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3 Pharma > Beta blockers > Flashcards

Beta blockers Flashcards

1
Q

What differentiates 3rd gen B blockers?

A

They have vasodilatory properties: alpha block or NO release.

They can be either non-selective or B1-selective.

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2
Q

Example of lipophilic BB?

A

propanolol, penbutolol

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3
Q

Example of hydrophilic BB?

A

atenolol, nadolol

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4
Q

Which BB has an uncharacteristic short duration and fast onset?

A

esmolol

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5
Q

Which enzyme’s genotype is a major determinant in interindividual differences of metabolism?

A

CYP2D6

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6
Q

General effects of SHORT-TERM use of BBs on CVS:

A 
Decreased CO (B1 block)
Increased PVR (B2 block = A1 vasoconstriction is unopposed)
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7
Q

BBs Anti-HTN properties can be explained by:

A

1) Sustained use results in decreased TPR in HTN patients
2) B1 block –> decreased renin secretion from JG cells (PINDOLOL does not affect)
3) Vasodilatory properties of some BBs

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8
Q

This effect or property of some BBs involves the inhibition or total abolition of action potential from being propagated across the membrane via SODIUM CHANNEL BLOCK.

What is the physiological basis behind treatment with these drugs?

Which drugs exhibit this pharmacological effect?

A

Membrane Stabilizing Activity. Decreased sinus rhythm, conduction –> generalized suppression of myocardial function.

PALOCA:
Propranolol
Alprenolol
Labetalol
Oxprenolol
Carvedilol
Acebutolol
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9
Q

Advantages of sodium channel blockade include:

A

prophylaxis to prevent recurrent MI and sudden death

limits size of infarct

reduce mortality

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10
Q

Disadvantages of sodium channel blockade

A

latent heart failure to overt heart failure

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11
Q

Cardioselective BB blockers block which receptor?

A

B1

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12
Q

Cardioselective BBs include the following drugs:

A 
CABNAME:
Celiprolol
Acebutolol
Betaxolol
Nebivolol
Atenolol
Metoproplol
Esmolol
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13
Q

Cardioselective BBs are preferred in patients with:

A

Bronchospasm/asthma/COPD
DM
Raynaud’s

(because B2 is not blocked…B2 blockage results in vasoconstriction and bronchoconstriction)

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14
Q

Beta blockers with partial agonist properties are said to exhibit:

A

Intrinsic sympathomimetic activity (ISA).

The structural specificity of the drugs allowing competitive binding to the receptor (antagonist activity) and partial interaction at the receptor’s activation site (agonist activity).

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15
Q

BBs with partial agonistic activity include:

A 
APOCAP
Alprenolol
Pindolol
Oxprenolol
Carteolol
Acebutolol
Penbutolol
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16
Q

Respiratory effect from BB

A

Nonselectives cause bronchoconstriction

Selective B1 and those with ISA at B2 are less likely to cause this.

17
Q

Metabolic effects from BB

A

Hypoglycemia

FFA release

18
Q

BBs effects on eyes

A

Decrease aqueous humor production

19
Q

Non-selective beta blocker used in CHF, Thyroid storm. High Vd, enters CND readily, low oral bioavailability due to extensive first-pass metabolism.

A

Propranolol

20
Q

Non-selective BB with no ISA or MSA activity. Does not cross BBB. Used in HTN, agina; off-labeled in migraine prophylaxis, parkinsonian tremors, variceal bleeding in portal HTN.

A

Nadolol

21
Q

Non-selective BB used in HTN, CHF, acute MI and OPEN-ANGLE GLAUCOMA (fewer side-effects than anti-cholinesterase or muscarics)

A

Timolol

22
Q

Non-selective BB with ISA, low MSA. Used in HTN, angina. Blocks exercise-induced increase in HR and CO.

A

Pindolol

23
Q

B1 blocker with MSA but no ISA.

Used in HTN, angina, tachycardia, heart failure, hyperthyroidism, migraine prophylaxis.

A

Metoprolol

24
Q

B1 blocker with (-) ISA, (-) MSA. Water soluble, longer half life than metoprolol.

A

Atenolol

25
Q

Ultra-short duration B1 blocker. Little ISA, (-) MSA. Used in critically ill, controlling supraventricular arrhythmias, thyrotoxicosis arrhythmias, perioperative HTN.

A

Esmolol

26
Q

A1 and non-selective B blocker. Partial agonist at B2. Used in pregnancy HTN.
Cocaine-like effect.

A

Labetalol

27
Q

A1 and non-selective B blocker.

Vasodilator, antioxidant, antiproliferative.

A

Carvedilol

Very popular for use in CHF

28
Q

3rd gen: A1 and non-selective B blocker. Partial B2 and B3 agonist. Reduces afterload. Increase plasma HDL.

A

Bucindolol

29
Q

BB Treatment of arrhythmias:

A

Esmolol

30
Q

BB Treatment of MI:

A

1) long-term use of timolol, propanolol, or metoprolol improve survival
2) esmolol, B blockers with MSA, carvedilol

31
Q

BB Migraine prophylaxis:

A

Propanolol (high lipid solubility)
Less extent: metoprolol
Also: atenolol, timolol, nadolol

32
Q

BB Treatment of thyrotoxicosis:

A

Propanolol and other B blockers

33
Q

BB Treatment of pheochromocytoma:

A

A blocker then B blocker

34
Q

BB (wide angle) Glaucoma

A

Timolol

35
Q

4 BBs with vasodilatory properties

A

Carvedilol
Labetalol
Celiprolol
Nebivolol

36
Q

Which BB is most likely to cause lethargy, mental depression, hallucinations?

A

propanolol

Most lipid solubility so it can cross BBB readily.

37
Q

Adverse metabolic effects of BBs

A

Increased triglycerides (except ISA)
impaired insulin release
impaired hepatic gluconeogenesis

3 Pharma (8 decks)

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