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Pharm Autonomic NS c
Cholinergic Blockers
| Question | Answer |
|---|---|
| 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] |