Guanfacine

Guanfacine
Clinical data
Pronunciation /ˈɡwɑːnfəsin/
GWAHN-fə-seen
Trade namesIntuniv, others
AHFS/Drugs.comMonograph
MedlinePlusa601059
License data
Routes of
administration
By mouth
Drug classα2A-adrenergic receptor agonist
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability80–100% (IR), 58% (XR)
Protein binding70%
MetabolismCYP3A4
Elimination half-lifeIR: 10–17 hours; XR: 17 hours (10–30) in adults & adolescents and 14 hours in children
ExcretionKidney (80%; 50% [range: 40–75%] as unchanged drug)
Identifiers
  • N-(Diaminomethylidene)-2-(2,6-dichlorophenyl)acetamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.044.933
Chemical and physical data
FormulaC9H9Cl2N3O
Molar mass246.09 g·mol−1
3D model (JSmol)
  • Clc1cccc(Cl)c1CC(=O)\N=C(/N)N
  • InChI=1S/C9H9Cl2N3O/c10-6-2-1-3-7(11)5(6)4-8(15)14-9(12)13/h1-3H,4H2,(H4,12,13,14,15) Y
  • Key:INJOMKTZOLKMBF-UHFFFAOYSA-N Y
 NY (what is this?)  (verify)

Guanfacine, sold under the brand name Tenex (immediate-release) and Intuniv (extended-release) among others, is an oral alpha-2a agonist medication used to treat attention deficit hyperactivity disorder (ADHD) and high blood pressure.

Common side effects include sleepiness, constipation, and dry mouth. Other side effects may include low blood pressure and urinary problems. It appears to work by activating α2A-adrenergic receptors in the brain, thereby decreasing sympathetic nervous system activity.

Guanfacine was first described in 1974 and was approved for medical use in the United States in 1986. It is available as a generic medication. In 2022, it was the 275th most commonly prescribed medication in the United States, with more than 800,000 prescriptions. Guanfacine is approved by the US FDA for monotherapy treatment of ADHD, as well as being used for augmentation of stimulant medications. Guanfacine is also used off-label to treat tic disorders, anxiety disorders, and post-traumatic stress disorder (PTSD).