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Peripheral vasadilators (Summary) Assoc. Prof. Iv. Lambev E-mail: itlambev@mail.bgitlambev@mail.bg
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I. Alpha (Alfa)-blockers Non-selective alpha-blockers (used in peripheral vascular disease): a) Ergot-alkaloids (from Secale cornutum) and their derivatives: Ergotamine (with ISA) Ergotoxine, Dihydroergocristine, Dihydroergotoxine, Dihydroergotamine b) Synthetic drugs Nicergolin (used in peripheral vascular spasms and cerebral vascular disease) Phentolamine (used in hypertensive emergencies)
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Blockade of postsynaptic 1 -receptors lowers blood pressure by: Lowering tone in arteriolar resistance vessels. Dilating venous capacitance vessels, which reduces venous return and cardiac output. Selective 1 -adrenoceptor antagonists spare the presynaptic 2 -adrenoceptors and do not produce reflex tachycardia. Postsynaptic 1 -blockers
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Postsynaptic 1 -blockers Doxazosin Prazosin
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Prazosin – indications: - Arterial hypertension - Congestive chronic heart failure Potentially beneficial effect: an increase in HDL and a reduction in triglycerides. Adverse reactions (ARs) Postural hypotension due to venous pooling (this can be troublesome after the first dose) Lethargy
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Alfuzosin (Xatral SR ® ), Doxazosin, Tamsulosin (Omnic ® ) Selective postsynaptic alpha- 1А -blockers: block alpha- 1А -receptors into the smooth muscles of the prostate gland, and the prostatic part of the urethra. Indication: hyperplasia of prostate gland
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ATP cAMP 3’,5’-AMP AC PDE () () (+) PKAEffects II. Phosphodiesterase inhibitors Pentoxifylline Drotaverine, Papaverine Sildenafil, Tadalafil, Vardenafil
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a) Methylxanthines Pentoxifylline: in cerebrovascular disease and peripheral vascular disease Poppy Nonselective inhibitors of PDE Pentoxifylline blocks PDE and TGFβ1- receptors. Acting through TGFβ1 inhibition in dose 400 mg/24 h it is also reported to be effective in Peyronie's disease (induratio penis plastica).
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ANGIOGENESIS PDGF TGF- TNF - (+) ()() VEGF (+)
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b) Papaverine and their analogues (spasmolytics) - Drotaverine (No-Spa ® ) - Papaverine (alkaloid, isolated from Poppy ) Poppy
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Selective inhibitors of PDE5 (used to treat erectile dysfunction) Sildenafil (Viagra ® ) Tadalafil (Cialis ® ) Vardenafil (Levitra ® ) PDE3 (1/4000) PDE6 (1/10)
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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.
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Prostavasin ® Caverject ® Alprostadil is a prodrug, which is transformed in the organism to PGE 1. It has a vasodilating effect in the treatment of trophic ulcers and erectile dysfunction. Alprostadil is injected intracavernously in erectile dysfunction.
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21 No comments
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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
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Ginkgo biloba
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VI. CEREBRAL VASCULAR DILATORS Calcium antagonist (used in cerebral vascular disease, ischemic cerebral stroke, hearing disorders)
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Combined preparations: Phezam (cinnarizine/piracetam) Methylxantines (PDE inhibitors): Pentoxyfilline Phytopreparations – NO donors: Extractum Ginkgo bilobae Other preparations: Naftidrofuryl, Vinpocetine
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Vinpocetine is an ethylester of apovincaminic acid, 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.
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