INTRODUCTION

Maham Azmat
Roll # 17007
Pharm-D 2nd Proff.
M Islam College of Pharmacy,Gujranwala
Presenting To:
Dr. Shumaila Shafique
SUBJECT: Pharmacology & Therapeutics-I

TOPIC: Heart Failure and its Drug

Classification
 CONTENTS
Definition of Heart Failure
Types of Heart Failure
Causes of Heart Failure
Symptoms of Heart Failure
Cardiac Performance
Drugs to treat Heart Failure
Classification of Drugs
ACE Inhibitors
Beta-Adrenoreceptors Blockers
 HEART FAILURE

Heart failure is complex disorder in which cardiac

output is inadequate to provide the oxygen needed for
the body.
 TYPES

1-Unilateral Heart Failure (Right or Left side)

2-Bilateral Heart Failure (both sides)
 CAUSES
 LOW OUTPUT FAILURE

Systolic dysfunction:
-Decreased cardiac output, contractility, ejection fraction.

Diastolic dysfunction:
-Hypertrophy &s stiffening of Myocardium
 HIGH OUTPUT FAILURE
Demands of the body are so great that even increased
cardiac output is insufficient.

CAUSES:
Anemia, Arteriovenous shunts, beriberi.
 SYMPTOMS
Trachycardia
Dyspnea
Cardiomegaly
Peripheral & Pulmonary Edema
Fatigue
 CARDIAC PERFORMANCE

Preload:
Volume of blood in ventricles at EDV.

 Afterload:
Pressure need to open aortic valve.
DRUGS TO TREAT HEART FAILURE

CLASSIFICATION

ACE Inhibitor AR Blockers

Captopril​ Candesartan​
Enalopril​ Losartan​
Fosinopril​ Telmisartan​
Lisinopril​ Valsartan​
Quinapril​
Ramipril​
CLASSIFICATION OF DRUGS
Beta-AR Blockers Diuretics
Atenolol​ Bumetanide​
Carvedilol​ Furosemide​
Metoprolol​ Hydrochlorothiazide​
Metolazone​
CLASSIFICATION OF DRUGS
Aldosterone Vasodilators Inotropic
Hydralazine​ Agents​
Antagonists Digoxin​
 Eplerenone​ Isosorbide- Dobutamine​
 Spironolacton dinitrate​ Inamarinone​
e​ Isosorbide- Milrinone​
  mononitrate​
Sodium 
Nitroprusside​
 ACE INHIBITORS
Teprotide
Versatile drugs like Captopril
Reduce afterload
Reduce preload (Vasodilation, netriuresis)
Reduce Sympathetic activity of Angiotensin-II on NE
 Inhibit Renin-Angiotensin-Aldosterone System
Reduces Blood pressure
ACE INHIBITORS
Renin-Angiotensin-Aldosterone System
 ANGIOTENSIN-II
Agiotensin-II
Induce CVS changes
Stimulate Adrenal cortex to secrete Aldosterone
Aldosterone
Vasoconstriction
Increase reabsorption (water & sodium)
Increase Blood volume & conc. of salts
Inc. Blood pressure(more work load on heart)
If this is persistant, Heart Failure can occur.
 MECHANISM OF ACTION OF ACE
INHIBITOR
INITIAL FALL
ACE Inhibitors inhibit ACE enzyme
Conversion of Angiotensin I to Ang II stops
Dec. water & sodium reabsorption
Dec. blood volume
Blood vessels relax
Dec. blood pressure
 MECHANISM OF ACTION OF
ACE INHIBITOR
ACE inhibitors causes increase in renin release
 overproduction of Ang I.
conversion to Ang II is blocked
Ang I is diverted to produce Ang (1-7) which has
vasodilator property
contribute to B.P lowering action of ACE inhibitors.
 ACE INHIBITORS
CAPTROPIL
Sulfhydryl containing dipeptide
Substitute of proline
Abolish Pressor action of Ang-I
Bradykynins (NO, prostaglandin) enhance ACE
Inhibitor vasodepressor activity
Lowers B.P depending on Na status and RAS activity
CAPTORPIL

In CHF, renin level is high that cause inc. in B.P

Hypertension –RAS is overactive (20%)
Captropil doses cause fall in B.P
Induce hypotension.
PHARMACOKINETICS
70% absorbed.
 Presence of food in stomach reduces its
bioavailability.
 Penetration in brain is poor.
It is partly metabolized and partly (renal) excreted
unchanged in urine.
Peak action- 1hr
The plasma t½ is ~2 hours, but actions last for 6–12
hours
ADVERSE EFFECTS
Hypotension
Hyperkalaemia
Cough
Angioedema
Dysgeusia
Foetopathic
Headache, dizziness, nausea and bowel upset
Acute Renal failure
INTERACTION
Diuretics
Indomethacin & NSAIDS
Hyperkalaemia
Antacids
DOSE
25 mg BD
 Inc.gradually upto 50 mg TDS according to
response. CHF patients -6.25 mg BD initially.
Tablets should be taken 1 hr before or 2 hr after a
meal.
THERAPEUTIC USES

Hypertention
CHF
Scleroderma crisis
MI
Other drugs of ACE Inhibitor
Features:
BETA-ADRENORECEPTOR
BLOCKERS

Effective in lowering blood pressure

Propanalol
Use in hypertension and heart disease
Reduce mortailty in MI and Heart failure
Decrease Systolic dysfyntion in Heart failure
TYPES

Beta 1- Heart
Beta 2- Lungs, liver, Skeletal muscles
Beta 3- Urinary bladder, Gall bladder
MECHANISM OF ACTION

Inhibit sympathetic NS
By blocking catecholamines ( E , NE) to bind with
beta-adrenergic reeptors
Effects:
Beta-1 – dec. heart rate and vasodilation
MECHANISM OF ACTION
Propanolol
Non-Selective Beta-Antagonist
Inotropic & Chronotropic
Decrease cardiac output
Depresses sinoatrial activity
During exercise or stress, decrease heart rate
Cardiac output, load on heart dec. oxygeen
consumption dec by bloackage of B1 receptor
PHARMACOKINETICS
Well absorbed, metabolized by liver, excreted in urine
 Can pass blood brain barrier
25% reach systemic circulation
High First pass metabolism
Plasma half life is from 3-6 hrs.
DOSE
Oral—10 mg Twice a day to 160 mg (average 40–160
mg/ day).
 i.v.—2 to 5 mg injected over 10 min with constant
monitoring.
Other Beta-blockers
THERAPEUTIC USE
Hypertention
Angina Pectoris
Mayocardial Infarction
Arythmias
SIDE EFFECTS
Bradycardia
Hypotention
Bronchoconstriction
Drowsiness , Fatigue
Weakness or dizziness
Cold hands and feet
Dry mouth, eyes and skin
Trouble breathing
Memory loss, confusion, hellucinations
REFERENCES
Jaypee-Essentials of Medical Pharmacology
Katzung-Basic and Clinical Pharmacology
Lippincott illustrated reviews