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TL - Anticholinester

Anticholinesterase Drugs

QuestionAnswer
Say Ambenonium Am bee NO knee um
Say Demecarium Deh meh CARE ee um
Say Donepezil Doe NEP is ill
Say edrophonium Ed draw PHONE ee um
Say galantamine Gal LANT tuh mean
Say guanidine GWINE uh deen
Say neostigmine KNEE-OH stig mean
Say Physostigmine FYE sew stig mean
Say pyridostigmine PIE rid oh stig mean
Say rivastigmine Riv uh stig mean
Say tacrine Tack green or tack grin
Name 11 reversible anti-cholinesterases (ADDEGGNPPRT) Ambenonium, demecarium, donepezil, edrophonium, galantmine, quanidine, neostigmine, physostigmine, pyridostigmine, rivastigmine, tacrine
How do anticholinesterases work? they prevent the breakdown of acetylcholine by blocking the action of actylcholinesterase
Name the only therapeutic non-reversible anticholinesterase. Echothiophate
What routes are used for administration of anticholinesterase? PO mostly – anticholinesterases are readily absorbed from the GI tract, subcutaneous tissue, and mucous membranes
Name the anticholinesterase drug that can cross the blood brain barrier. Physostigmine
Name the anticholinesterase drug that requires higher PO dosing because it is poorly absorbed from the GI tract. Neostigmine
What is the advantage of oral dosing of Neostigmine? longer duration of action, the patient will not have to take as often
How is neostigmine administered if a rapid effect is needed? IM or IV
Which anticholinesterase drugs bind to plasma protein? Donepezil (highly bound), tacrine (55%), rivastigmine (40%), galantamine (18%)
How are most anticholinesterases metabolized and excreted? metabolized by plasma enzymes and excreted in urine
How are protein bound anticholinestrases metabolized? in the liver
What’s weird about the pharmacodynamic effects of anticholinesterases? They can produce stimulant or depressant effects on cholinergic receptors depending on the drugs dose and duration of action.
Discuss the duration of action of reversible anticholinesterases as compared to irreversible. reversible anticholinesterases work for minutes to hours, irreversible last from days to weeks
What are the therapeutic uses of anticholinesterases? reduce eye pressure - glaucoma & surgery; increase bladder tone; improve peristalsis; promote muscle contraction & diagnose myasthenia gravis; antidote for anticholinergics, tricyclics, belladonna, & narcotics; improve cognition in Alzheimer’s dementia
Name some drug interactions that would increase the risk for toxic reaction if taken with anticholinesterase drugs. Cholinergics like bethanechol, carbachol, and pilocarpine
What drugs would increase donepezil’s rate of elimination? Carbamazepine, Dexamethasone, refampin, phenytoin, and phenobarbital
What drugs could decrease the effects of anticholinesterase drugs and mask early signs of cholinergic crises(AAAAMC)? Aminoglycosides, anesthetics, anticholinergics ( atropine, belladonna, scopolamine), magnesium, corticosteroids, Antiarrhytmics ( procainamide, quinidine)
What drug is used to determine if a patient with myasthenia gravis is having a myasthenic crisis or experiencing anticholinesterase toxicity? Edrophonium
What four items should be available when edrophonium is used? suction, oxygen, mechanical ventilation, and atropine in case of cholinergic crisis
What causes the side effects associated with cholinergic drugs? activation of the parasympathetic nervous system
What are the side effects of anticholinesterases? cardiac arrhythmias, diarrhea, N&V, SOB, wheezing, chest tightness, seizure, headache, anorexia, insomnia, pruritis, urinary frequency, nocturia
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