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Drugs to treat angina
47
Pharmacology
Undergraduate 1
12/02/2016

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Term
Define angina perctoris
Definition
chest pain caused by cardiac ischaemia, generally due to obstruction or spasm of the coronary arteries
Term
What are the symptoms of angina?
Definition
- pain in chest which radiates to the arm, neck and jaw and is intermittent, often with exertion
- pain is also brought on with cold or excitement
Term
What are the causes of angina?
Definition
- coronary blood flow is insufficient to supply the O2 requirements of the myocardium
- O2 demands of the heart are high
- CAD is due to atherosclerosis
Term
Define collaterals and give their importance
Definition
connect arterial systems derived from different major coronary arteries. Number of collaterals can be increased via exercise. More collaterals = more protection from blockage. Age also increases collaterals.
Term
Describe coronary flow
Definition
from the sub0epicardial (outer) surface to the sub-endocardial (inner) surface
Term
What are the main physiological factors that regulate coronary flow?
Definition
- physical factors
- vascular control by metabolites
- neural and humoral control
Term
What part of the heart is vunerable to changes in coronary flow?
Definition
endocardium
Term
When does the majority of coronary blood flow occur?
Definition
in diastole
Term
What affect does aortic pressure have on coronary blood flow have?
Definition
perfuses the coronary capillaries
Term
What affect does ventricular pressure have on coronary blood flow have?
Definition
prevents perfusion by compressing coronary capillaries
Term
What are the 3 types of angina?
Definition
Stable
Unstable
Prizmental's
Term
What causes stable angina?
Definition
- increased demand on the heart and is caused by a fixed narrowing (atherosclerosis)
Term
What causes unstable angina?
Definition
- atherosclerotic plaque ruptures, thrombi occlude artery
Term
What causes Varient (Prinzmetal's) angina?
Definition
- uncommon and unpredictable
- occurs at rest and is a coronary spasm
- possibly due to increased extracellular K+ or Ca2+ -> membrane depolarisation
Term
What does angina lead to?
Definition
other cardiac diseases
- necrosis/apoptosis
- acute myocardial infarction
- HF and dysrhythmias
- Death
Term
What do drugs used to treat angina do?
Definition
1. decrease cardiac o2 demand -> decrease cardiac work
2. increase cardiac o2 supply -> increase vasodilation
Term
What do drugs used to treat angina redress?
Definition
the balance between O2 supply and demand
they affect the coronary and systemic vasculature and/or heart
Term
What is the effect of decreasing venous return?
Definition
1. decreasing EDV (pre-load)
2. decrease wall stress and work (therefore O2 demand)
3. increase sub-endo O2 perfusion
Term
What is the effect of decreasing peripheral resistance?
Definition
(decreases afterload)
decreases work and therefore O2 demand
Term
What is the effect of decreasing rate and force of contraction?
Definition
1. decrease work and therefore O2 demand
2. increase O2 perfusion during diastole
Term
What is the effect of coronary vasodilation in collaterals?
Definition
increased O2 perfusion
Term
Why does increased HR not improve O2 to the myocardium?
Definition
less time spent in diastole
Term
Which angina drug is the only one that cannot be used to treat all types of angina?
Definition
beta blockers cannot treat Prinzmental angina
Term
What drugs are used to treat angina
Definition
1. nitrates
2. calcium channel blockers
3. beta blockers
4. potassium channel activators
Term
What nitrate treatment is there for less than 2 attacks a week?
Definition
Glyceryl trinitrate (nitroglycerin)
- short acting, sublingual (tablet) or aerosol spray (for treatment)
Term
What nitrate treatment is there for more than 2 attacks a week?
Definition
isosorbide mononitrate
- long lasting, oral (for prevention)
Term
Adverse effects of nitrates
Definition
- headache
- flushing: to become markedly red in the face (blushing is much milder)
- postural hypotension
- tolerance development
Term
What are the effects of nitrates?
Definition
POTENT SYSTEMIC AND CORONARY VASODILATORS
- decrease peripheral resistance (afterload)
- coronary vasodilation of collaterals
- decrease venous return
- decreased EDV (pre-load)
Term
Describe the mechanism of nitrates
Definition
In vascular smooth muscle:

1. Nitrates are metabolised and produce NO. NO activates soluble guanylate cyclase
2. increased cGMP formation
3. activates PKG
4. dephosphorylation of myosin light chains
5. removal of intracellular Ca2+ and conesquent relaxation
Term
When is the contractile machinery of smooth muscle activated? what causes relaxation?
Definition
- when the myosin light chain undergoes phosphorylation
- becomes detached from actin filaments
- catalysed by MLCK
- MLCK is activated when bound to Ca2+ via calmodulin
- myosin phosphatase reverses phosphorylation and causes relaxation
Term
How care voltage-dependent Ca2+ channels inactivated via nitrates?
Definition
NO eventually causes the activation of PKG which activates K+ channels. Movement of K+ out of the cell hyperpolarises the membrane and inactivates voltage dependent Ca2+ channels.
Term
What do drugs that activate K+ channels cause?
Definition
vasodilation via the K+ channels and NO
Term
How does NO cause relaxation?
Definition
1. NO activates soluble guanylate cyclase
2. increased cGMP formation
3. activates PKG
4. dephosphorylation of myosin light chains
5. removal of intracellular Ca2+ and conesquent relaxation
Term
What has the same mechanism as activation of K+ channels?
Definition
nitrates
they work simultaneously
Term
Give an example of a K+ channel activator
Definition
nicorandil
Term
What are the adverse effects of nicorandil?
Definition
headache, flushing and dizziness
Term
How are Ca2+ channel blockers administered?
Definition
prophalactically
(varied effects)
Term
What types of Ca2+ channel blockers are there?
Definition
- cardiac selective
- vascular selective
Term
How do cardiac selective Ca2+ channel blockers work? give an example
Definition
decrease rate and force of contraction on heart

verapamil
Term
How do vascular selective Ca2+ channel blockers work? give an example
Definition
decrease peripheral resistance (afterload)
increase coronary vasodilation
decrease venous return and therefore decrease EV

nifedipine
Term
Describe the Ca2+ channel blocker mechanism
Definition
1. block calcium entering vascular SMC
2. Ca2+ does not bind to calmodulin
3. MLCK not activated
4. myosin not phosphorylated therefore cannot interact with actin
Term
Adverse effects of Ca2+ channel blockers
Definition
- headache
- flushing
- ankle swelling
- heart block
- worsen heart failure
Term
What is the effect of beta blockers?
Definition
reduce effects of sympathetic stimulation of the heart
Term
Which form of angina do beta blockers not treat?
Definition
Prinzmentals angina because they exaserbate the spasm of the coronary artery
Term
Adverse effects of beta blockers?
Definition
- fatigue
- headache
- sleep disturbances
- sudden withdrawal may exaserbate angina
Term
What are additional treatments for unstable angina?
Definition
- antiplatelet (aspirin)
- anticoagulant (heparin/warfarin)
- revascularisation
Term
Treatment of CAD?
Definition
statins (atherosclerosis)
ACE inhibitors (vasodilation, antithrombotic, antiproliferative)
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