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Pharm Autonomic NS c

Cholinergic Blockers

QuestionAnswer
also referred to as: parasympatholytics, muscarinic antagonists, anticholinergics, muscarinic blockade
cholinergic blockers competitively block the actions of acetylcholine at muscarinic receptors
cardiovascular effects: blockade of muscarinic receptors increases HR, can reduce the PR interval by blocking receptors in the AV node
respiratory effects: relaxes bronchial muscle , bronchodilation, decreases bronchial secretions
exocrine gland effects: very effective on salivary glands causing dry mouth, suppress thermoregulatory sweating[which can produce fevers in children]
urinary and GI effects: GI smooth muscle is affected from the stomach to the colon[visceral walls are relaxed and both tone and peristalsis are diminished] smooth muscle of bladder and ureters is relaxed[can precipitate urinary retention]
CNS effects: mild CNS excitation, at high doses agitation, hallucinations, delirium can partially correct parkinsonian tremor and EPS associated with antipsychotic drugs[especially if combined with a dopamine precursor]
optic effects: unopposed sympathetic dilator activity producing mydriasis[b/c papillary contrictor depends on muscarinic receptor stimulation] cycloplegia[paralysis of the ciliary muscle]resulting in inability to accommodate near vision
belladonna alkaloid group: atropine, scopolamine
quaternary group: propantheline[Probanthine]
others benztropine[Cogentin], darifenacin[Enablex], fesoterodine[Toviaz], oxybutynin[Ditropan], solifenacin[Vesicare], tolterodine[Detrol], trihexyphenidyl[Trihexy], trospium[Sanctura]
contraindicated in: glaucoma, specially angle-closure b/c of mydriasis and cycloplegia
cautious use in: obstructive GI or GU tracts, older adults b/c of CNS effects of cholinergic blockers
ADRs in cardiovascular: tachycardia
ADRs in respiratory: tend to thicken and dry bronchial secretions
ADRs in exocrine system: anhidrosis[no sweating], xerostomia[dry mouth]
ADRs in GI and GU: constipation, urinary hesitancy nd retention, risk for UTIs, impotence
ADRs on eye: increased intraocular pressure, blurred vision, photophobia
ADRs on CNS: mild excitation to dizziness, confusion, CNS depression
drugs that are not cholinergic blockers but have significant muscarinic blockade: antihistamines, disopyramide[Norpace], quinidine, phenothiazine, antipsychotics, TCAs
Parkinson's disease: useful for control of tremor, early in course of tx, control of drooling Trihex and Cogentin
Tx of EPS drug of choice for this: Cogentin, Trihex
Tx for overactive bladder and urinary incontinence: Enablex, Toviaz, Ditropan, Vesicare, Detrol, Sanctura no cholinergic effects at the myoneural junction for any of these drugs
oxybutynin[Ditropan] increases blood levels and bioavailability of nitrofurantoin so different antibiotic should be chosen
assessment for bladder outlet obstruction should be done prior to prescribing these drugs b/c that contraindicates them
prevention of N/V from motion sickness scopolamine patch behind ear
adjunct therapy in IBS and PUD: atropine, dicyclomine[Bentyl], propantheline
atropine poisoning in children s/s: burning sensations in the mouth, difficulty in swallowing, rash, blurred vision, tachycardia, tachypnea, fever up to 109.8, muscle incoordination, seizure, respiratory paralysis, death
antidote for atropine poisoning is: physostigmine[Abrilirium, Isopto Eserine]
Created by: heatherbrown2020