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

Stem definition	Drug id	CAS RN
antihypertensives, clonidine derivatives	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

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	128.27	25.93	98	3549	169912	56118508
Renal impairment	94.51	25.93	61	3586	80652	56207768
Hypertensive crisis	72.43	25.93	29	3618	14007	56274413
Product prescribing error	70.60	25.93	33	3614	23153	56265267
Acute kidney injury	58.86	25.93	75	3572	240688	56047732
Electrocardiogram abnormal	53.28	25.93	20	3627	8124	56280296
Lactic acidosis	47.01	25.93	29	3618	35317	56253103
Bradycardia	44.40	25.93	36	3611	67468	56220952
Hyperammonaemia	39.24	25.93	14	3633	4926	56283494
Hypertension	36.06	25.93	60	3587	244218	56044202
Traumatic haemorrhage	35.80	25.93	8	3639	512	56287908
Mental disability	35.70	25.93	6	3641	83	56288337
Electrolyte imbalance	35.20	25.93	19	3628	18014	56270406
Language disorder	33.90	25.93	10	3637	1931	56286489
Hyperkalaemia	33.16	25.93	27	3620	50838	56237582
Therapeutic drug monitoring analysis not performed	30.56	25.93	8	3639	997	56287423
Skin haemorrhage	28.80	25.93	13	3634	8400	56280020
Eye movement disorder	28.58	25.93	11	3636	4778	56283642
Genotype drug resistance test positive	27.13	25.93	6	3641	366	56288054
Orthostatic hypotension	26.79	25.93	20	3627	33179	56255241
Arterial haemorrhage	26.76	25.93	8	3639	1617	56286803
Stevens-Johnson syndrome	26.14	25.93	17	3630	22646	56265774

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
Product prescribing error	64.48	25.71	35	3485	19607	31674217
Labelled drug-drug interaction medication error	62.23	25.71	30	3490	13133	31680691
Acute kidney injury	57.24	25.71	107	3413	279607	31414217
Benign gastrointestinal neoplasm	54.34	25.71	10	3510	135	31693689
Hyperkaliuria	49.74	25.71	9	3511	110	31693714
Product monitoring error	37.44	25.71	14	3506	3276	31690548
Peripheral artery stenosis	36.59	25.71	10	3510	853	31692971
Polypectomy	36.37	25.71	9	3511	519	31693305
Chylothorax	34.11	25.71	9	3511	671	31693153
Sprue-like enteropathy	32.19	25.71	8	3512	470	31693354
Hypotension	31.80	25.71	70	3450	204548	31489276
Linear IgA disease	30.73	25.71	10	3510	1552	31692272
Histology abnormal	30.52	25.71	7	3513	291	31693533
Drug interaction	28.69	25.71	68	3452	208475	31485349
Schizophrenia	26.64	25.71	16	3504	10814	31683010
Dizziness	26.37	25.71	64	3456	199083	31494741
Hyperkalaemia	26.28	25.71	34	3486	64317	31629507

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	133.35	21.08	68	6734	38884	70882758
Acute kidney injury	118.55	21.08	183	6619	474441	70447201
General physical health deterioration	108.58	21.08	123	6679	235908	70685734
Renal impairment	96.77	21.08	92	6710	143845	70777797
Hypertensive crisis	81.89	21.08	39	6763	19223	70902419
Labelled drug-drug interaction medication error	79.29	21.08	41	6761	24086	70897556
Bradycardia	62.42	21.08	68	6734	124547	70797095
Hyperkalaemia	58.38	21.08	61	6741	106530	70815112
Benign gastrointestinal neoplasm	55.53	21.08	10	6792	139	70921503
Hyperkaliuria	46.99	21.08	9	6793	178	70921464
Dizziness	44.95	21.08	121	6681	464020	70457622
Hypotension	41.75	21.08	108	6694	404273	70517369
Drug interaction	40.54	21.08	103	6699	381338	70540304
Hypertension	40.21	21.08	88	6714	295945	70625697
Electrolyte imbalance	39.06	21.08	27	6775	26834	70894808
Peripheral artery stenosis	38.78	21.08	11	6791	1246	70920396
Lactic acidosis	35.19	21.08	37	6765	64987	70856655
Polypectomy	31.81	21.08	9	6793	1010	70920632
Histology abnormal	30.98	21.08	7	6795	316	70921326
Product monitoring error	29.65	21.08	14	6788	6762	70914880
Medication error	28.35	21.08	31	6771	56881	70864761
Sprue-like enteropathy	26.67	21.08	8	6794	1102	70920540
Traumatic haemorrhage	26.19	21.08	8	6794	1172	70920470
Linear IgA disease	26.03	21.08	10	6792	2914	70918728
Language disorder	25.91	21.08	10	6792	2951	70918691
Skin haemorrhage	24.27	21.08	14	6788	10166	70911476
Hyperammonaemia	24.13	21.08	14	6788	10279	70911363
Therapeutic drug monitoring analysis not performed	24.07	21.08	8	6794	1536	70920106
Schizophrenia	22.38	21.08	16	6786	16752	70904890
Blood aldosterone increased	22.32	21.08	5	6797	217	70921425
Infected lymphocele	22.01	21.08	5	6797	231	70921411
Erysipelas	21.95	21.08	13	6789	9911	70911731
Musculoskeletal pain	21.20	21.08	34	6768	90293	70831349

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
5207	INN_ID
CC6X0L40GW	UNII
30257	RXNORM
006139	NDDF
318706009	SNOMEDCT_US
395805008	SNOMEDCT_US

Pharmaceutical products:

None