Brainscape's Knowledge GenomeTM

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


See full index

PTP&M: Neuro > Muscarinic Receptor Agonists/Antagonists > Flashcards

Muscarinic Receptor Agonists/Antagonists Flashcards

1
Q

Muscarinic Agonist Effect: Eye

A
  1. ) Accommodation (near sight adjustment)

2. ) Pupil constriction

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

Muscarinic Agonist Effect: Heart

A
  1. ) HR REDUCTION

2. ) Contraction force REDUCTION

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

Muscarinic Agonist Effect: Glands + Blood Vessels

A
  1. ) Increase sweat
  2. ) increase salivation
  3. ) increase tearing
  4. ) VASODILATION
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Muscarinic Agonist Effect: Lung

A
  1. ) BronchoCONSTICTION (avoid in asthmatics)

2. ) INCREASED secretions

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

Muscarinic Agonist Effect: Urinary Bladder

A
  1. ) Detrusor muscle CONTRACTION

2. ) Relax urinary sphincter

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

Muscarinic Agonist Effect: GI Tract

A
  1. ) Increased peristalsis
  2. ) Increased secretions (i.e. acid)
  3. ) DECREASE sphincter tone
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Muscarinic Receptors: Brain/CNS

A

M1 - M5 (all 5 classes)

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

Muscarinic Receptors: Heart

A

M2

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

Muscarinic Receptors: Glands/Smooth Muscles

A

M3

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

Muscarinic Receptor: GPCR or Ion Channel?

A

GPCR
Regulate Enzymes Fx: AC, PLC, MAPK
Regulate Ion Channels: K+, Ca++

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

Four Major Cholinergic Groups (CNS)

A
  1. ) Nucleus Basalis of Meynert*** (cortical innervation)
    • expands from ~hippocampus outwards
  2. ) Medial Septal Nucleus (hippocampus)
  3. ) Brainstem: thalamus
  4. ) Basal ganglia: interneurons
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Acetylcholine:
Cholinesterase activity
Muscarinic Activity
Nicotinic Activity

A

Quaternary Amine
CEA: ++++
M: +++
N: +++

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

Methacholine:
Cholinesterase activity
Muscarinic Activity
Nicotinic Activity

A

Quaternary Amine + CH3
CEA: +
M: +++
N: –

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Cabachol:
Cholinesterase activity
Muscarinic Activity
Nicotinic Activity

A

Quaternary Amine + NH2
CEA: –
M: ++
N: +++

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Bethanechol:
Cholinesterase activity
Muscarinic Activity
Nicotinic Activity

A

Quaternary Amine + CH3 + NH2
CEA: –
M: ++ (not subtype-selective)
N: –

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

MUSCARINE

A

Quaternary Amine
No BBB Cross
No longer used clinically

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

PILOCARPINE

A 
Secondary Amine
CROSSES BBB (therefore psychostimulant)

Treat: xerostomia, glaucoma (sometimes)

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

ARECOLINE

A 
Betel nut extract (stimulant/recreational drug)
Tertiary amine (crosses BBB)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Muscarinic Agonist Uses (5)

A
  1. ) Recreational (arecoline)
  2. ) Glaucoma
  3. ) Urinary retention (post-op)
  4. ) Gastrointestinal atony (post-op/neurogenic ileus)
  5. ) Xerostomia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Open Angel Glaucoma

A

90% Cases

  • clogged intratrabecular network prevents outflow of intraocular fluid (increased intraocular pressure)
  • contracts cilliary muscles –> frees exit via Schlemm

M3 stimulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Closed Angel Glaucoma

A

10% Cases (rare)
-lens + iris contact

M3 stimulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Xerostomia: 2 Causes + 2 Treatments

A
  1. ) Neck/head irradiation
  2. ) Sjogren’s Sx
  3. ) Pilocarpine
  4. ) Cevimeline
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Urinary Retention (musc. agon.) Treatment

A

Bethanechol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

GI Atony Treatment

A

Bethanecol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Glaucoma (sometimes)

A

Pilocarpine

26
Q

Muscarinic AGONIST: Contraindications

A
  1. ) SEVERE ASTHMA *****
  2. ) Severe bradycardia
  3. ) Parkinson’s disease
  4. ) Urinary/bowel obstruction
27
Q

Muscarinic AGONIST: ADEs

A
  1. ) Diarrhea
  2. ) Excessive salivation/tears/sweating
    • “Sweating mushroom”
  3. ) Miosis/accomdation (no far vision)
  4. ) N/V
  5. ) Urinary urgency
  6. ) Bronchoconstriction (no asthma)
  7. ) Hypotension/bradycardia
  8. ) Seizures/tremor/hypothermia
28
Q

Muscarinic ANTAGONIST Effect: Eyes

A
  1. ) NO accommodation (no near-sight)

2. ) Dilated pupils

29
Q

Muscarinic ANTAGONIST Effect: Heart

A
  1. ) TACHYcardia

2. ) Increased contractile force

30
Q

Muscarinic ANTAGONIST Effect: Glands

A
  1. ) Decreased salivation

2. ) Decreased sweating

31
Q

Muscarinic ANTAGONIST Effect: Lungs

A
  1. ) Bronchodilation

2. ) Decreased secretions

32
Q

Muscarinic ANTAGONIST Effect: Urinary Bladder

A
  1. ) Relaxation

2. ) Loss of sphincter tone

33
Q

Muscarinic ANTAGONIST Effect: GI Tract

A
  1. ) Decreased peristalsis

2. ) Decreased secretions (acids, etc.)

34
Q

ATROPINE

A

NO BBB CROSSING
-lacks oxygen bridge (on base ring)
M1, M2, M3
Little to no affinity for nicotinic receptors

35
Q

Atropine: Problems

A
  1. ) Side-effects
  2. ) Non-selective for M3 (off-target effects)
  3. ) Some BBB-crossing
  4. ) LONG duration of action
36
Q

SCOPOLAMINE

A 
Crosses BBB
-possess base oxygen bridge
-lacks oxygen bridge (on base ring)
M1, M2, M3
Little to no affinity for nicotinic receptors
37
Q

Ipatropium vs. Atropine

A

Ipatropium has fewer ADEs
*Quaternary amine prevents entrance into bloodstream
*Some xerostomia due to minimal systemic absorption
See also: tiotropium, aclidinium

38
Q

Solifenacin: Indication and advantages

A

*Urinary incontinence

  • M3-selective TERTIARY amine
  • Limited M2 affinity
  • Good bioavailability
  • great for elderly patients
39
Q

Muscarinic Receptor Antagonist: Ophthalmology

A 
Tropicamide        15-60min
Cyclopentolate    3-6hr
Homatropine       12-24hr
Scopolamine        3-7d
Atropine                5-6d
40
Q

Muscarinic ANTAGONIST: ADEs

A
  1. ) Blurred vision, mydriasis
  2. ) Urinary retention
  3. ) Constipation
  4. ) Tachycardia
  5. ) Reduced sweating
  6. ) Confusion, hallucinations

THINK OVER-ACTING ACH EFFECTS

41
Q

“Dry as a….” Phrase from Slide Set 3 (Muscarinic Antagonists)

A

DRY as a bone
BLIND as a bat
RED as a beet
MAD as a hatter

42
Q

Muscarinic Antagonist: Contraindications

A
  1. ) GLAUCOMA
  2. ) Benign prostatic hyperplasia
  3. ) Gastric ulcer
43
Q

Acetylcholinesterase Inhibitor Mechanism

A
  1. ) ACH binds active site
  2. ) Nucleophilic attack of active site serine on ester oxygen (release of choline)
  3. ) Hydrolysis of acetyl group (regenerate serine)
44
Q

Edrophonium

A

Competitive acetylcholinesterase inhibitor
-binds choline site + prevents binding
*quaternary amine strucutre
SHORT HALF LIFE (rare)

45
Q

Carbamate ACE Inhibitors

A
  1. ) Physostigmine
  2. ) Pyridostigmin (quat amine)
  3. ) Neostigmine (quat amine)

MOA: catalysis conjugates serine residue. slow hydrolysis (~mins) temporarily inactivate enzymes

46
Q

Organophosphate AChEs

A

1.) Oxygen binds phosphate group
2.) Leaving group (halide) facilitates Sn2 binding mechanism
3.) SLOW (~days) hydrolysis inactivates AChE
“permanent inactivation”

Example: diisopropyl fluorophosphate (DFP)

47
Q

Acute Organophosphate Toxicity: SLUDGEM

A 
Salivation
Lacrimation
Urination
Defecation
GI motility
Emesis
Miosis
48
Q

Acute Organophosphate Toxicity: BBB

A

Bronchospasm
Bronchial secretion
Bradycardia

49
Q

Organophosphate Toxicity: Antedotes

A

1.) 2-PAM (pralidoxime)
2.) Atropine
[atropine toxicity –> O.P. pyridostigmin]

50
Q

2-PAM

A

Pralidoxime
*strips organophosphate moiety from active site serine
(ineffective if OP-enzyme bond has aged)

Uses:

  • reverses effects at nicotinic receptors (NMJ)
  • muscarinic receptors (controversial)
  • no BBB travel (quaternary amine)
51
Q

Malathion

A

Pesticide (old)
Mammals (LD50 1.2g/kg) –> metabolizes into inactive/inert metabolite
Insects/Fish (LD50 0.5mcg/bee)–> metabolized into highly toxic metabolite (MALAOXON)

52
Q

Acetylcholine Esterase Inhibitor (AChE In.) Uses (4)

A
  1. ) Glaucoma (echothiophate)
  2. ) GI/Urinary tract effects
  3. ) Myasthinea Gravis (NMJ effects)
  4. ) CNS Effects (Alzheimers disease)
53
Q

Myasthinea Gravis Treatments (3)

A
  1. ) Immune suppressants
  2. ) Pyridostigmine
  3. ) Neostigmine
54
Q

Myasthinea Gravis Characteristics (3)

A
  1. ) autoimmune disease (antibodies are made vs. nicotinic receptors at NMJ)
  2. ) Abs block ACh binding with nicotinic receptors
  3. ) Abs initiate complement –> destroys post-synaptic membrane
55
Q

Pyridostigmine (ADEs)

A
  1. ) GI issues (diarrhea)
  2. ) Salivation
  3. ) Sweating
  4. ) Urinary urgency
  5. ) Bronchiole secretions
56
Q

AChE Inhibitors: AD (3)

A
  1. ) Rivastigmine (carbamate (reversible))
  2. ) Donepezil (competitive)
  3. ) Galantamine (competitive)
    • *effective for BOTH NICOTINIC + MUSCARINIC**
57
Q

Rivastigmine (AD)

A
  1. ) Effective in MILD and MODERATE disease
  2. ) High ADE potential (esp N/V)
  3. ) Have not been compared to Quat amine compounds (i.e. pyridostigmine)
58
Q

Inhibitor: VAT

A

VAT = vesicle-associated transporter (H+-mediated)

Vesamicol

59
Q

Inhibitor: Presynaptic Vesicle Binding

A

Botulinum Toxin

-cleaves SNAPs + VAMPs preventing fusion and release of neurotransmitters

60
Q

Inhibitor: CHT

A

Sodium-dependent Choline Transporter (CHT)

Hemicholiniums

PTP&M: Neuro (5 decks)

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