Peripheral vasadilators

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Medical University of Sofia, Faculty of
Medicine Department of Pharmacology and Toxicology
Peripheral vasadilators (Summary)
Assoc. Prof.Iv. Lambev E-mail itlambev_at_mail.bg
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• 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)

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• Pentoxifylline
• Drotaverine, Papaverine
• Sildenafil, Tadalafil, Vardenafil

II. Phosphodiesterase inhibitors
(-)
AC
PDE
cAMP
ATP
3,5-AMP
()
PKA
Effects
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? 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
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• Selective inhibitors of PDE5
• (used to treat erectile dysfunction)

PDE6 (1/10)
PDE3 (1/4000)

• Sildenafil (Viagra)
• Tadalafil (Cialis)
• Vardenafil (Levitra)

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III. Prostaglandine analogues (adenylate
cyclase activators)
Prostacycline (PGI2) has peripheral vasodilating
and coronary dilating effects. It also inhibits
thrombocyte aggregation. Iloprost (Ilomedin?) is
its PGI2- analogue, used i.v. in oblitering
thromboangitis and limb ischemia.
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Alprostadil is a prodrug, which is transformed
in organism to PGE1. It is has vasodilating
effect in the treatment of trophic ulcers and
erectile dysfunction. 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-HT2-RECEPTOR BLOCKERS
Naftidrofuryl used in peripheral vascular
disease and cerebrovascular disease
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• VI. CEREBRAL VASCULAR DILATORS
• Calcium antagonist (used in in cerebral vascular
• disease, ischemic cerebral stroke, hearing
  disorders)

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

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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.