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Anti hypertensive drugs
Classification, mechanism of action and adverse effects
What is hypertension
 Also called high blood pressure
 It is condition in which the force of blood against the artery wall
is too high.
 Hypertension is define as the blood pressure above 140/90
through risk appear to increase even above 80/120
 Arteriosclerosis may contribute to HBP but is not only the factor
 It is classified in two class i.e. primary and secondary
Non pharmacological therapy for the
treatment of hypertension
 140/90 blood pressure can be easily cure by treating
patient with weight loss
 By restriction of sodium intake
 Increasing aerobic exercise
 Moderating alcohol consumption
Anti hypertensive drugs
 Arterial pressure = cardiac output * peripheral vascular
resistance
 antihypertensive drugs are those drugs that decrease HBP
by either decreasing cardiac output or peripheral
resistance and both
Classification of anti hypertensive drugs
 Diuretic
 Angiotensinogen converting enzyme inhibitor (ACE inhibitor )
 Angiotensin blocker (AT1 BLOCKER )
 Calcium channel blocker
 Beta blocker
 Alpha blocker
 Central sympatholytic
 Vasodilator
Diuretics
 Thiazides and related agonist = hydrochlorothiazide,
chlorothiazide, indapamides
 High ceiling / loop inhibitor = furosemide , torsemide
 K+ sparing = amiloride spironolactone
Moa
 Diuretic decrease the total peripheral resistance.

 Diuretics drugs decrease extracellular vilume by intracting
with
 thiazide sensitive Nacl co- transpoter expressed Na+
 excreation in the urine blood pressure fall
Thiazide also promotes vasodilation in isolated arteies
High ceiling diuretics
 Furosemide is a protype drug
 Fall in bp entirely depend upon reduction in plasma
volume and c.o.
 T.p.r. and vascular response are not reduced
 K+ sparing diuretics decrease bp slightly but they are
used only in combination with thiazide diuretics to
prevent k+ loose
Diuretics
Positive
 No fluid retension and
tolerance
 No or less postural
hypotension
 No side affect on cns
 Effective for systolic
hypertension
 Low cost
 Flat drc
Negatives
 Hypokalemia
 Erectile dysfunction
 Carbs intolerance due to
inhibtion of insulin release
dyslipidemia
 Hyperureceemia ewdfscxz
ACE inhibitor
 Angiotensinogen
Renin
Angiotensinogen 1
Kininase
Angiotensinogen 2
AT2 receptor AT1 receptor
Moa
 Ace inhibitor
 Decrease tpr
 Dilation of arterioles and compliance of longer
artery is increase
 Both systolic and diastolic bp fall
Angiotensinogen receptor blocker
 At1 and AT2 are angiotensinogen receptor
present at a specific site
 ARB are the G protein coupled receptor
 Lorsartam is an AT1 antagonist while PD
123177 is a AT antagonist
MOA
 Losartam block AT receptor
Output of SNS decrease
Increase vasodilation of vaculasr smooth muscle
moa
 Losartan not inhibit ACE therefore more angiotensinogen
is produce
 Which act on AT2 receptor
 But Losartan block overpert action of angiotensinogen 2
on At2 receptor ( such as vasoconstriction central and
peripheral sympathetic stimulation etc.)
 Ccombination with ACE inhibitor will result in blockage of
both AT1 and AT2 receptor
Calcium channel blocker
They decrease the peripheral resistance without
compromising c.o.
Calcium channel blocker have –( chonotropic and ionotropic )
action on heart
They decrease sinus rate and rate of conduction which lead
to fall in bp
Beta adrenergic blocker
 Selective B1 antagonist : metroprolol , atenolol
 Non Selective beta blocker : propranolol
Non selective beta blocker
are not widely used alone
because of their
contraindication to cadiac,
pulmonary and peripheral
vascular disease
Beta blocker
 these drug act on b receptor
Decrease the heart rate and force of
construction
Cardiac output decrease
Alpha adrenergic blocker
 Selective alpha 1 adrenergic blocker : prazosin
 Other alpha blocker are terazosin doxazosin
Prazosin is moderately potent
antihypertensive drug with many
desirable features.
But not the first line of drug because
tolerance and fluid retention
developed with monotherapy
MOA
 They dilate both resistance and capacitance of
vessel
 Reduction in TPR
 Cardiac output decrease

 Blood pressure fall
Alpha blocker also have cardio
stimulation renin release action in long
term therapy therefore, fall in BP is
compensate by cardiac stimulation
Postural hypotension, headache,
drowsiness, dry mouth are some
of the adverse effect of Alpha
blocker
Central sympatholytic drugs
CLONIDINE, METHYL DOPA
CLONIDINE
It is an imidazoline derivative having a complex action
It is partial agonist with high affinity and internsic activity
toward ALPHA 2a subtype receptor
They decrease sympathetic stimulation out flow BP fall
Bradicardia
They also decrease NA release from peripheral adrenergic
neuron
Methyl dopa
 Methyl dopa is a alpha-methyl analoguos of
dopamine precursor

 IT act on Alpha 2 receptor to decrease the total
peripheral resistance more then heart rate and
cardiac output
 Larg dose of drug inhibite the enzyme dopa
decarboxylase in brain and periphery that lead to
decrease NA synthesis and formed false methyl
NA
VASODILATOR
ARTERIOLAR : Hydralazine, minoxidil, diazoxide
AND VENOUS ARTERIOLOAR : Sodium nitropusside
Arteriloar
Decrease in TPR
Great reduction in diastolic then systolic BP
Tolerance to hypertension developed uless diuretics
and Beta blocker given with drugs
Arteriolar + venous ( sodium
nitropuside)
 It relax both resistance and capacitance of vessel
 Reduction in TPR
 Cardiac output also decrease by decrease in venous return
It is used in patein with cardiac disease
ANIKET SONKER
DATED 29.08.2109

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Anti hypertensive drugs | diuretics

  • 1. Anti hypertensive drugs Classification, mechanism of action and adverse effects
  • 2. What is hypertension  Also called high blood pressure  It is condition in which the force of blood against the artery wall is too high.  Hypertension is define as the blood pressure above 140/90 through risk appear to increase even above 80/120  Arteriosclerosis may contribute to HBP but is not only the factor  It is classified in two class i.e. primary and secondary
  • 3. Non pharmacological therapy for the treatment of hypertension  140/90 blood pressure can be easily cure by treating patient with weight loss  By restriction of sodium intake  Increasing aerobic exercise  Moderating alcohol consumption
  • 4. Anti hypertensive drugs  Arterial pressure = cardiac output * peripheral vascular resistance  antihypertensive drugs are those drugs that decrease HBP by either decreasing cardiac output or peripheral resistance and both
  • 5. Classification of anti hypertensive drugs  Diuretic  Angiotensinogen converting enzyme inhibitor (ACE inhibitor )  Angiotensin blocker (AT1 BLOCKER )  Calcium channel blocker  Beta blocker  Alpha blocker  Central sympatholytic  Vasodilator
  • 6. Diuretics  Thiazides and related agonist = hydrochlorothiazide, chlorothiazide, indapamides  High ceiling / loop inhibitor = furosemide , torsemide  K+ sparing = amiloride spironolactone
  • 7. Moa  Diuretic decrease the total peripheral resistance.   Diuretics drugs decrease extracellular vilume by intracting with  thiazide sensitive Nacl co- transpoter expressed Na+  excreation in the urine blood pressure fall Thiazide also promotes vasodilation in isolated arteies
  • 8. High ceiling diuretics  Furosemide is a protype drug  Fall in bp entirely depend upon reduction in plasma volume and c.o.  T.p.r. and vascular response are not reduced  K+ sparing diuretics decrease bp slightly but they are used only in combination with thiazide diuretics to prevent k+ loose
  • 9. Diuretics Positive  No fluid retension and tolerance  No or less postural hypotension  No side affect on cns  Effective for systolic hypertension  Low cost  Flat drc Negatives  Hypokalemia  Erectile dysfunction  Carbs intolerance due to inhibtion of insulin release dyslipidemia  Hyperureceemia ewdfscxz
  • 10. ACE inhibitor  Angiotensinogen Renin Angiotensinogen 1 Kininase Angiotensinogen 2 AT2 receptor AT1 receptor
  • 11. Moa  Ace inhibitor  Decrease tpr  Dilation of arterioles and compliance of longer artery is increase  Both systolic and diastolic bp fall
  • 12. Angiotensinogen receptor blocker  At1 and AT2 are angiotensinogen receptor present at a specific site  ARB are the G protein coupled receptor  Lorsartam is an AT1 antagonist while PD 123177 is a AT antagonist
  • 13. MOA  Losartam block AT receptor Output of SNS decrease Increase vasodilation of vaculasr smooth muscle
  • 14. moa  Losartan not inhibit ACE therefore more angiotensinogen is produce  Which act on AT2 receptor  But Losartan block overpert action of angiotensinogen 2 on At2 receptor ( such as vasoconstriction central and peripheral sympathetic stimulation etc.)  Ccombination with ACE inhibitor will result in blockage of both AT1 and AT2 receptor
  • 15. Calcium channel blocker They decrease the peripheral resistance without compromising c.o. Calcium channel blocker have –( chonotropic and ionotropic ) action on heart They decrease sinus rate and rate of conduction which lead to fall in bp
  • 16. Beta adrenergic blocker  Selective B1 antagonist : metroprolol , atenolol  Non Selective beta blocker : propranolol Non selective beta blocker are not widely used alone because of their contraindication to cadiac, pulmonary and peripheral vascular disease
  • 17. Beta blocker  these drug act on b receptor Decrease the heart rate and force of construction Cardiac output decrease
  • 18. Alpha adrenergic blocker  Selective alpha 1 adrenergic blocker : prazosin  Other alpha blocker are terazosin doxazosin Prazosin is moderately potent antihypertensive drug with many desirable features. But not the first line of drug because tolerance and fluid retention developed with monotherapy
  • 19. MOA  They dilate both resistance and capacitance of vessel  Reduction in TPR  Cardiac output decrease   Blood pressure fall
  • 20. Alpha blocker also have cardio stimulation renin release action in long term therapy therefore, fall in BP is compensate by cardiac stimulation Postural hypotension, headache, drowsiness, dry mouth are some of the adverse effect of Alpha blocker
  • 22. CLONIDINE It is an imidazoline derivative having a complex action It is partial agonist with high affinity and internsic activity toward ALPHA 2a subtype receptor They decrease sympathetic stimulation out flow BP fall Bradicardia They also decrease NA release from peripheral adrenergic neuron
  • 23. Methyl dopa  Methyl dopa is a alpha-methyl analoguos of dopamine precursor   IT act on Alpha 2 receptor to decrease the total peripheral resistance more then heart rate and cardiac output  Larg dose of drug inhibite the enzyme dopa decarboxylase in brain and periphery that lead to decrease NA synthesis and formed false methyl NA
  • 24. VASODILATOR ARTERIOLAR : Hydralazine, minoxidil, diazoxide AND VENOUS ARTERIOLOAR : Sodium nitropusside
  • 25. Arteriloar Decrease in TPR Great reduction in diastolic then systolic BP Tolerance to hypertension developed uless diuretics and Beta blocker given with drugs
  • 26. Arteriolar + venous ( sodium nitropuside)  It relax both resistance and capacitance of vessel  Reduction in TPR  Cardiac output also decrease by decrease in venous return It is used in patein with cardiac disease