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

(78 cards)

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
What is a potential outcome of using Propranolol (B blocker) on patients with asthma or COPD?
Increased bronchoconstriction (since B2 receptors in lungs are blocked, thus blocking bronchodilation)
26
What drug is a 2nd generation B blocker?
Metoprolol
27
Is Metoprolol (B blocker) selective or non-selective
B1 selective
28
Which drugs are a 3rd generation B blocker?
Labetalol Carvedilol
29
Are Labetalol and Carvedilol (B blockers) selective or non-selective?
Non-selective
30
What other receptor do Labetalol and Carvedilol (B blockers) block?
a1 (but effect on B is > than a1)
31
What are the physiological effects of Labetalol and Carvedilol (B blockers)?
Decrease BP, HR, cardiac workload (blocks B1) Vasodilation (blocks a1)
32
Which B blockers are 1st line drugs?
Labetalol and Carvedilol
33
What is Carvedilol (B blocker) used to treat?
Hypertension Heart failure
34
What specific cardiovascular diseases are B blockers generally used for?
Arrhythmia Heart failure Angina Hypertension
35
Which drugs are a/B mixed antagonists (B non-specific, a1)
Labetalol Carvedilol
36
What are the adverse reactions of B blockers?
Bradycardia Fatigue
37
What happens to patients who chronically use B blockers?
B receptor becomes supersensitive (slow withdrawal of the drug is required)
38
What do B blockers not mix with?
Ca2+ channel blockers
39
What are the metabolic effects of B blockers?
Activation of B2 in liver (increases plasma glucose) Inhibition of B2 (hypoglycemia in type II diabetes)
40
Muscarinic agonists activate _______ subtypes of the receptor (M1-M5)
most (if not all!) (this explains their variety of pharmacological actions)
41
What are cholinergic drug receptors?
Muscarinic and nicotinic
42
What are muscarinic and nicotinic receptors stimulated by?
ACh
43
Which physiological systems do central cholinergic systems regulate and influence?
Regulate cardiovascular, respiratory, GI, etc Influence cognition and emotion
44
Do cholinergic drugs produce effects on the CNS?
Depends on the lipophilicity of the drug
45
Cholinergic/muscarinic agonists have ________ actions and have effects on _______ _______ (sympathetic)
parasympathomimetic; sweat glands
46
Cholinergic agonists affect which system?
Both parasympathetic and sympathetic (there are cholinergic receptors for ACh in both)
47
What do cholinergic agonists affect in the parasympathetic system?
Heart Lungs GI
48
What do cholinergic agonists affect in the sympathetic system?
Sweat glands
49
Muscarinic (parasympathomimetic) drugs have _________ parasympathetic responses
increased
50
What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the heart?
Decreased HR, BP, contractility, AV conduction, cardiac output
51
What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the lungs?
Bronchoconstriction (bad for asthma/COPD patients)
52
What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the eyes?
Miosis, decreased intraocular pressure
53
What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the blood vessels?
Vasodilation
54
What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the GI system?
Excite smooth muscle Increased GI activity, motility, secretion
55
What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the bladder?
Contract detrusor muscle Relax sphincter muscle Increased urination
56
What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the exocrine glands?
Increased lacrimation, GI secretions, sweating, salivation
57
What pharmacologic effects do Muscarinic (parasympathomimetic) drugs have on the brain?
Inhibit ACh-esterase, leading to increased ACh
58
Does every muscarinic drug produce all the physiological effects?
NO
59
Peripheral nicotinic effects are ________, since they are selective towards _________ receptors
minimal; muscarinic
60
T/F direct acting cholinergic agonists are clinically useful
FALSE, they are not clinically useful due to short duration of action
61
What are the analogs of ACh?
Bethanechol Methacholine
62
What is the naturally occurring alkaloid?
Pilocarpine (treats xerostomia)
63
Analogs of ACh and naturally occurring alkaloids produce prominent _________ effects
muscarinic (aka parasympathomimetic)
64
What are indirect acting cholinergic agonists called?
Anti-cholinesterases (ACh esterase inhibitors)
65
T/F both direct acting cholinergic agonists and anti-cholinesterases produce cholinergic effects
True
66
What drug is an anti-cholinesterase?
Neostigmine Physostigmine
67
What are the 2 subclasses of anti-cholinesterases?
1. Reversible inhibitors (neostigmine, physostigmine) 2. Irreversible inhibitors (organophosphates - pesticides and nerve gas)
68
What is the derivative of physostigmine (reversible anti-cholinesterase)?
Neostigmine
69
Anti-cholinesterases require _______ to be present
ACh
70
Anti-cholinesterases have pharmacological actions identical to those of ACh, producing _______ and _______ effects
Muscarinic and nicotinic
71
What is Myasthenia Gravis?
Chronic autoimmune disease
72
Myasthenia Gravis has auto-antibodies against ____ ________ receptors
ACh nicotinic
73
What is used to treat Myasthenia Gravis by increasing ACh and thus neuromuscular transmission via nicotinic receptors?
Reversible anti-cholinesterase inhibitors (neostigmine)
74
What neurochemical is affected early in the course of Alzheimer's?
ACh
75
What is used to treat Glaucoma?
Pilocarpine
76
What is used to treat paralytic ileus and bladder atony (after abdominal/pelvic surgery)?
Bethanechol Neostigmine
77
What are the adverse effects of cholinergic drugs?
Colon "choline" SLUDGE Salivation, sweating Lacrimation Urination Defecation GI distress Emesis
78
Do not take _______ drugs with GI or urinary tract obstruction
cholinergic