Beta Blockers Flashcards

1
Q

Pharmacologic properties of β-Blockers:

A
Relative affinity for β1 and β2 receptors
Intrinsic sympathetic action
Differences in solubility
Membrane stabilizing activity
Capacity to induce vasodilation
α1 and β receptor blockade
Difference in pharmacokinetic parameters
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2
Q

This genotype is a major determinant of interindividual metoprolol clearance:

A

CYP2D6

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3
Q

Initially, PVR is ____ and CO is ___ during β-blocker therapy:

A

increased; decreased

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4
Q

β-blocker with no effect on plasma renin activity:

A

Pindolol

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5
Q

MOA of β-blockers anti-HTN action:

A

Sustained low total PVR
Decreased renin release
Decreased NE release
Peripheral vasodilation (some)

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6
Q

NE release is decreased due to blockade of ____:

A

presynaptic β receptors

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7
Q

Non-selective β-blockers augment pressor response to ___ due to blockade of ___:

A

epinephrine; β2

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8
Q

β-blockers that stimulate NO production:

A

Celiprolol

Nebivolol

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9
Q

β-blockers with α1 antagonistic activity:

A

Carvedilol

Labetalol

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10
Q

β-blockers with Ca entry blockade activity:

A

Carvedilol

Betaxolol

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11
Q

β-blockers that open K channels:

A

Tilisolol

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12
Q

β-blocker that acts as β2 receptor agonist:

A

Celiprolol

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13
Q

β-blockers with membrane stabilizing activity:

PALOCA

A
Propranolol
Alprenolol
Labetalol
Oxprenolol
Carvedilol
Acebutolol
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14
Q

Cardioselective β1 blockers:

CABNAME

A
Celiprolol
Atenolol
Betaxolol
Nebivolol
Acebutolol
Metoprolol
Esmolol
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15
Q

β1 blockers are preferred in patients with:

A

Bronchospasm
Diabetes
Peripheral vascular disease

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16
Q

β-blockers with intrinsic sympathetic activity:

APOCAP

A
Alprenolol
Pindolol
Oxprenolol
Carteolol
Acebutolol
Penbutolol
17
Q

Major adverse effect of β-blockers:

A

Bronchoconstriction (use CABNAME or APOCAP)

18
Q

ISA β-blockers are useful in patients with:

A
Diminished cardiac reserve
Propensity for bradycardia
Bronchospasm
Diabetes
Peripheral vascular disease
19
Q

Non-cardio selective β-blockers are used in wide/open-angle glaucoma:

A

Timolol
Levobunolol
Carteolol
Metipranolol

20
Q

β1 blockers used in wide/open-angle glaucoma:

A

Betaxolol

Levobetaxolol

21
Q

Important adverse effects of propanolol:

A

Prolonged hypoglycemia
Uterine contractions
Increased risk of atherosclerosis
Withdrawal syndrome

22
Q

PK properties of propanolol:

A
Highly lipophilic
25-30% oral bioavailability (increases with fatty food)
Saturable hepatic extraction
Large volume of distribution
Weakly β-antagonistic active metabolite
23
Q

Therapeutic uses of propanolol:

A
HTN
Angina pectoris
Arrhythmias
MI
CHF
Thyroid storm
Prophylaxis for migraine
24
Q

β-blockers used for migraine:

A
Propanolol
Metoprolol
Atenolol
Nadolol
Timolol
25
Q

Non-cardioselective β-blockers and their MSA or ISA activity:

A

Propanolol (MSA)
Nadolol (none)
Timolol (none)
Pindolol (ISA)

26
Q

Long-acting β-blockers:

A

Nadolol

Nebivolol

27
Q

β1-blockers and their characteristic PK:

A

Metoprolol (Saturable 1st pass)
Atenolol (hydrophilic, longer 1/2 life)
Esmolol (10-15 min duration of action)

28
Q

α1 and non-selective β-blockers:

A
Labetalol (extensive 1st pass)
Carvedilol
Bucindolol (β3 agonist)
29
Q

Labetalol inhibits ___:

A

norepinephrine transporter

30
Q

Indications for α1 and non-selective β-blockers:

A

Hypertensive emergency and chronic HTN during pregnancy

31
Q

These decrease absorption β-blockers:

A

Aluminum salts

Cholestyramine

32
Q

These increase metabolism of β-blockers:

A

Phenytoin
Rifampin
Phenobarbital
Smoking

33
Q

These increase the BA of propanolol and metoprolol:

A

Cimetidine

Hydralazine

34
Q

These inhibit metabolism of β-blockers:

A
Cimetidine
Hydralazine
Ketoconazole
Antifungals
Antivirals
Macrolides
35
Q

β-blockers with this activity may cause overt CHF:

A

MSA activity