ANTIHYPERTENSIVES

BY
KENNETH CHISAMANGA
DRUGS
PHARMACIST
 INTRODUCTION
 Antihypertensive Agent which act to reduce
blood pressure are used to treat
HYPERTENSION, a disorder characterised by
elevation in SYSTOLIC Blood pressure,
DIASYSTOLIC blood pressure or both.
 Essential (Primary) or Secondary hypertension
occurs when homeostatic mechanisms fail to
regulate blood pressure.
INTRODUCTION CONTINUES
 ESSENTIAL Hypertension affects about 95% of
all hypertensive patients.
 Secondary Hypertension affects about 5% of
hypertensive patients and results from such
underlying disorders as aortic regurgitation,
renal artery stenosis, pheochromocytoma and
neurologic disease.
 Treatment of the underlying disorders
sometimes cures secondary hypertension.
 INTRODUCTION CONTINUES
 Uncontrolled hypertension can lead to
HYPERTENSIVE CRISIS and MALIGNANT
HYERTENSION, which are characterised by
diastolic blood pressure of above 140mmHg.
AIMS OF TREATMENT
1. Maintain normal Blood Pressure

2. Prevent complications due to hypertension

3. Prevent death
 NON PHARMACOLOGICAL
THERAPY
1. Life style changes
 Cessation of smoking.

 Moderation of alcohol intake.

 Weight reduction

 Make yourself happy all the times

2. Exercises
 Do some regular physical activity but not so

vigorous ones.
3. Diet
 Avoid and reduce on direct salt intake.

 Avoid eating a lot of oily foods

 DRUG TREATMENT
 Antihypertensive Agent are classified into the
following:
a. SYMPATHOLYTIC AGENTS
b. VASODILATING AGENTS
c. ACE INHIBITORS
d. DIURETICS
 SYMPATHOLYTIC AGENT
 These include various group of drugs that
reduce blood pressure by inhibiting or blocking
motor and secretory action in the sympathetic
Nervous System.
 They are classified according to their site of
action or mechanism of action
 CENTRAL ACTING SYMPATHETIC
NERVOUS SYSTEM INHIBITORS
Examples include:
 Methydopa

 Clonidine HCl

 Guanabenz acetate

 Guanfacine
 METHYLDOPA
 Comes as tablet of either 250mg/tablet or
500mg/tablet.

MoA
 They act by inhibiting stimulation of the
sympathetic nervous system.
 INDICATION (USES)
 Used in management of hypertension in
pregnancy
DOSE
 250 - 500mg, 2 – 3 times daily, increased
gradually to max. 3g daily.
 SIDE EFFECTS
 Postural hypertension
 Dry Mouth
 GIT disturbances
 Stomatitis
 Bradycardia
 Impotence
 Exacerbation of angina
 Parkinsonism
 BETA ADRENERGIC BLOCKING
AGENT (BETA BLOCKERS)
Examples include:
 Propranolol

 Atenolol

 Acebutolol

 Metoprolol

 Pindolol

 Nadolol

 Timolol
 PROPRANOLOL
 This comes as a tablet of 40mg each.
INDICATION
 Hypertension

DOSE
 20 to 80mg twice daily, increased gradually if

necessary to a max. of 640mg/day.

 Children 1 to 4mg/kg given in 2 equally

divided doses.
 SIDE EFFECTS
 Bradycardia
 Hypotension
 Depression
 Bronchospasms
 Thrombocytopenia
 Dry eyes
 Insomia
 hallucinations
 ALPHA ADRENERGIC BLOCKING
AGENT
Examples in this group include :
 Doxazosin

 Phentolamine

 Prazosin

 Terazosin
 PRAZOSIN HCL
INDICATIONS
 Hypertension

DOSE
 Adult: initially, 0-5 to 1mg P.O. bid or tid, for

maintenance dosage, increased gradually to 6 to 15mg

daily in divided doses.
SIDE EFFECTS
 orthostatic hypotension

 First dose syncope,

 anginal attack

 Palpitations

 Rebound tachycardia
 MIXED ALPHA AND BETA
ADRENERGIC BLOCKING AGENT
Examples include
 Labetolol

 Norepinephrine depletors such as:

 Guanadrel sulphate

 Guanethidine Monosulphate and

 Reserpine.
NURSING APPLICATION (GENERAL)

1. Obtain baseline data before beginning

sympatholytic therapy. Assess the patient’s
blood pressure and pulses in the sitting,
standing and supine positions.
2. Monitor and record the patient’s blood
pressure and pulse when starting therapy,
before administering each dose, and during
peak concentration times.
NURSING APPLICATION (GENERAL)

3. Monitor the patient’s vital signs, as instructed.

For example, expect to monitor the patient’s blood
pressure and pulse every 15 – 30 minutes for
atleast the first 2 hours during initial
administration.
4. Moniotor serum electrolyte levels and correct
any imbalances as prescribed, before
administering a norepinephrine depletor.
 VASODILATING AGENTS
There are two types of Vasodilating agent:
a. Direct Vasodilators

b. Calcium channel Blockers

These act by decreasing systolic and diastolic

blood pressure by relaxing arteriolar smooth
muscles, leading to arteriolar dilation and
decreasing peripheral resistance.
 DIRECT VASODILATORS
Examples:
 Hydrallazine

 Diazoxide

 Minoxidil

 Nitroprusside

MoA
 Act on arteries, veins or both by causing

relaxation of arteriolar smooth muscles,

leading to arteriolar dilation and decreasing
peripheral resistance.
 HYDRALLAZINE
INDICATION
 Adjunct therapy for moderate to severe

hypertension
DOSE
 40mg P.O. daily in divded doses for the first 2

to 4 days, increased to 100mg daily for the rest

of the week, then 200mg daily in divided doses
and upto a maximum of 300mg daily in four
divided doses.
 SIDE EFFECTS
 Palpitations
 Tachycardia
 Tremors
 Lacrimation
 Breast tenderness
 Constipation
 Orthostatic hypotension
 Facial flushing
 Shortness of Breath
 NURSING APPLICATION
 Obtain baseline blood pressure and pulse rates before
Hydrallazine administration. During administration,
monitor the blood pressure and pulse every 5 minutes
for the first 30 minutes and then every 15 minutes for
2 hours after each dose is given and blood pressure
stabilises.
 Monitor for signs of cerebral ischemia and impaired
renal blood flow. These signs are most likely to occur
when vasodilator administration causes rapid
reduction in blood pressure. If any of the signs
appear, help the patient into a supine position, elevate
the patient’s legs and notify the doctor immediately.
 NURSING APPLICATION
 Hydrallazine should not be administered with
food because food increases the drug’s plasma
levels.
 Ask the patient to report headache, angina pain
or muscle cramps.
CALCIUM CHANNEL BLOCKER
Examples:
 Nifedipine

 Amlodipine

 Nicardipine

 Felodipine

 Isradipine

 Diltiazem

 Verapamil
 NIFEDIPINE
This comes as a tablet of 20mg each.
MoA
Produce arteriolar relaxation by preventing the
entry of calcium into the cells, thus reducing the
mechanical activity of vascular smooth muscle.
SIDE EFFECTS
 Headache

 Hypotension

 Bradycardia

 Peripheral oedema
 DOSE
 10 TO 60mg once daily, increased to a
maximum of 120mg daily if necessary.
NURSING APPLICATION
 Monitor patients for orthostatic hypotension

and teach patient on how to manage it.

 Prevent orthostatic hypotension by keeping the

patient in a supine position for 15 to 30

minutes.
 ANGIOTENSIN – CONVERTING
ENZYME (ACE) INHIBITOR.
These reduce blood pressure by interrupting the
renin-angiotensin aldosterone system.
Examples include:
 Enalapril

 Captopril

 Lisinopril

 Fosinopril

 Quinapril

 Ramipril
 ENALAPRIL
This comes as tablet of 5mg, 10mg and 20mg.
INDICATION
 Hypertension

DOSE
5mg once daily, gradually increased to a maximum of
40mg daily.
SIDE EFFECTS
 Hypotension

 Persistent dry cough

 Proteinurea

 Elevation of BUN and creatinine levels

 NURSING APPLICATION
 Observe for the signs of angioedema such as
flushing or pallor and swelling of the face,
extremities, lips, tongue, glottis or larynx. If
angioedema occurs, withhold the drug, notify
the doctor and begin emergency treatment as
prescribed.
 Obtain baseline blood pressure and pulse rates
before beginning ACE inhibitor therapy.
 DIURETIC AGENT
 These are used to increase urine volume and
maximise excretion of solutes and water.
 They are five types of diuretics:
a. THIAZIDE AND THIAZIDE-LIKE DIURETIC.
 These are sulphonamides derivatives that
inhibits sodium reabsorption, thereby
increasing sodium and water excretion.
 These diuretics may produce hypersensitivity
reactions similar to those of sulphonamides.
 THIAZIDE AND THIAZIDE-LIKE
DIURETICS CONTINUES.
 They also increase the excretion of chloride,
potassium and bicarbonate ions, which can results in
electrolyte imbalances, particularly Hypokalemia.
Examples:
 Bendrofluazide

 Benzthiazide

 Chlorothiazide

 Hydrochlorothiazide

 Methyclothiazide

 Polythiazide

 Trichlorormeththiazide
 EXAMPLES OF THIAZIDE-LIKE
DIURETICS
 Chlorthalidone
 Indapamide
 Metolazone
 quinethazone
 MOA
 These interfere with transport of sodium ions
across the renal tubular epithelium at the
cortical-diluting, or distal, segment of the
nephrons.
INDICATIONS (USES)
 May be alone or in combination with other

drugs primarily to treat hypertension.

 Although their antihypertensive effects may

begin within 3 – 4 days after initiation of

treatment, the drugs are most effective after 3 to
4 weeks of continued therapy.
INDICATIONS (USES) CONTINUES.
 Treat Oedema associated with mild to moderate heart
failure.
BENDROFLUAZIDES 5mg Tablet.
INDICATIONS
 Hypertension

 Oedema

 Mild to moderate Heart Failure

SIDE EFFECTS
 Hypokalemia

 Postural Hypotension

 Gout

 Hyponatremia, hypomanesaemia, hypercalcaemia

 DOSE
 2.5 – 5mg once daily in hypertension.
 5 – 10mg once daily in the morning in

treatment of oedema.
NURSING APPLICATION.
 Be alert in patient’s serum sodium and

potassium levels. Also observe for signs and

symptoms of Hyponatremia, such as anxiety,
Hypotension, and nausea: and Hypokalemia,
such as drowsiness, muscle cramps,
hyporeflexia and paresthesia.
NURSING APPLICATION CONTINUES
 Administer Potassium supplements as prescribed to
maintain an acceptable serum potasium levels. Administer
normal or half-normal saline solution I.V. As prescribed
to correct hyponatremia.
 Monitor the Blood Glucose levels in diabetic patient
during long-term therapy with a thiazide or thiazide like
diuretic because these agents can cause Glucose
intolerance.
 Administer the diuretic in the morning or early afternoon,
if permissible, to prevent nocturia from upsetting the
patient’s normal sleep pattern. Keep a urinal or bedpan
within reach for bedridden patient; ensure that the
bathroom is easily accessible for an ambulatory patient.
 b. LOOP OR HIGH CEILING
DIURETICS
 These are highly potent agents and include the
following as examples:
 Furosemide
 Bumetanide
 Ethacrynate sodium
 Ethacrynic acid
MoA
They inhibit sodium and chloride reabsorption in
the renal tubules by direct action on the thick
ascending limb of the loop of henle.
 FUROSEMIDE
 It comes as tablet of 40mg and injection of
20mg /2ml.
INDICATIONS
 Resistant Hypertension

 Oedema

DOSE
 Resistant Hypertension 40 – 80mg daily

 Resistant Oedema 80 – 120mg daily

 SIDE EFFECTS
 Orthostatic Hypotension
 Hypokalemia
 hypochloremia
 Hyperuricemia
 Impaired glucose tolerance
 Transient deafness
 Abdominal discomfort or pain
 Tinnitus
 Hypersensitivity reactions.
 NURSING APPLICATION
 Administer Potassium supplements as prescribed to
maintain an acceptable serum potasium levels. Administer
normal or half-normal saline solution I.V. As prescribed
to correct hyponatremia.
 Monitor the Blood Glucose levels in diabetic patient
during long-term therapy with a thiazide or thiazide like
diuretic because these agents can cause Glucose
intolerance.
 Administer the diuretic in the morning or early afternoon,
if permissible, to prevent nocturia from upsetting the
patient’s normal sleep pattern. Keep a urinal or bedpan
within reach for bedridden patient; ensure that the
bathroom is easily accessible for an ambulatory patient.
NURSING APPLICATION CONTINUES
 Be alert in patient’s serum sodium and potassium
levels. Also observe for signs and symptoms of
Hyponatremia, such as anxiety, Hypotension, and
nausea: and Hypokalemia, such as drowsiness,
muscle cramps, hyporeflexia and paresthesia.
 Monitor the patient’s signs for dehydration such
as poor skin turgor and dry oral mucous
membrane. Check the vital signs to detect signs of
hypovalemia, such as tachycardia, hypotension
and dyspnea. If signs are present, notify the
doctor.
NURSING APPLICATION CONTINUES

 Accurately record the patient’s fluids intake

and output. If extreme discrepancies occur,
notify the physician and expect to decrease the
diuretic dosage, as prescribed.
 c. POTASSIUM – SPARING
DIURETICS
 These have weaker diuretic and
antihypertensive effects than other diuretics,
but they have the advantage of conserving
potassium.
Examples>
 Spironolactone

 Amiloride hydrochloride

 Triamterene
 MoA
 These act on the distal renal tubules to produce
mild diuretic and antihypertensive effects that
increases the urinary excretion of sodium,
chloride and calcium ions and reduce the
excretion of potassium and hydrogen ions.
 The effect leads to increased potassium levels
and urine pH.
 Spironolactone is an ALDOSTERONE
Antagonist.
 SPIRONOLACTONE TABLET
INDICATIONS
 Oedema

 Diuretic induced hypokalemia

 Cirrhosis

 Nephrotic Syndrome

 Hypertension

DOSE
25 – 100mg daily as single dose or 2 divided
doses.
 SIDE EFFECTS
 Hyperkalemia
 Megaloblastic anaemia
 Orthostatic hypotension
 Headache
 Abdominal cramps
 Gynecomastia in males
 Menstrual abnormalities
 Diarrhoea
 Breast soreness
 NURSING APPLICATION
 Monitor the patient for signs and symptoms of
hyperkalemia, such as confusion,
hyperexcitability, muscle weakness, paresthsia,
flaccid paralysis, arryhythmias, abdominal
distention, diarrhoea and intestinal colic. Also
monitor the patient’s electrolytes levels for
imbalances.
 Store spironolactone in a light resistant
container.
 Administer spironolactone in the morning or
early afternoon, if possible to avoid nocturia.
 d. OSMOTIC DIURETICS
 Osmotic Diuretic used because it is effective in
patient’s with compromised renal circulation.
Examples:
 Mannitol

MoA
 These act by increasing the osmolality of the

plasma, glomerular filtrates and tubular fluid.

This decreases the reabsorption of fluid and
electrolytes, which increases the excretion of
water, chloride, and sodium and slightly
increases the excretion of potassium.
 INDICATIONS
 Reduce intracranial or intraoccular pressure
 To prevent acute renal failure

 It is very effective in patients with

compromised renal circulation.

DOSE
 0.25 – 2g/kg by I.V. infusion over 30 – 60

minutes.
 SIDE EFFECTS
 Transient expansion of plasma volume during
infusion, (resulting in circulatory overload and
tachycardia),
 Electrolytes imbalances
 Volume depletion
 Cellular dehydration
 Headache
 Rebound increased intracranial pressure 8 – 12
hours after diuresis
 Angina like chest pain
 Thirst and blurred vision
 NURSING APPLICATION
 Document the patient’s fluid intake and output
hourly because therapy is based on an hourly
urine flow rate. Asses the patient for circulatory
overload if the urine output is less than 30 – 50
ml/hour.
 Do not administer crystallised medication. Also,
do not add blood products to I.V. lines for
mannitol administration because they are
incompatible.
 Store mannitol at 15 – 30 C unless otherwise
directed, and do not allow it to freeze.
 e. CARBONIC ANHYDRASE
INHIBITORS
 These are used to induce diuresis.
Examples:
 Acetazolamide

 Dichlorphenamide

 Methazolamide

They are primarily used to decrease the formation of

aqueous humor by the ciliary body and thereby to control
the excessive intraoccular pressure associated with
GLAUCOMA.
They are also used to treat Oedema related to cardiac
disorders, periodic paralysis, and acute mountain
sickness.
ZIKOMO AND
THANK.
THE END