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Pharmacology I > Reversal Agents > Flashcards

Reversal Agents Flashcards

1
Q

Primary neuro transmitter of SNS

A

Norepinephrine (dopamine, norepinephrine, epi) all related

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2
Q

_______ ____ ________ converts dopamine to ________.

A

Dopamine beta hyroxylase, Norepinephrine.

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3
Q

Norepinephrine is metabolized by…

A

Monamine oxidase (MAO) and catecholamines-o-methyltranserase (COMT).

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4
Q

Alpha 1

A

Postsynaptic (periphery)

“Fight or Flight”

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5
Q

Alpha 2

A

Presynaptic (CNS)

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6
Q

Beta 1

A

Heart

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7
Q

Beta 2

A

Other smooth muscle (periphery)

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8
Q

SLIDE 7 WTF

A

SLIDE 7

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9
Q

Alpha 1 Effects:

A

Postsynaptic

  • > intracellular Ca
  • Smooth muscle contraction
  • Vasoconstriction
  • Bronchoconstriction
  • Inhibits insulin secretion
  • Glycogenolysis and glucongenesis
  • Mydriasis
  • GI relaxation
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10
Q

Alpha 2 Effects:

A

Presynaptic effects in PNS

  • < Ca entry into cell
  • < release of norepinephrine

Postsynaptic in CNS

  • Sedation
  • < SNS outflow
  • < BP
  • Platelet aggregation
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11
Q

Beta 1 Effects:

A

Postsynaptic

  • > HR
  • > Conduction velocity (AV node)
  • > Contractility
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12
Q

Beta 2 Effects:

A

Postsynaptic

  • Smooth muscle relaxation
  • Vasodilation
  • < BP
  • Bronchodilation
  • > insulin secretion
  • > glycogenolysis and gluconeogensis
  • < GI mobility
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13
Q

________ binds to cholinergic receptors.

A

Acetylcholine

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14
Q

Acetylcholine

A

Activates both arms of the ANS

Ca mediated action potential

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15
Q

Cholinergic receptors can either be ________ or _______.

A

Nicotinic or Muscarinic.

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16
Q

See SLIDES 15-17

A

Slides 15-17

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17
Q

Down Regulation (results in)

A

> exposure to Agonists < # of receptors.

Results in tachyplaxis

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18
Q

Up Regulation

A

Use of antagonist > # of receptors.

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19
Q

Tone

A

“Nothing happens all in one direction, always an underlying of the other”.

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20
Q

Catecholamines (5):

A 
Dopamine 
Norepinephrine
Epinephrine
Isoproterenol
Dobutamine
(Neurotransmitters and hormones)
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21
Q

Sympathomimetics

A

Mimics Effects of SNS.

Not all sympatho are catecholamines

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22
Q

___________ ___________ occurs as we age and with diabetes.

A

Autonomic Dysfunction

  • Orthostasis
  • Temp instability
  • < stress response
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23
Q

80% of Epi and NE is released from the…

A

Adrenal Medulla

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24
Q

Are Quaternary Ammonium (NH4) > or < hydrophilic than Tertiary amines (NH3)?

A

>

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25
Q

(1) Tertiary Amine drug:

A

Physostigmine (small enough to cross BBB).

NH3

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26
Q

How many types of Anticholinesterase Drugs?

A

2

Tertiary Amines and Quaternary ammonium.

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27
Q

(3) Quaternary Ammonium drugs:

A

Edrophonium
Neostigmine
Pyridostigmine

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28
Q

Anticholinersterase Drugs have 3 main actions:

A

Enzyme inhibition
Presynaptic effects
Direct effect

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29
Q

Anticholinesterase enzyme inhibits _______________.

A

Acetylcholinesterase

Results in > availability of ACh
(> side effects)

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30
Q

How are enzymes blocked with Edrophonium?

A

Forms a reversible electrostatic attachment (fast action)

Ionic bond/magnetic force
(This changes the enzyme shape and ACh can’t bind)

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31
Q

What two anticholinesterase drugs are hydrolyzed by enzymes?

A

Neostigmine
Pyridostigmine

This carbamylates the enzyme blocking the enzyme’s ability to hydrolyze ACh (Slower)

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32
Q

Acetylcholinesterase inhibitors may produce __________ in the absence of neuromuscular blockers.

A

Fasiculations

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33
Q

Anticholinesterase drugs can produce some form of a ___________ _________ at doses greater than usual clinical doses.

A

Neuromuscular blockade

Like Succ) (receptors are stunned by overstimulation

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34
Q

Is electrostatic attachment (Edrophonium) to enzymes and the formation of Carbamyl esters (Neostigmine, Pyridostigime, Physostigmine) on enzymes reversible?

A

Yes

Enzymes return to original shape

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35
Q

Examples of irreversible inhibition:

A

Pesticides

Chemical warfare

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36
Q

How do Anticholinesterase Drugs differ in Pharmacodynamics?

A
  • Differences in potency

- Affinity most important determinant of relative potency

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37
Q

Do different half lives with Anticholinesterase Drugs pharmacokineticly / Clinically significant?

A

No

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38
Q

Anticholinesterase drug with fastest speed of onset:

A

Edrophonium (60 secs)

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39
Q

Speed of onset for Anticholinesterase Drugs:

A

Endrophponium (1-2 mins)
Neostigmine (7-11 mins)
Pyridostigime (up to 16 mins)

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40
Q

Anticholinesterase Drugs Principle site of action: (pre or post synaptic)

A

Endrophponium: Presynaptic
Neostigmine: Postsynaptic
Pyridostigime: Postsynaptic

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41
Q

What does pre vs post synaptic have on drug effect?

A

Speed of onset

Pre is faster than Post

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42
Q

Duration of action for Anticholinesterase Drugs:

A

All the same (t1/2 = 60-120 mins)

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43
Q

Neostigmine dose: infants__child__adult

Edrophonium doses are the ____ for all ages.

A

Less, less

Same

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44
Q

Where is Anticholinesterase drugs sites of action?

A

Alpha subunits of nicotinic receptors

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45
Q

Muscarinic Effects:

A 
“Rest and Digest”
< HR
Salivation
Bronchoconstriction
Miosis (pinpoint pupils) 
Hyperperistalsis
> PONV
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46
Q

Where do Nicotinic effects act?

A

Act at the neuromuscular junction and autonomic ganglia.

47
Q

________ and __________, not ________ produce prolonged inhibition of plasma _____________.

A

Neostigmine and pyridostigmine, not edrophonium …

cholinesterase

48
Q

Cardiovascular effects of > Parasympathetic

A

< HR, Bradyarrhythmia
AV block
< BP
< SVR

49
Q

GI/GU Effects of > Parasympathetic:

A

> fluid secretion
motility
PONV

50
Q

Respiratory Effects of > parasympathetic:

A

Bronchoconstriction

> Airway resistance

51
Q

Eye Effects of > parasympathetic:

A

Miosis
Inability to focus on near vision
< IOP

52
Q

What other uses do anticholinergic drugs have?

A
  • Tx of CNS effects of certain drugs (opioids) (tertiary amines cross BBB)
  • Tx of Myasthenia Gravis (> ACh @ neuromuscular junction)
  • Tx of Glaucoma (miosis)
  • Tx post op shivering and analgesia
53
Q

When do you administer Anticholinesterase drugs?

A

During time of SPONTANEOUS recovery from NMB

54
Q

Potency depends on: (4)

A
  • NMB being antagonized
  • Speed of spontaneous recovery
  • Depth of NMB when the reversal is initiated
  • End point selected
55
Q

Anticholinesterase drugs can be mixed with ____________ drugs.

A

Anticholinergic

56
Q

Can the acetylcholinesterase enzyme do any further blockade after it is maximally inhibited?

A

No

57
Q

Administer reversal only after the ____ ____ has recovered to ______.

A

Twitch height, >10%

58
Q

Factors influencing reversal of neuromuscular blockade.

A
  • The ND NMB drug being reversed

- Intensity of NMBlockade at the time of reversal.

59
Q

Antagonism of NMBlockade may be inhibited or prevented:

A 
Antibiotics
Aminoglycosides
Hypothermia
Respiratory Acidosis (PaCO2 >50)
< K
Metabolic Acidosis
60
Q

What drug is a tertiary amine that crosses the BBB?

A

Physostigmine (antagonizes adverse CNS effects of certain drugs)
(Used to be used for Drug OD before narcan etc..

61
Q

At what dose can an acute overdose from an anticholinesterase drug occur?

A

Any dose (> change with > dose)

62
Q

Muscarinic effects of acute OD from anticholinesterase drugs:

A
  • Miosis and difficulty focusing
  • Salivation
  • Bronchoconstriction
  • < HR (Significant)
  • Abdominal cramps
  • Loss of bowel and bladder control
63
Q

Nicotinic Effect of acute overdose from anticholinesterase drugs:

A

Skeletal muscle weakness to paralysis and apnea.

64
Q

CNS effects of acute OD from anticholinesterase drugs

A
  • Confusion
  • Ataxia
  • Seizures
  • Coma
  • Depressed ventilation
65
Q

Acute OD from Organophsphate Anticholinesterase drugs:

A

Insecticides and Nerve Agents:
Absorb through skin, GI , alveoli:
> lipid solubility that will cross BBB

66
Q

What drug to give for anticholinesterase overdose?

A
  • Atropine (for antimuscarinic effects)

- Pralidoxime (short 1/2 life, needs to be given over and over)

67
Q

Reversal agents > the amount of __________.

A

ACh

68
Q

Anticholinergics _______ the effects of ACh at _______ receptors. This includes effects of the …

A

Antagonize (block), MUSCARINIC (m1-m5)

Heart
Salivary glands
Smooth muscle GI and GU tracts

69
Q

There is _____ effect at the Nicotinic receptor with Anticholinergics. This includes the …

A

No (little)

Neuromuscular junction
Autonomic ganglia

70
Q

2 naturally occurring tertiary amines: (NH3+)

A

Atropine
Scopolamine

(Anticholinergic)

71
Q

Can tertiary amines cross the BBB?

A

Yes

72
Q

1 Semisynthetic quaternary ammonium drug:

A

Glycopyrrolate (Anticholinergic)

73
Q

The common cationic portion fits into the __________ receptor. The _____ + is the consistent structural component seen across these drugs.

A

Muscarinic, Nitrogen

74
Q

Anticholinergics are __________ _________ at the ______ ______ receptors.

A

Competitive antagonists, cholinergic muscarinic

Reversal binding, noting else.

75
Q

What does an > in ACh do to Anticholinergic drugs?

A

Overcomes effects of the Anticholinergic drug.

76
Q

Small doses of Anticholinergic drugs may …

A

Stimulate receptors and < HR.

77
Q

5 Subtypes of Muscarinic Cholinergic Receptors Location: Clinical effects:

A 
M1: CNS, Stomach: H ion secretion
M2: Lungs, Heart: Bradycardia
M3: CNS, Airway smooth muscles, glandular tissue: Salivation, Bronchodilation
M4: CNS: ?
M5: CNS: ?
78
Q

The smallest doses will < ________.

A

Salivation (M3) “baby dose”

M3

79
Q

Anticholinergic order > to < Sedation effects

A

Scopolamine > Atropine > Glycopyrrolate (none)

80
Q

Anticholinergic order of > HR effects

A

Atropine > Glycopyrrolate > Scopolamine

81
Q

Anticholinergic weakest smooth muscle relaxant effect

A

Scopolamine

82
Q

Anticholinergic order > to < Anti secretion (Antisialagogue) effects:

A

Scopolamine > Glycopyrrolate > Atropine

83
Q

Anticholinergic order > to < Mydriasis/cyclopegia effects:

A

Scopolamine > Atropine > Glycopyrrolate (none)

84
Q

Anticholinergic order > to < Prevention of N/V effects:

A

Scopolamine > Atropine > Glycopyrrolate

85
Q

“AT _____ doses all 3 Anticholinergic drugs can produce __ ___ due to direct agonist effects.

A

Small, < HR

86
Q

Duration of Anticholinergics:

A

1 hr max

(1-2 hrs for reversal agents) may need to redose Anticholinergic.

87
Q

Do Anticholinergic drugs easily cross the BBB

A

No

Poorly lipid soluble quaternary amines

88
Q

Anticholinergics can be used preoperatively for …

A
  • Sedation
  • Antisialagogue
  • Prevent vagal reflexes (CN X parasympathetic system) so we give an Anticholinergic (an antiparasympathetic) to prevent vagal stimulation.
89
Q

Other uses for Anticholinergics:

A
  • Tx reflex-mediated bradycardia
  • Combined w/ anticholinesterase drugs
  • Bronchodilitation
  • Prevent motion induced N/V
90
Q

2 Preoperative Medications given for sedation:

Reversed with:

A

Scopolamine (amnesia)
Atropine

(Sedation can range from restlessness/agitation to somnolence) reverse with physostigmine.

91
Q

Although Scopolamine is ____ potent than Atropine, Atropine has ___ memory deficits.

A

> ,>.

92
Q

Will Glycopyrrolate cross the BBB? Why?

A

No, “more positive NH4”

93
Q

As we get older our BBB ______, making us more susceptible to meds crossing the BBB that normally will not.

A

Thins

94
Q

There is a delay awakening with Anticholinergic in _______ patients.

A

Elderly

95
Q

Use Scopolamine and Atropine for pre op sedation cautiously in patients with _______.

A

Glaucoma.

96
Q

_____ and _____ will cross the placenta

A

Atropine and scopolamine

97
Q

How does Atropine MOA > HR?

A

It blocks effects of ACh on the SA node. Effects seen most on young adults.

98
Q

Anticholinergics combined with anticholinesterase ________ NMB. This prevents the parasympathomimetic effects of ___________.

A

Reverse, anticholinesterases

You kidding ME!

99
Q

Bronchodilation occurs from the ____ effects of Anticholinergics.

A

M3

100
Q

Due to antagonism of ACh there are _________ effects on the airway.

A

Broncholilitation

101
Q

Scopolamine patch takes how long to take effect?

A

4 hours

102
Q

Central Anticholinergic Syndrome is mostly seen in ______ patients

A

Elderly

Symptoms: restlessness hallucinations to somnolence and unconsciousness.

103
Q

Can Scopolamine and Atropine enter the CNS?

A

Yes

104
Q

Tx for Central Anticholinergic Syndrome:

A

Physostigmine

105
Q

Anticholinergic side effects:

A

Can’t see, can’t pee, can’t spit, can’t shit. (Dries you out)

  • Tachycardia
  • > temp (not sweating, dry)
  • Skeletal muscle weakness
  • Ortho hypotension
  • Can lead to fatal events (seizure, coma)
106
Q

Tx of Anticholinergic side effects:

A

Physostigmine (may need to repeat does < half life).

107
Q

Suggamedex: approved for reversal of aminosteroids. Specifically __________ and _________ only.

A

Vecuronium and Rocuronium (More so)

108
Q

What physiological effect on the body does Suggamedex have?

A

None.

109
Q

Suggamedex has a _________ center and a _________ exterior.

A

Hydrophobic, hydrophillic

110
Q

Do we adjust Suggamedex dose for the elderly?

A

No

111
Q

Suggamedex side effects:

A
  • Anaphylaxix (0.3%)
  • Bradycardia
  • Bleeding, coagulopathies
  • (most common) N/V, pain, hypotension, H/A
  • Not recommended for use in severe renal impairment.
112
Q

Is Suggamedex protein bound?

A

No

113
Q

Half life of Suggamedex?

Renal impairment (mid mod sev)

A

2 hours
(>90% eliminated renal in first 24 hours)

Mild: 4 hrs
Mod: 6 hrs
Severe: 19hrs

114
Q

Special considerations of Suggamedex?

A

Birth control pills

(Must consult with pt). Pt must use secondary contraceptive for 1 week after Suggamedex administration due to < effect.

Pharmacology I (6 decks)

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