Synthesis and effects on peripheral thyroid hormone conversion of (R)-4-hydroxypropranolol, a main metabolite of (R)-propranolol

✍ Scribed by Wolfgang Buchinger; Otto Eber; Georg Uray; Peter Lind; Doz. Dr. Wolfgang Lindner

• Book ID: 102797931
• Publisher: John Wiley and Sons
• Year: 1991
• Tongue: English
• Weight: 686 KB
• Volume: 3
• Category: Article
• ISSN: 0899-0042
• DOI: 10.1002/chir.530030212

✦ Synopsis

The inhibiting effect of (R,S)-propranolol on peripheral T4E3 conversion can be related to the (R)-isomer. The intention of this study is to clarify if (R)-4-hydroxypropranolol, a main metabolite of (R)-propranolol, develops the same or even a stronger effect on peripheral thyroxine metabolism as the parent drug. (R)-4-hydroxypropranolol was synthesized via (R)-4-methoxypropranolol and their optical purity was checked chromatographically. Twenty patients suffering from hyperthyroidism were divided into five groups and treated with (Rb4-h~droxypropranolol HC1 in dosages from 12 to 75 mg per day in a placebo controlled study over a period of 5 days. The serum hormone levels and resting pulse rate were measured. No significant changes of thyroid parameter could be observed but a significant decrease of resting pulse rate under treatment with 75 mg (R)-4hydroxypropranolol occurred. It could be concluded that (R)-4-hydroxypropran-0101 possesses negative chronotropic effects but develops no changes in thyroid hormone metabolism in hyperthyroid patients.