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Pharmacology Test #3 > Sympatholytic pharmacology > Flashcards

Sympatholytic pharmacology Flashcards

1
Q

orthosteric

A

site where NE binds directly to block the ability of the agonist to bind

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2
Q

allosteric

A

not binding directly to site where NE binds, but blocks binding at another site

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3
Q

side effects of alpha1 receptor antagonists

A

orthostatic hypotension, inhibition of ejaculation, nasal stuffiness, tachycardia

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4
Q

What kind of agonist is Phenoxybenzamine (Dibenzyline)?

A

non-selective alpha receptor antagonist

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5
Q

What else does Phenoxybenzamine block?

A

acetylcholine, histamine, and serotonin receptors

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6
Q

What kind of antagonist is Phenoxybenzamine?

A

irreversible antagonist resulting from covalent modification of receptor

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7
Q

When would you use Phenoxybenzamine?

A

not used anymore

historically was used in HTN crisis and pheochromocytoma

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8
Q

What type of antagonist is Phentolamine (Regitine)

A

non-selective alpha receptor antagonist
competitive/reversible blocker
muscarinic and histamine receptor agonist

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9
Q

What kind of effects does Phentolamine produce?

A

potent vasodilation, but induces pronounced reflex tachycardia

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10
Q

What does Phentolamine block?

A

blocks presynaptive alpha2 receptors (may promote release of NE) and 5-HT receptors

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11
Q

Quinazolines

A

Prazosin, Terazosin, and Doxazosin

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12
Q

What kind of antagonists are quinazolines?

A

alpha-1 adrenergic receptor antagonists

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13
Q

What do quinazolines do?

A

vasodilators, relaxation of smooth muscle in enlarged prostate and in bladder base

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14
Q

How do the three quinazolines vary?

A

Vary in half-life:
Prazosin - 3 hours
Terazosin - 12 hours
Doxazosin - 20 hours

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15
Q

Describe the “first dose” effect of quinazolines

A

orthostatic hypotension occurs with the first dose, but you’ll become tolerant over the first 24 hours

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16
Q

What kind of receptor antagonist is Yohimbine (Yocon)?

A

alpha2-adrenergic receptor antagonist

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17
Q

What does Yohimbine do?

A

blockade of alpha2 receptors increases sympathetic discharge, off the market, doesn’t really do anything, used in herbal supplements

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18
Q

Aryloxypropanolamines are what kind of drugs?

A

beta blockers

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19
Q

Propranolol

A

non-selective beta blocker, lipophilic (CNS penetration), local anesthetic properties (Na+ channel blocker), first gen but still used a lot

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20
Q

Therapeutic uses for beta-adrenergic receptor antagonists

A

hypertension, angina, cardiac arrhythmias, migraine, stage fright, thyrotoxicosis, glaucoma, congestive heart failure (types II and III)

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21
Q

Pharmacological effects of beta blockers

A

decreased cardiac output and heart rate, reduced renin release*, increase VLDL, decrease HDL, inhibit lipolysis, increase bronchial airway resistance, inhibit compensatory glycogenolysis and glucose release in response to hypoglycemia

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22
Q

Non-selective beta-adrenergic receptor antagonists

A

Propranolol, Nadolol, Timolol, (Pindolol, and Carteolol)

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23
Q

Uses of Nadolol

A

hypertension, angina, migraine

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24
Q

How is Nadolol different from propranolol?

A

less lipophilic than propranolol

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25
Q

Describe the structure of Timolol

A

thiadiazole nucleus with morpholine ring

26
Q

Uses of Timolol

A

hypertension, angina, migraine, glaucoma

27
Q

How do beta blockers affect pupil size?

A

they don’t

28
Q

What type of antagonist is Pindolol?

A

partial agonist, possesses “intrinsic sympathomimetic activity”

29
Q

Uses of Pindolol

A

hypertension, angina, migraines

30
Q

Significance of Pindolol and Carteolol being partial agonists

A

less likely to cause bradycardia and lipid abnormalities

31
Q

What type of antagonist is Carteolol?

A

partial agonist, possesses “intrinsic sympathomimetic activity”

32
Q

Uses of Carteolol

A

hypertension, glaucoma

33
Q

What type of antagonist are Metopropol and Bisopropol?

A

selective beta1-adrenergic receptor antagonists, cardioselective

34
Q

Consequence of “cardioselective” beta blockers

A

less bronchoconstriction

35
Q

Uses of Metoprolol and Bisoprolol

A

hypertension, angina, antiarrhythmic, congestive heart failure

36
Q

What type of antagonist is Atenolol?

A

selective beta1-adrenergic receptor antagonist; cardioselective

37
Q

What is the lipophilicity of Metoprolol and Bisoprolol?

A

moderate lipophilicity

38
Q

What is the lipophilicity of Atenolol?

A

low lipophilicity

39
Q

Uses of Atenolol

A

hypertension, angina

40
Q

What type of antagonist is Esmolol?

A

selective beta1-adrenergic receptor antagonist

41
Q

Uses of Esmolol

A

supraventricular tachycardia, atrial fibrillation/flutter, perioperative hypertension

42
Q

How long does it take Esmolol to act?

A

very short acting

half life is 9 minutes

43
Q

What kind of antagonist is Nebivolol

A

3rd generation beta1-adrenergic receptor antagonist

44
Q

Selectivity of Nebivolol

A

beta1 selectivity

45
Q

Effects of Nebivolol

A

vasodilation due to nitric oxide production

46
Q

Uses of Nebivolol

A

hypertension

47
Q

What type of antagonist is Labetalol

A

mixed adrenergic receptor antagonist:
non-selective beta receptor antagonist
alpha1 receptor antagonist

48
Q

What is the significance of Labetalol being a racemic mixture?

A

(1R, 1’R) isomer is a beta blocker

(1S, 1’R) isomer is an alpha1 blocker

49
Q

Beta-blocking activity of Labetalol prevents?

A

prevents reflex tachycardia normally associated with alpha1 receptor antagonists

50
Q

Uses of Labetalol

A

hypertension, hypertensive crisis

51
Q

What kind of antagonist is Carvedilol

A

mixed adrenergic receptor antagonist:
non-selective beta receptor antagonist
alpha1 receptor antagonist

52
Q

Significance of Carvedilol having enantiomers

A

both enantiomers antagonize alpha1 receptors

only (S) enantiomer possesses beta blocking activity

53
Q

beta blocking activity of Carvedilol prevents

A

prevents reflex tachycardia normally associated with alpha1 receptor antagonists

54
Q

Uses of Carvedilol

A

hypertension, congestive heart failure (II and III), anti-oxidant activity

55
Q

Side effects of beta blockers

A

bradycardia, AV block, sedation, mask symptoms of hypoglycemia, withdrawal syndrome (taper doses down)

56
Q

Withdrawal syndrome with beta blockers

A

pronounced tachycardia, hypertension

57
Q

contraindications of beta blockers

A

Asthma, COPD, congestive heart failure (type IV-final stage)

58
Q

What kind of drug is Reserpine

A

Catecholamine depleter

59
Q

Mechanism of Reserpine

A

blocks vesicular monoamine transporters, depletes vesicular pool of NE

60
Q

Use of Reserpine

A

used in the treatment of hypertension

61
Q

Side effect of Reserpine

A

may precipitate depression, lead to the discovery of anti-depressants

62
Q

Significance of the slow onset of action of Reserpine

A

doesn’t trigger baroreceptor reflex

Pharmacology Test #3 (13 decks)

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