Cholinergic Drugs

Front 1

What is the prototype drug of non-polarizing nicotinic blockers?
What is its therapeutic effect?
What are its side effects?

Back 1

d-Tubocurarine
competitive antagonism of nicotinic receptors leading to flaccid paralysis
hypotension, bronchospasm from histamine release

Front 2

What type of drug is atracurium?
What population is it useful in treating and why?

Back 2

Non-depolarizing nicotinic blocker
Patients with impaired hepatic or kidney function
Hoffman elimination

Front 3

What is characteristic of Hoffman elimination?

Back 3

Temperature and pH dependent
Independent of hepatic and renal function.

Front 4

What is the benefit of using cisatracurium (new, stereoisomer) over atracurium?

Back 4

Less histamine release (side effect that causes bronchospasm)

Front 5

What rapid onset, non-depolarizing nicotinic blocker may be used before intubation?

Back 5

Rocuronium

Front 6

What is the prototype depolarizing nicotinic blocker?
What is its intended effect?
What is the major side effect of this drug type?

Back 6

Succinylcholine
flaccid paralysis, short acting
fasciculations with pain

Front 7

What is given to reduce the effects of succinylcholine?

Back 7

pseudocholinesterase from healthy plasma

Front 8

Succinylcholine works by depolarizing and blocking nicotinic receptors (ganglionic blockade) but also causes bradycardia and increased bronchial secretions via these receptors

Back 8

muscarinic (this is unique to succinylcholine among depolarizing nicotinic blockers)

Front 9

Botulinim toxin is a poison that can be used therapeutically. What is its mechanism?

Back 9

Blocks acetylcholine release from presynaptic neuron.

Front 10

How is non-depolarizing NMJ blockade reversed?

Back 10

Atropine then Anti-cholinesterase (neostigmine)

Front 11

What are the characteristics of the muscarinic subtypes: M1, M2, and M3?

Back 11

M1: Neural, mostly excitatory

M2: Heart, inhibitory

M3: Smooth muscle and glands

Front 12

What type of receptor is muscarinic? nicotinic?

Which responds more quickly?

Back 12

Muscarinic = G-protein

Nicotinic = ligand-gated ion channel (quicker)

Front 13

What affects are seen at the organs with muscarinic stimulation?

Back 13

Eyes: sphincter contraction (miosis), ciliary contraction (near vision)

Heart: HR slows, decreased contractility
Blood vessels: some vasodilation

Lungs: bronchoconstriction, secretions

GI: increased motility, relaxed sphincters, secretion
Gall Bladder: contraction

Pancreatic acini: secretion

Bladder: detrusor contraction, sphincter relax
Penis: erection

Skin: sweating (sympathetic)

Glands (salivary, lacrimal, nasopharyngeal: secretion

Front 14

Why is it ineffective to give acetylcholine to a pt?

Back 14

Pseudocholinesterase is present in the plasma and hydrolyzes acetylcholine

Front 15

Acetylcholine action is terminated by hydrolysis into acetic acid and choline. How is this accomplished and where do these mechanisms take place?

Back 15

Acetylcholinesterase: neurons, NMJ, CNS, RBC

Pseudocholinesterase: plasma, glial cells, liver

Front 16

What type of drug is bethanechol, and why is it useful?

Back 16

Cholinomimetic, choline ester, quaternary, muscarinic agonist

To increase GI motility and increase bladder function

Front 17

Pilocarpine, Muscarine, and Nicotine are naturally occurring and contain nitrogen. What type of drug are they?

Back 17

Cholinomimetic alkaloids

Front 18

An elderly woman is experiencing xerostomia and has glaucoma. What drug might be used to treat both of these?

Back 18

Pilocarpine (orally, eye drops) (tertiary alkaloid)

Front 19

What is the difference between tertiary and quaternary amine drugs?

Back 19

Tertiary: nonpolar, lipid soluble. Absorbed enterally, crosses BBB

Quaternary: polar, not absorbed enterally, cannot cross BBB, absorbed intravenously

Front 20

What type of drugs are "-stigmines"?

Which of the following drugs is quaternary? Which of these can cross the BBB?
Which of these is used to treat Alzheimer's?

Physostigmine, Rivastigmine, Neostigmine

Back 20

Indirect cholinomimetics, anticholinesterases

1. Neostigmine

2. Physostigmine, Rivastigmine
3. Rivastigmine

Front 21

What is ectothiophate?

Back 21

Irreversible anticholinesterase. Used in medicated eyedrops for long-acting miotic activity.

Front 22

Why are the insecticide malathion and Sarin gas so dangerous?

Back 22

They are absorbed through the skin and can lead to irreversible anticholinesterase activity if "aging" of the phosphate bond occurs.

Front 23

A patient has come into contact with a toxic amount of pesticides. What measures should be taken?

Back 23

1. Remove clothing to avoid further contamination

2. Give atropine parenterally to block muscarinic activity

3. Maintain respiration with ventilation as necessary
4. Pralidoxime can be given to reactive cholinesterases if aging has not had time to occur. Benzodiazepines can be given for seizures.

Front 24

What cholinergic drug could be used to treat Myasthenia Gravis?

Back 24

Neostigmine (increases acetylcholine availability)

Front 25

What drug could be given for relief of atropine poisoning or tricyclic antidepressent affects?

Back 25

Physostigmine (indirect cholinomimetic, crosses BBB)

Front 26

In preparation for chemical warfare, what drug can be given to soldiers to resist the affects of Sarin gas or other organophosphate poisoning?
What may have been the result of doing this too frequently?

Back 26

Pyridostigmine is a short-acting anticholinesterase. While this seems counter-intuitive, it is helpful in keeping the dangerous irreversible organophosphates from binding up all the cholinesterase.

Gulf War Syndrome

Front 27

What are the three categories of antimuscarinics? Try to name a drug in each category.

Back 27

alkaloids: atropine, scopolamine
ipratropium (quaternary, for COPD)

semi-synthetics: homatropine

synthetics: dicyclomine (bowel spasm), tropicamide (used to produce mydriasis), benztropine and trihexyphenidyl (Parkinson's)

Front 28

What is the mechanism of atropine?

What affects gave its plant derivative the name Belladonna?

Back 28

competitive antagonist of acetylcholine at muscarinic receptor selectively

dilated pupils, blurred vision

Front 29

How would a patient with atropine poisoning present?

Back 29

Flushed, dry skin

Elevated temperature
Thirsty, dry mouth
Blurred vision, photophobia

Palpitations

Restless, Hallucinogenic

Front 30

Lomotil contains atropine and has a use that his reflected in its name. What is it?

Back 30

Treatment of diarrhea

Front 31

Atropine has a spectrum of dose-dependent affects. See flip side for review.

Back 31

In low dose, some drying of secretions

In mid dose, dry mouth, pupil dilation, tachycardia/palpitations may occur

In toxic dose, CNS affects, difficulty speaking, swallowing, urininating

Front 32

What antimuscarinic drug can be used as a CNS depressant or an anti-emetic depending on the dose?

Back 32

Scopolamine

Front 33

What is the use of the antimuscarinic drugs ipratropium and tiotropium?

Back 33

To induce bronchodilation in patients with asthma or COPD

Front 34

Oxybutinin, Solifenacin, Tolteridine are antimuscarinics turn down for what?

Back 34

To turn down urinary frequency, urgency

Front 35

What drug can be used to treat all of the following: hypersalivation, hyperhidrosis, bradycardia, heart block, muscarine poisoning, organophosphate poisoning?

Back 35

Atropine

Front 36

What is the short acting version of atropine that is used at the eye doctor to dilate your eye?

Back 36

Tropicamide

Front 37

Oh no, a patient has IBS or diverticulitis. What antimuscarinic drug that you memorized and forgot since medical school might you give them?

Back 37

Dicyclomine

Front 38

A resident at UF has given a patient a toxic amount of atropine. What can you give to correct their mistake? (1. Ideal drug, 2. Commonly used)

Back 38

1. Physostigmine (tertiary, crosses BBB)

2. Neostigmine in combination with Benzodiazepine