Nitrates
What clinical use is Glyceryl trinitrate (Nitroglycerine) used for?
- unstable angina
- LVF associated w/ MI
- hypertension during heart surgery
What are the adverse effects of Nitrates?
- Throbbing headache
- Palpitation
- Orthostatic hypotension
- Flushing
Which specific calcium channel blocker can abort acute angina?
Nifedipine
What is the mechanism of selective beta1 blockers (Atenolol/Metoprolol)?
reduce heart rate and contractility --> reduce cardiac work --> lesser O2 demand
Ranolazine and Trimetazidine are both pFOX inhibitor that does what?
Inhibits late NA+ current in the myocardium resulting in reduction of ...
-oxygen demand
- cardiac work
-contractility
What form can Nitroglycerine be administered?
-Sublingual tablets (act for 10-20min)
- Sublingual spray
- Oral tablets (act for 4-6hrs)
- Sustained released tablets
- Transdermal patch (acts up to 24hrs)
*Tolerance develops after 8-10hrs
- I.V. Infusion
What are some examples of DHP calcium channel blockers?
Nifedipine
Amlodipine
What are the adverse effects of selective beta1 blockers?
-increased heart size
- longer ejection period
What is Ranolazine and Trimeazidine used for in the clinical setting?
angina prophylaxis
What clinical use is Isosorbide dinitrate used for?
- Acute anginal pain via sublingual formulations
- Trandsermal formulations for prophylaxis
Which drug should not be used with nitrates due to result of severe hypotension?
Sildenafil
What is the clinical use for calcium channel blockers?
prophylaxis of angina
What is the clinical use of selective beta 1 blockers?
-prophylaxis of atherosclerotic angina
- prevents exercising induced angina
What is the heart rate inhibitor that reduces heart rate leading to reduced oxygen demand and prolongation of diastole, which improves O2 supply?
Ivabradine
What clinical use is Isosorbide mononitrate used for?
Used for prophylaxis of angina via oral tablets
What are some examples of non-DHP calcium channel blockers?
Varapamil
Diltiazem
What are the adverse effects of calcium channel blockers?
Common
-constipation
-pretibial edema
-flushing
-dizziness
Serious-heart failure
-AV blockade
-Sinus node depression
What drug can be useful in combination with selective beta1 blockers?
Nitrates
-evoke tachycardia and increase of cardiac force, which is then prevented by beta1 blockers
What is Ivabradine used for clinically?
-Improves exercise intolerance in stable angina
- Used for angina prophylaxis
-Can be used in cases where Beta blockers are not tolerated/contraindicated
What is the mechanism for Nitrates?
release nitric oxide in the body --> increase in cyclic GMP cell levels --> smooth muscle relaxation --> vasodilation that preferentially dilates in veins over arteries = decrease of preload on the heart
What is the mechanism of calcium channel blockers?
- block voltage dependent L-type calcium channels
- relax vascular smooth muscle
- reduce heart rate and contractility (non-DHP)
- cause coronary dilation resulting in increased oxygen supply to the myocardium