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CPR 2 Exam 1 > Kruse Cholinergic Agonists and Antagonist > Flashcards

Kruse Cholinergic Agonists and Antagonist Flashcards

1
Q

Direct acting cholinomimetics?

A
  • Acetyolcholine
  • Bethanechol
  • Carbachol
  • Cevimeline
  • Methacholine
  • Pilocarpine
  • Varenicline
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2
Q

Cholinesterase Inhibitors?

A
  • Ambenonium
  • Donepezil
  • Echothiophate
  • Edrophonium
  • Galantamine
  • Neostigmine
  • Physostigmine
  • Pyriedostigmine
  • Rivastigmine
  • Tacrine
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3
Q

Antimuscarinic drugs for motion sickness and GI disorders?

A
  • Scopolamine-motion sickness
  • GI disorders
    • Atropine
    • Dicyclomine
    • Glycopyrrolate
    • Hyoscyamine
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4
Q

Antimuscarinic drugs used for respiratory disorders?

A
  • Ipratropium
  • Tiotropium
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5
Q

Antimuscarinic drugs used for urinary disorders?

A
  • Darifenacin
  • Fesoterodine
  • Oxybutynin
  • Solifenacin
  • Tolterodine
  • Trospium
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6
Q

Antimuscarinic Drugs used for cholinergic poisoning?

A

Atropine

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7
Q

Antimuscarinic Drugs used for movement disorders?

A
  • Benztropine
  • Biperiden
  • Orphenadrine
  • Procyclidine
  • Trihexyphenidyl
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8
Q

In general, what are acetylcholine mimetics?

A

(Agonist)

drugs that mimic actions of ACh on nicotinic and muscarinic ACh receptors

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9
Q

Where are M1 receptors found, what G protein, and what mechanism is used?

A
  • Nerves
  • Gq
  • IP3 DAG cascade
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10
Q

Where are M2 receptors found, what G protein, and what mechanism is used?

A
  • Heart nerves smooth muscle
  • Gi
  • Inhibit cAMP production
  • Activation of K channels
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11
Q

Where are M3 receptors found, what G protein, and what mechanism is used?

A
  • Glands smooth muscle and endothelium
  • Gq
  • IP3 DAG cascade
  • Memory trick: QIQI-Q mart store (M1 Q M2 i M3 Q M4i M5Q)
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12
Q

Where are M4 receptors found, what G protein, and what mechanism is used?

A
  • CNS
  • Gi
  • Inhibit cAMP
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13
Q

Where are M5 receptors found, what G protein, and what mechanism is used?

A
  • CNS
  • Gq
  • IP3 DAG cascade
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14
Q

Direct action of cholinergic agonist effects on the eye?

A
  • contraction of iris sphincter and ciliary muscle resulting increase of aqueous humor outflow into canal of schlemm
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15
Q

Direct action of cholinergic agonist effects on the cardiovascular system?

A
  • ALL cardiac actions are mediated by M2 mAChR resulting in decrase in periphreal vascular resistance
  • Reduction in BP due to EDFR (NO) release causing vasodilation
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16
Q

Direct action of cholinergic agonist effects in the GIGU system?

A
  • Causes an increase in glandular secretions
  • M3 is needed for direct activation of sm mm contraction
  • M2 reduces cAMP formation and causes contraction
  • sphincter relaxation M3 via NO
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17
Q

What are the clinical uses of direct acting cholinergic agonists for glaucoma?

A
  • Muscarinic stimulants cause contraction of ciliary body that stimulates aqueous humor and reduces intraocular pressure
  • however they were replaced by topical Beta blockers and prostaglandin derivatives
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18
Q

How do we treat accommodative esotropia?

A

Cholinomimetic agonists

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19
Q

____ is the most widely used choline ester for GIGU disorders including post op ileus, megacolon, urinary retention, and esophageal reflux.

What category of drug does this fall under?

A

Bethanechol is the most widely used choline ester for GIGU disorders including post op ileus, megacolon, urinary retention, and esophageal reflux.

Direct acting cholinergic agonist

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20
Q

Before treating a patient with a GIGU disorder with Bethanechol, what must be done?

A

Make sure there are no obstructions as the drug may exacerbate the problem or case perforation

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21
Q

What two drugs are used to increase salivary secretion to treat Sjogren’s syndrome?

A
  • Pilocarpine
  • Cevimeline
  • Both are a direct acting cholinergic agonist
22
Q

What are major contraindications to the uses of MAChR agonists?

A
  • Asthma
  • hyperthyroidism
  • coronary insufficiency
  • acid peptic disease
23
Q

Overdoses of Pilocarpine and choline esters has what symptoms? How do you treat the OD?

*bonus what is pilocarpine used to treat?

A
  • cause N/V, diarrheae, urinary urgency, salivation, sweating, cutaneous vasodilation, bronchial constriction
  • Blocked by antimuscarinic compounds such as Atropine
  • Sjogren’s syndrome
24
Q

What are the acute toxicities of nicotinic stimulants? How do you treat this?

A
  • CNS stimulation such as convulsions progressing to coma/resp. arrest
  • Muscle and respiratory paralysis
  • Htn
  • Cardiac arrhythmias
  • Treat with atropine and diazepam for CNS stimulation
  • *Neuromuscular blockade is NOT responsive to pharmacologic treatment
25
Q

What does Acetylcholine do to the eye?

A
  • Causes Mioisis (reduces pupil size)
26
Q

What is Bethanechol used for? What type of drug is it? What AE can it cause?

A
  • treat patients with urinary retention and heartburn
  • mAChR agonsit
  • Produce UTI if sphincter fails to relax
27
Q

What is Carbachol used for?

A
  • Nonspecific cholinergic agonist used for tx of glaucooma or produce miosis during surgery or ophthalmology exam
28
Q

What is Cevimeline used for? What pathway is it metabolized?

A
  • Oral tablet to treat xerostomia in Sjogren’s syndrome
  • Metabolized via P450
29
Q

What is Pilocarpine used for?

A
  • Xerostomia in patients with Sjogren’s syndrome
  • Head/neck cancer related to xerostomia
  • Topical agent to cause Miosis during opthalmic procedures
  • Topical for glaucoma
30
Q

Varenicline use?

A
  • FDA approved for smoking cessation (chantix)
  • Partial agonist that binds with high affinity and selectivity to alpha 4 beta2 nicotinic AChR
31
Q

Varenicline AE and warnings?

A
  • Nausea, Neuropsychiatric sx
  • If depression, suicidal ideation, agitation, or behavior changes occur stop taking
32
Q

What are the three groups of cholinesterase inhibitors? How do they bind and is it reversible or irreversible?

A
  • Alcohols: positive or neutral charge non covalent binding and reversible
  • Carbamic acid esters: positive or neutral charge non covalent binding and reversible
  • Organophosphates: neutral charge, lipid soluble, covalent and irreversible
33
Q

What is the net cardiovascular effect of AChE inhibitors?

A

Bradycardia and an increase in BP

34
Q

What are the therapeutic uses of AChE inhibitors?

A
  • Glaucoma, accommodative esotropia
  • Post op atony, neurogenic bladder
  • Myasthenia gravis, curare induced neuromuscular paralysis
  • Alzheimer disease
35
Q

What does intoxication due to anticholinergic agents look like? How do you reverse it?

A
  • Cutaneous vasodilation
  • Anhidrosis
  • Anhydrotic hyperthermia
  • non-reactive mydriasis
  • Delirium
  • Hallucinations
  • reduction or elimination of urination

Use physostigmine to reverse (crosses BBB)

36
Q

What drugs do AChE inhibitors interact with?

A
  • Nondepolarizing neuromuscular blocking agents
  • Succinyolcholine
  • Cholinergic agonists (direct acting)
  • Beta blockers
  • Systemic corticosteroids
37
Q

How do you diagnose AChE poisoning? How do you reverse it?

A
  • AChE activity in erythrocytes and plasma
  • Atropine an mAChR antagonist
  • to regenerate AChE at NMJ cholinesterase regenerator can be given
38
Q

Organophosphate overexposure antidote?

A
  • parenteral atropine, pralidoxime, and benzodiazepine
39
Q

What receptors do Atropine target? (mAChR antagonist)

What tissues are most sensitive to least?

A
  • antagonizes all 5 mAChR’s and doesnt differentiate
  • salivary, bronchial, sweat glands, acid secretion gastric parietal cells
40
Q

mAChR antagonist effects on respiratory system?

A
  • bronchodilation & reduced secretion
41
Q

mAChR antagonist effects on GI system?

A
  • Decrease salivary secretion
  • Gastric secretion is decreased slightly
  • Pancreatic and intestinal secretions largely unaffected as under hormonal control not vagal
  • Gastric emptying is prolonged
42
Q

Why are mAChR antagonists good for urinary incontinence?

A
  • relax smooth muscle of the ureters and bladder wall and slow voiding
43
Q

What is atropine fever?

A
  • occurs in kids with normal doses of antimuscarinic agents
  • Atropine suppresses thermoregulatory sweating y inhibiting sympathetic cholinergic nerve fibers of sweat glands
44
Q

What three CNS disorders can antimuscarinic agents be used in?

A
  • Parkinsons
  • Motion sickness
  • Anesthesia
45
Q

What antimuscarinic agent is used to treat COPD?

A
  • Ipratropium, used an an inhalational agent (first line therapy)
  • Newly approved, Tiotropium is used once daily for COPD
46
Q

How are antimuscarinics used in GI disorders?

A
  • Can be used in treatment of traveler’s diarrhea and other mild conditions of hypermotility
  • Usually combined with an opioid antidiarrheal drug to prevent over use
47
Q

What muscarinic receptor is targeted for reduction of urinary frequency?

A
  • M3
  • Darifenacin, Solifenacin, Tolterodine select for M3 & have a long half life and lower incidence of xerostomia and constipation
48
Q

Contraindications of mAChR antagonists?

A
  • glaucoma
  • caution in elderly men with prostatic hyperplasia
  • atropine should be avoided with acid peptic disease
49
Q

MOA for ganglion blocking drugs?

A
  • competitvely block ACh and similar agonists at the nAChR of parasymp and symp autonomic ganglia
50
Q

How do ganglion blockers impact cardiovascular, GI, GU and eye?

A
  • decrease contractility and moderate tachycardia of heart bc SA node is dominated by PSNS
  • reduce secretion and inhibit motility of GI
  • Urination hesitancy and retention, possible prevention of ejaculation and erection
  • dilation of pupil bc PSNS usually dominates
51
Q

What ganglion blocker is approved for treatment of HTN?

A

Mecamylamine

CPR 2 Exam 1 (21 decks)

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