Cholinergic/anti-cholinergic Flashcards
0
Q
Varenicline
A
- Mech: partial Nicotinic agonist.
- Uses: smoking cessation
- PK: 12 hr duration
- Tox: HTN, sweating, sensory disturbance, diarrhea, polyuria, menstrual probs.
1
Q
Pilocarpine
A
- 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”
2
Q
Nicotine
A
- 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.
3
Q
SuccinylCholine
A
- 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.
4
Q
Muscarine
A
- Mech: same as bethanechol.
- Uses: found in mushrooms
- PK: readyily absorbed from gut
- Tox/Int: fast-onset mushroom poisoning
5
Q
Pyridostigmine
A
- 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).”
6
Q
Edrophonium
A
- 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.
8
Q
Parathion
A
- Mech: Organophosphate. AChE-inhib.
- Uses: insecticide, days to weeks.
- PK: highly lipid soluble
- Tox: all para effects plus muscle paralysis and coma
9
Q
BethaneCHOL
A
- 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.”
10
Q
Rivastigmine, donepezil, galantamine
A
- Mech: AChE-inhib
- Uses: Alzheimers
- PK: lipid soluble, enters CNS.
- Tox: nausea, vomitting.
11
Q
Atropine, homatropine, tropicamide
A
- 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.
12
Q
Darifenacin
A
- Mech: selective M3 antagonist.
- Uses: treat urinary urgency, incontinence
- PK: oral, 12-24hr duration
- Tox: para effects.
13
Q
Solifenacin
A
- Mech: selective M3 antagonist.
- Uses: treat urinary urgency, incontinence
- PK: oral, 12-24hr duration
- Tox: para effects.
14
Q
Tolterodine
A
- Mech: selective M3 antagonist.
- Uses: treat urinary urgency, incontinence
- PK: oral, 12-24hr duration
- Tox: para effects.
15
Q
Pirenzepine
A
- Mech: selective M1 antagonist
- Uses: Peptic disease
- PK: oral
- Tox: parasympatholytic
16
Q
Neostigmine
A
- 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.”
17
Q
Pralidoxime
A
- 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).
18
Q
NE
A
alpha 1, alpha 2, beta 1
- Uses: shock
- PK: like epi, IV only
- Tox: vasospasm, tissue necrosis, excessive BP inc., arrhythmias, infarction
