Anti Hypertensive Drugs

ANTI-HYPERTENSIVE Mechanism of Action &
DRUGS Classification
ANTI-HYPERTENSIVE DRUGS
Antihypertensives are a class of drugs that are
used to treat hypertension (high blood
pressure).Antihypertensive therapy seeks to
prevent the complications of high blood pressure,
such as stroke, heart failure, kidney failure and
myocardial infarction. Evidence suggests that
reduction of the blood pressure by 5 mmHg can
decrease the risk of stroke by 34% and of
ischaemic heart disease by 21%, and can reduce
the likelihood of dementia, heart failure, and
mortality from cardiovascular disease.
CLASSIFICATION OF THE
DRUGS
Hypertension is a very common disorder, particularly past middle age. It is not
a disease in itself, but is an important risk factor for cardiovascular mortality
and morbidity. The cutoff manometric reading between normotensives and
hypertensives is arbitrary. For practical purposes ‘hypertension’ could be that
level of BP at or above which long-term antihypertensive treatment will
reduce cardiovascular mortality. There are many classes of antihypertensives,
which lower blood pressure by different means. Among the most important
and most widely used medications are thiazide diuretics, calcium channel
blockers, ACE inhibitors, angiotensin II receptor antagonists (ARBs), and beta
blockers.
With the development of many types of
drugs, delineation of their long-term
benefits and complications, and
understanding of the principles on
which to combine them, hypertension
can now be controlled in most cases
with minimum discomfort.
DIURETICS
Diuretics have been the standard antihypertensive drugs over the past 4 decades,
though they do not lower BP in normotensives.
ADRS : • Hypokalaemia—muscle pain, fatigue and loss of energy.
• Erectile dysfunction in males.
• Carbohydrate intolerance: due to inhibition of insulin release (probably secondary
to K+ depletion which interferes with conversion of proinsulin to insulin),
precipitation of diabetes.
• Dyslipidemia: rise in total and LDL cholesterol and triglycerides with lowering of
HDL. This could increase atherogenic risk, but no direct evidence has been obtained.
• Hyperuricaemia: by inhibiting urate excretion—increased incidence of gout
ANGIOTENSIN CONVERTING
ENZYME
(ACE) INHIBITORS
The ACE inhibitors are one of the first choice drugs in all grades of essential as well
as renovascular hypertension (except those with bilateral renal artery stenosis).
Dry persistent cough is the most common side effect requiring discontinuation
of ACE inhibitors.
They are the most appropriate antihypertensives in patients with diabetes,
nephropathy (even nondiabetic), left ventricular hypertrophy, CHF, angina and post
MI cases.
ANGIOTENSIN 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. Angioedema, urticaria and taste disturbance are also rare.
Though effects of ACE inhibitors and ARBs are not identical, the latter have all the
metabolic and prognostic advantages of ACE inhibitors.
DIRECT RENIN INHIBITORS
Aliskiren the only available member of the latest class of
RAS inhibitors which act by blocking catalytic activity of
renin and inhibiting production of Ang I and Ang II. It is
described in Ch. 36. Aliskiren is an equally effective
antihypertensive as ACE inhibitors and ARBs, but experience
with it so far is limited. However, no remarkable features
have emerged and presently it is a second line antihypertensive
which may be employed when the more established ACE
inhibitors or ARBs cannot be used, or to supplement them
CALCIUM CHANNEL
BLOCKERS
Calcium channel blockers (CCBs) are another class of first line antihypertensive drugs.
They lower BP by decreasing peripheral resistance without compromising c.o. Despite
vasodilatation, fluid retention is insignificant.
Advantages :
1. Do not compromise haemodynamics: no ADRS :
impairment of physical work capacity. (i) The negative inotropic/dromotropic
2. No sedation or other CNS effects; cerebral action of verapamil/diltiazem may
perfusion is maintained.
worsen CHF and cardiac conduction
3. Not contraindicated in asthma, angina and PVD patients: may benefit these
conditions.
defects (DHPs are less likely to do
4. Do not impair renal perfusion. so).
5. Do not affect male sexual function. (ii) By their smooth muscle relaxant
6. No deleterious effect on plasma lipid profile, action, the DHPs can worsen
uric acid level and electrolyte balance. gastroesophageal reflux.
7. Shown to have no/minimal effect on quality (iii) CCBs (especially DHPs) may
of life. accentuate bladder voiding difficulty in
8. No adverse foetal effects; can be used during
elderly males.
pregnancy
BETA ADRENERGIC
BLOCKERS
They are mild antihypertensives; do not significantly lower BP in normotensives.
Used alone they suffice in 30–40% patients—mostly stage I cases. Additional BP
lowering may be obtained when combined with other drugs. The hypotensive
response to β blockers develops over 1–3 weeks and is then well sustained. Despite
short and differing plasma half lives, the antihypertensive action of most β blockers
is maintained over 24 hr with a single daily dose.
There are several contraindications to β blockers, including cardiac, pulmonary and
peripheral vascular disease. The nonselective β blockers have an unfavourable effect
on lipid profile (raise triglyceride level and LDL/HDL ratio). They have also fared
less well on quality of life parameters like decreased work capacity, fatigue, loss of
libido and subtle cognitive effects (forgetfulness, low drive), nightmares and
increased incidence of antidepressant use.
ALPHA + BETA BLOCKERS
Labetalol : It is a combined α and β blocker; reduces t.p.r. and acts faster than pure
β blockers. It has been used i.v. for rapid BP reduction in hyperadrenergic states,
cheese reaction, clonidine withdrawal, eclampsia, etc. Oral labetalol therapy is
restricted to moderately severe hypertension not responding to a pure β blocker,
because side effects of both α blocker and β blocker occur with it.
Carvedilol : This nonselective β + weak selective α1 blocker produces

vasodilatation and has additional antioxidant/free radical scavenging properties.
Whether these ancilliary properties confer any superiority is not known. Carvedilol
is a frequently selected drug for long-term treatment of CHF, and is approved as an
antihypertensive as well. Side effects are similar to labetalol; liver enzymes may rise
in some
ALPHA ADRENERGIC
BLOCKERS
Advantages : ADRS :
. Does not impair carbohydrate metabolism; Apart from postural hypotension related
suitable for diabetics, but not if neuropathy is symptoms (particularly in the beginning),
present, because postural hypotension is other side effects are headache,
accentuated. drowsiness, dry mouth, weakness,
palpitation, nasal blockade, blurred vision
• Has a small but favourable effect on lipid
profile: lowers LDL cholesterol and and rash. Ejaculation may be impaired in
triglycerides, increases HDL. males: especially with higher doses. Fluid
retention attending prazosin monotherapy
• Affords symptomatic improvement in may precipitate CHF.
coexisting benign prostatic hypertrophy
CENTRAL SYMPATHOLYTICS
VASODILATORS
Side effects mainly due to vasodilatation

are— palpitation, nervousness, vomiting,
perspiration, pain in abdomen, weakness,
disorientation, and lactic acidosis (caused
by the released cyanide).
THANK YOU By-
Vijayasekar Vishwant Vijeth

Anti Hypertensive Drugs

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Anti Hypertensive Drugs

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ANTI-HYPERTENSIVE Mechanism of Action &

Carvedilol : This nonselective β + weak selective α1 blocker produces

Side effects mainly due to vasodilatation

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