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| Pharmacokinetics |
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| º¸°ü»ó ÁÖÀÇ |
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| Á¶Á¦½Ã ÁÖÀÇ |
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 | ÇмúÁ¤º¸ |
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| Ç׸ñ |
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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]
¿¬·É´ë±Ý±â :
°í½ÃµÈ ¿¬·É±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
[¿¬·É´ë±Ý±â»ó¼¼°Ë»ö]
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| Mechanism of Action |
Cisapride¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Cisapride acts through the stimulation of the serotonin 5-HT4 receptors which increases acetylcholine release in the enteric nervous system (specifically the myenteric plexus). This results in increased tone and amplitude of gastric (especially antral) contractions, relaxation of the pyloric sphincter and the duodenal bulb, and increased peristalsis of the duodenum and jejunum resulting in accelerated gastric emptying and intestinal transit.
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| Pharmacology |
Cisapride¿¡ ´ëÇÑ Pharmacology Á¤º¸ Cisapride is a parasympathomimetic which acts as a serotonin 5-HT4 agonist. Stimulation of the serotonin receptors increases acetylcholine release in the enteric nervous system. Cisapride stimulates motility of the upper gastrointestinal tract without stimulating gastric, biliary, or pancreatic secretions. Cisapride increases the tone and amplitude of gastric (especially antral) contractions, relaxes the pyloric sphincter and the duodenal bulb, and increases peristalsis of the duodenum and jejunum resulting in accelerated gastric emptying and intestinal transit. It increases the resting tone of the lower esophageal sphincter. It has little, if any, effect on the motility of the colon or gallbladder. Cisapride does not induce muscarinic or nicotinic receptor stimulation, nor does it inhibit acetylcholinesterase activity.
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| Metabolism |
Cisapride¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)
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| Protein Binding |
Cisapride¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 97.5%
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| Half-life |
Cisapride¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 6-12 hours
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| Absorption |
Cisapride¿¡ ´ëÇÑ Absorption Á¤º¸ Cisapride is rapidly absorbed after oral administration, with an absolute bioavailability of 35-40%.
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| Pharmacokinetics |
CisaprideÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ë¹ßÇö½Ã°£ : 0.5-1 ½Ã°£
- »ýü³»ÀÌ¿ë·ü : 35-40%
- ºÐÆ÷ : ºÐÆ÷¿ëÀû : ¾à 180 L
- ´Ü¹é°áÇÕ : 97.5-98%
- ´ë»ç : ÁÖ·Î CYP 3A4¿¡ ÀÇÇØ ´ëºÎºÐ norcisapride·Î ´ë»çµÊ
- ¹Ý°¨±â : 6-12 ½Ã°£
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 1-1.5 ½Ã°£
- ¼Ò½Ç : ÁÖ·Î ´ë»çü·Î¼ ´¢ ¹× ´ëº¯À¸·Î ¹è¼³µÊ (¹Ìº¯Èü·Î´Â 10% ¹Ì¸¸)
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| Biotransformation |
Cisapride¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. Extensively metabolized via cytochrome P450 3A4 enzyme.
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| Toxicity |
Cisapride¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
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| Drug Interactions |
Cisapride¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Acetophenazine Increased risk of cardiotoxicity and arrhythmiasAmiodarone Increased risk of cardiotoxicity and arrhythmiasAmitriptyline Increased risk of cardiotoxicity and arrhythmiasAmoxapine Increased risk of cardiotoxicity and arrhythmiasAmprenavir Amprenavir increases the effect and toxicity of cisaprideAnisindione Increases the anticoagulant effectAprepitant Increased risk of cardiotoxicity and arrhythmiasAstemizole Increased risk of cardiotoxicity and arrhythmiasAtazanavir Increased risk of cardiotoxicity and arrhythmiasBepridil Increased risk of cardiotoxicity and arrhythmiasBretylium Increased risk of cardiotoxicity and arrhythmiasChlorpromazine Increased risk of cardiotoxicity and arrhythmiasClarithromycin Increased risk of cardiotoxicity and arrhythmiasClomipramine Increased risk of cardiotoxicity and arrhythmiasDelavirdine Increased risk of cardiotoxicity and arrhythmiasDesipramine Increased risk of cardiotoxicity and arrhythmiasDicumarol Increases the anticoagulant effectDihydroquinidine barbiturate Increased risk of cardiotoxicity and arrhythmiasDiltiazem Diltiazem increases the levels of cisaprideDisopyramide Increased risk of cardiotoxicity and arrhythmiasDoxepin Increased risk of cardiotoxicity and arrhythmiasEfavirenz Increased risk of cardiotoxicity and arrhythmiasEncainide Increased risk of cardiotoxicity and arrhythmiasErythromycin Increased risk of cardiotoxicity and arrhythmiasEthopropazine Increased risk of cardiotoxicity and arrhythmiasFexofenadine Increased risk of cardiotoxicity and arrhythmiasFlecainide Increased risk of cardiotoxicity and arrhythmiasFluconazole Increased risk of cardiotoxicity and arrhythmiasFluphenazine Increased risk of cardiotoxicity and arrhythmiasFosamprenavir Amprenavir increases the effect and toxicity of cisaprideImipramine Increased risk of cardiotoxicity and arrhythmiasIndinavir Increased risk of cardiotoxicity and arrhythmiasItraconazole Increased risk of cardiotoxicity and arrhythmiasJosamycin Increased risk of cardiotoxicity and arrhythmiasKetoconazole Increased risk of cardiotoxicity and arrhythmiasMaprotiline Increased risk of cardiotoxicity and arrhythmiasMesoridazine Increased risk of cardiotoxicity and arrhythmiasMethdilazine Increased risk of cardiotoxicity and arrhythmiasNelfinavir Increased risk of cardiotoxicity and arrhythmiasMibefradil Mibefradil increases levels of cisaprideNefazodone Nefazodone increases serum levels of cisaprideAcenocoumarol Increases the anticoagulant effectNifedipine Increases the effect and toxicity of nifedipineNortriptyline Increased risk of cardiotoxicity and arrhythmiasPerphenazine Increased risk of cardiotoxicity and arrhythmiasPosaconazole Contraindicated co-administrationProcainamide Increased risk of cardiotoxicity and arrhythmiasProchlorperazine Increased risk of cardiotoxicity and arrhythmiasPromazine Increased risk of cardiotoxicity and arrhythmiasPromethazine Increased risk of cardiotoxicity and arrhythmiasPropafenone Increased risk of cardiotoxicity and arrhythmiasPropiomazine Increased risk of cardiotoxicity and arrhythmiasProtriptyline Increased risk of cardiotoxicity and arrhythmiasQuinidine Increased risk of cardiotoxicity and arrhythmiasQuinidine barbiturate Increased risk of cardiotoxicity and arrhythmiasQuinupristin This combination presents an increased risk of toxicityRitonavir Increased risk of cardiotoxicity and arrhythmiasSaquinavir Increased risk of cardiotoxicity and arrhythmiasSotalol Increased risk of cardiotoxicity and arrhythmiasTelithromycin Increased risk of cardiotoxicity and arrhythmiasTerfenadine Increased risk of cardiotoxicity and arrhythmiasThiethylperazine Increased risk of cardiotoxicity and arrhythmiasThioridazine Increased risk of cardiotoxicity and arrhythmiasTrifluoperazine Increased risk of cardiotoxicity and arrhythmiasTriflupromazine Increased risk of cardiotoxicity and arrhythmiasTrimeprazine Increased risk of cardiotoxicity and arrhythmiasTrimipramine Increased risk of cardiotoxicity and arrhythmiasTroleandomycin Increased risk of cardiotoxicity and arrhythmiasVoriconazole Increased risk of cardiotoxicity and arrhythmiasWarfarin Increases the anticoagulant effectZafirlukast Increased risk of cardiotoxicity and arrhythmiasZiprasidone Increased risk of cardiotoxicity and arrhythmiasIbutilide Increased risk of cardiotoxicity and arrhythmiasMethotrimeprazine Increased risk of cardiotoxicity and arrhythmias
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Cisapride¿¡ ´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
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| Food Interaction |
Cisapride¿¡ ´ëÇÑ Food Interaction Á¤º¸ Increases absorption, take 30 minutes before a meal.Grapefruit and grapefruit juice should be avoided throughout treatment, grapefruit can significantly increase serum levels of this product.
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| Drug Target |
[Drug Target]
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| Description |
Cisapride¿¡ ´ëÇÑ Description Á¤º¸ In many countries (including Canada) cisapride has been either withdrawn or has had its indications limited due to reports about long QT syndrome due to cisapride, which predisposes to arrhythmias. The FDA issued a warning letter regarding this risk to health care professionals and patients.
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| Dosage Form |
Cisapride¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Suspension OralTablet Oral
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| Drug Category |
Cisapride¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Ulcer AgentsGastrointestinal AgentsProkinetic AgentsSerotonin Agonists
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| Smiles String Canonical |
Cisapride¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1CN(CCCOC2=CC=C(F)C=C2)CCC1NC(=O)C1=CC(Cl)=C(N)C=C1OC
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| Smiles String Isomeric |
Cisapride¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CO[C@H]1CN(CCCOC2=CC=C(F)C=C2)CC[C@@H]1NC(=O)C1=CC(Cl)=C(N)C=C1OC
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| InChI Identifier |
Cisapride¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C23H29ClFN3O4/c1-30-21-13-19(26)18(24)12-17(21)23(29)27-20-8-10-28(14-22(20)31-2)9-3-11-32-16-6-4-15(25)5-7-16/h4-7,12-13,20,22H,3,8-11,14,26H2,1-2H3,(H,27,29)/f/h27H
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| Chemical IUPAC Name |
Cisapride¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 4-amino-5-chloro-N-[1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-yl]-2-methoxybenzamide
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| Drug-Induced Toxicity Related Proteins |
CISAPRIDE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:HERG Drug:cisapride Toxicity:torsade de pointes. [¹Ù·Î°¡±â] Replated Protein:Misshapen-like kinase(Mink) Drug:cisapride Toxicity:torsade de pointes. [¹Ù·Î°¡±â] Replated Protein:Potassium voltage-gated channel subfamily KQT member 1 (KvLQT1) Drug:cisapride Toxicity:torsade de pointes. [¹Ù·Î°¡±â]
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ÃÖ±ÙÁ¤º¸¼öÁ¤ÀÏ 2021-12-09
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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
Ã¥ÀÓÀ» ÁöÁö ¾Ê½À´Ï´Ù. ÀÚ¼¼ÇÑ ³»¿ëÀº ¡°Ã¥ÀÓÀÇ ÇÑ°è ¹× ¹ýÀû°íÁö¡±¸¦ ÂüÁ¶ÇØ ÁֽʽÿÀ.
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. CISAPRIDE[GGT Increase][Composite Activity](Score) I(Marginal) 0(Active) 0[Alkaline Phosphatase Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.2[SGOT Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.3[SGPT Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.4[LDH Increase](Activity Score) I(Number of Rpts) <4(Index value) 0.1[GGT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0.2
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