Stem definition | Drug id | CAS RN |
---|---|---|
substances of the imipramine group | 701 | 303-49-1 |
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 |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 13.24 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 51 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 13 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 8.20 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.03 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 26 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Dec. 29, 1989 | FDA | MALLINCKRODT LLC |
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 |
---|---|---|---|---|---|---|
Coma | 297.57 | 46.53 | 74 | 891 | 8982 | 2348138 |
Toxicity to various agents | 245.97 | 46.53 | 85 | 880 | 32669 | 2324451 |
Serotonin syndrome | 238.84 | 46.53 | 52 | 913 | 3488 | 2353632 |
Overdose | 197.95 | 46.53 | 64 | 901 | 19843 | 2337277 |
Suicide attempt | 183.45 | 46.53 | 53 | 912 | 11229 | 2345891 |
Intentional overdose | 183.27 | 46.53 | 53 | 912 | 11268 | 2345852 |
Drug interaction | 166.58 | 46.53 | 62 | 903 | 29101 | 2328019 |
Hypotension | 128.61 | 46.53 | 53 | 912 | 32383 | 2324737 |
Confusional state | 121.51 | 46.53 | 47 | 918 | 24297 | 2332823 |
Somnolence | 108.87 | 46.53 | 43 | 922 | 23442 | 2333678 |
Tachycardia | 104.80 | 46.53 | 38 | 927 | 16371 | 2340749 |
Acute kidney injury | 104.72 | 46.53 | 44 | 921 | 28078 | 2329042 |
Neuroleptic malignant syndrome | 104.11 | 46.53 | 24 | 941 | 2056 | 2355064 |
Drug abuse | 100.34 | 46.53 | 34 | 931 | 11992 | 2345128 |
Poisoning deliberate | 94.19 | 46.53 | 20 | 945 | 1171 | 2355949 |
Electrocardiogram QT prolonged | 93.27 | 46.53 | 29 | 936 | 7785 | 2349335 |
Drug ineffective | 88.17 | 46.53 | 60 | 905 | 101564 | 2255556 |
Agitation | 87.28 | 46.53 | 30 | 935 | 11021 | 2346099 |
Fall | 85.92 | 46.53 | 45 | 920 | 47054 | 2310066 |
Cerebellar syndrome | 83.21 | 46.53 | 16 | 949 | 565 | 2356555 |
International normalised ratio abnormal | 76.41 | 46.53 | 15 | 950 | 591 | 2356529 |
Hyperchloraemia | 73.08 | 46.53 | 11 | 954 | 83 | 2357037 |
Polyuria | 71.88 | 46.53 | 16 | 949 | 1166 | 2355954 |
Bezoar | 70.96 | 46.53 | 12 | 953 | 201 | 2356919 |
Hyponatraemia | 70.80 | 46.53 | 27 | 938 | 13298 | 2343822 |
Tremor | 65.77 | 46.53 | 29 | 936 | 20632 | 2336488 |
Depressed level of consciousness | 65.29 | 46.53 | 22 | 943 | 7582 | 2349538 |
Intentional self-injury | 65.05 | 46.53 | 19 | 946 | 4108 | 2353012 |
Anxiety | 61.91 | 46.53 | 31 | 934 | 29328 | 2327792 |
Akathisia | 61.23 | 46.53 | 15 | 950 | 1659 | 2355461 |
Depression | 57.23 | 46.53 | 29 | 936 | 28103 | 2329017 |
Sopor | 56.86 | 46.53 | 17 | 948 | 3978 | 2353142 |
Drug withdrawal syndrome neonatal | 55.70 | 46.53 | 11 | 954 | 446 | 2356674 |
Myoclonus | 55.36 | 46.53 | 15 | 950 | 2468 | 2354652 |
Hypernatraemia | 53.79 | 46.53 | 12 | 953 | 882 | 2356238 |
Product use in unapproved indication | 53.42 | 46.53 | 21 | 944 | 11179 | 2345941 |
Antipsychotic drug level increased | 53.30 | 46.53 | 11 | 954 | 558 | 2356562 |
Off label use | 53.14 | 46.53 | 39 | 926 | 73559 | 2283561 |
Hepatitis | 53.06 | 46.53 | 18 | 947 | 6319 | 2350801 |
Completed suicide | 52.67 | 46.53 | 25 | 940 | 21009 | 2336111 |
Exposure during pregnancy | 51.28 | 46.53 | 26 | 939 | 25193 | 2331927 |
Sinus tachycardia | 51.02 | 46.53 | 15 | 950 | 3310 | 2353810 |
Suicidal ideation | 50.12 | 46.53 | 20 | 945 | 11067 | 2346053 |
Muscle rigidity | 50.04 | 46.53 | 13 | 952 | 1818 | 2355302 |
Constipation | 48.98 | 46.53 | 24 | 941 | 21605 | 2335515 |
Hyperthermia | 47.87 | 46.53 | 12 | 953 | 1456 | 2355664 |
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 |
---|---|---|---|---|---|---|
Toxicity to various agents | 207.29 | 45.20 | 74 | 563 | 29067 | 1717077 |
Overdose | 159.15 | 45.20 | 53 | 584 | 16648 | 1729496 |
Agitation | 129.11 | 45.20 | 41 | 596 | 10985 | 1735159 |
Suicide attempt | 122.86 | 45.20 | 36 | 601 | 7345 | 1738799 |
Serotonin syndrome | 120.58 | 45.20 | 29 | 608 | 2759 | 1743385 |
Intentional overdose | 108.45 | 45.20 | 33 | 604 | 7637 | 1738507 |
Obsessive-compulsive disorder | 105.83 | 45.20 | 21 | 616 | 807 | 1745337 |
Completed suicide | 98.48 | 45.20 | 37 | 600 | 16275 | 1729869 |
Therapeutic product effect variable | 83.05 | 45.20 | 13 | 624 | 119 | 1746025 |
Drug ineffective | 82.83 | 45.20 | 50 | 587 | 63751 | 1682393 |
Akathisia | 79.43 | 45.20 | 18 | 619 | 1310 | 1744834 |
Antipsychotic drug level below therapeutic | 78.38 | 45.20 | 13 | 624 | 176 | 1745968 |
Cardio-respiratory arrest | 78.18 | 45.20 | 27 | 610 | 9266 | 1736878 |
Coma | 72.47 | 45.20 | 24 | 613 | 7238 | 1738906 |
Disinhibition | 70.61 | 45.20 | 13 | 624 | 331 | 1745813 |
Euphoric mood | 70.19 | 45.20 | 15 | 622 | 830 | 1745314 |
Coma scale abnormal | 69.34 | 45.20 | 14 | 623 | 585 | 1745559 |
Poisoning deliberate | 64.58 | 45.20 | 14 | 623 | 828 | 1745316 |
Increased appetite | 62.60 | 45.20 | 14 | 623 | 957 | 1745187 |
Tremor | 62.06 | 45.20 | 25 | 612 | 13106 | 1733038 |
Hyperhidrosis | 59.77 | 45.20 | 24 | 613 | 12464 | 1733680 |
Neuroleptic malignant syndrome | 59.47 | 45.20 | 17 | 620 | 3131 | 1743013 |
Neutrophil count increased | 58.07 | 45.20 | 16 | 621 | 2577 | 1743567 |
Electrocardiogram QT prolonged | 57.98 | 45.20 | 19 | 618 | 5526 | 1740618 |
Speech disorder | 57.46 | 45.20 | 18 | 619 | 4530 | 1741614 |
Sopor | 57.32 | 45.20 | 15 | 622 | 1986 | 1744158 |
White blood cell count increased | 56.62 | 45.20 | 20 | 617 | 7292 | 1738852 |
Drug interaction | 55.21 | 45.20 | 29 | 608 | 27929 | 1718215 |
Hypovolaemic shock | 52.59 | 45.20 | 12 | 625 | 896 | 1745248 |
Hallucination, auditory | 47.09 | 45.20 | 13 | 624 | 2104 | 1744040 |
Therapeutic product effect incomplete | 46.36 | 45.20 | 16 | 621 | 5432 | 1740712 |
Loose associations | 45.28 | 45.20 | 6 | 631 | 13 | 1746131 |
Source | Code | Description |
---|---|---|
ATC | N06AA04 | NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Non-selective monoamine reuptake inhibitors |
CHEBI has role | CHEBI:50949 | serotonin uptake inhibitor |
CHEBI has role | CHEBI:35469 | antidepressant |
CHEBI has role | CHEBI:48279 | serotonergic antagonist |
CHEBI has role | CHEBI:48278 | serotonergic drug |
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 |
MeSH PA | D018490 | Serotonin Agents |
MeSH PA | D017367 | Serotonin Uptake Inhibitors |
FDA EPC | N0000175752 | Tricyclic Antidepressant |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Obsessive-compulsive disorder | indication | 191736004 | DOID:10933 |
Depressive disorder | off-label use | 35489007 | |
Cataplexy | off-label use | 46263000 | |
Anxiety | off-label use | 48694002 | |
Panic disorder | off-label use | 371631005 | DOID:594 |
Suicidal thoughts | contraindication | 6471006 | |
Alcoholism | contraindication | 7200002 | |
Glaucoma | contraindication | 23986001 | DOID:1686 |
Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
Acute nephropathy | contraindication | 58574008 | |
Epilepsy | contraindication | 84757009 | DOID:1826 |
Bipolar affective disorder, current episode manic | contraindication | 191618007 | |
Disease of liver | contraindication | 235856003 | DOID:409 |
Retention of urine | contraindication | 267064002 | |
Pheochromocytoma | contraindication | 302835009 | |
Malignant hyperthermia | contraindication | 405501007 | |
Myocardial infarction in recovery phase | contraindication | 418044006 | |
Neuroblastoma | contraindication | 432328008 | DOID:769 |
Atrioventricular Conduction Defect | contraindication |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 9.04 | Basic |
pKa2 | 6.19 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Sodium-dependent serotonin transporter | Transporter | INHIBITOR | Ki | 9.70 | PDSP | CHEMBL | |||
Sodium-dependent noradrenaline transporter | Transporter | INHIBITOR | Kd | 7.42 | WOMBAT-PK | IUPHAR | |||
5-hydroxytryptamine receptor 2A | GPCR | Ki | 7.45 | PDSP | |||||
D(1A) dopamine receptor | GPCR | Ki | 6.66 | PDSP | |||||
D(2) dopamine receptor | GPCR | Ki | 6.95 | PDSP | |||||
Alpha-2A adrenergic receptor | GPCR | Ki | 6.28 | PDSP | |||||
Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 6.24 | DRUG MATRIX | |||||
5-hydroxytryptamine receptor 2B | GPCR | Ki | 6.82 | DRUG MATRIX | |||||
Alpha-2B adrenergic receptor | GPCR | Ki | 7.34 | DRUG MATRIX | |||||
Histamine H1 receptor | GPCR | Ki | 8.01 | DRUG MATRIX | |||||
Histamine H2 receptor | GPCR | Ki | 5.70 | DRUG MATRIX | |||||
Muscarinic acetylcholine receptor M1 | GPCR | Ki | 7.66 | DRUG MATRIX | |||||
Muscarinic acetylcholine receptor M2 | GPCR | Ki | 7.07 | DRUG MATRIX | |||||
Muscarinic acetylcholine receptor M3 | GPCR | Ki | 7.44 | DRUG MATRIX | |||||
Muscarinic acetylcholine receptor M4 | GPCR | Ki | 7.89 | DRUG MATRIX | |||||
Muscarinic acetylcholine receptor M5 | GPCR | Ki | 7.42 | DRUG MATRIX | |||||
Alpha-2C adrenergic receptor | GPCR | Ki | 6.69 | DRUG MATRIX | |||||
Alpha-1D adrenergic receptor | GPCR | Ki | 7.40 | DRUG MATRIX | |||||
Solute carrier family 22 member 1 | Transporter | IC50 | 4.71 | CHEMBL | |||||
5-hydroxytryptamine receptor 6 | GPCR | Ki | 6.95 | CHEMBL | |||||
Sodium-dependent dopamine transporter | Transporter | IC50 | 5.56 | CHEMBL | |||||
Glutathione S-transferase P | Enzyme | WOMBAT-PK | |||||||
Cytochrome P450 2D6 | Enzyme | Ki | 5.66 | WOMBAT-PK | |||||
Aldehyde oxidase | Enzyme | IC50 | 6.32 | WOMBAT-PK | |||||
Alpha-1A adrenergic receptor | GPCR | Ki | 8.49 | WOMBAT-PK | |||||
D(3) dopamine receptor | GPCR | Ki | 7.41 | PDSP | |||||
5-hydroxytryptamine receptor 2C | GPCR | Ki | 7.19 | PDSP | |||||
Alpha-1B adrenergic receptor | GPCR | Ki | 7.14 | DRUG MATRIX | |||||
Membrane-associated progesterone receptor component 1 | Membrane receptor | Ki | 5.94 | DRUG MATRIX | |||||
Trypanothione reductase | Enzyme | Ki | 5.19 | CHEMBL | |||||
Serotonin 2 (5-HT2) receptor | GPCR | Ki | 8.08 | CHEMBL | |||||
Adrenergic receptor alpha-2 | GPCR | Ki | 7.29 | CHEMBL | |||||
Alpha-1A adrenergic receptor | GPCR | IC50 | 10.40 | CHEMBL | |||||
Serotonin 1 (5-HT1) receptor | GPCR | Ki | 5.30 | CHEMBL | |||||
Histamine H1 receptor | GPCR | IC50 | 9.70 | CHEMBL | |||||
Serotonin (5-HT) receptor | GPCR | IC50 | 8.30 | CHEMBL | |||||
Sodium-dependent noradrenaline transporter | Transporter | IC50 | 6.05 | CHEMBL | |||||
D(2) dopamine receptor | GPCR | Ki | 7.25 | CHEMBL | |||||
Sodium-dependent serotonin transporter | Transporter | IC50 | 7.15 | CHEMBL | |||||
Trypanothione reductase | Unclassified | IC50 | 5.47 | CHEMBL | |||||
G protein-activated inward rectifier potassium channel 2 | Ion channel | BLOCKER | IC50 | 4.40 | IUPHAR |
ID | Source |
---|---|
D002997 | MESH_DESCRIPTOR_UI |
4019687 | VUID |
N0000147779 | NUI |
C0009010 | UMLSCUI |
D00811 | KEGG_DRUG |
2LXW0L6GWJ | UNII |
17321-77-6 | SECONDARY_CAS_RN |
96209002 | SNOMEDCT_US |
4019687 | VANDF |
2597 | RXNORM |
004614 | NDDF |
372903001 | SNOMEDCT_US |
d00876 | MMSL |
CHEMBL415 | ChEMBL_ID |
CHEMBL1200710 | ChEMBL_ID |
2238 | INN_ID |
DB01242 | DRUGBANK_ID |
CHEBI:47780 | CHEBI |
2398 | IUPHAR_LIGAND_ID |
2801 | PUBCHEM_CID |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Clomipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-3025 | CAPSULE | 25 mg | ORAL | ANDA | 15 sections |
Clomipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-3050 | CAPSULE | 50 mg | ORAL | ANDA | 15 sections |
Clomipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-3075 | CAPSULE | 75 mg | ORAL | ANDA | 15 sections |
CLOMIPRAMINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0406-8806 | CAPSULE | 25 mg | ORAL | NDA | 15 sections |
CLOMIPRAMINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0406-8807 | CAPSULE | 50 mg | ORAL | NDA | 15 sections |
CLOMIPRAMINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0406-8808 | CAPSULE | 75 mg | ORAL | NDA | 15 sections |
ANAFRANIL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0406-9906 | CAPSULE | 25 mg | ORAL | NDA | 15 sections |
ANAFRANIL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0406-9907 | CAPSULE | 50 mg | ORAL | NDA | 15 sections |
ANAFRANIL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0406-9908 | CAPSULE | 75 mg | ORAL | NDA | 15 sections |
Clomipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-2027 | CAPSULE | 25 mg | ORAL | ANDA | 15 sections |
Clomipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-2037 | CAPSULE | 50 mg | ORAL | ANDA | 15 sections |
Clomipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0832-0630 | CAPSULE | 25 mg | ORAL | ANDA | 15 sections |
Clomipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0832-0631 | CAPSULE | 50 mg | ORAL | ANDA | 15 sections |
Clomipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0832-0632 | CAPSULE | 75 mg | ORAL | ANDA | 15 sections |
Clomipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-849 | CAPSULE | 25 mg | ORAL | ANDA | 15 sections |
Clomipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-850 | CAPSULE | 50 mg | ORAL | ANDA | 15 sections |
Clomipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-851 | CAPSULE | 75 mg | ORAL | ANDA | 15 sections |
Clomipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43063-257 | CAPSULE | 25 mg | ORAL | ANDA | 15 sections |
CLOMIPRAMINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51672-4011 | CAPSULE | 25 mg | ORAL | ANDA | 16 sections |
CLOMIPRAMINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51672-4012 | CAPSULE | 50 mg | ORAL | ANDA | 16 sections |
CLOMIPRAMINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51672-4013 | CAPSULE | 75 mg | ORAL | ANDA | 16 sections |
CLOMIPRAMINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-4023 | CAPSULE | 50 mg | ORAL | ANDA | 16 sections |
Clomipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59746-710 | CAPSULE | 25 mg | ORAL | ANDA | 16 sections |
Clomipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59746-711 | CAPSULE | 50 mg | ORAL | ANDA | 16 sections |
Clomipramine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59746-712 | CAPSULE | 75 mg | ORAL | ANDA | 16 sections |
CLOMIPRAMINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60429-287 | CAPSULE | 25 mg | ORAL | ANDA | 16 sections |
CLOMIPRAMINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60429-288 | CAPSULE | 75 mg | ORAL | ANDA | 16 sections |
CLOMIPRAMINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60429-289 | CAPSULE | 50 mg | ORAL | ANDA | 16 sections |
CLOMIPRAMINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68084-790 | CAPSULE | 25 mg | ORAL | ANDA | 16 sections |
CLOMIPRAMINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68084-818 | CAPSULE | 50 mg | ORAL | ANDA | 16 sections |