Phosphodiesterase-Inhibitors by Aseem

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Phosphodiesterase-Inhibitors by Aseem

  1. 1. PHOSPHODIESTERASE INHIBITORS
  2. 2. Introduction • Isolated by UZONOV & WEISS in 1972 from Rat Brain • Therapeutic Action documented in 1977 • Inhibits Platelet Aggregation by promoting hydrolysis and degradation of cAMP and / or cGMP and release of Protein Kinase A
  3. 3. Subtypes Non-Selective CAFFEINE/THEOBROMINE/METHYLXANTHINES AMINOPHYLLINE / THEOPHYLLINE (BDs) PENTOXYFILLINE (Circulation enhancer DM / PVD) PDE-1 Inhibitors VINPOCETINE (Nootropic)
  4. 4. Subtypes PDE-2 I Erythro Hydroxy Nonyl Adenine (EHNA) (Investigtive for CCF) PDE-3 I MILRINONE (Inotrope – CCF) CILOSTAZOL (Arterial VD – Intermittent Claudication)
  5. 5. Subtypes PDE-4 I MESEMBRINE (SRI) ROFLUMILAST (COPD Exacerbations – FDA) DROTAVERINE (Anti-spasmodic / Tocolytic) Anti-inflamm / Anti-depressant
  6. 6. Subtypes PDE-5 I (ED – degradation of cGMP in CC) SILDENAFIL (VIAGRA) TADALAFIL (CIALIS) VARDENAFIL (LEVITRA)UDENAFIL AVANAFIL PAH BPH / PAH t1/2 PE tmax
  7. 7. Subtypes PDE-10 I PAPAVERINE (Papaver Somniferum) Gastro-Intestinal Vasodilator ED (Intracavernosal) Coronary Vasodilator
  8. 8. THANK YOU

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