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

Stem definition	Drug id	CAS RN
alpha-2 adrenoreceptor agonists	2381	54187-04-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: rilmenidine oxaminozoline rilmenidene rilmenidine phosphate rilmenidine dihydrogen phosphate	Oxazole derivative that acts as an agonist for ALPHA-2 ADRENERGIC RECEPTORS and IMIDAZOLINE RECEPTORS. It is used in the treatment of HYPERTENSION. Molecular weight: 180.25 Formula: C10H16N2O CLOGP: 1.42 LIPINSKI: 0 HAC: 3 HDO: 1 TPSA: 33.62 ALOGS: -2.13 ROTB: 3

Molecule

Description

Molfile Inchi Smiles

Synonyms:

rilmenidine
oxaminozoline
rilmenidene
rilmenidine phosphate
rilmenidine dihydrogen phosphate

Oxazole derivative that acts as an agonist for ALPHA-2 ADRENERGIC RECEPTORS and IMIDAZOLINE RECEPTORS. It is used in the treatment of HYPERTENSION.

Molecular weight: 180.25
Formula: C10H16N2O
CLOGP: 1.42
LIPINSKI: 0
HAC: 3
HDO: 1
TPSA: 33.62
ALOGS: -2.13
ROTB: 3

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	8.30 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	7.10 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	4.50 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.90 %	Lombardo F, Berellini G, Obach RS

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Approvals:

None

FDA Adverse Event Reporting System (Female)

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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	328.41	32.34	209	4071	263206	63221536
Lactic acidosis	236.70	32.34	91	4189	38196	63446546
Hyperkalaemia	137.90	32.34	69	4211	54134	63430608
Allergic reaction to excipient	100.39	32.34	18	4262	355	63484387
Hyponatraemia	87.29	32.34	67	4213	111833	63372909
Mixed liver injury	75.76	32.34	23	4257	4712	63480030
Isosthenuria	75.65	32.34	12	4268	108	63484634
Rhabdomyolysis	72.51	32.34	42	4238	43909	63440833
Pyelitis	68.28	32.34	12	4268	210	63484532
Bladder hypertrophy	67.34	32.34	12	4268	228	63484514

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FDA Adverse Event Reporting System (Male)

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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	161.71	27.39	146	2256	304842	34649687
Cerebral haematoma	63.28	27.39	20	2382	4595	34949934
Lactic acidosis	61.56	27.39	35	2367	34737	34919792
Hyperkalaemia	61.12	27.39	45	2357	69344	34885185
Necrotising oesophagitis	51.16	27.39	11	2391	555	34953974
Hypovolaemic shock	47.54	27.39	18	2384	7067	34947462
Hemiplegia	33.77	27.39	14	2388	6958	34947571
Product name confusion	29.60	27.39	5	2397	67	34954462
Tubulointerstitial nephritis	28.91	27.39	18	2384	21006	34933523
Hypokalaemia	28.67	27.39	27	2375	58187	34896342

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FDA Adverse Event Reporting System (Geriatric)

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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	432.06	25.35	353	6428	519051	79218556
Lactic acidosis	261.96	25.35	125	6656	70234	79667373
Hyperkalaemia	177.11	25.35	114	6667	114284	79623323
Allergic reaction to excipient	97.24	25.35	18	6763	334	79737273
Hyponatraemia	78.97	25.35	86	6695	177762	79559845
Isosthenuria	72.56	25.35	12	6769	111	79737496
Cerebral haematoma	62.41	25.35	24	6757	7918	79729689
Electrocardiogram PR shortened	61.30	25.35	12	6769	303	79737304
Pyelitis	60.28	25.35	12	6769	331	79737276
Mixed liver injury	56.35	25.35	22	6759	7556	79730051

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C02AC06	CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIADRENERGIC AGENTS, CENTRALLY ACTING Imidazoline receptor agonists
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D000322	Adrenergic Agonists
MeSH PA	D058647	Adrenergic alpha-2 Receptor Agonists
MeSH PA	D000316	Adrenergic alpha-Agonists
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D013565	Sympatholytics

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

Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.22	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Type	Activity value (-log[M])	Bioact source
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN	Ki	7.44	CHEMBL
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN	Ki	5.05	CHEMBL
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN	Ki	7.37	CHEMBL
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN	Ki	7.90	CHEMBL
Nischarin	Membrane receptor	Q9Y2I1	NISCH_HUMAN	Ki	7.23	CHEMBL
Nischarin	Unclassified		NISCH_RAT	Ki	7.95	CHEMBL

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External reference:

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ID	Source
005772	NDDF
005773	NDDF
236379	RXNORM
5846	INN_ID
68712	PUBCHEM_CID
765332006	SNOMEDCT_US
765333001	SNOMEDCT_US
85409-38-7	SECONDARY_CAS_RN
C0140591	UMLSCUI
CHEBI:8862	CHEBI

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Pharmaceutical products:

None