Phosphodiesterase-Inhibitors by Aseem

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Dr. Aseem Sharma

Health & Medicine Technology

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

Subtypes
Non-Selective
CAFFEINE/THEOBROMINE/METHYLXANTHINES
AMINOPHYLLINE / THEOPHYLLINE (BDs)
PENTOXYFILLINE (Circulation enhancer DM / PVD)
PDE-1 Inhibitors

VINPOCETINE (Nootropic)

Subtypes
PDE-2 I
Erythro Hydroxy Nonyl Adenine (EHNA)
(Investigtive for CCF)
PDE-3 I
MILRINONE (Inotrope – CCF)
CILOSTAZOL (Arterial VD – Intermittent
Claudication)

Subtypes
PDE-4 I
MESEMBRINE (SRI)
ROFLUMILAST (COPD Exacerbations – FDA)
DROTAVERINE (Anti-spasmodic / Tocolytic)

Anti-inflamm / Anti-depressant

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

Subtypes
PDE-10 I
PAPAVERINE (Papaver Somniferum)
Gastro-Intestinal Vasodilator
ED (Intracavernosal)
Coronary Vasodilator

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Phosphodiesterase-Inhibitors by Aseem

1. PHOSPHODIESTERASE INHIBITORS

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. Subtypes Non-Selective CAFFEINE/THEOBROMINE/METHYLXANTHINES AMINOPHYLLINE / THEOPHYLLINE (BDs) PENTOXYFILLINE (Circulation enhancer DM / PVD) PDE-1 Inhibitors VINPOCETINE (Nootropic)

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. Subtypes PDE-4 I MESEMBRINE (SRI) ROFLUMILAST (COPD Exacerbations – FDA) DROTAVERINE (Anti-spasmodic / Tocolytic) Anti-inflamm / Anti-depressant

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. Subtypes PDE-10 I PAPAVERINE (Papaver Somniferum) Gastro-Intestinal Vasodilator ED (Intracavernosal) Coronary Vasodilator

8. THANK YOU

Phosphodiesterase-Inhibitors by Aseem

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