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Pharmacology -- Test #3 > Adrenergic Antagonists > Flashcards

Adrenergic Antagonists Flashcards

1
Q

Important side effect to remember with alpha adrenergic antagonists

A

Sexual Dysfunction

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2
Q

Three examples of alpha1 adrenergic antagonists

A

Prazosin
Terazosin
Doxazosin

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3
Q

Clinical use of alpha1 adrenergic antagonists

A

Hypertension, Benign Prostatic Hypertrophy

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4
Q

Side effects of alpha1 adrenergic antagonists

A

Orthostatic Hypertension
Inhibition of Ejaculation
Nasal stuffiness
Tachycardia

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5
Q

Important thing to remember about phenoxybenzamine

A

Nonselective (Dirty Drug)

Irreversible antagonist resulting from covalent modification of receptor

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6
Q

Chemical details about phentolamine

A

Non-selective alpha receptor agonist

Competitive

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7
Q

Effects of phentolamine use

A

Potent vasodilator, but gives pronounced tachycardia

blocks presynaptic alpha2 and 5HT

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8
Q

Important difference between Prazosin, Terazosin, and Doxazosin

A

Halflife.
P3
T12
D20

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9
Q

Effects of Prazosin, Terazosin, and Doxazosin?

A

Vasodilators

Relaxation of smooth muscle in enlarged prostate and bladder base

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10
Q

What is the first dose effect?

A

In drugs like Prazosin, Terazosin, and Doxazosin, first dose may lead to orthostatic hypotension

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11
Q

What is Yohimbine?

A

Indole alkaloid

Blocks alpha2 receptors, increasing sympathetic discharge

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12
Q

beta blockers were one of the first major _______ drugs

A

Rationally Designed

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13
Q

Who is the original G of beta blockers

A

Propranolol

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14
Q

Important chemical attributes of beta blockers

A

Non-selective
Lipophillic - CNS access
Local anesthetic properties
Blockade is activity-dependent

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15
Q

Pharmacological effects of Propranolol

A

Lowers CO and heart rate
Reduced Renin Release
Increased VLDL, HDL (inhibited lipolysis)
Inhib. compensatory glycogenolysis and GLU release
Increases bronchial airway resistance

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16
Q

Main way beta blockers inhibit HTN?

A

Reduced Renin Release

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17
Q

Therapeutic uses for beta-blockers?

A

HTN, angina, arrythmia,
migraine, stage fright,
thyrotoxicosis, glaucoma,
CHFII-III

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18
Q

What should you know about Nadolol

A

Less lipophilic than propranolol
Long Half life (20h)
Used for HTN, angina, migraine

19
Q

What should you know about Timolol

A

Thiadiazole nucleus with morpholine ring

HTN, angina, migraine, GLAUCOMA

20
Q

How do beta blockers affect pupil size?

A

They don’t

They’ll decrease pressure without effects like cholinergic

21
Q

What is unique about Pindolol?

A

Possesses Intrinsic sympathomimetic Activity (Partial Agonist)
Less likely to cause bradycardia and lipid abnormalities
HTN, Angina, Migraine

22
Q

Other than Pindolol, whats the other important partial agonist? Why care?

A

Carteolol
Less likely to cause bradycardia and lipid abnormalities
Used for HTN and glaucoma

23
Q

Three selective beta1 adrenergic receptor antagonists

A

Metoprolol, Bisoprolol, Atenolol, Esmolol

24
Q

Metoprolol and Bisoprolol – what does it do?

A

Cardioselective, doesn’t trigger the bronchoconstriction

25
Q

Metoprolol and Bisoprolol half life

A

3-4 hours

26
Q

Metoprolol and Bisoprolol uses?

A

HTN, angina, anti-arrhythmic, CHF

27
Q

What’s the deal with atenolol?

A

Cardioselective, low lipophilicity, 6-9 hour halflife

Treats HTN and angina

28
Q

What characteristic of Esmolol different from the other beta1 adrenergic receptor antagonists?

A

Very short half life (ex. 9 minutes) caused by rapid hydrolysis by esterases found in RBCs

29
Q

What is Esmolol used to treat?

A

Supraventricular tachycardia
Atrial fibrillation/Fluter
Perioperative HTN

30
Q

Who did he say was a 3rd gen beta blocker

A

Nebivolol (Bystolic)

31
Q

Important details for nebivolol

A

Beta1 selective, but also causes vasodilation by NO production
Used to treat HTN

32
Q

Two examples of mixed adrenergic receptor antagonists

A

Labetalol

Carvedilol

33
Q

Chemical mechanism of Labetalol

A

Non-selective beta receptor antagonist + alpha1 receptor antagonist

34
Q

What is Labetalol used for?

A

beta-blocking activity prevents reflex tachycardia normally associated with alpha 1 receptor antagonists

HTN, Hypertensive Crisis

35
Q

Chemical data for Carvedilol?

A

Non-selective beta antagonist, alpha1 receptor antagonist

36
Q

How does Carvedilol work?

A

Beta blocking activity prevents reflex tachycardia normally associated with alpha1 receptor antagonists

37
Q

Uses for Carvedilol?

A

HTN, CHF

38
Q

Side effects associated with beta-blockers

A

Bradycardia, AV block, sedation, mask symptoms of hypoglycemia, withdrawl

39
Q

Contraindications for beta blockers?

A

Asthma, COPD, CHF-Type 4

40
Q

Example given for a catecholamine depleter

A

Reserpine

41
Q

Molecular activity of Reserpine

A

Block vesicular monoamine transporters

Depletes the vesicular pool of NE

42
Q

Reserpine is used to treat…

A

HTN

43
Q

Important side effect of Reserpine

A

Depression

Pharmacology -- Test #3 (13 decks)

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