Cardiovascular Pharmacology (Drugs) Flashcards
What substances can mimic the effect of sympathetic stimulation of the heart?
- Cholera toxin: Stimulates β1-associated G-protein
- Forskolin: Adenylyl cyclase agonist
What are Vaughan Williams’ classifications of antidysrhythmic drugs?
- Class I: Voltage-gated Na+ channel blockers
- Class II: Sympathetic antagonists (β-blockers)
- Class III: Prolonge action potential
- Class IV: Ca2+ channel blockers
What are the subdivisions of class I drugs?
- Class Ia: Intermediate association/dissociation time. Displays both Ib and Ic properties.
- Class Ib: Fast association/dissociation time. Binds to Na+ channels during depolarisation phase of AP and prevents premature activation.
- Class Ic: Slow association/dissociation time. Binds to Na+ channel throughout AP. Has no effects on AP waveform but slows down rate of AP conduction.
What are examples of Ia antidysrhythmic drugs?
- Quinidine
- Procainamide
What are examples of Ib antidysrhythmic drugs?
Lidocaine
What are examples of Ic antidysrhythmic drugs?
- Flecainide
- encainide
What are examples of class II antidysrhythmic drugs?
- Propanolol
- Atenolol
- Metoprolol
What are examples of class III antidysthythmic drugs?
Amiodarone
What are examples of class IV antidysrhythmic drugs?
- Verapamil
What are the different types of drugs used to treat heart failure?
- Cardiac glycosides
- β agonists
- β antagonists
- Inodilators
- ACE inhibitors
- Calcium sensitisers
What are examples of cardiac glycosides?
- Digoxin
- Ouabain
What are examples of β1 agonists used in heart failure?
Dobutamine
What are the clinical uses of β1 agonists in heart failure?
- Shock
- Heart failure in absence of hypertension
What are examples of β-antagonists in heart failure?
- Bisoprolol
- Carvedilol
What are inodilators?
Phosphodiesterase inhibitors
What are the types of phosphodiesterases?
- Type I: Ca2+/calmodulin-dependent
- Type II: cGMP-stimulated
- Type III: cGMP-inhibited
- Type IV: cAMP-specific
- Type V: cGMP-specific
What are examples of type III phosphodiesterase-specific inodilators?
Milrinone
What are examples of type V phosphodiesterase-specific inodilators?
- Dipyridamole
- Sildenafil (viagra)
Which type of PDE is most widely targeted to treat heart failure?
Class III
What is the mechanism of methylxanthines in heart failure?
- Inhibition of PDE causes increased [cAMP] and sympathomimetic effects on heart.
- Inhibition of adenosine A1/2 receptors causes release of intracellular Ca2+.
What is an example of a Ca2+ sensitiser?
Levosimendan
What are the classes calcium channel antagonists?
- Dihydropyridines
- Phenylalkylamines
- Benzothiazepines
What are examples of dihydropyridines?
Nifedipine
What are examples of phenylalkylamines?
Verapamil
What are examples of benzothiazepines?
Diltiazem