Exam 2 Flashcards
Edrophonium
Reversible cholinesterase inhibitor
Quaternary ammonium compound (doesn’t enter CNS)
Short acting
Tensilon test for myasthenia gravis
Neostigmine
Reversible cholinesterase inhibitor
Quaternary ammonium compound (doesn’t enter CNS)
Long acting
Used in treatments of myasthenia gravis
Pyridostigmine
Reversible cholinesterase inhibitor
Quaternary ammonium compound (doesn’t enter CNS)
Long acting
Used in the treatment of myasthenia gravis
Used by military to protect troops against nerve gas
Physostigmine/eserine
Reversible cholinesterase inhibitor
Non quaternary (can enter CNS)
Used in treatment of antimuscarinic poisoning (atropine)
Parathion
Organophosphate insecticide
Cholinesterase inhibitor
Can be absorbed through skin
Treated with atropine, pralidoxime
Carbaryl
Carbamate insecticide
Cholinesterase inhibitor
Not highly absorbable through skin
Treated with Atropine (pralidoxime not useful)
DFP/Isoflurophate
Irreversible cholinesterase inhibitor
Poisoning treated with atropine and pralidoxime
Has been used in treatment of glaucoma
Sarin
Irreversible cholinesterase inhibitor
Nerve gas
Treated with atropine and pralidoxime
Pralidoxime/2-PAM
Cholinesterase reactivator
Organophosphate antidote (must give within 2 hours)
Doesn’t work for carbamate insecticides
Sildenafil
Phosphodiesterase-5 inhibitor
Inhibition of the breakdown of cGMP causes vasodilation, particularly in the corpus cavernosum where PDE-5 levels are high
Can cause hypotension and reflex tachycardia
Peak plasma levels after 1 hour
Metabolized by CYP3A4
Vardenafil
PDE-5 inhibitor, causes erection
Plasma levels peak at 1 hour
Tadalafil
PDE-5 inhibitor causes erection.
Much longer half life than sidenafil, vardenafil (up to 36 hours)
Botulism toxin
Prevents release of ACh from nerve endings (autonomic and muscular)
Causes paralysis of skeletal muscle with fatal diaphragmatic paralysis
13 Muscarinic Antagonists
Atropine Scopolamine Dicyclomine Propantheline Glycopyrrolate Ipratropium Benztropine Trihexyphenidyl Tolterodine Oxybutynin Fesoterodine Tropicamide
Atropine
Antimuscarinic
Belladonna alkaloid
Scopolamine
Antimuscarinic
Like atropine but with more CNS depression
Treatment for motion sickness, vertigo
Dicyclomine
Nonquaternary Antimuscarinic
Treatment for irritable bowel syndrome (antispasmodic)
Propantheline
Antimuscarinic
Antispasmodic effects on bowel (irritable bowel syndrome)
Quaternary, few CNS effects
Glycopyrrolate
Quaternary Antimuscarinic
No CNS effects
Used in preop by anesthesia to reduce respiratory secretions and inhibit Vagus reflexes.
Ipratropium, Tiatropium
Quaternary Antimuscarinic
Administered by inhalation for asthma and COPD
Tiatropium has a longer duration of action
Benztropine, Trihexyphenidyl
Antimuscarinic
Effect the CNS
Used to treat Parkinson’s
Tolterodine, Oxybutynin, Solifenacin
Antimuscarinic
Treatment for urinary incontinence due to overactive bladder
Tropicamide
Antimuscarinic
Used to dilate pupils for ophthalmologic exam
Pancuronium, Atracurium
Competitive (nondepolarizing) neuromuscular blockers
Competitive ACh antagonists at NM junctions
Can be reversed by Neostigmine
Succinylcholine
Depolarizing neuromuscular blocker
Causes weak contractions and then relaxation and paralysis
Acetylcholine
Narrow use (glaucoma) Rapidly hydrolyzed when administered systemically
Carbachol
ACh that resists hydrolysis
Used in Glaucoma
Can act on Muscarinic or Nicotonic receptors
Methacholine
ACh that resists hydrolysis
Only acts on Muscarinic receptors
Used in pulmonary function testing in asthma
Bethanchol
ACh that resists hydrolysis
Only acts on Muscarinic receptors
Used to stimulate GI motility
Used to combat urinary retention
Pilocarpine
Muscarinic agonist
Treats glaucoma and xerostoma
Cevimeline
Muscarinic agonist
Treats salivary gland dysfunction
Rivastigmine
Reversible cholinesterase inhibitor
Used to treat Alzheimer’s/dementia due to loss of cholinergic neurons in brain (Nucleus basilis of Meyner)
Donepezil
Reversible cholinesterase inhibitor
Used to treat Alzheimer’s/dementia due to loss of cholinergic neurons in brain (Nucleus basilis of Meyner)
3 Sedating Antihistamines
Doxylamine
Promethazine
Hydroxyzine
4 moderately sedating antihistamines
Diphenhydramine
Dimenhydrinate
Chlorpheniramine
Meclizine
5 non-sedating antihistamines
Loratadine Desloratidine Certirizine Fexofenadine Terfenadine
4 H2 Histamine Antagonists
Cimetidine (antiandrogenic, also has a bunch of other weird side effects to watch out for)
Ranitidine
Famotidine
Nizatidine
Treatment for peptic ulcer disease by decreasing gastric acid secretion
Metaclopramide
Dopamine antagonist in the CRTZ, decreases GI motility, increases lower esophageal sphincter tone
Treats nausea and vomiting during chemotherapy
Treats post op nausea
Ondansetron, granisetron
5-HT3 antagonist
Serotonin antagonist at 5-HT3 receptors
Treats nausea caused by activation of CRTZ, 5-HT from periphery
Metabolized by hepatic microsomal enzymes (possible drug interactions)
Side effects are headaches and constipation.
Dronabinol
Synthetic THC
Anti emetic, used in chemotherapy
Side effects are the effects of marijuana… (Sedation, confusion, paranoia, disorientation)
Dextromethorphan
Antitussive
No opioid effects, but not effective against severe coughs
May work on NDMA receptors
Sometimes kids try to abuse this (cough syrups) can be fatal.
Benzonatate
Antitussive
Anesthetic effect in the airway
Guaifenesin
Expectorant used as an antitussive
Increase mucus production in the airway.
They don’t work that well.
Acetylcysteine
Decreases the viscosity of mucus by breaking disulfide bonds
Also used as an antidote for Tylenol poisoning
Used to prevent mucus plugs when patients are at risk
