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Celecoxib
(¼¼·¹Ä۽úê)
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Synonyms |
celecoxib
SC-58635
YM-177 |
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Therapeutic Classification |
- NSAIDs (Nonsteroidal Anti-Inflammatory Drugs)
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Mechanism of Action |
- ºÐ·ù : NSAIDs (Nonsteroidal Anti-Inflammatory Drugs), COX-2 (cyclooxygenase-2) inhibitor
- ÀÛ¿ë±âÀü : cyclooxygenase enzyme (prostaglandin synthase H)´Â 2°³ÀÇ À̼ºÃ¼ (COX-1°ú COX-2)·Î ±¸¼ºµÇ¾î ÀÖ´Ù. Cyclooxygenase-2 (COX-2) inhibitors´Â COX-1Àº °ÅÀÇ ¾ïÁ¦ÇÏÁö ¾Ê°Å³ª ÀüÇô ¾ïÁ¦ÇÏÁö ¾Ê°í, COX-2ÀÇ ¼±ÅÃÀûÀÎ ¾ïÁ¦¸¦ ÅëÇØ prostaglandin H2ÀÇ ÇÕ¼ºÀ» ¾ïÁ¦½ÃÄÑ Ç׿°, ÁøÅë ÀÛ¿ëÀ» °®´Â´Ù. ÀüÅëÀûÀÎ ºñ½ºÅ×·ÎÀ̵强 ¼Ò¿°ÁøÅëÁ¦ (NSAIDs)¿Í ºñ½ÁÇÏÁö¸¸ COX-2¸¦ ¼±ÅÃÀûÀ¸·Î ¾ïÁ¦Çϸé, ºñ½ºÅ×·ÎÀ̵强 ¼Ò¿°ÁøÅëÁ¦ÀÇ ÀüÅëÀûÀÎ ºÎÀÛ¿ëÀÎ À§Àå°ü ºÎÀÛ¿ëÀÌ °ÅÀÇ ¾ø´Ù.
- COX icosanoidsÀÇ ºÐºñ¸¦ ÃËÁø½ÃÄÑ thromboxane A2, prostacyclin, and PGE2¸¦ »ý¼ºÇÑ´Ù. ÀÌ·¯ÇÑ °æ·Î¸¦ Â÷´ÜÇϸé À§Àå°ü ºÎÀÛ¿ë, Ç÷¼ÒÆÇ ±â´ÉÀå¾Ö, ±â°üÁö °æ·Ã µî°ú °°Àº ºÎÀÛ¿ëÀ» ÀÏÀ¸Å²´Ù.
- COX-2´Â ¿°Áõ°úÁ¤¿¡¼ »ý¼ºµÇ´Â À¯µµÇü È¿¼ÒÀÌ´Ù. COX-2°¡ È°¼ºÈµÇ¸é ÇÁ·Î½ºÅ¸±Û¶õµò°ú, ¿°Áõ, ÅëÁõÀ» ÀÏÀ¸Å°´Â ¸Å°³¹°ÁúÀÌ ÇÕ¼ºµÈ´Ù. COX-2´Â Ç÷¼ÒÆÇ ¶Ç´Â À§Á¡¸·¿¡´Â Á¸ÀçÇÏÁö ¾Ê´Â´Ù.
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Clinical Uses |
ÀûÀÀÁõ : °ñ°üÀý¿°°ú ·ù¸¶Æ¼½º°üÀý¿°ÀÇ Ä¡·á |
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Pharmacokinetics |
- Èí¼ö : Ç÷Áß ÃÖ°í³óµµ µµ´Þ½Ã°£ : 3½Ã°£
°íÁö¹æ½Ä°ú ÇÔ²² Åõ¿©Çϸé ÃÖ°í Ç÷Àå³óµµ¿¡ µµ´ÞÇÏ´Â ½Ã°£À» ´ë·« 1-2½Ã°£Á¤µµ Áö¿¬ ½ÃŲ´Ù.
- ºÐÆ÷ : celecoxib 200mgÀ» °æ±¸Åõ¿©ÇÏ¿´À»¶§ Cmax´Â 705 ng/mL ÀÌ´Ù.
°íÁö¹æ½Ä°ú ÇÔ²² Åõ¿©Çϸé Cmax´Â 1-2½Ã°£ Áö¿¬µÇ°í, AUC´Â 10-20% Áõ°¡ÇÑ´Ù.
Á¦»êÁ¦¿Í ÇÔ²² Åõ¿©Çϸé Cmax´Â 37% °¨¼ÒÇÏ°í, AUC´Â 10% °¨¼ÒÇÑ´Ù.
Celecoxib´Â ´Ü¹é°áÇÕ·üÀÌ ³ô´Ù. (¾à 97%) 1Â÷ÀûÀ¸·Î albumin°ú °áÇÕÇÏ°í ¼Ò·®Àº alpha-1 acid glycoprotein°ú °áÇÕÇÑ´Ù.
- ´ë»ç : Celecoxib´Â cytochrome P450 µ¿À§È¿¼ÒÀÎ 2C9 ¿¡ ÀÇÇØ °£¿¡¼ 1Â÷ÀûÀ¸·Î ´ë»çµÈ´Ù.
CelecoxibÀÇ ºÒÈ°¼ºÇü ´ë»ç»ê¹°Àº Ç÷Àå¿¡¼ ´ÙÀ½ 3°¡Áö´Ù. : 1Â÷ÀûÀ¸·Î alcohol, ±× ´ÙÀ½¿£ carboxylic acid°ú ±×ÀÇ glucuronide conjugateÀÎ Celebrex
- ¹è¼³
- ½ÅÀå : °æ±¸Åõ¿©µÈ celecoxibÀÇ ¾à 27%´Â ÁÖ·Î carboxylic acid ´ë»ç»ê¹°ÀÇ ÇüÅÂ¿Í ¼Ò·®ÀÇ glucuronide conjugateÀÇ ÇüÅ·Π¼Òº¯À¸·Î ¹è¼³µÈ´Ù.
- ´ëº¯ : celecoxib´Â 1Â÷ÀûÀ¸·Î´Â ´ëº¯À» ÅëÇØ ¹è¼³µÈ´Ù.(°æ±¸Åõ¿©¿ë·®ÀÇ ¾à 57%)
´ëº¯¿¡¼ÀÇ 1Â÷ ´ë»ç»ê¹°Àº carboxylic acid ´ë»ç»ê¹°ÀÌ´Ù.
- ±âŸ : °Ñº¸±â Ç÷Àå û¼ÒÀ²Àº 500 mL/minÀÌ´Ù.
- ¹Ý°¨±â´Â ´ë·« 11.2½Ã°£ÀÌ´Ù.
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Usual Dosage |
- ¼ºÀÎ : °ñ°üÀý¿° : 100mg 1ÀÏ 2ȸ ¶Ç´Â 200mg 1ÀÏ 1ȸ
·ù¸¶Æ¼½º°üÀý¿° : 100-200mg 1ÀÏ 2ȸ
°¡Á·¼º ¼±Á¾¾ç Æú¸³Áõ (Familial Adenomatous Polyposis, FAP) : 400mg 1ÀÏ 2ȸ
- ¼Ò¾Æ : 18¼¼ ÀÌÇÏ´Â °ñ°üÀý¿°°ú ·ù¸¶Æ¼½º°üÀý¿°ÀÇ Ä¡·á¿¡ È®¸³µÈ ÀÚ·á°¡ ¾ø´Ù.
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Adverse Reactions |
- ºÎÀÛ¿ë : ÁÖ¿ä ºÎÀÛ¿ë : ¼ÒȺҷ®, ¼³»ç, µÎÅë, ºÎºñµ¿¿°, »ó±âµµ°¨¿°
- ÀÚÁÖ ÀϾ´Â ºÎÀÛ¿ë :
- À§Àå°ü°è : º¯ºñ, °Ô½Ç¿°, ¿¬ÇÏ°ï¶õ, Æ®¸² (eructation), ½Äµµ¿°, À§¿°, À§Àå°ü¿°, À§½Äµµ¿ª·ù, Ä¡Áú, ¿°ø¼º Å»Àå (hiatal hernia), Ç÷º¯ (melena), ±¸°Ç, ±¸³»¿°, ÈÄÁß (tenesmus), Ä¡¾ÆÀÌ»ó (tooth disorder), ±¸Åä
- ½ÉÇ÷°ü°è : °íÇ÷¾Ð ¾ÇÈ, Çù½ÉÁõ, °ü»óµ¿¸ÆÁúȯ, ½É±Ù°æ»ö
- Àü½Å : °ú¹Î¹ÝÀÀ ¾ÇÈ, ¾Ë·¯Áö¹ÝÀÀ, ¹«·ÂÁõ (asthenia), ÈäÅë, cyst NOS, Àü½ÅºÎÁ¾, ¾ó±¼ºÎÁ¾, ÇÇ·Î, ¹ß¿, ¶ß°Å¿î ¼¶±¤, µ¶°¨Áõ»ó, ÅëÁõ, ¸»ÃÊ µ¿Åë
- ³»¼º±âÀüÁúȯ : ´Ü¼øÆ÷Áø, ´ë»óÆ÷Áø, ¼¼±Õ°¨¿°, Áø±Õ°¨¿°, ¿¬Á¶Á÷°¨¿°, ¹ÙÀÌ·¯½º°¨¿°, ¸ð´Ò¸®¾ÆÁõ, ¼º±â ¸ð´Ò¸®¾ÆÁõ, ÁßÀÌ¿°
- ÁßÃß, ¸»ÃÊ ½Å°æ°è : ´Ù¸®°æ·Ã, ±äÀå°úµµ, Áö°¢°¨Åð, ÆíµÎÅë, ½Å°æÅë, ½Å°æÁúȯ, °¨°¢ÀÌ»ó, Çö±âÁõ
- ¿©¼º»ý½Ä±â : Breast fibroadenosis, breast neoplasm, breast pain, dysmenorrhea, menstrual disorder, vaginal hemorrhage, vaginitis
- ³²¼º»ý½Ä±â : Àü¸³¼±Áúȯ
- û°¢, ÀüÁ¤±â°ü : ³Ã», ±ÍÀÇ ÀÌ»ó, ÀÌÅë, À̸í
- ½É¹Úµ¿ : ½É°èÇ×Áø, ºó¸Æ
- °£, ´ãÁó°è : °£±â´ÉÀÌ»ó, SGOT, SGPTÄ¡ »ó½Â
- ´ë»ç, ¿µ¾ç : BUN »ó½Â, CPK »ó½Â, ´ç´¢º´, °íÄÝ·¹½ºÅ×·ÑÇ÷Áõ, °úÇ÷´çÁõ, ÀúÄ®·ýÇ÷Áõ, NPN »ó½Â, creatinine »ó½Â, alkaline phosphatase »ó½Â, üÁßÁõ°¡
- ±Ù°ñ°Ý°è : °üÀý¿°, °üÀýÁõ, »ÀÀÇ ÀÌ»ó, °ñÀý¹ß»ý, ±ÙÀ°Åë, ¸ñÀÌ »»»»ÇØÁü, È°¸·¿°, °Ç¿°
- Ç÷¼ÒÆÇ (ÃâÇ÷ ¶Ç´Â Ç÷Àü) : ¹Ý»óÃâÇ÷, ºñÃâÇ÷, Ç÷¼ÒÆÇÇ÷Áõ
- <ºÎÁø, ºÒ¾È, ½Ä¿åÁõ°¡, ¿ì¿ï, ½Å°æ°ú¹Î, ±â¸é (somnolence)
- : ºóÇ÷
- È£Èí±â : ±â°üÁö¿°, ±â°üÁö°æ·Ã, ±â°üÁö°æ·Ã¾ÇÈ, ±âħ, È£Èí°ï¶õ, ÀÎÈÄ¿°, Æó·Å
- ÇÇºÎ¿Í ±× ºÎ¼Ó±â : Å»¸ð, ÇǺο°, ¼Õ¹ßÅéÁúȯ, ±¤°ú¹Î¼º, µÎµå·¯±â, È«¹Ý¼º ¹ßÁø, ¹ÝÁ¡±¸Áø¼º ¹ßÁø, ÇǺÎÁúȯ, ÇǺΰÇÁ¶, ¶¡ºÐºñÁõ°¡, µÎµå·¯±â
- ºñ´¢±â°è : ¾ËºÎ¹Î´¢Áõ, ¹æ±¤¿°, ¹è´¢°ï¶õ, Ç÷´¢, ºó´¢, ½Å°á¼®, ´¢½Ç±Ý, ¹è´¢°ü °¨¿°
- ½Ã·Â : ½Ã¾ß°¡ Èå·ÁÁü, ¹é³»Àå, °á¸·¿°, ¾È±¸µ¿Åë, ³ì³»Àå
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Overdosage / Toxicology |
COX-2 ÀúÇØÁ¦ÀÇ °ú·®Åõ¿©¿¡ ´ëÇÑ Á¤º¸´Â ¸¹Áö ¾Ê´Ù. ´Ù¸¥ NSAIDs¿Í ¸¶Âù°¡Áö·Î À§Àå°üÀå¾Ö, ±â¸é (lethargy) µîÀÌ ÀÖ´Ù°í »ý°¢µÈ´Ù. Á¦Á¶¾÷ÀÚ´Â µå¹°°Ô °íÇ÷¾Ð, ÁßÁõ ½ÅºÎÀü, È£Èí°ï¶õ, È¥¼ö µîÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù°í ÇÏ¿´Áö¸¸ º¸°íµÈ ÀûÀº ¾ø´Ù. |
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Contraindications |
- º»Á¦¿¡ °ú¹Î¼º
- sulfonamides¿¡ ¾Ë·¯Áö ±â¿Õ·ÂȯÀÚ
- aspirin ¶Ç´Â ´Ù¸¥ NSAIDs¿¡ õ½Ä, µÎµå·¯±â, ¾Ë·¯Áö ¹ÝÀÀÀ» º¸¿´´ø ȯÀÚ
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Precautions |
- µ¿¸Æ°üÀÇ Á¶±âÆó¼â (premature closure of the ductus arteriosus)¸¦ ÀÏÀ¸Å³ ¼ö ÀÖÀ¸¹Ç·Î ÀӽŸ»±â¿¡´Â Åõ¿©ÇÏÁö ¾Ê´Â´Ù.
- °£±â´ÉºÎÀü ±â¿Õ·ÂÀÚ
3. ¼öºÐÀú·ù³ª ºÎÁ¾À¸·Î ¾ÇȵǴ °íÇ÷¾ÐÀ̳ª ½ÉÀåÁúȯ
4. À§Àå°ü±Ë¾ç, ÃâÇ÷, õ°ø ±â¿Õ·ÂÀÚ
5. ½ÅºÎÀü
6. ƯÈ÷ ³ëÀÎȯÀÚ¿¡ ÀÖ¾î¼, warfarin°ú celecoxib¸¦ µ¿½ÃÅõ¿©ÇÏ´Â °æ¿ì, Ä¡·áÃʱ⳪ ¿ë·®À» º¯°æÇÏ´Â °æ¿ì¿¡ ÁÖÀÇÇÑ´Ù.
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Pregnancy Risk Factor |
Pregnancy Category : C
ÀӽŠ3±â¿¡ Åõ¿©½Ã: D
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Pregnancy Implication |
µ¿¸Æ°üÀÇ Á¶±âÆó¼â (premature closure of the ductus arteriosus)¸¦ ÀÏÀ¸Å³ ¼ö ÀÖÀ¸¹Ç·Î ÀӽŸ»±â¿¡´Â Åõ¿©ÇÏÁö ¾Ê´Â´Ù. |
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Stability |
¿, ½À±â, Á÷»ç±¤¼±À» ÇÇÇÏ¿© ½Ç¿Âº¸°ü |
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Interactions |
- ACE-inhibitors : È¿°ú °¨¼Ò
- lFurosemide, thiazides : È¿°ú °¨¼Ò
- Aspirin : À§Àå°ü ÃâÇ÷ÀÇ À§Çè Áõ°¡
- Fluconazole : celecoxibÀÇ Ç÷Àå³óµµ¸¦ 2¹è·Î Áõ°¡½ÃŲ´Ù.
- Lithium : lithium 450mg 1ÀÏ 2ȸ, celecoxib 200mg 1ÀÏ 2ȸ µ¿½ÃÅõ¿©Çϸé Æò±Õ ¾ÈÁ¤»óÅ (mean steady-state)ÀÇ lithium ³óµµ¸¦ 17% Áõ°¡½ÃŲ´Ù.
Á¦»êÁ¦ : aluminuv, magnesiumÀ» ÇÔÀ¯ÇÑ Á¦»êÁ¦¸¦ °°ÀÌ Åõ¿©Çϸé celecoxibÀÇ Cmax´Â 37% Áõ°¡ÇÏ°í AUC´Â 10% °¨¼ÒÇÑ´Ù.
Warfarin : wafarin°ú celecoxib¸¦ µ¿½ÃÅõ¿©Çϸé ƯÈ÷ ³ëÀÎȯÀÚ¿¡°Ô ÀÖ¾î¼ prothrombin time°ú ÃâÇ÷À» Áõ°¡½ÃŲ´Ù´Â º¸°í°¡ ÀÖ´Ù. Á¦Á¶È¸»ç¿¡¼´Â warfarinÀ» Åõ¿©¹Þ´Â ȯÀÚ¿¡°Ô celecoxib Ä¡·á¸¦ óÀ½ ½ÃÀÛÇϰųª º¯°æÇÏ´Â °æ¿ì Ç×ÀÀ°íÀÛ¿ëÀ» ¸ð´ÏÅÍÇϵµ·Ï ±Ç°íÇÏ°í ÀÖ´Ù. |
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monitoring parameters |
- °ú·®Åõ¿©ÇÑ °æ¿ì¿¡´Â Ç÷ûÀüÇØÁú, ½Å±â´É, ¿ä°Ë»ç µîÀ» ¸ð´ÏÅÍÇÑ´Ù.
- Ç×ÀÀ°íÁ¦ (¿¹:warfarin)¸¦ Åõ¿©ÁßÀΠȯÀÚ´Â celecoxib Åõ¿©Ãʱ⿡ ÀÀ°íÈ¿°ú¸¦ ¸ð´ÏÅÍÇØ¾ß ÇÑ´Ù. ÇÔ²² Åõ¿©ÇßÀ» ¶§ ÃâÇ÷°æÇâÀÌ Áõ°¡ÇÑ´Ù´Â º¸°í°¡ ÀÖ´Ù.
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Nursing Implications |
- Áã½ÇÇè¿¡¼ Ç÷Àå³óµµ¿Í ºñ½ÁÇÏ°Ô À¯ÁóÀ¸·Î ºÐºñµÈ´Ù. »ç¶÷¿¡¼´Â È®ÀεÇÁö ¾Ê¾Ò´Ù. ¼öÀ¯¸¦ Áß´ÜÇÒ °ÍÀÎÁö ¾àÀ» Áß´ÜÇÒ °ÍÀÎÁö´Â ȯÀÚ¿¡ µû¶ó °áÁ¤ÇÑ´Ù.
- µ¿¸Æ°üÀÇ Á¶±âÆó¼â (premature closure of the ductus arteriosus)¸¦ ÀÏÀ¸Å³ ¼ö ÀÖÀ¸¹Ç·Î ÀӽŸ»±â¿¡´Â Åõ¿©ÇÏÁö ¾Ê´Â´Ù.
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Patient Education |
- Lithium, fluconazole, furosemide, ACE inhibitors, warfarin µîÀ» º¹¿ëÁßÀΠȯÀÚ´Â ÀÇ»ç¿Í »óÀÇÇÑ´Ù.
- ¼úÀ̳ª ´ã¹è´Â ±Ë¾çÀ̳ª À§ÃâÇ÷ÀÇ À§ÇèÀ» Áõ°¡½Ãų ¼ö ÀÖ´Ù.
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Reference |
- Product Information: Celebrex ¢â, celecoxib. G.D. Searle & Co., Chicago, Ill, 1998.
- Simon LS, Lanza FL, Lipsky PE et al: Preliminary study of the safety and efficacy of SC-58635, a novel cyclooxygenase 2 inhibitor. Arthr Rheum 1998; 41:1591-1602.
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