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Guanfacine
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| Clinical data | |
|---|---|
| Trade names | Estulic, Intuniv, Tenex, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a601059 |
| License data |
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| Routes of administration | By mouth |
| Drug class | Centrally acting α2A- adrenergic receptor agonist |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | 80–100% (IR), 58% (XR)[5][6] |
| Protein binding | 70%[5][6] |
| Metabolism | CYP3A4[5][6] |
| Elimination half-life | IR: 10–17 hours; XR: 17 hours (10–30) in adults & adolescents and 14 hours in children[5][6][7][8] |
| Excretion | Kidney (80%; 50% [range: 40–75%] as unchanged drug)[5][6] |
| Identifiers | |
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| CAS Number | |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.044.933 |
| Chemical and physical data | |
| Formula | C9H9Cl2N3O |
| Molar mass | 246.09 g·mol−1 |
| 3D model (JSmol) | |
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  (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][9] Guanfacine is FDA-approved for monotherapy treatment of ADHD,[3] as well as being used for augmentation of other treatments, such as stimulants.[9] Guanfacine is also used off-label to treat tic disorders, anxiety disorders, and post-traumatic stress disorder (PTSD).[10]
Common side effects include sleepiness, constipation, and dry mouth.[9] Other side effects may include low blood pressure and urinary problems.[11] 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.[12][11] It appears to work by activating α2A-adrenergic receptors in the brain, thereby decreasing sympathetic nervous system activity.[9]
Guanfacine was first described by 1974[13] and was approved for medical use in the United States in 1986.[9] It is available as a generic medication.[9] In 2021, it was the 231st most commonly prescribed medication in the United States, with more than 1 million prescriptions.[14][15]
- ^ "Prescription medicines: registration of new chemical entities in Australia, 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 9 April 2023.
- ^ "Prescription medicines and biologicals: TGA annual summary 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 31 March 2024.
- ^ 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.
- ^ "Intuniv EPAR". European Medicines Agency. 17 September 2015. Retrieved 13 June 2024.
- ^ 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.
- ^ a b c d e "guanfacine (Rx) - Intuniv, Tenex". Medscape Reference. WebMD. Archived from the original on 18 May 2019. Retrieved 9 November 2013.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ a b British national formulary: BNF 76 (76 ed.). Pharmaceutical Press. 2018. pp. 349–350. ISBN 978-0-85711-338-2.
- ^ "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.
- ^ Cite error: The named reference
Turner1974was invoked but never defined (see the help page). - ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
- ^ "Guanfacine - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
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