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Pharmacology-1 > Cholinergic Pharmacology > Flashcards

Cholinergic Pharmacology Flashcards

1
Q

Muscarinic R: GPCRS 3 Subtypes and targets?

A

M1 Gq CNS

M2 Gi Heart, Smooth Muscle, some nerves

M3 Gq exocrine glands, Sm. musc, endothelium

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2
Q

Nicotinic R. what types are there?

A

pentameric ligand-gated ion channels NA & K

  1. Nm= muscle type: found at neuromuscular jxn
  2. Nn= neuronal-type: found in nerves, autonomic ganglia
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3
Q

parasympathomimetic

A

mimic activation of PNS

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4
Q

cholinomimetic

A

mimic action of activating cholinoceptors

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5
Q

cholinergic

A

activates ach R.

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6
Q

Cholinomimetic (cholinergic) drugs chart

A
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7
Q

Direct Cholinomimetic action

A

binds to/activates ach R/

receptor agonism

eg. ach, muscarine, nicotine

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8
Q

Indirect cholinomimetic effect

A

inhibit acetylcholinesterase (AChE)

amplify action of endogenous ACh

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9
Q

What is the results of cholinoreceptor activation in the eye?

A

(alpha) sphincter muscle of iris: contrict pupils (miosis)

(M) ciliary muscle: accomodation

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10
Q

What is the results of cholinoreceptor activation in the heart?

A

SA node: decrese in rate

atria: decrease contract

AV node: decrease in conduction velocity

Ventricles: small decrease in contractile strength

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11
Q

What is the results of cholinoreceptor activation in the blood vessels?

A

arteries, veins: dilation (via EDRG). construciton (high-dose direct effect)

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12
Q

What is the results of cholinoreceptor activation in the lung?

A

bronchial muscle: contraction (bronchoconstriction)

bronchial glands: stimulation

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13
Q

What is the results of cholinoreceptor activation in the GI tract?

A

motility: increase
sphincters: relaxation
secretion: stimulation

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14
Q

What is the results of cholinoreceptor activation in the urinary bladder?

A

detrusor: contraction

trigone & sphincter: relaxation

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15
Q

What is the results of cholinoreceptor activation in the glands?

A

sweat, salivary, lacrimal, nasopharyngeal: secretion

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16
Q

List 3 choline esters

A
  1. Methacholine
  2. Carbachol
  3. Bethanecol

resistant to cholinesterases

not well absorbed because of charge

can be applied topically

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17
Q

Methacholine

A

Provocative asthma test

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18
Q

Bethanechol

A

Promote GI and GU motility

-for post operative ileus/ urinary retention

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19
Q

Carbachol

A

Increase aqueous humor outflow in glaucoma

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20
Q

Pilocarpine

A

Alkaloid

Muscarinic action

used for Glucoma

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21
Q

Indirect acting cholinenometric drugs mechanism.

A

Inhibit AChE

  • prolong ach signaling
  • occurs at muscarinic and nicotinic receptors
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22
Q

What two drugs are used to treat myasthenia gravis?

A

Neostigmine

Edrophonium

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23
Q

Physostigmine is used to treat?

A

Anticholinergic toxicity

  • uncharged: cross BBB into CNS
  • can reverse altered mental status from anticholinergic toxcitiy
  • cannot use for MG because will cause seizures, short acting need to dose frequently.
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24
Q

What is carbaryl used for.

A

Its an insecticide poison

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25
Q

What is the mechanism for myesthinia gravis ?

A

Disease of an impaired transmission of NMJ

Autoantobodies against Nm AchR

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26
Q

What are some characteristics of Myasthenia Gravis?

A

muscle weakness

-diaphragm/ airway control muscle weakness

Eyelid ptosis

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27
Q

Edrophonium

A

SHORT Acting AChE inhibitor

  1. charged/quarternary ammonium

~poorly absorbed, so given IV

  1. Temporarily improved NMJ signaling

~tensilon test: to help diagnose

28
Q

What helps diagnose Myasthenia Gravis?

A

Tensilon test

29
Q

What are two reasons MG patients can be weak?

A

Myasthenic Crisis vs Cholinergic Crisis

30
Q

What is the myasthenic crisis?

A
  1. disease is out of control, dose is not high enough.

tx/ w AChE inhibiors can save them

31
Q

What is cholinergic Crisis?

A
  1. toxicity from AChE inhibitor

Tx w/ AChE inhibitors can kill them

32
Q

What clinical test/ Drug intervention can you use to differentiated between myasthenic crisis vs cholinergic crisis?

A

Use Edrophonium

  1. if fixes them, then it was MG
  2. if its worse tx w/ anticholinergics
33
Q

Neostigmine & Pyridostigmine: Indications?

A
  • Myasthenia Gravis long-term therapy
  • Post-operative ileus/Urinary retention
  • Pyridostigmine: longer duration of action
34
Q

What is special about the structure of Neostigmine & Pyridostigmine

A

-Charged: do not cross BBB (MG is a peripheral (non-CNS) disease

35
Q

4 examples of AChE inhibitor insecticides.

A

very potent

  1. parathion
  2. paraoxon
  3. malathion
  4. malaxon
36
Q
  1. carbamates
A

reversible AChE inhibition

“stigmine” drugs are also carbamates

37
Q

Organophosphates (OPs)=

A

irriversible

-only rare/obsolete OP Rx drufs- _Echothiophate _

38
Q

Soman

A

AChE inhibitor

“nerve agent”

39
Q

What is the mechanism of organophosphate irreversibility? What is aging

A

OP drugs/ poisons fit in AChE active site

Aging: OP will enventually covalently bind to active site and irreversibily inhibit AChE.

  • antidotal tx before aging occurs can regenerate enzyme
  • aging DOES NOT occur in carbamates
40
Q

Anticholinergic Drugs

A

Cholinoceptor blockers & cholinesterase regenerators

-“Anticholinergic”= “Anti-muscarinic for MDs

41
Q

Nicotinic ACh receptors

A

if drug not muscarinis specific, increase signal at:

  1. autonomic ganglia (increase PNS & SNS output to effector organs)
  2. NMJ (muscle twitching, fasciculations, paralysis
42
Q

List of anticholinergic drugs

A
43
Q

What is the mechanism of action for Antimuscarinic Drugs?

A
  1. MOA
    - Reversible bloackade of Muscarinic ACh R (Most non specific for R, R are constitutively active thus drugs are Inverse Agonist)
  2. tertiary amines (eg. atropine) better absorbed
  3. qyaternary ammonium ions, used for local effect, poorly absorbed (eg. tiotripium inhaled in lungs for asthma/COPD)
44
Q

What are the Antimuscarinic Clinical Effects?

A

Opposite of choinergic drugs

  • big pupils
  • increase HR
  • dry you up
45
Q

Antimuscarinic Clinical Effects: Eye?

A

dilated pupil= Mydriasis

loss of accomodation for near vision

46
Q

Antimuscarinic Clinical Effects: Upper Aerodigestive Tract?

A

Dry mouth, Dry nose/sinuses

47
Q

Antimuscarinic Drug Indications: Ocular?

A

Myadriatic & Cycloplegic

  • dilate pupill for ophthalmologic exam or therapy
  • paralyze ciliary body of eye for ophtho disease
48
Q

What are the indications for tropicaminde, and cyclopentolate?

A

Dilate pupil for ophthal. exam or therapy

49
Q

Antimuscarinic drug indications for Atropin & Glycopyrrolate?

A

Decrease oral/Nasal/ Airway secretions

50
Q

Antimuscarinic Drug Indications: Heart?

A

Treats Bradycardia

-blocks vafal tone (ACh acting on M cholinoceptors) at cardiac pacemaker

51
Q

Antimuscarinic Drug Indication: Lungs?

A

Asthma/COPR to

  • decrese secretions
  • decrease SM tone (Bronchospasm)
52
Q

What are the indications of Ipratropium & Triotropium?

A

Decrease bronchial secrestion and SM tone

53
Q

What are the antimuscarinic Drug Indications for Slow GI motility? Example drug?

A

Slow GI motility

  • adjunct txt for diarrhea/ GI cramping
    ex. Dicyclomine
54
Q

What are the antimuscarinic Drug Indications for Urinary tract? Example drug?

A

Incotinence/Excess urinary frequency

ex. Oxybytynin, Tolterodine

55
Q

What are the antimuscarinic Drug Indications for CNS? Example drug?

A

antinausea/ vertigo/ motion sickness

ex. scopolamine, dimenhydrinate

56
Q

What are the anticholinergic Side Effects?

A
  1. Hot as a hare
  2. Dry as a bone
  3. Blind as a bat
  4. Red as a beet
  5. Mad as a hatter
57
Q

Impiramine

A

anticholinergic

  • TCA
  • Rxn for Enuresis (Bed wetting)
  • Decrease Urinary frequency
58
Q

Antidotal theraphy for too much cholinergic tone

A

treat with anti-cholinergic drug

ex. Pyridostigmine induced cholinergic crisis can be reversed wtih Atropine

59
Q

Antidotal Therapy for too much anti-muscarinic activity

A

treat with cholinergic agonist

ex. altered mental status from antimuscarinic side effects of diphenhydramine (Benadryl) reversed w/ Physostigmine

60
Q

Can Atropine reverse Nicotinic Effects?

A

No, only Muscarinic

61
Q

OP toxicity/ cholinergic crisis also involves?

A
  1. Hyperstimulation at nAChR in ganglia
  2. Hyperstimuation at nAChR at NMJ (Skeletal weakness cannot be reverse by atropine)

* need an anti-Nicotinic drug

62
Q

How can we regenerate AChE?

A

Oximes!

-kick OP out of active site if given before “aging”

63
Q

What is an example of an Oxime?

A

Pralidoxine

  • only commercially available in US
  • given along w/ atropine for OP poisoning
64
Q

Ganglionic blocking drugs. 2 examples?

A

-very rarely used clinically

block Nicotinic R inautonomic ganglia

ex. mecamylamine
ex. trimethaphan- short acting IV for hypertensive emergencies

65
Q

What are Neuromuscular Nicotinic Blockers?

A

for cheimcal paralysis in Anesthesia

Pharmacology-1 (15 decks)

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