pirenzepine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tricyclic compounds | 2200 | 28797-61-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An antimuscarinic agent that inhibits gastric secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular, and urinary function. It promotes the healing of duodenal ulcers and due to its cytoprotective action is beneficial in the prevention of duodenal ulcer recurrence. It also potentiates the effect of other antiulcer agents such as CIMETIDINE and RANITIDINE. It is generally well tolerated by patients.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
| 20 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 50 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 43 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 7.11 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 14 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.71 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 2.77 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 11.10 hours | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.91 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Approvals:
None
FDA Adverse Event Reporting System (Female)
None
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 |
|---|---|---|---|---|---|---|
| Differential white blood cell count abnormal | 73.90 | 68.92 | 13 | 618 | 2064 | 79741693 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A02BX03 | ALIMENTARY TRACT AND METABOLISM DRUGS FOR ACID RELATED DISORDERS DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) Other drugs for peptic ulcer and gastro-oesophageal reflux disease (GORD) |
| MeSH PA | D000897 | Anti-Ulcer Agents |
| MeSH PA | D018678 | Cholinergic Agents |
| MeSH PA | D018680 | Cholinergic Antagonists |
| MeSH PA | D005765 | Gastrointestinal Agents |
| MeSH PA | D018727 | Muscarinic Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| CHEBI has role | CHEBI:48876 | muscarinic antagonists |
| CHEBI has role | CHEBI:49201 | anti-ulcer drugs |
| CHEBI has role | CHEBI:53784 | antispasmodics |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Peptic ulcer | indication | 13200003 | DOID:750 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.89 | acidic |
| pKa2 | 7.77 | Basic |
| pKa3 | 2.58 | Basic |
| pKa4 | 1.96 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M1 | GPCR | ANTAGONIST | Ki | 7.68 | WOMBAT-PK | IUPHAR | |||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 6.76 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 6.61 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 7.12 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 6.55 | WOMBAT-PK | |||||
| Adenosine receptor A3 | GPCR | IC50 | 7.66 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 6.92 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 8.28 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 7.55 | CHEMBL | |||||
| Muscarinic receptor M1 | GPCR | Ki | 8.44 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 6.48 | CHEMBL | |||||
| Muscarinic acetylcholine receptor | GPCR | Ki | 6.96 | CHEMBL | |||||
| Muscarinic acetylcholine receptor DM1 | GPCR | Ki | 6.41 | CHEMBL | |||||
| Muscarinic acetylcholine receptor | GPCR | Ki | 7.22 | CHEMBL | |||||
| Muscarinic acetylcholine receptor | GPCR | IC50 | 6.12 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4025257 | VUID |
| N0000171787 | NUI |
| D01297 | KEGG_DRUG |
| 4025257 | VANDF |
| 4025258 | VANDF |
| C0031978 | UMLSCUI |
| CHEBI:8247 | CHEBI |
| CHEMBL9967 | ChEMBL_ID |
| DB00670 | DRUGBANK_ID |
| D010890 | MESH_DESCRIPTOR_UI |
| 4848 | PUBCHEM_CID |
| 328 | IUPHAR_LIGAND_ID |
| 3476 | INN_ID |
| 29868-97-1 | SECONDARY_CAS_RN |
| 3G0285N20N | UNII |
| 235775 | RXNORM |
| 003754 | NDDF |
| 003755 | NDDF |
| 349802000 | SNOMEDCT_US |
| 398669004 | SNOMEDCT_US |
| CHEMBL1531864 | ChEMBL_ID |
| CHEMBL1257024 | ChEMBL_ID |
Pharmaceutical products:
None