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orciprenaline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| bronchodilators, phenethylamine derivatives | 1720 | 586-06-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A beta-2 adrenergic agonist used in the treatment of ASTHMA and BRONCHIAL SPASM.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 6 | mg | Inhal.aerosol |
| 60 | mg | O |
| 60 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Hosey CM, Chan R, Benet LZ |
| Vd (Volume of distribution) | 6.03 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 14.07 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.90 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 6.41 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 6.92 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BA (Bioavailability) | 25 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -0.989 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.381 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.426 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 7.499 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 84.300 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 37.010 | % | High | 1 |
| herg | hERG pIC50 | 4.063 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.992 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.707 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 76.890 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK2,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,IGF1R,ITK,JAK1,JAK2,JAK3,KDR,KIT,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MTOR,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIM2,PLK1,PLK2,PLK3,PLK4,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ZAP70 | 61 | |||
| kinase-selectivity-class | GRK2,MAP2K6 | 2 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 0.525 | Moderate | 0.66 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.684 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 46.238 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 80.220 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.592 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 0 | Moderate | 0.66 | |
| pppb | Pig plasma protein binding (% unbound) | 77.930 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.054 | % | Moderate | 0.66 |
| rh-clint | Rat hepatocyte intrinsic clearance | 5.082 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 86.980 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 61.040 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 810.961 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 31, 1973 | 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 | R03AB03 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Non-selective beta-adrenoreceptor agonists |
| ATC | R03CB03 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS FOR SYSTEMIC USE Non-selective beta-adrenoreceptor agonists |
| ATC | R03CB53 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS FOR SYSTEMIC USE Non-selective beta-adrenoreceptor agonists |
| FDA MoA | N0000009922 | Adrenergic beta2-Agonists |
| MeSH PA | D000318 | Adrenergic beta-Agonists |
| MeSH PA | D001993 | Bronchodilator Agents |
| MeSH PA | D012102 | Reproductive Control Agents |
| MeSH PA | D013566 | Sympathomimetics |
| MeSH PA | D015149 | Tocolytic Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018927 | Anti-Asthmatic Agents |
| MeSH PA | D019141 | Respiratory System Agents |
| MeSH PA | D058666 | Adrenergic beta-2 Receptor Agonists |
| FDA EPC | N0000175779 | beta2-Adrenergic Agonist |
| CHEBI has role | CHEBI:35522 | β-adrenergic agonist |
| CHEBI has role | CHEBI:35523 | bronchodilator agent |
| CHEBI has role | CHEBI:49167 | anti-asthmatic drug |
| CHEBI has role | CHEBI:65023 | anti-asthmatic agent |
Related Drugs by ATC class:
R03AB Non-selective beta-adrenoreceptor agonists 1 drug
R03CB Non-selective beta-adrenoreceptor agonists 2 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Bronchitis | indication | 32398004 | DOID:6132 |
| Pulmonary emphysema | indication | 87433001 | |
| Asthma | indication | 195967001 | DOID:2841 |
| Asthma management | indication | 406162001 | |
| Acute exacerbation of asthma | indication | 708038006 | |
| Bronchospasm Prevention | indication | ||
| Tachyarrhythmia | contraindication | 6285003 | |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Chronic heart failure | contraindication | 48447003 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Seizure disorder | contraindication | 128613002 | |
| Disorder of coronary artery | contraindication | 414024009 | |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.48 | acidic |
| pKa2 | 11.49 | acidic |
| pKa3 | 12.6 | acidic |
| pKa4 | 8.55 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Beta-2 adrenergic receptor | GPCR | AGONIST | Kd | 6.30 | CHEMBL | CHEMBL | |||
| Beta-2 adrenergic receptor | GPCR | Kd | 5.04 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019817 | VUID |
| N0000147906 | NUI |
| D00685 | KEGG_DRUG |
| 5874-97-5 | SECONDARY_CAS_RN |
| 4018762 | VANDF |
| 4019817 | VANDF |
| CHEBI:6792 | CHEBI |
| CHEMBL776 | ChEMBL_ID |
| CHEMBL1568057 | ChEMBL_ID |
| 7250 | IUPHAR_LIGAND_ID |
| DB00816 | DRUGBANK_ID |
| 6804 | RXNORM |
| 1956 | MMSL |
| 5060 | MMSL |
| d00750 | MMSL |
| 001786 | NDDF |
| 004408 | NDDF |
| 372797004 | SNOMEDCT_US |
| 54172006 | SNOMEDCT_US |
| 6067003 | SNOMEDCT_US |
| C0029193 | UMLSCUI |
| D009921 | MESH_DESCRIPTOR_UI |
| 1586 | INN_ID |
| 4086 | PUBCHEM_CID |
| 53QOG569E0 | UNII |
| 53QOG569E0 | INXIGHT DRUGS |
Pharmaceutical products:
None