Angiotensin receptor blockers

ANGIOTENSIN RECEPTOR BLOCKERS [ARBS]

DR PADMAVATHI SASSOCIATE PROFESSOR - DEPT OF PHARMACOLOGY

ANGIOTENSIN ANTAGONISTS

ANGIOTENSIN RECEPTORSAT1

VASCULAR S. M, MYOCARDIUM GPCR

VASOCONSTRICTIONCELL GROWTH IN HEART & ARTERIESSECRETION OF ALDOSTERONEPERIPHERAL SYM. ACTIVITY INCREASED

AT2 FOETUS, ADRENAL MEDULLA –

ADULTS GPCR

VASODILATATIONANTI-PROLIFERATIVEAPOPTOSIS

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 ADJUSTMENTPRODRUG

ADVERSE EFFECTS

HYPOTENSION

HYPERKALEMIA

TERATOGENECITY

USES

HYPERTENSIONCONGESTIVE HEART FAILUREMYOCARDIAL INFARCTIONDIABETIC NEPHROPATHY

PREVENTS REMODELING

CONTRAINDICATI

ONBilateral

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