Details of the Drug

General Information of Drug (ID: DM6RZ9Q)

Drug Name

Clonidine

Synonyms

clonidine; Clonidin; Duraclon; Chlornidinum; 4205-90-7; Catapres-TTS; Catarpresan; Catarpres; Adesipress; Catapres; Catapressan; Catapresan; ST 155BS; ST-155-BS; Clonidinum; Clonidina; Clonidinum [INN-Latin]; Clonidinhydrochlorid; CATAPRES-TTS-3; CATAPRES-TTS-1; CATAPRES-TTS-2; N-(2,6-Dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine; Isoglaucon; 2-(2,6-Dichloroanilino)-2-imidazoline; Dixarit; SKF 34427; Catapres- TTS; Clonidina [INN-Spanish]; M-5041T; Hemiton; CLORPRES; clonidine (amino form); Adesipress; Clofenil; Clopheline; Duraclont; Gemiton; Klofelin; Klofenil; M 5041T; Catapres (TN); Catarpres-TTS; ST-155BS; Tenso-Timelets; Catarpres-TTS (TN); Clonidine [USAN:BAN:INN]; Clonidine (JAN/USAN/INN); 1H-Imidazol-2-amine, N-(2,6-dichlorophenyl)-4,5-dihydro-(9CI); 2,6-Dichloro-N-2-imidazolidinylidenebenzenamine; 2,6-dichloro-N-(2-imidazolidinylidene)aniline; 2,6-dichloro-N-2-imidazolidinylidenebenzenamide; 2,6-dichloro-N-imidazolidin-2-ylideneaniline; 2-((2,6-Dichlorophenyl)imino)imidazolidine; 2-(2,6-Dichloroanilino)-1,3-diazacyclopentene-(2);2-(2,6-Dichloroanilino)-2-imidazoline; 2-(2,6-Dichlorophenylamino)-2-imidazoline; 2-(2,6-Dichlorophenylimino)imidazolidine; 2-Imidazoline, 2-(2,6-dichloroanilino)-(7CI,8CI); 2-[(2,6-Dichlorophenyl)imino]imidazoline; 2-[(2,6-dichlorophenyl)imino]-2-imidazoline; 734571A; 2,6-DICHLORO-N-IMIDAZOLIDIN-2-YLIDENEANILINE

Indication

Disease Entry	ICD 11	Status	REF
Hypertension	BA00-BA04	Approved	[1], [2]
Diabetic neuropathy	8C0Z	Phase 3	[3]

Therapeutic Class

Antihypertensive Agents

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

230.09

Topological Polar Surface Area (xlogp)

1.6

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Absorption AUC: The area under the plot of plasma concentration (AUC) of drug is 5.607 mcgh/L [4]
Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 400.72 ng/L [4]
BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [5]
Bioavailability: The bioavailability of drug is 55-87% [4]
Clearance: The clearance of drug is 1.9-4.3 mL/min/kg [6]
Elimination: Approximately 50% of a clonidine dose is excreted in the urine as the unchanged drug and 20% is eliminated in the feces [6]
Half-life: The concentration or amount of drug in body reduced by one-half in 30 minutes [6]
Metabolism: The drug is metabolized via the CYP2D6, CYP1A2, CYP3A4, CYP1A1, and CYP3A5 [7]
MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.17384 micromolar/kg/day [8]
Unbound Fraction: The unbound fraction of drug in plasma is 0.56% [9]
Vd: The volume of distribution (Vd) of drug is 1.7-2.5 L/kg [6]

Chemical Identifiers

Formula: C9H9Cl2N3
IUPAC Name: N-(2,6-dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine
Canonical SMILES: C1CN=C(N1)NC2=C(C=CC=C2Cl)Cl
InChI: InChI=1S/C9H9Cl2N3/c10-6-2-1-3-7(11)8(6)14-9-12-4-5-13-9/h1-3H,4-5H2,(H2,12,13,14)
InChIKey: GJSURZIOUXUGAL-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 2803
ChEBI ID: CHEBI:3757
CAS Number: 4205-90-7
DrugBank ID: DB00575
TTD ID: D03SKR
VARIDT ID: DR00521
INTEDE ID: DR0352
ACDINA ID: D00141

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Adrenergic receptor Alpha-2 (ADRA2)	TTQ8AFT	NOUNIPROTAC	Agonist	[10], [11], [12]
Membrane copper amine oxidase (AOC3)	TT7HC21	AOC3_HUMAN	Inhibitor	[13]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Organic cation transporter 3 (SLC22A3)	DT6201N	S22A3_HUMAN	Substrate	[14]
Organic cation transporter 1 (SLC22A1)	DTT79CX	S22A1_HUMAN	Substrate	[14]
Organic cation transporter 2 (SLC22A2)	DT9IDPW	S22A2_HUMAN	Substrate	[14]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[15]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)_{Main DME}	DE4LYSA	CP3A4_HUMAN	Substrate	[16]
Cytochrome P450 2D6 (CYP2D6)_{Main DME}	DECB0K3	CP2D6_HUMAN	Substrate	[16]
Cytochrome P450 1A2 (CYP1A2)_{Main DME}	DEJGDUW	CP1A2_HUMAN	Substrate	[16]
Cytochrome P450 3A5 (CYP3A5)_{Main DME}	DEIBDNY	CP3A5_HUMAN	Substrate	[16]

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Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease

Hypertension

ICD Disease Classification

BA00-BA04

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Membrane copper amine oxidase (AOC3)	DTT	AOC3	8.36E-22	-1.03	-1.54
P-glycoprotein 1 (ABCB1)	DTP	P-GP	2.00E-01	2.57E-02	6.18E-02
Organic cation transporter 1 (SLC22A1)	DTP	SLC22A1	2.90E-01	-1.11E-01	-2.75E-01
Organic cation transporter 2 (SLC22A2)	DTP	SLC22A2	5.61E-04	-1.80E-01	-4.16E-01
Organic cation transporter 3 (SLC22A3)	DTP	SLC22A3	1.68E-07	4.84E-01	1.17E+00
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	4.87E-15	-3.01E-01	-6.41E-01
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	5.05E-02	4.52E-01	5.39E-01
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	7.74E-01	-3.86E-02	-1.04E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	8.67E-01	-3.83E-03	-1.24E-02

Molecular Expression Atlas (MEA)

MEA Detail

Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Clonidine (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Linezolid	DMGFPU2	Moderate	Additive hypotensive effects by the combination of Clonidine and Linezolid.	Bacterial infection [1A00-1C4Z]	[96]
Cariprazine	DMJYDVK	Moderate	Additive hypotensive effects by the combination of Clonidine and Cariprazine.	Bipolar disorder [6A60]	[97]
Olopatadine	DMKMWQG	Moderate	Additive CNS depression effects by the combination of Clonidine and Olopatadine.	Conjunctiva disorder [9A60]	[98]
Selegiline	DM6034S	Moderate	Additive hypotensive effects by the combination of Clonidine and Selegiline.	Depression [6A70-6A7Z]	[96]
Isocarboxazid	DMAF1NB	Moderate	Additive hypotensive effects by the combination of Clonidine and Isocarboxazid.	Depression [6A70-6A7Z]	[96]
Tranylcypromine	DMGB5RE	Moderate	Additive hypotensive effects by the combination of Clonidine and Tranylcypromine.	Depression [6A70-6A7Z]	[96]
OPC-34712	DMHG57U	Moderate	Additive hypotensive effects by the combination of Clonidine and OPC-34712.	Depression [6A70-6A7Z]	[97]
Phenelzine	DMHIDUE	Moderate	Additive hypotensive effects by the combination of Clonidine and Phenelzine.	Depression [6A70-6A7Z]	[96]
Procarbazine	DMIK367	Moderate	Additive hypotensive effects by the combination of Clonidine and Procarbazine.	Hodgkin lymphoma [2B30]	[96]
ITI-007	DMUQ1DO	Moderate	Additive hypotensive effects by the combination of Clonidine and ITI-007.	Insomnia [7A00-7A0Z]	[97]
Allopregnanolone	DMNLHAC	Moderate	Additive CNS depression effects by the combination of Clonidine and Allopregnanolone.	Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z]	[99]
Lasmiditan	DMXLVDT	Moderate	Additive CNS depression effects by the combination of Clonidine and Lasmiditan.	Migraine [8A80]	[100]
Flibanserin	DM70DTN	Moderate	Additive CNS depression effects by the combination of Clonidine and Flibanserin.	Mood disorder [6A60-6E23]	[101]
Thalidomide	DM70BU5	Moderate	Additive CNS depression effects by the combination of Clonidine and Thalidomide.	Multiple myeloma [2A83]	[102]
Ozanimod	DMT6AM2	Moderate	Additive hypotensive effects by the combination of Clonidine and Ozanimod.	Multiple sclerosis [8A40]	[96]
Promethazine	DM6I5GR	Moderate	Additive hypotensive effects by the combination of Clonidine and Promethazine.	Nausea/vomiting [MD90]	[97]
Dextropropoxyphene	DM23HCX	Major	Additive CNS depression effects by the combination of Clonidine and Dextropropoxyphene.	Pain [MG30-MG3Z]	[103]
Safinamide	DM0YWJC	Moderate	Additive hypotensive effects by the combination of Clonidine and Safinamide.	Parkinsonism [8A00]	[96]
Rasagiline	DM3WKQ4	Moderate	Additive hypotensive effects by the combination of Clonidine and Rasagiline.	Parkinsonism [8A00]	[96]
Levomepromazine	DMIKFEL	Moderate	Additive hypotensive effects by the combination of Clonidine and Levomepromazine.	Psychotic disorder [6A20-6A25]	[97]
Quetiapine	DM1N62C	Moderate	Additive hypotensive effects by the combination of Clonidine and Quetiapine.	Schizophrenia [6A20]	[97]
Mesoridazine	DM2ZGAN	Moderate	Additive hypotensive effects by the combination of Clonidine and Mesoridazine.	Schizophrenia [6A20]	[97]
Thioridazine	DM35M8J	Moderate	Additive hypotensive effects by the combination of Clonidine and Thioridazine.	Schizophrenia [6A20]	[97]
Aripiprazole	DM3NUMH	Moderate	Additive hypotensive effects by the combination of Clonidine and Aripiprazole.	Schizophrenia [6A20]	[97]
Iloperidone	DM6AUFY	Moderate	Additive hypotensive effects by the combination of Clonidine and Iloperidone.	Schizophrenia [6A20]	[97]
Paliperidone	DM7NPJS	Moderate	Additive hypotensive effects by the combination of Clonidine and Paliperidone.	Schizophrenia [6A20]	[97]
Perphenazine	DMA4MRX	Moderate	Additive hypotensive effects by the combination of Clonidine and Perphenazine.	Schizophrenia [6A20]	[97]
Molindone	DMAH70G	Moderate	Additive hypotensive effects by the combination of Clonidine and Molindone.	Schizophrenia [6A20]	[97]
Thiothixene	DMDINC4	Moderate	Additive hypotensive effects by the combination of Clonidine and Thiothixene.	Schizophrenia [6A20]	[97]
Trifluoperazine	DMKBYWI	Moderate	Additive hypotensive effects by the combination of Clonidine and Trifluoperazine.	Schizophrenia [6A20]	[97]
Risperidone	DMN6DXL	Moderate	Additive hypotensive effects by the combination of Clonidine and Risperidone.	Schizophrenia [6A20]	[97]
Amisulpride	DMSJVAM	Moderate	Additive hypotensive effects by the combination of Clonidine and Amisulpride.	Schizophrenia [6A20]	[97]
Asenapine	DMSQZE2	Moderate	Additive hypotensive effects by the combination of Clonidine and Asenapine.	Schizophrenia [6A20]	[97]
Methdilazine	DMAUHQX	Moderate	Additive hypotensive effects by the combination of Clonidine and Methdilazine.	Vasomotor/allergic rhinitis [CA08]	[97]
Trimeprazine	DMEMV9D	Moderate	Additive hypotensive effects by the combination of Clonidine and Trimeprazine.	Vasomotor/allergic rhinitis [CA08]	[104]
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⏷ Show the Full List of 35 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Allura red AC dye	E00338	33258	Colorant
FD&C blue no. 1	E00263	19700	Colorant
FD&C blue no. 2	E00446	2723854	Colorant
Quinoline yellow WS	E00309	24671	Colorant
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sunset yellow FCF	E00255	17730	Colorant
Ammonium chloride	E00321	25517	Acidulant
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Brushite	E00392	104805	Diluent
Calcium hydrogenphosphate	E00294	24441	Diluent
Calcium phosphate	E00298	24456	Anticaking agent; Buffering agent; Desiccant; Diluent
Carmellose sodium	E00625	Not Available	Disintegrant
Crospovidone	E00626	Not Available	Disintegrant
Dextrin	E00359	62698	Binding agent; Diluent; Microencapsulating agent; Stiffening agent; Suspending agent; Viscosity-controlling agent
Eisenoxyd	E00585	56841934	Colorant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Glycerin	E00026	753	Antimicrobial preservative; Emollient; Flavoring agent; Humectant; Lubricant; Plasticizing agent; Solvent; Suppository base; Tonicity agent; Viscosity-controlling agent
Hydroxypropyl cellulose	E00632	Not Available	Binding agent; Coating agent; Emulsifying agent; Film/Membrane-forming agent; Modified-release agent; Suspending agent; Viscosity-controlling agent
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Povidone	E00667	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Sodium silicate	E00276	23266	Buffering agent; Complexing agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Triacetin	E00080	5541	Humectant; Plasticizing agent; Solvent
Vinylpyrrolidone	E00668	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
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⏷ Show the Full List of 27 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Clonidine 0.3 mg tablet	0.3 mg	24 HR Extended Release Oral Tablet	Oral
Clonidine 0.1 mg tablet	0.1 mg	12 HR Extended Release Tablet	Oral
Clonidine 0.2 mg tablet	0.2 mg	12 HR Extended Release Tablet	Oral
Clonidine 0.1 mg tablet	0.1 mg	12 HR Extended Release Oral Tablet	Oral
Clonidine 0.2 mg tablet	0.2 mg	12 HR Extended Release Oral Tablet	Oral
Clonidine 0.2 mg tablet	0.2 mg	24 HR Extended Release Oral Tablet	Oral
Clonidine 0.1 mg tablet	0.1 mg	Oral Tablet	Oral
Clonidine 0.2 mg tablet	0.2 mg	Oral Tablet	Oral
Clonidine 0.3 mg tablet	0.3 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

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100	Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
101	Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
102	Product Information. Thalomid (thalidomide). Celgene Corporation, Warren, NJ.
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104	Product Information. Clozaril (clozapine). Novartis Pharmaceuticals, East Hanover, NJ.