prucalopride 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| sulpiride derivatives and analogues | 3502 | 179474-81-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a 5-HT4 agonist enterokinetic compound
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 2 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 8.73 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 4.55 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.70 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 22.50 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 97 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 15, 2009 | EMA | ||
| Dec. 14, 2018 | FDA | SHIRE DEV LLC |
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 |
|---|---|---|---|---|---|---|
| Pituitary tumour benign | 132.91 | 28.81 | 28 | 2840 | 1967 | 63484187 |
| Hyperprolactinaemia | 94.22 | 28.81 | 24 | 2844 | 3876 | 63482278 |
| Secondary adrenocortical insufficiency | 83.49 | 28.81 | 18 | 2850 | 1410 | 63484744 |
| Head banging | 72.06 | 28.81 | 13 | 2855 | 403 | 63485751 |
| Screaming | 54.53 | 28.81 | 15 | 2853 | 3247 | 63482907 |
| Psychiatric symptom | 47.56 | 28.81 | 15 | 2853 | 5208 | 63480946 |
| No adverse event | 44.40 | 28.81 | 26 | 2842 | 41379 | 63444775 |
| Arthropod bite | 41.33 | 28.81 | 15 | 2853 | 7963 | 63478191 |
| Headache | 41.27 | 28.81 | 89 | 2779 | 633152 | 62853002 |
| Anger | 38.17 | 28.81 | 16 | 2852 | 12440 | 63473714 |
| Crying | 37.05 | 28.81 | 19 | 2849 | 23324 | 63462830 |
| Wrist fracture | 36.83 | 28.81 | 16 | 2852 | 13571 | 63472583 |
| Therapeutic drug monitoring analysis not performed | 36.01 | 28.81 | 9 | 2859 | 1343 | 63484811 |
| Depressed mood | 34.77 | 28.81 | 22 | 2846 | 40169 | 63445985 |
| Feeling jittery | 33.79 | 28.81 | 15 | 2853 | 13388 | 63472766 |
| Heliotrope rash | 33.41 | 28.81 | 6 | 2862 | 181 | 63485973 |
| Adrenal insufficiency | 32.60 | 28.81 | 16 | 2852 | 17899 | 63468255 |
| Suicidal ideation | 32.46 | 28.81 | 25 | 2843 | 62396 | 63423758 |
| Poikiloderma | 32.20 | 28.81 | 6 | 2862 | 223 | 63485931 |
| Transferrin decreased | 31.77 | 28.81 | 6 | 2862 | 240 | 63485914 |
| Inability to afford medication | 31.09 | 28.81 | 9 | 2859 | 2338 | 63483816 |
| Hypoacusis | 30.82 | 28.81 | 17 | 2851 | 24134 | 63462020 |
| Inappropriate schedule of product administration | 30.44 | 28.81 | 30 | 2838 | 103935 | 63382219 |
| Iron binding capacity total decreased | 29.86 | 28.81 | 6 | 2862 | 332 | 63485822 |
| Insurance issue | 29.81 | 28.81 | 11 | 2857 | 6110 | 63480044 |
| Mental disorder | 29.70 | 28.81 | 17 | 2851 | 25902 | 63460252 |
| Vasculitis | 29.41 | 28.81 | 15 | 2853 | 18194 | 63467960 |
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Pituitary tumour benign | 133.80 | 31.02 | 28 | 2675 | 2548 | 79739137 |
| Hyperprolactinaemia | 96.75 | 31.02 | 24 | 2679 | 4652 | 79737033 |
| Secondary adrenocortical insufficiency | 75.25 | 31.02 | 18 | 2685 | 2996 | 79738689 |
| Head banging | 65.85 | 31.02 | 12 | 2691 | 529 | 79741156 |
| Screaming | 56.02 | 31.02 | 15 | 2688 | 3918 | 79737767 |
| Headache | 49.46 | 31.02 | 83 | 2620 | 653689 | 79087996 |
| Psychiatric symptom | 43.29 | 31.02 | 14 | 2689 | 7021 | 79734664 |
| Arthropod bite | 40.74 | 31.02 | 14 | 2689 | 8457 | 79733228 |
| Wrist fracture | 39.66 | 31.02 | 15 | 2688 | 11906 | 79729779 |
| Therapeutic drug monitoring analysis not performed | 35.37 | 31.02 | 9 | 2694 | 1927 | 79739758 |
| Feeling jittery | 35.06 | 31.02 | 14 | 2689 | 12827 | 79728858 |
| Heliotrope rash | 34.67 | 31.02 | 6 | 2697 | 196 | 79741489 |
| Crying | 33.14 | 31.02 | 16 | 2687 | 23027 | 79718658 |
| Anger | 31.15 | 31.02 | 14 | 2689 | 17148 | 79724537 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A06AX05 | ALIMENTARY TRACT AND METABOLISM DRUGS FOR CONSTIPATION DRUGS FOR CONSTIPATION Other drugs for constipation |
| MeSH PA | D005765 | Gastrointestinal Agents |
| MeSH PA | D054368 | Laxatives |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D058828 | Serotonin 5-HT4 Receptor Agonists |
| MeSH PA | D018490 | Serotonin Agents |
| MeSH PA | D017366 | Serotonin Receptor Agonists |
| FDA MoA | N0000193870 | Serotonin 4 Receptor Agonists |
| FDA EPC | N0000193871 | Serotonin-4 Receptor Agonist |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Constipation | indication | 14760008 | DOID:2089 |
| Perforation of intestine | contraindication | 56905009 | DOID:2074 |
| Ulcerative colitis | contraindication | 64766004 | DOID:8577 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.83 | acidic |
| pKa2 | 8.57 | Basic |
| pKa3 | 1.07 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 1MG BASE | MOTEGRITY | TAKEDA PHARMS USA | N210166 | Dec. 14, 2018 | RX | TABLET | ORAL | Dec. 14, 2023 | NEW CHEMICAL ENTITY |
| EQ 2MG BASE | MOTEGRITY | TAKEDA PHARMS USA | N210166 | Dec. 14, 2018 | RX | TABLET | ORAL | Dec. 14, 2023 | NEW CHEMICAL ENTITY |
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 | 8.60 | CHEMBL | DRUG LABEL | |||
| D(4) dopamine receptor | GPCR | Ki | 5.63 | PDSP | |||||
| 5-hydroxytryptamine receptor 3A | Ion channel | Ki | 5.40 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 4 | GPCR | EC50 | 7.58 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D09205 | KEGG_DRUG |
| 179474-85-2 | SECONDARY_CAS_RN |
| 4038160 | VANDF |
| CHEBI:135552 | CHEBI |
| CHEMBL117287 | ChEMBL_ID |
| CHEMBL2105748 | ChEMBL_ID |
| C406662 | MESH_SUPPLEMENTAL_RECORD_UI |
| 243 | IUPHAR_LIGAND_ID |
| 7702 | INN_ID |
| DB06480 | DRUGBANK_ID |
| 0A09IUW5TP | UNII |
| 2107309 | RXNORM |
| 26947 | MMSL |
| 304089 | MMSL |
| d07541 | MMSL |
| 013402 | NDDF |
| 013403 | NDDF |
| 1149428003 | SNOMEDCT_US |
| 699273008 | SNOMEDCT_US |
| 774192009 | SNOMEDCT_US |
| C0913506 | UMLSCUI |
| 3052762 | PUBCHEM_CID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| MOTEGRITY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54092-546 | TABLET, FILM COATED | 1 mg | ORAL | NDA | 29 sections |
| MOTEGRITY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54092-546 | TABLET, FILM COATED | 1 mg | ORAL | NDA | 29 sections |
| MOTEGRITY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54092-547 | TABLET, FILM COATED | 2 mg | ORAL | NDA | 29 sections |
| MOTEGRITY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54092-547 | TABLET, FILM COATED | 2 mg | ORAL | NDA | 29 sections |