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Antianginal Drugs

Terms in this set (53)

indication in therapy of chronic stable angina: antiplatelet therapy class 1
-treatment with aspirin 75-162 mg daily should be continued indefinitely in the absence of contraindications in patients with SIHD
-treatment with clopidogrel is reasonable when aspirin is contraindicated in patients with SIHD
indication in therapy of chronic stable angina: antiplatelet therapy class IIb
treatment with aspirin 75-162 mg daily and clopidogrel 75 mg daily might be reasonable in certain high-risk patients with SIHD
indication in therapy of chronic stable angina: antiplatelet therapy class III
dipyridamole is not recommended as antiplatelet therapy for patients with SIHD
indication in therapy of chronic stable angina: statins
most patients based on arthersclerosis diagnosis
indication in therapy of chronic stable angina: beta-blockers class I
-should be started and continued for 3 years in all patients with normal LV function after MI or ACS
-should be used in all patients with LV systolic dysfunction with heart failure or prior MI
-initial therapy
indication in therapy of chronic stable angina: beta blockers class IIb
considered as chronic therapy for all other patients with coronary or other vascular disease
indication in therapy of chronic stable angina: calcium-channel blockers class I
-prescribed for relief of symptoms when BBs are contraindicationed or cause unacceptable side effects in pts with SIHD
-in combo with BBs, should be prescribed for relief of symptoms when initial treatment with BBs is unsuccessful
indication in therapy of chronic stable angina: calcium-channel blockers class IIa
treatment with a non-DHP CCB instead of a BB as initial therapy for relief of symptoms
indication in therapy of chronic stable angina: nitrates class 1
-long-acting should prescribed for relief of symptoms when BBs are contraindicated or cause unacceptable side effects
-in combo with BBs, should be prescribed when initial treatment when BBs are unsuccessful

-sublingual = immediate relief
indication in therapy of chronic stable angina: ranolazine class IIa
can be useful when prescribed as a substitute for BBs for relief of symptoms if initial treatment with BBs leads to unacceptable side effects or contraindicated

-in combo with BBs can be useful when prescribed for relief of symptoms when initial treatment with BBs is not successful
BB mechanisms to relieve anginal pain
slowing HR --> increased diastolic perfusion time
slowing HR and contractility --> decreased myocardial oxygen demand
BB precautions: diabetes
delays recovery form hypoglycemia, masks signs of hypoglycemia, Amy causes new onset of diabetes
sweating will be present
BB precautions: asthma
bronchoconstirction with nonselective BBs
BB precautions: COPD
bronchoconstriction with nonselective BBs
BB precautions: peripheral vascular disease (PVD)
unopposed alpha 1-mediated peripheral vasoconstriction with potential exacerbation of PVD and Raynaud's disease (may be less cardio-selective BBs or BBs with alpha 1 blocking activity
effect on HR: NTG
reflex increase
effect on HR: BB
decrease
effect of HR: combined NTG and BB
net decrease
effect on contractility: NTG
reflex increase
effect on contractility: BB
decrease
effect on contractility: combined NTG and BB
unchanged or decreased
diastolic perfusion time: NTG
decreased
diastolic perfusion time: BB
increased
diastolic perfusion time: combined NTG and BB
net increase
myocardial oxygen consumption: NTG
decrease to may increase
myocardial oxygen consumption: BB
decrease
myocardial oxygen consumption: NTG and BB
net decrease
MOA of nitrates
-NO activates guanyl cycles to increase intracellular levels of cyclic GMP (cGMP)
-cGMP activates cyclic GMP-dependent protein kinase which phosphorylates various proteins in smooth muscle, including myosin light chain phosphatase
-activated phospatase inhibits any contractile response leading to relaxation
net effects of nitrates
smooth muscle relaxation and vasodilation resulting in decreased myocardial oxygen demand
types of angina where nitrates are indicated
-chronic stable (decrease myocardial O2 demand)
-variant (relax smooth muscle and relieve coronary artery vasospasm)
-unstable
effect of NTG on unstable angina
-dilate the epicardial coronary arteries and reduce myocardial oxygen demand
-decrease platelet aggregation (through inhibition of thromboxane synthetase)
first-pass metabolism of NTG
hepatic organic nitrate reductase remove nitrate groups from NTG one at a time to form dinitrate and then mononitrate
-bioavailability of NTG is very low (10-20%) from this first-pass effect
what oral route of administration avoids the first-pass effect of NTG
sublingual
short-acting dosage forms of NTG
sublingual nitroglycerin tablet (Nitrostat), translingual nitroglycerin spray (better than tablets but more expensive)
long-acting dosage forms of NTG
-topical = much faster absorption than oral due to extensive first-pass of NTg
-formulations: nitroglycerin ointment 2% (Nitro-BID), nitroglycerin TD patch, isosorbide mononitrate IR/ER tablet, isosorbide dinitrate
nitrate contraindication
PDE5-inhibitors (vasodilators; several decreased BP)
sildenafil (Viagra), tadalafil (Cialis), vardenafil (Levitra), avanafil (Stendra)
nitrate side effects
dizziness/lightheadedness, flushing, syncope
nitrate warnings
hypotension, headache, tolerance (tachyphylaxis) needs long-acting
what needs to be monitored when taking nitrates?
BP, HR, chest pain
CCB MOA of antianginal action
-inhibit calcium entry/release into myocardial cell --> limits contraction of cardiac and smooth muscle
-decreases cardiac workload and O2 demand--> decreases coronary vascualar resistance and causes peripheral vasodilation
-metabolic protection of ischemic tissue --> extends the "therapeutic window" for thrombolytic therapy
-lowering of TPR triggers baroreceptor responses --> tachycardia and increased contractility
indications for NDHP CCBs
-unstable
-stable
-variant
CCB that is preferred in combo with BBs; why?
DHP CCBs ; decreased bradycardia risk
indications for DHP CCBs
-stable
-variant
CCB that causes the greatest amount of reflex tachycardia
Nifedipine
CCB that is the most potent peripheral vasodilator
Nifedipine
CCB that causes the greatest amount of flushing, headache, and hypotension
nifedipine
CCB that causes the most constipation
verapamil
why may the chronotropic and inotropic effects of verapamil and diltiazem be highly variable?
when used in combo with other negative inotropes, there is that highest risk of depressed contractility that can lead to bradycardia
drugs indicated for vasospastic angina
-DHP CCBs (DOC)
-NDHP CCBs
-NTG
drugs contraindicated for vasospastic angina
BBs
MOA for ranolazine (Ranexa)
may decrease myocardial O2 demand by decreasing late phase sodium current which facilitates calcium entry via the Na-Ca exchanger
-decreases ventricular tension, decreases cardiac contractility, and improves blood flow
contraindications for ranolazine
liver cirrhosis, use with strong 3A4 inhibitors
ranolazine effect on HR and BP
little to no effect
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