Xamoterol Explained

Xamoterol, sold under the brand names Corwin, Carwin, Corwil, and Xamtol among others, is a cardiac stimulant which is used in the treatment of heart failure.[1] It acts as a selective partial agonist of the β1-adrenergic receptor with around 50% intrinsic sympathomimetic activity (ISA) (i.e., intrinsic activity).[2] [3] The drug has no significant β2-adrenergic receptor agonistic activity.[4] Xamoterol provides cardiac stimulation at rest but acts as a blocker during exercise.[5] It is taken by mouth.

Xamoterol is not available in the United States.[6] [7] It is marketed in the United Kingdom, Austria, Belgium, and Luxembourg.

Xamoterol is a hydrophilic compound with a predicted log P of -0.31 to -1.11.[8] [9] [10] [11] Due to its hydrophilicity, xamoterol does not cross the blood–brain barrier and has no central nervous system effects. Hence, it is a peripherally selective drug.

Notes and References

  1. Marlow HF . Xamoterol, a beta 1-adrenoceptor partial agonist: review of the clinical efficacy in heart failure . British Journal of Clinical Pharmacology . 28 . 23S–30S . 1989 . Suppl 1 . 2572251 . 1379873 . 10.1111/j.1365-2125.1989.tb03570.x .
  2. Campbell RW . The management of heart failure and the scope for new therapies: what role for xamoterol? . Br J Clin Pharmacol . 28 Suppl 1 . Suppl 1 . 59S–64S . 1989 . 2572256 . 1379877 . 10.1111/j.1365-2125.1989.tb03574.x .
  3. Cruickshank JM . The xamoterol experience in the treatment of heart failure . Am J Cardiol . 71 . 9 . 61C–64C . March 1993 . 8465800 . 10.1016/0002-9149(93)90088-t .
  4. Web site: Xamoterol: Uses, Interactions, Mechanism of Action . DrugBank Online . 23 June 2017 . 23 July 2024.
  5. Book: Rang HP, Dale MM, Ritter JM, Moore PK . Pharmacology. 1999. Churchill Livingstone. Edinburgh; New York. 0443059748. 163. 5th.
  6. Web site: Drugs@FDA: FDA-Approved Drugs . accessdata.fda.gov . 23 July 2024.
  7. Book: Schweizerischer Apotheker-Verein . Index Nominum 2000: International Drug Directory . Medpharm Scientific Publishers . Index nominum . 2000 . 978-3-88763-075-1 . 23 July 2024 . 1099.
  8. Web site: Xamoterol . PubChem . 1 August 2024.
  9. Web site: Xamoterol: Uses, Interactions, Mechanism of Action . DrugBank Online . 23 June 2017 . 1 August 2024.
  10. Web site: Xamoterol [USAN:BAN:INN] ]. ChemSpider . 21 July 2022 . 1 August 2024.
  11. Vigholt-Sørensen E, Faergeman O, Snow HM . Effects of xamoterol, a beta 1 adrenoceptor partial agonist, in patients with ischaemic dysfunction of the left ventricle . Br Heart J . 62 . 5 . 335–341 . November 1989 . 2574049 . 1224831 . 10.1136/hrt.62.5.335 .

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