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	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 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

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
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:

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