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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
2
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
3
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.
4
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.
5
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
6
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.
7
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
8
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
9
 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.
10
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
11
 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
12
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)
13
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
14
 Dizziness
 Headache
 Flushing
 Excessive hair growth
 Nasal congestion
Contraindications Vasodilators
 Alcohol
 Pregnancy
 Cerebral insuficency

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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
  • 2. 2 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
  • 3. 3 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.
  • 4. 4 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.
  • 5. 5 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
  • 6. 6 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.
  • 7. 7 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
  • 8. 8 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
  • 9. 9  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.
  • 10. 10 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
  • 11. 11  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
  • 12. 12 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)
  • 13. 13 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
  • 14. 14  Dizziness  Headache  Flushing  Excessive hair growth  Nasal congestion Contraindications Vasodilators  Alcohol  Pregnancy  Cerebral insuficency