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D1 Spring > Pharmacology - Adrenergic Antagonists and Cholinergic Agonists (Exam 2) > Flashcards

Pharmacology - Adrenergic Antagonists and Cholinergic Agonists (Exam 2) Flashcards

1
Q

Which system do adrenergic antagonists inhibit?

A

SNS (fight or flight)

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2
Q

Most adrenergic antagonists are _________ antagonists for ____ or ____ receptors

A

competitive; a or B

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3
Q

Some adrenergic antagonists are _______ acting ____ receptor agonists

A

centrally; a2

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4
Q

What are adrenergic antagonists used to treat?

A

Cardiovascular and non-cardiovascular diseases

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5
Q

What do a1 antagonists (blockers) INHIBIT?

A

Vasoconstriction
Bladder sphincter contraction

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6
Q

Which drug is an a1 selective antagonist/blocker?

A

Prazosin (and other -osins)

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7
Q

What does Prazosin (a1 selective antagonist) block?

A

a1 receptors in vascular smooth muscles

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8
Q

What is the pharmacological effect of Prazosin (a1 selective antagonist)?

A

Vasodilation (decreases BP)

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9
Q

Prazosin (a1 selective antagonist) is used for the treatment of what?

A

Hypertension
Congestive heart failure
Benign prostate hyperplasia

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10
Q

What kind of drug is Tamsulosin (Flomax)?

A

a1 selective antagonist/blocker

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11
Q

What does Tamsulosin (Flomax) (a1 selective antagonist/blocker) have an effect on?

A

Prostate - helps older men urinate

(little effect on BP)

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12
Q

What are the adverse effects of a1 blockers?

A

Orthostatic and postural hypotension

Floppy iris syndrome during cataract surgery
(a1 agonist is given to dilate the pupil for surgery, but pt taking a1 blocker will have interaction that causes iris to be confused and “floppy”)

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13
Q

Which drugs are non-selective a blockers?

A

Phentolamine
Phenoxybenzamine

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14
Q

What do Phentolamine
and Phenoxybenzamine (non-selective a blockers) treat?

A

Epinephrine secreting tumors of adrenal gland

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15
Q

What drugs are B blockers?

A

-lol drugs

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16
Q

What are B blockers used to treat?

A

Cardiovascular effects due to B1 blockage

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17
Q

What are the cardiovascular effects of B blockers?

A

Decreased HR (anti-arrhythmic)
Decreased force of contraction
Decreased BP

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18
Q

What are the physiological effects of B blockers?

A

Decreased BP, O2 demand, and cardiac workload

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19
Q

What are the adverse effects of B blockers?

A

Bronchoconstriction
Vasoconstriction

(since B blockers are non-selective, they can affect B2 receptors as well)

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20
Q

Which drug is a 1st generation B blocker?

A

Propranolol

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21
Q

Is Propranolol (B blocker) selective or non-selective?

A

Non-selective

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22
Q

What are the side effects of Propranolol (B blocker)?

A

Bronchoconstriction
Vasoconstriction

(blocks B2 receptors since it is non-selective)

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23
Q

What is a potential outcome of using lidocaine with epinephrine on patients taking Propranolol (B blocker)?

A

Cardiac arrest

(Patients taking Propranolol have blockage of B2 receptors which inhibits vasodilation. Too much epinephrine causes enhanced vasoconstriction in these patients)

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24
Q

Epinephrine works on which receptors?

A

a1 (vasoconstriction)
B2 (vasodilation)

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25
Q

What is a potential outcome of using Propranolol (B blocker) on patients with asthma or COPD?

A

Increased bronchoconstriction

(since B2 receptors in lungs are blocked, thus blocking bronchodilation)

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26
Q

What drug is a 2nd generation B blocker?

A

Metoprolol

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27
Q

Is Metoprolol (B blocker) selective or non-selective

A

B1 selective

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28
Q

Which drugs are a 3rd generation B blocker?

A

Labetalol
Carvedilol

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29
Q

Are Labetalol and Carvedilol (B blockers) selective or non-selective?

A

Non-selective

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30
Q

What other receptor do Labetalol and Carvedilol (B blockers) block?

A

a1

(but effect on B is > than a1)

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31
Q

What are the physiological effects of Labetalol and Carvedilol (B blockers)?

A

Decrease BP, HR, cardiac workload (blocks B1)

Vasodilation (blocks a1)

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32
Q

Which B blockers are 1st line drugs?

A

Labetalol and Carvedilol

33
Q

What is Carvedilol (B blocker) used to treat?

A

Hypertension
Heart failure

34
Q

What specific cardiovascular diseases are B blockers generally used for?

A

Arrhythmia
Heart failure
Angina
Hypertension

35
Q

Which drugs are a/B mixed antagonists (B non-specific, a1)

A

Labetalol
Carvedilol

36
Q

What are the adverse reactions of B blockers?

A

Bradycardia
Fatigue

37
Q

What happens to patients who chronically use B blockers?

A

B receptor becomes supersensitive

(slow withdrawal of the drug is required)

38
Q

What do B blockers not mix with?

A

Ca2+ channel blockers

39
Q

What are the metabolic effects of B blockers?

A

Activation of B2 in liver (increases plasma glucose)

Inhibition of B2 (hypoglycemia in type II diabetes)

40
Q

Muscarinic agonists activate _______ subtypes of the receptor (M1-M5)

A

most (if not all!)

(this explains their variety of pharmacological actions)

41
Q

What are cholinergic drug receptors?

A

Muscarinic and nicotinic

42
Q

What are muscarinic and nicotinic receptors stimulated by?

A

ACh

43
Q

Which physiological systems do central cholinergic systems regulate and influence?

A

Regulate cardiovascular, respiratory, GI, etc

Influence cognition and emotion

44
Q

Do cholinergic drugs produce effects on the CNS?

A

Depends on the lipophilicity of the drug

45
Q

Cholinergic/muscarinic agonists have ________ actions and have effects on _______ _______ (sympathetic)

A

parasympathomimetic; sweat glands

46
Q

Cholinergic agonists affect which system?

A

Both parasympathetic and sympathetic

(there are cholinergic receptors for ACh in both)

47
Q

What do cholinergic agonists affect in the parasympathetic system?

A

Heart
Lungs
GI

48
Q

What do cholinergic agonists affect in the sympathetic system?

A

Sweat glands

49
Q

Muscarinic (parasympathomimetic) drugs have _________ parasympathetic responses

A

increased

50
Q

What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the heart?

A

Decreased HR, BP, contractility, AV conduction, cardiac output

51
Q

What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the lungs?

A

Bronchoconstriction

(bad for asthma/COPD patients)

52
Q

What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the eyes?

A

Miosis, decreased intraocular pressure

53
Q

What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the blood vessels?

A

Vasodilation

54
Q

What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the GI system?

A

Excite smooth muscle
Increased GI activity, motility, secretion

55
Q

What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the bladder?

A

Contract detrusor muscle
Relax sphincter muscle
Increased urination

56
Q

What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the exocrine glands?

A

Increased lacrimation, GI secretions, sweating, salivation

57
Q

What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the brain?

A

Inhibit ACh-esterase, leading to increased ACh

58
Q

Does every muscarinic drug produce all the physiological effects?

A

NO

59
Q

Peripheral nicotinic effects are ________, since they are selective towards _________ receptors

A

minimal; muscarinic

60
Q

T/F direct acting cholinergic agonists are clinically useful

A

FALSE, they are not clinically useful due to short duration of action

61
Q

What are the analogs of ACh?

A

Bethanechol
Methacholine

62
Q

What is the naturally occurring alkaloid?

A

Pilocarpine (treats xerostomia)

63
Q

Analogs of ACh and naturally occurring alkaloids produce prominent _________ effects

A

muscarinic (aka parasympathomimetic)

64
Q

What are indirect acting cholinergic agonists called?

A

Anti-cholinesterases

(ACh esterase inhibitors)

65
Q

T/F both direct acting cholinergic agonists and anti-cholinesterases produce cholinergic effects

A

True

66
Q

What drug is an anti-cholinesterase?

A

Neostigmine
Physostigmine

67
Q

What are the 2 subclasses of anti-cholinesterases?

A
  1. Reversible inhibitors (neostigmine, physostigmine)
  2. Irreversible inhibitors (organophosphates - pesticides and nerve gas)
68
Q

What is the derivative of physostigmine (reversible anti-cholinesterase)?

A

Neostigmine

69
Q

Anti-cholinesterases require _______ to be present

A

ACh

70
Q

Anti-cholinesterases have pharmacological actions identical to those of ACh, producing _______ and _______ effects

A

Muscarinic and nicotinic

71
Q

What is Myasthenia Gravis?

A

Chronic autoimmune disease

72
Q

Myasthenia Gravis has auto-antibodies against ____ ________ receptors

A

ACh nicotinic

73
Q

What is used to treat Myasthenia Gravis by increasing ACh and thus neuromuscular transmission via nicotinic receptors?

A

Reversible anti-cholinesterase inhibitors (neostigmine)

74
Q

What neurochemical is affected early in the course of Alzheimer’s?

A

ACh

75
Q

What is used to treat Glaucoma?

A

Pilocarpine

76
Q

What is used to treat paralytic ileus and bladder atony (after abdominal/pelvic surgery)?

A

Bethanechol
Neostigmine

77
Q

What are the adverse effects of cholinergic drugs?

A

Colon “choline” SLUDGE

Salivation, sweating
Lacrimation
Urination
Defecation
GI distress
Emesis

78
Q

Do not take _______ drugs with GI or urinary tract obstruction

A

cholinergic

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