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moxonidine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
alpha-2 adrenoreceptor agonists	1856	75438-57-2

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.30	mg	O

ADMET properties:

Property	Value	Reference
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

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1991	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

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	124.36	25.07	102	3895	201300	63283725
Renal impairment	100.80	25.07	65	3932	88290	63396735
Product prescribing error	86.06	25.07	39	3958	26250	63458775
Hypertensive crisis	77.72	25.07	31	3966	15255	63469770
Acute kidney injury	74.41	25.07	87	3910	263328	63221697
Lactic acidosis	53.27	25.07	32	3965	38255	63446770
Electrocardiogram abnormal	51.51	25.07	20	3977	9159	63475866
Hyperkalaemia	43.14	25.07	32	3965	54171	63430854
Bradycardia	42.72	25.07	36	3961	73191	63411834
Electrolyte imbalance	39.33	25.07	21	3976	20055	63464970
Hyperammonaemia	38.85	25.07	14	3983	5218	63479807
Language disorder	37.48	25.07	11	3986	2149	63482876
Mental disability	35.87	25.07	6	3991	83	63484942
Traumatic haemorrhage	35.24	25.07	8	3989	566	63484459
Therapeutic drug monitoring analysis not performed	33.04	25.07	9	3988	1343	63483682
Peripheral arterial occlusive disease	30.29	25.07	11	3986	4190	63480835
Hyperglycaemia	29.51	25.07	23	3974	41844	63443181
Eye movement disorder	27.94	25.07	11	3986	5217	63479808
Left ventricular hypertrophy	27.77	25.07	11	3986	5304	63479721
Skin haemorrhage	26.89	25.07	13	3984	10081	63474944
Arterial haemorrhage	26.55	25.07	8	3989	1709	63483316
Genotype drug resistance test positive	26.40	25.07	6	3991	427	63484598
Orthostatic hypotension	25.78	25.07	20	3977	36140	63448885
Renal failure	25.31	25.07	34	3963	117618	63367407
Postrenal failure	25.14	25.07	5	3992	187	63484838
Stevens-Johnson syndrome	25.09	25.07	17	3980	24933	63460092

FDA Adverse Event Reporting System (Male)

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
Acute kidney injury	64.54	24.41	117	3687	304871	34648256
Product prescribing error	62.74	24.41	36	3768	22891	34930236
Labelled drug-drug interaction medication error	59.19	24.41	30	3774	14909	34938218
Benign gastrointestinal neoplasm	54.55	24.41	10	3794	135	34952992
Hyperkaliuria	51.13	24.41	9	3795	95	34953032
Hypotension	38.05	24.41	78	3726	221571	34731556
Product monitoring error	37.24	24.41	15	3789	4366	34948761
Papillary renal cell carcinoma	36.95	24.41	8	3796	260	34952867
Peripheral artery stenosis	36.68	24.41	10	3794	862	34952265
Schizophrenia	36.06	24.41	18	3786	8648	34944479
Polypectomy	35.87	24.41	9	3795	561	34952566
Chylothorax	33.06	24.41	9	3795	772	34952355
Sprue-like enteropathy	31.78	24.41	8	3796	505	34952622
Drug interaction	31.34	24.41	73	3731	225873	34727254
Hyperkalaemia	31.08	24.41	38	3766	69351	34883776
Linear IgA disease	30.54	24.41	10	3794	1616	34951511
Histology abnormal	30.48	24.41	7	3797	299	34952828
Dizziness	27.49	24.41	68	3736	218453	34734674
Bradycardia	25.54	24.41	36	3768	75382	34877745
Hemiparaesthesia	25.06	24.41	5	3799	108	34953019
Inappropriate affect	24.70	24.41	7	3797	696	34952431
Hypertensive crisis	24.61	24.41	14	3790	8737	34944390

FDA Adverse Event Reporting System (Geriatric)

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
Product prescribing error	146.17	20.11	75	7351	44738	79692224
Acute kidney injury	141.10	20.11	205	7221	519199	79217763
General physical health deterioration	110.75	20.11	132	7294	275106	79461856
Renal impairment	108.90	20.11	101	7325	157682	79579280
Hypertensive crisis	89.32	20.11	42	7384	20728	79716234
Labelled drug-drug interaction medication error	75.15	20.11	41	7385	27609	79709353
Hyperkalaemia	72.68	20.11	70	7356	114328	79622634
Bradycardia	62.75	20.11	70	7356	135487	79601475
Benign gastrointestinal neoplasm	55.82	20.11	10	7416	139	79736823
Hyperkaliuria	47.70	20.11	9	7417	169	79736793
Dizziness	47.24	20.11	131	7295	526310	79210652
Electrolyte imbalance	45.64	20.11	31	7395	30850	79706112
Hypotension	44.97	20.11	115	7311	440202	79296760
Drug interaction	44.02	20.11	110	7316	415073	79321889
Product monitoring error	41.35	20.11	19	7407	8887	79728075
Lactic acidosis	40.82	20.11	41	7385	70318	79666644
Peripheral artery stenosis	38.64	20.11	11	7415	1300	79735662
Papillary renal cell carcinoma	32.30	20.11	7	7419	268	79736694
Histology abnormal	30.97	20.11	7	7419	326	79736636
Polypectomy	30.59	20.11	9	7417	1195	79735767
Language disorder	28.95	20.11	11	7415	3203	79733759
Schizophrenia	28.95	20.11	18	7408	15422	79721540
Arrhythmia	28.93	20.11	32	7394	61240	79675722
Medication error	27.61	20.11	33	7393	68609	79668353
Blood creatinine increased	26.63	20.11	50	7376	155007	79581955
Therapeutic drug monitoring analysis not performed	26.38	20.11	9	7417	1927	79735035
Linear IgA disease	25.65	20.11	10	7416	3122	79733840
Sprue-like enteropathy	25.54	20.11	8	7418	1310	79735652
Traumatic haemorrhage	25.46	20.11	8	7418	1325	79735637
Musculoskeletal pain	24.14	20.11	38	7388	102316	79634646
Hyperglycaemia	23.78	20.11	31	7395	70304	79666658
Hyperammonaemia	23.54	20.11	14	7412	11079	79725883
Renal failure	23.10	20.11	55	7371	200913	79536049
Hypoglycaemia	22.97	20.11	37	7389	101557	79635405
Skin haemorrhage	22.54	20.11	14	7412	11967	79724995
Blood aldosterone increased	22.33	20.11	5	7421	223	79736739
Hemiparaesthesia	22.08	20.11	5	7421	235	79736727
Infected lymphocele	21.99	20.11	5	7421	239	79736723
Hypertension	21.76	20.11	74	7352	330918	79406044
Postrenal failure	21.40	20.11	6	7420	671	79736291
Erysipelas	21.23	20.11	13	7413	10837	79726125
Tachypnoea	21.04	20.11	20	7406	32043	79704919
Inappropriate affect	20.38	20.11	7	7419	1529	79735433
Arterial haemorrhage	20.35	20.11	8	7418	2553	79734409

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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

Disease	Relation	SNOMED_ID	DOID
Essential hypertension	indication	59621000	DOID:10825

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Nischarin	Membrane receptor	Q9Y2I1	NISCH_HUMAN	AGONIST	Ki	8.38	CHEMBL	SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	6.40	DRUG MATRIX
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	5.70	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.82	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		IC50	6.15	CHEMBL
Nischarin	Unclassified		NISCH_RAT		Ki	7.11	CHEMBL
Alpha-2B adrenergic receptor	GPCR		ADA2B_RAT		Ki	6	CHEMBL

External reference:

ID	Source
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