Angiotensin receptor blockers

Angiotensin receptor blockers

1. A ngiotensin r eceptor b lockers [ ARB s ] DR PADMAVATHI S ASSOCIATE PROFESSOR - DEPT OF PHARMACOLOGY

2. Angiotensin antagonists

3. Angiotensin receptors AT1 VASCULAR S. M, MYOCARDIUM GPCR VASOCONSTRICTION CELL GROWTH IN HEART & ARTERIES SECRETION OF ALDOSTERONE PERIPHERAL SYM. ACTIVITY INCREASED AT2 FOETUS, ADRENAL MEDULLA – ADULTS GPCR VASODILATATION ANTI-PROLIFERATIVE APOPTOSIS

4. COMPETITIVE blockers

5. ARB s  saRTANS LO SARTAN CANDE SARTAN IRBE SARTAN VAL SARTAN OLME SARTAN TELMI SARTAN

6. MAJOR ADVERSE EFFECT DUE TO TREATMENT WITH ACE INHIBITORS NOT SEEN WITH ARBS ?

7. arb S VS Ace INHIBITORS DO NOT INTERFERE WITH DEGRADATION OF BRADYKININ – COUGH IS RARE COMPLETE INHIBITION OF AT1 RECEPTOR ACTIVATION INDIRECT AT2 ACTIVATION

8. Individual drugs LOSARTAN – HIGH FIRST PASS METABOLISM, NO DOSE ADJUSTMENT – RENAL / LIVER DISEASE CANDESARTAN – NON COMPETITIVE ANTAGONISM VALSARTAN – ABSORPTION AFFECTED BY FOOD OLMESARTAN – NO DOSE ADJUSTMENT PRODRUG

9. ADVERSE EFFECTS HYPOTENSION HYPERKALEMIA TERATOGENECITY

10. USES HYPERTENSION CONGESTIVE HEART FAILURE MYOCARDIAL INFARCTION DIABETIC NEPHROPATHY

11. PREVENTS REMODELING

12. CONTRAINDICATION Bilateral

13. CAN WE COMBINE ARB S WITH ACE INHIBITORS ?

14. THEORETICAL REASONS MORE COMPLETE SUPPRESSION OF RAS ANGIOTENSIN II GENERATED BY ALTERNATE PATHWAYS BLOCKED BY ARBS ACE INHIBITORS – BRADYKININ RELATED VASODILATATION ARBS – COMPENSATORY RISE IN ANG II  checked by ACEI

15. Direct Renin inhibitor ALISKIREN