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Uploaded byMahatma Gandhi Medical College & Hospital
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Angiotensin receptor blockers

This document discusses angiotensin receptor blockers (ARBs) which are used to treat hypertension and other cardiovascular conditions. It notes that ARBs work by competitively blocking the angiotensin receptor type 1, leading to vasodilation and other effects. Some examples of individual ARB drugs are provided like losartan, candesartan, and valsartan. The document compares ARBs to ACE inhibitors, noting that ARBs do not cause cough like ACE inhibitors. It concludes by discussing the theoretical rationale and benefits of combining ARBs with ACE inhibitors to more completely suppress the renin-angiotensin system.

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ANGIOTENSIN RECEPTOR BLOCKERS [ARBS] DR PADMAVATHI S ASSOCIATE PROFESSOR - DEPT OF PHARMACOLOGY
ANGIOTENSIN ANTAGONISTS
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
COMPETITIVE blockers
ARBS  SARTANS  LO SARTAN  CANDESARTAN  IRBESARTAN  VALSARTAN  OLMESARTAN  TELMISARTAN
MAJOR ADVERSE EFFECT DUE TO TREATMENT WITH ACE INHIBITORS NOT SEEN WITH ARBS ?
ARBS VS ACE INHIBITORS  DO NOT INTERFERE WITH DEGRADATION OF BRADYKININ – COUGH IS RARE  COMPLETE INHIBITION OF AT1 RECEPTOR ACTIVATION  INDIRECT AT2 ACTIVATION
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
ADVERSE EFFECTS HYPOTENSION HYPERKALEMIA TERATOGENECITY
USES  HYPERTENSION  CONGESTIVE HEART FAILURE  MYOCARDIAL INFARCTION  DIABETIC NEPHROPATHY
PREVENTS REMODELING
Bilateral
CAN WE COMBINE ARBS WITH ACE INHIBITORS?
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
DIRECT RENIN INHIBITOR ALISKIREN