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CMBM Exam 2 > Cholinergics > Flashcards

Cholinergics Flashcards

1
Q

Synthetic direct acting cholinergic receptor drugs

A

Esters of choline:

  • Bethanecol
  • Carbachol
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2
Q

Natural direct acting cholinergic receptor drugs

A
  • Acetylcholine
  • Cholinomimetic alkaloids
  • Pilocarpine
  • Nicotine
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3
Q

Indirect acting cholinergic receptor drugs

A

Elevate endogenous levels of ACh through inhibition of cholinesterase

  • Donepezil
  • Edrophonium
  • Neostigmine
  • Physostigmine
  • Pyridostigmine
  • Rivastigmine
  • Tacrine
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4
Q

Irreversible cholinergic receptor drugs

A
  • Isoflurophate
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5
Q

Irreversible cholinergic receptor drug OD antidote

A
  • Pralidoxime
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6
Q

Enhanced release of acetylcholine drug

A
  • Guanidine
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7
Q

Miochol major therapeutic use

A
  • Produces rapid, complete miosis for ocular surgery (e.g.,

cataracts, iridectomy)

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8
Q

Carbachol MOA

A
  • Direct-Acting Cholinomimetic Agents

- Synthetic Choline Ester

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9
Q

Carbachol ADR’s

A

flushing, sweating, cramping, urinary urgency, severe headache

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10
Q

Carbachol contraindications

A
  • Parkinsonism; too much acetylcholine is going to make Parkinson’s worse
  • Corneal abrasions, acute iritis
  • Precautions necessary in presence of asthma, peptic ulcer, or urinary distress
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11
Q

Bethanechol MOA

A
  • Direct-Acting Cholinomimetic Agents
  • Synthetic Choline Ester
  • Activates muscarinic receptors: increases GI peristalsis and defecation - ↑ tone of detrusor muscle; stimulates micturition
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12
Q

Bethanechol ADR’s

A

Sweating, flushing, salivation, abdominal discomfort, nausea, diarrhea, GI pain and cramping

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13
Q

Bethanechol contraindications

A

peptic ulcer, bronchial asthma, urinary obstruction, parkinsonism

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14
Q

Pilocarpine major therapeutic uses

A
  • Used for open-angle glaucoma, reversal of cycloplegics and mydriatics after eye exam or surgery
  • Pilocarpine Ocular Therapeutic System: continuous release form of pilocarpine (20 μg or 40 μg/h) placed into lower conjunctival cul-de-sac. Used primarily for continuous therapy of open-angle glaucoma.
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15
Q

Carbachol major therapeutic uses

A
  • pupillary miosis during surgery

- chronic treatment of open-angle glaucoma

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16
Q

Bethanechol major therapeutic uses

A
  • nonobstructive urinary retention
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17
Q

Pilocarpine MOA

A
  • Natural product
  • Cholinomimetic alkaloid
  • Direct cholinergic receptor activation produces contraction of ciliary muscle and ciliary body; miosis occurs which ↑s outflow of aqueous humor from the anterior chamber.
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18
Q

Nicotine MOA

A
  • Activates cholinergic receptors in autonomic ganglia, NMJ, adrenal medulla, and brain
  • CNS: Stimulates cerebral cortex via locus ceruleus; increases alertness and cognitive performance
  • CV: peripheral vasoconstriction, tachycardia, increased BP
  • Stimulates limbic system: ↑ ‘reward’ and ‘pleasure’ action
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19
Q

Nicotine addiction treatment

A

Transdermal:
- Habitrol: peak nicotine levels between 6-12 hrs
- Nicoderm: peak nicotine levels between 2-4 hrs
P.O.:
- Varenicline: Partial agonist action at nicotinic receptors; weaker than nicotine. Can cause serious neuropsychiatric events: suicide, agitation, hostility, depressed mood, or changes in behavior

20
Q

Nicotine ADR’s

A

CV: hypertension
GI: diarrhea, constipation
GU: MI, Buerger’s Disease (limbs start to get cold due to blood vessel constriction)

21
Q

Physostigmine MOA

A
  • Reversible inhibitor of cholinesterase

- Highly lipid-soluble; readily penetrates CNS

22
Q

Physostigmine major therapeutic uses

A
  • Reversal of cycloplegia and mydriasis caused by anticholinergic drugs
  • Antidote to toxic neurologic effects caused by drugs having central anticholinergic activity (e.g., scopolamine, tricyclic antidepressants)
  • Generally short-acting cholinergic drugs used both topically and systemically. Primarily employed for ophthalmic use and for diagnosis and treatment of myasthenia gravis
23
Q

Edrophonium major therapeutic uses

A

Given only by injection
- Diagnosis of myasthenia gravis
- Treatment of poisoning with nondepolarizing skeltal muscle relaxants
- Used to test for underdosage or OD of cholinergic agents in patients with myasthenia. IV test dose given:
improvement of muscle strength = underdose (myasthenic crisis)
increased muscle weakness = OD (cholinergic crisis)

24
Q

Neostigmine MOA

A
  • Reversible inhibitor of cholinesterase
  • Exhibits direct ACh-like stimulating effect at cholinergic receptors on skeletal muscle
  • May increase release of presynaptic stores of ACh
25
Q

Neostigmine major therapeutic uses

A

Treatment of:

  • myasthenia gravis
  • poisoning with non-depolarizing skeletal muscle relaxants
26
Q

Pyridostigmine MOA

A
  • Reversible inhibitor of cholinesterase
27
Q

Pyridostigmine major therapeutic uses

A

Treatment of:

  • myasthenia gravis
  • poisoning with non-depolarizing skeletal muscle relaxants
28
Q

Isoflurophate MOA

A
  • Irreversible acetylcholine inhibitor

- Effects may persist for several weeks because of the permanent inactivation of cholinesterase

29
Q

Pralidoxime MOA

A
  • Cholinesterase Inhibitor Antidote
  • Disrupts bond between phosphorus group of enzyme inhibitor and esteratic site of cholinesterase enzyme; then displaces cholinesterase inhibitor from enzymatic binding sites
  • Antagonizes effects of reversible cholinesterase inhibitors
30
Q

Guanidine MOA

A
  • Enhances release of acetylcholine after nerve impulse
31
Q

Guanidine major therapeutic uses

A
  • Unique cholinergic agent that alleviates symptoms (muscle weakness, fatigability) of myasthenic syndrome of Eaton-Lambert syndrome.
  • Due to relatively high toxicity, use generally restricted to treatment of myasthenic syndrome of Eaton-Lambert syndrome (carcinomatous myopathy, i.e., muscle weakness accompanying a malignant disease, particularly bronchogenic carcinoma)
32
Q

Various changes in CNS cholinergic neurons appear to occur as humans age; such alterations may include:

A
  • reduced activity of choline acetylcholine transferase
  • reduced synthesis of ACh
  • reduced responsiveness of post-synaptic M1 receptors in frontal cortex and hippocampus
  • loss of cortical neurons (>50% in some areas by age 85)
33
Q

Alzheimer’s Disease (AD) neuronal changes

A
  • increased deposition of Beta-amyloid protein
  • reduced number of synapses (increased synaptic size occurs; possible compensation)
  • reduced activity of acetylcholinesterase (possible compensation for reduced ACh synthesis)
34
Q

Lecithin MOA

A
  • Increase Synthesis of ACh

* Precursor of ACh —> increases ACh levels in central synapses (e.g., lecithin reduces tardive dyskinesias)

35
Q

Lecithin major therapeutic uses

A
  • Therapeutic effects oberved only when combined with physostigmine or tacrine
  • improvement in memory and cognition in AD when used
36
Q

4-Aminopyridine (4-AP) MOA

A
  • Increase Release of ACh
  • K+ channel blockers reduce K+ efflux and ↑ release of blockade of K+ channel➡️reduced K+ efflux➡️longer time to repolarize (prolongation of action potential; longer excitation)➡️increased Ca+ influx➡️increased release of ACh
37
Q

4-Aminopyridine (4-AP) major therapeutic uses

A
  • K+ channel blocker, is an investigational agent that has been employed in clinical trials for treatment for AD
38
Q

Physostigmine MOA

A
  • Centrally-acting reversible anticholinesterase agent
    • Enhancement of central cholinergic activity
    • Reduce Catabolism of ACh
39
Q

Acetylcholinesterase inhibitors major therapeutic uses

A
  • Have been associated with reduced rate of deterioration in dementia. This conclusion is from many clinical trials and meta-analyses
  • Produced slight ↑ in memory performance in 6-week trial
40
Q

Tacrine MOA

A
  • Centrally-acting reversible anticholinesterase agent
    • Enhancement of central cholinergic activity
    • Reduce Catabolism of ACh
41
Q

Tacrine major therapeutic uses

A
  • Significant (51% of pts receiving 80 mg/day) increase in cognitive performance during 12-week study
42
Q

Tacrine ADR’s

A
  • Hepatotoxic
  • sig. (3x norm.) asymptomatic ↑ in ALT (25% of pts)
  • reversible upon d.c.
43
Q

Donepezil MOA

A
  • Centrally-acting reversible anticholinesterase agent
44
Q

Donepezil major therapeutic uses

A
  • First product approved by FDA for Tx of all degrees of dementia of the Alzheimer’s type: mild, moderate, and severe
45
Q

Rivastigmine MOA

A
  • Centrally-acting reversible anticholinesterase agent

- Inhibits AChE and butyrylcholinesterase; both bio-transform central acetylcholine

46
Q

Rivastigmine major therapeutic uses

A
  • For Tx of mild to moderate dementia of the Alzheimer type

CMBM Exam 2 (13 decks)

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