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670602250[A29554931]
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1¹ÙÀ̾Ë(2ML) ¡¿ ÀÚ»çÆ÷Àå´ÜÀ§ |
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192106BIJ
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1. ´ÙÀ½°ú °°Àº ¾Ï»óÅÂÀÇ ±¤¹üÀ§ÇÑ Ã³Ä¡
±Þ¼º ¹éÇ÷º´, ºñÈ£ÁöŲ¼º ÀÓÆÄÁ¾, ¿¬Á¶Á÷ ¹× °ñ¿ø¼º À°Á¾
À¯¹æ¾Ï, Æó¾Ï, µÎ°æºÎ¾Ï, ¹æ±¤¾Ï, °æºÎ¾Ï, ³¼Ò¾Ï ¹× °íȯ¾Ï, °íÇü¾Ï, À¶¸ð¾Ï
2. Ç× °Ç¼± È¿°ú
ŸÁ¦·Î¼ È¿°ú°¡ ¾ø´Â ½ÉÇÑ ºÒÀÀ¼º °Ç¼±
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Methotrexate
µ¶¼ºÇ÷û³óµµ: < 9.1ng/§¢(Àú¿ë·®¿ä¹ý), < 454ng/§¢(°í¿ë·®¿ä¹ý)
1. Åõ¿©¹æ¹ý
1) ¼Ò·®Åõ¿©(Á¤ÁÖ ¶Ç´Â ±ÙÁÖ)
2) ´ë·®Åõ¿©¡²±Þ¼Ó Á¤¸ÆÁÖ»ç(bolus injection) ¶Ç´Â ÁÖÀÔ (infusion)¡³
3) ¼ö¸·°³» ¶Ç´Â ³ú½Ç³» ÁÖ»ç
2. °¢ ÀûÀÀÁõ¿¡ µû¸¥ Åõ¿©·®Àº ´ÙÀ½°ú °°´Ù.
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3) À¯¹æ¾Ï, Æó¾Ï, µÎ°æºÎ¾Ï ¹× ¹æ±¤¾Ï, °ñÀ°Á¾, ºñÈ£ÁöŲ¼º ÀÓÆÄÁ¾ : 1,000§·/§³(¾à 33§·/§¸)
4) Æó¾Ï ¹× °ñÀ°Á¾ : 1¢¦5g/§³(¾à 33¢¦166§·/§¸)
5) °ñÀ°Á¾ : 5¢¦14g/§³(¾à 166¢¦466§·/§¸)
ÀÌ»óÀÇ Åõ¿©Ã³¹æÀº ¸ÞÅ䯮·º¼¼ÀÌÆ® ´ÜÀÏÅõ¿© ¶Ç´Â Á¾Á¾ ŸÁ¦¿Í º´¿ëÇϸç, ŸÁ¦¿ÍÀÇ º´¿ë½Ã º´¿ë¿¡ ÀÇÇÑ µ¶¼ºÁõ°¡¸¦ °í·ÁÇÏ¿© Åõ¿©·®À» °æ°¨ÇØ¾ß ÇÑ´Ù.
6) °Ç¼±¿¡ ´ëÇÑ Åõ¿© : ±âÁ¸ÀÇ ¿ä¹ý¿¡ ºÒÀÀ¼ºÀÎ, ½ÉÇϰí ÅëÁ¦ºÒ´ÉÇÑ °Ç¼±¿¡ ´ëÇÑ Åõ¿©´Â Åë»ó 1ÁÖ 1ȸ 10¢¦25§·À» °æ±¸·Î Åõ¿©Çϳª, Á¤ÁÖ ¶Ç´Â ±ÙÁÖ·Î Åõ¿©Çϱ⵵ ÇÑ´Ù.
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°¡´ÉÇÑ ÇÑ ÁÖÀÔ¿ë Æ©ºê¸¦ ÅëÇØ 2¢¦3ºÐ ÀÌ»ó Åõ¿©ÇÑ´Ù. 100§· Ãʰú·® Åõ¿©½Ã´Â Åë»ó Á¤¸Æ ÁÖÀÔÀ¸·Î ÇÏ¿© 24½Ã°£ À̳»¿¡¼ ½Ç½ÃÇÑ´Ù. (ÃÖÃÊ Åõ¿©½Ã ±Þ¼ÓÅõ¿©·Î ÇÑ´Ù.)
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1) ÀÌ ¾à¿¡ ´ëÇÑ °ú¹ÎÁõÀÇ º´·ÂÀÌ Àִ ȯÀÚ.
2) ÁßÁõÀÇ ½ÅºÎÀü ¶Ç´Â °£ºÎÀü ȯÀÚ
3) Èä¼ö, º¹¼ö µîÀÌ Àִ ȯÀÚ (Èä¼ö, º¹¼ö µîÀÇ Àå±â°£ Àú·ù½Ã µ¶¼ºÀÌ Áõ°µÉ ¼ö ÀÖÀ½.)
4) ´ÙÀ½°ú °°Àº »óÅÂÀÇ °Ç¼± ¶Ç´Â ·ù¸¶Æ¼½º¼º °üÀý¿° ȯÀÚ
(1) °ñ¼öÇü¼º ºÎÀü, ¹éÇ÷º´°¨¼ÒÁõ, Ç÷¼ÒÆÇ°¨¼ÒÁõ, ½ÉÇÑ ºóÇ÷°ú °°Àº Ç÷¾×ÁúȯÀÌ ¼±ÀçÇØ ÀÖ´Â »óÅÂ
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2) °£Àå¾Ö ȯÀÚ
3) ¼³»ç ¶Ç´Â ±Ë¾ç¼º ±¸³»¿°ÀÌ ³ªÅ¸³ª´Â ȯÀÚ (Àåõ°øÀ¸·Î ÀÎÇÑ ÃâÇ÷¼º Àå¿°°ú »ç¸ÁÀ» ÃÊ·¡ÇÒ ¼ö ÀÖÀ½.)
4) À§±Ë¾ç ¶Ç´Â ±Ë¾ç¼º ´ëÀå¿°ÀÌ Àִ ȯÀÚ
5) Ç÷¾×ÇÐÀû ÀÌ»ó, ¾Ç¼º ¶Ç´Â ¼±ÀçÇÏ´Â Á¶Ç÷ ¼Õ»óÀÌ Àִ ȯÀÚ
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7) ¼öµÎ ȯÀÚ (Ä¡¸íÀûÀÎ Àü½ÅÀåÇØ°¡ ³ªÅ¸³¯ ¼ö ÀÖ´Ù.)
8) °¨¿°ÁõÀ» ÇÕº´Çϰí Àִ ȯÀÚ
9) Á¤½ÅÀû Àå¾Ö°¡ Àִ ȯÀÚ
10) °í·ÉÀÚ ¹× ¼Ò¾Æ
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1) ¼ï : µå¹°°Ô ¼ïÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î °üÂûÀ» ÃæºÐÈ÷ ÇÏ¿© ÀÌ»óÀÌ ÀÎÁöµÇ´Â °æ¿ì¿¡´Â Åõ¿©¸¦ ÁßÁöÇϰí ÀûÀýÈ÷ óġ¸¦ ÇÑ´Ù.
2) ¼Òȱâ°è : ÃâÇ÷¼º Àå¿°, ±«»ç¼º Àå¿° µîÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î ½ÉÇÑ À§Àå°ü±Ë¾ç, ÃâÇ÷, ±¸³»¿°, º¹Åë, ¼³»ç, ±¸¿ª, ±¸Åä µîÀÌ ³ªÅ¸³ª¸é Å»¼ö¸¦ ÃÊ·¡ÇÒ ¼ö ÀÖÀ¸¹Ç·Î ȸº¹½Ã±îÁö Åõ¿©¸¦ ÁßÁöÇϰí ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù. ¶ÇÇÑ ½Ä¿åºÎÁø, ÈæÅäÁõ, ÀåÆó»ö µîÀÇ Áõ»óÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù.
3) È£Èí±â°è : °£Áú¼º Æó·ÅÀ¸·Î ÀÎÇÑ »ç¸ÁÀÌ º¸°íµÇ¾úÀ¸¸ç ¶§¶§·Î ¸¸¼º°£Áú¼º ÆóÁúȯ, Æó¼¶À¯ÁõÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù. ¶ÇÇÑ ÀÌ ¾à »ç¿ë½Ã¿¡ ³ªÅ¸³ª´Â ÆóÁõ»ó (ƯÈ÷ °´´ãÀ» ¼ö¹ÝÇÏÁö ¾Ê´Â ¸¶¸¥±âħ) ¶Ç´Â ºñƯÀ̼º Æó·ÅÀº À§ÇèÇÑ ÀáÀçÀû ÀåÇØÀÇ Â¡ÈÄÀÏ ¼ö ÀÖ°í ¸ðµç Åõ¿©·®¿¡¼ ¹ß»ýÇÒ ¼ö ÀÖÀ¸¹Ç·Î Áï½Ã Åõ¾àÀ» Áß´ÜÇϰí ÁÖÀDZí°Ô °Ë»çÇÑ´Ù. ÀÌ ¾àÀ¸·Î À¯¹ßµÈ ÆóÁúȯÀÌ Àִ ȯÀÚ´Â ºñ·Ï ÀÓ»óÀû ¡Èİ¡ ´Ù¾çÇÏÁö¸¸ °¨¿°ÀÌ ¹ß»ýÇÏÁö ¾Ê¾ÒÀ» °æ¿ì¿¡´Â ¹ß¿, ±âħ, È£Èí°ï¶õ, Àú»ê¼ÒÇ÷Áõ, ÈäºÎ X-ray »óÀÇ Ä§À±¹°ÀÌ ÀüÇüÀûÀ¸·Î ³ªÅ¸³´Ù.
4) Á¤½Å½Å°æ°è : µÎÅë, Á¹À½, ½Ã¾ßÈ帲, ½Ç¾îÁõ, Æí¸¶ºñ, ¸¶ºñ, °æ·Ã, È¥¼ö, Ä¡¸Å, ¸ñºÎ ¹× µÐºÎ±äÀå, ¹èºÎÅë µîÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù.
5) »ý½Ä±â°è : ¹«Á¤ÀÚÁõ, ³¼Ò±â´ÉºÎÀü, ¿ù°æºÎÀü, ºÒÀÓ, À¯»ê, žÆ, ±âÇü µîÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù.
6) Ç÷¾× : ºóÇ÷, ¹éÇ÷±¸ °¨¼ÒÁõ, Ç÷¼ÒÆÇ °¨¼ÒÁõ, ÃâÇ÷, ÆÐÇ÷Áõ, Àú °¨¸¶±Û·Îºí¸°Ç÷Áõ µîÀÇ Áõ»óÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù. ¶ÇÇÑ °ñ¼ö¾ïÁ¦, °ú¸³±¸ °¨¼ÒÁõ°ú ¹ß¿ÀÌ ³ªÅ¸³ª¸é Áï½Ã °Ë»ç¸¦ ÇàÇÏ°í ºñ°æ±¸¿ë ±¤¹üÀ§ Ç×»ýÁ¦¸¦ Åõ¿©ÇÏ´Â µî ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù.
7) °£Àå : ½ÉÇÑ °£¿°, °£ºÎÀü, °£ÀåÇØ (AST?ALT?ALPÀÇ »ó½Â), Ȳ´Þ, Áö¹æ°£, °£Á¶Á÷±«»ç, °£Á¶Á÷ ¼¶À¯È, °£°æº¯ µîÀÇ Áõ»óÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î ¿©·¯ Â÷·Ê °£±â´É °Ë»ç¸¦ ÇàÇÏ´Â µî ȯÀÚÀÇ »óŸ¦ ÃæºÐÈ÷ °üÂûÇÏ¿© ÀÌ»óÀÌ ÀÎÁ¤µÇ´Â °æ¿ì¿¡´Â Åõ¿©¸¦ ÁßÁöÇϰí ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù.
8) ½ÅÀå : ±Þ¼º ½ÅºÎÀü, ¿ä¼¼°ü ±«»ç, ÁßÁõÀÇ ½ÅÀ庴Áõ, Ç÷´¢, BUN ¶Ç´Â Å©·¹¾ÆÆ¼´ÑÄ¡ÀÇ »ó½Â µîÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î ¿©·¯ Â÷·Ê ½Å±â´É°Ë»ç¸¦ ÇÏ´Â µî ȯÀÚÀÇ »óŸ¦ ÃæºÐÈ÷ °üÂûÇϰí ÀÌ»óÀÌ ÀÎÁ¤µÇ´Â °æ¿ì¿¡´Â Åõ¿©¸¦ ÁßÁöÇϰí ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù. ¶ÇÇÑ °ñÀ°Á¾ Ä¡·á¸¦ À§ÇØ Åõ¿©µÈ °í¿ë·®ÀÇ ¸ÞÅ䯮·º¼¼ÀÌÆ®¿¡ ÀÇÇØ ±Þ¼º½ÅºÎÀüÀÌ ¹ß»ýÇÒ ¼ö ÀÖ´Ù.
9) °ú¹ÎÁõ : Ç÷¾Ð°ÇÏ, ºó¸Æ, ¸¶ºñ°¨, Àçä±â, È£Èí°ï¶õ, Èä³»°í¹Î, ³Ã.¹ßÇÑ µîÀÇ Áõ»óÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î ÀÌ·¯ÇÑ Áõ»óÀÌ ³ªÅ¸³ª¸é ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù.
10) ÇǺΠ: ½ºÆ¼ºì½¼-Á¸½ºÁõÈıº(Á¡¸·¾ÈÁõÈıº), ¸®¿¤ÁõÈıº(Áßµ¶¼ºÇ¥ÇDZ«»çÁõ)ÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î °üÂûÀ» ÃæºÐÈ÷ ÇÏ°í ±¤°ú¹ÎÁõ, ¹ß¿, ¹ßÁø, µÎµå·¯±â, °¡·Á¿ò, È«¹Ý¼ºÇÇÁø, È«¹Ý, »ö¼ÒÄ§Âø, Å»»ö, ÇÇÇϹݻóÃâÇ÷, ¿©µå¸§, Å»¸ð, ¸ð¼¼Ç÷°ü È®ÀåÁõ, Àýâ, ¾ÈÃæÇ÷, ±¸³»¿° µîÀÌ ³ªÅ¸³ª´Â °æ¿ì¿¡´Â Åõ¿©¸¦ ÁßÁöÇϰí ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù.
11) ±âŸ : ±Çۨ, ÀÌÇϼ±¿°, °á¸·¿°, ¹æ±¤¿°, °üÀý¿°, ±ÙÀ°Åë, ´ç´¢º´, °ñÁ¶¼ÛÁõ, µ¹¿¬»ç¸Á µîÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù.
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4) ÀÌ ¾à Åõ¿©¿¡ ÀÇÇÑ ½ÅÀåÇØ´Â ÁÖ·Î ÀÌ ¾àÀÇ ¼ººÐ°ú 7-hydroxy methotrexateÀÇ °áÁ¤ÀÌ ½Å¼¼´¢°ü¿¡ Ä§ÂøµÇ¾î ³ªÅ¸³ª´Â °ÍÀ̹ǷΠ¾à¹°ÀÇ °áÁ¤È¸¦ ¹æÁöÇϱâ ÀÇÇØ ´¢ÀÇ ¾ËÄ®¸®È, ÃæºÐÇÑ ¼öºÐ°ø±Þ, ´¢¸¦ ÅëÇÑ ¹è¼³ µîÀ» °í·ÁÇϰí Ç÷Áß³óµµ¿Í Å©·¹¾ÆÆ¼´ÑÄ¡ÀÇ ÃøÁ¤ µîÀ» ÅëÇÏ¿© ¼¼½ÉÇÏ°Ô °üÂûÇÑ´Ù.
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| Mechanism of Action |
Methotrexate¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Methotrexate anti-tumor activity is a result of the inhibition of folic acid reductase, leading to inhibition of DNA synthesis and inhibition of cellular replication. The mechanism involved in its activity against rheumatoid arthritis is not known.
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| Pharmacology |
Methotrexate¿¡ ´ëÇÑ Pharmacology Á¤º¸ Methotrexate is an antineoplastic anti-metabolite. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (of the cell cycle), stopping normal development and division. Methotrexate inhibits folic acid reductase which is responsible for the conversion of folic acid to tetrahydrofolic acid. At two stages in the biosynthesis of purines and at one stage in the synthesis of pyrimidines, one-carbon transfer reactions occur which require specific coenzymes synthesized in the cell from tetrahydrofolic acid. Tetrahydrofolic acid itself is synthesized in the cell from folic acid with the help of an enzyme, folic acid reductase. Methotrexate looks a lot like folic acid to the enzyme, so it binds to it quite strongly and inhibits the enzyme. Thus, DNA synthesis cannot proceed because the coenzymes needed for one-carbon transfer reactions are not produced from tetrahydrofolic acid because there is no tetrahydrofolic acid. Methotrexate selectively affects the most rapidly dividing cells (neoplastic and psoriatic cells). Methotrexate is also indicated in the management of severe, active, classical, or definite rheumatoid arthritis.
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| Protein Binding |
Methotrexate¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 50%, primarily to albumin
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| Half-life |
Methotrexate¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ Low doses: 3 to 10 hours; High doses: 8 to 15 hours.
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| Absorption |
Methotrexate¿¡ ´ëÇÑ Absorption Á¤º¸ Generally well absorbed with a mean bioavailability of about 60%.
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| Pharmacokinetics |
MethotrexateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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- °æ±¸ : ½Å¼ÓÇÏ°Ô Èí¼öµÈ´Ù.
- Àú¿ë·® (30 mg/m2)¿¡¼´Â Àß Èí¼öµÇÁö¸¸ °í¿ë·®¿¡¼´Â ºÒ¿ÏÀüÇÏ°Ô Èí¼öµÈ´Ù.
- ±ÙÀ°ÁÖ»ç : ¿ÏÀüÇÏ°Ô Èí¼öµÈ´Ù.
- ºÐÆ÷ :
- È丷»ïÃâ, º¹¼ö µîÀÇ Á¦3ÀÇ °ø°£(third space)À¸·Î ¼¼È÷ ºÐÆ÷µÇ¸ç ÀÌ °÷À¸·ÎºÎÅÍ ¼¼È÷ ºüÁ®³ª¿Â´Ù.
- ŹÝÀ» Åë°úÇϸç À¯ÁóÀ¸·Î ¼Ò·® ºÐºñµÈ´Ù.
- ³úô¼ö¾×¿¡´Â À¯È¿ Ç÷Á߳󵵿¡ µµ´ÞÇÒ ¼ö ¾øÀ¸¹Ç·Î ÁßÃ߽Űæ°èÀÇ ¿¹¹æ ¹× Ä¡·á ¸ñÀûÀ¸·Î´Â ô¼ö³»·Î Åõ¿©ÇØ¾ß ÇÑ´Ù.
- ½ÅÀå, °£¿¡¼´Â Áö¼ÓÀûÀ¸·Î ³óµµ°¡ À¯ÁöµÈ´Ù.
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- ¹Ý°¨±â :
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- Àú¿ë·® : 3-10 ½Ã°£
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- ºñ°æ±¸ Åõ¿© : 30-60ºÐ
- ¼Ò½Ç :
- »ç±¸Ã¼ ¿©°ú ¹× ´Éµ¿ ¼ö¼Û¿¡ ÀÇÇØ ÁÖ·Î ½Å¹è¼³µÈ´Ù. (44-100%)
- ¼Ò·®Àº ´ëº¯À¸·Î ¹è¼³µÈ´Ù.
- ±âŸ :
- ¼¼Æ÷µ¶¼ºÀº ¾à¹°³óµµ ¹× ¼¼Æ÷ ³ëÃâ Áö¼Ó½Ã°£¿¡ ÀÇÇØ °áÁ¤µÈ´Ù.
- Thymidylate ÇÕ¼º ÀúÇØ È¿°ú¸¦ ³ªÅ¸³»±â À§Çؼ´Â ¼¼Æ÷¿Ü ¾à¹°³óµµ°¡ 1¡¿10-8 MÀÌ µÇ¾î¾ß ÇÑ´Ù.
- ȯ¿øÇü folate (¿¹, leucovorin)¸¦ MTX Åõ¿© 48½Ã°£ À̳»¿¡ Åõ¿©ÇÏ¸é ¼¼Æ÷ ±¸Á¶(ºÎȰ)°¡ °¡´ÉÇϸç MTXÀÇ µ¶¼ºÀ» ¿ªÀü½Ãų ¼ö ÀÖ´Ù. MTX ³óµµ°¡ 10 ¥ìM ÀÌ»óÀÎ °æ¿ì¿¡´Â ȯ¿øÇü folate´Â È¿°ú ¾ø´Ù.
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| Biotransformation |
Methotrexate¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic.
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| Toxicity |
Methotrexate¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include bone marrow suppression and gastrointestinal toxicity. LD50=43mg/kg(orally in rat).
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| Drug Interactions |
Methotrexate¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Acitretin Acitretin/etretinate increases the effect and toxicity of methotrexateEtretinate Acitretin/etretinate increases the effect and toxicity of methotrexateAmoxicillin The penicillin increases the effect and toxicity of methotrexateAmpicillin The penicillin increases the effect and toxicity of methotrexateBacampicillin The penicillin increases the effect and toxicity of methotrexateCarbenicillin The penicillin increases the effect and toxicity of methotrexateCiprofloxacin Ciprofloxacin increases methotrexate toxicityCisplatin Cisplatin increases methotrexate toxicityCloxacillin The penicillin increases the effect and toxicity of methotrexateCyclosporine Cyclosporine increases the effect and toxicity of methotrexateDicloxacillin The penicillin increases the effect and toxicity of methotrexateFlucloxacillin The penicillin increases the effect and toxicity of methotrexateMethicillin Acyl-Serine The penicillin increases the effect and toxicity of methotrexateMezlocillin The penicillin increases the effect and toxicity of methotrexateNafcillin The penicillin increases the effect and toxicity of methotrexatePenicillin G The penicillin increases the effect and toxicity of methotrexatePenicillin V The penicillin increases the effect and toxicity of methotrexatePiperacillin The penicillin increases the effect and toxicity of methotrexatePivampicillin The penicillin increases the effect and toxicity of methotrexateTicarcillin The penicillin increases the effect and toxicity of methotrexateTrimethoprim Timethoprim increases methotrexate toxicityProcarbazine Increased nephrotoxicity with this combinationRofecoxib Rofecoxib increases the levels of methotrexateProbenecid Probenecid increases the effect and toxicity of methotrexateOmeprazole Omeprazole increases the levels of methotrexateHydroxychloroquine Hydroxychloroquine increases the effect and toxicity of methotrexateAspirin The salicylate increases the effect and toxicity of methotrexateBismuth Subsalicylate The salicylate increases the effect and toxicity of methotrexateSalicylate-magnesium The salicylate increases the effect and toxicity of methotrexateSalicylate-sodium The salicylate increases the effect and toxicity of methotrexateSalsalate The salicylate increases the effect and toxicity of methotrexateTrisalicylate-choline The salicylate increases the effect and toxicity of methotrexateCholestyramine Decreased levels of methotrexateDiclofenac The NSAID increases the effect and toxicity of methotrexateEtodolac The NSAID increases the effect and toxicity of methotrexateFenoprofen The NSAID increases the effect and toxicity of methotrexateFlurbiprofen The NSAID increases the effect and toxicity of methotrexateIbuprofen The NSAID increases the effect and toxicity of methotrexateIndomethacin The NSAID increases the effect and toxicity of methotrexateKetoprofen The NSAID increases the effect and toxicity of methotrexateKetorolac The NSAID increases the effect and toxicity of methotrexateMeclofenamic acid The NSAID increases the effect and toxicity of methotrexateMefenamic acid The NSAID increases the effect and toxicity of methotrexateNabumetone The NSAID increases the effect and toxicity of methotrexateNaproxen The NSAID increases the effect and toxicity of methotrexateOxaprozin The NSAID increases the effect and toxicity of methotrexatePhenylbutazone The NSAID increases the effect and toxicity of methotrexatePiroxicam The NSAID increases the effect and toxicity of methotrexateSulindac The NSAID increases the effect and toxicity of methotrexateTiaprofenic acid The NSAID increases the effect and toxicity of methotrexateTolmetin The NSAID increases the effect and toxicity of methotrexateDigoxin The antineoplasic agent decreases the effect of digoxinEthotoin The antineoplasic agent decreases the effect of hydantoinFosphenytoin The antineoplasic agent decreases the effect of hydantoinMephenytoin The antineoplasic agent decreases the effect of hydantoinPhenytoin The antineoplasic agent decreases the effect of hydantoinDoxycycline The tetracycline increases methotrexate toxicityTetracycline The tetracycline increases methotrexate toxicitySulfacytine The sulfamide increases the toxicity of methotrexateSulfadiazine The sulfamide increases the toxicity of methotrexateSulfadoxine The sulfamide increases the toxicity of methotrexateSulfamerazine The sulfamide increases the toxicity of methotrexateSulfamethazine The sulfamide increases the toxicity of methotrexateSulfamethizole The sulfamide increases the toxicity of methotrexateSulfamethoxazole The sulfamide increases the toxicity of methotrexateSulfapyridine The sulfamide increases the toxicity of methotrexateSulfathiazole The sulfamide increases the toxicity of methotrexateSulfisoxazole The sulfamide increases the toxicity of methotrexateSulfadimethoxine The sulfamide increases the toxicity of methotrexate
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
|
| Drug Target |
[Drug Target]
|
| SNP Á¤º¸ |
Name:Methotrexate (DB00563)
Interacting Gene/Enzyme:Canalicular multispecific organic anion transporter 1 (Gene symbol = ABCC2) Swissprot Q92887
SNP(s):ABCC2 IVS 23+56 (T allele)
Effect:General toxicity (gastrointestinal and hepatotoxicity)
Reference(s):Ranganathan P, Culverhouse R, Marsh S, Mody A, Scott-Horton TJ, Brasington R, Joseph A, Reddy V, Eisen S, McLeod HL: Methotrexate (MTX) pathway gene polymorphisms and their effects on MTX toxicity in Caucasian and African American patients with rheumatoid arthritis. J Rheumatol. 2008 Apr;35(4):572-9. Epub 2008 Mar 15. [PubMed]
|
| Description |
Methotrexate¿¡ ´ëÇÑ Description Á¤º¸ An antineoplastic antimetabolite with immunosuppressant properties. It is an inhibitor of tetrahydrofolate dehydrogenase and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component of DNA. [PubChem]
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| Dosage Form |
Methotrexate¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Solution IntramuscularSolution IntrathecalSolution IntravenousTablet Oral
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| Drug Category |
Methotrexate¿¡ ´ëÇÑ Drug_Category Á¤º¸ Abortifacient AgentsAbortifacient Agents, NonsteroidalAntimetabolitesAntimetabolites, AntineoplasticAntineoplastic AgentsAntirheumatic AgentsDermatologic AgentsEnzyme InhibitorsFolic Acid AntagonistsImmunosuppressive AgentsNucleic Acid Synthesis Inhibitors
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| Smiles String Canonical |
Methotrexate¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN(CC1=CN=C2N=C(N)N=C(N)C2=N1)C1=CC=C(C=C1)C(=O)NC(CCC(O)=O)C(O)=O
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| Smiles String Isomeric |
Methotrexate¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN(CC1=CN=C2N=C(N)N=C(N)C2=N1)C1=CC=C(C=C1)C(=O)N[C@@H](CCC(O)=O)C(O)=O
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| InChI Identifier |
Methotrexate¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C20H22N8O5/c1-28(9-11-8-23-17-15(24-11)16(21)26-20(22)27-17)12-4-2-10(3-5-12)18(31)25-13(19(32)33)6-7-14(29)30/h2-5,8,13H,6-7,9H2,1H3,(H,25,31)(H,29,30)(H,32,33)(H4,21,22,23,26,27)/t13-/m0/s1/f/h25,29,32H,21-22H2
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| Chemical IUPAC Name |
Methotrexate¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methylamino]benzoyl]amino]pentanedioic acid
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| Drug-Induced Toxicity Related Proteins |
METHOTREXATE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Thymidine kinase Drug:methotrexate Toxicity:apoptotic cell death and epidermal hyperplasia. [¹Ù·Î°¡±â] Replated Protein:Pulmonary surfactant-associated protein D Drug:methotrexate Toxicity:lung injury. [¹Ù·Î°¡±â] Replated Protein:Glutamate oxaloacetate transaminase Drug:methotrexate Toxicity:increase in the death rate. [¹Ù·Î°¡±â] Replated Protein:Cellular tumor antigen p53 Drug:Methotrexate Toxicity:induce apoptotic cell death. [¹Ù·Î°¡±â] METHOTREXATE (MTX) ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Uracil-DNA glycosylase Drug:methotrexate (MTX) Toxicity:MTX-induced genotoxic damage. [¹Ù·Î°¡±â]
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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