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tripelennamine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2762 | 91-81-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A histamine H1 antagonist with low sedative action but frequent gastrointestinal irritation. It is used to treat ASTHMA; HAY FEVER; URTICARIA; and RHINITIS; and also in veterinary applications. Tripelennamine is administered by various routes, including topically.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.15 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 2.84 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.435 | Moderate | 0.74 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.759 | Moderate | 0.74 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 32.285 | 10^-6 cm/s | Moderate | 0.74 |
| dh-clint | Dog hepatocyte intrinsic clearance | 111.173 | uL/min/10^6 cells | Moderate | 0.74 |
| dppb | Dog plasma protein binding (% unbound) | 61.800 | % | Moderate | 0.74 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 67.170 | % | Moderate | 0.74 |
| herg | hERG pIC50 | 5.267 | pIC50 | Moderate | 0.74 |
| hh-clint | Human hepatocyte intrinsic clearance | 13.868 | uL/min/10^6 cells | Moderate | 0.74 |
| hlm-clint | Human liver microsomal intrinsic clearance | 29.376 | uL/min/mg protein | Moderate | 0.74 |
| hppb | Human plasma protein binding (% unbound) | 53.510 | % | Moderate | 0.74 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAP3K7,MAPK12,MAPK7,MET,MTOR,NTRK2,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK | 35 | |||
| kinase-selectivity-class | AXL,BRAF,ERBB2 | 3 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.303 | Moderate | 0.74 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 266.073 | Moderate | 0.74 | |
| mppb | Mouse plasma protein binding (% unbound) | 64.800 | Moderate | 0.74 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.711 | Moderate | 0.74 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 77.810 | % | Moderate | 0.74 |
| rh-clint | Rat hepatocyte intrinsic clearance | 294.442 | uL/min/10^6 cells | Moderate | 0.74 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 81.670 | % | Moderate | 0.74 |
| rppb | Rat plasma protein binding (% unbound) | 65.740 | % | Moderate | 0.74 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 950.605 | uM | Moderate | 0.74 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 19, 1948 | FDA | NOVARTIS |
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 | D04AA04 | DERMATOLOGICALS ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. Antihistamines for topical use |
| ATC | R06AC04 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Substituted ethylene diamines |
| MeSH PA | D006633 | Histamine Antagonists |
| MeSH PA | D006634 | Histamine H1 Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018926 | Anti-Allergic Agents |
Related Drugs by ATC class:
D04AA Antihistamines for topical use 13 drugs
R06AC Substituted ethylene diamines 5 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Dermatographic urticaria | indication | 7632005 | DOID:743 |
| Vasomotor rhinitis | indication | 8229003 | DOID:4730 |
| Allergic rhinitis | indication | 61582004 | |
| Nasal discharge | indication | 64531003 | |
| Nasal congestion | indication | 68235000 | |
| Sneezing | indication | 76067001 | |
| Urticaria | indication | 126485001 | |
| Itching of skin | indication | 418363000 | |
| Allergic conjunctivitis | indication | 473460002 | DOID:11204 |
| Anaphylaxis Adjunct | indication | ||
| Ocular hypertension | contraindication | 4210003 | DOID:9282 |
| Peptic ulcer | contraindication | 13200003 | DOID:750 |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Chronic idiopathic constipation | contraindication | 82934008 | |
| Bladder outflow obstruction | contraindication | 236645006 | |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Retention of urine | contraindication | 267064002 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Cats | Antihistaminic therapy | Indication |
| Cattle | Antihistaminic therapy | Indication |
| Dogs | Antihistaminic therapy | Indication |
| Horses | Antihistaminic therapy | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| RE-COVR | Kinetic Technologies LLC | 1 |
| Tripelennamine Hydrochloride Injection | Huvepharma EOOD | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.62 | Basic |
| pKa2 | 4.33 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | GPCR | ANTAGONIST | IC50 | 7.40 | CHEMBL | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019963 | VUID |
| N0000148048 | NUI |
| D02091 | KEGG_DRUG |
| 4018394 | VANDF |
| 4018395 | VANDF |
| 4019963 | VANDF |
| C0041090 | UMLSCUI |
| CHEBI:9741 | CHEBI |
| CHEMBL1241 | ChEMBL_ID |
| CHEMBL1200446 | ChEMBL_ID |
| CHEMBL151676 | ChEMBL_ID |
| DB00792 | DRUGBANK_ID |
| CHEMBL1200769 | ChEMBL_ID |
| D014309 | MESH_DESCRIPTOR_UI |
| 5587 | PUBCHEM_CID |
| 7318 | IUPHAR_LIGAND_ID |
| 1548 | INN_ID |
| 6138-56-3 | SECONDARY_CAS_RN |
| 154-69-8 | SECONDARY_CAS_RN |
| 3C5ORO99TY | UNII |
| 10847 | RXNORM |
| 3076 | MMSL |
| 5638 | MMSL |
| d00781 | MMSL |
| 003374 | NDDF |
| 003375 | NDDF |
| 003376 | NDDF |
| 25014009 | SNOMEDCT_US |
| 373475006 | SNOMEDCT_US |
| 53405009 | SNOMEDCT_US |
| 3C5ORO99TY | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| PBZ OTC | HUMAN OTC DRUG LABEL | 1 | 69993-151 | CREAM | 1 g | TOPICAL | OTC Monograph Drug | 11 sections |
| Blue-Emu Thrive Pain Relief Cream | HUMAN OTC DRUG LABEL | 1 | 69993-600 | CREAM | 0.50 g | TOPICAL | OTC Monograph Drug | 12 sections |
| Blue-Emu THRIVE Cooling | HUMAN OTC DRUG LABEL | 1 | 69993-650 | CREAM | 0.50 g | TOPICAL | OTC Monograph Drug | 11 sections |