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cisapride 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| sulpiride derivatives and analogues | 660 | 81098-60-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A substituted benzamide used for its prokinetic properties. It is used in the management of gastroesophageal reflux disease, functional dyspepsia, and other disorders associated with impaired gastrointestinal motility. (Martindale The Extra Pharmacopoeia, 31st ed)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 30 | mg | O |
| 30 | mg | R |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.00 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 2.85 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 40 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.20 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.50 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.02 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 11.70 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 1.476 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | High | 1 | |
| rat-kpuu-brain | Rat brain Kpuu | 0.038 | % | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 29, 1993 | FDA |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Electrocardiogram QT prolonged | 774.61 | 66.77 | 145 | 250 | 72311 | 90555741 |
| Hypoventilation | 89.01 | 66.77 | 16 | 379 | 5280 | 90622772 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Electrocardiogram QT prolonged | 373.32 | 85.49 | 68 | 60 | 47877 | 42573330 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Electrocardiogram QT prolonged | 1082.88 | 57.02 | 209 | 339 | 108751 | 110480000 |
| Hypoventilation | 80.12 | 57.02 | 16 | 532 | 8065 | 110580686 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A03FA02 | ALIMENTARY TRACT AND METABOLISM DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS PROPULSIVES Propulsives |
| CHEBI has role | CHEBI:35941 | serotonergic agonist |
| CHEBI has role | CHEBI:49201 | anti-ulcer drug |
| CHEBI has role | CHEBI:55324 | gastrointestinal drug |
| MeSH PA | D000897 | Anti-Ulcer Agents |
| MeSH PA | D005765 | Gastrointestinal Agents |
| MeSH PA | D017366 | Serotonin Receptor Agonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018490 | Serotonin Agents |
Related Drugs by ATC class:
A03FA Propulsives 9 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Gastroesophageal reflux disease | indication | 235595009 | DOID:8534 |
| Gastroparesis | off-label use | 235675006 | |
| Hypophosphatemia | contraindication | 4996001 | |
| Hypocalcemia | contraindication | 5291005 | |
| Hypokalemia | contraindication | 43339004 | |
| Ventricular arrhythmia | contraindication | 44103008 | |
| Mechanical ileus | contraindication | 46420000 | |
| Chronic heart failure | contraindication | 48447003 | |
| Bradycardia | contraindication | 48867003 | |
| Gastrointestinal hemorrhage | contraindication | 74474003 | |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Prolonged QT interval | contraindication | 111975006 | |
| Hypomagnesemia | contraindication | 190855004 | |
| Angina pectoris | contraindication | 194828000 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Disorder of electrolytes | contraindication | 237840007 | |
| Respiratory insufficiency | contraindication | 409623005 | |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
| Congenital long QT syndrome | contraindication | 442917000 | |
| Severe dehydration | contraindication | 450316000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.79 | acidic |
| pKa2 | 7.8 | Basic |
| pKa3 | 1.0 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 4 | GPCR | AGONIST | Ki | 7.54 | CHEMBL | CHEMBL | |||
| D(1A) dopamine receptor | GPCR | IC50 | 5.77 | CHEMBL | |||||
| D(2) dopamine receptor | GPCR | IC50 | 6.64 | CHEMBL | |||||
| Alpha-2A adrenergic receptor | GPCR | Ki | 6.18 | DRUG MATRIX | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 6.38 | DRUG MATRIX | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 8.19 | CHEMBL | |||||
| Cytochrome P450 3A4 | Enzyme | IC50 | 6.52 | DRUG MATRIX | |||||
| Sodium-dependent serotonin transporter | Transporter | Ki | 6.69 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 6.10 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 8.96 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 7.15 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.40 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | EC50 | 5.70 | WOMBAT-PK | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 6.28 | DRUG MATRIX | |||||
| D(3) dopamine receptor | GPCR | Ki | 7.31 | DRUG MATRIX | |||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 6.95 | DRUG MATRIX | |||||
| Cytochrome P450 2D6 | Enzyme | IC50 | 7.16 | DRUG MATRIX | |||||
| Alpha-1D adrenergic receptor | GPCR | Ki | 7.31 | DRUG MATRIX | |||||
| 3-hydroxy-3-methylglutaryl-coenzyme A reductase | Enzyme | IC50 | 5.47 | DRUG MATRIX | |||||
| Serotonin 3 (5-HT3) receptor | Ion channel | Ki | 6.82 | CHEMBL | |||||
| Alpha-1B adrenergic receptor | GPCR | Ki | 8.06 | DRUG MATRIX | |||||
| Membrane-associated progesterone receptor component 1 | Membrane receptor | Ki | 6.96 | DRUG MATRIX | |||||
| Alpha-1A adrenergic receptor | GPCR | Ki | 7.52 | CHEMBL | |||||
| D(2) dopamine receptor | GPCR | Ki | 6.64 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | AGONIST | Ki | 5.80 | IUPHAR | ||||
| D(1A) dopamine receptor | GPCR | Ki | 5.77 | CHEMBL | |||||
| Alpha-2A adrenergic receptor | GPCR | Ki | 7.52 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 4 | GPCR | AGONIST | Ki | 8 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 8.14 | CHEMBL | |||||
| Serotonin 3 (5-HT3) receptor | Ion channel | Ki | 7.02 | CHEMBL | |||||
| Serotonin 1 (5-HT1) receptor | GPCR | IC50 | 5.35 | CHEMBL | |||||
| Adrenergic receptor alpha-2 | GPCR | Ki | 5.35 | CHEMBL | |||||
| Serotonin 2 (5-HT2) receptor | GPCR | Ki | 8.21 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 4 | GPCR | Ki | 7.84 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 4 | GPCR | AGONIST | Ki | 7.50 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| D00274 | KEGG_DRUG |
| 260779-88-2 | SECONDARY_CAS_RN |
| 151323 | RXNORM |
| C0072916 | UMLSCUI |
| CHEBI:3720 | CHEBI |
| CHEMBL1729 | ChEMBL_ID |
| CHEMBL1200788 | ChEMBL_ID |
| D020117 | MESH_DESCRIPTOR_UI |
| DB00604 | DRUGBANK_ID |
| 240 | IUPHAR_LIGAND_ID |
| 5338 | INN_ID |
| UVL329170W | UNII |
| 6917698 | PUBCHEM_CID |
| 3864 | MMSL |
| 4453 | MMSL |
| 4454 | MMSL |
| d03166 | MMSL |
| 003705 | NDDF |
| 003808 | NDDF |
| 30317002 | SNOMEDCT_US |
| 387164008 | SNOMEDCT_US |
| 725787005 | SNOMEDCT_US |
| 4020825 | VANDF |
| UVL329170W | INXIGHT DRUGS |
Pharmaceutical products:
None