Alpha blockers
In pharmacology , alpha blockers are drugs which, as antagonists at α 1 - and α 2 - adrenoceptors, neutralize the effects of adrenaline and noradrenaline . They are used therapeutically to lower high blood pressure (α 1 -adrenoceptor antagonists), to treat benign prostatic hyperplasia (α 1 -adrenoceptor antagonists) and to treat sexual dysfunctions (α 2 -adrenoceptor antagonists).
Alpha blockers include:
Alpha blockers, beta blockers and antisympathotonics are grouped under the name sympatholytics .
The antidepressants mianserin and mirtazapine are also alpha blockers and are known as NaSSA . They block presynaptic α 2 -receptors and thus inhibit the negative feedback via which noradrenaline normally inhibits its own release, making it more effective.
history
In 1818, Claviceps purpurea was first used by Jean Baptiste Desgranges (1751-1831) for the treatment of gynecological diseases. 1831 isolated August Wiggers ergotine (see. Also Julius Denzels ergotine and Rudolf Koberts Cornutin ) as the first alkaloid having an α-receptor blocking effect of ergot. Dale discovered the effect in 1906. The first pure alkaloid ( ergotamine ) was isolated by Arthur Stoll in 1918 . Together with Albert Hofmann , he also succeeded in developing the more water-soluble alkaloids of the ergometrine group, which have a direct effect on the smooth muscles.
Tolazoline was first presented by Adolf von Sonn (1882–1945) and finally described pharmacologically in 1940 by H. Schnetz. J. Scholz recognized the potential of the imidazoline derivatives and then synthesized phentolamine in 1949 , which Rolf Meier (1897–1966) investigated. In the early 1970s, the Searle company discovered the first selective α 1 blocker, prazosin (Minipress®). From this, further quinazoline derivatives were synthesized and brought to the German market, e.g. B. Doxazin (Cardular®) and Terazosin (Heitrin®). Since 1995, α-blockers (terazosin and alfuzosin ) have also been used to treat benign prostatic hyperplasia .
Web links
Individual evidence
- ↑ E. Graefe: The ergot and the new Kobert'schen ergot preparations. In: Centralblatt für Gynäkologie. Volume 10, No. 33, August 14, 1886, pp. 529-532.
- ^ Wolf-Dieter Müller-Jahncke , Christoph Friedrich , Ulrich Meyer: Medicinal history . 2., revised. and exp. Ed. Wiss. Verl.-Ges, Stuttgart 2005, ISBN 978-3-8047-2113-5 , pp. 170 f .
