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🄼💊 M2 Adrenergic/Cholinergics > 8-21 Cholinergics > Flashcards

8-21 Cholinergics Flashcards

1
Q

[M1 Muscarinic Receptors]

A: Molecular Mechanism when activated (3)

B: Activates _______ Plexus—> INC _______ _______

A

[M1 Muscarinic Receptors]

A: INC IP3 / DAG / Ca+

B: Activates Myenteric Plexus—> INC GI Motility

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2
Q

[M2 Muscarinic Receptors]

A: Molecular Mechanism when activated (3)

B: Effects of Molecular Mechanism
ºPrevents _______ release from _______ nerve terminals by DEC _______ and _______

º _______[INC/DEC] [HR/Contraction/Cardiac Output] by opening ___ channels

A

[M2 Muscarinic Receptors]

A:
1) Opens K+ channels–> DEC HR/Contraction/Cardiac Output

2) DEC cAMP
3) DEC Ca+

B: [2 & 3] –> Inhibits NorEpi release from sympathetic nerve terminals

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3
Q

A: [M3 Muscarinic Receptors] _______[INC/DEC] IP3, DAG and Ca+.

B: What are the effects of this?

  1. Contracts ___ muscle (5)
  2. VasoDilation or vasoconstriction?
  3. Stimulates Secretions from _____ (6)
A

[M3 Muscarinic Receptors] INCREASE IP3, DAG and Ca+

Effects:
-Contracts circular ciliary muscle / bronchioles/GI smooth m/ uterine / bladder

  • VasoDilation (via NO from endothelium)
  • Stimulates secretions of GI tract / sweat glands / tear glands / salivary glands / pancreas / bile
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4
Q

NICOTINE

MOA

A

NICOTINE

MOA: ACTIVATES Neuronal NICOTINIC RECEPTORS

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5
Q

NICOTINE

Usage / Rx

A

NICOTINE

Usage / Rx: Reduces Withdrawal Sx associated with Smoking Cessation

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6
Q

SUCCINYLLCHOLINE

MOA

A

SUCCINYLLCHOLINE

MOA: BLOCKS MUSCULAR NICOTINIC RECEPTORS VIA DEPOLARIZATION –> NEUROMUSCULAR BLOCK!

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7
Q

SUCCINYLLCHOLINE

USAGE / RX (2)

A

SUCCINYLLCHOLINE

Usage / Rx:

  1. Emergent Intubation
  2. Electroconvulsive Shock Therapy
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8
Q

SUCCINYLLCHOLINE

Elimination

A

SUCCINYLLCHOLINE

Elimination: ButyrlCholinesterase

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9
Q

ACETYLCHOLINE

HALF-LIFE

A

ACETYLCHOLINE

HALF-LIFE = 150 milliseconds

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10
Q

ACETYLCHOLINE

USAGE / RX

A

ACETYLCHOLINE

USAGE / RX = NONE!

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11
Q

METHACHOLINE

HALF-LIFE (Longer or shorter than Ach?)

A

METHACHOLINE

HALF-LIFE = LONGER THAN ACH

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12
Q

METHACHOLINE

TOXICITY

A

METHACHOLINE

Toxicity: Bronchoconstriction

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13
Q

CARBACHOL

MOA

A

CARBACHOL

MOA: [Nicotinic and Muscarinic Receptor] Agonist

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14
Q

BETHANECHOL

MOA

A

BETHANECHOL

MOA: Muscarinic Agonist (specifically of the GI and Urinary Bladder)

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15
Q

BETHANECHOL

USAGE / RX (2)

A

BETHANECHOL

USAGE / RX: U

  • Urinary Retention
  • Neurogenic Bladder Atony
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16
Q

BETHANECHOL

CONTRAINIDICATION (3)

A

BETHANECHOL

CONTRAINDICIATIONS: 
DO NOT USE IN PT WITH: 
a)PUD [peptic ulcer dz] 
b) bradycardia
c) asthma
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17
Q

CARBACHOL

USAGE / RX (2)

A

CARBACHOL

USAGE / RX:

  • INDUCES MIOSIS IN OCULAR SURGERY
  • REDUCES PRESSURE (via miosis) POST-OCULAR SURGERY
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18
Q

METHACHOLINE

Contraindications

A

METHACHOLINE

Contraindications: DO NOT GIVE TO PT TAKING BETA BLOCKERS SINCE [BETA 2 AGONIST] IS USED TO REVERSE TESTING

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19
Q

METHACHOLINE

MOA

A

METHACHOLINE

MOA: Muscarinic Agonist

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20
Q

METHACHOLINE

USAGE / RX

A

METHACHOLINE

Usage/Rx: Dx of subclinical asthma or test of severe asthma

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21
Q

ACETYLCHOLINE

ELIMINATION

A

ACETYLCHOLINE

Elimination = Acetylcholinesterase

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22
Q

ACETYLCHOLINE

MOA

A

ACETYLCHOLINE

MOA= [Nicotinic and Muscarinic Receptor] Agonist

23
Q

Pralidoxime:

Half-life

A

~75 mins

24
Q

Pralidoxime:

Mechanism of Action

A

Peripheral AchE reactivator

25
Q

Pralidoxime:

Rx

A

Respiratory muscle weakness in organophosphate poisoning

[Tx for organophosphate poisoning/serine gas - reactivation of alkylphosphorylated AChE with Pralidoxime Chloride (2-PAM) ]

26
Q

Echothiophate:

Half-life

A

Very long

27
Q

Echothiophate:

Mechanism of Action

A

Irreversible AchE inhibitor

28
Q

Echothiophate:

Rx

A

Used to produce long-term miosis in the treatment of open angle glaucoma

29
Q

Atropine:

Mechanism of Action

A

Muscarinic ANTagonist

30
Q

Atropine:

Rx (6)

A
  1. Reduces Excess secretions during surgery,
  2. Treats ↑ freq and urgency micturition associated
    with cystitis/UTI
  3. Relieves hypermobility of colon and hypertonicity of small intestines
  4. organophosphate poisoning/cholinesterase inhibitor induced poisoning
  5. Reverses bradycardia of vagal origin,
  6. Reduces mydriasis and cycloplegia (ie- paralysis of the ciliary muscle)
31
Q

Scopolamine:

Mechanism of Action

A

Muscarinic antagonist

32
Q

Scopolamine:

Rx (2)

A
  1. Motion Sickness and Chemotherapy N/V

2. Pre-OP anti-salilagogue (minimizes secretions for surgical anesthesia)

33
Q

Glycopyrrolate:

Mechanism of Action

A

GI Muscarinic ANTagonist

34
Q

Glycopyrrolate:

Rx (2)

A
  • Prevents excessive [GUT muscarinic activation] during reversal of neuromuscular blockade
  • antisalilagogue
35
Q

Pilocarpine:

Half-life

A

1 hr

36
Q

Pilocarpine:

MOA

How well does it move through BBB?

A

Neuronal Muscarinic agonist (crosses BBB very well)

37
Q

Pilocarpine:

Rx (Indications) (2)

A
  1. Dry mouth from head and neck radiation

2. Narrow angle glaucoma

38
Q

Pilocarpine:

Contraindications

A

Administer with care to pts taking B-blockers due to exacerbation of conduction slowing.

39
Q

Neostigmine:

MOA (2)

How well does it move through BBB?

A

(1) AchE inhibitor (poor penetration of BBB)

(2) Direct stimulatory effect on nicotinic receptors of skeletal muscle endplate

40
Q

Neostigmine:

Rx (Indications) (2)

A
  1. Myasthemia gravis

2. Reverse neuromuscular block

41
Q

Neostigmine:

Side effects

A

Side effects related to excessive Ach action at peripheral muscarinic and nicotinic receptors.

42
Q

Edrophonium:

Half-life

A

10 min

43
Q

Edrophonium:

MOA (2)

A
  1. AchE inhibitor

2. Stimulates nicotinic receptors

44
Q

Edrophonium:

Rx (Indications) (2)

A
  1. Diagnosis of myasthenia gravis (as oppose to a cholinergic crisis)
  2. Reversal of neuromuscular block
45
Q

Edrophonium has a very ______ (rapid/slow) onset of action.

A

Edrophonium has a very RAPID(rapid/slow) onset of action.

46
Q

Edrophonium:

Side effects (2)

A
  1. Excessive use can result in muscle weakness which can mimic and be mistaken for myasthenia gravis progression
  2. Bradycardia
47
Q

Physostigmine:

MOA

How well does it move through the BBB?

A

Reversible AchE inhibitor

Readily cross the BBB

48
Q

Physostigmine:

Rx (Indications) (2)

A
  1. Delirium from anticholinergic drugs

2. Glaucoma

49
Q

How is Physostigmine inactivated?

A

Inactivated by plasma cholinesterases, but it takes a long time

50
Q

Physostigmine:

Side effects

A

Side effects related to increased Ach at muscarinic or nicotinic receptors

51
Q

Physostigmine:

Contraindications (3)

A
  1. Asthma
  2. Cardiac insufficiency
  3. Gut obstruction
52
Q

Donepezil:

Rx (Indications)

A

Treatment of Alzheimer’s

53
Q

Donepezil:

MOA

How well does it move through the BBB?

A

Reversible inhibitor of AchE in the CNS (so moves through BBB well)

🄼💊 M2 Adrenergic/Cholinergics (5 decks)

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