Stem definition | Drug id | CAS RN |
---|---|---|
substances of the imipramine group | 1427 | 50-49-7 |
Dose | Unit | Route |
---|---|---|
0.10 | g | O |
0.10 | g | P |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 1.50 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 5.09 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 42 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 12 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 13 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.08 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 16 hours | Lombardo F, Berellini G, Obach RS |
S (Water solubility) | 50 mg/mL | Bocci G, Oprea TI, Benet LZ |
Date | Agency | Company | Orphan |
---|---|---|---|
April 16, 1959 | FDA |
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 |
---|---|---|---|---|---|---|
Paranoia | 67.85 | 18.91 | 25 | 3385 | 11654 | 63473958 |
Hallucination, auditory | 65.57 | 18.91 | 25 | 3385 | 12799 | 63472813 |
Completed suicide | 64.37 | 18.91 | 57 | 3353 | 145616 | 63339996 |
Psychotic disorder | 51.79 | 18.91 | 26 | 3384 | 25686 | 63459926 |
Toxicity to various agents | 45.62 | 18.91 | 61 | 3349 | 247189 | 63238423 |
Stress cardiomyopathy | 36.33 | 18.91 | 15 | 3395 | 9435 | 63476177 |
Procedural hypotension | 30.71 | 18.91 | 8 | 3402 | 1182 | 63484430 |
Skin hyperpigmentation | 28.31 | 18.91 | 11 | 3399 | 5910 | 63479702 |
Iris hyperpigmentation | 25.65 | 18.91 | 4 | 3406 | 41 | 63485571 |
Urinary hesitation | 21.39 | 18.91 | 7 | 3403 | 2293 | 63483319 |
Decreased activity | 20.85 | 18.91 | 9 | 3401 | 6311 | 63479301 |
Limb mass | 19.06 | 18.91 | 7 | 3403 | 3225 | 63482387 |
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 |
---|---|---|---|---|---|---|
Blepharospasm | 57.32 | 24.72 | 13 | 1789 | 1125 | 34954004 |
Toxicity to various agents | 56.59 | 24.72 | 60 | 1742 | 200302 | 34754827 |
Completed suicide | 50.20 | 24.72 | 41 | 1761 | 98127 | 34857002 |
Long QT syndrome | 45.68 | 24.72 | 13 | 1789 | 2790 | 34952339 |
Neuroleptic malignant syndrome | 42.51 | 24.72 | 20 | 1782 | 17914 | 34937215 |
Pyelitis | 42.36 | 24.72 | 7 | 1795 | 111 | 34955018 |
Muscle rigidity | 38.76 | 24.72 | 16 | 1786 | 10502 | 34944627 |
Dystonia | 38.29 | 24.72 | 16 | 1786 | 10829 | 34944300 |
Trismus | 38.10 | 24.72 | 11 | 1791 | 2484 | 34952645 |
Delusion | 26.61 | 24.72 | 13 | 1789 | 12622 | 34942507 |
Brain oedema | 25.51 | 24.72 | 13 | 1789 | 13808 | 34941321 |
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 |
---|---|---|---|---|---|---|
Completed suicide | 103.13 | 18.10 | 97 | 4577 | 245670 | 79494044 |
Toxicity to various agents | 65.13 | 18.10 | 100 | 4574 | 421440 | 79318274 |
Paranoia | 62.88 | 18.10 | 28 | 4646 | 19404 | 79720310 |
Neuroleptic malignant syndrome | 59.35 | 18.10 | 30 | 4644 | 27529 | 79712185 |
Hallucination, auditory | 48.91 | 18.10 | 24 | 4650 | 20669 | 79719045 |
Overdose | 45.55 | 18.10 | 55 | 4619 | 184151 | 79555563 |
Psychotic disorder | 38.15 | 18.10 | 26 | 4648 | 41376 | 79698338 |
Blepharospasm | 34.62 | 18.10 | 13 | 4661 | 5838 | 79733876 |
Long QT syndrome | 34.39 | 18.10 | 13 | 4661 | 5942 | 79733772 |
Pyelitis | 34.00 | 18.10 | 7 | 4667 | 336 | 79739378 |
Stress cardiomyopathy | 32.66 | 18.10 | 15 | 4659 | 11151 | 79728563 |
Dystonia | 28.59 | 18.10 | 17 | 4657 | 21382 | 79718332 |
Trismus | 28.23 | 18.10 | 11 | 4663 | 5456 | 79734258 |
Procedural hypotension | 25.82 | 18.10 | 8 | 4666 | 2015 | 79737699 |
Skin hyperpigmentation | 25.15 | 18.10 | 11 | 4663 | 7292 | 79732422 |
Muscle rigidity | 24.51 | 18.10 | 15 | 4659 | 19867 | 79719847 |
Electrocardiogram QT prolonged | 23.97 | 18.10 | 28 | 4646 | 90358 | 79649356 |
Respiratory depression | 22.29 | 18.10 | 16 | 4658 | 27614 | 79712100 |
Drug interaction | 20.47 | 18.10 | 62 | 4612 | 415121 | 79324593 |
Withdrawal syndrome | 20.41 | 18.10 | 15 | 4659 | 26839 | 79712875 |
Suicide attempt | 19.22 | 18.10 | 24 | 4650 | 82908 | 79656806 |
Parkinsonism | 19.14 | 18.10 | 12 | 4662 | 16572 | 79723142 |
Electrocardiogram abnormal | 19.04 | 18.10 | 12 | 4662 | 16725 | 79722989 |
Iris hyperpigmentation | 18.95 | 18.10 | 3 | 4671 | 31 | 79739683 |
Speech disorder | 18.12 | 18.10 | 19 | 4655 | 54426 | 79685288 |
None
Source | Code | Description |
---|---|---|
ATC | N06AA02 | NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Non-selective monoamine reuptake inhibitors |
MeSH PA | D018663 | Adrenergic Agents |
MeSH PA | D018759 | Adrenergic Uptake Inhibitors |
MeSH PA | D000928 | Antidepressive Agents |
MeSH PA | D000929 | Antidepressive Agents, Tricyclic |
MeSH PA | D002491 | Central Nervous System Agents |
MeSH PA | D049990 | Membrane Transport Modulators |
MeSH PA | D018377 | Neurotransmitter Agents |
MeSH PA | D014179 | Neurotransmitter Uptake Inhibitors |
MeSH PA | D011619 | Psychotropic Drugs |
CHEBI has role | CHEBI:35469 | antidepressants |
FDA EPC | N0000175752 | Tricyclic Antidepressant |
CHEBI has role | CHEBI:35640 | adrenergic uptake inhibitors |
CHEBI has role | CHEBI:76779 | post-proline endopeptidase inhibitors |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Nocturnal enuresis | indication | 8009008 | |
Depressive disorder | indication | 35489007 | |
Neuralgia | off-label use | 16269008 | |
Cataplexy | off-label use | 46263000 | |
Anxiety | off-label use | 48694002 | |
Narcolepsy | off-label use | 60380001 | DOID:8986 |
Bulimia nervosa | off-label use | 78004001 | |
Neuropathic pain | off-label use | 247398009 | |
Panic disorder | off-label use | 371631005 | DOID:594 |
Attention deficit hyperactivity disorder | off-label use | 406506008 | |
Ocular hypertension | contraindication | 4210003 | DOID:9282 |
Suicidal thoughts | contraindication | 6471006 | |
Alcoholism | contraindication | 7200002 | |
Bipolar disorder | contraindication | 13746004 | DOID:3312 |
Electroconvulsive therapy | contraindication | 23835007 | |
Alcohol intoxication | contraindication | 25702006 | |
Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
Conduction disorder of the heart | contraindication | 44808001 | |
Chronic heart failure | contraindication | 48447003 | |
Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
Paralytic ileus | contraindication | 55525008 | DOID:8442 |
Schizophrenia | contraindication | 58214004 | DOID:5419 |
Intestinal obstruction | contraindication | 81060008 | DOID:8437 |
Epilepsy | contraindication | 84757009 | DOID:1826 |
Kidney disease | contraindication | 90708001 | DOID:557 |
Seizure disorder | contraindication | 128613002 | |
Cerebrovascular accident | contraindication | 230690007 | |
Mania | contraindication | 231494001 | |
Hypomania | contraindication | 231496004 | |
Disease of liver | contraindication | 235856003 | DOID:409 |
Benign prostatic hyperplasia | contraindication | 266569009 | |
Retention of urine | contraindication | 267064002 | |
Syncope | contraindication | 271594007 | |
Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
Surgical procedure | contraindication | 387713003 | |
Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
Disorder of coronary artery | contraindication | 414024009 | |
Myocardial infarction in recovery phase | contraindication | 418044006 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 9.04 | Basic |
pKa2 | 5.01 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Sodium-dependent noradrenaline transporter | Transporter | INHIBITOR | Kd | 7.43 | WOMBAT-PK | CHEMBL | |||
Sodium-dependent serotonin transporter | Transporter | INHIBITOR | Kd | 8.85 | WOMBAT-PK | CHEMBL | |||
Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 5.90 | WOMBAT-PK | |||||
5-hydroxytryptamine receptor 1A | GPCR | Ki | 5.24 | PDSP | |||||
5-hydroxytryptamine receptor 2A | GPCR | Ki | 6.83 | WOMBAT-PK | |||||
5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.80 | WOMBAT-PK | |||||
Alpha-1A adrenergic receptor | GPCR | IC50 | 7.50 | WOMBAT-PK | |||||
Alpha-2B adrenergic receptor | GPCR | IC50 | 7.10 | WOMBAT-PK | |||||
D(3) dopamine receptor | GPCR | Ki | 6.41 | WOMBAT-PK | |||||
Histamine H1 receptor | GPCR | IC50 | 7.61 | WOMBAT-PK | |||||
Muscarinic acetylcholine receptor M1 | GPCR | Ki | 7.38 | WOMBAT-PK | |||||
Muscarinic acetylcholine receptor M2 | GPCR | Ki | 8.08 | WOMBAT-PK | |||||
Muscarinic acetylcholine receptor M3 | GPCR | Ki | 7.22 | WOMBAT-PK | |||||
Muscarinic acetylcholine receptor M4 | GPCR | Ki | 6.95 | WOMBAT-PK | |||||
Muscarinic acetylcholine receptor M5 | GPCR | Ki | 7.08 | WOMBAT-PK | |||||
Sodium-dependent dopamine transporter | Transporter | Ki | 5.07 | PDSP | |||||
Adenosine receptor A3 | GPCR | IC50 | 8.36 | CHEMBL | |||||
Voltage-dependent N-type calcium channel subunit alpha-1B | Ion channel | IC50 | 4.66 | CHEMBL | |||||
Major prion protein | Surface antigen | EC50 | 5 | CHEMBL | |||||
Solute carrier family 22 member 1 | Transporter | IC50 | 4.77 | CHEMBL | |||||
Potassium voltage-gated channel subfamily H member 1 | Ion channel | BLOCKER | IC50 | 5.70 | IUPHAR | ||||
Solute carrier family 22 member 2 | Transporter | IC50 | 5.22 | WOMBAT-PK | |||||
Sodium channel alpha subunits; brain (Types I, II, III) | Ion channel | IC50 | 5.44 | CHEMBL | |||||
Sphingomyelin phosphodiesterase | Enzyme | IC50 | 5.30 | CHEMBL | |||||
D(2) dopamine receptor | GPCR | Ki | 6.17 | WOMBAT-PK | |||||
Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 6.28 | WOMBAT-PK | |||||
Alpha-1A adrenergic receptor | GPCR | IC50 | 8.77 | CHEMBL | |||||
Sodium-dependent serotonin transporter | Transporter | Ki | 7.38 | CHEMBL | |||||
Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 6.46 | CHEMBL | |||||
Transporter | Transporter | Ki | 7.92 | CHEMBL | |||||
Sodium-dependent dopamine transporter | Transporter | Ki | 7.38 | CHEMBL | |||||
Sodium-dependent noradrenaline transporter | Transporter | Ki | 7.92 | CHEMBL | |||||
5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.80 | CHEMBL | |||||
D(2) dopamine receptor | GPCR | Ki | 6.14 | CHEMBL | |||||
Sodium-dependent serotonin transporter | Transporter | Ki | 8.30 | CHEMBL | |||||
Histamine H1 receptor | GPCR | IC50 | 10.22 | CHEMBL | |||||
Muscarinic acetylcholine receptor M5 | GPCR | IC50 | 6.52 | CHEMBL | |||||
Pleiotropic ABC efflux transporter of multiple drugs | Transporter | IC50 | 4.66 | CHEMBL | |||||
Glutamate NMDA receptor | Ion channel | IC50 | 4.85 | CHEMBL | |||||
Muscarinic acetylcholine receptor | GPCR | Ki | 7.19 | CHEMBL | |||||
Serotonin (5-HT) receptor | GPCR | IC50 | 7.36 | CHEMBL | |||||
Adrenergic receptor alpha-2 | GPCR | Ki | 6.59 | CHEMBL | |||||
Dopamine receptor | GPCR | IC50 | 6.19 | CHEMBL | |||||
Adrenergic receptor alpha-1 | GPCR | Ki | 7.34 | CHEMBL | |||||
Serotonin 2 (5-HT2) receptor | GPCR | Ki | 7.64 | CHEMBL | |||||
G protein-activated inward rectifier potassium channel 4 | Ion channel | BLOCKER | EC50 | 4.50 | IUPHAR | ||||
G protein-activated inward rectifier potassium channel 2 | Ion channel | BLOCKER | IC50 | 4.30 | IUPHAR | ||||
Sigma intracellular receptor 2 | Unclassified | Ki | 5.68 | CHEMBL |
ID | Source |
---|---|
4019785 | VUID |
N0000147875 | NUI |
D00815 | KEGG_DRUG |
73-07-4 | SECONDARY_CAS_RN |
113-52-0 | SECONDARY_CAS_RN |
10075-24-8 | SECONDARY_CAS_RN |
4017862 | VANDF |
4017863 | VANDF |
4019785 | VANDF |
C0020934 | UMLSCUI |
CHEBI:47499 | CHEBI |
IXX | PDB_CHEM_ID |
CHEMBL11 | ChEMBL_ID |
DB00458 | DRUGBANK_ID |
CHEMBL2105257 | ChEMBL_ID |
CHEMBL1692 | ChEMBL_ID |
CHEMBL3989845 | ChEMBL_ID |
D007099 | MESH_DESCRIPTOR_UI |
3696 | PUBCHEM_CID |
357 | IUPHAR_LIGAND_ID |
793 | INN_ID |
OGG85SX4E4 | UNII |
150816 | RXNORM |
2328 | MMSL |
4870 | MMSL |
4871 | MMSL |
81685 | MMSL |
d00259 | MMSL |
001498 | NDDF |
001499 | NDDF |
001500 | NDDF |
3378009 | SNOMEDCT_US |
36113004 | SNOMEDCT_US |
372718005 | SNOMEDCT_US |
4203009 | SNOMEDCT_US |
1916 | INN_ID |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Imipramine Pamoate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0273 | CAPSULE | 75 mg | ORAL | ANDA | 20 sections |
Imipramine Pamoate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0273 | CAPSULE | 75 mg | ORAL | ANDA | 20 sections |
Imipramine Pamoate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0274 | CAPSULE | 100 mg | ORAL | ANDA | 20 sections |
Imipramine Pamoate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0274 | CAPSULE | 100 mg | ORAL | ANDA | 20 sections |
Imipramine Pamoate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0275 | CAPSULE | 125 mg | ORAL | ANDA | 20 sections |
Imipramine Pamoate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0275 | CAPSULE | 125 mg | ORAL | ANDA | 20 sections |
Imipramine Pamoate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0276 | CAPSULE | 150 mg | ORAL | ANDA | 20 sections |
Imipramine Pamoate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0276 | CAPSULE | 150 mg | ORAL | ANDA | 20 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-1762 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 19 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-1764 | TABLET, FILM COATED | 25 mg | ORAL | ANDA | 19 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-1766 | TABLET, FILM COATED | 50 mg | ORAL | ANDA | 19 sections |
IMIPRAMINE PAMOATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-963 | CAPSULE | 75 mg | ORAL | NDA | 22 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-345 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 24 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-346 | TABLET, FILM COATED | 25 mg | ORAL | ANDA | 24 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-347 | TABLET, FILM COATED | 50 mg | ORAL | ANDA | 24 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49884-054 | TABLET | 10 mg | ORAL | ANDA | 20 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49884-055 | TABLET | 25 mg | ORAL | ANDA | 20 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49884-056 | TABLET | 50 mg | ORAL | ANDA | 20 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-0035 | TABLET, FILM COATED | 25 mg | ORAL | ANDA | 21 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-3148 | TABLET, FILM COATED | 25 mg | ORAL | ANDA | 21 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-3148 | TABLET, FILM COATED | 25 mg | ORAL | ANDA | 21 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50436-2022 | TABLET, FILM COATED | 25 mg | ORAL | ANDA | 21 sections |
IMIPRAMINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51655-455 | TABLET, FILM COATED | 50 mg | ORAL | ANDA | 12 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-1344 | TABLET, FILM COATED | 25 mg | ORAL | ANDA | 20 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-2221 | TABLET, FILM COATED | 50 mg | ORAL | ANDA | 20 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-2571 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 20 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55289-144 | TABLET, FILM COATED | 25 mg | ORAL | ANDA | 19 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55700-709 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 20 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55700-709 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 20 sections |
Imipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55700-710 | TABLET, FILM COATED | 25 mg | ORAL | ANDA | 20 sections |