Guanfacine
Clinical data | |
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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)[4][5] |
Protein binding | 70%[4][5] |
Metabolism | CYP3A4[4][5] |
Elimination half-life | IR: 10–17 hours; XR: 17 hours (10–30) in adults & adolescents and 14 hours in children[4][5][6][7] |
Excretion | Kidney (80%; 50% [range: 40–75%] as unchanged drug)[4][5] |
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JSmol) | |
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Guanfacine, sold under the brand name Tenex (
Common
Guanfacine was first described by 1974
Medical uses
Guanfacine is FDA-approved as monotherapy or augmentation with stimulants to treat
Guanfacine is also used off-label to treat tic disorders, anxiety disorders such as generalized anxiety disorder, and PTSD.
Adverse effects
Very common (>10% incidence) adverse effects include
Common (1–10% incidence) adverse effects include
Guanfacine has been reported to cause high rates of somnolence in children with ADHD, for instance 73% with guanfacine versus 6% with placebo in one trial.[30][31]
Guanfacine may worsen
A 2020
Interactions
Guanfacine availability is significantly affected by the
Pharmacology
Pharmacodynamics
Site | Ki (nM) | Species | Ref |
---|---|---|---|
α2A | 50.3 – 93.3 | Human | [34][35] |
α2B | 1,020 – 1,380 | Human | [34][35] |
α2C | 1,120 – 3,890 | Human | [34][35] |
The smaller the value, the more strongly the drug binds to the site. |
Guanfacine is a highly
Guanfacine works by activating α2A-adrenoceptors
In ADHD, guanfacine is thought to work by strengthening the regulation of attention and behavior by the
Guanfacine is much more selective for α2A-adrenergic receptors than
Activation of the 5-HT2B receptor is a well-known
Pharmacokinetics
Guanfacine has an
Preparation
Guanfacine can be prepared from equal parts methyl 2,6-dichlorophenylacetate and guanidine:[49]
History
Guanfacine was first described in the literature by 1974.[12][50][51][52][53] In 1986, guanfacine was approved by the FDA for the treatment of hypertension under the brand name Tenex.[54] In 2010, guanfacine was approved by the FDA for the treatment of attention deficit hyperactivity disorder for people 6 to 17 years old.[15] It was approved for ADHD by the European Medicines Agency under the name Intuniv in 2015.[55] It was added to the Australian Pharmaceutical Benefits Scheme for the treatment of ADHD in 2018.[56]
Society and culture
Brand names
Brand names include Tenex, Afken, Estulic, and Intuniv (an
Research
Guanfacine has been studied as a treatment for post-traumatic stress disorder (PTSD). Evidence of efficacy in adults is limited, but one study found positive results in children with comorbid ADHD.[57] It may be also useful in adult PTSD patients who do not respond to selective serotonin reuptake inhibitors (SSRIs).[58]
Results of studies using guanfacine to treat
Guanfacine does not appear to be effective for improving
Guanfacine has been investigated for treatment of withdrawal for opioids, ethanol, and nicotine.[60] Guanfacine has been shown to help reduce stress-induced craving of nicotine in smokers trying to quit, which may involve strengthening of prefrontal cortex-mediated self-control.[61]
Guanfacine has been researched for treatment of a variety of conditions impacting
Guanfacine is being studied for the possible treatment of long COVID.[63][64][65]
References
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- ^ "Prescription medicines and biologicals: TGA annual summary 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 31 March 2024.
- ^ a b c d "Intuniv- guanfacine tablet, extended release Intuniv- guanfacine kit". DailyMed. 26 January 2021. Archived from the original on 6 August 2022. Retrieved 6 August 2022.
- ^ 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 f "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.
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- ^ a b c d e f g "Guanfacine Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 15 January 2018. Retrieved 18 March 2019.
- ^ OCLC 1264172789. Archived from the original on 8 February 2023. Retrieved 12 January 2023.)
{{cite book}}
: CS1 maint: location missing publisher (link - ^ 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.
- ^ a b Turner, A. S. (1974). BS 100-141 in the treatment of arterial hypertension. Seventh World Congr. of Cardiol., Abstr, 336.
- ^ "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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- ^ a b Roth BL, Driscol J (12 January 2011). "PDSP Ki Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Archived from the original on 8 November 2013. Retrieved 15 November 2013.
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These results strongly indicate substantial risks for treatments involving 5-HT2B agonists, and it has been recommended that all serotonergic drugs be screened for this functional profile.43,59 [...] Additionally, there are cases of marketed drugs that were only later determined to have 5-HT2B activity. Of particular note is guanfacine, an FDA-approved medication for the treatment of attention deficit hyperactivity disorder (ADHD) that possesses potent 5-HT2B agonist activity in functional readouts to a similar degree as known valvulopathogens.66
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- ^ Tardner P (May 2023). "A Comprehensive Literature Review on Guanfacine as a Potential Treatment for Attention-Deficit/Hyperactivity Disorder (ADHD)". International Journal of Environmental Science and Technology.
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- ^ a b c d e Therapeutic Goods Administration (May 2018). "Australian Public Assessment Report for Guanfacine (as hydrochloride)" (PDF).
- ^ a b Roihuvuo, E. (2022). Classical psychedelics and NBOMes as serotonin 2B receptor agonists: Valvulopathogenic signaling pathways and cardiac safety concerns (Master's thesis, Itä-Suomen yliopisto). http://urn.fi/urn:nbn:fi:uef-20220118
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The list of valvulopathic drugs is short and can be seen in Table 7. According to a recent analysis, other drugs, in particular guanfacine, might possess some risk, but clinical data are yet not available.368–370
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- ^ "New drugs listed on the PBS for rheumatoid arthritis, cystic fibrosis and ADHD". Royal Australian College of General Practitioners. Archived from the original on 11 September 2018. Retrieved 11 September 2018.
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