Clonidine

Central alpha-2 Adrenergic Agonist — CARDIOVASCULAR SYSTEM

Key facts

Clonidine is an ofp drug in the Central alpha-2 Adrenergic Agonist class catalogued in DrugCentral. It was first approved by the FDA in 1974. Its mechanism of action is classified as Adrenergic alpha2-Agonists. DrugCentral lists 30 molecular targets, including Adra2a, Adra2b|Adra2c|Adra2a and ADRA2A. Recorded indications include Attention deficit hyperactivity disorder, Hypertensive disorder, Increased Intraocular Pressure after Ocular Procedure and Open-angle glaucoma.

• Approval status: ofp (first approved 1974 by the FDA).
• Drug class: Central alpha-2 Adrenergic Agonist.
• Mechanism of action: Adrenergic alpha2-Agonists.
• Molecular targets: Adra2a, Adra2b|Adra2c|Adra2a, ADRA2A and ADRA2A (30 listed in DrugCentral).
• Indications: Attention deficit hyperactivity disorder, Hypertensive disorder, Increased Intraocular Pressure after Ocular Procedure, Open-angle glaucoma and Severe pain.
• ATC code: C02AC01 (Imidazoline receptor agonists).
• Molecular formula: C9H9Cl2N3; molecular weight 230.09 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (5)

• Attention deficit hyperactivity disorder
• Hypertensive disorder
• Increased Intraocular Pressure after Ocular Procedure
• Open-angle glaucoma
• Severe pain

Off-label uses (8)

• Diarrhea
• Gilles de la Tourette's syndrome
• Menopausal flushing
• Nicotine Withdrawal Symptoms
• Ocular hypertension
• Opioid withdrawal
• Pain
• Smoking cessation assistance

Contraindications (40)

• Acute nephropathy
• Acute pancreatitis
• Anuria
• Atrioventricular block
• Blood coagulation disorder
• Bradycardia
• Cerebrovascular disease
• Chronic myocardial ischemia
• Conduction disorder of the heart
• Decreased respiratory function
• Depressive disorder
• Diabetes mellitus type 1
• Diabetes mellitus type 2
• End stage renal disease
• Gout
• Hepatic failure
• Hypercalcemia
• Hypercholesterolemia
• Hyperuricemia
• Hypochloremic alkalosis
• Hypokalemia
• Hypomagnesemia
• Hyponatremia
• Inflammatory dermatosis
• Labor pain
• Low blood pressure
• Magnetic resonance imaging
• Myocardial infarction
• Myocardial ischemia
• Oliguria
• + 10 more

Mechanism & targets

• Mechanism of action (MoA): Adrenergic alpha2-Agonists
• Established pharmacologic class: Central alpha-2 Adrenergic Agonist

Molecular targets (30)

Target	Gene	Action	Activity
Alpha-2A adrenergic receptor	Adra2a	unknown	Ki 9.41
Adrenergic receptor alpha-2	Adra2b|Adra2c|Adra2a	unknown	Ki 8.82
Alpha-2A adrenergic receptor	ADRA2A	unknown	IC50 8.70
Alpha-2A adrenergic receptor	ADRA2A	agonist	Ki 8.42
Alpha-2B adrenergic receptor	Adra2b	unknown	Ki 8.08
Nischarin	NISCH	unknown	Ki 8.05
Alpha-2B adrenergic receptor	ADRA2B	agonist	Ki 7.50
Alpha-1B adrenergic receptor	—	unknown	EC50 7.08
Alpha-1A adrenergic receptor	ADRA1A	unknown	EC50 7.05
Nischarin	Nisch	unknown	Ki 6.95
Alpha-1D adrenergic receptor	Adra1d	agonist	Ki 6.90
Alpha-2C adrenergic receptor	ADRA2C	agonist	EC50 6.70
Alpha-1A adrenergic receptor	Adra1a	unknown	Kd 6.59
Alpha-1B adrenergic receptor	ADRA1B	unknown	Ki 6.50
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 6.50
Alpha-1D adrenergic receptor	ADRA1D	unknown	Ki 6.22
5-hydroxytryptamine receptor 7	HTR7	unknown	Ki 6.06
Alpha-1B adrenergic receptor	Adra1b	unknown	Ki 5.99
Transmembrane protein 97	TMEM97	unknown	Ki 5.56
5-hydroxytryptamine receptor 1A	HTR1A	unknown	Ki 5.49

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1974-09-03	FDA	—	BOEHRINGER INGELHEIM	Yes

ATC classification

ATC code	Therapeutic hierarchy
C02AC01	CARDIOVASCULAR SYSTEM › ANTIHYPERTENSIVES › ANTIADRENERGIC AGENTS, CENTRALLY ACTING › Imidazoline receptor agonists
C02LC01	CARDIOVASCULAR SYSTEM › ANTIHYPERTENSIVES › ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION › Imidazoline receptor agonists in combination with diuretics
C02LC51	CARDIOVASCULAR SYSTEM › ANTIHYPERTENSIVES › ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION › Imidazoline receptor agonists in combination with diuretics
N02CX02	NERVOUS SYSTEM › ANALGESICS › ANTIMIGRAINE PREPARATIONS › Other antimigraine preparations
S01EA04	SENSORY ORGANS › OPHTHALMOLOGICALS › ANTIGLAUCOMA PREPARATIONS AND MIOTICS › Sympathomimetics in glaucoma therapy

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Completed suicide	978.5
Food allergy	776.1
Temperature regulation disorder	715.3
Immunodeficiency	563.9
Drug withdrawal syndrome	502.6
Bradycardia	456.8
Hypertension	453.2
Hyperhidrosis	441.9
Overdose	411.0
Upper respiratory tract infection	341.8
Coeliac disease	317.2
Rash erythematous	313.5

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Clonidine is on its molecule page.

• Molecular formula: C₉H₉Cl₂N₃
• Molecular weight: 230.09 g/mol
• CAS number: 4205-90-7
• InChIKey: GJSURZIOUXUGAL-UHFFFAOYSA-N
• PubChem CID: 2803

ClC1=CC=CC(Cl)=C1NC1=NCCN1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Clonidine used for?

DrugCentral lists the following indications for Clonidine: Attention deficit hyperactivity disorder, Hypertensive disorder, Increased Intraocular Pressure after Ocular Procedure, Open-angle glaucoma and Severe pain.

How does Clonidine work?

Clonidine is classified as Adrenergic alpha2-Agonists; its molecular targets in DrugCentral include Adra2a, Adra2b|Adra2c|Adra2a, ADRA2A and ADRA2A (agonist).

When was Clonidine first approved?

Clonidine was first approved by the FDA in 1974.

What drug class does Clonidine belong to?

Clonidine is in the Central alpha-2 Adrenergic Agonist class.

What is the chemical formula of Clonidine?

Clonidine has the molecular formula C9H9Cl2N3 and a molecular weight of 230.09 g/mol.

Sources

• DrugCentral drug card 704 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL134 — compound record and bioactivity
• PubChem CID 2803 — chemical identifiers
• DrugBank DB00575 — drug record
• FDA UNII MN3L5RMN02 — substance identity
• DailyMed: FDA labels for Clonidine — current prescribing information (label search)
• UniProt P08913 (ADRA2A) — target protein
• UniProt Q9Y2I1 (NISCH) — target protein
• UniProt P18089 (ADRA2B) — target protein
• UniProt P18825 (ADRA2C) — target protein
• UniProt P35368 (ADRA1B) — target protein
• UniProt P35348 (ADRA1A) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.