Class cardiotonic
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CARDIOTONIC DRUGS
Dr. RAGHU PRASADA M SMBBS,MDASSISTANT PROFESSOR DEPT. OF PHARMACOLOGYSSIMS & RC.
Inotropic Definition
Force of myocardial contractionAn ideal cardiotonic agent should not
increase heart rate & should be devoid of toxic effects.
Positive inotropic drug: increases force of contractions
Increase force of myocardial contractionCauses improved heart’s pumping abilityNegative inotropic drug: decreases force
of contraction
Positive inotropic drugs
Cardiac glycosides: Digitoxin, Digoxin
β-adrenergic agonists (New dopamine receptor agonist): dopamine, Dobutamine, Dopexamine
Phosphodiesterase inhibitors : Amrinone Milrinone
Source & Chemistry of CG
SOURCE GLYCOSIDES
1.D.PURPUREA - Digitoxin, Gitoxin, Gitalin 2.D.Lanata - Digitoxin, Gitoxin
Aglycon consist of cyclopentanoperhydrophenanthrene (steroid) ring 5 or 6 membered unsaturated lactones ring.
Mechanism 0f action
Digitalis increase force of cardiac contraction by a direct action independent of innervations.
It selectively binds to extra cellular face of membrane associated NA+K+ ATPase of myocardial fibres & inhibits this enzyme.
Inhibition of this cation pump results in progressive accumulation of NA+ intracellularly.
This indirectly results in intracellular Ca+ accumulation.
Therapeutic use
CHF Cardiac Arrhythmias :
Atrial fibrillation, Atrial flutter (AFL) Proxysmal supraventricular tachycardia (PSVT
Precaution & contraindications :-HypokalemiaThyrotoxicosis
Adverse effects
Extra cardiac – anorexia, nausea, vomiting, abdominal pain
are usually reported first , are due to gastric irritation, mesenteric vasoconstriction & CTZ stimulation.
Cardiac -- almost every type of arrhythmia can be
produced by digitalis ; pulses big minus , nodal & ventricular extra systoles, ventricular tachycardia & terminally fibrillation.
β -Adrenoceptor agonists They are used intravenously in CHF emergencies Example of β -Adrenoceptor agonists Dobutamine • Exciting β1 Adrenoceptor → positive inotropic
action →the volume of output↑• Exciting β2 Adrenoceptor→dilate the vascular →
afterload↓
have benefits within short time
Phosphodiesterase- inhibitorsⅢ
Inodilator / inodilating drugsInhibiting the activity of PDE → cAMP↑→ causes an Ⅲincrease in myocardial contractility and vasodilatation →total peripheral resistance →cardiac output ↑ Examples: Amrininone: Inhibits the excess product of NO, TNF and affects the neurohormone, anti-the forming of thrombus Milrinone: stronger 20 time
Uses
Congestive heart failure Shock conditions-hypovolumic,
septic, cardiogenic Cardiac emergencies