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