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CV PHARM...Antihypertensives > Beta-Blockers > Flashcards

Beta-Blockers Flashcards

1
Q

MOA of BB w/ no ISA

A

decrease HR and contractility–> Decrease CO

inhibit renin release (EXCEPT Pindolol)

Decrease central sympathetic outflow (except for those w/ low lipid solubility)

Decrease release of peripheral NE by inhibiting presynaptic beta adrenergic receptors

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2
Q

Pindolol

A

does not inhibit decrease renin release

High ISA, some MSA, no cardioselectivity, lipid soluble

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3
Q

Utility of BB w/ no ISA

A

Especially useful in pts w/ high renin level HTN

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4
Q

Effects of BBs w/ no ISA

A

w/ chronic use…

decrease CO and peripheral resistance and arterial pressure

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5
Q

Clinical uses of 1st and 2nd generation B-blockers in HTN

A

effective therapy for all grades of HTN

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6
Q

Clinical uses of 1st and 2nd generation B-blockers in HTN…

More effective in…

A

High renin HTN

young and caucasian

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7
Q

Clinical uses of 1st and 2nd generation B-blockers in HTN:

Less effective in…

A

Low renin HTN

elderly and AA

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8
Q

BBs and diuretics

A

BBs do not cause H20 and salt retention
–so can be administered w/out diuretic

But has additive antihypertensive effect when administered w/ diuretic

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9
Q

Highly preferred in hypertensive pts w/…

A 
MI
ischemic heart disease
HF
hyperthyroidism
migraines
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10
Q

CHF

A

3rd generation BBs
carvedilol
metaprolol-XL
bisoprolol

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11
Q

MI

A

useful in preventing 2nd MI

perhaps b/c of bradycardia?

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12
Q

Other indications

A

Sinus and AV arrhythmias
open angle glaucoma
anxiety

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13
Q

Propranolol uses

A

Non-selective BB that produces resting bradycardia and decrease HR during exercise –> hypotension

membrane stabilizing activity: antiarrhythmic

produces bronchospasm; contraindicated in asthmatics

slow withdrawal of drug to prevent reflex tachycardia

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14
Q

Metoprolol and Atenolol

A

50-100-fold more selective in blocking β1-adrenergic receptors

“Cardioselective agents”

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15
Q

Bisoprolol

A

Long-acting drug (take once a day

significantly decreases all case mortality

glaucoma eyedrops

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16
Q

PIndolol and acebutolol

A

Non-selective drugs with partial agonist activity.

Decrease CO and HR less than other drugs.

17
Q

Esmolol

A

ARRHYTHMIAS!!!

Selective drug w/ VERY short half-life

Given IV for management of tachycardia, arrhythmias during surgery and postoperative tachycardia caused by halothane anesthetic

18
Q

Timolol

A

non-selective drug

eye-drops for Rx of chronic open angle glaucoma

19
Q

Side effects

A

Cold extremities

Bradycardia

Bronchospasm (avoid ALL drugs w/ asthma; permitted w/ COPD)

CNS side effects

Metabolic

Drug withdrawal syndrome

fatigue, decreased exercise tolerance, impotence

20
Q

Cold extremities side effect

A
  • -Unopposed α adrenergic action constricts BV in the skin and limits blood flow causing cold extremities.
  • -Prolonged use worsens peripheral arterial insufficiency; Raynaud’s phenomenon.
21
Q

Bradycardia side effect

A

Decreased AV nodal conduction; contraindicated with verapamil
and diltiazem

22
Q

Metabolic side effects

A
  • Block glycogenolysis and delay recovery from hypoglycemia in type 1 diabetics (seen with non-selective drugs but less frequently with ß1-selective agents).
  • Block HSL in adipocytes and increase LDL and reduce HDL and increase triglycerides.
23
Q

Drug withdrawal syndrome

A

Prolonged drug use upregulates β-receptors in the heart.

Abrupt withdrawal causes tachycardia; withdraw slowly!!!!

24
Q

3rd Generations:

Labetalol

A

non-selective beta + a1 antagonist

given IV for HTN emergencies

25
Q

3rd Generations:

Carvedilol

A

non-selective β + α1-receptor antagonist

By blocking α1-AR, CO maintained with increased fall in peripheral resistance.

  • Antioxidant; binds and scavenges ROS
  • Protects membranes from lipid peroxidation. Prevents LDL oxidation and decreases LDL uptake into coronary blood vessels.
  • Primarily used for CHF & HTN; decreased mortality and morbidity in pts w/ mild to moderate CHF
  • PO; extensively protein bound; hepatic (2D6) metabolism
26
Q

3rd Generations;

Celiprolol

A

Cardio-selective + beta2 agonism

Directly vasodilates BV due to partial ß2- agonist activity.

Used for treatment of HTN and angina.

27
Q

3rd Generations

Nebivolol

A

drugs w/ NO mediated vasodilation

Highly β1 selective; devoid of ISA, membrane stabilizing activities, and α1 blocking activities.

  • Has antioxidant activity/neutral to favorable effects on both carb and lipid metabolism.
  • decreased BP by decreasing HR and peripheral vascular resistance.
  • Significantly increases stroke volume, maintains CO and systemic blood flow.
  • Drug of choice for HTN with metabolic syndrome!!!
28
Q

Propanolol

A

MSA, lipid soluble

29
Q

Metoprolol

A

some MSA, cardioselective, lipid soluble

30
Q

Atenolol

A

cardioselective, NOT lipid soluble

31
Q

Timolol

A

some ISA, lipid soluble

CV PHARM...Antihypertensives (11 decks)

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