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Clonidine

From Wikipedia
clonidine
type of chemical entity
Subclass ofchemical compound Edit
Get useMedication Edit
Stylized namecloNIDine Edit
Chemical formulaC₉H₉Cl₂N₃ Edit
Canonical SMILESC1CN=C(N1)NC2=C(C=CC=C2Cl)Cl Edit
Active ingredient inDuraclon, Kapvay, Catapres-TTS-3, Catapres-TTS-2, Catapres-TTS-1 Edit
Legal status (medicine)boxed warning Edit
Pregnancy categoryAustralian pregnancy category B3, US pregnancy category C Edit
LiverTox likelihood scoreLiverTox toxicity likelihood category E Edit
Subject has roleAdrenergic alpha-2 Receptor Agonists, antihypertensive drug, analgesic, Sympatholytic Edit

Clonidine, dem sell under de brand name Catapres among odas, be an α2-adrenergic receptor agonist, hypotensive, sedative den anxiolytic drug dem use to treat high blood pressure, attention deficit hyperactivity disorder, perioperative pain, drug withdrawal (e.g., alcohol, opioids, anaa nicotine), den menopausal flushing.[1][2][3] Clonidine often be prescribed off-label for tics. E be used orally (by mouth), by injection, anaa as a transdermal skin patch.[3] Onset of action typically be within an hour plus de effects on blood pressure wey dey last for up to eight hours.[3] Xylazine be a structural analog of clonidine.[4]

Common side effects dey include dry mouth, dizziness, headaches, hypotension, den sleepiness.[3] Severe side effects fi include hallucinations, heart arrhythmias, den confusion.[5] If dem rapidly stop, withdrawal effects fi occur, such as a dangerous rise in blood pressure.[3] Use during pregnancy anaa breastfeeding no be recommended.[5] Clonidine dey lower blood pressure by stimulating α2-adrenergic receptors den imidazoline receptors insyd de brain, wich dey result in relaxation of chaw arteries.[1][3]

Dem patent clonidine insyd 1961 wey e cam into medical use insyd 1966.[6][7][8] E be available as a generic medication.[3] Insyd 2023, e be de 82nd most commonly prescribed medication insyd de United States, plus more dan 8 million prescriptions.[9][10]

References

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  1. 1 2 Stahl SM (2021). Stahl's essential psychopharmacology: neuroscientific basis and practical applications (5th ed.). Cambridge: Cambridge University Press. pp. 482–83. ISBN 978-1-108-97529-2. Clonidine is a relatively nonselective agonist at α2 receptors, with actions on α2A, α2B, and α2C receptors. In addition, clonidine has actions on imidazoline receptors, thought to be responsible for some of clonidine's sedating and hypotensive actions. Although the actions of clonidine at α2A receptors exhibit therapeutic potential for ADHD, its actions at other receptors may increase side effects. Clonidine is approved for the treatment of hypertension, but only the controlled release version of clonidine is approved for treatment of ADHD. ... Unlike clonidine, guanfacine is 15–60 times more selective for α2A receptors than for α2B and α2C receptors. Additionally, guanfacine is 10 times weaker than clonidine at inducing sedation and lowering blood pressure, yet it is 25 times more potent in enhancing prefrontal cortical function.
  2. ↑ Westfall TC, Macarthur H, Westfall DP (2017). "Chapter 12:Adrenergic Agonists and Antagonists". In Brunton L, Knollmann B, Hilal-Dandan R (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics (13th ed.). McGraw-Hill Education / Medical. ISBN 978-1-259-58473-2.
  3. 1 2 3 4 5 6 7 "Clonidine, Clonidine Hydrochloride Monograph for Professionals". Drugs.com. 10 June 2024. Retrieved 25 December 2025.
  4. ↑ Greene SA, Thurmon JC (December 1988). "Xylazine–a review of its pharmacology and use in veterinary medicine". Journal of Veterinary Pharmacology and Therapeutics. 11 (4): 295–313. doi:10.1111/j.1365-2885.1988.tb00189.x. PMID 3062194.
  5. 1 2 British national formulary: BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 144. ISBN 978-0-85711-338-2.
  6. ↑ Neil MJ (November 2011). "Clonidine: clinical pharmacology and therapeutic use in pain management". Current Clinical Pharmacology. 6 (4): 280–287. doi:10.2174/157488411798375886. PMID 21827389. S2CID 40756251.
  7. ↑ Stähle H (June 2000). "A historical perspective: development of clonidine". Best Practice & Research Clinical Anaesthesiology. 14 (2): 237–246. doi:10.1053/bean.2000.0079.
  8. ↑ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 550. ISBN 978-3-527-60749-5. Archived from the original on 29 April 2023. Retrieved 12 September 2020.
  9. ↑ "Top 300 of 2023". ClinCalc. Archived from the original on 12 August 2025. Retrieved 12 August 2025.
  10. ↑ "Clonidine Drug Usage Statistics, United States, 2013 - 2023". ClinCalc. Retrieved 18 August 2025.
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  • Alpha-2 agonists in ADHD
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