Guanfacine
Medication used for high blood pressure and ADHD / From Wikipedia, the free encyclopedia
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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]
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Trade names | Estulic, Intuniv, Tenex, others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a601059 |
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Routes of administration | By mouth |
Drug class | Centrally acting α2A- adrenergic receptor agonist |
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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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ECHA InfoCard | 100.044.933 |
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Formula | C9H9Cl2N3O |
Molar mass | 246.09 g·mol−1 |
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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]