Back غوانفاسين Arabic Gwanffacin Welsh Guanfacin German Guanfacina Spanish گوانفاسین Persian Guanfasiini Finnish Guanfacine French גואנפצין HE グアンファシン Japanese ଗୁଆନଫେସିନ OR

Guanfacine

Not to be confused with Guanine, Guanosine, Guanidine, Guaifenesin, or Clonidine.

Guanfacine
Clinical data
Trade namesEstulic, Intuniv, Tenex, others
AHFS/Drugs.comMonograph
MedlinePlusa601059
License data
Routes of
administration		By mouth
Drug classCentrally acting α2A- adrenergic receptor agonist
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability80–100% (IR), 58% (XR)[4][5]
Protein binding70%[4][5]
MetabolismCYP3A4[4][5]
Elimination half-lifeIR: 10–17 hours; XR: 17 hours (10–30) in adults & adolescents and 14 hours in children[4][5][6][7]
ExcretionKidney (80%; 50% [range: 40–75%] as unchanged drug)[4][5]
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 Edit this at Wikidata
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) checkY
  • Key:INJOMKTZOLKMBF-UHFFFAOYSA-N checkY
 ☒NcheckY (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.[3][8] Guanfacine is FDA-approved for monotherapy treatment of ADHD,[3] as well as being used for augmentation of other treatments, such as stimulants.[8] Guanfacine is also used off-label to treat tic disorders, anxiety disorders, and post-traumatic stress disorder (PTSD).[9]

Common side effects include sleepiness, constipation, and dry mouth.[8] Other side effects may include low blood pressure and urinary problems.[10] The FDA has categorized Guanfacine as "Category B" in pregnancy, which means animal-reproduction studies have not demonstrated a fetal risk or an adverse effect during pregnancy or breastfeeding.[11][10] It appears to work by activating α2A-adrenergic receptors in the brain, thereby decreasing sympathetic nervous system activity.[8]

Guanfacine was first described by 1974[12] and was approved for medical use in the United States in 1986.[8] It is available as a generic medication.[8] In 2021, it was the 231st most commonly prescribed medication in the United States, with more than 1 million prescriptions.[13][14]

  1. ^ "Prescription medicines: registration of new chemical entities in Australia, 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 9 April 2023.
  2. ^ "Prescription medicines and biologicals: TGA annual summary 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 31 March 2024.
  3. ^ a b c "Intuniv- guanfacine tablet, extended release Intuniv- guanfacine kit". DailyMed. 26 January 2021. Archived from the original on 6 August 2022. Retrieved 6 August 2022.
  4. ^ a b c d e "Guanfacine (guanfacine) Tablet [Genpharm Inc.]". DailyMed. Genpharm Inc. March 2007. Archived from the original on 26 June 2022. Retrieved 9 November 2013.
  5. ^ a b c d e "guanfacine (Rx) - Intuniv, Tenex". Medscape Reference. WebMD. Archived from the original on 18 May 2019. Retrieved 9 November 2013.
  6. ^ Hofer KN, Buck ML (2008). "New Treatment Options for Attention-Deficit/Hyperactivity Disorder (ADHD): Part II. Guanfacine". Pediatric Pharmacotherapy (14): 4. Archived from the original on 31 October 2015. Retrieved 30 July 2014.
  7. ^ Cruz MP (August 2010). "Guanfacine Extended-Release Tablets (Intuniv), a Nonstimulant Selective Alpha(2A)-Adrenergic Receptor Agonist For Attention-Deficit/Hyperactivity Disorder". P & T. 35 (8): 448–451. PMC 2935643. PMID 20844694.
  8. ^ a b c d e f "Guanfacine Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 15 January 2018. Retrieved 18 March 2019.
  9. ^ Boland RJ, Verduin ML, Sadock BJ (2023). Ruiz P (ed.). Kaplan & Sadock's Concise Textbook of Clinical Psychiatry (5th ed.). Philadelphia: Wolters Kluwer. pp. 1811–1812. ISBN 978-1-9751-6748-6. OCLC 1264172789. Archived from the original on 8 February 2023. Retrieved 12 January 2023.
  10. ^ a b British national formulary: BNF 76 (76 ed.). Pharmaceutical Press. 2018. pp. 349–350. ISBN 978-0-85711-338-2.
  11. ^ "Patient Information. INTUNIV (in-TOO-niv) (guanfacine). Extended-Release Tablets" (PDF). FDA.gov. Archived (PDF) from the original on 13 October 2022. Retrieved 12 October 2022.
  12. ^ Cite error: The named reference Turner1974 was invoked but never defined (see the help page).
  13. ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  14. ^ "Guanfacine - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.

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