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49 Cards in this Set

  • Front
  • Back

Parasympathetic stimulation

increases activity of GI, genitourinary systems


decreases activity of CV system


drugs that increase, decrease parasympathetic activity

cholinergic, anticholinergic

cholinergic drugs indicated for what?

Alzheimers, glaucoma, MG, urinary/intestinal stasis

Anticholinergics indicated for what?

overactive urinary/intestinal conditions


asthma/COPD


motion sickness


various opthalmic procedures

neurotransmitter of PS system

ACH

acetylcholinesterase

inactivates ACH when outside nerve ending and not on receptor

pseudocholinesterase

enzyme, located in liver and plasma, hydrolyzes ACH, other drugs

location muscarinic (M) receptors

internal organs, glands

location Nn (nicotinic neural) receptors

autonomic ganglia

location Nm (nicotinic muscle) receptors

skeletal muscle

cholinergic receptors at PS postganglionic nerve endings

muscarinic receptors

cholinergic receptors at ganglionic sites of both S, PS nerves

nicotinic-neural (Nn)

drugs that act like ACH, low doses of nicotine at Nn receptors

ganglionic stimulents

drugs that block ACH or act like high doses nicotine at Nn receptors

ganglionic blockers

drugs that act like ACH or muscarine at muscarinic receptors

cholinergic/muscarinic

drugs that block ACH at muscarinic receptors

anticholinergic/antimuscarinic

cholinergic receptors at NMJ of skeletal muscle

nicotinic-muscle (Nm)

srugs that block effect of ACH at NMJ

neuromuscular blockers


skeletal muscle relaxants

parasympathomimetic

cholinergic drugs that mimic actions of ACH at cholinergic (muscarinic) receptors

Cholinergic drug subdivisions

direct acting


indirect acting

direct acting drugs

bind to cholinergic (muscarinic) receptors, produce effects similar to ACH


increase activity only at cholinergic (muscarinic) sites

indirect acting drugs

inhibit acetylcholinesterase (increase ACH concentration, actions at all muscarinic, nicotinic receptor sites).

Direct-acting drug examples

Acetylcholine (Miochol-E)


(miotic in ophthalmology)



bethanecol (Urecholine)


(urinary retention, postoperative ileus)



Carbachol (Isopto carbachol)


(Glaucoma)

indirect acting drug (anticholinesterases) examples

Ambenonium (Mytelase)- MG


Demecarium (Humorsal)- glaucoma


Donepezil (Aricept)- Alzheimers


Galantamine (Reminyl)- Alzheimers


Rivastigmine (Exelon)- Alzheimers

effects of direct acting drugs

increase GI secretions/motility


increase urination


cause miosis



decrease heart rate


bronchoconstriction (usually insignificant)

Pilocarpine

used as eyedrops in glaucoma treatment

Bethanechol

direct acting; administered orally to stimulate urinary, intestinal tracts


adverse effects due to overstimulation (increased frequency, diarrhea)

use of cholinergics for glaucoma

eyedrops produce miosis, prpomotes better drainage of intraocular fluid from eye. Lowers pressure, helps prevent retinal damage

anticholinesterases

indirect acting drugs

anticholinesterase subdivisions

reversible inhibitors


irreversible inhibitors (of acetylcholinesterase)+

reversible inhibitors

diagnose/treat MG, Alzheimers, antidotes to reverse effects of drugs that block cholinergic, nicotinic receptors

Method of diagnosing MG

IV injection of low dose edrophonium


increase in muscle strength within 1 minute positive for MG

neostigmine


pyridostigmine


ambenonium

administered orally for treatment of MG, IV to reverse effects of excessive cholinergic blockade

physostigmine

used parenterally to reverse CNS effects of excessive anticholinergic blockade, eyedrops in treatment of glaucoma

Irreversible inhibitors

derivatives of compounds used as insecticides, pesticides, chemical warfare agents

Echothiophate (Phospholine)

only irreversible inhibitor used clinically. Administered as eyedrops in treatment of glaucoma

Atropine

used for excessive cholinergic stimulation

Pralidoxime

antidote to organophosphate chemical warfare agents

Organophosphates

irreversible anticholinesterase drugs found in insecticides, pesticides, chemical warfare agents

reversible anticholinesterase drugs

More widely used than direct acting cholinergic drugs.


Used for MG, Glaucoma, urinary retention. intestinal paralysis, Alzheimers, antidotes to curare-type skeletal muscle blockers, AC drugs

Drugs used to treat MG

pyridostigmine


ambenonium


used orally

treatment for urinary retention (atony of bladder), intestinal stasis/paralysis (paralytic ileus)

neostigmine

Drugs to treat Alzheimers

Tacrine (Cognex)- 1st drug introduced, more side effects


Donepezil (Aricept)- approved all stages


Galantamine (Reminyl), rivastigmine (Exelon)- newest for mild/moderate disease


Memantine (Namenda)- newest, better tolerated

Antidote for anticholinergic drug poisoning

physostigmine- can pass blood/brain barrier

Anticholinergic drug examples

atropine- used for drug poisoning, eye exams


scopolamine- used for intestinal disorders, motion sickness


oldest, obtained from belladonna plant

common AC side effects

dry mouth, blurred vision (mydriasis) sedation, mental confusion

AC contraindications

glaucoma, prostate hypertrophy, urinary/intestinal obstruction

treatment for AC overdose

inducing emesis, gastric lavage,activated charcoal, saline cathartics


Physostigmine

njn

njnn