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Pharmacology > Reversal Agents > Flashcards

Reversal Agents Flashcards

1
Q

T/F: PNS postganglia secrete epinephrine

A

False: secrete ACh.

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2
Q

Where does PNS originate from?

A

Craniosacral origin (III, V, VII, X).

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3
Q

Where is the highest concentration of acetylcholinesterases?

A

In between the synapses.

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4
Q

What are the two types of cholinergic receptors?

A

Nicotinic and muscarinic

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5
Q

What does SNS stimulation of bronchial smooth muscle cause? PNS?

A

SNS causes relaxation.

PNS causes normal activity to contraction

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6
Q

What does SNS stimulation cause on gallbladder? PNS?

A

SNS= relaxation.

PNS=Contraction.

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7
Q

What does SNS stimulation cause on urinary bladder? PNS?

A

SNS=smooth muscle relaxation and sphincter contraction.

PNS=Smooth muscle contraction and sphincter relaxation

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8
Q

What does SNS stimulation cause on GI tract? PNS?

A

SNS=Dec motility/secretions, sphincter constriction.

PNS=Inc motility/secretion and sphincter relaxation

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9
Q

What is gluconeogenesis?

A

Making new glucose

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10
Q

SNS or PNS cause miosis?

A

PNS=miosis

SNS=mydriasis

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11
Q

SNS or PNS decrease beta cell secretion of pancreas?

A

SNS= want more glucose available so insulin will decrease

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12
Q

What is down regulation?

A

Extended exposure to agonists reduces the number, but not their response. (results in tachyphylaxis)

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13
Q

What is tachyphylaxis?

A

Rapidly diminishing response to successive doses of a drug, rendering it less efective.

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14
Q

What is up regulation?

A

Chronic depletion of catecholamines or use of antagonists increases the number of receptors, but not their sensitivity. May account for withdrawal syndrome with beta blockers.

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15
Q

What is sequestration?

A

Occurs slowly. Movement of receptors from the cell surface to intracellular compartments.

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16
Q

What does pheochromocytoma cause?

A

Uncontrolled release of catecholamines due to an adrenal gland tumor. Constant SMS stimulation

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17
Q

What causes the adrenal medulla to release hormones?

A

Release triggered by ACh at cholinergic fibers due to calcium ion influx.

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18
Q

What are the two classes of anticholinesterase drugs?

A

Tertiary amines and Quaternary ammoniums.

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19
Q

Which class of anticholinesterase drugs enters the CNS more easily?

A

Tertiary amines

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20
Q

What is an example of a tertiary amine anticholinesterase drug?

A

Physostigmine

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21
Q

What is an example of a quaternary ammonium anticholinesterase?

A

Edrophonium.
Neostigmine.
Pyridostigmine.

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22
Q

Which anticholinesterase class is more lipophilic?

A

tertiary amines like physostigmine.

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23
Q

What is the general idea behind giving anticholinesterase drugs as reversal of ND-NMBAs?

A

Attempting to increase the amount of acetylcholine so it “bullies” off the drug.

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24
Q

What are the three actions performed by anticholinesterase drugs?

A
  1. Enzyme Inhibition.
  2. Presynaptic effects.
  3. Direct effects.
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25
Q

What action is the primary action of anticholinesterase drugs?

A

Enzyme inhibition: Inhibites acetylcholinesterase

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26
Q

T/F: Anticholinesterase is a competitive agonist?

A

False: it is a competitive antagonist

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27
Q

By inhibiting acetylcholinesterase, anticholinesterase drugs increase availability of acetylcholine at what three sites?

A
  1. Neuromuscular junction.
  2. Muscarinic receptors.
  3. Autonomic ganglia
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28
Q

Which drug forms a reversible electrostatic attachment ?

A

Edrophonium.

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29
Q

T/F:Even at greater than clinical doses, anticholinesterase drugs have not been reported to produce neuromuscular blockade?

A

False; they do

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30
Q

What are the three classifications for anticholinesterase drugs?

A
  1. Reversible inhibition.
  2. Formation of carbamyl esters.
  3. Irreversible inhibition.
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31
Q

Which drug would be considered a reversible inhibitory anticholinesterase?

A

Edrophonium: Electrostatic attachment to the anionic site.

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32
Q

What is the most important determinant of potency for anticholinesterase drugs?

A

Affinity for receptor

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33
Q

What is the onset of different anticholinesterase drugs?

A

Edrophonium- 1-2 min.
Neostigmine 7-11min
Pyridostigmin 16 min.

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34
Q

Why does edrophonium have such a fast onset?

A

Electrostatic attachment

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35
Q

What is the duration of action for anticholinesterase drugs?

A

60-120 mins

36
Q

What is the influence of age on neostigmine dose?

A

dose in Infants

37
Q

What are the muscarinic effects of anticholinesterase drugs?

A

bradycardia, salivation, bronchoconstriction, miosis, hyperperistalsis, increase risk of PONV.

38
Q

T/F: Edrophonium produces marked and prolonged inhibition of plasma cholinesterase?

A

False: neostigmine and pyridostigmine.

39
Q

Which drug is used for treatment of myasthenia gravis?

A

pyridostigmine.

40
Q

How does pyridostigmine treat myasthenia gravis?

A

Increases ACh at the neuromuscular junction.

41
Q

Does the reversal of NMB by anticholinesterase drugs act presynaptically or postsynaptically?

A

Both

42
Q

What must first occur before administration of anticholinesterase for NMB reversal?

A

Must be spontaneously recovering from NMB.

43
Q

What type of drug is given simultaneously with an anticholinesterase drug to block muscarinic effects?

A

Anticholinergic.

44
Q

Do you want the anticholinergic or the anticholinesterase drug to have a faster onset and why?

A

Anticholinergic.

To minimize bradycardia.

45
Q

At what percent of twitch height recovery would you administer reversal ?

A

> 10%

46
Q

What can inhibit or prevent antagonism of neuromuscular blockade?

A

Antibiotics (aminoglycosides).
Hypothermia.
Resp Acidosis.
Hypokalemia and metabolic acidosis.

47
Q

Physostigmine reverses what 4 things?

A
  1. Anticholinergic OD.
  2. Opiods (not the analgesia).
  3. Benzodiazepines.
  4. Anesthetics
48
Q

What are some secondary uses for physostigmine?

A

Glaucoma, Alzheimer’s disease, Chronic Fatigue Syndrome, Diagnosis and management of cardiac arrhythmias, postop analgesia, postop shivering.

49
Q

What are two examples of naturally occuring tertiary amines anticholinergic?

A

Atropine and scopolamine.

50
Q

What is an example of a quaternary ammonium anticholinergic?

A

Glycopyrrolate.

51
Q

Which has the ability to cross the blood brain barrier - glycopyrrolate, atropine, scopolamine?

A

Atropine and scopolamine (they are tertiary amines).

52
Q

Anticholinergic drugs come in racemic mixtures that are left or right antiomers?

A

Left- levo-antiomers.

53
Q

What structurally binds to the receptor on an anticholinergic drug?

A

The positively charged nitrogen.

54
Q

Are anticholinergic drugs competive/noncompetitive? Antagonist/agonist?

A

Competitive antagonists.

55
Q

What is the main mechanism of action of anticholinergic drugs?

A

Reversibly binds to muscarinic receptors (through competitive antagonism) which prevents ACh from binding.

56
Q

How many muscarinic subtypes are there?

A

5 (M1, M2, M3, M4, M5).

57
Q

What does acetylcholine do once it binds to a muscarinic cholinergic receptor?

A

Binds to one of the M1-M5 receptor subtypes. Causes second messengers to be sent and boosts the signal of M1-M5 to the appropriate site of action.

58
Q

Which muscarinic receptor subtype has clinical effects on the heart and what does it do?

A

M2. Causes bradycardia

59
Q

Why does M2 stimulation via ACh cause bradycardia?

A

Decreases/inhibits Ca++

60
Q

Which muscarinic receptor subtypes are most susceptible to effects of drugs?

A

M3>M2, M1.

61
Q

Why should small (subclinical) dosing of anticholinergics be avoided?

A

Can produce bradycardia due to direct agonist effects.

62
Q

What is the onset and duration of atropine?

A

1 minute.

30-60mins.

63
Q

What is the onset and duration of glycopyrrolate?

A

2-3mins.
.
30-60mins

64
Q

What are all the uses of anticholinergic drugs?

A 
Preop for sedation/antisialagogue,/ prevent vagal reflexes.
Treat reflex-mediated bradycardia.
Combined with anticholinesterase drugs.
Bronchodilation.
Prevent motion-induced nausea.
65
Q

Which anticholinergics can be used for their sedative effects?

A

Scopolamine.

Atropine.

66
Q

Since atropine has mydriatic effects, which patients should it be avoided in?

A

Glaucoma. Increased IOP

67
Q

Which anticholinergic drugs have more potent antisialagogue effects?

A

Scopolamine 3x more potent and glycopyrrolate 2x more potent than atropine.

68
Q

Which anticholinergic is the drug of choice for intraoperative bradycardia?

A

Atropine.

69
Q

What is atropine’s MOA when given for bradycardia?

A

Blocks effects of ACh on the SA node.

70
Q

Which age patients have the most profound response to atropine for bradycardia?

A

Young adults

71
Q

What are examples of anticholinergics that ause bronchodilation specifically?

A

Ipatropium/atrovent/duoneb.

72
Q

Which muscarinic receptor subtype is involved in bronchodilation?

A

M3

73
Q

Scopolamine must be given how many hours before noxious stimuli?

A

4 hours prior.

74
Q

How long should scopolamine stay on as transdermal patch after surgery?

A

24 hours

75
Q

What is Central Anticholinergic Syndrome?

A

When scopolamine and atropine enter the CNS and cause Restlessness and hallucinations to somnolence and unconsciousness.

76
Q

What are symptoms of anticholinergic overdose?

A

(can’t see, cant pee, cant spit, cant shit).Dry mouth, blurred vision, photophobia, tachycardia, dry/flushed skin,

77
Q

What is treatment of anticholinergic overdose?

A

Physostigmine 15-60mcg/kg IV

78
Q

Why did the FDA initially not approve suggamedex?

A

Bleeding and anaphylactic complications

79
Q

Which NMBAs does suggamedez reverse?

A

Vecuronium and rocuronium.

80
Q

What is suggamedex dose if 1-2 post-tetanic counts and there is not response to TOF?

A

4mg/kg

81
Q

What is suggamedex dose if reappearance of the second twitch response to TOF?

A

2mg/kg

82
Q

What is suggamedex dose for rapid reversal of roc bolus dose?

A

16mg/kg

83
Q

What are side effects of suggamedex?

A 
0.3% anaphylaxis.
Bradycardia.
Bleeding/coagulopathies.
N/V, pain, hypotension, headache.
Not recommended for use in severe renal impairment.
BC pills have reduced efficacy.
84
Q

What is a Cochrane Review?

A

A bunch of smaller studies combined to strengthen an argument.

85
Q

What did the Cochrane Review 2017 determine?

A
  1. Suggamedex will reverse deep blockade.

2. Neostigmine really only works on spontaneously reversing patients (not DEEP blockade.

Pharmacology (9 decks)

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