Cholinomimetic agents

Question 1

• Clinical applications:
  
  • postoperative ileus, neurogenic ileus, and urinary retention
• Action:
  
  • Activates bowel and bladder smooth muscle; resistant to AChE
• ID the drug
• direct/indirect agonists

Answer 1

• Bethanechol
• direct agonist

Question 2

• Clincial applications:
  
  • Glaucoma, pupillary constriciton, and relief of intraocular pressure
• Action:
  
  • Carbone copy of acetylcholine
• ID the drug
• direct/indirect agonists

Answer 2

• Carbachol
• Direct agonist

Question 3

• Clincial applications:
  
  • potent stimulator of sweat and tears, and saliva,
  • open angle and closed angle glaucoma
• Action:
  
  • contracts ciliary muscle of eye (open angle glaucoma)
  • pupillary sphincter (closed angle glaucoma)
  • resistant to AChE
• ID the drug
• direct/indirect agonists

​’you cry drool and sweat in your pillow’

Answer 3

• Pilocarpine
• Direct agonist

Question 4

• Clincial applications:
  
  • Challenge test for diagnosis of asthma
• Action:
  
  • Stimulates muscarinic receptors in airway when inhaled
• ID the drug
• direct/indirect agonists

Answer 4

• Methacholine**
• Direct agonist

Question 5

• Clincial applications:
  
  • Popstoperative and neurogenic ileus adn urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postperative)
• Action:
  
  • inc endogenous ACh
  • Neo CNS=No CNS penetration
• ID the drug
• direct/indirect agonists

Answer 5

• Neostigmine
• indirect agonists (anticholinesterase)

Question 6

• Clincial applications:
  
  • Myasthenia gravis (long acting)
  • doesnt penetrate CNS
• Action:
  
  • inc endogenous ACh
  • inc strength
• ID the drug
• direct/indirect agonists

Answer 6

• Pyridostigmine
• indirect agonist (anticholineasterases)

Question 7

• Clincial applications:
  
  • Anticholinergic toxicity (crosses blood brain barrier–> CNS
• Action:
  
  • inc endogenous ACh
  • phyxes atropine overdose
• ID the drug
• direct/indirect agonists

Answer 7

• Physostigmine
• indirect agonists (anticholinesterases)

Question 8

• Clincial applications:
  
  • Alzheimer disease
• Action:
  
  • Inc endogenous ACh
• ID the drug
• direct/indirect agonists

Answer 8

• Donepezil, rivastigmine, galantamine
• indirect agonists (anticholinersterases)

Question 9

• Clincial applications:
  
  • Historically, diagnosis of myasthenia gravis (extremely short acting),
  • myasthenia gravis now diagnosised by anti-AChR (anti-acetylcholine receptor antibody) test
• Action:
  
  • inc endogenous ACh
• ID the drug
• direct/indirect agonists

Answer 9

• Edrophonium
• indirect agonists (anticholinesterases)

Question 10

With all cholinomimetic agents watch out for exacerbation of what 3 diseases?

Answer 10

COPD, asthma, and peptic ulcers

Question 11

Cholinesterase inhibitor poisoning

is often due to organophosphates, such as parathion, that irreversibly inhibit AChE.

Define DUMBBELSS

Answer 11

• Biarrhea, Urinariton , Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimatino, sweating, and salivation

Question 12

What is used to treat Anticholinesterases poisoning?

2 drugs

Answer 12

• Atorpine (competitive inhibitor)
• Pralidoxime (2-PAM) regenerates AChE if given early)

Question 13

• Drugs
  
  • Atropine, homatropine, tropicamide
• What organ system
• Applications

Answer 13

• Eye
• Produce mydriaisis and cycloplegia

Question 14

• Drugs
  
  • Benztropine
• What organ system
• Applications

Answer 14

• CNS
• parkinson disease- park my benz!

Question 15

• Drugs
  
  • Scopolamine
• What organ system
• Applications

Answer 15

• CNS
• Motion sickness

Question 16

• Drugs
  
  • Ipratropium, tiotropium
• What organ system
• Applications

Answer 16

• Respiratory
• COPD, asthma (I pray I can breathe soon!)

Question 17

• Drugs
  
  • Oxybutynin, Darifenacin, Solifenacin
• What organ system
• Applications

Answer 17

• Genitourinary
• Reduce urgency in mild cystits and reduce bladder spasms
  
  • Other agents: tolterodine, fesoterodine, trospium

Question 18

• Drugs
  
  • Glycopyrrolate
• What organ system
• Applications
  
  • parenteral
  • oral

Answer 18

• GI, respiratory
• Applications
  
  • Parenteral: preoperative use to reduce airawy secretions
  • Oral: drooling, peptic ulcer

Question 19

Atropine

• general
• organs (actions)
  
  • eye
  • airway
  • stomach
  • gut
  • gladder

Answer 19

• general
  
  • muscarininc antagonist
  • used to treat bradycardia and for ophthalmic app
• organs (actions)
  
  • eye: pupil dilation, cycloplegia
  • airway: dec secretions
  • stomach: dec acid secretion
  • gut: dec motility
  • gladder: dec urgency in cystitis

Question 20

Atropine

• toxicity
  
  • inc body temp (due to dec sweating),
  • rapid pulse, dry mouth, dry flushed skin, cycloplegia, constipation, disorientation
• **causes what **
  
  • ​in elderly
  • men with prostatic hyperplasia
  • in infants

Answer 20

• _{<strong>Elderly</strong>: Angle-closure glaucoma (due to mydriasis)}
• _{<strong>men w/PHP</strong>: Urinary retention}
• _{<strong>Infants</strong>: Hyperthermia}

Question 21

Atropine

• Side effects
• Jimson weed (datura)

Answer 21

Atropine

• SE:
  
  • hot as a hare
  • dry as a bone
  • red as a beet
  • blind as a bat
  • mad as a hatter
• Jimson Weed (Datura)
  
  • gardeners pupil (mydriasis due to plant alkaloids)