antazoline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihistaminics or local vasoconstrictors, antazoline derivatives | 224 | 91-75-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An ethylenediamine derivative with histamine H1 antagonistic and sedative properties. Antazoline antagonizes histamine H1 receptor and prevents the typical allergic symptoms caused by histamine activities on capillaries, skin, mucous membranes, and gastrointestinal and bronchial smooth muscles. These histamine activities include vasodilation, bronchoconstriction, increased vascular permeability, pain, itching, and spasmodic contractions of gastrointestinal smooth muscles. Antazoline is used to provide symptomatic relieve of allergic symptoms.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.30 | g | O |
| 0.30 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 3.90 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 19.67 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2.29 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 0.66 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 30, 1990 | 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 | R01AC04 | RESPIRATORY SYSTEM NASAL PREPARATIONS DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE Antiallergic agents, excl. corticosteroids |
| ATC | R06AX05 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use |
| MeSH PA | D018926 | Anti-Allergic Agents |
| MeSH PA | D018494 | Histamine Agents |
| MeSH PA | D006633 | Histamine Antagonists |
| MeSH PA | D006634 | Histamine H1 Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| CHEBI has role | CHEBI:35703 | Xenobiotic |
| CHEBI has role | CHEBI:37955 | H1 receptor antagonists |
| CHEBI has role | CHEBI:48873 | acetylcholine receptor antagonist |
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 | |
| Red eye | indication | 75705005 | |
| Sneezing | indication | 76067001 | |
| Urticaria | indication | 126485001 | |
| Itching of skin | indication | 418363000 | |
| Allergic conjunctivitis | indication | 473460002 | DOID:11204 |
| Anaphylaxis Adjunct | indication | ||
| Ocular Itching | indication | ||
| Ocular hypertension | contraindication | 4210003 | DOID:9282 |
| Peptic ulcer | contraindication | 13200003 | DOID:750 |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Hyperglycemia | contraindication | 80394007 | DOID:4195 |
| Chronic idiopathic constipation | contraindication | 82934008 | |
| Eye infection | contraindication | 128351009 | |
| Bladder outflow obstruction | contraindication | 236645006 | |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Retention of urine | contraindication | 267064002 | |
| Injury of eye region | contraindication | 282752000 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.35 | Basic |
| pKa2 | 3.96 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | GPCR | ANTAGONIST | CHEMBL | CHEMBL | |||||
| Histamine H1 receptor | GPCR | Kd | 7.14 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019615 | VUID |
| N0000147709 | NUI |
| D02950 | KEGG_DRUG |
| 3131-32-6 | SECONDARY_CAS_RN |
| 24359-81-7 | SECONDARY_CAS_RN |
| 81954 | RXNORM |
| C0003143 | UMLSCUI |
| CHEBI:84115 | CHEBI |
| CHEMBL1305 | ChEMBL_ID |
| DB08799 | DRUGBANK_ID |
| D000865 | MESH_DESCRIPTOR_UI |
| 2200 | PUBCHEM_CID |
| 7116 | IUPHAR_LIGAND_ID |
| 1142 | INN_ID |
| 154-68-7 | SECONDARY_CAS_RN |
| 2508-72-7 | SECONDARY_CAS_RN |
| DHA8014SS1 | UNII |
| 4205 | MMSL |
| 373544004 | SNOMEDCT_US |
| 387061002 | SNOMEDCT_US |
| 396006001 | SNOMEDCT_US |
| 7816005 | SNOMEDCT_US |
| 85408000 | SNOMEDCT_US |
| CHEMBL1200550 | ChEMBL_ID |
| CHEMBL1256819 | ChEMBL_ID |
| 4019060 | VANDF |
| 4019150 | VANDF |
| 4019615 | VANDF |
| 003378 | NDDF |
| 003379 | NDDF |
| 003380 | NDDF |
| 003724 | NDDF |
| 005437 | NDDF |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Nestabs ONE | HUMAN PRESCRIPTION DRUG LABEL | 10 | 50967-410 | CAPSULE, GELATIN COATED | 225 mg | ORAL | unapproved drug other | 12 sections |
| Nestabs ONE | HUMAN PRESCRIPTION DRUG LABEL | 10 | 50967-410 | CAPSULE, GELATIN COATED | 225 mg | ORAL | unapproved drug other | 12 sections |