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84 Cards in this Set

  • Front
  • Back
M1 Receptor Locations
Ganglia
Enteric
Nerves
M2 Receptor Locations
Smooth muscle
Heart
Nerves
M3 Receptor Locations
Smooth muscle
Parietal
Endothelium
Glands
NM Receptor Locations
NMJ
NN Receptor Locations
Postganglionic cell bodies
Varicosities
Hemicholinium MOA
Inactivates Na+ Choline symporter in cholinergic neuron
Vesamicol MOA
Inactivates ACh transport into vesicle through ACh H+ antiporter
Botulinum toxin MOA
Inhibits presynaptic fusion of vesicle
Reserpine MOA
Inhibits VMAT (dopamine H+ antiporter) from allowing dopamine into a vesicle where it is altered to form NE
Name the two sympathetic muscarinic receptors and the location
M4 that relaxes skeletal muscle vessels
M that increases thermoregulatory effects of sweat glands
Direct acting cholinergic agonists
Acetylcholine
Bethanechol
Methacholine
Carbachol
Pilocarpine
Muscarine
Nicotine
Cevimeline
Indirect acting Reversible cholinergic agonists
Edrophonium
Neostigmine
Physostigmine
Pyridostigmine
Indirect acting Irreversible cholinergic agonists
Nerve gases
Organophosphates
Ecothiophate
Isoflurophate
Esters of direct acting cholinergic agonists
Acetylcholine
Methacholine (M only)
Carbachol (not broken down by cholinesterase)
Bethanechol (M only) (not broken down by cholinesterase)
Alkaloids of direct acting cholinergic agonists
Muscarine
Pilocarpine
Nicotine
(Kidney excretion)
Tertiary direct acting cholinergic agonists
Pilocarpine
Nicotine
Acetylcholine:
Specificity
Breakdown
Therapeutic effect
NM
AChE hydrolyzed
parasympathetic and sympathetic
Bethanecol:
Specificity
Breakdown
Therapeutic effect
Mn
Not readily hydrolyzed
GI/bladder motility in atony or in neurogenic bladder
Bethanecol side effects
Sweating
Urinary urgency
Diarrhea
Decreased BP & HR
Nausea
Abdominal Pain
Bronchoconstriction & spasms
Increased salivation & lacrimation
Bethanechol contraindications
Asthma patients
Methacholine:
Specificity
Breakdown
Therapeutic effect
Mn
Less hydrolyzed by AChE
Methacholine challen test (for asthma)
Carbachol:
Specificity
Breakdown
Therapeutic effect
Nm
Not hydrolyzed by AChE
Miosis of iris & glaucoma
Pilocarpine:
Specificity
Breakdown
Therapeutic effect
M
Not hydrolyzed by AChE
Miosis of iris, dec intra-ocular pressure, blurred vision
Cevimeline:
Specificity
Breakdown
Therapeutic effect
M1 & M3
Xerostomia in Sjogren's, antineoplastic agents, neck radiation, aging
Glaucoma Treatment
Carbachol
Pilocarpine
Postoperative GI Atony Treatment
Bethanechol
Neurogenic Bladder Treatment
Bethanechol
Dry Mouth Treatment
Cevimeline
Bronchoprovocation Challenge Treatment
Methacholine
Physostigmine Use
Reversible indirect cholinergic agonist
Glaucoma
Induce tone in bladder and GI after surgery or postpartum
Antidote to Atropine poisoning
Counteract dextromethorphan use (crosses BBB)
Neostigmine Use
Reversible indirect cholinergic agonist
Antidote to Tubocurarine poisoning
Myasthenia gravis
Xerostomia
Induce tone in bladder and GI
Edrophonium Use
Reversible indirect cholinergic agonist (Stigmine)
Diagnosis for myasthenia gravis
Parathion Use
Irrevversible organophosphate cholinergic agonist
Insecticides
Crosses BBB
Penetrates skin & mucous membranes
Malathion - head lice treatment
Isoflurophate (DFP)
Irreversible organophosphate cholinergic agonist
Glaucoma
Echothiophate longer half life
Penetrate skin & mucous membrane
Stigmine MOA of inhibiting AChE
Carbamoylate enzyme
Organophosphate MOA of inhibiting AChE
Phosphorylates and "ages" enzyme
Antidotes to Organophoshate phosphorylation of AChE
Pralidoxime (2-PAM)
Atropine (MARK I kit)
Scopolamine
Prophylaxis for organophosphates
Pyridostigmine Bromide
Myasthenia gravis treatment
Edrophonium (diagnostic)
Neostigmine
Pyridostigmine (longer acting w/ fewer GI side effects)
Paralytic ileus
Neostigmine
Physostigmine
Glaucoma Treatment
Echothiophate
Physostigmine
Bladder atony
Neostigmine
Physostigmine
Atropine poisoning antidote
Physostigmine
Reversal agent for NMJ blockers (curare-like)
Edrophonium
Atropine Chemistry
Naturally Occuring
Antimuscarinic
Alkaloid ester
Tertiary amine
Skin absorption
BBB
Scopolamine Chemistry
Naturally Occuring
Antimuscarinic
Alkaloid ester
Tertiary amine
Skin absorption
BBB
Tiotropium Chemistry
Antimuscarinic
Quaternary amine
Tiotropium Use
Asthma
COPD
Ipratropium Chemistry
Antimuscarinic
Quaternary amine
Tolterodine Use
Antimuscarinic
Enuresis in overactive bladder
Oxybutynin Use
Antimuscarinic
Enuresis in overactive bladder
M3 blocker
Tolterodine (most bladder exclusive)
Pirenzepine Use
Antimuscarinic
Peptic Ulcers in Europe
M1 ganglionic
Antidiarrheal
Antimuscarinic Uses
Ophthalmology - dilation
Dentistry - dec salivation
Parkinsonism - Offset dec DA and inc choinergic function in basal ganglia/striatum
Sedation - low doses
Amnesia - Hippocampus
Motion sickness - inner ear
ER - mycetism & organophosphate insecticides
IBS or ulcers
COPD & Asthma (Beta 2 agonists better)
Atropine Use
Decrease salivation
Decrease gut motility
Allow urinary retention
Decrease sweating
CNS depression
Dilate bronchioles
Increase HR
"Atropine blush"
Atropine contraindications
Glaucoma patients (increases pressure)
Atropine Side Effects
Restlessness
Hallucinations
Delirium
Coma
Scopolamine Use
Crosses BBB
Sedative
Preanesthetic medication
Motion sickness
Ipratropium Use
Bronchodilator
COPD
Also elevates mucociliary clearance
Motion Sickness Treatment
Scopolamine
Dramamine
Ophthalmoscopic Exam
Atropine
Scopolamine
Asthma or COPD
Ipratropium
Weaken vasovagal attack in response to MI
Atropine
Peptic Ulcer Disease
Pirenzepine
Symptomatic relief of urinary urgency
Oxygutynin
Tolterodine
Relieve bladder spasm after urologic surgery
Oxybutynin
Nicotine Uses
Nicotinic antagonist
Stimulant that increases arousal, attention, and learning
Dependence producing drug
Trimethaphan Use
Competitive blocker of Nicotinic Receptors
Hypotensive agent
Dissecting aortic aneurysm
Controlled hypotension in surgery
Hexamethonium Use
Competitive blocker of nicotinic receptors
Mecamylamine
Non-competitive blocker of nicotinic receptors
NMJ blocker drug interactions
Aminoglycosides (dec ACh release)
Volatile anesthetics (dec signaling)
Depolarizing NMJ Blockers
Succinylcholine
Non-Depolarizing NMJ Blockers
D-tubocurarine
Atracurium
Mivacurium
Pancuronium
Vecuronium
Rocuronium
Curare Use
Non-depolarizing
Competitively blocks ACh receptors
Can be surmounted by AChE inhibitors
Isoquinolines Non-depolarizing NMJ Blockers
Renal excretion & histamine release
Tubocurarine (quaternary can block ganglion)
Atracurium (Hoffman elim)
Mivacurium (AChE degraded)
Steroid Non-depolarizing NMJ Blockers
Hepatic metabolism
Pancuronium (kidney metabolism)
Vecuronium
Rocuronium
Succinylcholine Use & Breakdown
Rapid intubation
Hydrolized by butyrylcholinesterase in liver and plasma
Histamine release through mast cell contraction
Succinylcholine Adverse Effects
Arrhythmias
Hyperthermia
Severe muscle pain
Hyperkalemia
Increased intraocular pressure
Increased risk of emesis (6 pack)
Malignant hyperthermia treatment
Dantrolene
Benzodiazepine Uses
Spasmolytic
Promote GABA
Sleep disorder
MS
Cerebral Palsy
Stroke
Chronic back pain & sprains
Carisoprodol Use
Spasmolytic
Skeletal muscle pain
Cyclobenzaprine Use
Spasmolytic
Skeletal muscle pain
Methocarbamol Use
Spasmolytic
Skeletal muscle pain
Meprobamate Use
Spasmolytic
Skeletal muscle pain
Dantrolene Use
Spasmolytic
Decrease Ca2+ levels