moxonidine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antihypertensives, clonidine derivatives 1856 75438-57-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • moxonidine
  • normoxocin
  • moxonidin
  • Molecular weight: 241.68
  • Formula: C9H12ClN5O
  • CLOGP: 1.51
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 71.43
  • ALOGS: -3.33
  • ROTB: 2

Drug dosage:

DoseUnitRoute
0.30 mg O

ADMET properties:

PropertyValueReference
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

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1991 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Essential hypertension indication 59621000 DOID:10825




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.96 Basic
pKa2 2.26 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA 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

External reference:

IDSource
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

Pharmaceutical products:

None