This document discusses various classes of antihypertensive agents, including diuretics, beta blockers, calcium channel blockers, ACE inhibitors, angiotensin receptor blockers, and direct arterial vasodilators. It provides details on the mechanisms of action, indications, side effects, and contraindications of each class. The document was submitted by a pharmacy student as an assignment on antihypertensive agents.
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Anti - Hypertensive agent/ Drug
1. GONO Bishwabidwalay
Sub code:pharm-3506p
[Assignment on Anti-hypertensive Agent]
Sub code:pharm-3506p
Submitted to:
Mst. Rozina parul
Senior lecturer
Department of pharmacy
Gono BIshwabidyalay
Submitted by:
Md.Moshiur Rahman
Roll:07
Exam roll:(2047)
Semester:5th
(31th
Batch)
Department : Pharmacy
Gono BIshwabidyalay
Submission date: 6/03/2019
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Anti-Hypertensive Agent
Definition : Antihypertensive agent comprise several classes of compound with the therapeutic
intention of preventing, controlling, or treating hypertension.
CLASSIFICATION
1. Diuretics.
2. Beta Adrenergic Drug.
3. Calcium Channel Blocker.
4. Agiotensin Receptor Blocker.
5. Agiotensin Converting Enzymatic inhibitor .
6.Direct Arterial Vasodilator
7. Sympatholytics and Adrenergic Blocker
Classes and subclasses of antihypertensive medications with common examples
Class Examples
Targeting renin–angiotensin
system
Angiotensin receptor antagonists Candesartan, losartan, valsartan
Direct renin antagonists Aliskiren
Adrenoceptor antagonists
β-Blockers Atenolol, metoprolol, propranolol
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α-Blockers Doxazosin, labetalol (also a β-blocker), phentolamine,
phenoxybenzamine
Calcium channel blockers
Phenylalkamines Verapamil
Dihydropyridines Amlodipine, nifedipine, nimodipine
Benzothiazepines Diltiazem
Diuretics
Thiazides Bendroflumethiazide, hydrochlorothiazide
Loop
Furosemide, bumetanide
Potassium sparing/ aldosterone antagonist Amiloride, spironolactone
Vasodilators Hydralazine, minoxidil
Centrally acting agents Clonidine, methyldopa
Ganglion block Trimetaphan
1. Diuretics
Diuretics, also called water pills, are medications designed to increase the amount of water and
salt expelled from the body as urine.
.Types of diuretics
•Thiazides and related diuretics.
•Loop diuretics.
•Potassium sparing diuretics.
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Mechanism of Action
• Osmotic diuretics- Inhibition of water and Na+ reabsorption
Sites of action :1. Proximal tubules.
2.loop of Henle.
3.collecting duct.
• Loop Diuretics – inhibition of Na+,K+,Cl –
contransport.
Sites of action : Loop of henle
Carbonic Anhydrase inhibitor- Inhibition of biocarbonate reabsorption
Thiazide – inhibition of Na+, Cl –
contransport.
sites of action : early distal tubules
indication of diuretics
• liver failure.
• Edema
• heart failure.
• Kidney disorderes
• Renal impairment: loop diuretics.
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Side effects of diuretics
low sodium
Headache
dizziness
thirst
increased blood sugar
muscle cramps
Skin Rash
Increase cholesterol
Gout
Diarrhoea
In rare cases, diuretics may cause serious side effects. These can include:
allergic reaction
irregular heartbeat
Kidney failure
Contraindication of diuretics
Diabetes
increased activity of the parathyroid gland
high cholesterol
low amount of magnesium in the blood
high amount of calcium in the blood
low amount of sodium in the blood
Loss of Body Water
low amount of potassium in the blood
Liver Failure
Yellowing of the Skin in a Newborn Child
High Amount of Uric Acid in the Blood
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2.Beta - Adrenergic Blocking Agents
Beta-adrenergic blocking agents, are medications that reduce your blood pressure.
Mechanisms of Action
Blood pressure falls with beta-blockers that have beta 1-selectivity, intrinsic sympathomimetic activity
and membrane activity, but not those with a high level of pure beta-stimulation. Several suggestions
have been made to explain this effect; a direct action on the central nervous system, adrenergic
neurone blocking, perhaps via pre-synaptic beta 2-receptors, anti-renin activity, an increase of
vasodilator prostaglandins, effects secondary to reduced cardiac output, and resetting of baroreceptors
secondary to reduced pressor peaks to various pressor stimuli from the reduction in cardiac activity
consequent to beta-blockade. There are also beta-blocking drugs which additionally have direct action
to reduce peripheral resistance, via beta 2-mediated vasodilation, an alpha-blocking action or a direct
vasodilator activity. Most attention has been given to a possible correlation to the effect of beta-
adrenoceptor blocking drugs on the blood pressure and renin levels. Several investigations have found
patients with high renin levels respond best, normal renin patients respond less well and low renin
patients relatively poorly.
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Indications of Beta – Adrenergic
• Hypertension associated with coronary artery disease.
Anxiety
Myocardial Infraction
Arrhythmia migraine
Glaucoma
thyrotoxicity
Side Effects Beta – Adrenergic
Weight gain
Shortness of breath
Trouble sleeping
Depression.
Fatigue
nausea, weakness, and dizziness
slow heartbeat
swelling of the hands and feet
abdominal cramps
memory loss, or confusion
back or joint pain
Bronchospasm
• Bradycardia
Contraindication of Beta – Adrenergic
asthma
Anti-anginal drugs
diabetes
Congestive heart failure
Anesthetics
Hypotension
Heart block
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3.Calcium channel blockers
Calcium channel blockers, also called calcium antagonists, relax and widen blood vessels by affecting the
muscle cells in the arterial walls.
Types
•Dihydropyridine: nifedipine, amlodipine, felodipine, nicardipine, lacidipine.
•Non dihydropyridine :
- Phenylalkylamine: verapamil.
- Benzothiazepine: diltiazem.
Mechanisms of action
•Calcium enters muscle cell through special voltage sensitive calcium channel level.
•Normally L-type of channel s admit Ca+ & cause depolarization –excitation contraction couple
through phosphorylation of myosin chain –ctraction of vascular smooth muscle.
•Decrease blood pressure
Decrease systemic vascular resistance
Indications Calcium channel blockers
• Ischemic heart disease
High blood pressure
Coronary artery disease
Chest pain (angina)
Irregular heartbeats (arrhythmia)
Some circulatory conditions, such as Raynaud's disease
Side Effects Calcium channel blockers
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Constipation
Headache
Palpitations
Dizziness
Rash
Drowsiness
Flushing
Nausea
Swelling in the feet and lower legs
4.Angiotensin Converting Enzyme Inhibitor
Angiotensin-converting enzyme (ACE) inhibitors help relax blood vessels. ACE inhibitors prevent an
enzyme in your body from producing angiotensin II, a substance in your body that narrows your blood
vessels and releases hormones that can raise your blood pressure.
Examples of ACE inhibitors include:
Benazepril (Lotensin)
Captopril
Enalapril (Vasotec)
Fosinopril
Types
•Class I: captopril
•Class II (prodrug) : e.g., ramipril, enalapril, perindopril
•Class III ( water soluble) : lisinopril.
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Mechanism of Action of ACE
•Inhibition of circulating and tissue
angiotensin- converting enzyme.
•Increased formation of bradykinin and vasodilatory prostaglandins.
•Decreased secretion of aldosterone; help sodium excretion.
Indications of Angiotensin Converting Enzyme
• Congestive heart failure.
High blood pressure
Coronary artery disease
Heart failure
Diabetes
Certain chronic kidney diseases
Heart attacks
Scleroderma
Migraines
Side Effects of Angiotensin Converting Enzyme
Dry cough
Increased blood-potassium level (hyperkalemia)
Fatigue
Dizziness
Headaches
Loss of taste
Skin rash
Renal failure
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Hyperkalaemia
Contraindications Angiotensin Converting Enzyme
Angioneurotic edema:
Pregnancy (serious Teratogenicity – black box warning)
Renal Artery Stenosis
ACE Inhibitor related Allergic Reaction
Hypertrophic Cardiomyopathy
5.Angiotensin Receptor Blockers
Angiotensin II receptor blockers (ARBs) help relax your blood vessels, which lowers your blood pressure
and makes it easier for your heart to pump blood.
Mechanism of action:They act by blocking type I angiotensin II receptors generally, producing
more blockade of the renin -
angiotensin - aldosterone axis.
Reduce excreation of potassium
Block access Angiotensin ||
Decrease release of aldosteron
Main actions are:
1.vasodilation
2.incease salt water secretion
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Indications angiotensin Receptor Blockers
• Diabetes mellitus
• High blood pressure
Heart failure
Kidney failure in diabetes
Chronic kidney diseases
Side Effects
Prazocin: postural hypotension, diarrhea, occasional tachycardia, and tolerance
Dizziness
Elevated blood potassium level (hyperkalemia)
Localized swelling of tissues
6. Direct Arterial Vasodilators
Vasodilators are a group of medicines that dilate (open) blood vessels, which allows blood to flow more
easily.
Types
: hydralazine, diazoxide, nitroprusside,
Mechanism of action Direct Arterial Vasodilators
Stimulation of peripheral β2 adrenoceptor
Antagonism of alpha adrenoreceptor
Inhibition Of inward flow of calcium ions through calcium channels
Stimulation of dopaminergic receptor
Angiotensin converting enzyme inhibition (enalapril)
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Indication of Direct Arterial Vasodilators
Preeclampsia (high blood pressure during pregnancy)
Angina
Pulmonary hypertension (high blood pressure that affects the arteries in your lungs)
Anal fissure and fistula
Angina
Angina pectoris prophylaxis
Erectile Dysfunction
Heart Attack
Heart Failure
High blood pressure
Pulmonary Hypertension
Side Effects of Vasodilators
Chest pain
Heart palpitations (fluttering or pounding heartbeat)
Rapid heartbeat
Fluid retention
Nausea or vomiting