ» Âü°íÇÑ´Ù.
14) Å©·¹¾ÆÆ¼´Ñû¼ÒÀ²ÀÌ 25mL/min ÀÌÇÏÀΠȯÀÚ¿¡°Ô ±¸¿¬»ê¶ó´ÏƼµò ºñ½º¹«½º¿ä¹ý°ú º´¿ëÇÏ´Â °ÍÀº ¹Ù¶÷Á÷ÇÏÁö ¾Ê´Ù. ±Þ¼ºÆ÷¸£ÇǸ°ÁõÀÇ º´·ÂÀÌ Àִ ȯÀÚ¿¡°Ô´Â ±¸¿¬»ê¶ó´ÏƼµò ºñ½º¹«½º¿Í º´¿ëÇÏÁö ¾Ê´Â´Ù. ±¸¿¬»ê¶ó´ÏƼµòºñ½º¹«½º¿Í º´¿ëÅõ¿© ½Ã Ç÷Áß ¶ó´ÏƼµòÀÇ ³óµµ´Â 57% »ó½Â, Ç÷Áß ºñ½º¹«½º ÃÖÀú ³óµµ´Â 48% »ó½ÂÇßÀ¸¸ç 14-ÇÏÀ̵å·Ï½Ã-Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ ³ó µµ´Â 31% Áõ°¡ÇßÀ¸³ª ÀÌ´Â ÀÓ»óÀû Àǹ̰¡ ¾ø´Ù.
15) Ŭ·¡¸®Æ®·Î¸¶À̽Űú ÀÌÆ®¶óÄÚ³ªÁ¹Àº CYP3AÀÇ ±âÁúÀÌ¸é¼ ¶ÇÇÑ ÀúÇØÁ¦À̸ç, ¾ç¹æÇ⠾๰ »óÈ£ÀÛ¿ëÀ» ÀÏÀ¸Å²´Ù. Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀº ÀÌÆ®¶óÄÚ³ªÁ¹ÀÇ Ç÷Àå ³óµµ¸¦ Áõ°¡½Ã۸ç, ÀÌÆ®¶óÄÚ³ªÁ¹Àº Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ Ç÷Àå ³óµµ¸¦ Áõ°¡½ÃŲ´Ù. ÀÌÆ®¶óÄÚ³ªÁ¹°ú Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀ» º´¿ë Åõ¿©¹Þ´Â ȯÀÚ´Â ¾à¹°ÇÐÀû Ȱ¼ºÀÇ Áõ°¡ ¶Ç´Â ¿¬ÀåÀÇ Â¡ÈÄ¿¡ ´ëÇØ ÁÖÀÇ ±í°Ô ¸ð´ÏÅ͸µ µÇ¾î¾ß ÇÑ´Ù.
16) °æ±¸¿ë Ç÷´ç°ÇÏÁ¦(¿¹: ¼³Æ÷´ÒÀ¯¸®¾Æ°è ¾à¹°) ±×¸®°í/¶Ç´Â Àν¶¸°°ú º´¿ë Åõ¿© ÇÏ´Â °æ¿ì¿¡´Â ÇöÀúÇÏ°Ô ÀúÇ÷´çÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù. ³ªÅ×±Û¸®³ªÀ̵å, ÇÇ¿À±Û¸®Å¸Á¸, ·¹ÆÄ±Û¸®³ªÀ̵å, ·ÎÁö±Û¸®Å¸Á¸°ú º´¿ë½Ã, Ŭ·¡¸®Æ®·Î¸¶À̽ſ¡ ÀÇÇØ CYP3A È¿¼Ò°¡ ÀúÇØµÉ ¼ö ÀÖÀ¸¸ç, ÀúÇ÷´çÀ» ÀÏÀ¸Å³ ¼ö ÀÖ´Ù. Ç÷´çÀ» ÁÖÀDZí°Ô ¸ð´ÏÅ͸µ Çϵµ·Ï ÇÑ´Ù.
17) Æç·ÎµðÇɰú º´¿ë Åõ¿©ÇÏ´Â °æ¿ì¿¡´Â ¾à¹°¹è¼³ÀÌ Áö¿¬µÇ¾î ¾à¹°È¿°ú°¡ »ó½ÂµÉ ¼ö ÀÖÀ¸¹Ç·Î ÁÖÀÇÇÑ´Ù.
18) º£ÇÁ¸®µô, ¹ÌÁ¹¶ó½ºÆ¾, ¿¡¹Ù½ºÆ¾°ú º´¿ë Åõ¿©ÇÏ´Â °æ¿ì¿¡´Â ½É½Ç¿îµ¿, ƯÈ÷ Torsades de pointes Àå¾ÖÀÇ À§ÇèÀÌ ÀÖ´Ù.
19) Ä«º£°ñ¸°, Æä¸£°ñ¸®µå¿Í º´¿ë Åõ¿©ÇÏ´Â °æ¿ì¿¡´Â °ú´ÙÅõ¿© ½Ã ÀÛ¿ëÀÌ Áõ°¡Çϰí Ç÷Àå³óµµ°¡ Áõ°¡µÉ ¼ö ÀÖ´Ù.
20) ÅçÅͷεò°ú º´¿ë Åõ¿©ÇÏ´Â °æ¿ì ÅçÅͷεòÀ» ½ÅÁø´ë»ç°¡ ´À¸° ȯÀÚ¿¡°Ô °ú´ÙÅõ¿© ½Ã ÅçÅͷεòÀÇ Ç÷û³óµµ°¡ Áõ°¡ÇÒ ¼ö ÀÖ´Ù. ÅçÅͷεòÀÇ ÁÖ¿ä ´ë»ç °æ·Î´Â ½ÃÅäÅ©·Ò P450ÀÇ 2D6 isoform(CYP2D6)À̳ª, CYP2D6°¡ °á¿©µÈ Áý´Ü¿¡¼´Â CYP3A·Î ´ë»çµÇ´Â °ÍÀ¸·Î È®ÀεǾú´Ù. ÀÌ·¯ÇÑ Áý´Ü¿¡¼ CYP3A¸¦ ÀúÇØÇϸé, ÅçÅͷεò Ç÷û³óµµÀÇ Áß´ëÇÑ »ó½ÂÀÌ ¾ß±âµÇ¾ú´Ù. CYP2D6¿¡ ´ëÇØ ¾àÇÑ ´ë»ç´ÉÀ» °¡Áø Áý´Ü(CYP2D6 poor metabolizer)¿¡°Ô Ŭ·¡¸®Æ®·Î¸¶À̽Űú °°Àº CYP3A ÀúÇØÁ¦¸¦ º´¿ëÇÏ´Â °æ¿ì, ÅçÅͷεòÀÇ ¿ë·® °¨¼Ò°¡ ¿ä±¸µÈ´Ù.
21) ÇÒ·ÎÆÇÆ®¸°°ú º´¿ë Åõ¿©ÇÏ´Â °æ¿ì¿¡´Â ½É½Ç¿îµ¿, ƯÈ÷ Torsades de pointes Àå¾ÖÀÇ À§ÇèÀÌ ÀÖÀ¸¹Ç·Î °¡´ÉÇϸé QT °Ë»ç¸¦ ¹Ì¸® ½Ç½ÃÇϰųª ½ÉÀüµµ¸¦ ¸ð´ÏÅ͸µ °¨µ¶ÇÑ´Ù.
22) INR(±¹Á¦Á¤»óȺñÀ²)ÀÇ º¯È : ÀÌ ¾àÀ» Æ÷ÇÔÇÑ Ç×»ý¹°ÁúÀ» Ç×ÀÀ°íÁ¦¿Í µ¿½Ã¿¡ Åõ¿© ¹ÞÀº ȯÀÚ¿¡¼ Ç×ÀÀ°í Ȱ¼ºÀÇ Áõ°¡°¡ º¸°íµÇ¾ú´Ù. °¨¿°¼ºÁúȯ(±×¸®°í ¿°Áõ¼º °úÁ¤À» µ¿¹ÝÇÑ), ȯÀÚÀÇ ¿¬·É°ú ÀϹÝÀûÀÎ »óÅ´ À§Çè¿ä¼Ò°¡ µÈ´Ù. ÀÌ ¾à°ú ¿ÍÆÄ¸°À» º´¿ëÅõ¿© ÇßÀ» ¶§, ½É°¢ÇÑ ÃâÇ÷ÀÇ À§ÇèÀÌ ÀÖ°í, INR°ú ÇÁ·ÎÆ®·Òºó ½Ã°£ÀÇ ÇöÀúÇÑ Áõ°¡°¡ ÀÖ¾ú´Ù. ÀÌ ¾à°ú °æ±¸¿ë Ç×ÀÀ°íÁ¦¸¦ º´¿ëÅõ¿©ÇÒ ¶§´Â INR°ú ÇÁ·ÎÆ®·Òºó ½Ã°£À» ÀÚÁÖ ¸ð´ÏÅ͸µÇØ¾ß ÇÑ´Ù. ÇÊ¿äÇÑ °æ¿ì °æ±¸¿ë Ç×ÀÀ°íÁ¦ÀÇ ¿ë·®À» ÀûÀýÈ÷ Á¶ÀýÇÑ´Ù. Ç×»ý¹°ÁúÀÇ ÀϺΠÁ¾·ùµé, ƯÈ÷ Ç÷ç¿À·ÎÄû³î·Ð, ¸¶Å©·Î¶óÀ̵å, »çÀÌŬ¸°, ÄÚÆ®¸®¸ñ»çÁ¹°ú ÀϺΠ¼¼ÆÈ·Î½ºÆ÷¸°ÀÇ °æ¿ì´Â ´õ ½ÉÇÏ´Ù.
23) Ä®½·±æÇ×Á¦(´ÏÆäµðÇÉ, ¿°»êº£¶óÆÄ¹Ð µî)¿Í º´¿ë ½Ã ÁÖÀÇÇÑ´Ù. Ŭ·¡¸®Æ®·Î¸¶À̽Űú º£¶óÆÄ¹ÐÀ» º´¿ëÇϴ ȯÀÚ¿¡°Ô¼ ÀúÇ÷¾Ð, ¼¸Æ¼º ºÎÁ¤¸Æ ¹× À¯»êÁõ (lactic acidosis)ÀÌ °üÂûµÇ¾ú´Ù.
24) °Ç°ÇÑ Áö¿øÀÚ¿¡ ´ëÇØ ÇÁ·çÄÚ³ªÁ¹ 200mg 1ÀÏ 1ȸ¿Í Ŭ·¡¸®Æ®·Î¸¶À̽Š500mg 1ÀÏ 2ȸ º´¿ë Åõ¿©ÇßÀ»¶§ ÀÌ ¾àÀÇ Æò±Õ Ç×Á¤»óÅ Cmin¿Í AUC°¡ °¢°¢ 33%, 18% Áõ°¡ÇßÀ¸³ª 14-OH-Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ ³óµµ´Â ÇöÀúÇÑ ¿µÇâÀ» ¹ÞÁö ¾Ê¾Ò´Ù. Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ ¿ë·®Á¶ÀýÀº ¿ä±¸µÇÁö ¾Ê´Â´Ù.
25) ÄÝŰ½Å°ú º´¿ëÅõ¿© ½Ã, ƯÈ÷ °í·ÉÀÚ¿Í ÀϺΠ½ÅºÎÀüȯÀÚ¿¡¼ ÄÝŰ½Å µ¶¼ºÀÌ º¸°íµÇ¾úÀ¸¸ç ÀϺο¡¼´Â »ç¸Á»ç·Êµµ º¸°íµÇ¾ú´Ù. ÄÝŰ½ÅÀº CYP3A ¹× À¯Ãâ¿î¹ÝÀÚ(efflux transporter)ÀÎ P-glycoprotein(Pgp)ÀÇ ±âÁúÀÌ´Ù. Ŭ·¡¸®Æ®·Î¸¶À̽Űú ´Ù¸¥ ¸¶Å©·Î¶óÀ̵å°è Ç×»ý¹°ÁúÀº CYP3A ¹× Pgp¸¦ ¾ïÁ¦ÇÏ¿© ÄÝŰ½Å¿¡ ´ëÇÑ ³ëÃâÀÌ Áõ°¡µÉ ¼ö ÀÖÀ¸¹Ç·Î ÄÝŰ½Å°ú ÀÌ ¾àÀ» º´¿ëÅõ¿©Çؼ´Â ¾È µÈ´Ù.
26) Ŭ·¡¸®Æ®·Î¸¶À̽Űú ¾ÆÅ¸ÀÚ³ªºñ¸£´Â CYP3AÀÇ ±âÁúÀÌ¸é¼ ¶ÇÇÑ ÀúÇØÁ¦À̸ç, ¾ç¹æÇâ (bi- directional) ¾à¹°»óÈ£ÀÛ¿ë¿¡ ´ëÇÑ ±Ù°ÅµéÀÌ Á¸ÀçÇÑ´Ù. Ŭ·¡¸®Æ®·Î¸¶À̽Å(500mg 1ÀÏ 2ȸ)°ú ¾ÆÅ¸ÀÚ³ªºñ¸£(400mg 1ÀÏ 1ȸ)¸¦ º´¿ëÅõ¿©Çϸé, Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ ¼öÄ¡´Â 2¹è Áõ°¡Çϸç 14-OH-Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀº 70% °¨¼ÒÇϰí, ¾ÆÅ¸ÀÚ³ªºñ¸£ÀÇ AUC´Â 28% Áõ°¡ÇÑ´Ù. Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ ³ÐÀº Ä¡·á¹üÀ§(therapeutic window)·Î ÀÎÇÏ¿©, Á¤»óÀûÀÎ ½Å±â´ÉÀ» °¡Áø ȯÀÚ¿¡°Ô Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ ¿ë·® °¨¼Ò´Â ¿ä±¸µÇÁö ¾Ê´Â´Ù. ¿Â°ÇÇÑ ½Å±â´É(creatinine clearance 30~60 mL/min)À» °¡Áø ȯÀÚÀÇ °æ¿ì, Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ ¿ë·®Àº 50% ±îÁö °¨¼ÒµÇ¾î¾ß ÇÑ´Ù. Å©·¹¾ÆÅ¸´Ñ Ŭ¸®¾î·±½º(creatinine clearance)°¡ 30 mL/min ¹Ì¸¸ÀΠȯÀÚÀÇ °æ¿ì, Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ ¿ë·®Àº ÀûÀýÇÑ Å¬·¡¸®Æ®·Î¸¶À̽Šó¹æ¿¡ µû¶ó 75% ±îÁö °¨¼ÒµÇ¾î¾ß ÇÑ´Ù. Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ 1ÀÏ ¿ë·®ÀÌ 1000mgÀ» ÃʰúÇÏ´Â °æ¿ì, ÇÁ·ÎÅ×¾ÆÁ¦ ÀúÇØÁ¦¿Í º´¿ëÅõ¿©Çؼ´Â ¾ÈµÈ´Ù.
27) Ŭ·¡¸®Æ®·Î¸¶À̽Űú »çÄû³ªºñ¸£´Â CYP3AÀÇ ±âÁúÀÌ¸é¼ ¶ÇÇÑ ÀúÇØÁ¦À̸ç, ¾ç¹æÇâ (bi-directional) ¾à¹°»óÈ£ÀÛ¿ë¿¡ ´ëÇÑ ±Ù°ÅµéÀÌ Á¸ÀçÇÑ´Ù. °Ç°ÇÑ 12¸íÀÇ Áö¿øÀÚ¸¦ ´ë»óÀ¸·Î Ŭ·¡¸®Æ®·Î¸¶À̽Š(500mg 1ÀÏ 2ȸ)°ú »çÄû³ªºñ¸£ (¿¬Áúĸ½¶ 1200mg 1ÀÏ 3ȸ)¸¦ º´¿ëÅõ¿© ÇÑ °á°ú, »çÄû³ªºñ¸£ÀÇ Ç×Á¤»óÅÂÀÇ AUC ¿Í Cmax ¼öÄ¡´Â ´Üµ¶ Åõ¿© ½Ã º¸´Ù 177% ¹× 187% »ó½ÂÇÏ¿´´Ù. Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ AUC ¿Í Cmax ¼öÄ¡´Â ´Üµ¶ Åõ¿© ½Ã º¸´Ù ¾à 40% »ó½ÂÇÏ¿´´Ù. ½ÃÇè¿¡ »ç¿ëµÈ ¿ë·®/Á¦Çü ¿¡¼ µÎ ¾à¹°ÀÇ ¿ë·®Á¶ÀýÀº ¿ä±¸µÇÁö ¾Ê´Â´Ù. »çÄû³ªºñ¸£ ¿¬Áú ĸ½¶ Á¦ÇüÀ» ÀÌ¿ëÇÑ ¾à¹°»óÈ£ÀÛ¿ë ½ÃÇèÀÇ °á°ú´Â °æÁú ĸ½¶ Á¦ÇüÀ» »ç¿ëÇßÀ» ¶§ÀÇ È¿°ú¸¦ ´ëÇ¥ÇÏÁö ¾Ê´Â´Ù. »çÄû³ªºñ¸£¸¦ ´Üµ¶ Åõ¿©ÇÏ¿© ¼öÇàÇÑ ¾à¹° »óÈ£ÀÛ¿ë ½ÃÇèÀÇ °á°ú´Â, »çÄû³ªºñ¸£/¸®Å䳪ºñ¸£¸¦ Åõ¿©ÇßÀ» ¶§ÀÇ È¿°ú¸¦ ´ëÇ¥ÇÏÁö ¾Ê´Â´Ù. »çÄû³ªºñ¸£¸¦ ¸®Å䳪ºñ¾î¿Í º´¿ëÇÏ¿© Åõ¿©ÇßÀ» ¶§¿¡´Â, ¸®Å䳪ºñ¸£ÀÇ Å¬·¡¸®Æ®·Î¸¶À̽ſ¡ ´ëÇÑ ÀáÀçÀûÀÎ ¿µÇâ¿¡ ´ëÇÑ °í·Á¸¦ ÇÏ¿©¾ß ÇÑ´Ù.
28) Ŭ·¡¸®Æ®·Î¸¶À̽гëÃâÀº ¿¡Æ®¶ó¸®ºó¿¡ ÀÇÇØ °¨¼ÒµÇ¾úÀ¸³ª, Ȱ¼º´ë»çü 14-OH-Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀÇ ³óµµ´Â Áõ°¡µÇ¾ú´Ù. 14-OH-Ŭ·¡¸®Æ®·Î¸¶À̽ÅÀº Mycobacterium avium complex (14)¿¡ ´ëÇØ °¨¼ÒµÈ Ȱ¼ºÀ» °¡Áö¹Ç·Î, ÀÌ º´¿ø±Õ¿¡ ´ëÇÑ ÃÑ È°¼ºÀÌ º¯°æµÉ ¼öµµ ÀÖ´Ù. µû¶ó¼, MACÀÇ Ä¡·á¿¡ ÀÖ¾î¼ ÀÌ ¾àÀÇ ´ëüÁ¦¸¦ °í·ÁÇÏ¿©¾ß ÇÑ´Ù.
 
   
  
    
  
  
       	
  
     
  
  
  
  
  
  
 
    
   
  
    
       
      
        
          
            
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    DUR (ÀǾàǰ»ç¿ëÆò°¡) 
    º´¿ë±Ý±â :
     
	 °í½ÃµÈ º´¿ë±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
	 
	 [»óÈ£ÀÛ¿ë/º´¿ë±Ý±â°Ë»ö]  										
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    Mechanism of Action 
    
      Clarithromycin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸  Clarithromycin is first metabolized to 14-OH clarithromycin. Like other macrolides, it then binds to the 50 S subunit of the 70 S ribosome of the bacteria, blocking RNA-mediated bacterial protein synthesis. Clarithromycin also inhibits the hepatic microsomal CYP3A4 isoenzyme and P-glycoprotein, an energy-dependent drug efflux pump. 
     
   
  
   
    Pharmacology 
     
      Clarithromycin¿¡ ´ëÇÑ Pharmacology Á¤º¸  Clarithromycin, a macrolide antibiotic similar to erythromycin and azithromycin, is effective against Mycobacterium avium complex (MAC) and is used for the treatment of Helicobacter pylori -associated peptic ulcer disease, community-acquired pneumonia, sinusitis, and chronic bronchitis. Clarithromycin is also used to treat respiratory tract, sexually transmitted, otitis media, and AIDS-related infections. 
     
   
  
   
    Protein Binding 
    
      Clarithromycin¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸  Low protein binding 
     
   
  
   
    Half-life 
    
      Clarithromycin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸  3-4 hours 
     
   
  
   
    Absorption 
    
      Clarithromycin¿¡ ´ëÇÑ Absorption Á¤º¸  50% 
     
   
  
   
    Toxicity 
    
      Clarithromycin¿¡ ´ëÇÑ Toxicity Á¤º¸  Symptoms of toxicity include diarrhea, nausea, abnormal taste, dyspepsia, and abdominal discomfort. Pseudomembraneous colitis has been reported with clarithromycin use, allergic reactions ranging from urticaria and mild skin eruptions to rare cases of anaphylaxis and Stevens-Johnson syndrome have occurred. Rare cases of severe hepatic dysfunctions also have been reported. Hepatic failure is usually reversible, but fatalities have been reported. 
     
   
  
   
    Drug Interactions 
    
      Clarithromycin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸  Alprazolam	The macrolide increases the effect of the benzodiazepineAminophylline	Increases the effect and toxicity of theophyllineAmiodarone	Increased risk of cardiotoxicity and arrhythmiasAnisindione	The macrolide increases the anticoagulant effectAprepitant	This CYP3A4 inhibitor increases the effect and toxicity of aprepitantAstemizole	Increased risk of cardiotoxicity and arrhythmiasAtazanavir	Atazanavir increases levels of clarithromycinAtorvastatin	The macrolide possibly increases the statin toxicityBretylium	Increased risk of cardiotoxicity and arrhythmiasBuspirone	Increases the effect and toxicity of buspironeCarbamazepine	The macrolide increases the effect of carbamazepineCerivastatin	The macrolide possibly increases the statin toxicityCisapride	Increased risk of cardiotoxicity and arrhythmiasCitalopram	Possible serotoninergic syndrome with this combinationColchicine	Severe colchicine toxicity can occurCyclosporine	The macrolide increases the effect of cyclosporineDarifenacin	This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolismDarunavir	Increased levels of clarithromycinDiazepam	The macrolide increases the effect of the benzodiazepineDicumarol	The macrolide increases anticoagulant effectDigoxin	The macrolide increases the effect of digoxin in 10% of patientsDihydroergotamine	Risk of ergotism and severe ischemia with this associationDyphylline	Increases the effect and toxicity of theophylline Disopyramide	Increased risk of cardiotoxicity and arrhythmiasDofetilide	Increased risk of cardiotoxicity and arrhythmiasDyphylline	Increases the effect and toxicity of theophyllineEfavirenz	Efavirenz decreases levels of clarithromycinEletriptan	This macrolide increases the effect and toxicity of eletriptanEplerenone	This macrolide increases the effect and toxicity of eplerenoneErgotamine	Risk of ergotism and severe ischemia with this associationErlotinib	This CYP3A4 inhibitor increases levels/toxicity of erlotinibFluoxetine	Possible serotoninergic syndrome with this combinationFosphenytoin	Increases the effect and toxicity of phenytoinGefitinib	This CYP3A4 inhibitor increases levels/toxicity of gefitinibImatinib	The macrolide increases levels of imatinibIndinavir	Increases the effect and toxicity of indinavirItraconazole	The macrolide increases the effect and toxicity of itraconazoleLovastatin	The macrolide possibly increases the statin toxicityMethylprednisolone	The macrolide increases the effect of corticosteroidMethysergide	Risk of ergotism and severe ischemia with this associationMidazolam	The macrolide increases the effect of the benzodiazepineAcenocoumarol	The macrolide increases anticoagulant effectOxtriphylline	Increases the effect and toxicity of theophyllinePhenytoin	Increases the effect and toxicity of phenytoinPimozide	Increased risk of cardiotoxicity and arrhythmiasQuetiapine	This macrolide increases the effect/toxicity of quetiapineQuinidine	Increased risk of cardiotoxicity and arrhythmiasQuinidine barbiturate	Increased risk of cardiotoxicity and arrhythmiasQuinupristin	This combination presents an increased risk of toxicityRanolazine	Increased levels of ranolazine- risk of toxicityRepaglinide	Increases the effect of repaglinideRifabutin	The rifamycin decreases the effect of the macrolideRifampin	The rifamycin decreases the effect of the macrolideSertraline	Possible serotoninergic syndrome with this combinationSildenafil	Increases the effect and toxicity of sildenafilSimvastatin	The macrolide possibly increases the statin toxicitySirolimus	The macrolide increases sirolimus levelsSotalol	Increased risk of cardiotoxicity and arrhythmiasSunitinib	Possible increase in sunitinib levelsTacrolimus	This antibiotic increases the effect and toxicity of tacrolimusTerfenadine	Increased risk of cardiotoxicity and arrhythmiasTheophylline	Increases the effect and toxicity of theophyllineTriazolam	The macrolide increases the effect of the benzodiazepineVardenafil	Increases the effect and toxicity of vardenafilWarfarin	The macrolide increases anticoagulant effectEverolimus	The macrolide increases everolimus levels/toxicitySolifenacin	This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism 
     
   
  
   
    CYP450  Drug Interaction 
    
      [CYP450 TableÁ÷Á¢Á¶È¸] Clarithromycin¿¡ ´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 
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 
     
   
  
   
    Drug Target 
    
      
      [Drug Target]  
     
   
  
   
    Description 
    
      Clarithromycin¿¡ ´ëÇÑ Description Á¤º¸  A semisynthetic macrolide antibiotic derived from erythromycin that is active against a variety of microorganisms. It can inhibit protein synthesis in bacteria by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation. [PubChem] 
     
   
  
   
    Dosage Form 
    
      Clarithromycin¿¡ ´ëÇÑ Dosage_Form Á¤º¸  Tablet	OralTablet, extended release	Oral 
     
   
  
   
    Drug Category 
    
      Clarithromycin¿¡ ´ëÇÑ Drug_Category Á¤º¸  Anti-Bacterial AgentsOther MacrolidesProtein Synthesis Inhibitors 
     
   
  
   
    Smiles String Canonical 
    
      Clarithromycin¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸  CCC1OC(=O)C(C)C(OC2CC(C)(OC)C(O)C(C)O2)C(C)C(OC2OC(C)CC(C2O)N(C)C)C(C)(CC(C)C(=O)C(C)C(O)C1(C)O)OC 
     
   
  
   
    Smiles String Isomeric 
    
      Clarithromycin¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸  CC[C@@H]1OC(=O)[C@H](C)[C@@H](O[C@H]2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@@H]([C@H]2O)N(C)C)[C@@](C)(C[C@@H](C)C(=O)[C@@H](C)[C@@H](O)[C@]1(C)O)OC 
     
   
  
   
    InChI Identifier 
    
      Clarithromycin¿¡ ´ëÇÑ InChI_Identifier Á¤º¸  InChI=1/C38H69NO13/c1-15-26-38(10,45)31(42)21(4)28(40)19(2)17-37(9,47-14)33(52-35-29(41)25(39(11)12)16-20(3)48-35)22(5)30(23(6)34(44)50-26)51-27-18-36(8,46-13)32(43)24(7)49-27/h19-27,29-33,35,41-43,45H,15-18H2,1-14H3/t19-,20-,21-,22+,23-,24+,25+,26+,27+,29-,30+,31-,32+,33-,35+,36-,37-,38-/m1/s1 
     
   
  
   
    Chemical IUPAC Name 
    
      Clarithromycin¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸  (3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-6-[(2S,3R,4S,6R)-4-dimethylamino-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-12,13-dihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-7-methoxy-3,5,7,9,11,13-hexamethyl-1-oxacyclotetradecane-2,10-dione 
     
   
  
   
    Drug-Induced Toxicity Related Proteins 
    
      CLARITHROMYCIN   ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸Replated Protein  :HERGDrug  :clarithromycin Toxicity  :torsade de pointes. [¹Ù·Î°¡±â] Replated Protein  :Potassium voltage-gated channel subfamily KQT member 1 (KvLQT1)Drug  :clarithromycin Toxicity  :torsade de pointes. [¹Ù·Î°¡±â] Replated Protein  :Misshapen-like kinase(Mink)Drug  :clarithromycin Toxicity  :torsade de pointes. [¹Ù·Î°¡±â]  
     
   
    
 
    
     
  
    
       
      
        
          
            
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                ÃÖ±ÙÁ¤º¸¼öÁ¤ÀÏ 2024-12-18
               
              
                
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                          ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
 
  
                  
 
               
  
  
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