ANTIHYPERTENSIVE

ANTIHYPERTENSIVE

1. CHEMISTR Y OF AN T IHYPE R T E N S I VE A G EN T S Presentation by Abhishek Ghara I M. Pharm Dept. Pharmaceutical Chemistry

2. Hy p er t ens i on Also known as h i gh b l o o d p r e s su r e . It i s a diso r der t o whic h b o th e n vi r o nmenta l and gen e tic f ac t o rs contribu t e. Structural narrowing of arteries.

3. C l ass i f i ca t i o n o f B l o o d P ress u re Ca t e g o ry S y st e m i c B P ( m m H g ) D i a s t o li c B P (mm Hg ) No rm a l < 1 20 < 8 H y p e rt e n s i o n S t a g e 1 14 - 15 9 9 - 9 9 S t a g e 2 16 - 16 9 1 - 1 9 S t a g e 3 18 - 20 9 1 1 - 1 1 9 S t a g e 4 >2 1 > 1 2

4. Classification of antihypertensive drug 1) Sympat h o ly t ic drugs Centrally acting antia d renergic agents. A drenergi c neu r o n blo c king agents. A lph a adrenergi c blo c k e r s. B e t a adrenergi c blo c k e r s. Alpha-b e ta adrenergi c blo c k e r s. 2) V asodi la t o r s Nitric o xide release r s. P ota s sium c h annel opene r s. C a lcium c h annel b lo c k e r s. 3) Diur e t ics Thiazide s an d congene r s. Loo p diur e tics. P o tassium-sparing diur e tics 4) Angio t ensin inhibi t o r s and antagonist s . Angi o t ensi n Co n v e r ting Enzyme ( A CE) inhibi t o r s. Angi o t ensi n recep t or antagonists.

5. Sympatholytic drugs The mechanism of action of these drug is caused by stimulation of α 2-adrenoreceptors in the inhibitory structure of the brain. Interaction of these drug with α 2-adrenergic receptors is expressed in the suppression of vasomotor centre neurons of the medulla and reduction of hypothalamus activity, which leads to a decline in sympathetic impulses to the vessels and the heart. In the result cardiac output and heart rate are moderately reduced and arterial pressure is reduced.

6. Synthesis of Clonidine

7. Vasodilators

8. Synthesis of diazoxide

9. Diuretics

10. Synthesis of chlorothiazide

11. Angiotensin inhibitors

12. Synthesis of Cpatopril

13. SAR of Captopril

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