moxonidine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
alpha-2 adrenoreceptor agonists 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 µM/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
S (Water solubility) 0.80 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 4 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -0.320 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.871 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 4.305 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 2.649 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 89.330 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 85.680 % High 1
herg hERG pIC50 4.271 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.258 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 79.510 % High 1
kinase-safety-class ACVR2B,AURKA,AXL,BRAF,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK2,MAP3K21,MAPK7,MARK4,NTRK2,PDK1,PDK2,PIK3CB,PIK3CD,PRKDC,SIK2,STK33,TEK,TTK 26
kinase-selectivity-class GRK2 1
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 1.455 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 1.614 High 1
mh-clint Mouse hepatocyte intrinsic clearance 3.006 High 1
mppb Mouse plasma protein binding (% unbound) 92.470 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 2.051 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 85.790 % High 1
rat-kpuu-brain Rat brain Kpuu 0.158 % High 1
rh-clint Rat hepatocyte intrinsic clearance 2.399 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 95.300 % High 1
rppb Rat plasma protein binding (% unbound) 87.060 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 939.723 uM High 1

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
Renal impairment 225.01 25.90 113 5085 105308 90517941
Serositis 155.70 25.90 31 5167 1286 90621963
Body mass index abnormal 134.60 25.90 25 5173 714 90622535
Central nervous system lupus 119.33 25.90 25 5173 1338 90621911
Hyperkalaemia 107.99 25.90 59 5139 64905 90558344
General physical health deterioration 98.38 25.90 111 5087 355004 90268245
Hypertensive crisis 89.88 25.90 35 5163 17749 90605500
Haematuria 87.95 25.90 42 5156 34895 90588354
Lupus nephritis 87.89 25.90 25 5173 4807 90618442
Product prescribing error 84.39 25.90 39 5159 30106 90593143
Lactic acidosis 78.80 25.90 44 5154 50419 90572830
Acute kidney injury 71.86 25.90 90 5108 320297 90302952
Cardiac failure 70.86 25.90 55 5143 109441 90513808
Gout 63.93 25.90 27 5171 16832 90606417
Electrocardiogram abnormal 51.07 25.90 20 5178 10278 90612971
Stevens-Johnson syndrome 46.89 25.90 26 5172 29350 90593899
Bradycardia 41.37 25.90 36 5162 83811 90539438
Electrolyte imbalance 37.85 25.90 21 5177 23724 90599525
Hyperammonaemia 37.20 25.90 14 5184 6461 90616788
Abdominal pain 36.41 25.90 74 5124 395647 90227602
Language disorder 36.26 25.90 11 5187 2641 90620608
Traumatic haemorrhage 35.67 25.90 8 5190 589 90622660
Therapeutic drug monitoring analysis not performed 34.03 25.90 9 5189 1320 90621929
Mental disability 31.54 25.90 6 5192 195 90623054
Peripheral arterial occlusive disease 30.26 25.90 11 5187 4610 90618639
Blood creatinine increased 30.18 25.90 33 5165 101353 90521896
Hyperglycaemia 29.49 25.90 24 5174 50946 90572303
Renal failure 28.00 25.90 36 5162 130971 90492278
Left ventricular hypertrophy 27.21 25.90 11 5187 6133 90617116
Eye movement disorder 27.12 25.90 11 5187 6187 90617062
Orthostatic hypotension 26.99 25.90 21 5177 41806 90581443
Drug interaction 26.95 25.90 53 5145 276400 90346849
Genotype drug resistance test positive 26.74 25.90 6 5192 443 90622806

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
Acute kidney injury 66.20 22.17 132 4525 367205 42249473
Basal cell carcinoma 62.86 22.17 36 4621 22697 42593981
Labelled drug-drug interaction medication error 57.86 22.17 30 4627 15552 42601126
Product prescribing error 55.71 22.17 35 4622 26077 42590601
Benign gastrointestinal neoplasm 55.14 22.17 10 4647 126 42616552
Hemiparaesthesia 51.34 22.17 10 4647 189 42616489
Hyperkaliuria 51.09 22.17 9 4648 95 42616583
Superficial spreading melanoma stage I 43.84 22.17 7 4650 38 42616640
Hyperkalaemia 42.44 22.17 48 4609 80410 42536268
Papillary renal cell carcinoma 40.04 22.17 9 4648 347 42616331
Product monitoring error 37.03 22.17 15 4642 4408 42612270
Peripheral artery stenosis 36.25 22.17 10 4647 897 42615781
Linear IgA disease 35.71 22.17 12 4645 2091 42614587
Schizophrenia 35.43 22.17 19 4638 10531 42606147
Polypectomy 34.71 22.17 9 4648 637 42616041
Hypotension 34.14 22.17 82 4575 257549 42359129
Drug interaction 31.18 22.17 81 4576 266918 42349760
Hypertensive crisis 30.45 22.17 17 4640 10189 42606489
Sprue-like enteropathy 29.91 22.17 8 4649 639 42616039
Histology abnormal 29.51 22.17 7 4650 343 42616335
Chylothorax 29.39 22.17 9 4648 1165 42615513
Inappropriate affect 28.67 22.17 8 4649 748 42615930
Suspected product contamination 27.48 22.17 6 4651 202 42616476
Renal impairment 25.16 22.17 44 4613 110184 42506494
Bradycardia 24.75 22.17 38 4619 85446 42531232
Periodontitis 23.81 22.17 9 4648 2202 42614476
Death 23.68 22.17 11 4646 471174 42145504
Manufacturing materials contamination 23.59 22.17 4 4653 33 42616645
Cardiac failure 23.54 22.17 42 4615 106814 42509864
Dizziness 23.51 22.17 70 4587 249184 42367494
Paradoxical drug reaction 23.15 22.17 11 4646 4727 42611951
Product contamination 22.27 22.17 7 4650 988 42615690

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
Renal impairment 190.39 19.24 144 9165 188301 110391689
Acute kidney injury 150.43 19.24 223 9086 635207 109944783
Hyperkalaemia 141.99 19.24 106 9203 135690 110444300
Product prescribing error 140.79 19.24 74 9235 51257 110528733
Serositis 138.39 19.24 31 9278 1538 110578452
Body mass index abnormal 119.32 19.24 25 9284 903 110579087
Central nervous system lupus 109.93 19.24 25 9284 1328 110578662
Hypertensive crisis 105.49 19.24 48 9261 24324 110555666
General physical health deterioration 90.07 19.24 142 9167 425153 110154837
Lupus nephritis 79.37 19.24 25 9284 4620 110575370
Labelled drug-drug interaction medication error 76.79 19.24 41 9268 29261 110550729
Cardiac failure 67.45 19.24 81 9228 187545 110392445
Bradycardia 64.02 19.24 72 9237 155445 110424545
Basal cell carcinoma 62.68 19.24 42 9267 45228 110534762
Drug interaction 61.37 19.24 132 9177 500051 110079939
Benign gastrointestinal neoplasm 57.45 19.24 10 9299 130 110579860
Lactic acidosis 56.40 19.24 53 9256 92758 110487232
Hyperkaliuria 54.09 19.24 10 9299 186 110579804
Hypotension 52.88 19.24 128 9181 523721 110056269
Haematuria 49.66 19.24 47 9262 82958 110497032
Hemiparaesthesia 46.78 19.24 10 9299 398 110579592
Product contamination 44.13 19.24 13 9296 1918 110578072
Electrolyte imbalance 43.37 19.24 31 9278 36997 110542993
Superficial spreading melanoma stage I 43.20 19.24 7 9302 57 110579933
Product monitoring error 43.14 19.24 19 9290 8908 110571082
Peripheral artery stenosis 39.39 19.24 11 9298 1343 110578647
Gout 36.93 19.24 28 9281 36538 110543452
Papillary renal cell carcinoma 36.44 19.24 8 9301 361 110579629
Dizziness 35.52 19.24 134 9175 698059 109881931
Blood creatinine increased 33.10 19.24 57 9252 182832 110397158
Urosepsis 32.11 19.24 24 9285 30651 110549339
Hypoglycaemia 30.54 19.24 43 9266 116061 110463929
Histology abnormal 30.34 19.24 7 9302 396 110579594
Linear IgA disease 30.14 19.24 12 9297 4377 110575613
Hyperglycaemia 29.34 19.24 36 9273 85054 110494936
Polypectomy 29.25 19.24 9 9300 1540 110578450
Arrhythmia 28.24 19.24 32 9277 69543 110510447
Language disorder 28.14 19.24 11 9298 3827 110576163
Renal failure 27.93 19.24 60 9249 226514 110353476
Suspected product contamination 27.33 19.24 6 9303 271 110579719
Therapeutic drug monitoring analysis not performed 27.29 19.24 9 9300 1922 110578068
Schizophrenia 27.24 19.24 19 9290 21807 110558183
Drug hypersensitivity 25.26 19.24 4 9305 454086 110125904
Osteochondrosis 24.94 19.24 9 9300 2512 110577478
Manufacturing materials contamination 24.64 19.24 4 9305 33 110579957
Sprue-like enteropathy 24.35 19.24 8 9301 1688 110578302
Inappropriate affect 24.34 19.24 8 9301 1691 110578299
Lichen planopilaris 24.30 19.24 5 9304 165 110579825
Traumatic haemorrhage 23.70 19.24 8 9301 1836 110578154
Blood aldosterone increased 22.86 19.24 5 9304 222 110579768
Glomerular filtration rate decreased 22.47 19.24 19 9290 28937 110551053
Infected lymphocele 22.40 19.24 5 9304 244 110579746
Hyperammonaemia 22.08 19.24 14 9295 13718 110566272
Syncope 21.99 19.24 51 9258 202485 110377505
Tumour lysis syndrome 21.45 19.24 19 9290 30782 110549208
Disorientation 21.35 19.24 28 9281 70643 110509347
Circulatory collapse 21.34 19.24 22 9287 42971 110537019
Dehydration 20.72 19.24 61 9248 279450 110300540
Postrenal failure 20.47 19.24 6 9303 870 110579120
Joint swelling 20.37 19.24 6 9303 442839 110137151
Parvovirus B19 infection 20.22 19.24 8 9301 2873 110577117
Skin squamous cell carcinoma recurrent 20.14 19.24 4 9305 110 110579880
Erysipelas 20.13 19.24 13 9296 13145 110566845
Pain 19.98 19.24 31 9278 954924 109625066
Urogenital infection bacterial 19.87 19.24 4 9305 118 110579872
Orthostatic hypotension 19.63 19.24 26 9283 66223 110513767
Renin decreased 19.53 19.24 4 9305 129 110579861
Tachypnoea 19.27 19.24 20 9289 39375 110540615

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
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:50514 vasoconstrictor agent

Related Drugs by ATC class:

C02AC Imidazoline receptor agonists 4 drugs
clonidineguanfacinerilmenidinetolonidine
C02LC Imidazoline receptor agonists in combination with diuretics 1 drug
clonidine

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Essential hypertension indication 59621000 DOID:10825




🐶 Veterinary Drug Use

None

🐶 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-2B adrenergic receptor GPCR AGONIST IC50 7.50 IUPHAR
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 Membrane receptor 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
12574 IUPHAR_LIGAND_ID
5207 INN_ID
CC6X0L40GW UNII
30257 RXNORM
006139 NDDF
318706009 SNOMEDCT_US
395805008 SNOMEDCT_US

Pharmaceutical products:

None