Guanfacine

Central alpha-2 Adrenergic Agonist — CARDIOVASCULAR SYSTEM

Key facts

Guanfacine is an ofp drug in the Central alpha-2 Adrenergic Agonist class catalogued in DrugCentral. It was first approved by the FDA in 1986. Its mechanism of action is classified as Adrenergic alpha2-Agonists. DrugCentral lists 10 molecular targets, including NISCH, ADRA2A and ADRA1D. Recorded indications include Attention deficit hyperactivity disorder and Hypertensive disorder.

• Approval status: ofp (first approved 1986 by the FDA).
• Drug class: Central alpha-2 Adrenergic Agonist.
• Mechanism of action: Adrenergic alpha2-Agonists.
• Molecular targets: NISCH, ADRA2A, ADRA1D and HTR2C (10 listed in DrugCentral).
• Indications: Attention deficit hyperactivity disorder and Hypertensive disorder.
• ATC code: C02AC02 (Imidazoline receptor agonists).
• Molecular formula: C9H9Cl2N3O; molecular weight 246.09 g/mol.

Indications & contraindications

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

Indications (2)

• Attention deficit hyperactivity disorder
• Hypertensive disorder

Contraindications (15)

• Alcohol intoxication
• Bradycardia
• Cerebrovascular disease
• Chronic myocardial ischemia
• Constipation
• Dehydration
• Depressive disorder
• Disease of liver
• Drowsy
• End stage renal disease
• Heart block
• Low blood pressure
• Myocardial infarction
• Orthostatic hypotension
• Syncope

Mechanism & targets

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

Molecular targets (10)

Target	Gene	Action	Activity
Nischarin	NISCH	unknown	Ki 7.72
Alpha-2A adrenergic receptor	ADRA2A	agonist	EC50 7.16
Alpha-1D adrenergic receptor	ADRA1D	unknown	Ki 6.26
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 6.12
5-hydroxytryptamine receptor 2A	HTR2A	unknown	Ki 6.07
Alpha-2B adrenergic receptor	ADRA2B	agonist	EC50 5.93
5-hydroxytryptamine receptor 2B	HTR2B	unknown	Ki 5.88
Alpha-1A adrenergic receptor	Adra1a	unknown	IC50 5.87
Alpha-2C adrenergic receptor	ADRA2C	agonist	EC50 5.68
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 5.33

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2017-03-30	PMDA	—	Shionogi & Co., Ltd.
2015-09-17	EMA	—	Takeda Pharmaceuticals International AG Ireland Branch
1986-10-27	FDA	—	PROMIUS PHARMA

ATC classification

ATC code	Therapeutic hierarchy
C02AC02	CARDIOVASCULAR SYSTEM › ANTIHYPERTENSIVES › ANTIADRENERGIC AGENTS, CENTRALLY ACTING › Imidazoline receptor agonists

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
Aggression	553.8
Product substitution issue	436.9
Electrocardiogram QT prolonged	405.7
Bradycardia	381.4
Intentional overdose	359.7
Somnolence	321.6
Abnormal behaviour	249.4
Suicidal ideation	212.9
Agitation	197.1
Psychomotor hyperactivity	196.5
Impulsive behaviour	195.8
Irritability	188.7

Chemical structure

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

• Molecular formula: C₉H₉Cl₂N₃O
• Molecular weight: 246.09 g/mol
• CAS number: 29110-47-2
• InChIKey: INJOMKTZOLKMBF-UHFFFAOYSA-N
• PubChem CID: 3519

NC(=N)NC(=O)CC1=C(Cl)C=CC=C1Cl

Frequently asked questions

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

What is Guanfacine used for?

DrugCentral lists the following indications for Guanfacine: Attention deficit hyperactivity disorder and Hypertensive disorder.

How does Guanfacine work?

Guanfacine is classified as Adrenergic alpha2-Agonists; its molecular targets in DrugCentral include NISCH, ADRA2A (agonist), ADRA1D and HTR2C.

When was Guanfacine first approved?

Guanfacine was first approved by the FDA in 1986.

What drug class does Guanfacine belong to?

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

What is the chemical formula of Guanfacine?

Guanfacine has the molecular formula C9H9Cl2N3O and a molecular weight of 246.09 g/mol.

Sources

• DrugCentral drug card 1343 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1200494 — compound record and bioactivity
• PubChem CID 3519 — chemical identifiers
• DrugBank DB01018 — drug record
• FDA UNII 30OMY4G3MK — substance identity
• DailyMed: FDA labels for Guanfacine — current prescribing information (label search)
• UniProt Q9Y2I1 (NISCH) — target protein
• UniProt P08913 (ADRA2A) — target protein
• UniProt P25100 (ADRA1D) — target protein
• UniProt P28335 (HTR2C) — target protein
• UniProt P28223 (HTR2A) — target protein
• UniProt P18089 (ADRA2B) — 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.