Peripheral vasadilators (Summary) Assoc. Prof. Iv. Lambev Medical University of Sofia, Faculty of Medicine Department.

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Peripheral vasadilators (Summary) Assoc. Prof. Iv. Lambev Medical University of Sofia, Faculty of Medicine Department of Pharmacology and Toxicology

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 disease) Phentolamine (used in hypertensive emergencies)

ATP cAMP 3’,5’-AMP AC PDE () () (+) PKAEffects II. Phosphodiesterase inhibitors Pentoxifylline Drotaverine, Papaverine Sildenafil, Tadalafil, Vardenafil

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

 Selective inhibitors of PDE5 (used to treat erectile dysfunction) Sildenafil (Viagra ® ) Tadalafil (Cialis ® ) Vardenafil (Levitra ® ) PDE3 (1/4000) PDE6 (1/10)

III. Prostaglandine analogues (adenylate cyclase activators) Prostacycline (PGI 2 ) has peripheral 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 treatment of trophic ulcers and erectile dysfunction. Alprostadil is injected intracavernously in erectile dysfunction. Prostavasin ® Caverject ®

21 No comments

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 DILATORS  Calcium antagonist (used in in cerebral vascular disease, ischemic cerebral stroke, hearing disorders)

 Combine preparations: Phezam (cinnarizine/piracetam)  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.