Clonidine

• CAT Number: R023441
• CAS Number: 4205-90-7
• Molecular Formula: C9H9Cl2N3
• Molecular Weight: 230.092
• Purity: ≥95%
• Target: α2 adrenergic agonist
• Storage: Store at +4C
• IUPAC Name: N-(2,6-dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine
• InChI: 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)
• InChIKey: GJSURZIOUXUGAL-UHFFFAOYSA-N
• SMILES: C1CN=C(N1)NC2=C(C=CC=C2Cl)Cl

Clonidine (trade names Catapres, Kapvay, Nexiclon, Clophelin, and others) is a sympathomimetic medication used to treat high blood pressure, attention deficit hyperactivity disorder, anxiety disorders, withdrawal (from either alcohol, opioids, or smoking), migraine, menopausal flushing, diarrhea, and certain pain conditions. It is classified as a centrally acting α2 adrenergic agonist and imidazoline receptor agonist that has been in clinical use for over 40 years. Clonidine treats high blood pressure by stimulating α2-receptors in the brain, which decreases peripheral vascular resistance, lowering blood pressure. It has specificity towards the presynaptic α2-receptors in the vasomotor center in the brainstem. This binding decreases presynaptic calcium levels, thus inhibiting the release of norepinephrine (NE). The net effect is a decrease in sympathetic tone.[40] It has also been proposed that the antihypertensive effect of clonidine is due to agonism on the I1-receptor (imidazoline receptor), which mediates the sympatho-inhibitory actions of imidazolines to lower blood pressure. Its mechanism of action in the treatment of ADHD is to increase noradrenergic tone in the prefrontal cortex (PFC) directly by binding to postsynaptic α2A adrenergic receptors and indirectly by increasing norepinephrine input from the locus coeruleus. (Souce: https://en.wikipedia.org/wiki/Clonidine). (Last update: 12/18/2015).

Reference

1:Perineural Dexmedetomidine Is More Effective Than Clonidine When Added to Local Anesthetic for Supraclavicular Brachial Plexus Block: A Systematic Review and Meta-analysis. El-Boghdadly K, Brull R, Sehmbi H, Abdallah FW.Anesth Analg. 2017 Jun;124(6):2008-2020. doi: 10.1213/ANE.0000000000002014. PMID: 28525514 2:Clonidine adhesive patch for the treatment of tic disorders: A systematic review and meta-analysis. Wang S, Wei YZ, Yang J, Zhou Y, Zheng Y.Eur J Paediatr Neurol. 2017 Apr 7. pii: S1090-3798(17)30182-4. doi: 10.1016/j.ejpn.2017.03.003. [Epub ahead of print] PMID: 28495246 3:Clonidine for sedation and analgesia for neonates receiving mechanical ventilation. Romantsik O, Calevo MG, Norman E, Bruschettini M.Cochrane Database Syst Rev. 2017 May 10;5:CD012468. doi: 10.1002/14651858.CD012468.pub2. [Epub ahead of print] Review. PMID: 28488361 4:Respiration driven excessive sinus tachycardia treated with clonidine. Li Kam Wa ME, Taraborrelli P, Hayat S, Lim PB.BMJ Case Rep. 2017 Apr 28;2017. pii: bcr2016216818. doi: 10.1136/bcr-2016-216818. PMID: 28455405 5:A comparative study of the effect of clonidine, fentanyl, and the combination of both as adjuvant to intrathecal bupivacaine for postoperative analgesia in total abdominal hysterectomy. Ahmed F, Khandelwal M, Sharma A.J Anaesthesiol Clin Pharmacol. 2017 Jan-Mar;33(1):102-106. doi: 10.4103/0970-9185.202194. PMID: 28413281 Free PMC Article6:Effect of Addition of Fentanyl and Clonidine to Local Anesthetic Solution in Peribulbar Block. Nehra P, Oza V, Parmar V, Fumakiya P.J Pharmacol Pharmacother. 2017 Jan-Mar;8(1):3-7. doi: 10.4103/jpp.JPP_109_16. PMID: 28405129 Free PMC Article7:Evaluation of Gabapentin and Clonidine Use in Children Following Spinal Fusion Surgery for Idiopathic Scoliosis: A Retrospective Review. Choudhry DK, Brenn BR, Sacks K, Shah S.J Pediatr Orthop. 2017 Apr 10. doi: 10.1097/BPO.0000000000000989. [Epub ahead of print] PMID: 28399049 8:Inhibition of Voltage-Gated Na+ Channels by Bupivacaine Is Enhanced by the Adjuvants Buprenorphine, Ketamine, and Clonidine. Stoetzer C, Martell C, de la Roche J, Leffler A.Reg Anesth Pain Med. 2017 Apr 7. doi: 10.1097/AAP.0000000000000596. [Epub ahead of print] PMID: 28394849 9:A highly sensitive method for the simultaneous UHPLC-MS/MS analysis of clonidine, morphine, midazolam and their metabolites in blood plasma using HFIP as the eluent additive. Veigure R, Aro R, Metsvaht T, Standing JF, Lutsar I, Herodes K, Kipper K; CloSed Consortium..J Chromatogr B Analyt Technol Biomed Life Sci. 2017 May 1;1052:150-157. doi: 10.1016/j.jchromb.2017.03.007. Epub 2017 Mar 10. PMID: 28388512 10:Clonidine use in the outpatient management of severe secondary dystonia. Sayer C, Lumsden DE, Kaminska M, Lin JP.Eur J Paediatr Neurol. 2017 Mar 14. pii: S1090-3798(17)30163-0. doi: 10.1016/j.ejpn.2017.03.001. [Epub ahead of print] PMID: 28372940