Stem definition | Drug id | CAS RN |
---|---|---|
2113 | 58-39-9 |
Dose | Unit | Route |
---|---|---|
30 | mg | O |
7 | mg | P |
10 | mg | P |
16 | mg | R |
Property | Value | Reference |
---|---|---|
MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.99 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 40 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 18 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 27 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.07 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 9.40 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Feb. 27, 1957 | 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 |
---|---|---|---|---|---|---|
Blood magnesium increased | 78.99 | 26.26 | 20 | 2713 | 2931 | 56286403 |
Pleural fibrosis | 75.84 | 26.26 | 20 | 2713 | 3439 | 56285895 |
Pleural thickening | 75.59 | 26.26 | 19 | 2714 | 2704 | 56286630 |
Presbyacusis | 74.81 | 26.26 | 19 | 2714 | 2819 | 56286515 |
Tardive dyskinesia | 71.26 | 26.26 | 23 | 2710 | 8008 | 56281326 |
Deafness neurosensory | 65.32 | 26.26 | 19 | 2714 | 4679 | 56284655 |
Sopor | 62.71 | 26.26 | 27 | 2706 | 20895 | 56268439 |
Epigastric discomfort | 59.98 | 26.26 | 19 | 2714 | 6229 | 56283105 |
Drug abuse | 56.12 | 26.26 | 37 | 2696 | 67573 | 56221761 |
Mitochondrial encephalomyopathy | 52.59 | 26.26 | 7 | 2726 | 22 | 56289312 |
Cyst | 50.15 | 26.26 | 20 | 2713 | 12758 | 56276576 |
Ileus paralytic | 45.46 | 26.26 | 14 | 2719 | 4181 | 56285153 |
Blood potassium increased | 44.35 | 26.26 | 20 | 2713 | 17241 | 56272093 |
Osteopenia | 43.40 | 26.26 | 20 | 2713 | 18121 | 56271213 |
Neuroleptic malignant syndrome | 38.32 | 26.26 | 16 | 2717 | 11462 | 56277872 |
Deformity | 36.62 | 26.26 | 15 | 2718 | 10240 | 56279094 |
Bone cyst | 35.93 | 26.26 | 10 | 2723 | 2100 | 56287234 |
Skin lesion | 35.11 | 26.26 | 20 | 2713 | 28115 | 56261219 |
Moaning | 34.68 | 26.26 | 8 | 2725 | 791 | 56288543 |
Hyperprolactinaemia | 34.58 | 26.26 | 11 | 2722 | 3650 | 56285684 |
Osteosclerosis | 34.57 | 26.26 | 11 | 2722 | 3652 | 56285682 |
Onychophagia | 31.93 | 26.26 | 5 | 2728 | 59 | 56289275 |
Intentional self-injury | 31.81 | 26.26 | 18 | 2715 | 24974 | 56264360 |
Extrapyramidal disorder | 30.73 | 26.26 | 14 | 2719 | 12342 | 56276992 |
Dry eye | 30.70 | 26.26 | 20 | 2713 | 35696 | 56253638 |
Metabolic syndrome | 30.26 | 26.26 | 8 | 2725 | 1385 | 56287949 |
Muscle rigidity | 29.44 | 26.26 | 13 | 2720 | 10658 | 56278676 |
Bradykinesia | 27.73 | 26.26 | 10 | 2723 | 4844 | 56284490 |
Sports injury | 27.30 | 26.26 | 4 | 2729 | 29 | 56289305 |
Blood glucose | 26.84 | 26.26 | 4 | 2729 | 33 | 56289301 |
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 |
---|---|---|---|---|---|---|
Akathisia | 350.38 | 47.21 | 85 | 2186 | 7168 | 31687905 |
Therapeutic product effect variable | 335.74 | 47.21 | 65 | 2206 | 1873 | 31693200 |
Antipsychotic drug level below therapeutic | 333.22 | 47.21 | 65 | 2206 | 1950 | 31693123 |
Obsessive-compulsive disorder | 317.60 | 47.21 | 73 | 2198 | 4864 | 31690209 |
Disinhibition | 314.41 | 47.21 | 65 | 2206 | 2628 | 31692445 |
Euphoric mood | 285.92 | 47.21 | 67 | 2204 | 4853 | 31690220 |
Increased appetite | 258.97 | 47.21 | 65 | 2206 | 6279 | 31688794 |
Suicide attempt | 152.54 | 47.21 | 67 | 2204 | 37181 | 31657892 |
Therapeutic product effect incomplete | 139.21 | 47.21 | 66 | 2205 | 43630 | 31651443 |
Dyslipidaemia | 126.17 | 47.21 | 37 | 2234 | 6369 | 31688704 |
Leukopenia | 124.50 | 47.21 | 67 | 2204 | 57761 | 31637312 |
Toxicity to various agents | 122.88 | 47.21 | 102 | 2169 | 181385 | 31513688 |
Leukaemia | 114.50 | 47.21 | 31 | 2240 | 3994 | 31691079 |
Weight increased | 112.00 | 47.21 | 71 | 2200 | 82876 | 31612197 |
Obesity | 102.32 | 47.21 | 36 | 2235 | 11064 | 31684009 |
Prescribed overdose | 89.26 | 47.21 | 31 | 2240 | 9161 | 31685912 |
Neuroleptic malignant syndrome | 74.26 | 47.21 | 32 | 2239 | 16837 | 31678236 |
Drug ineffective | 53.02 | 47.21 | 98 | 2173 | 395475 | 31299598 |
Schizoaffective disorder | 51.58 | 47.21 | 13 | 2258 | 1262 | 31693811 |
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 |
---|---|---|---|---|---|---|
Akathisia | 120.05 | 28.47 | 39 | 3858 | 12254 | 70912293 |
Neuroleptic malignant syndrome | 88.27 | 28.47 | 38 | 3859 | 25969 | 70898578 |
Blood magnesium increased | 74.11 | 28.47 | 20 | 3877 | 3311 | 70921236 |
Presbyacusis | 73.84 | 28.47 | 19 | 3878 | 2618 | 70921929 |
Pleural thickening | 72.50 | 28.47 | 19 | 3878 | 2813 | 70921734 |
Antipsychotic drug level below therapeutic | 69.45 | 28.47 | 15 | 3882 | 970 | 70923577 |
Tardive dyskinesia | 67.43 | 28.47 | 24 | 3873 | 9905 | 70914642 |
Therapeutic product effect variable | 66.33 | 28.47 | 16 | 3881 | 1694 | 70922853 |
Completed suicide | 65.36 | 28.47 | 71 | 3826 | 227064 | 70697483 |
Pleural fibrosis | 65.36 | 28.47 | 19 | 3878 | 4120 | 70920427 |
Toxicity to various agents | 56.80 | 28.47 | 86 | 3811 | 382086 | 70542461 |
Disinhibition | 56.80 | 28.47 | 15 | 3882 | 2286 | 70922261 |
Deafness neurosensory | 56.54 | 28.47 | 19 | 3878 | 6613 | 70917934 |
Hyperprolactinaemia | 55.53 | 28.47 | 17 | 3880 | 4396 | 70920151 |
Ileus paralytic | 55.07 | 28.47 | 20 | 3877 | 8741 | 70915806 |
Epigastric discomfort | 54.92 | 28.47 | 19 | 3878 | 7214 | 70917333 |
Obsessive-compulsive disorder | 52.25 | 28.47 | 17 | 3880 | 5353 | 70919194 |
Sopor | 51.96 | 28.47 | 28 | 3869 | 31239 | 70893308 |
Mitochondrial encephalomyopathy | 50.61 | 28.47 | 7 | 3890 | 27 | 70924520 |
Euphoric mood | 48.10 | 28.47 | 17 | 3880 | 6872 | 70917675 |
Cyst | 47.83 | 28.47 | 20 | 3877 | 12699 | 70911848 |
Intentional self-injury | 46.14 | 28.47 | 26 | 3871 | 31624 | 70892923 |
Drug abuse | 42.22 | 28.47 | 46 | 3851 | 147210 | 70777337 |
Dyslipidaemia | 42.16 | 28.47 | 17 | 3880 | 9843 | 70914704 |
Osteopenia | 39.54 | 28.47 | 19 | 3878 | 16678 | 70907869 |
Muscle rigidity | 37.55 | 28.47 | 19 | 3878 | 18631 | 70905916 |
Schizoaffective disorder | 35.12 | 28.47 | 10 | 3887 | 2013 | 70922534 |
Deformity | 34.42 | 28.47 | 14 | 3883 | 8283 | 70916264 |
Increased appetite | 34.32 | 28.47 | 15 | 3882 | 10598 | 70913949 |
Blood potassium increased | 33.33 | 28.47 | 20 | 3877 | 27306 | 70897241 |
Bradyphrenia | 31.98 | 28.47 | 14 | 3883 | 9932 | 70914615 |
Bone cyst | 31.65 | 28.47 | 10 | 3887 | 2864 | 70921683 |
Moaning | 31.46 | 28.47 | 8 | 3889 | 1051 | 70923496 |
Obesity | 31.12 | 28.47 | 19 | 3878 | 26752 | 70897795 |
Dry eye | 30.27 | 28.47 | 20 | 3877 | 32262 | 70892285 |
Osteosclerosis | 29.16 | 28.47 | 10 | 3887 | 3695 | 70920852 |
Onychophagia | 28.88 | 28.47 | 5 | 3892 | 99 | 70924448 |
None
Source | Code | Description |
---|---|---|
ATC | N05AB03 | NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Phenothiazines with piperazine structure |
FDA CS | M0016525 | Phenothiazines |
MeSH PA | D014150 | Antipsychotic Agents |
MeSH PA | D002491 | Central Nervous System Agents |
MeSH PA | D002492 | Central Nervous System Depressants |
MeSH PA | D015259 | Dopamine Agents |
MeSH PA | D018492 | Dopamine Antagonists |
MeSH PA | D018377 | Neurotransmitter Agents |
MeSH PA | D011619 | Psychotropic Drugs |
MeSH PA | D014149 | Tranquilizing Agents |
CHEBI has role | CHEBI:37930 | phenothiazine antipsychotic drugs |
CHEBI has role | CHEBI:48561 | dopaminergic antagonists |
CHEBI has role | CHEBI:50919 | antiemetico |
FDA EPC | N0000175746 | Phenothiazine |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Nausea and vomiting | indication | 16932000 | |
Schizophrenia | indication | 58214004 | DOID:5419 |
Mixed anxiety and depressive disorder | indication | 231504006 | |
Suicidal thoughts | contraindication | 6471006 | |
Alcoholism | contraindication | 7200002 | |
Organophosphate poisoning | contraindication | 8260003 | |
Weight gain finding | contraindication | 8943002 | |
Sinus tachycardia | contraindication | 11092001 | |
Neuroleptic malignant syndrome | contraindication | 15244003 | DOID:14464 |
Senile dementia | contraindication | 15662003 | |
Chronic disease of respiratory system | contraindication | 17097001 | |
Myocardial infarction | contraindication | 22298006 | DOID:5844 |
Glaucoma | contraindication | 23986001 | DOID:1686 |
Orthostatic hypotension | contraindication | 28651003 | |
Torsades de pointes | contraindication | 31722008 | |
Parkinsonism | contraindication | 32798002 | |
Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
Conduction disorder of the heart | contraindication | 44808001 | |
Chronic heart failure | contraindication | 48447003 | |
Bradycardia | contraindication | 48867003 | |
Paralytic ileus | contraindication | 55525008 | DOID:8442 |
Extrapyramidal disease | contraindication | 76349003 | |
Hyperglycemia | contraindication | 80394007 | DOID:4195 |
Chronic idiopathic constipation | contraindication | 82934008 | |
Open-angle glaucoma | contraindication | 84494001 | DOID:1067 |
Epilepsy | contraindication | 84757009 | DOID:1826 |
Leukopenia | contraindication | 84828003 | DOID:615 |
Stupor | contraindication | 89458003 | |
Tardive dyskinesia | contraindication | 102449007 | |
Prolonged QT interval | contraindication | 111975006 | |
Acute disease of cardiovascular system | contraindication | 128487001 | |
Bipolar affective disorder, current episode manic | contraindication | 191618007 | |
Angina pectoris | contraindication | 194828000 | |
Disease of liver | contraindication | 235856003 | DOID:409 |
Metabolic syndrome X | contraindication | 237602007 | DOID:14221 |
Hyperprolactinemia | contraindication | 237662005 | DOID:12700 |
Benign prostatic hyperplasia | contraindication | 266569009 | |
Retention of urine | contraindication | 267064002 | |
Syncope | contraindication | 271594007 | |
Anemia | contraindication | 271737000 | DOID:2355 |
Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
Coma | contraindication | 371632003 | |
At risk for aspiration | contraindication | 371736008 | |
Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
Visual impairment | contraindication | 397540003 | |
Breastfeeding (mother) | contraindication | 413712001 | |
Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
Obesity | contraindication | 414916001 | DOID:9970 |
Myocardial infarction in recovery phase | contraindication | 418044006 | |
Congenital long QT syndrome | contraindication | 442917000 | |
Carcinoma of female breast | contraindication | 447782002 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 8.21 | Basic |
pKa2 | 4.21 | Basic |
pKa3 | 2.21 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
D(2) dopamine receptor | GPCR | ANTAGONIST | Ki | 9.32 | WOMBAT-PK | CHEMBL | |||
Potassium voltage-gated channel subfamily H member 2 | Ion channel | Ki | 5.46 | DRUG MATRIX | |||||
5-hydroxytryptamine receptor 1A | GPCR | Ki | 6.07 | WOMBAT-PK | |||||
5-hydroxytryptamine receptor 2A | GPCR | Ki | 8.25 | WOMBAT-PK | |||||
5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.88 | WOMBAT-PK | |||||
5-hydroxytryptamine receptor 6 | GPCR | Ki | 7.55 | WOMBAT-PK | |||||
5-hydroxytryptamine receptor 7 | GPCR | Ki | 7.64 | WOMBAT-PK | |||||
Alpha-1A adrenergic receptor | GPCR | Ki | 8 | WOMBAT-PK | |||||
Alpha-2B adrenergic receptor | GPCR | Ki | 6.98 | WOMBAT-PK | |||||
D(3) dopamine receptor | GPCR | Ki | 9.52 | WOMBAT-PK | |||||
Histamine H1 receptor | GPCR | Ki | 8.09 | WOMBAT-PK | |||||
Muscarinic acetylcholine receptor M3 | GPCR | Ki | 5.73 | PDSP | |||||
Aldehyde oxidase | Enzyme | IC50 | 7.48 | WOMBAT-PK | |||||
Alpha-2C adrenergic receptor | GPCR | Ki | 7.07 | WOMBAT-PK | |||||
D(4) dopamine receptor | GPCR | Ki | 7.59 | WOMBAT-PK | |||||
Alpha-2A adrenergic receptor | GPCR | Ki | 6.19 | WOMBAT-PK | |||||
5-hydroxytryptamine receptor 7 | GPCR | ANTAGONIST | Ki | 7.60 | IUPHAR | ||||
5-hydroxytryptamine receptor 6 | GPCR | ANTAGONIST | Ki | 7.80 | IUPHAR | ||||
Pleiotropic ABC efflux transporter of multiple drugs | Transporter | IC50 | 5.85 | CHEMBL |
ID | Source |
---|---|
4017939 | VUID |
N0000146289 | NUI |
D00503 | KEGG_DRUG |
4017939 | VANDF |
C0031184 | UMLSCUI |
CHEBI:8028 | CHEBI |
CHEMBL567 | ChEMBL_ID |
D010546 | MESH_DESCRIPTOR_UI |
DB00850 | DRUGBANK_ID |
4748 | PUBCHEM_CID |
209 | IUPHAR_LIGAND_ID |
637 | INN_ID |
FTA7XXY4EZ | UNII |
8076 | RXNORM |
2271 | MMSL |
5261 | MMSL |
d00855 | MMSL |
001477 | NDDF |
387229007 | SNOMEDCT_US |
41147003 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Perphenazine and Amitriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-0042 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 20 sections |
Perphenazine and Amitriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-0042 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 20 sections |
Perphenazine and Amitriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-0073 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 20 sections |
Perphenazine and Amitriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-0073 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 20 sections |
Perphenazine and Amitriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-0330 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 20 sections |
Perphenazine and Amitriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-0330 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 20 sections |
Perphenazine and Amitriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-0442 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 20 sections |
Perphenazine and Amitriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-0442 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 20 sections |
Perphenazine and Amitriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-0574 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 20 sections |
Perphenazine and Amitriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-0574 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 20 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-5350 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 18 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-5351 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 18 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-5352 | TABLET, FILM COATED | 8 mg | ORAL | ANDA | 18 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-5353 | TABLET, FILM COATED | 16 mg | ORAL | ANDA | 18 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-4101 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 20 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-4102 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 20 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-4103 | TABLET, FILM COATED | 8 mg | ORAL | ANDA | 20 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-4104 | TABLET, FILM COATED | 16 mg | ORAL | ANDA | 20 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0603-5060 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 19 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0603-5060 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 19 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0603-5061 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 19 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0603-5061 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 19 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0603-5062 | TABLET, FILM COATED | 8 mg | ORAL | ANDA | 19 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0603-5062 | TABLET, FILM COATED | 8 mg | ORAL | ANDA | 19 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0603-5063 | TABLET, FILM COATED | 16 mg | ORAL | ANDA | 19 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0603-5063 | TABLET, FILM COATED | 16 mg | ORAL | ANDA | 19 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-8046 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 20 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-8046 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 20 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-8047 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 20 sections |
Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-8047 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 20 sections |