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ANTIHYPERTENSIVE DRUGS
Presented by:
Mr. Shaikh Akhil
M.Pharm
Asst. Prof. Dept. of
Pharmacology,
BCCO Pharmacy, Naigaon,
S.R.T.M. University,
Nanded
Definition-Hypertension is common cardiovascular disease
determined by increase blood pressure (pressure exerted
by blood against the wall of a blood vessel )in arteries.
Normal blood pressure-
120/80 mmHg
systolic/diastolic
Symptoms that may occur
include:
•Confusion
•Ear noise or buzzing
•Fatigue
•Irregular heartbeat
•Nosebleed
•Vision changes
BP= CO X SVR
BP = Blood pressure
CO =Cardiac output
SVR=Systemic vascular
resistance
Category Systolic Blood
Pressure(mmHg)
Diastolic Blood
Pressure(mmHg)
Pre-hypertension 120-139 80
Hypertension – Stage 1 140-159 90-99
Hypertension – Stage 2 160-179 100-109
Hypertension – Stage 3 >180 >110
CATEGORIES OF HYPERTENSION
ACCORDING TO EUROPEAN SOCIETY OF
CARDIOLOGY.
Types of
Hypertension
Essential Secondary
A disorder of unknown origin affecting the
Blood Pressure regulating mechanisms
Secondary to other disease processes
RISK FACTORS-
•Hyperlipidaemia –more LDL content
•Tension and stress
•Smoking-more nicotine intake
•Diabetes mellitus
•Imbalance between vasoconstrictor and
vasodilators peptides
Treatment-Why???
Antihypertensive Drug Therapy
DIURETICS :
EXAMPLES:Thiazides: chlorthalidone
High ceiling:Furosemide
K+ sparing:Spironolactone,
MOA: Act on V-2 receptor in kidneys (vasopressin
receptor) having an antediuretic function----
leads to diuresis----increased secretion of Na &
H2O decrease in blood volume ----decreased CO--
--decreased BP.
Adverse Reactions
•dizziness,
•electrolyte
imbalance/depletion,
•hypokalemia,
•hyperlipidemia,
•hyperglycemia
(Thiazides)
Contraindications
•hypersensitivity,
•compromised kidney
function
•hyponatremia
Central Sympatholytics (a-2
Agonists) Drugs: clonidine, methyldopa
Site of Action:CNS medullary ,cardiovascular
centers
MOA: CNS a-2 adrenergic stimulation----
autoinhibitory feed back mechanism----
decreased sympathetic outflow----decreased
norepinephrine release----vasodilatation----
decreased PR---- decreased BP.
Adverse Effect:dry mouth; sedation; drowsiness;nasal
congestion
SYMPATHOLYTIC DRUGS
a-1 Adrenergic blockers (Antagonists)
Drugs:Prazocin,Terazocin
Site of Action: peripheral arterioles, smooth muscle
MOA:Blocks a-1 receptor(in post synaptic neurone as well as in
vascular smooth muscles)---- cause vasodialatation due to relaxation
of vascular smooth muscles---- decreased PR----also reduces preload
by pooling of blood----decreased CO ---- decreased BP.
Adverse Effects:nausea; drowsiness; postural hypotension;headache
b -ADRNERGIC BLOCKERS(ANTAGONISTS)
Drugs: Non Selective– Propranolol,Timolol, Pindolol
Cardioselective –Atenolol, Metoprolol(acts only on
beta-1 receptor )
Site of Action: heart,kidney.
MOA: 1.heart:blocks b -1receptor---reduce heart rate ----
decreased CO---- decreased BP
2.kidney:decreased renin production(mediated by b-
1 receptor)----depresses RAS system---- decreased PR----
decreased BP
Advantages:No postural hypotension;No salt and water
retention
Low incidence of side effects
Adverse Effects:impotence; bradycardia; fatigue; exercise
intolerance
Contraindication: asthma;bradycardia;hypersensitivity
CALCIUM CHANNEL BLOCKERS (CCBs)
Drugs: verapamil ; nifedipine ; diltiazem ;
amlodipine:felodipine
Site of Action- Vascular
smooth muscle
K
Ca
Na
MOA:Blocks long acting
voltage sensitive calcinm
channels
Advantages:
No sedation or other CNS effects
Can be given to asthma patients &
angina patients
No impairment of renal perfusion
No deleterious effect on uric acid
level& electrolyte
balance
Side effects:
flushing; headache; tachycardia;
peripheral oedema
gastroesophageal reflux
Contraindications:
Congestive heart failure;
Pregnancy and lactation
DRUGS ACTING ON RENIN
ANGIOTENSIN SYSTEM (RAS)
1ACE inhibitors: captopril;enalapril;
lisinopril
2 renin inhibitors: Aliskiren; remikinen
3 AT1 receptor antagonists:losartan
;candesartan
1st line of Drug:
No postural hypotension or
electrolyte imbalance (no fatigue or
weakness)
Safe in asthmatics and diabetics
Prevention of secondary
hyperaldosteronism and K+ loss
Reverse the ventricular hypertrophy
and increase in lumen size of vessel
No hyperuraecemia or deleterious
effect on plasma lipid profile
Side effects:
Dry cough;
Steep fall in BP with 1st dose
Skin rash
Angioneurotic oedema
Anti hypertensive drug
Anti hypertensive drug

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Anti hypertensive drug

  • 1. ANTIHYPERTENSIVE DRUGS Presented by: Mr. Shaikh Akhil M.Pharm Asst. Prof. Dept. of Pharmacology, BCCO Pharmacy, Naigaon, S.R.T.M. University, Nanded
  • 2. Definition-Hypertension is common cardiovascular disease determined by increase blood pressure (pressure exerted by blood against the wall of a blood vessel )in arteries. Normal blood pressure- 120/80 mmHg systolic/diastolic Symptoms that may occur include: •Confusion •Ear noise or buzzing •Fatigue •Irregular heartbeat •Nosebleed •Vision changes BP= CO X SVR BP = Blood pressure CO =Cardiac output SVR=Systemic vascular resistance
  • 3. Category Systolic Blood Pressure(mmHg) Diastolic Blood Pressure(mmHg) Pre-hypertension 120-139 80 Hypertension – Stage 1 140-159 90-99 Hypertension – Stage 2 160-179 100-109 Hypertension – Stage 3 >180 >110 CATEGORIES OF HYPERTENSION ACCORDING TO EUROPEAN SOCIETY OF CARDIOLOGY.
  • 4. Types of Hypertension Essential Secondary A disorder of unknown origin affecting the Blood Pressure regulating mechanisms Secondary to other disease processes RISK FACTORS- •Hyperlipidaemia –more LDL content •Tension and stress •Smoking-more nicotine intake •Diabetes mellitus •Imbalance between vasoconstrictor and vasodilators peptides
  • 7. DIURETICS : EXAMPLES:Thiazides: chlorthalidone High ceiling:Furosemide K+ sparing:Spironolactone, MOA: Act on V-2 receptor in kidneys (vasopressin receptor) having an antediuretic function---- leads to diuresis----increased secretion of Na & H2O decrease in blood volume ----decreased CO-- --decreased BP. Adverse Reactions •dizziness, •electrolyte imbalance/depletion, •hypokalemia, •hyperlipidemia, •hyperglycemia (Thiazides) Contraindications •hypersensitivity, •compromised kidney function •hyponatremia
  • 8.
  • 9. Central Sympatholytics (a-2 Agonists) Drugs: clonidine, methyldopa Site of Action:CNS medullary ,cardiovascular centers MOA: CNS a-2 adrenergic stimulation---- autoinhibitory feed back mechanism---- decreased sympathetic outflow----decreased norepinephrine release----vasodilatation---- decreased PR---- decreased BP. Adverse Effect:dry mouth; sedation; drowsiness;nasal congestion SYMPATHOLYTIC DRUGS a-1 Adrenergic blockers (Antagonists) Drugs:Prazocin,Terazocin Site of Action: peripheral arterioles, smooth muscle MOA:Blocks a-1 receptor(in post synaptic neurone as well as in vascular smooth muscles)---- cause vasodialatation due to relaxation of vascular smooth muscles---- decreased PR----also reduces preload by pooling of blood----decreased CO ---- decreased BP. Adverse Effects:nausea; drowsiness; postural hypotension;headache
  • 10. b -ADRNERGIC BLOCKERS(ANTAGONISTS) Drugs: Non Selective– Propranolol,Timolol, Pindolol Cardioselective –Atenolol, Metoprolol(acts only on beta-1 receptor ) Site of Action: heart,kidney. MOA: 1.heart:blocks b -1receptor---reduce heart rate ---- decreased CO---- decreased BP 2.kidney:decreased renin production(mediated by b- 1 receptor)----depresses RAS system---- decreased PR---- decreased BP Advantages:No postural hypotension;No salt and water retention Low incidence of side effects Adverse Effects:impotence; bradycardia; fatigue; exercise intolerance Contraindication: asthma;bradycardia;hypersensitivity
  • 11.
  • 12. CALCIUM CHANNEL BLOCKERS (CCBs) Drugs: verapamil ; nifedipine ; diltiazem ; amlodipine:felodipine Site of Action- Vascular smooth muscle K Ca Na MOA:Blocks long acting voltage sensitive calcinm channels Advantages: No sedation or other CNS effects Can be given to asthma patients & angina patients No impairment of renal perfusion No deleterious effect on uric acid level& electrolyte balance Side effects: flushing; headache; tachycardia; peripheral oedema gastroesophageal reflux Contraindications: Congestive heart failure; Pregnancy and lactation
  • 13. DRUGS ACTING ON RENIN ANGIOTENSIN SYSTEM (RAS) 1ACE inhibitors: captopril;enalapril; lisinopril 2 renin inhibitors: Aliskiren; remikinen 3 AT1 receptor antagonists:losartan ;candesartan 1st line of Drug: No postural hypotension or electrolyte imbalance (no fatigue or weakness) Safe in asthmatics and diabetics Prevention of secondary hyperaldosteronism and K+ loss Reverse the ventricular hypertrophy and increase in lumen size of vessel No hyperuraecemia or deleterious effect on plasma lipid profile Side effects: Dry cough; Steep fall in BP with 1st dose Skin rash Angioneurotic oedema