Angiotensin receptor blockers
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Transcript of 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