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[A22551191]
[º¸ÇèÄڵ忡 µû¸¥ ¾àǰ±âº»Á¤º¸ Á÷Á¢Á¶È¸]
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Á¤Á¦¼ö (1x25mg / kg °æ¿ì) |
üÁß(kg) |
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| 22-26 |
1 |
20-25/26 |
3/4 |
| 27-33 |
1 1/4 |
26/27-33 |
1 |
| 34-38 |
1 1/2 |
34-41 |
1 1/4 |
| 39-44 |
1 3/4 |
42-48 |
1 1/2 |
| 45-50 |
2 |
49-56 |
1 3/4 |
| 51-56 |
2 1/4 |
57-63 |
2 |
| 57-62 |
2 1/2 |
64-70 |
2 1/4 |
| 63-68 |
2 3/4 |
71-78 |
2 1/2 |
| 69-75 |
3 |
79-81 |
2 3/4 |
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| Mechanism of Action |
Praziquantel¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Praziquantel works by causing severe spasms and paralysis of the worms' muscles. This paralysis is accompanied - and probably caused - by a rapid Ca 2+ influx inside the schistosome. Morphological alterations are another early effect of praziquantel. These morphological alterations are accompanied by an increased exposure of schistosome antigens at the parasite surface. The worms are then either completely destroyed in the intestine or passed in the stool. An interesting quirk of praziquantel is that it is relatively ineffective against juvenile schistosomes. While initially effective, effectiveness against schistosomes decreases until it reaches a minimum at 3-4 weeks. Effectiveness then increases again until it is once again fully effective at 6-7 weeks. Glutathione S-transferase (GST), an essential detoxification enzyme in parasitic helminths, is a major vaccine target and a drug target against schistosomiasis.
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| Pharmacology |
Praziquantel¿¡ ´ëÇÑ Pharmacology Á¤º¸ Praziquantel is an anthelmintic used in most schistosome and many cestode infestations. Praziquantel effects the permeability of the cell membrane resulting in the contraction of schistosomes. The drug further causes vacuolization and disintegration of the schistosome tegument. The effect is more marked on adult worms compared to young worms. An increased calcium influx may play an important role. Secondary effects are inhibition of glucose uptake, lowering of glycogen levels and stimulation of lactate release. The action of praziquantel is limited very specifically to trematodes and cestodes; nematodes (including filariae) are not affected.
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| Protein Binding |
Praziquantel¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 80 to 85%
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| Half-life |
Praziquantel¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 0.8-1.5 hours (in serum)
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| Absorption |
Praziquantel¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly absorbed (80%)
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| Pharmacokinetics |
PraziquantelÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : °æ±¸ : 80% ±îÁö
- ºÐÆ÷ : ³úô¼ö¾×ÀÇ ³óµµ°¡ Ç÷Áß³óµµÀÇ 14-20% Á¤µµ, À¯Áó ºÐºñ
- ´Ü¹é°áÇÕ : 80% ±îÁö
- ´ë»ç : ÃÊȸÅë°úÈ¿°ú¸¦ ¸¹ÀÌ ¹Þ´Â´Ù.
- ¹Ý°¨±â :
- Praziquantel : 0.8-1.5 ½Ã°£
- ´ë»çü : 4.5 ½Ã°£
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 1-3 ½Ã°£ À̳»
- ¼Ò½Ç : ½Å¹è¼³, 99%°¡ ´ë»çü·Î ¹è¼³
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| Biotransformation |
Praziquantel¿¡ ´ëÇÑ Biotransformation Á¤º¸ renal
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| Toxicity |
Praziquantel¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
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| Drug Interactions |
Praziquantel¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Carbamazepine Markedly lower praziquantel levelsChloroquine Markedly lower praziquantel levelsPhenytoin Markedly lower praziquantel levelsRifampin Significant decrease in praziquantel level
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Praziquantel¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take with food.Grapefruit and grapefruit juice should be avoided throughout treatment. Grapefruit can increase serum levels of this product.
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| Drug Target |
[Drug Target]
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| Description |
Praziquantel¿¡ ´ëÇÑ Description Á¤º¸ An anthelmintic used in most schistosome and many cestode infestations. [PubChem]
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| Dosage Form |
Praziquantel¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
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| Drug Category |
Praziquantel¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anthelmintics
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| Smiles String Canonical |
Praziquantel¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ O=C1CN(CC2N1CCC1=CC=CC=C21)C(=O)C1CCCCC1
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| Smiles String Isomeric |
Praziquantel¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ O=C1CN(C[C@H]2N1CCC1=CC=CC=C21)C(=O)C1CCCCC1
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| InChI Identifier |
Praziquantel¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C19H24N2O2/c22-18-13-20(19(23)15-7-2-1-3-8-15)12-17-16-9-5-4-6-14(16)10-11-21(17)18/h4-6,9,15,17H,1-3,7-8,10-13H2
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| Chemical IUPAC Name |
Praziquantel¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-(cyclohexanecarbonyl)-3,6,7,11b-tetrahydro-1H-pyrazino[6,1-a]isoquinolin-4-one
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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. PRAZIQUANTEL[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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