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Scientific basis of phytotherapy
PHG-803
Topic :Cardiac glycoside
Course incharge :Dr.Asma wazir
Aignment submitted by:Sanober kamal
Cardiac glycoside
 Cardiac glycoside consists of a large family of naturally
derived compounds. several plants which contain a
small group of C23 or C24 steroidal glycoside
possesses slowing and strengthening effect on failing
heart .such compounds are known as cardiac glycoside
.
 It is of two types ,in one case a five-membered lactone
ring is attached to the steroid at C -17 which is known
as Cardenolides and in other case a six-membered
lactone ring is attached to the steroid at C-17 which is
known as bufadienolide .
Mechanism of Action
 Cardiac glycoside gives positive inotropic effect by
inducing the inhibition of Na+/K+ ATPase ,which lead
to increase the level of intracellular Na+ ions.Due to
this the activity of Na+/Ca+ exchanger is reduced and
therefore the intracellular concentration of Ca++ ions
are increased and thus gives the positive inotropic
effect.[1]
Pharmacological properties of
cardiac glycoside
1. Cardiac glycoside increase the force and velocity of
myocardial systolic contraction by direct action on
myocardium .
2. In CHF, it causes reflex reduction in peripheral resistance
by increasing myocardial contractility .
3. In patient with CHF ,cardiac glycosides increase the
myocardial contractility ,increases the cardiac output,
decreases the sympathetic tone ,slowing of heart rate .
4. In patients with no CHF ,it increases the myocardial
contractility and increase of myocardial oxygen
consumption.
5. In Patients with heart failure ,the cardiac
glycoside decrease the venticular end
diastolic pressure ,increase myocardial
contractility, produce net decrease or no
change in myocardial O2 consumption.
6.Cardiac glycoside do not decrease coronary
blood flow and cardiac glycoside have minor
inotropic effect on skeletal muscle .
7.Low concentration of cardiac glycoside
produce little effect on action potential but
toxic concentration cause progressive loss of
action potential ,decrease rate of risk of
action potential [2]
Uses of cardiac glycoside
 It is drug of choice for CHF (congestive heart failure)
 It is also a drug of choice for controlling rapid
ventricular rate in patient with atrial fibrillation and
flutter
 It is used primarily in prophylactic management and
treatment of heart failure
 It is also used to treat and prevent paroxymal artial
tachycardia [2]
Dosage of cardiac glycoside
 Cardiac glycosides are administered orally. For
emergency cases it is administerd by IV injections.it
should not be given Sc.
 Cardiac glycosides have low therapeutic index
therefore catious dosage determination is essential
 The dosage of these drugs must be reduced in patients
with renal impairments [2]
Dosage Forms & Strengths of cardiac
glycoside(digoxin,lanoxin) available in the
market
1.oral solution
0.05mg/mL
2.injectable solution
0.1mg/mL
0.25mg/mL
3.tablet
0.0625mg (Lanoxin only)
0.125mg
0.1875mg (Lanoxin only)
0.25mg
Contraindication
 Cardiac glycoside are contraindicted in patient with
venticular fibrillation
 patient with known hypersensitivity to digoxin
 Hyper calcemia
 Hypokalemia
 Venticular arrhytmia
 Carotid sinus hypersensitivity.[3]
Side effect of cardiac glycoside
 GIT: digoxin may cause anorexia,nausea,vomiting,and
diarrhea.
 CNS:it produce visual
disorders,headache,weakness,diziness,confusion,ment
al disturbances like anxeity,depression ,hallucination
 Cardiac:all type of arrhytmia,venticular
ectopics,severe bradycardia,AV block
 Other :prolong use of digoxin cause
gynecomastica,skin rashes.[3]
Pharmaceutical prepration of
cardiac glycoside
1.Digoxin tablet containing 0.25mg digoxin
Digoxin/B-cyclodextrin complex(1:3) 1 mg
Lactose 87 mg
Maize starch 10 mg
Hydrolyzed starch 2 mg
Magnessium stearate 1 mg
2.Digoxin injection containing 0.5 mg digoxin
Digoxin /B-cyclodextrin complex(1:3) 2mg
Water for injection 2 ml
3.Digoxin capsule containing 0.125 mg digoxin
Digoxin 0.5 mg
Lactose 75 mg
Maize starch 10 mg
Magnessium stearate into a soft gelatin capsule 1 mg [4]
REFRENCES
1. Novel therapeutic applications of cardiac glycosides Ioannis
Prassas*‡ and Eleftherios P. Diamandis*‡
2. Am J Hosp Pharm 35:1495-1507 (Dec) 1978 Current drug therapy:
Cardiac glycosides American Hospital Formulary Service
3.CARDIAC GLYCOSIDES USES IN HEART
Ramesh Ganpisetti1*, Praneeth Chandluri2*, Dr. B.V.S. Lakshmi3, Dr. P.
Aravinda Swami4, *Corresponding Author: Ramesh Ganpisetti
Department of Pharmacy Practice, Malla Reddy Hospital, Hyderabad,
Telangana, India-500055.Email ID: ramiganpisetti@gmail.com
4. EUROPEAN PATENT APPLICATION @ Application number: 82100450.4
(9) Date of filing: 22.01.82 ©, ) Publication number: 0 056 995 A1

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Cardiac glycosides

  • 1. Scientific basis of phytotherapy PHG-803 Topic :Cardiac glycoside Course incharge :Dr.Asma wazir Aignment submitted by:Sanober kamal
  • 2. Cardiac glycoside  Cardiac glycoside consists of a large family of naturally derived compounds. several plants which contain a small group of C23 or C24 steroidal glycoside possesses slowing and strengthening effect on failing heart .such compounds are known as cardiac glycoside .  It is of two types ,in one case a five-membered lactone ring is attached to the steroid at C -17 which is known as Cardenolides and in other case a six-membered lactone ring is attached to the steroid at C-17 which is known as bufadienolide .
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  • 5. Mechanism of Action  Cardiac glycoside gives positive inotropic effect by inducing the inhibition of Na+/K+ ATPase ,which lead to increase the level of intracellular Na+ ions.Due to this the activity of Na+/Ca+ exchanger is reduced and therefore the intracellular concentration of Ca++ ions are increased and thus gives the positive inotropic effect.[1]
  • 6. Pharmacological properties of cardiac glycoside 1. Cardiac glycoside increase the force and velocity of myocardial systolic contraction by direct action on myocardium . 2. In CHF, it causes reflex reduction in peripheral resistance by increasing myocardial contractility . 3. In patient with CHF ,cardiac glycosides increase the myocardial contractility ,increases the cardiac output, decreases the sympathetic tone ,slowing of heart rate . 4. In patients with no CHF ,it increases the myocardial contractility and increase of myocardial oxygen consumption.
  • 7. 5. In Patients with heart failure ,the cardiac glycoside decrease the venticular end diastolic pressure ,increase myocardial contractility, produce net decrease or no change in myocardial O2 consumption. 6.Cardiac glycoside do not decrease coronary blood flow and cardiac glycoside have minor inotropic effect on skeletal muscle . 7.Low concentration of cardiac glycoside produce little effect on action potential but toxic concentration cause progressive loss of action potential ,decrease rate of risk of action potential [2]
  • 8. Uses of cardiac glycoside  It is drug of choice for CHF (congestive heart failure)  It is also a drug of choice for controlling rapid ventricular rate in patient with atrial fibrillation and flutter  It is used primarily in prophylactic management and treatment of heart failure  It is also used to treat and prevent paroxymal artial tachycardia [2]
  • 9. Dosage of cardiac glycoside  Cardiac glycosides are administered orally. For emergency cases it is administerd by IV injections.it should not be given Sc.  Cardiac glycosides have low therapeutic index therefore catious dosage determination is essential  The dosage of these drugs must be reduced in patients with renal impairments [2]
  • 10. Dosage Forms & Strengths of cardiac glycoside(digoxin,lanoxin) available in the market 1.oral solution 0.05mg/mL 2.injectable solution 0.1mg/mL 0.25mg/mL 3.tablet 0.0625mg (Lanoxin only) 0.125mg 0.1875mg (Lanoxin only) 0.25mg
  • 11. Contraindication  Cardiac glycoside are contraindicted in patient with venticular fibrillation  patient with known hypersensitivity to digoxin  Hyper calcemia  Hypokalemia  Venticular arrhytmia  Carotid sinus hypersensitivity.[3]
  • 12. Side effect of cardiac glycoside  GIT: digoxin may cause anorexia,nausea,vomiting,and diarrhea.  CNS:it produce visual disorders,headache,weakness,diziness,confusion,ment al disturbances like anxeity,depression ,hallucination  Cardiac:all type of arrhytmia,venticular ectopics,severe bradycardia,AV block  Other :prolong use of digoxin cause gynecomastica,skin rashes.[3]
  • 13. Pharmaceutical prepration of cardiac glycoside 1.Digoxin tablet containing 0.25mg digoxin Digoxin/B-cyclodextrin complex(1:3) 1 mg Lactose 87 mg Maize starch 10 mg Hydrolyzed starch 2 mg Magnessium stearate 1 mg 2.Digoxin injection containing 0.5 mg digoxin Digoxin /B-cyclodextrin complex(1:3) 2mg Water for injection 2 ml 3.Digoxin capsule containing 0.125 mg digoxin Digoxin 0.5 mg Lactose 75 mg Maize starch 10 mg Magnessium stearate into a soft gelatin capsule 1 mg [4]
  • 14. REFRENCES 1. Novel therapeutic applications of cardiac glycosides Ioannis Prassas*‡ and Eleftherios P. Diamandis*‡ 2. Am J Hosp Pharm 35:1495-1507 (Dec) 1978 Current drug therapy: Cardiac glycosides American Hospital Formulary Service 3.CARDIAC GLYCOSIDES USES IN HEART Ramesh Ganpisetti1*, Praneeth Chandluri2*, Dr. B.V.S. Lakshmi3, Dr. P. Aravinda Swami4, *Corresponding Author: Ramesh Ganpisetti Department of Pharmacy Practice, Malla Reddy Hospital, Hyderabad, Telangana, India-500055.Email ID: ramiganpisetti@gmail.com 4. EUROPEAN PATENT APPLICATION @ Application number: 82100450.4 (9) Date of filing: 22.01.82 ©, ) Publication number: 0 056 995 A1