Cholinergic/anti-cholinergic

Question 0

Varenicline

Answer 0

• Mech: partial Nicotinic agonist.
• Uses: smoking cessation
• PK: 12 hr duration
• Tox: HTN, sweating, sensory disturbance, diarrhea, polyuria, menstrual probs.

Question 1

Pilocarpine

Answer 1

• Mech: M receptor agonist, inc. IP3 and DAG
• Uses: Sjogrens (to inc. salivation), glaucoma (to causes miosis b/c dilitation makes glaucoma worse).
• PK: topically active in eye
• Tox/Int: all parasympatholytic effects. May cause vasoconstriction via ganglionic effect.
• resistant to AChE
• “you cry, drool, sweat on you PILOw”

Question 2

Nicotine

Answer 2

• Mech: direct nicotinic agonist
• Uses: smoking cessation
• PK: absorbed by all routes, usually gum or transdermal patch. 4-6hr duration.
• Tox/Int: general ganglionic stim: HTN, tachy, nausea, vomiting, diarrhea.

Question 3

SuccinylCholine

Answer 3

• Mech: N agonist, mildl selective for Nm receptor (NMJ).
• Uses: Muscle relaxation (prod. sustained depol and prevents muscle contraction).
• PK: Highly polar, given as IV. (polar things can’t be readily absorbed in the guy
• Tox: initial muscle spasms and post-op pain. Prolonged action in people w/abnormal butyrylcholinesterase.

Question 4

Muscarine

Answer 4

• Mech: same as bethanechol.
• Uses: found in mushrooms
• PK: readyily absorbed from gut
• Tox/Int: fast-onset mushroom poisoning

Question 5

Pyridostigmine

Answer 5

• Mech: AChE-inhibitor. Carbamate.
• Uses: treatment of myasthenia
• PK: orally active. 4-8 hr duration
• Tox: Like edrophonium but longer
• “pyRIDostiGMine gets RID of MG (myasthenia gravis).”

Question 6

Edrophonium

Answer 6

• Mech: indirect-acting, alcohol. AChE-inhibitor.
• Uses: Reversal of Nm block by nondepolarizing drugs. *Diagnosis of myasthenia gravis.
• PK: highly polar, used in IV. 5-10min duration. does NOT enter CNS.
• Tox: inc. para effects, esp nausea, vomiting, diarrhea, urinary urgency.

Question 8

Parathion

Answer 8

• Mech: Organophosphate. AChE-inhib.
• Uses: insecticide, days to weeks.
• PK: highly lipid soluble
• Tox: all para effects plus muscle paralysis and coma

Question 9

BethaneCHOL

Answer 9

• Mech: Direct-acting, activates M, inc. IP3 and DAG
• Uses: bladder and bowel atony (ie. after surgery or spinal cord injury)
• PK: does NOT enter CNS
• Tox/Int: all parasympatholytic actions (cyclospasm, diarrhea, urinary urgency, vasodil., reflex tachy, sweating.
• resistant to AChE
• “BETHany, CALL, me if you want to activate your bowels and bladder.”

Question 10

Rivastigmine, donepezil, galantamine

Answer 10

• Mech: AChE-inhib
• Uses: Alzheimers
• PK: lipid soluble, enters CNS.
• Tox: nausea, vomitting.

Question 11

Atropine, homatropine, tropicamide

Answer 11

• Mech: nonselective M antagonist.
• Uses: antidote for AChE inhibitor toxicity (too much ACh).
• PK: lipid solube, 2-4hr duration except in eye its >72hr
• tox: all para plus sedation, delirium, HYPERTHERMIA (b/c no sweating), flushing.

Question 12

Darifenacin

Answer 12

• Mech: selective M3 antagonist.
• Uses: treat urinary urgency, incontinence
• PK: oral, 12-24hr duration
• Tox: para effects.

Question 13

Solifenacin

Answer 13

• Mech: selective M3 antagonist.
• Uses: treat urinary urgency, incontinence
• PK: oral, 12-24hr duration
• Tox: para effects.

Question 14

Tolterodine

Answer 14

• Mech: selective M3 antagonist.
• Uses: treat urinary urgency, incontinence
• PK: oral, 12-24hr duration
• Tox: para effects.

Question 15

Pirenzepine

Answer 15

• Mech: selective M1 antagonist
• Uses: Peptic disease
• PK: oral
• Tox: parasympatholytic

Question 16

Neostigmine

Answer 16

• Mech: AChE inhib. Carbamate. also small direct nicotinic agonist.
• Uses: Reversal of Nm block, treatment of Myasthenia.
• PK: orally active. 2-4hr duration.
• Tox: like edrophonium but longer.
• “Neo CNS. No CNS penetration.”

Question 17

Pralidoxime

Answer 17

• Mech: chemical antagonist of organophosphates
• Uses: organophosphate poisoning (too much AChE inhibition)
• PK: parenteral
• Tox: muscle weakness (b/c it regenerates AChE, so too much will give you ACh deficiency).

Question 18

NE

Answer 18

alpha 1, alpha 2, beta 1

• Uses: shock
• PK: like epi, IV only
• Tox: vasospasm, tissue necrosis, excessive BP inc., arrhythmias, infarction

Question 19

Dopamine

Answer 19

All receptors

• Uses: shock (esp. w/renal shutdown), sometimes heart failure.
• PK: like epi, IV only.
• Tox: CV disturbance, arrhythmias

Question 20

Physostigmine

Answer 20

-Mech: AChE inihib. Carbamate
-Uses: reversal of severe Atropine (M antagonist) poisoning.
-PK: lipid soluble. Can be used topically in the eye. 2-4hr duration. Enters CNS.
-Tox: like Edrophonium plus CNS effects like seizures.
(“PHYsostigmine PHYxes atropine overdose”.

Question 21

Phenylephrine

Answer 21

alpha 1 agonist

• Uses: decongestant, mydriatic, neurogenic hypotension
• PK: oral, inhalant, topical, parenteral, 15-60min duration
• Tox: HTN, stroke, MI

Question 22

Albuterol, metaproterenol, terbutaline

Answer 22

Beta-2 agonist

• Uses: prompt onset for acute bronchospasm
• PK: inhalant via aerosol canister, 2-6hr duration
• Tox: tachy, tremor.

Question 23

Amphetamine, methamphetamine

Answer 23

displaced stored catecholamines from nerve endings.

• Uses: anorexiant, ADHD, narcolepsy.
• PK: oral and parenteral. >4-6hr duration
• Tox: addiction, paranoia, aggression, insomnia, HTN

Question 24

Telenzepine

Answer 24

• Mech: selective M1 antagonist
• Uses: Peptic disease
• PK: oral
• Tox: parasympatholytic

Question 25

Fesoterodine

Answer 25

- Mech: selective M3 antagonist. - Uses: treat urinary urgency, incontinence - PK: oral, 12-24hr duration - Tox: para effects.

Question 25

Epinephrine

Answer 25

All receptors - Uses: anaphylaxis, hemostatic, cardiac arrest. - PK: parenteral and topical only, does NOT enter CNS. short duration - Tox: HTN, arrhythmia, stroke, MI, pulm edema.

Question 26

Cocaine

Answer 26

Blocks NE reuptake via NET and dopamine reuptake via DAT - Uses: local anesthetic w/instrinsic homeostatic action. - PK: parenteral only. 2 hr duration - Tox: addiction, HTN, arrhythmias, seizures

Question 27

Tyramine

Answer 27

Displaces stored catecholamines - Uses: no clinical use, found in fermented foods. - PK: high first-pass effect, but in pts on MAO inhibitors, it is absorbed.

Question 28

Dobutamine

Answer 28

beta-1 agonist

Question 29

Isoproterenol

Answer 29

beta-agonist

Question 30

Clonidine

Answer 30

alpha-2 agonist

Question 31

phenylephrine

Answer 31

alpha-1 agonist

Question 32

Carbachol

Answer 32

M agonist. | -Glaucoma treatment (miosis helps w/narrow-angle glaucoma)

Question 33

Methacholine

Answer 33

M agonist - Challenge test for asthma. - bronchoconstrictor, M3 in lungs. - Short half life, metabolized by AChE.

Question 34

Donepezil, rivastigmine, galantamine

Answer 34

AChE inhibitors. | -Alzheimers treatment

Question 35

Benztropine

Answer 35

M antagonist - CNS - Parkinsons "Park my Benz"

Question 36

Scopolamine

Answer 36

M antagonist - CNS - Motion sickness - can cause anterograde amnesia

Question 37

Ipratropium, tiotropium

Answer 37

M antagonist - Respiratory. - treats COPD, asthma - "i PRA i can breathe soon"

Question 38

Oxybutynin, darifenacin, solifenacin

Answer 38

M antagonist - genitourinary - Reduces urgency/bladder spasms.

Question 39

Glycopyrrolate

Answer 39

M antagonist - GI, respiratory - Parenteral. Pre-op to reduce airway secretions. - also for drooling and peptic ulcer.

Question 40

alpha-methyldopa

Answer 40

alpha2-agonist

Question 41

Phenoxybenzamine

Answer 41

irreversible alpha-blocker | -Used in pheochromocytoma to prevent hypertensive crisis

Question 42

Phentolamine

Answer 42

reversible alpha-blocker | -give to pts on MAO inhibitors who eat tyramine-containing foods.

Question 43

Prazosin, terazosin, doxazosin, tamsulosin

Answer 43

alpha1-blockers | -treats urinary symptoms in BPH

Question 44

Mirtazapine

Answer 44

alpha2-blocker | -used in depression.

Question 45

hexamethonium

Answer 45

ganglion blocker.