terfenadine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2600 | 50679-08-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.12 | g | O |
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 | Bocci G, Oprea TI, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 0 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 4.24 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 1 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | 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 | R06AX12 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use |
| MeSH PA | D018494 | Histamine Agents |
| MeSH PA | D006633 | Histamine Antagonists |
| MeSH PA | D006634 | Histamine H1 Antagonists |
| MeSH PA | D039563 | Histamine H1 Antagonists, Non-Sedating |
| MeSH PA | D018377 | Neurotransmitter Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Vasomotor rhinitis | indication | 8229003 | DOID:4730 |
| Allergic rhinitis | indication | 61582004 | |
| Nasal discharge | indication | 64531003 | |
| Nasal congestion | indication | 68235000 | |
| Sneezing | indication | 76067001 | |
| Common cold | indication | 82272006 | DOID:10459 |
| Chronic idiopathic urticaria | indication | 302162004 | |
| Seasonal allergic rhinitis | indication | 367498001 | |
| Allergic conjunctivitis | indication | 473460002 | DOID:11204 |
| Urticaria | off-label use | 126485001 | |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Coronary arteriosclerosis | contraindication | 53741008 | DOID:3393 |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Retention of urine | contraindication | 267064002 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Hypertensive urgency | contraindication | 443482000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.85 | 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 | Ki | 8.70 | WOMBAT-PK | IUPHAR | |||
| D(2) dopamine receptor | GPCR | Ki | 5.69 | DRUG MATRIX | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 7.25 | WOMBAT-PK | |||||
| Multidrug resistance protein 1 | Transporter | IC50 | 5.85 | WOMBAT-PK | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 5.72 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 7.14 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 7.52 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.19 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 6 | GPCR | Ki | 6.22 | DRUG MATRIX | |||||
| D(3) dopamine receptor | GPCR | Ki | 6.29 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | IC50 | 5.54 | CHEMBL | |||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 6.26 | DRUG MATRIX | |||||
| Sodium-dependent dopamine transporter | Transporter | Ki | 6.69 | DRUG MATRIX | |||||
| Epidermal growth factor receptor | Kinase | IC50 | 5.45 | DRUG MATRIX | |||||
| C-C chemokine receptor type 5 | GPCR | Ki | 6.07 | DRUG MATRIX | |||||
| Tyrosine-protein kinase Fyn | Kinase | IC50 | 5.21 | DRUG MATRIX | |||||
| Cytochrome P450 2J2 | Enzyme | IC50 | 5.09 | CHEMBL | |||||
| Substance-K receptor | GPCR | Ki | 6.05 | DRUG MATRIX | |||||
| Potassium voltage-gated channel subfamily H member 1 | Ion channel | BLOCKER | IC50 | 7.80 | IUPHAR | ||||
| Heat shock protein HSP 90-alpha | Cytosolic other | IC50 | 5.46 | WOMBAT-PK | |||||
| Adrenergic receptor alpha-1 | GPCR | IC50 | 5.63 | CHEMBL | |||||
| D(1A) dopamine receptor | GPCR | Ki | 5.87 | DRUG MATRIX | |||||
| Alpha-1B adrenergic receptor | GPCR | Ki | 5.73 | DRUG MATRIX | |||||
| Histamine H1 receptor | GPCR | Kd | 7.45 | CHEMBL | |||||
| Transcriptional activator protein luxR | Unclassified | IC50 | 4.04 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019295 | VUID |
| N0000147493 | NUI |
| D00521 | KEGG_DRUG |
| 4019295 | VANDF |
| C0085173 | UMLSCUI |
| CHEBI:9453 | CHEBI |
| CHEMBL17157 | ChEMBL_ID |
| D016593 | MESH_DESCRIPTOR_UI |
| DB00342 | DRUGBANK_ID |
| 2608 | IUPHAR_LIGAND_ID |
| 3674 | INN_ID |
| 7BA5G9Y06Q | UNII |
| 5405 | PUBCHEM_CID |
| 202960 | RXNORM |
| 1520 | MMSL |
| 2365 | MMSL |
| 5550 | MMSL |
| d00387 | MMSL |
| 003412 | NDDF |
| 16037009 | SNOMEDCT_US |
| 387089004 | SNOMEDCT_US |
Pharmaceutical products:
None