Cholinergic Agonists and Antagonists Flashcards

1
Q

Muscarinic Receptors

A

GPCR receptors M1,M2,M3

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2
Q

M1 Receptors

A

Increases IP3, DAG and therefore Calcium

Activated myenteric plexus for GI motility and secretions

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3
Q

M2 Receptors

A

Open potassium channels to decrease heart rate and contractility
Decrease cAMP and Calcium at sympathetic nerves to decrease NE release

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4
Q

M3

A

Increase Ip3, DAG and calcium
Contract ciliary muscles for accomodation and AH drain
Contract GI, bladder and bronchiolar muscle
Secretions at GI, sweat, tear, salivary glands

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5
Q

Nicotinic Receptors

A

Ligand gated ion channels

Pentameric structures that open upon ACH binding and cause flow into the cell to initiate downstream effects

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6
Q

Nn

A

Postganglionic sympathetic and parasympathetic cells

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7
Q

Nm

A

Neuromuscular junction

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8
Q

Direct Acting Nicotinic

A

Nicotinic- nicotine, succinylcholine

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9
Q

Competitive Muscarinic Antagonists

A

Atropine, Scopalamine, Glycopyrrolate

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10
Q

Organophosphate Poisoning

A

SLUDGE or DUMBBELS

Treat with 2-PAM

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11
Q

SLUDGE and DUMBBELS

A

Sweating, LAcrimation, Urination, Diarrhea, Gastric Distress, Emesis
Diarrhea, Urination, Miosis, Bronchorrea, Bradycardia, Emesis, Lacrimation, Salivation

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12
Q

Atropine Poisoning

A
Blind as a bat (dilated, blurred vision)
Mad as a hatter (Nervous, confused, hallucinate)
Red as a beet (Flushed skin)
Hot as a hare (hot skin)
Dry as a bone (dry mouth, skin)
Bowel and bladder lose their tone 
And the heart runs alone (tachycardia)
Treat with physostigmine, lavage, lower temp, cathertization, barbituates
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13
Q

Nicotine

A

Activates neuronal nictoinic receptors and is used clinically to help with smoking cessation

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14
Q

Sucinylcholine

A

Depolarizing block of Nm receptors
Eliminated by butyryl cholinesterase
Used as a neuromuscular block during shock therapy or emergency intubation

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15
Q

Acetylcholine

A

Quartenary Nitrogen Analog
RAPID half life and is a nicotinic/muscarinic agonst
Eliminated by acetylcholinesterase
No therapeutic use

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16
Q

Metacholine

A

Quarenary Nitrogen Analog

Slective for muscarinic receptors and is used to diagnose asthma/test for severity

17
Q

Carbachol

A

Quartenary Nitrogen Analog
Muscarinic and Nicotinic Agonist
Long half life
Miotic agent in ocular surgery to reduce pressure

18
Q

Bethanechol

A

Quartenary Nitrogen Analog
Muscarinic selectivity and a long half life
Urinary retention, bladder atony

19
Q

Pilocarpine

A

Tertiary Amine
1 hour half life, selective for musarinic receptor
Treats dry mouth from radiation or sjorgens
Treat narrow angle glaucoma

20
Q

Neostigmine

A

Reversible AChE inhibitor with a mid half life
Treats muscle weakness from myasthenia gravis
REverse neuromuscular block

21
Q

Edrophonium

A

REversible AChE inhibitor with a short 10 min half life

USed to diagnose muscle weakness from disease or too much neostigmine

22
Q

Physostigmine

A

Reversible AChE inhibitor with a longer half life
Treats delirium from anticholinergic drugs (Atropine)
TReats glaucoma

23
Q

Donepezil

A

Reversible AChE inhibitor to treat alzheimers

24
Q

Pralidoxime (2-PAM)

A

Reverse organophosphate poisoning with a 75 min half life by being a peripheral AChE REactivator

25
Q

Echothiophate

A

Irreversible AChE inhibitor (LONG half life)

Treats open angle glaucoma

26
Q

Atropine

A
Muscarinic antagonist
Treats: - excessive secretions in surgery
- high frequency/urgency of peeing
- cystitis association
- hypertonic gut
- organophosphate poisoning
- bradycardia
27
Q

Scopolamine

A

Muscarininc antagonist to treat motion sickness and as an anti-saligogue (salivay secretion) during surgery

28
Q

Glycopyrrolate

A

Muscarinic receptor antagonist that is used to protect agains excessive muscarinic activation during the reversal of neuro-muscular blockade during surgery, anti-saligogue

29
Q

Quartenary N Analog Muscarinic Agonists

A

ACH, methachoine, carbachol, bethanechol

30
Q

Tertiary Amine Muscarinic Agonists

A

Muscarine, Pilocarpine

31
Q

Cholinesterase Inhibitors

A

Neostigmine, edrophonium, physostigmine, donepezil

32
Q

Irreversible cholinesterase inhibitors

A

organophosphates (reverse with 2PAM), echothiophate

33
Q

Muscarinic Antagonists

A

Atropine, Scopolamine, Glycopyrrolate