Beta-Blockers Flashcards
What class are Beta-Blockers
Class 2 anti-arrhythmic agents
what does beta stimulation do to the heart
increases contraction and heart rate
Why do athletes take beta blockers
to calm them down, reduce their heart rate
What do beta-blockers inhibit
The sympathetic activation of B-adrenergic receptors
What does B1 agonists do
increased heart rate, increased contractile force, workload and AVN conduction
what do beta-2 agonists do
stimulates bronchodilation/relaxtion
Non-Selective B-Blockers
inhibits B1 and B2 (in the heart and lungs)
Cardio-selective beta blockers benefit?
lower side-effect profile s
What conditions are cardio-selective beta blockers preferred for?
coronary heart disease
compensated heart failure
acute coronary syndrome
certain arrhythmias
Propranolol is what type of beta blocker
Non selective
What is propranolol a first line drug for?
essential tremor
portal hypertension
migraine prophylaxis
thyroid storm
What conditions are cardio-selective B-blockers (B1 selective) indicated for
coronary heart disease
compensated heart failure
cardiac arrhythmias (a-fib, atrial flutter, PSVT)
Where does B-1 selective blockers bind
B1 receptors in the heart
-there are SOME in other places of the body (like the kidney)
What do cardioselective B1 blockers do to the heart
-decrease heart rate
-decrease contractility
-decrease AVN conductivity
What is the only drug that causes NO-mediated vasodilation
Nebivolol
What does Nebivolol do in the body
decreases vascular resistance by stimulating B3 receptors and activating NO synthase in the vasculature
Compensated heart failure is
heart is overcompensating to give the other organs what they need (at expense of itself)
Side effects of Cardioselective Beta blockers
bradycardia
bradyarrhythmia
are cardioselective beta blockers dose dependent? what does this mean for B2 receptors
Yes they are dose dependent
-B2 receptor blocking increases at higher doses
What are not side effects of cardioselective beta blockers
generally:
-bronchoconstriction or vasoconstriction
-interference with glycogenolysis
are cardioselective beta blockers safe for diabetic patients
yes
because it does not interfere with glycogenolysis
AVN is
Atrial ventricular node
Cardioselective beta blockers with ISA (drugs)
*acebutolol
celiprolol
Example of beta-blocker that stimulates NO-mediated vasodilation
Nitroglycerin
ISA
intrinsic sympathomimetic activity
Cardioselective beta blockers without ISA (drugs)
*Atenolol
*Metoprolol (Lopressor)
*Esmolol
Bisoprolol
Betaxolol
Glycogenolysis
Destruction of glycogen
where is glycogen stored mainly?
Liver
Non-selective Beta-Blockers indications
-cardioselective B1-blocker alternative
-angina
-essential tremor
-portal hypertension
-migraine prophylaxis
!!!!! thyroid storm !!!!!
Indications to use Propranolol (non-selective b-blocker)
Angina
Indications to use Sotalol (non-selective b-blocker)
cardiac arrhythmia
Indication to use timolol (non-selective b-blocker)
glaucoma
Effects of nonselective beta-blockers
bronchoconstriction
vasoconstriction
Hypoglycemia and hyperglycemia
bradycardia
syncope
Mechanism of Non-Selective Beta-blocker
Blocks B1, B2 and B3 receptors
What does Sotalol (non selective b-blocker) also blocks
cardiac potassium channels (anti-arrhythmic effect)
For what type of patients are Non-selective Beta blockers NOT suggested for
-history of asthma/COPD
-history with peripheral vascular disease
-
Why would you choose Non-selective beta blockers?
Because they can affect other parts of the body (and this is the desired effect when using)
“OFF LABEL USE”
Non-Selective beta blockers with ISA (drugs)
*Pindolol
Penbutolol
Oxprenolol
Non-selective beta blockers withOUT ISA (drugs)
*Propranolol (Inderal)
Nadolol
Sotalol
*Timolol
Tertalol
Non-Selective Beta Blockers with alpha blocking action (drugs)
*Labetalol
Bucindolol
*Carvedilol
Indications for Non-Selective Beta-blocker with alpha blocking action
pregnancy-induced hypertension
Esophageal variceal bleeding (prophylactic use)
What do Alpha1 adrenergic receptors do
vasoconstriction of the blood vessels
(increases BP)
2 Benefits of Nonselective BetaBlockers with alpha blocking action
- calms the heart down
- decreases the pressure in the vascular
What beta blocker begins with the letters A-M
Cardioselective B-Blocker (exception of Nebivolol)
(B1=first)
What beta blocker begins with the letters N-Z?
Non-selective beta blockers
(excludes the a-blocking action drugs)
(B2=second)
what is a risk factor for esophageal variceal bleeding
alcohol use
Effects of Non-selective beta blocker with alpha blocking action within the BODY
vasodilation (decreased peripheral vascular resistance, decreased preload and afterload, increased renal blood flow)
-reduce portal hypertension and pressure gradient in hepatic venous
-improved endothelial function and vascular remodeling
What do Non-selective beta blocker with alpha blocking action do to the portal BP
decreases the portal hypertension and pressure gradient in hepatic venous
Side effects of Non-selective beta blocker with alpha blocking action
same side effects as non-selective beta blockers
-orthostatic hypotension
Pharmacodynamics of Beta-Blockers
competitively bind to and block B-adrenergic receptors
-inhibits sympathetic stimulation of B-receptors
Mechanism of action of ISA
partial agonists activity
-binds and stimulate B-adrenergic receptor (agonist effect)
-competitively inhibits the binding of EPI and NE (antagonist effect)
What do ISA beta blockers produce
partial sympathetic activity while inhibiting the normal and activated sympathetic activity
what is the Effects of ISA drugs in the body (3 things)
-less bradycardia & peripheral vasoconstriction (bc of mild agonist action)
-Favorable effect on lipid profile
When are ISA drugs not indicated
congestive heart failure, ischemic heart disease and tachyarrhythmias
ISA agents
Pindolol
acebutolol
carteolol
alprenolol
Why are ISA agents recommended for pt’s with metabolic syndrome
because they have a favorable effect on lipid profile
What type of mechanism is ISA
partial agonist and competitive inhibitor for alpha and beta receptors (for NE and EPI)
Epinephrine stimulates what receptors
alpha and beta receptors
what 2 drugs are especially favorable for favorable effect on lipid profile
pindolol and acebutolol
Examples of metabolic syndrome
Hyperlipidemia and diabetes mellitus
what three things can we use for energy
carbs (main)
lipids
protein
What is defective in metabolic syndrome
problems processing the energy sources
what kind of clearance do Lipophilic agents undergo
hepatic clearance
What agent can cross the blood brain barrier? what does this mean in terms of effects?
Lipophilic agents
causers neurological adverse effects (nightmares and insomnia)
What is the longest acting agent
lipophilic
examples of lipophilic agents
carvedilol
labetalol
metaprolol
propranolol
What type of clearance do hydrophilic agents undergo
renale clearance
What types of agents don’t cross the blood brain barriers?
hydrophilic
are hydrophilic agents short acting or long acting? how many doses are required?
Short acting
multiple doses
example of hydrophilic agents
acebutolol
atenolol
celiprolol
pindolol
sotalol
examples of mixed agents
bisoprolol
Nebivolol
Non selective beta blockers and cardioselective beta blockers effect on the heart
bradycardia
bradyarrhythmia
ventricular tachyarrhythmia
worsened heart failure
vasopsasms
orthostatic hypotension
Non selective beta blockers and cardioselective beta blockers effect on the CNS
fatigue
sleep disorders
nightmares
depression
hallucination
seizures
Non selective beta blockers and cardioselective beta blockers effect on the skin
psoriasis
Non selective beta blockers effect on the pulmonary system
Bronchoconstriction
-dyspnea
-bronchospasm
-respiratory exacerbation
Non selective beta blockers effect on the Peripheral vasculature system
peripheral vasoconstriction
-ED
-secondary Raynauds
-cold extremities
Non selective beta blockers effect on the Metabolic system
-hypertriglyceridemia
-hyperglycemia
-hypoglycemia
-weigh gain
What are the clinical features of B-Blocker over dose (7)
bradycardia/bradyarrhythmia
cardiogenic shock
hypoglycemia
hyperkalemia
wheezing
neurological symptoms
what is Cardiogenic shock? What does it present as?
poor perfusion
hypotension, cold/clammy extremities
What is the treatment for beta-blocker overdose
-secure the airway
-correct the cardiovascular decompensation
-prevention of further beta-blocker absorption
What treatments are included in correcting cardiovascular decompensation VIA IV ACCESS
-Fluids (saline) and vasopressors (epinephrine)
-Atropine
-Glucagon
-calcium salts
-high dose insulin with glucose
What does atropine administration do?
corrects bradycardia
what does glucagon administration do in b-blocker overdose treatment?
acts as antidote for b-blocker poisoning
what does calcium salts administration do in b-blocker overdose treatment?
improves cardiac contractility
what does High-dose insulin with glucose administration do in b-blocker overdose treatment? when is it used?
Last resort if nothing else worrks
-it has a positive inotropic effect
How do you prevent further absorption of beta-blockers?
activated charcoal
gastric lavage
IV lipid emulsions
When is hemodialysis indicated for B-Blocker overdose treatmetn
hydrophilic beta blocker overdose
dialysis removes drug completely from circulation
What is the process for administering/stopping beta blocker treatmetn
administer gradually and slowly taper off when stopping
what is hypertriglyceridemia
Decreased levels of HDL with B-BLocker w/o ISA
Clinical features of Beta-Blocker withdraw (4)
tachycardia
tachyarrhythmia
hypertension
Acute coronary syndrome (sudden death)
How to prevent Beta-Blocker withdrawl
taper the dose over 7-10 days before discontinuing
Pathophysiology of B-Blocker treating hypertension
Beta blockers lower BP which decreases cardiac output and renin secretion
Pathophysiology of B-Blocker treating Acute myocardial infarction
INITIATE EARLY in ALL pts without CI
-decreases the size of the infarct
-reduces early and delayed mortality rates
When do you use B-Blocker to treat angina pectoris? Do you add any other medications
First line treatment for stable angina pectoris
-add ACE inhibitors or ARBS
How do you use B-Blocker to treat heart failure? Do you add any other medications
Cardioselective B-blockers + ACE inhibitor/ARB + Spironolactone
What does Spironolactone do for CHF
slows the progression
How does insulin work?
lowers the blood glucose
allows the glucose to enter into the cell
without insulin you can’t get the glucose in
What does not need insulin?
Central nervous tissue
What do B-Blockers do for arrhythmias
regulate atrial flutter, atrial fibrillation, PSVT, VT and premature ventricular contractions
What class antiarrhythmic agents are Beta Blockers? what are 3 examples
Class 2 antiarrhythmic agent
metoprolol
esmolol
propranolol
What are 9 specific indications for Propranolol
- tremor
- migraine prophylaxis
- portal hypertension
- hyperthyroidism/thyroid storm
- infantile hemangioma
- akathisia
- Hypertensive crises
- Glaucoma
- Pregnancy induced hypertension
What to do in hypertensive crisis
IV labetalol
How is glaucoma treated by beta blockers? Give 2 examples
topical beta blockers
timolol
betaxolol
What is the first line drug for pregnancy induced hypertension
Labetalol
Absolute contraindications of BetaBlocker treatment? (6)
- Symptomatic bradycardia
- cardiogenic shock and HTN
- Pheochromocytoma
- Decompensated heart failure
- CCB combination
- sick sinus syndrome
what is Pheochromocytoma?
tissue that produces an excess amount of EPI (mainly) and NE
what can combining CCB and beta blockers do?
AV block
examples of calcium channel blockers
diltiazem
verapamil
Relative contraindications to using Beta Blockers
- asthma and copd
- psoriasis
- Raynaud phenomenon
- Pregnancy
what drug is used to treat pregnancy induced hypertension
labetalol
What happens if Beta Blockers are administered before alpha blockers when a pheochromocytoma is present?
there is an unopposed alpha-adrenoceptor mediated vasoconstriction
a hypertensive crisis occurs
what two B-Blocker medications do not illicit a hypertensive crisis when a pheochromocytoma is present?
carvedilol
labetalol
non selective beta blockers w/ alpha-antagonism
what is Raynaud phenomenon
peripheral artery occlusive disease
-finger tips and toes get discolored
adverse affect from administration of B-Blocker in a patient with sick sinus syndrome
heart block greater than first-degree
what tissue does not conduct?
Dead tissue
why is psoriasis a CI for B-Blocker
the reaction of psoriasis being an autoimmune disease