mizolastine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihistaminics | 1824 | 108612-45-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a long-acting H1-antihistamine indicated for the symptomatic relief of seasonal allergic rhinoconjunctivitis (hay fever), perennial allergic rhinoconjunctivitis and urticaria
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 10 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.01 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 5 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.33 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 65 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.38 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.03 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 9.60 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 7, 2003 | UK Medicines and Healthcare Products Regulatory Agency (MHRA) | SANOFI |
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 | R06AX25 | 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 |
|---|---|---|---|
| Allergic rhinitis | indication | 61582004 | |
| Perennial allergic rhinitis | indication | 446096008 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.99 | acidic |
| pKa2 | 5.99 | Basic |
| pKa3 | 3.2 | 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 | 8.84 | WOMBAT-PK | SCIENTIFIC LITERATURE | |||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 6.46 | WOMBAT-PK | |||||
| Arachidonate 5-lipoxygenase | Enzyme | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| D01117 | KEGG_DRUG |
| C0171302 | UMLSCUI |
| CHEBI:31857 | CHEBI |
| CHEMBL94454 | ChEMBL_ID |
| DB12523 | DRUGBANK_ID |
| C076170 | MESH_SUPPLEMENTAL_RECORD_UI |
| 65906 | PUBCHEM_CID |
| 10102 | IUPHAR_LIGAND_ID |
| 6663 | INN_ID |
| 244O1F90NA | UNII |
| 153888 | RXNORM |
| 007534 | NDDF |
| 320830000 | SNOMEDCT_US |
| 395798005 | SNOMEDCT_US |
Pharmaceutical products:
None