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Antianginal Drugs

Terms in this set (96)

What is angina?
pain or discomfort in the chest that happens when some part of the heart does not receive enough oxygen
What are 7 risk factors of angina?
• Overweight
• Family history
• Alcohol
• Smoker
• Hyperlipidemia
• Poor diet, (fat, salt, sugar)
• Lack of exercise
What are differential diagnosis of angina?
• Gastritis
• Hiatal hernia
How does angina appear in women?
Women having fewer calcifications
less focal obstruction
more diffuse patterns of atherosclerosis, soft plaques
What are symptoms of angina in women?
nausea
vomiting
indigestion
breathlessness
back pain
What is the most common cause of mortality worldwide?
Cardiovascular disease (Coronary artery disease and Ischemic heart disease)
What type of lifestyle modifications can you make for ischemic heart disease?
smoking cessation
physical activity
weight management
What are 3 types of management of modifiable risk factors?
hypertension
diabetes
dyslipidemia
What does dyslipidemia consist of?
increased cholesterol, increased triglycerides
What are 3 types of angina?
stable, classic, effort-induced angina
unstable angina
prinzmetal's, variant, vasospastic, rest angina
What does stable, classic, effort-induced angina cause?
atherosclerosis, ischemia ‐ dec coronary perfusion, dec blood supply, when inc demand, physical activity, emotional stress, excitement, or any inc cardiac workload
What is typical stable, classic, effort-induced angina?
effort‐induced, short‐lasting , self‐limited episodes of ischemia
What is atypical stable, classic, effort-induced angina cause?
dyspnea, indigestion, n/v, diaphoresis, fatigue, more common, women, diabetics, elderly
What is stable, classic, effort-induced angina relieved by?
nitroglycerin
NO cellular death
What is unstable angina?
deterioration of cardiac function, characteristics , sudden, severe, chest pain, may radiate to neck, jaw, back, arm
Is unstable angina relieved by rest or nitroglycerine?
no, not for more than 20 minutes
What is unstable angina characteristically between?
stable angina and MI
What can unstable angina progress to?
Acute coronary syndrome
How should you treat someone who is having an acute coronary syndrome?
hospitalize to prevent MI and death, increase troponins and creatine kinase
What is Prinzmetal's, Variant, Vasospastic, Rest angina?
• uncommon, caused by vessel wall spasms
• spontaneous coronary spasm, episodic, often night or early am, at rest, may be triggered by cold
What is Prinzmetal's, Variant, Vasospastic, Rest angina unrelated to?
physical activity, heart rate, or BP, not caused by atherosclerosis
What is Prinzmetal's, Variant, Vasospastic, Rest angina treated with?
coronary vasodilators, i.e. nitroglycerin, CCB
What are 4 categories of drugs that are used for angina treatment?
Calcium channel blockers
organic nitrates
beta blockers
sodium channel blockers (ranolazine)
What are 4 beta blockers used for tx of angina?
atenolol
bisoprolol
metoprolol
propranolol
What are CCBs (dihydropyridines) used for tx of angina?
amlodipine
felodipine
nifedipine
What are CCBs (non-dihydropyridines) used for tx of angina?
diltiazem
verapamil
What are 3 nitrates used for tx of angina?
nitroglycerine
isosorbide dinitrate
isosorbide mononitrate
What are sodium channel blockers used for tx of angina?
Ranolozine
What are beneficial actions in angina of beta blockers ?
• inc HR, dec contractility, dec CO, dec BP

• dec O2 demand, exertion and rest

• dec frequency and severity of angina attacks

• inc exercise duration and tolerance with stable (effort‐induced) angina
What is the therapeutic use of beta blockers in hypertension?
Primary benefit, HTN with concomitant heart disease, (atrial fibrillation, previous MI stable ischemic heart disease , chronic HF)
What are beneficial actions of beta blockers in heart failure?
↓ BP primarily by ↓ CO↓ HR
↓sympathetic outflow ↓renin release from kidneys ↓ angiotensin II and ↓ aldosterone
↓ cardiac remodeling
What are therapeutic uses of beta blockers?
•initial antianginal tx, unless contraindicated
• unstable angina/ Acute MI
•not recommended for vasospastic angina‐ ineffective and may worsen symptoms
How are beta blockers therapeutically effective in initial antianginal tx?
reduces the risk of death and MI
improve mortality in patients with HTN and HF with HRrEF
How are beta blockers therapeutically effective in unstable angina/Acute MI?
beta blockers first 24 hrs to decrease infarct size, continue long term, ↓ mortality
When should you not use beta blockers in unstable angina/acute MI?
If there is bradycardia, acute HF, cardiogenic shock
Are beta blockers used for vasospastic angina? Why?
no, increase coronary resistance
What is characteristic of propranolol and nadolol?
• β1 β2 receptors. contraindicated asthma
What is characteristic of pindolol?
• intrinsic sympathomimetic activity (ISA)
When should you avoid taking pindolol?
‐avoid in angina and previous MI
What are Preferred‐ cardio‐selective‐β1 selective beta blockers?
metoprolol succinate
metoprolol tartrate
atenolol
What is characteristic of nebivolol?
• β1 receptors, ↑ nitric oxide
All beta blockers are ______ at high doses and can inhibit β2 receptors
non selective
What are comorbid conditions of beta blockers ?
asthma/COPD
Acute heart failure
Raynaud's disease
Diabetes
2nd, 34d degree heart block
Severe bradychardia
Why shouldn't you use a beta blocker in diabetic patients (and if you decide to you should monitor the patient closely)?
masks hyperglycemia
What should a patient caution in doing when taking a beta blocker?
do not discontinue abruptly, taper over 2-3 weeks to avoid rebound angina, MI, hypertension
What should you use first line for variant/vasospastic/prinzmetal angina? Why?
Calcium channel blockers due to relaxation of the coronary arteries
Is ranolazine used for Prinzmetal's angina?
no
What types of angina should calcium channel blockers be used in?
stable
variant/vasospastic/prinzmetal angina
How are CCBs used in stable angina?
oral to prevent anginal attacks
What do CCBs do in stable angina?
decrease myocardial O2 consumption by decreasing vascular resistance, thereby decreasing afterload
What is the mechanism of CCBs?
-block the inward movement of calcium by binding to L‐type Ca+ channels in heart and in smooth muscle of coronary and periphery
-causes vascular smooth muscle to relax, dilating arterioles, (not veins)
What does ischemia cause in relation to calcium in the heart?
ischemia causes membrane depolarization and calcium influx, requiring energy worsens ischemia
What is characteristic of non-dihydropyridines?
↑ affinity cardiac decreased inotropic
Cardio selective‐ depressant action decrease heart rate and contractility, which leads to a reduction in myocardial 02 demand
•Also dilate coronary arteries, preventing or reversing coronary vasospasms (in Prinzmetal's Angina)
What is characteristic of dihydropyridines?
↑ affinity vasculature
• Systemic vasodilation reduces arterial pressure, which reduces afterload (wall stress) thereby reducing 02 demand
What is characteristic of amoldopine?
• arterial vasodilator
•minimal effect on cardiac conduction
What is amlodipine used for?
stable angina
vasospastic angina
What is nifedipine used for?
oral extended‐release
used Short‐acting
• should be avoided ⇢evidence ↑ mortality in HTN due to ↑risk of MI due to excessive vasodilation and reflex cardiac stimulation
• use‐ only when drop BP very quickly
What are adverse effects of CCBs?
AV block, HF
Constipation
Flushing, dizziness, headache, fatigue
Hypotension, reflex tachycardia
Peripheral/bilateral edema
Gingival hyperplasia
What is the mechanism of organic nitrates?
• By ↑intracellular conversion to nitric oxide, which activates guanylate cyclase and increased (cGMP) → leads to dephosphorylation of myosin light chain, resulting in vascular smooth muscle relaxation
• Results in vasodilation of large veins (venous return to the heart) ⇢ decreased preload ⇢ decreased cardiac workload • ↑ blood supply‐heart muscle
What are therapeutic uses of organic nitrates?
• Stable Angina
•Unstable (acute) Angina
•Variant Angina
How does organic nitrates act to relieve symptoms?
by decreasing myocardial O2 demand
• Relaxes vascular smooth muscle
• Dilation of large veins → decreases preload
• Dilates coronary vasculature
What is characteristic of isosorbide mononitrate?
long duration of action (improved bioavailability due to stability against hepatic breakdown)
How much sublingual/buccan nitroglycerine should be used?
-0.4 mg (0.3-0.6 mg)
-if no relief after 3rd dose seek prompt medical attention
-May take 2 additional doses, sublingual q 5 min up to a total of 3 doses maximum
Do not exceed 3 doses in 15 minutes of nitroglycerine or what may occur? (3)
hypotension
reflex tachycardia
MI
What is characteristic of nitroglycerine?
significant 1st pass effect
Differ in onset of action (1‐30 min) / rate of elimination , different uses
What are forms of acute nitroglycerine tx?
-sublingual/buccal
-IV
What are forms of preventative nitroglycerine tx?
-transdermal patch/ ointment
-oral capsules sustained release‐used less, rapid breakdown
When is a nitroglycerine patch used?
during the day when cardiac workload is increased and oxygen demand doesn't meet that
What are 4 advantages of sublingual/buccal route?
• Absorption quick
• Avoid first pass metabolism
• Self‐ administered
• economical
What are 2 disadvantages of the sublingual/buccal route?
• Few can be absorbed this route
• Cannot use large quantities
When should you be worried and discontinue nitroglycerine IV?
if hypotension
What is nitroglycerine used for?
anal fissures/external hemorrhoids
What are anal fissures/external hemorrhoids caused by?
• increased muscle tension, in the internal anal sphincter can lead to fissures. Spasms and ↓ blood flow to anus and rise in pressure keeps fissures from healing
What is 0.25 nitroglycerine ointment mechanism of action?
dilates vasculature, helps to heal, works well
What are adverse effects of organic nitrates/nitroglycerine?
•Headache
• Facial flushing
• Postural hypotension
•Reflex tachycardia
• Tolerance
What is contraindicated with the treatment of organic nitrates/nitroglycerine?
migraines
phosphodiesterase type 5 inhibitors
What is a phosphodiesterase type 5 inhibitor that when paired with organic nitrates causes life threatening hypotension?
sildenafil
When is renolazine used?
stable angina
When is renolazine often used?
when other antianginal treatments have failed
What is the mechanism of renolazine?
•inhibits Na+ current (INa), [relationship to angina is uncertain]
• anti‐ischemic and antianginal effects →improves O2 supply and demand equation
• effects do not depend upon decreases HR or decreases BP
How is renolazine metabolised?
liver by CYP 45CYP3A (major) CYP2D6 (minor)
• substrate of P‐glycoprotein
What are adverse effects of renolazine?
QT prolongation i dose dependent manner
effect that is increased with hepatic management
renal impairment
What types of drug interactions are present with Ranolazine? (3)
strong inhibitors of CYP3A
Inducers of CYP3A
P-glycoprotein substrates
What is used to treat acute stable angina?
sublingual nitroglycerine
What is used to prevent stable angina?
beta blockers
CCB or long acting nitrates (nitroglycerine patch)
renolazine
(treat in this order)
What is used for treatment of acute variant angina?
nitroglycerine sublingual
What is used to prevent variant angina?
CCB or long acting nitrates (patches)
What is a category of medication most commonly associated with peripheral edema?
CCB
Name a category of medication most associated with hypokalemia?
thiazide diuretic
loop diuretic
Name a medication associated with hypomagnesemia?
loop diuretic
Name a medication associated with AV block?
beta blockers
CCB-nondihydropyridines
Which CCB has the most potent myocardial depressant effects?
verapamil
This diuretic is considered a thiazide diuretic and may be used in reduced kidney function?
metazolone
This med is on the WHO list of essential meds, cost a penny a day, has been used in race horses for the tx of pulmonary hemorrhage and this diuretic can be used for the tx of hypercalcemia.
loop diuretic: furosemide/lasix
In 2008, 4 NFL players were being suspended under the steroid policy as a result of taking this medication, this medication is sometimes used for weight loss because as a diuretic, it removes water, but also masks other drugs including steroids by diluting the content of the user's urine, yielding a lower concentration of filtered substances which mekes them less likely to be detected.
bumetanide
What drug was falsely marketed as a dietary supplement, causing water loss?
bumetanide
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