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Pharmacology Angina Month 2 Week 2 Day 5
Pharmacology Angina Month 2 Week 2 Day 5
36
Pharmacology
Graduate
06/15/2018

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Cards

Term
types of angina pectoris and pathophys of each
Definition
Typical (stable, effort) angina
• ↑ O2 demand—fixed supply (atherosclerosis)
Variant (Prinzmetal’s) angina
• ↓ O2 supply—unchanged demand
• At rest, coronary spasm (prostaglandins)
Unstable angina (ACS)
• ↓ O2 supply, plaque rupture, plt activation, clot
Microvascular angina (Syndrome X)
• Atherosclerosis in small coronary arteries
Term
O2 demand angina and pharmacotherapy for 2 groups
Definition
[image]
Term
O2 supply in angina and pharacotherapy for 2 groups
Definition
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Term
antiplatelet therapies for angina
Definition
• Aspirin75–162mg/day(I,LOEA)
• Alternative Clopidogrel 75mg/day(I,LOEB)
• Hig hrisk SIHD-ASA+Clopidogrel(IIb,LOEB)
Term
beta adrenergic antagonists for angina and MOA
Definition
Block cardiac B-1 receptors
• Decrease heart rate/↑ diastolic filling • Decrease contractility/CO
• Reduce wall tension- Reduce O2 Demand
Goal HR 50–60 bpm
Term
beta blocker agonists indications for angina
Definition
• Symptomatic SIHD(I,LOEB)
• MI/ACS with normal EF—start and continue three years (I, LOE B)
• HF/ prior MI with LVEF<40%—carvedilol, metoprolol succinate, or bisoprolol (I, LOE A)
• All other patients w/ASCVD(IIb,LOEC)
Term
cardioselective BBA
Definition
acebutolol, atenolol, betaxolol, bisoprolol, esmolol, metoprolol
Term
non-selective BBA
Definition
carvedilol, labetalol
nadolol, propanolol, sotalol
Term
Adverse effects:

• Cardiac—fatigue, dizziness, ↓reserve • Hypotension
• Bradycardia—attenuate with ISA BBA --CI sev. brady, high degree AV block, SSS w/pacer, refractory HF
• Caution reactive airway disease—attenuate with cardioselective BBA
• PAD—attenuate w/ low dose cardioselective BBA or BBA with α- blocking
• Diabetes-- Mask hypoglycemic symptoms
• CNS—nightmares, depression, insomnia
• Impotence
• Abrupt withdrawal—rebound phenomena
Definition
BBA
Term
calcium channel blockers MOA
Definition
• InhibitCa++channel influx in cardiac and vascular smooth muscle
• Decrease heart rate
• Decrease contractility/CO -- Reduce O2 Demand, Increase Coronary Blood Flow
• Non-DHP CCB goal HR 55–60bpm
• Monotherapy not recommended with DHPCCB due to reflex tachycardia -- DHP titrate to reduction in symptoms and BP
Term
CCB indications
Definition
• Symptomatic SIHD with intolerance or CI to BBA (I, LOE B)
• Combo w/ BBA—persistent symptoms
• Symptomatic SIHD—long-acting non-DHP alternative to BBA (IIa, LOE B)
Term
non-DHP CCB agents
Definition
Diltiazem, Verapamil
Term
DHP CCB agents
Definition
Amlodipine, Clevidipine, Felodipine, Isradipine, NiCARdipine, NIFEdipine, Nimodipine
Term
adverse effects:
• Constipation
• Bradycardia/AV block/↓CO
• Avoid combo with BBA unless rate control afib
Definition
Non-DHP CCBs

constibation esp Verapamil in elderly
Term
• Hypotension, reflex tachycardia, flushing, headache
• Peripheral edema
• Caution in severe Ao valve stenosis
Definition
DHP CCB

peripheral edema esp amlodipine
reflex tachycardia (avoid short-acting DHP)
Term
has drug interactions:
• CYP3A4
• Cyclosporine
• Carbamazepine
• Li
• Amiodarone
• Digoxin (50–70% inc dig lvl in 1st week)
Definition
CCB
Term
Ivabridine MOA Angina
Definition
• Block I(f) → reduce diastolic depolarization slope → lower HR
• Nonegativechronotropicorlusitropiceffect
• NoeffectonBP
• No guideline update since U.S.availability
Term
has adverse effects:
• Phosphenes—enhanced visual brightness
• Symptomatic bradycardia
Definition
ivabridine
Term
organic nitrates MOA
Definition
• Direct smooth muscle relaxation --- ↑ NO → activate guanylate cyclase → Ca++ uptake SR → dephosphorylation of myosin-LC
• Reduce preload(veins>arteries)
• Myocardial wall tension -- Reduce O2 Demand
• Epicardial coronary artery dilation -- Increase O2 Supply
Term
Nitrates indications
Definition
• All SIHD patients
• Acute angina symptoms—SL NTG tab or spray—(I, LOE B)
• Activation of EMS if unrelieved by 1st dose
• Symptomatic SIHD with intolerance or CItoBBA (1, LOE B)
• Combow/BBA—persistent symptoms
Term
Nitrates agents and differences
Definition
Isosorbide dinitrate (ISDN)
• Schedule nitrate-free period
Isosorbide mononitrate
• Active metabolite of ISDN
• No first pass metabolism
• Excellent bioavailability
• Asymmetric dosing (nitrate-free period)
Term
nitroglycerin
Definition
sl tablet or topical (longer duration)
Term
has adverse effects:
• Hypotension
• Flushing/headache
• Tachycardia—attenuatedwithcomboBBA
Tolerance—loss of antianginal effect
• Oxidation of sulfhydral groups and formation of disulfide bonds
• Develops fast and recovers fast (10–14 hours free) • Combat w/ACEI, carvedilol, hydralazine
• Dose dependent
Avoid in severe Ao valve stenosis
Definition
Nitrates
Term
Drug interactions w
• PDE5 inhibitors (sildenafil (Viagra), tadalafil (Cialis) or vardenafil (Levitra)
• Profound hypotension
Definition
Nitrates
Term
Ranolazine MOA
Definition
• Inhibits late I(Na), ↓ Ca++
• ↓cardiac metabolic action/fatty acid oxidation -- Reduce O2 Demand
• No effect on HR or BP
Term
Ranolazine indications
Definition
• SIHD—Combine with refractory symptoms (IIa, LOE A) or in place with intolerance to BBA (IIa, LOE B)
Term
has adverse effects
QT prolongation
• 15 msec at therapeutic concentrations
• Avoid combo with other QT prolonging drugs
Constipation
• Nausea
• Dizziness
• Headache
• Accumulation in CKD
• CI in clinically significant hepatic impairment
Beneficial
• Reduction in VT, bradycardia, and afib
• Improved Hgb A1c
Definition
Ranolazine
Term
has drug interactions:
• CYP3A4 inhibitors
• Ketoconazole and other azole antifungals
• Macrolide antibiotics
• HIV protease inhibitor
• Grapefruit products/juice
Simvastatin–increase simva/metabolite lvls
Digoxin increased digoxin lvls
Definition
Ranolazine
Term
ACEI/ARB indication for angina
Definition
• ACEi—All SIHD patients w/ HTN, DM, LVEF<40% or CKD (I, LOE A)
• ARBs—above w/ intolerance to ACEi (I, LOE A)
• ACEi reasonable in SIHD w/ vascular dz (IIa, LOE B)
• ARBs—above w/ intolerance to ACEi (IIa, LOE C)
Term
chelation therapy for angina
Definition
• EDTA->complex with Ca++andcadmium-> excretion of soluble complexes -> regression of plaques -> relief of angina/oxidative stress in vascular wall
• Improve coronary bloodflow
Term
has adverse effects:
• 18% lost to follow-up
• Hypocalcemia
• Renal failure
• Death
Definition
chelation therapy
Term
Enhanced External Counterpulsation (EECP)
Definition
-angina
• Technique with inflatable cuffs wrapped around LEs ↑venous return/augment DBP
• 1-hour session 5 days/week X 35
Term
has adverse effects:
• 55% reported AEs • Leg and back pain • Skin abrasions
Definition
EECP
Term
SIHD RX not recommended
Definition
• Estogen in post-menopausal women
• Vit C, E, or beta-carotene
• Folate, B6, or B12—for elevated homocysteine levels
• Garlic, CoEnz Q10, selenium, chromium
Term
revascularization methods
Definition
• PCI (preferred in lower risk pts)
CABG preferred in higher risk
• Diabetes mellitus
• Complex multivessel disease
Term
overall takeaways for therapy for stable ischemic heart disease
Definition
It's a good take-home point to understand that we will initially start with pharmacotherapeutic interventions, particularly with beta blockers. Aspirin, for instance, and statin should be used to lower the risk of a secondary event from occurring in patients who are at high risk.
Calcium channel blockers and nitrates may also need to be used for patients who develop acute chest pain. But if all pharmacotherapy fails, patients may warrant PCI, or CABG if they are particularly high risk with multivessel diabetes or other clinical conditions.
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