Stem definition | Drug id | CAS RN |
---|---|---|
antihypertensives, clonidine derivatives | 1856 | 75438-57-2 |
Molecule | Description |
---|---|
Synonyms:
|
|
Dose | Unit | Route |
---|---|---|
0.30 | mg | O |
Property | Value | Reference |
---|---|---|
MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.12 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 88 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 1.80 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 11 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.93 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 2.20 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Jan. 1, 1991 | YEAR INTRODUCED |
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 |
---|---|---|---|---|---|---|
General physical health deterioration | 138.37 | 26.69 | 97 | 3303 | 142337 | 50459387 |
Renal impairment | 93.63 | 26.69 | 60 | 3340 | 75601 | 50526123 |
Hypertensive crisis | 69.75 | 26.69 | 28 | 3372 | 13126 | 50588598 |
Acute kidney injury | 58.37 | 26.69 | 74 | 3326 | 227984 | 50373740 |
Product prescribing error | 54.25 | 26.69 | 27 | 3373 | 20934 | 50580790 |
Electrocardiogram abnormal | 53.91 | 26.69 | 20 | 3380 | 7585 | 50594139 |
Lactic acidosis | 47.60 | 26.69 | 29 | 3371 | 33326 | 50568398 |
Bradycardia | 42.62 | 26.69 | 35 | 3365 | 64391 | 50537333 |
Hyperammonaemia | 39.36 | 26.69 | 14 | 3386 | 4710 | 50597014 |
Traumatic haemorrhage | 36.18 | 26.69 | 8 | 3392 | 470 | 50601254 |
Mental disability | 35.55 | 26.69 | 6 | 3394 | 82 | 50601642 |
Electrolyte imbalance | 35.43 | 26.69 | 19 | 3381 | 17150 | 50584574 |
Therapeutic drug monitoring analysis not performed | 33.09 | 26.69 | 8 | 3392 | 697 | 50601027 |
Hyperkalaemia | 31.53 | 26.69 | 26 | 3374 | 48063 | 50553661 |
Genotype drug resistance test positive | 28.40 | 26.69 | 6 | 3394 | 284 | 50601440 |
Orthostatic hypotension | 28.27 | 26.69 | 20 | 3380 | 29461 | 50572263 |
Arterial haemorrhage | 26.81 | 26.69 | 8 | 3392 | 1549 | 50600175 |
Medication error | 26.80 | 26.69 | 21 | 3379 | 36083 | 50565641 |
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 |
---|---|---|---|---|---|---|
Labelled drug-drug interaction medication error | 66.13 | 24.43 | 30 | 3074 | 12129 | 29559294 |
Product prescribing error | 55.01 | 24.43 | 30 | 3074 | 17946 | 29553477 |
Benign gastrointestinal neoplasm | 54.91 | 24.43 | 10 | 3094 | 135 | 29571288 |
Hyperkaliuria | 51.46 | 24.43 | 9 | 3095 | 95 | 29571328 |
Acute kidney injury | 47.70 | 24.43 | 93 | 3011 | 265174 | 29306249 |
Peripheral artery stenosis | 37.33 | 24.43 | 10 | 3094 | 837 | 29570586 |
Polypectomy | 36.95 | 24.43 | 9 | 3095 | 515 | 29570908 |
Chylothorax | 34.98 | 24.43 | 9 | 3095 | 644 | 29570779 |
Drug interaction | 33.90 | 24.43 | 68 | 3036 | 197317 | 29374106 |
Sprue-like enteropathy | 33.29 | 24.43 | 8 | 3096 | 432 | 29570991 |
Schizophrenia | 31.93 | 24.43 | 15 | 3089 | 6550 | 29564873 |
Linear IgA disease | 31.89 | 24.43 | 10 | 3094 | 1459 | 29569964 |
Histology abnormal | 30.99 | 24.43 | 7 | 3097 | 288 | 29571135 |
Hypotension | 26.49 | 24.43 | 61 | 3043 | 194293 | 29377130 |
Cardiac failure | 25.17 | 24.43 | 36 | 3068 | 79251 | 29492172 |
Pneumonia haemophilus | 24.77 | 24.43 | 6 | 3098 | 335 | 29571088 |
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 |
---|---|---|---|---|---|---|
General physical health deterioration | 112.44 | 20.93 | 118 | 6178 | 204307 | 64288129 |
Product prescribing error | 106.66 | 20.93 | 57 | 6239 | 35212 | 64457224 |
Acute kidney injury | 105.48 | 20.93 | 170 | 6126 | 449070 | 64043366 |
Renal impairment | 94.63 | 20.93 | 89 | 6207 | 134928 | 64357508 |
Labelled drug-drug interaction medication error | 82.08 | 20.93 | 41 | 6255 | 22021 | 64470415 |
Hypertensive crisis | 65.19 | 20.93 | 33 | 6263 | 18215 | 64474221 |
Bradycardia | 55.68 | 20.93 | 63 | 6233 | 118156 | 64374280 |
Benign gastrointestinal neoplasm | 55.35 | 20.93 | 10 | 6286 | 139 | 64492297 |
Hyperkalaemia | 52.99 | 20.93 | 57 | 6239 | 101072 | 64391364 |
Hyperkaliuria | 47.43 | 20.93 | 9 | 6287 | 166 | 64492270 |
Drug interaction | 42.88 | 20.93 | 103 | 6193 | 361980 | 64130456 |
Dizziness | 39.28 | 20.93 | 111 | 6185 | 430052 | 64062384 |
Peripheral artery stenosis | 39.01 | 20.93 | 11 | 6285 | 1198 | 64491238 |
Electrolyte imbalance | 37.77 | 20.93 | 26 | 6270 | 25217 | 64467219 |
Hypotension | 37.43 | 20.93 | 101 | 6195 | 380873 | 64111563 |
Lactic acidosis | 36.41 | 20.93 | 37 | 6259 | 61373 | 64431063 |
Polypectomy | 32.13 | 20.93 | 9 | 6287 | 957 | 64491479 |
Histology abnormal | 31.07 | 20.93 | 7 | 6289 | 306 | 64492130 |
Sprue-like enteropathy | 27.13 | 20.93 | 8 | 6288 | 1021 | 64491415 |
Traumatic haemorrhage | 26.42 | 20.93 | 8 | 6288 | 1118 | 64491318 |
Linear IgA disease | 26.37 | 20.93 | 10 | 6286 | 2764 | 64489672 |
Therapeutic drug monitoring analysis not performed | 25.83 | 20.93 | 8 | 6288 | 1204 | 64491232 |
Schizophrenia | 25.43 | 20.93 | 15 | 6281 | 11153 | 64481283 |
Hyperammonaemia | 24.40 | 20.93 | 14 | 6282 | 9890 | 64482546 |
Therapeutic drug monitoring analysis incorrectly performed | 22.95 | 20.93 | 5 | 6291 | 187 | 64492249 |
Medication error | 22.42 | 20.93 | 26 | 6270 | 49940 | 64442496 |
Blood aldosterone increased | 22.32 | 20.93 | 5 | 6291 | 213 | 64492223 |
Infected lymphocele | 22.14 | 20.93 | 5 | 6291 | 221 | 64492215 |
Orthostatic hypotension | 22.12 | 20.93 | 25 | 6271 | 46713 | 64445723 |
Spinal pain | 21.27 | 20.93 | 14 | 6282 | 12607 | 64479829 |
Arterial haemorrhage | 21.05 | 20.93 | 8 | 6288 | 2223 | 64490213 |
None
Source | Code | Description |
---|---|---|
ATC | C02AC05 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIADRENERGIC AGENTS, CENTRALLY ACTING Imidazoline receptor agonists |
ATC | C02LC05 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION Imidazoline receptor agonists in combination with diuretics |
MeSH PA | D000959 | Antihypertensive Agents |
MeSH PA | D002317 | Cardiovascular Agents |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Essential hypertension | indication | 59621000 | DOID:10825 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 7.96 | Basic |
pKa2 | 2.26 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Nischarin | Membrane receptor | AGONIST | Ki | 8.38 | CHEMBL | SCIENTIFIC LITERATURE | |||
5-hydroxytryptamine receptor 1A | GPCR | Ki | 6.40 | DRUG MATRIX | |||||
Alpha-2C adrenergic receptor | GPCR | Ki | 5.70 | CHEMBL | |||||
Alpha-2A adrenergic receptor | GPCR | Ki | 6.82 | CHEMBL | |||||
5-hydroxytryptamine receptor 1A | GPCR | IC50 | 6.15 | CHEMBL | |||||
Nischarin | Unclassified | Ki | 7.11 | CHEMBL | |||||
Alpha-2B adrenergic receptor | GPCR | Ki | 6 | CHEMBL |
ID | Source |
---|---|
D05087 | KEGG_DRUG |
C0066837 | UMLSCUI |
CHEBI:7009 | CHEBI |
CHEMBL19236 | ChEMBL_ID |
DB09242 | DRUGBANK_ID |
4810 | PUBCHEM_CID |
C043482 | MESH_SUPPLEMENTAL_RECORD_UI |
5207 | INN_ID |
CC6X0L40GW | UNII |
30257 | RXNORM |
006139 | NDDF |
318706009 | SNOMEDCT_US |
395805008 | SNOMEDCT_US |
None