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sibutramine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2440 | 106650-56-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
serotonin and norepinephrine transporter inhibitor; Meridia is tradename for sibutramine hydrochloride
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 10 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 2.90 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.77 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK3,MAP3K7,MAPK10,MAPK7,MET,NTRK2,PDK2,PDK4,PIM2,PRKDC,TEK,TGFBR1 | 28 | |||
| kinase-selectivity-class | AKT1,AKT2,AKT3,EIF2AK3,PDK4 | 5 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 22, 1997 | FDA |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Suspected counterfeit product | 93.63 | 67.08 | 12 | 305 | 514 | 90627616 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Suspected counterfeit product | 90.52 | 57.95 | 12 | 315 | 794 | 110588178 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A08AA10 | ALIMENTARY TRACT AND METABOLISM ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS Centrally acting antiobesity products |
| FDA MoA | N0000000102 | Norepinephrine Uptake Inhibitors |
| FDA MoA | N0000000109 | Serotonin Uptake Inhibitors |
| FDA MoA | N0000000114 | Dopamine Uptake Inhibitors |
| FDA PE | N0000175372 | Appetite Suppression |
| FDA EPC | N0000175424 | Norepinephrine, Serotonin, and Dopamine Reuptake Inhibitor Anorectic |
| MeSH PA | D000928 | Antidepressive Agents |
| MeSH PA | D001067 | Appetite Depressants |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D019440 | Anti-Obesity Agents |
| CHEBI has role | CHEBI:50949 | serotonin uptake inhibitor |
| CHEBI has role | CHEBI:74518 | anti-obesity agent |
Related Drugs by ATC class:
A08AA Centrally acting antiobesity products 15 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Obesity | indication | 414916001 | DOID:9970 |
| Tachyarrhythmia | contraindication | 6285003 | |
| Neuroleptic malignant syndrome | contraindication | 15244003 | DOID:14464 |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Chronic heart failure | contraindication | 48447003 | |
| Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
| Anorexia nervosa | contraindication | 56882008 | DOID:8689 |
| Acute nephropathy | contraindication | 58574008 | |
| Hepatic failure | contraindication | 59927004 | |
| Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Bulimia nervosa | contraindication | 78004001 | |
| Chronic renal failure syndrome | contraindication | 90688005 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Seizure disorder | contraindication | 128613002 | |
| Angina pectoris | contraindication | 194828000 | |
| Cerebrovascular accident | contraindication | 230690007 | |
| Transient ischemic attack | contraindication | 266257000 | DOID:224 |
| Serotonin syndrome | contraindication | 371089000 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Cardiovascular event risk | contraindication | 395112001 | |
| Peripheral arterial occlusive disease | contraindication | 399957001 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Disorder of coronary artery | contraindication | 414024009 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.18 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Sodium-dependent serotonin transporter | Transporter | INHIBITOR | Ki | 6.53 | WOMBAT-PK | CHEMBL | |||
| Sodium-dependent noradrenaline transporter | Transporter | INHIBITOR | Ki | 5.26 | WOMBAT-PK | CHEMBL | |||
| Sodium-dependent dopamine transporter | Transporter | INHIBITOR | Ki | 6.03 | WOMBAT-PK | CHEMBL | |||
| Alpha-2C adrenergic receptor | GPCR | WOMBAT-PK | |||||||
| Potassium voltage-gated channel subfamily D member 3 | Ion channel | IC50 | 4.70 | WOMBAT-PK | |||||
| Cytochrome P450 2B6 | Enzyme | INHIBITOR | IC50 | 5.79 | IUPHAR | ||||
| Solute carrier family 22 member 2 | Transporter | IC50 | 4.54 | WOMBAT-PK | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 5.96 | DRUG MATRIX | |||||
| Potassium voltage-gated channel subfamily D member 3 | Ion channel | BLOCKER | IC50 | 4.70 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4024106 | VUID |
| N0000022111 | NUI |
| D02571 | KEGG_DRUG |
| 125494-59-9 | SECONDARY_CAS_RN |
| 4021089 | VANDF |
| 4024106 | VANDF |
| C0074493 | UMLSCUI |
| CHEBI:9137 | CHEBI |
| CHEMBL1419 | ChEMBL_ID |
| DB01105 | DRUGBANK_ID |
| CHEMBL3989830 | ChEMBL_ID |
| C058254 | MESH_SUPPLEMENTAL_RECORD_UI |
| 5210 | PUBCHEM_CID |
| 2586 | IUPHAR_LIGAND_ID |
| 6124 | INN_ID |
| WV5EC51866 | UNII |
| 1294535 | RXNORM |
| d04260 | MMSL |
| 007298 | NDDF |
| 108373009 | SNOMEDCT_US |
| 386838007 | SNOMEDCT_US |
| 783113003 | SNOMEDCT_US |
| 84467-54-9 | SECONDARY_CAS_RN |
| WV5EC51866 | INXIGHT DRUGS |
Pharmaceutical products:
None