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19 Cards in this Set
- Front
- Back
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Methacholine |
Muscarinic Agonist (direct cholinomimetic)
B methyl group makes it less susceptible to AChE
Cardiovascularly active (acts on M2 subtype)
Used to diagnose asthma |
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Carbachol |
Muscarinic Agonist (direct cholinomimetic)
NH2 group replaces terminal methyl makes it less susceptible to AChE
Low dose = mAChR agonist; High = nAChR agonist
Treats glaucoma by opening up Canal of Schlemm |
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Bethanechol |
Muscarinic Agonist (direct cholinomimetic)
ACh + B methyl + NH2 to make less susceptible to AChE
Increases GI motility and bladder contraction |
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Atropine |
Muscarinic Antagonist Competitive inhibitor of ACh
Lipid Soluble; crosses BBB
Blocks DUMBBELSS (diarrhea, urination, miosis, bronchoconstriction, bradycardia, excitation, lacrimation, salivation, sweating) |
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Curare |
Nicotinic Antagonist
Bulky w/ 10 C between N groups -- acts at muscular nAChR
Blocks ACh at NMJ to cause skeletal muscle paralysis during surgery |
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Hexamethonium/Trimethephan |
Nicotinic Antagonist
Bulky w/ 6 C's between N's -- acts at the neuronal nAChR
Ganglionic Blocker affects both SNS and PSNS
Action on system depends on the predominant tone (most are PSNS except sweat glands and vasculature) |
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Tolterodine (Detrol) |
Muscarinic Antagonist
Causes urinary retention to treat overactive bladder
FX associated with anti-cholinergics |
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Edrophonium |
Anticholinesterase/indirect cholinomimetic
Reversible AChE inhibitor @ NMJ
Used to diagnose Myasthenia Gravis in the Tensilon test
Used in OR to reverse paralysis along with neostigmine |
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Physostigmine |
Anticholinesterase
Neutral drug - can cross BBB
Mainly used to treat atropine and anti-cholinergic drug overdose
Can also treat Glaucoma by inducing miosis |
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Pyridostigmine |
Anticholinesterase
Does not cross BBB; absorbed in the GI tract
Used to treat Myasthenia gravis |
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Neostigmine |
Anticholinesterase
Does not cross BBB
Used to reverse NMJ blocking anesthesia in OR |
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Donepezil (Rivastigmine) |
Anticholinesterase
Crosses BBB - treatment for Alzheimers to increase relative amounts of ACh in brain
Given as a patch --> good for cognitive impairment |
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Sarin, Soman, Tabun, Mustard Gas |
Potent AChE inhibitor leads to cholinergic poisoning (bronchoconstriction, Gi motility, secretions, bradycardia)
Treatment: Atropine and Pralidoxime
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Pralidoxime |
Treatment for organophosphate poisoning
Breaks bond between nerve agent and cholinesterase |
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Sildenafil |
AKA viagra
Phosphodiesterase inhibitor
Blocks PGE from increasing levels of cGMP to inhibit relaxation of penis smooth muscle |
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Aminophylline/Theophylline |
Phosphodiesterase (PDE) inhibitor increases levels of cAMP in the cells
Allow for bronchodilation (Beta2 Gs effects)
Causes unwanted side effects of increased cardiac contractility and CNS excitation |
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Pentobarbital |
Barbituric Acid with ethyl and methyl substitution
CNS depressant - sedative effect from enhancing GABAa receptor activity and blocking AMPA/voltage-gated Ca2+ channels
Lipid and water soluble Gastric emptying time is RLS |
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Thiopental |
Sulfur replaces Oxygen in Pentobarbital = more lipid soluble
Crosses BBB easily into central compartment-- faster, stronger anesthetic onset and shorter duration of the drugs effects
Good for induction of surgical anesthesia |
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Phenobarbital |
CNS depressant - Only GABAa receptor effects at low doses
Phenol replaces the methyl-butyl group making the drug MORE CHARGED
Unable to cross BBB rapidly -> given for epilepsy but not anesthesia |
