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protriptyline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antidepressants, dibenzo[a,d]cycloheptane or cyclopheptene derivatives | 2320 | 438-60-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Tricyclic antidepressant similar in action and side effects to IMIPRAMINE. It may produce excitation.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 30 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 50 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 1 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 3.25 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 85 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| fu (Fraction unbound in plasma) | 0.14 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.106 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.501 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 40.087 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 35.727 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 7.500 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 24.920 | % | High | 1 |
| herg | hERG pIC50 | 5.186 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 24.660 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 17.418 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 24.070 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK | 52 | |||
| kinase-selectivity-class | AXL,BRAF,GRK2,PDK4,STK33,TTK | 6 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.813 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 169.824 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 13.150 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.047 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 23.940 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 390.841 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 48.220 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 22.500 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 961.612 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 27, 1967 | FDA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N06AA11 | NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Non-selective monoamine reuptake inhibitors |
| MeSH PA | D000928 | Antidepressive Agents |
| MeSH PA | D000929 | Antidepressive Agents, Tricyclic |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D014179 | Neurotransmitter Uptake Inhibitors |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018759 | Adrenergic Uptake Inhibitors |
| MeSH PA | D049990 | Membrane Transport Modulators |
| FDA EPC | N0000175752 | Tricyclic Antidepressant |
| CHEBI has role | CHEBI:35469 | antidepressant |
Related Drugs by ATC class:
N06AA Non-selective monoamine reuptake inhibitors 20 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Depressive disorder | indication | 35489007 | |
| Cataplexy | off-label use | 46263000 | |
| Ocular hypertension | contraindication | 4210003 | DOID:9282 |
| Suicidal thoughts | contraindication | 6471006 | |
| Alcoholism | contraindication | 7200002 | |
| Bipolar disorder | contraindication | 13746004 | DOID:3312 |
| Electroconvulsive therapy | contraindication | 23835007 | |
| Glaucoma | contraindication | 23986001 | DOID:1686 |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Low blood pressure | contraindication | 45007003 | |
| Dementia | contraindication | 52448006 | |
| Schizophrenia | contraindication | 58214004 | DOID:5419 |
| Chronic idiopathic constipation | contraindication | 82934008 | |
| Hiatal hernia | contraindication | 84089009 | DOID:12642 |
| Seizure disorder | contraindication | 128613002 | |
| Asthma | contraindication | 195967001 | DOID:2841 |
| Gastroesophageal reflux disease | contraindication | 235595009 | DOID:8534 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Retention of urine | contraindication | 267064002 | |
| Surgical procedure | contraindication | 387713003 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Myocardial infarction in recovery phase | contraindication | 418044006 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.04 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Sodium-dependent serotonin transporter | Transporter | INHIBITOR | Ki | 7.34 | WOMBAT-PK | CHEMBL | |||
| Sodium-dependent noradrenaline transporter | Transporter | INHIBITOR | Ki | 8.39 | WOMBAT-PK | CHEMBL | |||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 5.93 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.50 | WOMBAT-PK | |||||
| Histamine H1 receptor | GPCR | Ki | 7.22 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 7.70 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 6.90 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 7 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 6.94 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 6.86 | WOMBAT-PK | |||||
| Sodium-dependent dopamine transporter | Transporter | Ki | 5.68 | PDSP | |||||
| Adenosine receptor A3 | GPCR | IC50 | 8.96 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 7.20 | WOMBAT-PK | |||||
| Voltage-dependent N-type calcium channel subunit alpha-1B | Ion channel | IC50 | 4.85 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 7 | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4019918 | VUID |
| N0000148003 | NUI |
| D00484 | KEGG_DRUG |
| 1225-55-4 | SECONDARY_CAS_RN |
| 4017927 | VANDF |
| 4019918 | VANDF |
| C0033743 | UMLSCUI |
| CHEBI:8597 | CHEBI |
| CHEMBL668 | ChEMBL_ID |
| DB00344 | DRUGBANK_ID |
| CHEMBL1200332 | ChEMBL_ID |
| D011530 | MESH_DESCRIPTOR_UI |
| 4976 | PUBCHEM_CID |
| 7285 | IUPHAR_LIGAND_ID |
| 1663 | INN_ID |
| 4NDU154T12 | UNII |
| 203199 | RXNORM |
| 2338 | MMSL |
| 5381 | MMSL |
| d00875 | MMSL |
| 001504 | NDDF |
| 004603 | NDDF |
| 372760009 | SNOMEDCT_US |
| 46950002 | SNOMEDCT_US |
| 49299006 | SNOMEDCT_US |
| 4NDU154T12 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Protriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0210 | TABLET | 5 mg | ORAL | ANDA | 17 sections |
| Protriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0211 | TABLET | 10 mg | ORAL | ANDA | 17 sections |
| Protriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42794-004 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 15 sections |
| Protriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42794-007 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 15 sections |
| Protriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42806-096 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 19 sections |
| Protriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42806-097 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 19 sections |