Terazosin Explained

Terazosin, sold under the brand name Hytrin among others, is a medication used to treat symptoms of an enlarged prostate and high blood pressure.[1] For high blood pressure, it is a less preferred option.[1] It is taken by mouth.[1]

Common side effects include dizziness, headache, tiredness, swelling, nausea, and low blood pressure with standing.[1] Severe side effects may include priapism and low blood pressure.[1] Prostate cancer should be ruled out before starting treatment.[1] It is an alpha-1 blocker and works by relaxing blood vessels and the opening of the bladder.[1]

Terazosin was patented in 1975 and came into medical use in 1985.[2] It is available as a generic medication.[3] In 2021, it was the 234th most commonly prescribed medication in the United States, with more than 1million prescriptions.[4] [5]

Synthesis

Reaction of piperazine with 2-furoyl chloride followed by catalytic hydrogenation of the furan ring leads to 2. This, when heated in the presence of 2-chloro-6,7-dimethoxyquinazolin-4-amine (1) undergoes direct alkylation to terazosin (3).

Research

A 2022 study suggests that terazosin may have the potential to confer neuroprotection upon motor neurons in motor neuron disease, as a result of its ability to activate PGK1.[6]

Notes and References

  1. Web site: Terazosin Hydrochloride Monograph for Professionals . Drugs.com . American Society of Health-System Pharmacists . 17 March 2019 . en.
  2. Book: Fischer J, Ganellin CR . Analogue-based Drug Discovery . 2006 . John Wiley & Sons . 9783527607495 . 455 . en.
  3. Book: British national formulary : BNF 76 . 2018 . Pharmaceutical Press . 9780857113382 . 768 . 76 .
  4. Web site: The Top 300 of 2021 . ClinCalc . 14 January 2024 . 15 January 2024 . https://web.archive.org/web/20240115223848/https://clincalc.com/DrugStats/Top300Drugs.aspx . live .
  5. Web site: Terazosin - Drug Usage Statistics . ClinCalc . 14 January 2024.
  6. Chaytow H, Carroll E, Gordon D, Huang YT, van der Hoorn D, Smith HL, Becker T, Becker CG, Faller KM, Talbot K, Gillingwater TH . Targeting phosphoglycerate kinase 1 with terazosin improves motor neuron phenotypes in multiple models of amyotrophic lateral sclerosis . eBioMedicine . 83 . 104202 . September 2022 . 35963713 . 9482929 . 10.1016/j.ebiom.2022.104202 .