User:Mr. Ibrahem/Clonidine

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Mr. Ibrahem/Clonidine
Clinical data
Pronunciation/ˈklɒnədiːn/
Trade namesCatapres, Kapvay, Nexiclon, others
AHFS/Drugs.comMonograph
MedlinePlusa682243
License data
Pregnancy
category
  • AU: B3
Routes of
administration		By mouth, epidural, IV, transdermal, topical
Drug classα2 receptor agonist[1]
Legal status
Legal status
Pharmacokinetic data
Bioavailability70–80% (oral),[2] 60–70% (transdermal)[3]
Protein binding20–40%[4]
MetabolismLiver to inactive metabolites,[4] 2/3 CYP2D6 [1]
Onset of actionIR:30-60 minutes after an dose by mouth[5]
Elimination half-lifeIR: 12–16 hours; 41 hours in kidney failure,[6][7] 48 hours for repeated dosing[3]
ExcretionUrine (72%)[4]
Identifiers
  • N-(2,6-Dichlorophenyl)-4,5--1H-imidazol-2-amine
Chemical and physical data
FormulaC9H9Cl2N3
Molar mass230.09 g·mol−1
3D model (JSmol)
  • Clc1cccc(Cl)c1N/C2=N/CCN2
  • InChI=1S/C9H9Cl2N3/c10-6-2-1-3-7(11)8(6)14-9-12-4-5-13-9/h1-3H,4-5H2,(H2,12,13,14) checkY
  • Key:GJSURZIOUXUGAL-UHFFFAOYSA-N checkY
  (verify)

Clonidine, sold as the brand name Catapres among others, is a medication used to treat high blood pressure, attention deficit hyperactivity disorder, drug withdrawal (alcohol, opioids, or smoking), menopausal flushing, diarrhea, and certain pain conditions.[1] It is used by mouth, by injection, or as a skin patch.[1] Onset of action is typically within an hour with the effects on blood pressure lasting for up to eight hours.[1]

Common side effect include dry mouth, dizziness, headaches, and sleepiness.[1] Severe side effects may include seeing or hearing things that other people do not, heart arrhythmias, and confusion.[9] If rapidly stopped, withdrawal effects may occur.[1] Use during pregnancy or breastfeeding is not recommended.[9] Clonidine lowers blood pressure by stimulating α2 receptors in the brain, which results in relaxation of many arteries.[1]

Clonidine was patented in 1961 and came into medical use in 1966.[10][11][12] It is available as a generic medication.[1] As of 2019 a month of medication costs the NHS about £8.[9] In the United States this amount costs about US$2.70 as of 2019.[13] In 2017, it was the 79th most commonly prescribed medication in the United States, with more than ten million prescriptions.[14][15]

References[edit]

  1. ^ a b c d e f g h i j "Clonidine Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 3 February 2019. Retrieved 2 February 2019.
  2. ^ "Catapres- clonidine hydrochloride tablet". DailyMed. 2016-09-06. Archived from the original on 2020-08-04. Retrieved 2019-12-21. The pharmacokinetics of clonidine is dose-proportional in the range of 100 to 600 µg.The absolute bioavailability of clonidine on oral administration is 70% to 80%. Peak plasma clonidine levels are attained in approximately 1 to 3 hours.
  3. ^ a b Lowenthal, DT; Matzek, KM; MacGregor, TR (May 1988). "Clinical pharmacokinetics of clonidine". Clinical Pharmacokinetics. 14 (5): 287–310. doi:10.2165/00003088-198814050-00002. PMID 3293868.
  4. ^ a b c "clonidine (Rx) - Catapres, Catapres-TTS, more." Medscape Reference. WebMD. Archived from the original on 4 December 2020. Retrieved 10 November 2013.
  5. ^ "Catapres- clonidine hydrochloride tablet". DailyMed. 2016-09-06. Archived from the original on 2020-08-04. Retrieved 2019-12-21. Catapres tablets act relatively rapidly. The patient's blood pressure declines within 30 to 60 minutes after an oral dose, the maximum decrease occurring within 2 to 4 hours.
  6. ^ "Catapres- clonidine hydrochloride tablet". DailyMed. 2016-09-06. Archived from the original on 2020-08-04. Retrieved 2019-12-21. Following intravenous administration, clonidine displays biphasic disposition with a distribution half-life of about 20 minutes and an elimination half-life ranging from 12 to 16 hours. The half-life increases up to 41 hours in patients with severe impairment of renal function. Clonidine crosses the placental barrier. It has been shown to cross the blood-brain barrier in rats.
  7. ^ "Kapvay". RxList. Archived from the original on 2017-10-12. Retrieved 2014-10-30.
  8. ^ "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 30 October 2020. Retrieved 9 September 2020.
  9. ^ a b c British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 144. ISBN 9780857113382.
  10. ^ Neil, MJ (November 2011). "Clonidine: clinical pharmacology and therapeutic use in pain management". Current Clinical Pharmacology. 6 (4): 280–7. doi:10.2174/157488411798375886. PMID 21827389.
  11. ^ Stähle, Helmut (June 2000). "A historical perspective: development of clonidine". Best Practice & Research Clinical Anaesthesiology. 14 (2): 237–246. doi:10.1053/bean.2000.0079.
  12. ^ Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 550. ISBN 9783527607495. Archived from the original on 2019-03-06. Retrieved 2019-03-03.
  13. ^ "NADAC as of 2019-01-30". Centers for Medicare and Medicaid Services. Archived from the original on 2019-03-27. Retrieved 3 February 2019.
  14. ^ "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 11 April 2020.
  15. ^ "Clonidine - Drug Usage Statistics". ClinCalc. Archived from the original on 8 July 2020. Retrieved 11 April 2020.
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