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

Stem definition	Drug id	CAS RN
alpha-2 adrenoreceptor agonists	704	4205-90-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: clonidine clonidine hydrochloride clonidine HCl	An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION. Molecular weight: 230.09 Formula: C9H9Cl2N3 CLOGP: 1.73 LIPINSKI: 0 HAC: 3 HDO: 2 TPSA: 36.42 ALOGS: -2.68 ROTB: 1 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

clonidine
clonidine hydrochloride
clonidine HCl

An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.

Molecular weight: 230.09
Formula: C9H9Cl2N3
CLOGP: 1.73
LIPINSKI: 0
HAC: 3
HDO: 2
TPSA: 36.42
ALOGS: -2.68
ROTB: 1

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.45	mg	O
0.45	mg	P
0.10	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	95 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	7.60 hours	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	62 %	Hosey CM, Chan R, Benet LZ
S (Water solubility)	50 mg/mL	Bocci G, Oprea TI, Benet LZ
CL (Clearance)	4 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	3.30 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Hosey CM, Chan R, Benet LZ
fu (Fraction unbound in plasma)	0.56 %	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.17 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Sept. 3, 1974	FDA	BOEHRINGER INGELHEIM

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
Temperature regulation disorder	399.07	9.97	171	65427	5961	63417463
Completed suicide	328.90	9.97	561	65037	145112	63278312
Food allergy	301.13	9.97	172	65426	11229	63412195
Coeliac disease	280.13	9.97	171	65427	12626	63410798
Immunodeficiency	211.41	9.97	172	65426	20082	63403342
Bradycardia	193.46	9.97	303	65295	72924	63350500
Bursitis	186.00	9.97	210	65388	36831	63386593
Hypertension	183.19	9.97	669	64929	278634	63144790
Hyperhidrosis	180.02	9.97	365	65233	107471	63315953
Hypertensive crisis	164.16	9.97	132	65466	15154	63408270

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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
Completed suicide	229.73	11.35	418	41605	97750	34817158
Drug withdrawal syndrome	208.00	11.35	180	41843	19654	34895254
Aggression	161.35	11.35	216	41807	38748	34876160
Bradycardia	157.45	11.35	306	41717	75112	34839796
Withdrawal hypertension	129.51	11.35	33	41990	168	34914740
Respiratory depression	124.86	11.35	124	41899	16121	34898787
Drug dependence	98.29	11.35	133	41890	24084	34890824
Hypertensive crisis	88.84	11.35	78	41945	8673	34906235
Hypertension	86.69	11.35	359	41664	136084	34778824
Withdrawal syndrome	81.13	11.35	87	41936	12368	34902540

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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
Completed suicide	594.01	10.24	1018	88031	244749	79410590
Temperature regulation disorder	380.87	10.24	167	88882	5686	79649653
Bradycardia	350.16	10.24	579	88470	134978	79520361
Drug withdrawal syndrome	324.65	10.24	286	88763	34432	79620907
Food allergy	270.68	10.24	162	88887	10662	79644677
Coeliac disease	268.68	10.24	164	88885	11187	79644152
Hypertensive crisis	265.10	10.24	205	88844	20565	79634774
Hypertension	200.98	10.24	816	88233	330176	79325163
Immunodeficiency	187.03	10.24	171	88878	21597	79633742
Cardiac failure congestive	183.90	10.24	456	88593	141946	79513393

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C02AC01	CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIADRENERGIC AGENTS, CENTRALLY ACTING Imidazoline receptor agonists
ATC	C02LC01	CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION Imidazoline receptor agonists in combination with diuretics
ATC	C02LC51	CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION Imidazoline receptor agonists in combination with diuretics
ATC	N02CX02	NERVOUS SYSTEM ANALGESICS ANTIMIGRAINE PREPARATIONS Other antimigraine preparations
ATC	S01EA04	SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Sympathomimetics in glaucoma therapy
CHEBI has role	CHEBI:35569	alpha-adrenergic agonists
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:66991	sympatholytic drug
FDA EPC	N0000175554	Central alpha-2 Adrenergic Agonist
FDA MoA	N0000009918	Adrenergic alpha2-Agonists

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

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Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Severe pain	indication	76948002
Open-angle glaucoma	indication	84494001	DOID:1067
Attention deficit hyperactivity disorder	indication	406506008
Increased Intraocular Pressure after Ocular Procedure	indication
Ocular hypertension	off-label use	4210003	DOID:9282
Gilles de la Tourette's syndrome	off-label use	5158005	DOID:11119
Pain	off-label use	22253000
Diarrhea	off-label use	62315008
Opioid withdrawal	off-label use	87132004

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.5	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	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN	AGONIST	Ki	7.50	CHEMBL	CHEMBL
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN	AGONIST	EC50	6.70	WOMBAT-PK	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN	AGONIST	Ki	8.42	CHEMBL	CHEMBL
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	6.22	CHEMBL
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	6.50	PDSP
Nischarin	Membrane receptor	Q9Y2I1	NISCH_HUMAN		Ki	8.05	CHEMBL
Solute carrier family 22 member 1	Transporter	O15245	S22A1_HUMAN		IC50	4.65	CHEMBL
Solute carrier family 22 member 2	Transporter	O15244	S22A2_HUMAN		IC50	4.80	WOMBAT-PK
Multidrug and toxin extrusion protein 1	Transporter	Q96FL8	S47A1_HUMAN		IC50	4.48	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	5.49	CHEMBL

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External reference:

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ID	Source
CLU	PDB_CHEM_ID
000644	NDDF
004495	NDDF
142432	RXNORM
2624	INN_ID
27687	MMSL
2803	PUBCHEM_CID
372805007	SNOMEDCT_US
381	MMSL
387121001	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Catapres-TTS	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0031	PATCH	0.10 mg	TRANSDERMAL	NDA	23 sections
Catapres-TTS	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0031	PATCH	0.10 mg	TRANSDERMAL	NDA	23 sections
Catapres-TTS	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0032	PATCH	0.20 mg	TRANSDERMAL	NDA	23 sections
Catapres-TTS	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0032	PATCH	0.20 mg	TRANSDERMAL	NDA	23 sections
Catapres-TTS	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0033	PATCH	0.30 mg	TRANSDERMAL	NDA	23 sections
Clonidine	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0871	PATCH	0.10 mg	TRANSDERMAL	ANDA	17 sections
Clonidine	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0871	PATCH	0.10 mg	TRANSDERMAL	ANDA	17 sections
Clonidine	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0872	PATCH	0.20 mg	TRANSDERMAL	ANDA	17 sections
Clonidine	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0872	PATCH	0.20 mg	TRANSDERMAL	ANDA	17 sections
Clonidine	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0873	PATCH	0.30 mg	TRANSDERMAL	ANDA	17 sections

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