Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharm > Anticholinesterase & Anticholinergic Drugs > Flashcards

Anticholinesterase & Anticholinergic Drugs Flashcards

1
Q

What do anticholinesterases do?

A

Inhibit the enzyme that breaks down Ach, which then increases the amount of Ach available in the synapse, increases concentration at both nicotinic and muscarinic receptors, stimulates presynaptic receptors to release more Ach

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What are the implications of inhibiting both acetylcholinesterase and pseudocholinesterase?

A

acetylcholinesterase: increases ach at nicotinic and muscarinic receptors.
pseudocholinesterase: can’t break down succ so it causes a prolonged effect. Also can’t break down ester local anesthetics or remifentanil

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What type of receptors are Nicotinic receptors?

A

Ligand gated ion channels

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What type of receptors are muscarinic receptors?

A

G protein coupled receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

With reversal, which receptors are we trying to maximize and which are we trying to minimize the side effects of?

A

maximize: nicotinic
minimize: muscarinic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Stimulation of muscarinic receptors results in:

A 
parasympathetic effects:
Diarrhea
Urination
Miosis 
Bradycardia
Bronchoconstriction
Emesis
Laxation (peristalsis)
Lacrimation
Salivation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are 3 examples of muscarinic receptor antagonists?

A

atropine, scopolamine, pilocarpine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What are 3 ways anticholinergics inhibit acetylcholinesterase?

A

Electrostatic attachement
Formation of carbamyl esters
Phosphorylation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

The duration of action for anticholinesterase drugs is determined by the _____ of the bond that is formed during hydrolysis.

A

Strength

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What is the only anticholinesterase that crosses the blood brain barrier?

A

Physostigmine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Anticholinesterases are ______ amines except or physostigmine which is a _____ amine.

A

Quaternary, tertiary

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Anticholinesterases are primary excreted by _____

A

kidneys

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

All anticholinesterases have a “ceiling effect”. What does that mean?

A

There is no therapeutic effect after the max dose

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q 
Neostigmine:
Dose:
Onset:
Duration:
Administered with:
Uses:
A

Dose: 0.05 mg/kg (max dose 5mg)
Onset: <3 min
Duration: 40-60min
Administered with: glycopyrrolate 0.2mg per 1mg of neo
Uses: antagonize (reverse) non depolarizing neuromuscular blocking drugs, treatment of myasthenia gravis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q 
Physostigmine:
Dose:
Onset:
Duration:
Administered with:
Uses:
A

Dose: 0.01-0.03 mg/kg
Onset: 3-8 min
Duration: 30min-5hr
Uses: reverse scopalamine, tx of anticholinergic syndrome (atropine poisoning), reverse prolonged somnolence, treat post op shivering, antagonize opioid induced respiratory depression.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Which anticholinesterase is metabolized by plasma esterases, unlike the others which are primarily renal and hepatic?

A

Physostigmine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What type of bond is formed between organophosphates and Ach?

A

Irreversible bond

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What is ecothiophate used to treat?

A

Glaucoma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What are muscarinic signs of anticholinesterase poisoning?

A

(SLUDGE) salivation, lacrimation, urination, diaphoresis, GI upset, emesis. Can progress to bronchospasm, blurred vision, bradycardia or tachycardia, hypotension, confusion and shock

20
Q

What are nicotinic signs of anticholinesterase poisoning?

A

Skeletal muscle fasciculations followed by weakness then paralysis. Severe reactions can result in ventilatory failure and death (cholinergic crisis)

21
Q

What is the treatment for anticholinesterase poisoning?

A

Atropine and Pralidoxime (an acetylcholinesterase reactivator)

22
Q

What is central cholinergic sydrome?

A

aka cholinergic crisis. Overdose of cholinesterase inhibitors causing excessive Ach in brain

23
Q

What are the other names for anticholinergics?

A

Antimuscarinics, parasympatholytics

24
Q

What is the mechanism of action for anticholinergics?

A

reversibly bind with muscarinic cholinergic receptors; preventing ach binding to these sites, then causes PNS effects

25
Q

Which anticholinergic does not cross the blood brain barrier?

A

Glycopyrrolate

26
Q

Which anticholinergic has the most effect on causing tachycardia?

A

Atropine

27
Q

Which anticholinergic has the most effect on causing sedation?

A

Scopolamine

28
Q

What effects on the respiratory system do anticholinergics have?

A

Bronchodilation and decreased secretions

29
Q

What effects on the eyes do anticholinergics have?

A

pupil dilation, cycloplegia (paralysis of ciliary muscle causes loss of accommodation or blurred vision)

30
Q

What effects on the cardiac system do anticholinergics have?

A

Increases rate of SA and AV node

31
Q

What effects on the GI/urinary system do anticholinergics have?

A

Decreased GI motility and urinary retention

32
Q

What are clinical uses of anticholinergics?

A

use with anticholinesterases, parkinsons, motion sickness, bradycardia, cholinergic poinsoning

33
Q

What are the side effects of atropine poisoning (Central Anticholinergic Syndrome)?

A

“Dry as bone, blind as a bat, red as a beet, mad as a hatter”

dry mouth, mydriasis, tachycardia, hot/flushed skin, agitation, delerium

34
Q

What is the treatment for atropine poisoning (Central Anticholinergic Syndrome)?

A

Physostigmine 15-60mcg/kg

35
Q

What are contraindications to using anticholinergic drugs?

A

Glaucoma, gastric ulcer

36
Q

Atropine
Dose:
Onset:
Duration:

A

Dose: 0.4-0.8mg every 3-5min
Onset: 45-60sec
Duration: 1 hr

37
Q

Never less than ____mg of Atropine for bradycardia to adults, and never less than ____mg of Atropine to peds

A

0.4, 0.1mg

38
Q

Glycopyrrolate
Dose:
Onset:
Duration:

A

Dose: 0.01mg/kg (0.2 mg for each 1mg of neostigmine)
Onset: <1min
Duration: 2hr

39
Q

Scopolamine
Dose:
Onset:
Duration:

A

Dose: 0.2-0.6mg sedation/amnesia
Onset: <1 min
Duration: 2-6hr

Also for PONV prevention
Dose: 0.1mg transdermal patch
Onset: 2-4hr
Duration: 24hr

40
Q

Which Anticholinergic pairs with the following Anticholinesterase drug?

Neostigmine
Pyridostigmine
Edrophonium
Physostigmine

A

Neostigmine–Glycopyrrolate
Pyridostigmine–Glycopyrrolate
Edrophonium–Atropine
Physostigmine–not necessary (crosses BBB)

41
Q

What is sugammadex’s mechanism of action?

A

encapsulates the neuromuscular blocker (steroidals NOT benzyls or succs) and makes it ineffective and unable to bind with nicotinic receptors

42
Q

What are the nondepolarizing neuromuscular blockers that sugammadex can reverse?

A

Rocuronium, vecuronium, pancuronium

43
Q

How much of sugammadex is metabolized?

A

None

44
Q

Which organ excretes sugammadex?

A

kidneys

45
Q

How long is the onset of Sugammadex?

A

3-5 min

46
Q

What are side effects of Sugammadex?

A

Bradycardia, anaphylaxis, bleeding, makes hormonal contraceptives ineffective for 7 days, not recommended with severe renal impairment

47
Q

Sugammadex:
dose with 2 twitches
dose with 0 twitches

A

2mg/kg

4mg/kg

Pharm (12 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions