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| Mechanism of Action |
Hydromorphone¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Hydromorphone is a narcotic analgesic; its principal therapeutic effect is relief of pain. Hydromorphone interacts predominantly with the opioid mu-receptors. These mu-binding sites are discretely distributed in the human brain, with high densities in the posterior amygdala, hypothalamus, thalamus, nucleus caudatus, putamen, and certain cortical areas. They are also found on the terminal axons of primary afferents within laminae I and II (substantia gelatinosa) of the spinal cord and in the spinal nucleus of the trigeminal nerve. In clinical settings, Hydromorphone exerts its principal pharmacological effect on the central nervous system and gastrointestinal tract. Hydromorphone also binds with kappa-receptors which are thought to mediate spinal analgesia, miosis and sedation.
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| Pharmacology |
Hydromorphone¿¡ ´ëÇÑ Pharmacology Á¤º¸ Hydromorphone is a hydrogenated ketone derivative of morphine that acts as a narcotic analgesic. It has a shorter duration of action than morphine. Hydromorphone is approximately 8 times more potent on a milligram basis than morphine. In addition, hydromorphone is better absorbed orally than is morphine. In clinical settings, Hydromorphone exerts its principal pharmacological effect on the central nervous system and gastrointestinal tract. Its primary actions of therapeutic value are analgesia and sedation. Hydromorphone appears to increase the patient's tolerance for pain and to decrease discomfort, although the presence of the pain itself may still be recognized. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Opioids also produce respiratory depression by direct action on brain stem respiratory centers.
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| Protein Binding |
Hydromorphone¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 20%
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| Half-life |
Hydromorphone¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2.6 hours (oral); 18.6 hours for sustained release Palladone
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| Absorption |
Hydromorphone¿¡ ´ëÇÑ Absorption Á¤º¸ Better absorbed orally than morphine
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| Pharmacokinetics |
Hydromorphone HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÁøÅëÈ¿°ú ¹ßÇö½Ã°£ : 15-30ºÐ À̳»
- ÃÖ´ëÈ¿°ú ¹ßÇö½Ã°£ : 0.5-1.5 ½Ã°£ À̳»
- ÀÛ¿ëÁö¼Ó½Ã°£ : 4-5 ½Ã°£
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- »ýü³»ÀÌ¿ë·ü : 62%
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- ¼Ò½Ç : ´¢¸¦ ÅëÇØ glucuronide Æ÷ÇÕü·Î ¹è¼³µÊ.
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| Biotransformation |
Hydromorphone¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic. After absorption hydromorphone is metabolized by the liver to the glucuronide conjugate which is then excreted in the urine. Hydromorphone is metabolized to the major metabolites hydromorphone-3-glucuronide, hydromorphone-3-glucoside and dihydroisomorphine-6-glucuronide.
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| Toxicity |
Hydromorphone¿¡ ´ëÇÑ Toxicity Á¤º¸ Hydromorphone is a schedule II narcotic which can lead to physical dependence or addiction. High doses lead to respiratory depression, nausea, and vomiting. Overdoses lead to extreme somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, and sometimes bradycardia and hypotension. In severe overdosage, apnea, circulatory collapse, cardiac arrest and death may occur.
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| Drug Interactions |
Hydromorphone¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Cimetidine Cimetidine increases the effect of the narcoticNaltrexone Naltrexone may precipitate a withdrawal syndrome in opioid-dependent individual
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Drug Target |
[Drug Target]
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| Description |
Hydromorphone¿¡ ´ëÇÑ Description Á¤º¸ An opioid analgesic made from morphine and used mainly as an analgesic. It has a shorter duration of action than morphine. [PubChem]
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| Drug Category |
Hydromorphone¿¡ ´ëÇÑ Drug_Category Á¤º¸ Analgesics, OpioidNarcotics
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| Smiles String Canonical |
Hydromorphone¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN1CCC23C4CCC(=O)C2OC2=C(O)C=CC(CC14)=C32
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| Smiles String Isomeric |
Hydromorphone¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN1CC[C@@]23[C@H]4CCC(=O)[C@@H]2OC2=C(O)C=CC(C[C@@H]14)=C32
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| InChI Identifier |
Hydromorphone¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C17H19NO3/c1-18-7-6-17-10-3-5-13(20)16(17)21-15-12(19)4-2-9(14(15)17)8-11(10)18/h2,4,10-11,16,19H,3,5-8H2,1H3/t10-,11+,16-,17-/m0/s1
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| Chemical IUPAC Name |
Hydromorphone¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 4,5 alpha-epoxy-3-hydroxy-17-methyl morphinan-6-one
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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
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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. HYDROMORPHONE[GGT Increase][Composite Activity](Score) I(Marginal) 0(Active) 0[Alkaline Phosphatase Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[SGOT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[SGPT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[LDH Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[GGT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0
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