Medical University of Sofia Faculty of M Department

Medical University of Sofia, Faculty of M Department of Pharmacology and Toxico Peripheral vasadilators (Summary) Assoc. Prof. Iv. Lambev E-mail: itlambev@mail. bg

I. Non-selective alpha-blockers (used in peripheral vascular disease): Ergot-alkaloids (from Secale cornutum) and their derivatives: Ergotamine (with ISA) Ergotoxine, Dihydroergocristine, Dihydroergotoxine, Dihydroergotamine Synthetic drugs Nicergolin (used in peripheral vascular spasms and cerebral vascular

• Pentoxifylline II. Phosphodiesterase • Drotaverine, Papaverine inhibitors • Sildenafil, Tadalafil, Varden (-) AT P AC c. AMP PDE 3’, 5’-AMP (+) PKA Effects

Nonselective inhibitors of PDE a) Methylxanthines Pentoxifylline (in cerebrovascular disease, peripheral vascular disease) b) Papaverine and their analogues (spasmolytics) Drotaverine (No-Spa®) Papaverine (alkaloid, isolated from Poppy) Poppy

v Selective inhibitors of PDE 5 (used to treat erectile dysfunc PDE 3 (1/4000) PDE 6 (1/10) • Sildenafil (Viagra®) • Tadalafil (Cialis®) ® • Vardenafil (Levitra )

III. Prostaglandine analogues (adenylate cyclase activat Prostacycline (PGI 2) has periphera vasodilating and coronary dilating effects. It also inhibits thrombocyte aggregation. Iloprost (Ilomedin ) is its PGI 2 analogue, used i. v. in oblitering thromboangitis and limb ischemia.

Alprostadil is a prodrug, which is transformed in organism to PGE 1. It is has vasodilating effect in the treatmen of trophic ulcers and erectile dysfuncti Alprostadil is injected intracavernously in erectile dysfunction. • Prostavasin® • Caverject®

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IV. PHYTOPREPARATIONS Extr. Ginkgo bilobae (Tanakan®) – NO donor, used in peripheral vascular disease, cerebrovascular disease and atherosclerotic hearing disorders V. 5 -HT 2 -RECEPTOR BLOCKERS Naftidrofuryl – used in peripheral vascular disease and cerebrovascular disease

VI. CEREBRAL VASCULAR DILATO u Calcium antagonist (used in in cerebral disease, ischemic cerebral stroke, hearing d

Combine preparations: Phezam (cinnarizine/piracetam) w Methylxantines (PDE inhibitors): Pentoxyfilline Phytopreparations – NO donors: Extractum Ginkgo bilobae Other preparations: Naftidrofuryl, Vinpocetine

Vinpocetine is ethylester of apovincaminic acids, extracted from Vinca minor plant (Lesser periwinkle). It increases brain blood flow and inhibits thrombocyte aggregation. Vinpocetine has antihypoxic and neuroprotective effect exerted by NMDA-glutamate receptor blockade. It increases glucose and oxygen supply and utilization in the brain, prevents oxidative stress.