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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
(1) Tertiary Amine drug:
Physostigmine (small enough to cross BBB). | NH3
26
How many types of Anticholinesterase Drugs?
2 | Tertiary Amines and Quaternary ammonium.
27
(3) Quaternary Ammonium drugs:
Edrophonium Neostigmine Pyridostigmine
28
Anticholinersterase Drugs have 3 main actions:
Enzyme inhibition Presynaptic effects Direct effect
29
Anticholinesterase enzyme inhibits _______________.
Acetylcholinesterase | Results in > availability of ACh (> side effects)
30
How are enzymes blocked with Edrophonium?
Forms a reversible electrostatic attachment (fast action) | Ionic bond/magnetic force (This changes the enzyme shape and ACh can’t bind)
31
What two anticholinesterase drugs are hydrolyzed by enzymes?
Neostigmine Pyridostigmine This carbamylates the enzyme blocking the enzyme’s ability to hydrolyze ACh (Slower)
32
Acetylcholinesterase inhibitors may produce __________ in the absence of neuromuscular blockers.
Fasiculations
33
Anticholinesterase drugs can produce some form of a ___________ _________ at doses greater than usual clinical doses.
Neuromuscular blockade | Like Succ) (receptors are stunned by overstimulation
34
Is electrostatic attachment (Edrophonium) to enzymes and the formation of Carbamyl esters (Neostigmine, Pyridostigime, Physostigmine) on enzymes reversible?
Yes | Enzymes return to original shape
35
Examples of irreversible inhibition:
Pesticides | Chemical warfare
36
How do Anticholinesterase Drugs differ in Pharmacodynamics?
- Differences in potency | - Affinity most important determinant of relative potency
37
Do different half lives with Anticholinesterase Drugs pharmacokineticly / Clinically significant?
No
38
Anticholinesterase drug with fastest speed of onset:
Edrophonium (60 secs)
39
Speed of onset for Anticholinesterase Drugs:
Endrophponium (1-2 mins) Neostigmine (7-11 mins) Pyridostigime (up to 16 mins)
40
Anticholinesterase Drugs Principle site of action: (pre or post synaptic)
Endrophponium: Presynaptic Neostigmine: Postsynaptic Pyridostigime: Postsynaptic
41
What does pre vs post synaptic have on drug effect?
Speed of onset | Pre is faster than Post
42
Duration of action for Anticholinesterase Drugs:
All the same (t1/2 = 60-120 mins)
43
Neostigmine dose: infants__child__adult Edrophonium doses are the ____ for all ages.
Less, less Same
44
Where is Anticholinesterase drugs sites of action?
Alpha subunits of nicotinic receptors
45
Muscarinic Effects:
``` “Rest and Digest” < HR Salivation Bronchoconstriction Miosis (pinpoint pupils) Hyperperistalsis > PONV ```
46
Where do Nicotinic effects act?
Act at the neuromuscular junction and autonomic ganglia.
47
________ and __________, not ________ produce prolonged inhibition of plasma _____________.
Neostigmine and pyridostigmine, not edrophonium ... cholinesterase
48
Cardiovascular effects of > Parasympathetic
< HR, Bradyarrhythmia AV block < BP < SVR
49
GI/GU Effects of > Parasympathetic:
> fluid secretion > motility > PONV
50
Respiratory Effects of > parasympathetic:
Bronchoconstriction | > Airway resistance
51
Eye Effects of > parasympathetic:
Miosis Inability to focus on near vision < IOP
52
What other uses do anticholinergic drugs have?
- 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
When do you administer Anticholinesterase drugs?
During time of SPONTANEOUS recovery from NMB
54
Potency depends on: (4)
- NMB being antagonized - Speed of spontaneous recovery - Depth of NMB when the reversal is initiated - End point selected
55
Anticholinesterase drugs can be mixed with ____________ drugs.
Anticholinergic
56
Can the acetylcholinesterase enzyme do any further blockade after it is maximally inhibited?
No
57
Administer reversal only after the ____ ____ has recovered to ______.
Twitch height, >10%
58
Factors influencing reversal of neuromuscular blockade.
- The ND NMB drug being reversed | - Intensity of NMBlockade at the time of reversal.
59
Antagonism of NMBlockade may be inhibited or prevented:
``` Antibiotics Aminoglycosides Hypothermia Respiratory Acidosis (PaCO2 >50) < K Metabolic Acidosis ```
60
What drug is a tertiary amine that crosses the BBB?
Physostigmine (antagonizes adverse CNS effects of certain drugs) (Used to be used for Drug OD before narcan etc..
61
At what dose can an acute overdose from an anticholinesterase drug occur?
Any dose (> change with > dose)
62
Muscarinic effects of acute OD from anticholinesterase drugs:
- Miosis and difficulty focusing - Salivation - Bronchoconstriction - < HR (Significant) - Abdominal cramps - Loss of bowel and bladder control
63
Nicotinic Effect of acute overdose from anticholinesterase drugs:
Skeletal muscle weakness to paralysis and apnea.
64
CNS effects of acute OD from anticholinesterase drugs
- Confusion - Ataxia - Seizures - Coma - Depressed ventilation
65
Acute OD from Organophsphate Anticholinesterase drugs:
Insecticides and Nerve Agents: Absorb through skin, GI , alveoli: > lipid solubility that will cross BBB
66
What drug to give for anticholinesterase overdose?
- Atropine (for antimuscarinic effects) | - Pralidoxime (short 1/2 life, needs to be given over and over)
67
Reversal agents > the amount of __________.
ACh
68
Anticholinergics _______ the effects of ACh at _______ receptors. This includes effects of the ...
Antagonize (block), MUSCARINIC (m1-m5) Heart Salivary glands Smooth muscle GI and GU tracts
69
There is _____ effect at the Nicotinic receptor with Anticholinergics. This includes the ...
No (little) Neuromuscular junction Autonomic ganglia
70
2 naturally occurring tertiary amines: (NH3+)
Atropine Scopolamine (Anticholinergic)
71
Can tertiary amines cross the BBB?
Yes
72
1 Semisynthetic quaternary ammonium drug:
Glycopyrrolate (Anticholinergic)
73
The common cationic portion fits into the __________ receptor. The _____ + is the consistent structural component seen across these drugs.
Muscarinic, Nitrogen
74
Anticholinergics are __________ _________ at the ______ ______ receptors.
Competitive antagonists, cholinergic muscarinic Reversal binding, noting else.
75
What does an > in ACh do to Anticholinergic drugs?
Overcomes effects of the Anticholinergic drug.
76
Small doses of Anticholinergic drugs may ...
Stimulate receptors and < HR.
77
5 Subtypes of Muscarinic Cholinergic Receptors Location: Clinical effects:
``` M1: CNS, Stomach: H ion secretion M2: Lungs, Heart: Bradycardia M3: CNS, Airway smooth muscles, glandular tissue: Salivation, Bronchodilation M4: CNS: ? M5: CNS: ? ```
78
The smallest doses will < ________.
Salivation (M3) “baby dose” M3
79
Anticholinergic order > to < Sedation effects
Scopolamine > Atropine > Glycopyrrolate (none)
80
Anticholinergic order of > HR effects
Atropine > Glycopyrrolate > Scopolamine
81
Anticholinergic weakest smooth muscle relaxant effect
Scopolamine
82
Anticholinergic order > to < Anti secretion (Antisialagogue) effects:
Scopolamine > Glycopyrrolate > Atropine
83
Anticholinergic order > to < Mydriasis/cyclopegia effects:
Scopolamine > Atropine > Glycopyrrolate (none)
84
Anticholinergic order > to < Prevention of N/V effects:
Scopolamine > Atropine > Glycopyrrolate
85
“AT _____ doses all 3 Anticholinergic drugs can produce __ ___ due to direct agonist effects.
Small, < HR
86
Duration of Anticholinergics:
1 hr max (1-2 hrs for reversal agents) may need to redose Anticholinergic.
87
Do Anticholinergic drugs easily cross the BBB
No | Poorly lipid soluble quaternary amines
88
Anticholinergics can be used preoperatively for ...
- Sedation - Antisialagogue - Prevent vagal reflexes (CN X parasympathetic system) so we give an Anticholinergic (an antiparasympathetic) to prevent vagal stimulation.
89
Other uses for Anticholinergics:
- Tx reflex-mediated bradycardia - Combined w/ anticholinesterase drugs - Bronchodilitation - Prevent motion induced N/V
90
2 Preoperative Medications given for sedation: Reversed with:
Scopolamine (amnesia) Atropine (Sedation can range from restlessness/agitation to somnolence) reverse with physostigmine.
91
Although Scopolamine is ____ potent than Atropine, Atropine has ___ memory deficits.
>,>.
92
Will Glycopyrrolate cross the BBB? Why?
No, “more positive NH4”
93
As we get older our BBB ______, making us more susceptible to meds crossing the BBB that normally will not.
Thins
94
There is a delay awakening with Anticholinergic in _______ patients.
Elderly
95
Use Scopolamine and Atropine for pre op sedation cautiously in patients with _______.
Glaucoma.
96
_____ and _____ will cross the placenta
Atropine and scopolamine
97
How does Atropine MOA > HR?
It blocks effects of ACh on the SA node. Effects seen most on young adults.
98
Anticholinergics combined with anticholinesterase ________ NMB. This prevents the parasympathomimetic effects of ___________.
Reverse, anticholinesterases | You kidding ME!
99
Bronchodilation occurs from the ____ effects of Anticholinergics.
M3
100
Due to antagonism of ACh there are _________ effects on the airway.
Broncholilitation
101
Scopolamine patch takes how long to take effect?
4 hours
102
Central Anticholinergic Syndrome is mostly seen in ______ patients
Elderly Symptoms: restlessness hallucinations to somnolence and unconsciousness.
103
Can Scopolamine and Atropine enter the CNS?
Yes
104
Tx for Central Anticholinergic Syndrome:
Physostigmine
105
Anticholinergic side effects:
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
Tx of Anticholinergic side effects:
Physostigmine (may need to repeat does < half life).
107
Suggamedex: approved for reversal of aminosteroids. Specifically __________ and _________ only.
Vecuronium and Rocuronium (More so)
108
What physiological effect on the body does Suggamedex have?
None.
109
Suggamedex has a _________ center and a _________ exterior.
Hydrophobic, hydrophillic
110
Do we adjust Suggamedex dose for the elderly?
No
111
Suggamedex side effects:
- Anaphylaxix (0.3%) - Bradycardia - Bleeding, coagulopathies - (most common) N/V, pain, hypotension, H/A - Not recommended for use in severe renal impairment.
112
Is Suggamedex protein bound?
No
113
Half life of Suggamedex? Renal impairment (mid mod sev)
2 hours (>90% eliminated renal in first 24 hours) Mild: 4 hrs Mod: 6 hrs Severe: 19hrs
114
Special considerations of Suggamedex?
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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