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FIU - Cholinesterase Inhibitors
Cholinesterase inhibitors
21
Pharmacology
Professional
12/30/2011

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Term
Uses of cholinesterase inhibitors
Definition
Alzheimer's disease (symptom development reduction), reversal of NDMR (an anesthesia), Myasthenia gravis (disease with antibodies against Ach receptors) tx, Central Anticholinergic syndrome (dry as a bone..etc) tx
Term
Tacrine mode of action? Use? SE?
Definition
Non-specific cholinesterase inhibitor (AChE and BuChE = butyrylcholine found mostly in liver/periphery), Alzheimer tx. SE: Nausea, vomiting and liver damage (enzymes up)
Term
Donepezil mode of action and advantage? Use? Halflife?
Definition
More selective ChEI (for ACh in the CNS) = less BuChE inhibition in periphery and less hepatoxicity. Alzheimer's tx
t1/2 = 70 hrs so once a day drug
Term
Rivastigmine mode of action, use?
Definition
AChE and BuChE inhibitor, Alzheimer's tx
Term
Tubocurarine mode of action, effect
Definition
Type of curare (isoquinoline alkaloids) that blocks ACh receptors (nicotinic) at neuromuscular junction, relaxation/paralysis of muscle
Term
Intocostrin, effect?
Definition
Synthetic curare, muscle relaxation
Term
Malouetine, mode of action, effect
Definition
African aminosteroid that blocks neuromuscular junction, muscle relaxation
Term
3 components of anesthesia
Definition
1)analgesia like fentanyl 2)sedative like lorazepam 3)NDMR (non-depolarizing muscle relaxant) like pancuronium
Term
Pancuronium
Definition
synthetic aminosteriod NDMR (non-depoloarizing muscle relaxant)
Term
Edrophonium mode of action, effect, advantage, SE?, reversal of its effect?
Definition
AChE inhibitor w/o CNS penetration, reversal of NDMR, fewer muscarinic effects than neostigmine and distribution terminates after 10 min (low potency); SE: Brochoconstriction, bronchospasm, bradycardia ... Note: don't use atropine to reverse, goes into CNS, use glycopyrrolate (muscarinic blocker w/o BBB penetration)
Term
Neostigmine, mode of action, effect
Definition
AChE inhibitor w/o CNS penetration, NDMR reversal (most potent/common)
Term
Myasthenia gravis drug types?
Definition
Immunosuppressants, steriods (reduce reactivity of immune system), AChE-Inhibitors...also thymectomy
Term
Methotrexate mode of action, use, drug interaction
Definition
immunosuppressant (low dose) = inhibitor of T cell activation and suppression of intercellular adhesion molecule expression, Myasthenia gravis tx; decreased excretion when used along with penicillin like antibiotics (renal tubular competition)
Term
cyclosporin A mode of action, use
Definition
immunosuppressant, binds to cyclophilin (immunophilin) of T-lymphocytes. This inhibits calcineurin which normally activates transcription of IL2; myasthenia gravis tx
Term
Pyridostigmine mode of action, use, SE?
Definition
AChE inhibitor w/o CNS penetration (more potent/long acting than other AChE inhibitors; first-line tx of Myasthenia gravis, preemptive tx before potential OP/nerve gas exposure; SE: can antagonize muscle relaxants (that block ACh receptors)
Term
Tacrolimus mode of action, use
Definition
immunosuppressant (calcineurin inhibitor like cyclosporin), myasthenia gravis tx (gradual reduction of anti-AChR antibodies)
Term
Organophosphates, toxic effects
Definition
Pesticides that inhibit AChE; DUMBBELLS (diarrhea, urination, mitosis, bronchorrhea, bronchospasm, emesis, lacrimation, laxation, salivation)
Term
Treatment of OP (organophosphate poisoning)
Definition
A FLOP (Atropine [anti-cholinergic], FLuid [atropine makes dry], Oxygen, Pralidoxime [removes OP from Cholinesterase, reactivates]
Term
-stigmine
Definition
AChE inhibitors
Term
Physostigmine mode of action, use
Definition
Cholinesterase inhibitor that penetrates BBB. Used in ordeal by poison, counters Central Anticholinergeic Syndrome (mad as a hatter, dry as a bone, red as a beet, hot as a hare, blind as a bat).
Term
Random facts: K effects on digitoxicity, QRS widened in? Verapamil effect on ventricular arrhythmias? insulin inotropic effect? dopamine effect on renal perfusion?
Definition
hyperkalemia enhances acute, hypokalemia enhances chronic; QRS widened in ventricular arrhthymias, verapamil is counterindicated, slows heart/lowers bp w/o need; insulin most potent inotrope; low dose dopamine increases renal perfusion
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