PPT Cholinergic drugs/ anticholinergic drugs Flashcards

1
Q

What kind of IV tubing will you put a Neo drip on?

A

micro drip which is 60 drops per milliliter.

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2
Q

How to mix a Neo drip from a vial?

A

1ml of Neo =10mg, place that 1ml into a 100ml NS bag.

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3
Q

Cholinergic drugs are also called what? Why?

A

parasympathomimetic drugs, copy the PSN system.

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4
Q

what are the two major classes of cholinergic drugs?

A

cholinergic agonists and anticholinesterase drugs.

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5
Q

what do cholinergic agonist drugs do?

A

bind to cholinergic receptors and mimic the action of acetylcholine.

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6
Q

anticholinesterase drugs, what do they do?

A

Inhibit acetylcholinesterase (the enzyme that destroys acetylcholine). This increases acetylcholine levels at the receptor sites and prolonging its effects.

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7
Q

what breaks down acetylcholine?

A

acetylcholinesterase

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8
Q

Examples of Cholinergic agonists?

A

Bethanechol
Carbachol
Cevimeline
Pilocarpine (eye drops)

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9
Q

Cholinergic agonists are metabolized by who and where?

A

metabolized at the muscarinic and nicotinic receptor sites in the plasma and liver.

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10
Q

ACTION of cholinergic agonists?

A
mimic acetylcholine thus acts like parasympathetic so...
salivation
slow heart rate
dilation of blood vessels, 
constriction of bronchioles,
increased gut activity
contraction of urinary bladder 
constriction of pupils
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11
Q

what conditions would cholinergic agonists be used?

A

Urinary retention due to weak or atonic bladder

Lack of bowl movements especially post op period

Glaucoma to reduce intraocular pressure

Salivary gland hypofunction

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12
Q

applies breaks on heart but accelerates gut and bladder smooth muscles, what NT does that describe?

A

Acetylcholine, thus it also describes cholinergic agonists.

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13
Q

adverse reactions to cholinergic agonists?

A

Adverse reactions (wet as ocean)

Decrease heart rate* and lower BP

Nausea/vomiting

Increased activity of gut leading to cramping and diarrhea

Excessive sweating/salivation

Increase urination

Blurred vision due to pupillary constriction

Shortness of breath due to bronchoconstriction

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14
Q

prevents breakdown of acetylcholine, what drug is this?

A

anticholinesterase drugs

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15
Q

Anticholinesterase drugs can be divided into two groups?

A

Reversible- short duration of action example - physostigmine

irreversible- long-lasting effects, example - nerve gas and insecticides.

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16
Q

what do you give physostigmine with and neostigmine with?

A

physo with atropine

Neostigmine with glycopyrlate.

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17
Q

what drug will improve muscle strength in MG?

A

anticholinesterase drugs

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18
Q

diff. between anticholinergic and anticholinesterase?

A

anticholinergic blocks acetylcholine in the central and peripheral nervous system (Not at NMJ)

anticholinesterase blocks the breakdown of acetylcholine thus MORE Ach!

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19
Q

Antidote for cholinergic blocking agents?

A

anticholinesterase drugs

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20
Q

what drugs do we use to treat alzheimers’disease ?

deficiency of acetylcholine in the brain

A

Anticholinesterase drugs

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21
Q

Cholinergic blocking agents also called?

A

Anticholinergic Drugs

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22
Q

Examples of anticholinergic drugs?

A

Atropine, belladonna, scopolamine.

23
Q

what kind of antagonist is atropine?

A

atropine competes with acetylcholine for receptor sites - COMPETITIVE agonists.

24
Q

All cholinergic blocking agents relax smooth muscles of GI and urinary bladder. Therefore these are used in?

A

Hyperactive bladder (e.g. Detrol ®)

Hyperactive gut (colic/ irritable bowel syndrome)

Biliary colic

Before endoscopy or sigmoidoscopy to relax GI smooth muscles

Atropine is given before surgery to dry up secretions

To speed up heart rate during bradycardia *

To dilate pupil for eye exam.

25
Q

acronym used for cholinergic blocking agents (as an antidote for pesticide poising)?

A

DUMBELSS

26
Q

another way to say cholinergic blocking agents?

A

ANTIcholinergics

27
Q

If you block Ach too much with cholinergic blocker (anticholinergic) then what will you give to reverse? (too much scopolamine, glyco, atropine)

A

physostigmine

28
Q

anticholinergics make you wet or dry you up?

A

anticholinergics (cholinergic blockers) dry you out!

29
Q

what drugs do cholinergic blockers interact with (badly)

A

Tricyclic and tetracyclic antidepressants

30
Q

Atropine overdose will look like?

A
blurred vision, mydriasis, urinary retention, confusion, constipation. 
or
hot as a hare
dry as a bone
blind as a bat
red as a beet
mad as a hatter
31
Q

How does atropine speed up the heart rate?

A

Atropine a cholinergic blocking drug, competes with Ach for cholinergic receptor sites on the SA and VA notes. By blocking Ach, atropine sppeds up the heart rate.

(parasympathetic effect on the heart is opposite of sympathetic thus slows it down, so when you block that parasympathetic response by blocking Ach, then you speed up the heart)

32
Q

parasympathetic system acts on the resp. system how?

A

bronchial constriction, thus if you give a cholinergic antagonist, anticholinergic = bronchodilation.

33
Q

Where are Muscarinic receptors located?

A

Heart
salivary glands
GI smooth muscle
GU tract

34
Q

Naturally occurring tertiary amine belladonna alkaloids are what two anticholinergic drugs?

A

atropine and scopolamine

35
Q

Semisynthetic anticholinergic drug?

A

Glycopyrrolate

36
Q

what is diff. about glycopyrrolate in relation to CNS effects?

A

It has no CNS effects

37
Q

Which two anticholinergics resemble cocoaine structurally?

A

atropine and scopolomine

38
Q

what form causes the anticholinergic effects of atropine and scopolomine?

A

levorotatory form

39
Q

DO NOT prevent release of Ach or react with it?

So what do they do?

A

Anticholinergic drugs

They are competitive antagonists, the effects of anticholinergic drugs can be overcome by increase concentration of Ach in the area of the muscarinic receptors.

40
Q

There are how many Muscarinic cholinergic receptor subtypes?

A

M1 M2 M3 M4 M5

41
Q

All M receptors are what type ?

A

All are G-protein coupled receptors depending on second messenger coupling.

42
Q

what do each M receptor go with (body system wise)

A

M1…CNS & stomach

M2…Lungs, heart & eyes

M3…CNS, airway smooth muscle & glandular tissue

M4 & M5…CNS

43
Q

Which M receptor does not have to do with the CNS?

A

M2

44
Q

What does scopolamine do better than atropine?

A

Scopolamine has greater antisialagogue (decreased production of saliva) & ocular effects than atropine.

45
Q

Atropine does what better than scopolamine?

A

Atropine has greater anticholinergic effects on the heart, bronchial smooth muscle & GI tract than scopolamine.

46
Q

What does Glycoprrolate increase that the other two do not?

A

Glycopyrrolate increases metabolic O2 consumption, atropine has no effect, & scopolamine has a decreased effect.

47
Q

If glyco and neostigmine are given which one is given first?

A

glyco first bc it takes longer to work. (if you give them together it does not matter)

48
Q

which anticholinergics can pass through the BBB and which ones can not?

A

Atropine and scopolamine CAN penetrate the BBB.

Glycopyrrolate CANNOT cross BBB.

49
Q

onset and duration of atropine?

A

onset is 1 min

duration is 30-60 sec

50
Q

what is the onset and duration of glycopyrrolate?

A

onset 2-3 min (IM injection - 16 min)

51
Q

How much breakdown does scopolamine go through?

A

broken down almost entirely, about 1% excreted unchanged in the urine.

52
Q

glyco elimination is more rapid than atropine, and is significantly prolonged in what?

A

uremia

53
Q

anticholinergics are not very selective, so what does that mean?

A

difficult to obtain desired therapeutic responses without associated side effects.

54
Q

what two types of drugs do you combine in order to treat NMB?

A

anticholinesterase drugs and anticholinergics.