Drugs for ischemic heart disease Flashcards
What is angina
Angina pectoralis is when the supply of coronary blood and oxygen is insufficient to meed the demands of the myocardium
Presents clinically as crushing chest pain, especially on exertion
Types of angina
- Stable artherosclerotic angina : plaque formation that occludes the lumen
- Vasospastic angina (in women for no apparent reason)
- unstable angina: prone to rupture and thrombus formation
What are the classes of drugs used to treat angina
Demand:
- Contractility- Calcium channel blockers, beta blockers
- Heart rate- beta blockers
Supply:
- Vasodilators- nitrates, glyceryltrinitrate
- Atherosclerosis drugs: Lipid lowering (statin) + post ami antithrombotic drugs (aspirin and clopidogrel)
Name the shortterm vasodilator and the route of admin
glyceryl trinitrate, administer sublingually (rapid onset ,1 hr half life), or transdermal patch (longer half life)
What is the mechanism of action of vasodilators
Glycerol trinitrate reduced by GSH will release nitric oxide.
Nitric oxide increases activity of guanylyl cyclase
This causes cGMP which causes inactivation of myosin light chain
MLC is then relaxed
Venodilation, arteriodilation–> decreased blood pressure (preload and after load) reduction in demands of myocardium
What are the adverse effects of vasodilators
- reflex tachy due to drop in bp
- hypotension due to venodilation
- meningeal artery dilation causing headaches
What are vasodilators usually combined with and why
CCB or BB because they cause opposing effects, especially with regards to reflex tachycardia by depressing cardiac function
What is the MOA of beta blockers
Beta blockers, stop adenylyl cyclase –> less cAMP–> less PKA–> less CICR
What is the MOA of calcium channel blockers
DHP: nifedipine
Block calcium channels of the heart myocardium and smooth muscle, less CICR, less contractility and tone
reduced bp , reduce contractility : for hypertension and angina
non-DHP: verapamil, diltiazem
Block SA node AV node, prevent rentry supraventricular tachy
- anti-arrhythmic effects
What are differences between the DHP and non DHP CCBs
- Cardiac depressant
- Blood pressure lowering
- vasodilator activity
- Cardiac depressant: Verapamil> diltiazem>nifedipine
- BP lowering all equal
- Vasodilator activity: nifedipine>diltiazem > verapamil
Adverse effects of CCB
Bradycardia, AV heart block, worsen heart failure
Why is GTN not used LT
tolerance, receptors sensitised and subsequently effect is not as trong