DRUGS ON

HYPERTENSION
• . ANTI HYPERTENSIVE DRUGS
• Diuretic
• ACE inhibitors
• Angiotensin (AT 1 receptor) blockers
• Direct renin inhibitor
• Calcium channel blockers
• β Adrenergic blockers
• β + α Adrenergic blockers
• α Adrenergic blockers
• Central sympatholytics
• Vasodilators
 Diuretics

Thiazides (hydrochlorothiazide, chlorthalidone)

• These are the diuretic of choice for uncomplicated hypertension; have

similar efficacy and are dose to dose equivalent
• Chlorthalidone is longer acting (~ 48 hours) than hydro-chlorothiazide
(< 24 hours) and may have better round-the-clock action.
• Indapamide is also mainly used as antihypertensive, and is equally
effective.
• Antihypertensive action of diuretics is lost when salt intake is high.
• The fall in BP develops gradually over2–4 weeks.
• Thiazides are mild antihypertensives, average fall in mean arterial
pressure is ~10 mm Hg.
• In combination, they are useful in any grade of hypertension. They are
more effective in the elderly and maximal antihypertensive efficacy is
reached at 25 mg/day dose, though higher doses produce greater
diuresis.
• Their antihypertensive action is attenuated by NSAIDs
 High ceiling diuretics
• Furosemide, the prototype of this class, is a strong diuretic, but is a
weaker antihypertensive than thiazides: fall in BP is entirely
dependent on reduction in plasma volume and c.o.
• high ceiling diuretics are more liable to cause fluid and electrolyte
imbalance, weakness and other side effects. They are indicated in
hypertension only when it is complicated by:
•
(a) Chronic renal failure: thiazides are ineffective, both as diuretic and
as antihypertensive.
(b) Coexisting refractory CHF.
(c) Resistance to combination regimens containing a thiazide, or
marked fluid retention due to use of potent vasodilators
 Potassium sparing diuretics

• Spironolactone,eplerenone and amiloride

• they are used only in conjunction with a thiazide diuretic to prevent
K+ loss and to augment the anti-hypertensive action.
• JNC 7 recommends instituting low-dose(12.5–25 mg) thiazide
therapy, preferably with added K + sparing diuretic, as a first choice
treatment of essential hypertension, especially in the elderly.
 ACE inhibitors
• The ACE inhibitors are one of the first choice drugs in all grades of
essential as well as renovascular hypertension
• Used alone they control hypertension in ~50% patients, and addition
of a diuretic/β blocker extends efficacy to ~90%
• They are the most appropriate antihypertensives in patients with
diabetes, nephropathy (even nondiabetic), left ventricular
hypertrophy, CHF, angina and post MI cases.
• They appear to be more effective in younger (< 55year) hypertensives
than in the elderly.
• Dry persistent cough is the most common side effect requiring
discontinuation of ACE inhibitors
 Angiotensin (AT 1 receptor) blockers

• The newer ARBs—valsartan, candesartan, irbesartan and telmisartan

have been shown to be as effective antihypertensives as ACE
inhibitors, while losartan may be somewhat weaker than high doses
of ACE inhibitors.
• ARBs are remarkably free of side effects.
• Because they do not increase kinin levels, the ACE inhibitor related
cough is not encountered
 CALCIUM CHANNEL BLOCKERS
• Calcium channel blockers (CCBs) are another class of first line
antihypertensive drugs.
• All 3 subgroups of CCBs, viz. dihydropyridines (DHPs, e.g.
amlodipine), phenylalkylamine (verapamil) and benzothiazepine
(diltiazem) are equally efficacious antihypertensives.
• They lower BP by decreasing peripheral resistance without
compromising c.o. Despite vasodilatation, fluid retention is
insignificant.
• The onset of antihypertensive action is quick. With the availability of
long acting preparations, most agents can be administered once a day
• Monotherapy with CCBs is effective in ~ 50% hypertensives; their
action is independent of patient’s renin status, and they may improve
arterial compliance.
• Not contraindicated in asthma, angina(especially variant) and PVD
patients: may benefit these conditions.
• Do not affect male sexual function.
• No adverse foetal effects; can be used during pregnancy (but can
weaken uterine contractions during labour).
• They are used as one of the first line monotherapy options because
of their high efficacy and excellent tolerability.
• They are preferred in the elderly hypertensive
 β-ADRENERGIC BLOCKERS

• They are mild anti hypertensives; do not significantly lower BP in

normotensives. Used alone they suffice in 30–40% patients—mostly
stage I cases.
• The hypotensive response to β blockers develops over 1–3 weeks and
is then well sustained.
• The antihypertensive action of most β blockers is maintained over 24
hr with a single daily dose.
• The group of selected β blockers includes metoprolol, bisoprolol,
carvedilol, nebivolol
• β blockers and ACE inhibitors are the most effective drugs for
preventing sudden cardiac death in post-infarction patients.
• β blockers retain their place among the first choice drugs
recommended by JNC 7 and WHO,especially for relatively young non-
obese hyper-tensives, those prone to psychological stress or those
with ischaemic heart disease.
 α-ADRENERGIC BLOCKERS

Prazosin

• This prototype selective α1 antagonist dilates both resistance and

capacitance vessels.
• Renal blood flow and g.f.r. are maintained but fluid retention may
attend fall in B.P, postural hypotension and fainting may occur in the
beginning—called ‘first dose effect’.
• For this reason, prazosin is always started at low dose (0.5 mg) given
at bedtime and gradually increased with twice daily administration
till an adequate response is produced (max. dose 10 mg BD).
 β + α Adrenergic blockers

• β + α Adrenergic blockers are a subclass of beta blockers .

• This group includes drug like – carvedilol, labetalol, dilevalol.
• They play central role in sympathetic nervous system.
• They prevent stimulation of alpha 1 and beta receptor and do dilation
of blood vessels.
• They are generally use in emergency condition.
 DIRECT RENIN INHIBITORS

• This group of drugs works on RAS. They act as non peptide renin
inhibitors , they binds with renin and block the generation of
angiotensin.
• Renin convert angiotensin into angiotensin I and then into
angiotensin II which causes vasoconstriction.
• It includes drugs like Aliskiren , Remikiren, Enalkiren
 CENTRAL SYMPATHOLYTICS

• This groups of drugs are use as fourth line treatment in hypertension.

• This includes drugs like methyldopa, guanabenz, clonidine,
moxonidine.
• They have variety of antihypertensive actions like, they increase
sodium excretion, and decrease C.O, heart rate
• Adverse effect includes sedation , depression, dry mouth etc.
• They should be use on PRN basis