Anti Hypertensives

It is most common disease of
CVS.
Definition : Persistent and sustained increased
BP has damaging effects on heart, brain,
kidney,
Types : eye, lungs.
1) Primary / essential
hypertension No specific
causes 95% cases
2)Secondary hypertension
Other : Genetic factors, psychological stress,
environmental and dietary factors as contributing to
the development of
hypertension
Classification of Hypertension Based on
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
➜ 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.
➜ 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
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:
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 :
- 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.
ADR :
Overdose
having.
→Hypokalemia.
→Hyponatremi
a
→Hypocalcaemi
a
→Hyperglycemi
-Loop
diuretics:
➜Inhibition of
epithelial sodium
transport at the late
distal and collecting
ducts.
ADR:
➜hyponatremia,
hypokalemia,
hypomagnesemia,
dehydration, hyperuricemia,
-K+ Sparing
Diuretics:
➜potassium sparing
diuretics are competative
that either compete with
aldosterone(Spironolactone
& eplerenone), or
➜directly block the
epithelial sodium
channel. (Amiloride)
➜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
➜ Over dose having
hypotension
➜ Hyperkalemia
➜ Cough
➜ Rashes, urticaria
➜ Angioedema
➜ Dysgeusia / parageusia
➜ Headache, dizziness,
nausea.
➜ Hypertension
➜ Congestive Heart Failure
(CHF)
➜ Myocardial Infarction.
➜ Diabetic nephropathy.
➜ Nondiabetic nephropathy.
➜ Scleroderma Crisis.
➜ 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.
➜ 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.
Angioed
α
-
Phentolamine, Phenoxybenzamine is a α1-adrenergic
blocking agent.
Alpha blockers reduce the arterial pressure.
ADR :
Postural hypotension.
Sedation.
Tachycardia.
Miosis.
Nasal
β
➜ 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
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 :
➜ Bronchospasm,
➜ Heart failure,
➜ Bradycardia,
➜ Heart block,
➜ Neurological reactions include depression,
fatigue,
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
➜ 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.
➜ 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
Treatment of hypertension in patients with
concomitant diseases
CONCOMITANT
DISEASE DRUG CLASSES INDICATED INTREATING HYPERTENSION
HIGH CORONARY
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