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lofexidine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| alpha-2 adrenoreceptor agonists | 1593 | 31036-80-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Lofexidine is a central alpha-2 adrenergic agonist that binds to receptors on adrenergic neurons. This reduces the release of norepinephrine and decreases sympathetic tone.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.40 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Hosey CM, Chan R, Benet LZ |
| BA (Bioavailability) | 90 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| S (Water solubility) | 20 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK10,MAPK7,NTRK2,PDK2,PDK4,PIK3CB,PIK3CG,PRKDC,TEK | 19 | |||
| kinase-selectivity-class | AXL,EIF2AK3,GRK2,PDK4,PIK3CD | 5 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 16, 2018 | FDA | US WORLDMEDS LLC |
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 | N07BC04 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS DRUGS USED IN ADDICTIVE DISORDERS Drugs used in opioid dependence |
| MeSH PA | D000316 | Adrenergic alpha-Agonists |
| MeSH PA | D000322 | Adrenergic Agonists |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D009292 | Narcotic Antagonists |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018689 | Sensory System Agents |
| MeSH PA | D058647 | Adrenergic alpha-2 Receptor Agonists |
| CHEBI has role | CHEBI:35569 | α-adrenergic agonist |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
Related Drugs by ATC class:
N07BC Drugs used in opioid dependence 5 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Opioid withdrawal | indication | 87132004 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.49 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Alpha-2A adrenergic receptor | GPCR | AGONIST | Ki | 8.36 | CHEMBL | SCIENTIFIC LITERATURE | |||
| Alpha-2B adrenergic receptor | GPCR | Ki | 7.17 | CHEMBL | |||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 7.16 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 6.90 | CHEMBL | |||||
| Adrenergic receptor alpha-2 | GPCR | IC50 | 8.60 | CHEMBL | |||||
| Adrenergic receptor alpha-1 | GPCR | IC50 | 6.18 | CHEMBL | |||||
| Nischarin | Membrane receptor | Ki | 8.25 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4025252 | VUID |
| N0000171822 | NUI |
| D04765 | KEGG_DRUG |
| 21498-08-8 | SECONDARY_CAS_RN |
| 4025251 | VANDF |
| 4025252 | VANDF |
| C0065152 | UMLSCUI |
| CHEBI:51368 | CHEBI |
| CHEMBL17860 | ChEMBL_ID |
| CHEMBL1788132 | ChEMBL_ID |
| DB04948 | DRUGBANK_ID |
| C025655 | MESH_SUPPLEMENTAL_RECORD_UI |
| 30668 | PUBCHEM_CID |
| 9868 | IUPHAR_LIGAND_ID |
| 3766 | INN_ID |
| UI82K0T627 | UNII |
| 235853 | RXNORM |
| 34252 | MMSL |
| 388979 | MMSL |
| d04956 | MMSL |
| 004132 | NDDF |
| 004133 | NDDF |
| 349934008 | SNOMEDCT_US |
| 395773009 | SNOMEDCT_US |
| 395989000 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Lofexidine | Human Prescription Drug Label | 1 | 14445-146 | TABLET, COATED | 0.18 mg | ORAL | ANDA | 24 sections |
| Lofexidine hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66993-345 | TABLET, FILM COATED | 0.20 mg | ORAL | NDA authorized generic | 32 sections |
| Lofexidine | Human Prescription Drug Label | 1 | 70954-909 | TABLET | 0.18 mg | ORAL | ANDA | 27 sections |
| Lofexidine | Human Prescription Drug Label | 1 | 71921-250 | TABLET, COATED | 0.18 mg | ORAL | ANDA | 24 sections |
| lofexidine hydrochloride | Human Prescription Drug Label | 1 | 72205-246 | TABLET, FILM COATED | 0.20 mg | ORAL | ANDA | 24 sections |
| Lucemyra | HUMAN PRESCRIPTION DRUG LABEL | 1 | 78670-050 | TABLET, FILM COATED | 0.20 mg | ORAL | NDA | 32 sections |