Cholinergics

Question 1

What direct cholinergic agonists are sensitive to cholinesterase

Answer 1

Acetylcholine ++++, methacoline +

Question 2

What drugs are direct pure mAChR agonists

Answer 2

Methacoline, bethanechol, pilocarpine

Question 3

What direct cholinergic agonists can cross the membrane

Answer 3

Alkaloids

Question 4

What direct cholinergic agonists are used to cause miosis in intraocular surgery

Answer 4

ACh, carbachol, pilocarpine

Question 5

What direct cholinergic agonists is used to treat urinary retention

Answer 5

Bethanechol

Question 6

What direct cholinergic agonist is used to treat heart burn

Answer 6

Bethanechol

Question 7

What direct cholinergic agonists are used to treat glaucoma

Answer 7

Carbachol, pilocarpine

Question 8

What direct cholinergic agonists is used to treat sjogrens/xerostomia

Answer 8

Pilocarpine

Question 9

What direct cholinergic agonist is used to treat smoking

Answer 9

Varenicline

Question 10

What are the side effects of varenicline

Answer 10

Nausea, neuropsychiatric

Question 11

What are the symptoms of a muscarinic toxicity

Answer 11

Sludge. Salivation, lacrimation, urination, defecation, GI, emesis

Question 12

What are the contraindications for direct cholinergic agonists

Answer 12

Asthma, hyperthyroidism, coronary insufficiency, acid peptic disease

Question 13

What are the symptoms of nicotinic toxicity

Answer 13

CNS stimulation, skeletal m end plate depolarization, respiratory paralysis, hypertension, Arrhythmias

Question 14

Tx for nicotinic toxicity

Answer 14

Atropine and diazepam

Question 15

What are the 3 types of AChE inhibitors and what about their binding

Answer 15

Alcohols - reversible
Carbamic acid esters - reversible and longer lasting
Organophosphates - irreversible

Question 16

What are the charged AChE inhibitors

Answer 16

Edrophonium, pyridostigmine, neostigmine, echothiophate, ambenonium

Question 17

What are the neutral AChE inhibitors

Answer 17

Physostigmine, donepezil, galantamine, rivastigmine, tacrine

Question 18

What are the uses for AChE inhibitors

Answer 18

Glaucoma, dementia, antidote to anticholinergics, reversal of neuromuscular paralysis, myasthenia gravis

Question 19

What can cause anticholinergics poisoning

Answer 19

Atropine, antihistamine, TCAs, sleep aids, cold preparations

Question 20

What are the symptoms of anticholinergics poisoning

Answer 20

Cutaneous vasodilation, anhidrosis, anhydrotic HTN, nonreactive mydriasis, delirium, hallucinations, reduced desire to urinate

Question 21

What are the symptoms of AChE inhibitor poisoning

Answer 21

Sludge plus muscle fasciculations

Question 22

Treatment for AChE inhibitor toxicity

Answer 22

Atropine and pralidoxine

Question 23

Do choline esters cross membranes? Why?

Answer 23

No because they are permanently charged

Question 24

Drugs used for cholinergic poisoning?

Answer 24

Atropine + pralidoxine

Question 25

What are the anticholinergics used to treat parkinson disease

Answer 25

Tertiary amines - benzotropine, trihexyphenidyl, and procyclidine. This is used in combination with dopaminergic therapy.

Question 26

What is the anticholinergic used to treat motion sickness

Answer 26

Scopolamine - PO,injection, transdermal

Question 27

What are the role of anticholinergics in anesthesia? Ex?

Answer 27

Atropine is given to block responses to vagal reflexes induced by surgical manipulation of viscera. Atropine or glycopryrrolate is paired with the cholinesterase inhibitor neostigmine to block its parasympathetic effects

Question 28

What anticholinergics are used to prevent synechia formation in uveitis and irits (iris adhering to lens or cornea)?

Answer 28

Homatropine or atropine

Question 28

What anticholinergics are used to treat asthma and COPD?

Answer 28

Ipratropium and tiotropium

Question 28

What mAChR antagonists are used to treat GI hypermotility?

Answer 28

Lomotil - combination of atropine and diphenoxylate

Question 29

What specific receptor is targeted for symptomatic relief in Tx of urinary urgency

Answer 29

M3

Question 30

What are the selective M3 antagonists?

Answer 30

Oxybutynin, darifenacin, solifenacin, and tolterodine

Question 31

What are the side effects of oxybutynin

Answer 31

dry mouth/eyes, dizziness, constipation, blurred vision

Question 32

What are the adverse effects of antimuscarinic agents used to reduce GI secretion

Answer 32

Mydriasis (pupillary dilation) & cycloplega (paralysis of ciliary m - loss of accomodation)

Question 33

What are the contraindications for anticholinergics?

Answer 33

Glaucoma, prostatic hyperplasiam acid-peptic disease

Question 34

What are the symptoms of anticholinergic overdose?

Answer 34

Dry as a bone, blind as a bat, red as a beet, mad as a hatter, hot as a hare. Tx with AChE inhibitors