Congestive Heart Failure Pharmacology-2

1. Cardiac glycoside ACE INHIBITORS Angiotensin
Antagonist ARBs
β- Adrenergic Blockers Diuretics Calcium channel blockers
Digoxin/ Drug
used
Increase force of
cardiac contraction
Lisinopril,
benazepril,
Ramipril etc.
Losartan, irbesartan,
valsartan,
telmisartan, etc
Carvedilol, Metoprolol,
Bisoprolol, Bucindolol
Furosemide,
Hydrochlorothiazide,
spironolactone,
Triameterene Amiloride
MOA 1. Inhibits Na-K-
ATPase enzyme
2. Indirectly
accumulates Ca2+
3. Reduce the
sympathetics out
flow from the CNS
4. Reduce the heart
rate and relief the
symptoms
1. Inhibits
pressor action
of A-I
2. Blocks
formation of
A-H
3. Block kinase-II
decrease
degradation of
kinin
Prolong the
effect of kinin
1. For patient who
are unable to
tolerate the ACE
inhibitors
2. Act on the same
hormonal
pathway as the
ACE inhibitors,
3. Blocks the action
of angiotensin II
as its receptors
site directly
1. Reduction in
damaging
sympathetic influence
in the heart
(tachycardia, LVEDP,
remodeling, necrosis)
2. Inhibition of renin
release
3. Berta blocker
improve EF
4. Peripheral
vasodilatation via
(Carvedilol)
1. Block the reabsorption
of Na+, K+, Cl- from
glomerular filtrate at
proximal tubules and
ascending loop of
henle
2. Spironolactone binds
with aldosterone
lowering the blood
pressure
3. Reduction of
facilitation of
sympathetics nervous
system
1. Calcium channel are
have 5 subtypes L,N,T,P,
and R
2. L-type in cardiac and
smooth muscle cells
It blocks voltage sensitive L-
type Ca channels by binding
to specific site on the a-1
subunit.
Prevent entry of Ca into cell
No excitation –coupling
reaction in heart and
vascular smooth muscles
Indication LV dysfunction, atrial
fibrillation
1. Hypertension
2. Intolerance to
ACE inhibitors
3. Post—MI
patients
Treatment of
hypotension shock,
bronchospasm, and some
types of asthma
4. Prescribed for patient
who have fluid
retention
5. Elimination sign and
symptoms of fluid
retention
6. Produces symptomatic
relief more rapidly
Pharmacokine
tics
1. Lipid soluble,
polar
2. Presence of food
delays absorption
3. Volume of
distribution is
larger
4. Metabolism in
liver
5. Primarily excreted
unchanged by
glomerular
filtration
6. Therapeutics
index: 1.5—3
1. 70% orally
2. Presence of
food decrease
absorption
3. Poor BBB
penetration
4. Partly
metabolized
and excreted
unchanged
urine
5. Plasma t1/2 –
2hrs, action
last for 6—12
hrs
1. Losartan—Oral
bioavailability:
33% half—life:
.2hours
2. All compound
are
administration
by oral route
only
1. Rapidly absorbed
after injection or
passage through
mucous membrane
2. Metabolized in the
liver and excreted in
the urine
1. Well absorbed through
Git
2. First pass metabolism
3. Highly bound to plasma
proteins
4. Metabolized in liver
5. Excreted through urine
Dose 1. Oral—0.0625mg,
0.125mg, and
0.25mg
2. Parenteral—
0.25mg/mL
3. Oral dose
effective within
34—45 minutes
4. Digitalizing dose,
effect within 35—
45 minutes last
Metoprolol- 12.5 to 50
mg BD
Bisoprolol:- 2.5-10mg OD
Bucindolol:- 12.5 -50mg
BD
The dose is increase every
2-4 week till a target dose
is achieved uses: CHF,
HTN, Angina pectoris,
cardiac arrhythmias
1. Therapy is initiated
with a low dose of 20-
40mg/day
2. The dose is increased
till sign and symptoms
of patient is reduced
 Oral dose- 20-
120mg/day, the action
starts within in 2 hours
and may last for 96-
8hrs or more
 Acute pulmonary
edema slow iv 4
mg/min to a dose of 40
mg
5-10mg orally once daily
Adverse effect 1. Cardiac—AV
block,
Bradycardia,
Ventricular,
extrasystole,
Arrhythmias
2. Central Nervous
System
3. Gastro Intestinal
Cough, Fetal
damage, Rashes,
Acute renal
failure,
Angioedema
Hyperkalemia,
Hypotension,
teratogenicity
1. Arrhymias,
hypertension,
palpitations, angina,
dyspnea
2. Nausea and vomiting
3. Headache and
sweeting
Drowsiness, paresthesia,
disorientation, renal stone
1. Postural hypotension
2. Palpitation
3. Reflex tachycardiac
4. Edema
5. Dizziness
6. Constipation
7. Sedation
8. Headache
9. Fatigue
Contra
indication
Hypokalemia, MI,
Myxoedema,
Ventricular
Hyperkaliemia 1. Bilateral Renal
Artery Stenosis
2. Hypersensitivity
1. Phenchromocyto
ma
2. Tachyarrhythmia’
s or ventricular
fibrillation
3. Hypovolemia
4. Halogenated
hydrocarbon
Liver cirrhosis
NH3 increased
encephalopathy
1. Heart failure
2. Bradycardia
3. Atrioventricular block
4. Dihydropyridine calcium-
channel blockers should
not be used in people
with uncontrolled heart
failure

2. general
anesthetics
Uses CCF, Cardiac HTN, CHF, MI 1. Hypertension
2. Congestive
Heart Failure
3. Myocardial
Infraction
1. Uses in treatment of
Glaucoma
2. Reducing intraocular
pressure
1. Angina pectoris
2. Supraventricular
arrhythmias
3. Hypertension
4. Migraine
Brands
available
Digitran Tab, Digox
Tab, Digoxin Inj.
Lanoxin Tab
Acezide Tab,
Acetan tab,
Capotril tab,
Capotril-H Tab
Adpace 4 Tab(sun),
candesar Tab(rbxy),
Diovan cap(Novartis)
1. Carvedilol Circa
tab (intas), cardivas
tab(sun), Carlo
tab(cipla)
2. Metoprol Betaloc
H tab
3. Bisoprolol Iodoz
tab
Amifru, amimide tab(gsk) 1. Phenylalkylamines—
calan, isoptin
2. Benzothiazepines-
cardizem CD Dilactor