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Hypertension

Anti-Hypertensive drugs
Hypertension

Anti-Hypertensive drugs
Presented by
A. Gowtham Sashtha 1st M.pharm
Department of pharmacology
K.M College of pharmacy
Madurai - 625107.
Introduction :
It is most common disease of CVS.
Definition : Persistent and sustained increased BP has
damaging effects on heart, brain, kidney, eye, lungs.
Types :
1) Primary / essential hypertension
No specific causes 95% cases
2) Secondary hypertension
Due to specific disease or drug 5% cases
Other : Genetic factors, psychological stress, environmental
and dietary factors as contributing to the development of
hypertension
Classification of Hypertension Based on Blood pressure
Normal Regulations of Blood pressure:
BP according to the equation - BP = CO × PVR
Arterial blood pressure is directly proportional to the
product of the blood flow (cardiac output) and the resistance
to passage of blood through arterioles (peripheral vascular
resistance)
Blood pressure maintained by
Arterioles, postcapillary venules and heart.
Kidney and Baroreflexes
Regulation of blood pressure:
Pulmonary Hypertension :
➜Pulmonary hypertension is increasing blood pressure in
pulmonary circulation (either arteries or in both arteries and
veins)
➜Normal pressure is 14-18mmHg at rest.
➜20-25mmHg at exercise.
➜It can be measured by
pulmonary catheterization.
Treatment of pulmonary hypertension :
➜ Endothelin receptor antagonists.
eg: sitaxentan, ambrisentan, atrasentan
➜ Vasodilators.
➜ High-dose calcium channel blockers.
➜ Diuretics.
➜ Oxygen therapy.
Regulation of blood pressure in systemic circulation
and actions of antihypertensive drugs
Baroreceptor reflex control :
Control of smooth muscles in blood vessels
Control of
renin release,
formation and
action of
angiotensin II
Control of cardiac output
Anti - Hypertensive drugs
1) Diuretics:
-Thiazides: Hydrochlorothiazide, chlorthalidone, Indapamide
-Loop diuretics: Furosemide,Torsemide, Ethacrynic acid.
-K+ Sparing: Spironolactone, Amiloride.
2) ACE Inhibitors:
-Captopril, Enalapril, Lasinopril, prendopril,Ramipril,Fosinopril.
etc.
3) Angiotensin (AT1 receptor) blockers:
-Telmisartan, Losartan, Camdesartan, Valsartan,Irbesartan.
4) Direct renin inhibitors:
-Aliskiren, Enalkiren
5) Ca++ channel blockers:
-Verapamil, Diltiazem, Nifedipine, Amlodipine, Felodipine,
Notrendipine, Lacidipine.......etc
6) Central sympatholytics:
-Clonidine, methyldopa
7) α Adrenergic blockers:
-Prazosin, Terazosin, Doxazosin, Phentolamine,
Phenoxybenzamine.
8) β Adrenergic blockers:
-Propranolol, Metaprolol, Atenolol.....etc
9) β+α Adrenergic blockers:
-Labetalol, Carvedilol.
10) Vasodilators:
-Arteriolar: Hydralazine, Minoxidil, Diazoxide.
-Arteriolar + Venous: Sodium nitroprusside.
11) Others:
-Adrenergic neurone blockers (Reserpine,Guanethidine,...etc)
-Ganglion blockers (Pentolinium...etc)
Physiology of Urine formation :
1) Diuretics :
- Thiazide diuretics :
This drugs are directly
acting on Distal convoluted
tubules cells.
Such as lower blood pressure
initially by the increasing sodium
and water excretion.
Mechanism of action :
ADR :
Overdose having.
→Hypokalemia.
→Hyponatremia
→Hypocalcaemia
→Hyperglycemia
→Hyperuricemia
-Loop diuretics:
➜Inhibition of epithelial
sodium transport at the late
distal and collecting ducts.
ADR:
➜hyponatremia,
hypokalemia, hypomagnesemia,
dehydration, hyperuricemia,
gout, dizziness, postural
hypotension, syncope
-K+ Sparing Diuretics:
➜potassium sparing
diuretics are competative that
either compete with
aldosterone(Spironolactone 
eplerenone), or
➜directly block the
epithelial sodium channel.
(Amiloride)
2) ACE Inhibitors :
➜The ACE inhibitors are recommended as first line treatment
of hypertension in patients with variety of compelling indication
included High coronary artery disease, diabetes, strok, heart
failure, congestive heart failure, chronic kidney disease.
MOA:
➜ACE Inhibitors decrease the angiotensin ll level and increase
the bradykinin levels.
Decrease angiotensin level causes decrease the vasoconstriction.
Increase bradykinin level causes enhanced vasodilation.
Adverse effects of ACE Inhibitors:
➜ Over dose having hypotension
➜ Hyperkalemia
➜ Cough
➜ Rashes, urticaria
➜ Angioedema
➜ Dysgeusia / parageusia
➜ Headache, dizziness, nausea.
➜ Acute renal failure.
Uses of ACE Inhibitors:
➜ Hypertension
➜ Congestive Heart Failure (CHF)
➜ Myocardial Infarction.
➜ Diabetic nephropathy.
➜ Nondiabetic nephropathy.
➜ Scleroderma Crisis.
3) Angiotensin Receptor Blockers(ARB):
➜ARBs do not be used as first line agent for the treatment of
hypertension, especially patients with diabetes, Heart Failure,
and chronic kidney disease.
➜Their pharmacologic effects of ARBs are similar to those of
ACE Inhibitors.
➜ARBs do not increase bradykinin levels.
4) Direct Renin Inhibitors:
➜A selective renin inhibitor, directly inhibit renin and acts as
renin angeotensin-aldosterone system.
➜Aliskiren should not be routinely combined with an ACE
inhibitor or ARBs.
ADR:
Diarrhea.
cough.
Angioedema.
Mechanism of action
5) α-Adrenergic blockers :
Phentolamine, Phenoxybenzamine is a α1-adrenergic blocking
agent.
Alpha blockers reduce the arterial pressure.
ADR :
Postural hypotension.
Sedation.
Tachycardia.
Miosis.
Nasal stuffness.
6) β - Adrenergic blockers :
➜β - Adrenergic blockers are mild anti hypertensive activitie.
➜30-40% β-adrenergic blockers are used.
➜Propranolol is the first β blocker showed effective in
hypertension and ischemic heart disease.
➜Propranolol has now been largely replaced by cardioselective
β blockers such as metoprolol, Atenolol.
Metaprolol  Atenolol.
➜It is the cardio selective drugs it directly inhibition of β1
adenoreceptors.
➜Sustained release of metaprolol is effective in reducing
mortality from heart failure and is particularly useful in
patients with hypertension and heart failure.
➜Atenolol is reported to be less effective than Metaprolol in
preventing the complications of hypertension.
Other beta blockers :
➜Nadolol and carteolol is non selective β blockers
ADR :
➜Bronchospasm,
➜Heart failure,
➜Bradycardia,
➜Heart block,
➜Neurological reactions include depression, fatigue,
7) Centrally acting Adrenergic drugs:
Clonidine :
➜It act as the α2 agonist to produce inhibition of sympathetic
vasomotor centers ➝ Decreasing sympathetic outflow ➝ leads
to reduce the total peripheral resistance ➝ decreased blood
pressure.
Methyldopa :
➜It is an α 2 agonist that converted into methylnorepinephrine
centrally decreasing the Adrenergic out flow.
➜It is mainly used for management of hypertension in
pregnancy.
Mechanism of action :
8) Vasodilators:
➜Hydralazine / Dihydralazine and minoxidil are not used for
primary drugs to treat hypertension
➜This vasodilators acting the relaxation of vascular smooth
muscles especially arteries and arteriolous, This result in
reduce the peripheral resistance .
➜Hydralazine is accepted medication for controlling blood
pressure in pregnancy induced hypertension.
9) Calcium Channel blockers:
➜Calcium channel blockers are another classes of first line anti
hypertensive drugs .
➜Cause smooth muscle relaxation by blocking the binding
calcium to its receptors, preventing muscle contraction.
Results in,
➝Decreased peripheral smooth muscle tone
➝Decreased systemic vascular resistance
➝Decreased blood pressure
ADR: Constipation. Dizziness. Fast heartbeat (palpitations)
Mechanism of action :
THANK YOU
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Hypertesion  Anti-…rtensive drugs.pdf
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Hypertesion & Anti-Hypertensive drugs

  • 1. Hypertension Anti-Hypertensive drugs Hypertension Anti-Hypertensive drugs Presented by A. Gowtham Sashtha 1st M.pharm Department of pharmacology K.M College of pharmacy Madurai - 625107.
  • 2. Introduction : It is most common disease of CVS. Definition : Persistent and sustained increased BP has damaging effects on heart, brain, kidney, eye, lungs. Types : 1) Primary / essential hypertension No specific causes 95% cases 2) Secondary hypertension Due to specific disease or drug 5% cases
  • 3. Other : Genetic factors, psychological stress, environmental and dietary factors as contributing to the development of hypertension Classification of Hypertension Based on Blood pressure
  • 4. Normal Regulations of Blood pressure: BP according to the equation - BP = CO × PVR Arterial blood pressure is directly proportional to the product of the blood flow (cardiac output) and the resistance to passage of blood through arterioles (peripheral vascular resistance) Blood pressure maintained by Arterioles, postcapillary venules and heart. Kidney and Baroreflexes
  • 6. Pulmonary Hypertension : ➜Pulmonary hypertension is increasing blood pressure in pulmonary circulation (either arteries or in both arteries and veins) ➜Normal pressure is 14-18mmHg at rest. ➜20-25mmHg at exercise. ➜It can be measured by pulmonary catheterization.
  • 7. Treatment of pulmonary hypertension : ➜ Endothelin receptor antagonists. eg: sitaxentan, ambrisentan, atrasentan ➜ Vasodilators. ➜ High-dose calcium channel blockers. ➜ Diuretics. ➜ Oxygen therapy.
  • 8. Regulation of blood pressure in systemic circulation and actions of antihypertensive drugs
  • 10. Control of smooth muscles in blood vessels
  • 11. Control of renin release, formation and action of angiotensin II
  • 13. Anti - Hypertensive drugs 1) Diuretics: -Thiazides: Hydrochlorothiazide, chlorthalidone, Indapamide -Loop diuretics: Furosemide,Torsemide, Ethacrynic acid. -K+ Sparing: Spironolactone, Amiloride. 2) ACE Inhibitors: -Captopril, Enalapril, Lasinopril, prendopril,Ramipril,Fosinopril. etc.
  • 14. 3) Angiotensin (AT1 receptor) blockers: -Telmisartan, Losartan, Camdesartan, Valsartan,Irbesartan. 4) Direct renin inhibitors: -Aliskiren, Enalkiren 5) Ca++ channel blockers: -Verapamil, Diltiazem, Nifedipine, Amlodipine, Felodipine, Notrendipine, Lacidipine.......etc 6) Central sympatholytics: -Clonidine, methyldopa
  • 15. 7) α Adrenergic blockers: -Prazosin, Terazosin, Doxazosin, Phentolamine, Phenoxybenzamine. 8) β Adrenergic blockers: -Propranolol, Metaprolol, Atenolol.....etc 9) β+α Adrenergic blockers: -Labetalol, Carvedilol.
  • 16. 10) Vasodilators: -Arteriolar: Hydralazine, Minoxidil, Diazoxide. -Arteriolar + Venous: Sodium nitroprusside. 11) Others: -Adrenergic neurone blockers (Reserpine,Guanethidine,...etc) -Ganglion blockers (Pentolinium...etc)
  • 17. Physiology of Urine formation :
  • 18. 1) Diuretics : - Thiazide diuretics : This drugs are directly acting on Distal convoluted tubules cells. Such as lower blood pressure initially by the increasing sodium and water excretion.
  • 19. Mechanism of action : ADR : Overdose having. →Hypokalemia. →Hyponatremia →Hypocalcaemia →Hyperglycemia →Hyperuricemia
  • 20. -Loop diuretics: ➜Inhibition of epithelial sodium transport at the late distal and collecting ducts. ADR: ➜hyponatremia, hypokalemia, hypomagnesemia, dehydration, hyperuricemia, gout, dizziness, postural hypotension, syncope
  • 21. -K+ Sparing Diuretics: ➜potassium sparing diuretics are competative that either compete with aldosterone(Spironolactone eplerenone), or ➜directly block the epithelial sodium channel. (Amiloride)
  • 22. 2) ACE Inhibitors : ➜The ACE inhibitors are recommended as first line treatment of hypertension in patients with variety of compelling indication included High coronary artery disease, diabetes, strok, heart failure, congestive heart failure, chronic kidney disease. MOA: ➜ACE Inhibitors decrease the angiotensin ll level and increase the bradykinin levels. Decrease angiotensin level causes decrease the vasoconstriction. Increase bradykinin level causes enhanced vasodilation.
  • 23. Adverse effects of ACE Inhibitors: ➜ Over dose having hypotension ➜ Hyperkalemia ➜ Cough ➜ Rashes, urticaria ➜ Angioedema ➜ Dysgeusia / parageusia ➜ Headache, dizziness, nausea. ➜ Acute renal failure.
  • 24. Uses of ACE Inhibitors: ➜ Hypertension ➜ Congestive Heart Failure (CHF) ➜ Myocardial Infarction. ➜ Diabetic nephropathy. ➜ Nondiabetic nephropathy. ➜ Scleroderma Crisis.
  • 25. 3) Angiotensin Receptor Blockers(ARB): ➜ARBs do not be used as first line agent for the treatment of hypertension, especially patients with diabetes, Heart Failure, and chronic kidney disease. ➜Their pharmacologic effects of ARBs are similar to those of ACE Inhibitors. ➜ARBs do not increase bradykinin levels.
  • 26. 4) Direct Renin Inhibitors: ➜A selective renin inhibitor, directly inhibit renin and acts as renin angeotensin-aldosterone system. ➜Aliskiren should not be routinely combined with an ACE inhibitor or ARBs. ADR: Diarrhea. cough. Angioedema.
  • 28. 5) α-Adrenergic blockers : Phentolamine, Phenoxybenzamine is a α1-adrenergic blocking agent. Alpha blockers reduce the arterial pressure. ADR : Postural hypotension. Sedation. Tachycardia. Miosis. Nasal stuffness.
  • 29. 6) β - Adrenergic blockers : ➜β - Adrenergic blockers are mild anti hypertensive activitie. ➜30-40% β-adrenergic blockers are used. ➜Propranolol is the first β blocker showed effective in hypertension and ischemic heart disease. ➜Propranolol has now been largely replaced by cardioselective β blockers such as metoprolol, Atenolol.
  • 30. Metaprolol Atenolol. ➜It is the cardio selective drugs it directly inhibition of β1 adenoreceptors. ➜Sustained release of metaprolol is effective in reducing mortality from heart failure and is particularly useful in patients with hypertension and heart failure. ➜Atenolol is reported to be less effective than Metaprolol in preventing the complications of hypertension. Other beta blockers : ➜Nadolol and carteolol is non selective β blockers
  • 31. ADR : ➜Bronchospasm, ➜Heart failure, ➜Bradycardia, ➜Heart block, ➜Neurological reactions include depression, fatigue,
  • 32. 7) Centrally acting Adrenergic drugs: Clonidine : ➜It act as the α2 agonist to produce inhibition of sympathetic vasomotor centers ➝ Decreasing sympathetic outflow ➝ leads to reduce the total peripheral resistance ➝ decreased blood pressure. Methyldopa : ➜It is an α 2 agonist that converted into methylnorepinephrine centrally decreasing the Adrenergic out flow. ➜It is mainly used for management of hypertension in pregnancy.
  • 34. 8) Vasodilators: ➜Hydralazine / Dihydralazine and minoxidil are not used for primary drugs to treat hypertension ➜This vasodilators acting the relaxation of vascular smooth muscles especially arteries and arteriolous, This result in reduce the peripheral resistance . ➜Hydralazine is accepted medication for controlling blood pressure in pregnancy induced hypertension.
  • 35. 9) Calcium Channel blockers: ➜Calcium channel blockers are another classes of first line anti hypertensive drugs . ➜Cause smooth muscle relaxation by blocking the binding calcium to its receptors, preventing muscle contraction. Results in, ➝Decreased peripheral smooth muscle tone ➝Decreased systemic vascular resistance ➝Decreased blood pressure ADR: Constipation. Dizziness. Fast heartbeat (palpitations)
  • 37.
  • 39. Zoho Show To create beautiful presentations, download Zoho Show from Play Store https://zoho.to/cy7 Hypertesion Anti-…rtensive drugs.pdf (This PDF has been generated using Zoho Show)