Pharm II (Antianginal drugs) 1a
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What are some Peculiarities of Coronary circulation?
- 1.Functional end arteries
- 2.Maximum oxygen extraction (low O2 concentration in venous blood)
- 3. Increased blood flow during diastole (enters through the coronary arteries)
Terms: Angina due to
Printzmetals Variant angina (Beta Blockers can causes a small vasoconstriction, thus they are contraindicated here)
Chronic Stable Angina (AKA Angina Pectoris or Angina of effort)
What drugs increase O2 delivery?
What drugs decrease O2 demand?
- -Coronary Vasodilators--- Ca++ entry blockers
- -Anti-thrombotic drugs
- -Vasodilators--- Organic Nitates and Ca++ entry blockers
- -Cardiac depressents- Beta blockers
What are the Antianginal agents?
-CALCIUM CHANNEL BLOCKERS
----OTHERS : Ranolazine, Trimetazidine, Nicorandil
Name the Nitrates/ Nitrites
How do they work?
What is the Quickest mode of treatment?
- 1.Isosorbide dinitrate
- 3.Isosorbide mononitrate
- 4.Amyl nitrite
They release NO--> which increases cGMP concentrations--> leading to vasodilation.
- Fastest action if given Sublingually, because it is LIPID SOLUBLE and can cross through membranes fast, and does NOT pass the liver circulation.
What are Nitrodilators actions?
- -Reduces preload and afterload
- -Decreases oxygen demands
- -Prevents vasospasm
- -Improves subendocardial perfusion-- helps develope colateral blood supplies
- -Increases Oxygen delivery
What are Nitrates degraded by?
- -Nitrates are denitrated by glutathione reductase
- -Denitrated metabolites are less active but longer acting.
What are the adverse effects of Nitrates/ Nitrites
How is tolerance generated?
- throbbing headache--inclination that drug is working
- methemoglobinemia-- Fe3+--losses its O2 carrying capasity. If it gets too high can lead to cyanosis and ischemia. Has a higher affinity for Cyanide.
- Tolerance-- activation of thimpathietics and volume expansion. This decreases Nitrates effect. Prevent with NItrate free periods (10-12 hours)
What are the clinical uses of Nitrates?
- -CCF and LVF
- -Cyanide poisoning (Nitrites)
- Methemoglobin binds CN- --> Cyanomethemoglobin treat with Sodium Thiosufate that takes Cyanomethemoglobin to methemoglobin and Sodium ThioCN
Name some Beta blockers
What are their Cardiac effects?
What are their Vascular effects?
Atenolol, metoprolol and propranolol
-Decrease contractility, heart rate, conduction velocity
-Causes smooth muscle contraction ( and a mild vasoconstriction )
What is are common side effects of Beta blockers?
Feeling of coldness in the extremities
they decrease the workload on the heart and reduce the hearts response to excersize
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