1-3 Henderson Flashcards
Lidocaine
Local anaesthetic acting on VGNa channels
Stabilise inactivated state and make it harder to reactivate
Acts on intracellular surface Shows use dependence
Verapamil
L-type Ca channel blocker
Phenylalkylamine
Binding site at S6 and part of S5-6 loop
Class 4 antidysrhythmic agent
Diltiazem
Ca channel blocker
Benzothiazepines
Block from outside
Modulate DHP binding
Propanolol
Non-specific B-antagonist
Blocks the effect of catecholamines
Quinidine
Anti-dysrhythmic drug
Class 1A
Block VGNa channels
Increased AP duration, intermediate rate of association/dissociation
Procainamide
Anti-dysrhythmic drug
Class 1A
Block VGNa channels
Increased AP duration, intermediate rate of association/dissociation
Lidocaine (Class)
Anti-dysrhythmic drug
Class 1B
Block VGNa channels
Decreased AP duration, fast rate of association/dissociation
Flecainide
Anti-dysrhythmic drug
Class 1C
Block VGNa channels
No effect on AP duration, slow rate of association/dissociation
Propanolol/Atenolol
Antidysrhythmic agent
Class2
Sympathetic antagonists (B blockers)
Digoxin / Digitoxin
Cardiac glycosides Antidysrhythmic Alleviate oedema Inhibit NaKATPase pump Increase intracellular Na, reduce driving force for Ca exit, Ca builds up in cell
Oubain
Cardiac glycosides
Inhibit NaKATPase pump
Used experimentally - too powerful to be used clinically
Bisoprolol / Carvedilol
3rd generation B1 antagonist
Used in stable heart failure
Limit damaging effects of chronic stimulation by catecholamines and improve cardiac function
(reverse desensitization and downregulation of B adrenoceptors)
Inodilators
Phosphodiesterase inhibitors Raise intracellular cAMP Mimic B stimulation Can lead to dysrhythmias Vasodilation in smooth muscle, decreases afterload on heart
Milrinone
Inodilator Phosphodiesterase type 3 inhibitor Raise intracellular cAMP cGMP inhibited Dysrhythmias - short term treatment of severe heart failure
Sildenafil
Inodilator
Phosphodiesterase type 5 inhibitor
Raise intracellular cAMP
cGMP specific
Caffeine
Methylxanthine (caffeine/theophylline)
Non selective phosphodiesterase inhibitors
Also adenosine A1 A2 antagonists –> release of Ca from intracellular stores
Positive ionotropic and chronotropic effects
Pimobendan
Inodilator
Calcium sensitizer
Increase cardiac Ca binding efficiency to troponin without more energy requirement
Peripheral vasodilation (PDE3 inhibitor)
-canine dilated cardiomyopathy
-canine mitral valve regurgitation
Levosimendan
Inositol/Ca sensitizer
Licensed for human use in heart failure in the UK