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Pharmacology > Cholinergic Pharm > Flashcards

Cholinergic Pharm Flashcards

1
Q

Steps in synaptic transmission

A
  1. Neurotransmitter synthesized and stored in neuron
  2. Action potential depolarizers presynaptic neurons
  3. Influx Ca2+
  4. Fusion and release of vesicle contents
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2
Q

Autonomic neurotransmitters

A
  1. Acetylcholine
  2. Norepinephrine
  3. Sympathetic NS
    A. Norepinephrine: at effectors
    B. Acetylcholine: ganglia and some receptors
    C. Dopamine: some effectors
  4. Parasympathetic NS
    A. Acetylcholine: ganglia and effectors
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3
Q

ANS receptors

A 
1. Transmembrane receptors
  A. Ion channels
    1. Nicotinic cholinergic receptors (all)
2. G-protein couples receptors (GPCR)
  A. Serpentine structure
    1. Muscarinic cholinergic receptors
    2. Alpha adrenergic 
    3. Beta adrenergic
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4
Q

Signal transduction

A 
1. NE or E and ACh 
  A. Receptors: alpha-1, M1, M3, M5
  B. Gq = stimulatory 
  C. Secondary messengers: IP3, DAG, Ca2+
1. NE or E and ACh
  A. ReceptorsL alpha-2, M2, M4
  B. Gi = inhibitory 
  C. Dec. cAMP
3. NE or E
  A. Receptors: all betas (1-3)
  B. Gs = stimulatory
  C. Inc cAMP
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5
Q

Direct ACh angonists

A 
AKA: cholinomimetics
1. Esters
  A. Methacholine (provocholine)
  B. Carbochol (isopto carbachol)
  C. Bethanechol (Urecholine)
  D. Acetylcholine 
2. Alkaloids
  A. Muscarine 
  B. Nicotine
  C. Pilocarpine (isopto carpine)
3. Synthetic
  A. Cevimeline (evoxac)
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6
Q

Methacholine

A
  1. AChE susceptibility: low
  2. Muscarinic action: high
  3. Nicotinic action: none
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7
Q

Carbachol

A
  1. AChE susceptibility: negligible
  2. Muscarinic action: ++
  3. Nicotinic action: +++
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8
Q

Bethanechol

A
  1. AChE susceptibility: negligible
  2. Muscarinic action: ++
  3. Nicotinic action: none
  4. Tx for urinary retention
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9
Q

Acetylcholine

A
  1. AChE susceptibility: ++++
  2. Muscarinic action: +++
  3. Nicotinic action: +++
    * not helpful to have equal actions
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10
Q

Pilocarpine (isopto carpine)

A
  1. M3
  2. Inc salivary and lacrimal secretions
  3. Treat: Sjogren’s syndrome
  4. Common side effects (wet)
    A. Nausea
    B. Inc. urination
    C. Diaphoresis (sweating)
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11
Q

Indirect-acting cholinomimetics

A 
AChE inhibitors
A. Reversible
 1. Quaternary amines
   A. Edrophonium (Enlon)
   B. Neostigmine (prostigmin)
   C. Pyridostigmine (mestinon)
   D. Ambenonium (mytelase)
 2. Tertiary amines
   A. Physostigmine (antillrium)
B. Irreversible (organophosphates)
  A. Echothiophate
  B. Malathion (ovide)
  C. Parathion
  D. Sarin
  E. So man
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12
Q

Edrophonium

A
  1. Quaternary
  2. Myasthenia gravis (test)
  3. Reversal neuromuscular blockade
  4. 5-15 min
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13
Q

Neostigmine

A
  1. Quaternary
  2. Myasthenia gravis
  3. Ilieus
  4. Reversal neuromuscular blockade
  5. Urinary retention
  6. 0.5-2 hrs.
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14
Q

Pyridostigmine

A
  1. Quaternary
  2. Myasthenia gravis
  3. reversal neuromuscular blockade
  4. 3-6 hrs
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15
Q

Ambenonium

A
  1. Quaternary
  2. Myasthenia gravis
  3. 4-8 hrs
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16
Q

Physostigmine

A
  1. Tertiary
  2. Open-angle glaucoma
  3. Anti-cholinergic syndrome
  4. 0.5-2 hrs
17
Q

Direct and indirect acting agent side effects

A 
1. Systemic 
  A. Salivation
  B. Lacrimation
  C. Urination
  D. Defecation
2. Specific
  A. Diaphoresis
  B. Bradycardia
  C. Miosis
18
Q

Organophosphates

A 
Irreversible AChE inhibitors
1. Echothiophate (phospholine)
  A. H2O soluble
2. Malathion (ovide)
3. Dioxathion
4. Parathion
5. Sarin and soman
19
Q

Cholinergic antagonists

A 
Allow sympathetic to take over
1. Tertiary amines (CNS)
  A. Atropine***
  B. Scopolamine (motion sickness)
  C. Benztropine (congentin)- Parkinson’s (M3)
  D. Trihexyphenidyl (artane)- Parkinson’s
  E. Tropicamide (tropicacyl) - pupil dilation
  F. Oxybutynin (ditropan)
  G. Darifenacin (enablex)
  H. Dicyclomine HCl- (Bentyl)
  I. Solifenacin succinate (vasicare)
  J. Tolterodine tartrate (Detrol)
2. Quaternary amines (peripheral effects)
  A. Ipratropium (atrovent) - COPD
  B. Tiotropium (spiriva) - COPD
  C. Propantheline (probanthine)
20
Q

Organ antagonist sensitivity

A
  1. Most: secretion organs
  2. More: eyes, mouth, resp
  3. Less: heart, gut
  4. Least: CNS
21
Q

Atropine mechanism

A
  1. Binds muscarinic receptor
  2. Inhibits ACh binding
    * *side effects = anti-SLUD
22
Q

Atropine effects

A
  1. 0.5-1 mg: dry mouth, dry skin
  2. 2 mg: dilated pupils, accommodation paralyzed, tachycardia
  3. 5 mg: very dry, dec GI and bladder tome, dec gastric acid, CNS effects
  4. 10 mg: CNS toxicity
  5. 100-200 mg: coma
23
Q

Organophosphate poisoning tx

A
  1. Atropine
  2. 2-PAM (pralidoxime) = AChE reactivator
    A. Must be given quickly
    B. Can’t break aged bond
24
Q

Parkinson’s disease

A 
1. Dec dopamine
  A. Needed for fine motor control
  B. ACh -> muscle contraction
  C. Dopamine + ACh -> smooth movement
2. Antagonists dec ACh at nicotinic receptors -> closer balance w/ dopamine
  A. Less rigidity and tremors
  B. Benztropine (cogentin)
  C. Trihexyphenidyl (artane)
    1. Adjunctive therapy w/ levodopa
    2. Side effects: dry mouth, sedation
25
Q

Ophthalmology

A
  1. Tropicamide (tropicacyl) -> dilation

A. Side effects: dry eyes, acute glaucoma

26
Q

COPD tx

A
  1. Ipratropium (atrovent)
  2. Tiotropiun (spiriva)
    *inhibit muscarinic receptor -> block parasympathetic
    A. Bronchodlilation
    B. Dec pulm secretions
27
Q

Urinary incontinence and overactive bladder tx

A 
1. Nonselective muscarinic antagonists
  A. Oxbutynin (Ditropan) -M1 and M3
  B. Tolterodine (detrol)
  C. Propantheline (Probanthine)
  D. Fesoterodine (toviaz)
  E. Trospium (sanctura)
  F. Mirabegron (myrbebrig)
2. Selective M3 antagonists 
  A. Darifenacin (enablex)
  B. Solifenacin (vesicare)
28
Q

Bradycardia tx

A 
1. Atropine
  A. Mod-high does -> tachycardia
  B. Pts w/ sinus bradycardia
    1. Give 0.5 mg
    2. Observe inc HR
    3. Improved signs/symptoms
  C. Paradox
    1. <0.5 mg dec. HR
    2. Attributed to autoreceptor blockade on presynaptic -> release ACh

Pharmacology (4 decks)

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