Diltiazem is a calcium channel blocker. It is known in the USA under the trade names of Cardizem, Dilacor, Taztia, Tiazac, and other brand names. It is used to treat angina, hypertension, acute, MI, supraventricular arrhythmias, and hyperthyroidism. It has been used off-label to be a prophylactic for cluster headaches and migraines. It has been shown to decrease cocaine cravings in rats and to enhance the analgesic response to morphine without an increase in the incidence of respiratory depression and reduces the development of tolerance. Lastly, it has been used to treat anal fissures, both orally and topically. https://en.wikipedia.org/wiki/Diltiazem
The most interesting thing about diltiazem is the history of its discovery. Since it was approved for use in 1982 this research must have occurred in the late 1960s and 1970s. Apparently, the Tanabe Seiyaku Company of Japan wanted to enter the growing market of psychoactive drugs. They produced many benzodiazepines (Valium type drugs) with many different side chains. During the screening of these compounds, it was found that a certain benzothiazepine had a strong coronary vasodilating effect. It was then discovered that the “dextro” form of this molecule possessed the vasodilating activity. Since there are two basic types of calcium channels, slow and fast, it was shown that diltiazem blocks the slow channel and delays their recovery, thus making it a good antiarrhythmic drug. (Sneader, Walter, Drug Discovery, A History, 2015, Wiley)
Anyway, I found it interesting that a major cardiovascular drug was discovered while searching for psychotropic drugs. Go figure!
WG
What do you think?