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35 Cards in this Set
- Front
- Back
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muscarinic
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nerve
heart/smooth m glands/endotheilum |
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nicotinic
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Neuromusc end plate
skeletale m autonomic ggl cells |
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musc agonists
cholinesters |
ACh
carbachol bethanechol |
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musc agnoists
alkaloids |
pilocarpine
muscaine |
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cholinesterASE inhibitors
reversible |
edrophonium
physiotigmine neostigmine donepezil |
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cholinesterASE inhibitors
IRRVS |
organophosphates
parathion |
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cholinesterASE Reactivators
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pralidoxime
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choline esters/alkaloids
mechanisms |
act of PREsynapic receptors inhibts release of various NT
some activate NICOTINIC receptors...(POSTGGLinc) prolonged act = ....no change in resting potential therefore no respones by organ (depolization blockade) |
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M, 1,3,5
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IP3 formation DAG cascade
ca+2 increase cell excite |
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M 2,4
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inhibit cAMP
open K+ channels cell INHIBITion |
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Heart
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M2
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SMooth muscle
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M3
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brain
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all 5
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endothelium
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M3
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exocrine gland
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m3
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carbachol-sensitity
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M3 and Nm
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bethancehol - sensitivity
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M3 and no Nm
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ACh- sensitiivy
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all three and Nm....VERY sensitve to cholinesterase
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Cholinesters - dynamics
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Heart SA node (m2) decrease hr
atira - refractiveness decreased av - decrease in conduction venticles - minimal change |
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cholinesters - dynamics 2
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vessles vasodilation (m3, w/ NO)
GI - increased tone/contractions/peristalsis rlx of spincters - contact LES mild stimulation of INSULIN Genitouninary - contract detrussor m, errection Resp - bronch muscle contraction increased secretions eye - miosis (spintcer contractions) cyclospam - leans curvature increase for near vision (ciliary m contracts) aq humor outflow/lacrimal glands increase skin - sweat glands |
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pharmokinetics
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oral - low
distripution - periph tissues only, No CNS biotrans - achASE & butASE (breaksdown)....Carbachhol and bethanechol resistance AcH & carbachol - topical on conjuctivia Bethanechol - (AVOID IV or IM) |
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adverse affects (on conjuctiva))
(carbacol/acH) |
CATARACTS!!
difficult seeing far |
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advrese affects bethaechol
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nausea/vomit/hypotension
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contraindications
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asthma, COPD, hyperthyoridsm, arrhymithas, Pep ucler disease
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Alkaloids
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pilocarine tertiary
muscarine quaternary only M1,2,3 ( no Nm) stimulates sweating/salivation arousal/excite/headache/tremors |
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alkaloids - adverse
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similar to choiline esterrs...nausea sweating with posiion mushrooms....no muscle tone affected
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alkaloids USES
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open angle glaucoma - pilocarpine
xerostomia (in sjorgnes syndrome) muscarine (no use) |
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cholinestASE INHIBITORS
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reversible - carbamates (physotigmene & neostigmeans....alcohols...donepezil (good for CNS)
irrves - organophosphates |
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cASE inhib cont
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edrophonium - short lived
carbates - 1-6 hour 1/2 life organophosphates - esteratic site (w/ AGING) then it becomes irrvs |
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pharmokinetics
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CNS - MD - alterness/
HD - confusion, ataxia, loss of reflex eye,resp, GI, urinary = same as choloniestere CVS - symp ggl/psns ggl - M3 receptors m2 on heart relase of epi from adrenal medulla -MD = bracycardia HD- markked bradycardia NMJ - MD (contractions) HD - fasculations, NM blockage...small muscles first paralyzed diaphram last to go |
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pharmokineites of cASE inhib
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oral - ok for teritary
low for quant very good for ORGANOPHOSPHATES Distribution teritary CNS quat - perio organo - all tissue Biotrans -carbamates plasma esterase organophosphates - paraoxases physotigmene 1-2 t1/2 |
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adverese affects of cASE inhib
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fatigue,muscle cramps, fasiculations
CATARACTS death - resp failure diagnosis - check enz activity of cholinestease act treatment - with Diazpam, atropine |
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posining of cASE inhib
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eye - miosis, lacrimation
resp - rhinorreaha, salivary & bronch sections skin - sweating/flush skeletal - weakness/paralysis GI - invol urination/penil erection cvs - bradicardia, hypotension CNS - ataxias, slurred speech. coma convulsions |
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cholinesterase reactivators
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oximes...PRALIDOOXIME
works as long as AGING did not happen to the complex oral bio - <1% no brain t1/2 - 1.-1.5 hours use with organophosphate posining |
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use of chol drugs
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open angle glaucoma
MG (use edrophonium IV) for diagnosis Neostigmine for MG (TREATMENT PO) GI - exosteoma, post op CNS - AD ...donepezil inhib achASE of brain) |
