Cholinergic/anti-cholinergic Flashcards
Varenicline
- Mech: partial Nicotinic agonist.
- Uses: smoking cessation
- PK: 12 hr duration
- Tox: HTN, sweating, sensory disturbance, diarrhea, polyuria, menstrual probs.
Pilocarpine
- 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”
Nicotine
- 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.
SuccinylCholine
- 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.
Muscarine
- Mech: same as bethanechol.
- Uses: found in mushrooms
- PK: readyily absorbed from gut
- Tox/Int: fast-onset mushroom poisoning
Pyridostigmine
- 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).”
Edrophonium
- 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.
Parathion
- Mech: Organophosphate. AChE-inhib.
- Uses: insecticide, days to weeks.
- PK: highly lipid soluble
- Tox: all para effects plus muscle paralysis and coma
BethaneCHOL
- 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.”
Rivastigmine, donepezil, galantamine
- Mech: AChE-inhib
- Uses: Alzheimers
- PK: lipid soluble, enters CNS.
- Tox: nausea, vomitting.
Atropine, homatropine, tropicamide
- 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.
Darifenacin
- Mech: selective M3 antagonist.
- Uses: treat urinary urgency, incontinence
- PK: oral, 12-24hr duration
- Tox: para effects.
Solifenacin
- Mech: selective M3 antagonist.
- Uses: treat urinary urgency, incontinence
- PK: oral, 12-24hr duration
- Tox: para effects.
Tolterodine
- Mech: selective M3 antagonist.
- Uses: treat urinary urgency, incontinence
- PK: oral, 12-24hr duration
- Tox: para effects.
Pirenzepine
- Mech: selective M1 antagonist
- Uses: Peptic disease
- PK: oral
- Tox: parasympatholytic
Neostigmine
- 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.”
Pralidoxime
- 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).
NE
alpha 1, alpha 2, beta 1
- Uses: shock
- PK: like epi, IV only
- Tox: vasospasm, tissue necrosis, excessive BP inc., arrhythmias, infarction
Dopamine
All receptors
- Uses: shock (esp. w/renal shutdown), sometimes heart failure.
- PK: like epi, IV only.
- Tox: CV disturbance, arrhythmias
Physostigmine
-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”.
Phenylephrine
alpha 1 agonist
- Uses: decongestant, mydriatic, neurogenic hypotension
- PK: oral, inhalant, topical, parenteral, 15-60min duration
- Tox: HTN, stroke, MI
Albuterol, metaproterenol, terbutaline
Beta-2 agonist
- Uses: prompt onset for acute bronchospasm
- PK: inhalant via aerosol canister, 2-6hr duration
- Tox: tachy, tremor.
Amphetamine, methamphetamine
displaced stored catecholamines from nerve endings.
- Uses: anorexiant, ADHD, narcolepsy.
- PK: oral and parenteral. >4-6hr duration
- Tox: addiction, paranoia, aggression, insomnia, HTN
Telenzepine
- Mech: selective M1 antagonist
- Uses: Peptic disease
- PK: oral
- Tox: parasympatholytic
Fesoterodine
- Mech: selective M3 antagonist.
- Uses: treat urinary urgency, incontinence
- PK: oral, 12-24hr duration
- Tox: para effects.
Epinephrine
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.
Cocaine
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
Tyramine
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.
Dobutamine
beta-1 agonist
Isoproterenol
beta-agonist
Clonidine
alpha-2 agonist
phenylephrine
alpha-1 agonist
Carbachol
M agonist.
-Glaucoma treatment (miosis helps w/narrow-angle glaucoma)
Methacholine
M agonist
- Challenge test for asthma.
- bronchoconstrictor, M3 in lungs.
- Short half life, metabolized by AChE.
Donepezil, rivastigmine, galantamine
AChE inhibitors.
-Alzheimers treatment
Benztropine
M antagonist
- CNS
- Parkinsons “Park my Benz”
Scopolamine
M antagonist
- CNS
- Motion sickness
- can cause anterograde amnesia
Ipratropium, tiotropium
M antagonist
- Respiratory.
- treats COPD, asthma
- “i PRA i can breathe soon”
Oxybutynin, darifenacin, solifenacin
M antagonist
- genitourinary
- Reduces urgency/bladder spasms.
Glycopyrrolate
M antagonist
- GI, respiratory
- Parenteral. Pre-op to reduce airway secretions.
- also for drooling and peptic ulcer.
alpha-methyldopa
alpha2-agonist
Phenoxybenzamine
irreversible alpha-blocker
-Used in pheochromocytoma to prevent hypertensive crisis
Phentolamine
reversible alpha-blocker
-give to pts on MAO inhibitors who eat tyramine-containing foods.
Prazosin, terazosin, doxazosin, tamsulosin
alpha1-blockers
-treats urinary symptoms in BPH
Mirtazapine
alpha2-blocker
-used in depression.
hexamethonium
ganglion blocker.
