Adrenergic And Cholinergic Effects, Agonists And Antagonists

Front 1

cholinergic agonists are divided into two groups which are:

Back 1

esters of chline (ACh, methacholine, bethanecol, carbachol)

Alkoloids (muscarine, nicotine, pilocarpine,)

Front 2

Muscarinic effects on the eye and cardiovascular system include

Back 2

decrease IOP

vasodilation, dec HR and reduced contractility

Front 3

Muscarinic effects on the respiratory and GI tract include

Back 3

bronchoconstriction, increased secretion (contraindicated in asthma)

increased secretory and motorof gut activity..digestion

Front 4

Nicotine effects on PNS in cardiovascular system, GI, respiratory, and genitourinary

Back 4

-will activate both through post ganglionic neurons

cardiovascular effects are sympathetic

all the rest are parasympathetic

MATCH (muscle weakness, fasciculations, Adrenal medula inc, tachycardia, cramping of skeletal muscle, hypertension)

Front 5

organophosphates are

Back 5

nonselective ACHe inhibitors- inhibits both nicotinic and muscarinic

Front 6

All esters of choline cross the bbb T/F

Back 6

false

Front 7

esters of choline are contraindicated for

Back 7

hyperthyroidism, asthma, coronary disease (hypotension), acid peptic disorders, obstructive urinary retention

Front 8

ACH

Back 8

ester of choline
-need high IV doses to detect effects- used to dec IOP post operatively and sweat spot test

Front 9

Methacholine

Back 9

ester of choline

more resistant to cholinesterase and longer lasting-

-used to diagnose bronchial airway hypersensitivity

Front 10

carbachol

Back 10

-ester of choline
significant nicotinic activity at ganglia, skeletal muscle and adrenal medulla

used for intracameral instillation to produce miosis in ocular surgery and to reduce postoperative rises in IOP. Ophthalmic drops to reduce IOP in glaucoma or hypertension

limited to ophtalmic applications

Front 11

bethanechol

Back 11

ester of choline
-not nicotinic, inc GI motility,
-only ester of choline given systemically
used for empying bladder in postpartum nonobstructive urinary retention

Front 12

alkaloids-

Back 12

muscarine, pilocarpine, nicotine, varenecline

Front 13

pilocarpine

Back 13

-alkaloid-
crosses BBB
-active on eye and sweat glands
-miosis, accomodation
-initial tx of open angle glaucoma- red IOP (not use if IOP is >45mmHg.
-if taken orally causes Xerostomia assoc with Sjogren's syndrome

Front 14

Nicotine

Back 14

cholinomimetic-> alkaloid
All autonomic ganglia including skeletal muscles and cns.
-can activate and inhibit nicotinic ACH receptors
-used as smoking cessasion agent
-rapid activation of receptor followed by desensitized state.

Front 15

Varenecline

Back 15

-Alkaloid-
partial agonist

Front 16

ACHe inhibitor groups

Back 16

-simple alcohols - quarternary ammonium (edrophonium) 5-15 min
-Carbamic acid esters (carbamates, neostigmine) 30min-6hrs
-organic derivatives of phosphoric acid (organophosphates) (irreversible 2 step process)
hundreds of hours

Front 17

pralidoxime

Back 17

PAM- if used before aging in organophosphate (ACHe inhibitor) occurs, then enzyme can be restored.

Front 18

ACHe inhibitors effects on organ systems

Back 18

mostly parasymphathetic-
CV-reduced CO, no VSM effect,

CNS- coma, convulsions, respiratory failure

NMJ- can be beneficial for someone with myasthenia gravis or someone given curare

Front 19

edrophonium

Back 19

-reversible ACHe
5-15 min
-dx for myasthenia gravis and evaluating efficacy of myasthenia therapies

-give 2mg followed by 8ngm if muscle weakness occurs -> cholinergic crisis- need atropine

-used to assess efficacy of long term tx- pyridostigmine- if patient is stronger, dosage not enough

Front 20

physostigmine salicylate

Back 20

reversible ACHe
30m to 6hrs-
-local application causes miosis, accomodation, decrease in IOP. Pilocarpine is more effective.

Front 21

neostigmine

Back 21

reversible cholinesterase inhibitor
.5-2hrs
myasthenia gravis,
alleviate postoperative urinary retention and paralytic ileus
-reverse neuromuscular blockade,
-lower IOP in glaucoma or post ophthalmic surgery

Front 22

donepezil

Back 22

-reversible anticholinesterase
long duration, for symptomatic tx of AD
-no hepatic toxicity

Front 23

tacrine

Back 23

like donepezil but with hepatic toxicity

Front 24

galantamine

Back 24

mild to moderate tx of AD
reversible ACHe inhibitor

Front 25

pyridostigmine

Back 25

long term ACHe inhibitor
3-6hrs
myasthenia gravis

Front 26

ambenonium

Back 26

reversible anticholinesterase
4-8hrs

Front 27

demarcium

Back 27

reversible ACHe
glaucoma

Front 28

carbaryl

Back 28

reversible ACHe
lice

Front 29

Pralidoxime 2-PAM

Back 29

irreversible ACHe
-regenerate enzyme if given before aging for organophosphates

Front 30

echothiopate

Back 30

irreversible ACHe inhibitor
-low lipid solubility- not absorbed systemically
-glaucoma
-100 hrs

Front 31

malathion and parathion

Back 31

-irreversible ACHe inhibitor
-rapidly metabolized by birds and mammals to non-toxic metabolites but not by insects or fish
-parathion is not detoxified in vertebrates, more dangerous

Front 32

nerve agents

Back 32

sarin, soman, tabun and vx
-chemical warfare
-flaccid paralysis, respiratory failure
-pyridostigmine given prophylactically to block binding of irreversible agents so more time for tx with atropine or 2-PAM

Front 33

toxicity of cholinomimetics-direct acting stimulants

Back 33

tx is atropine
o

Front 34

toxicity of cholinomimetics- direct acting nicotinic stimulants

Back 34

-toxic dose = 40mg - 2 cigarettes but it is an emetic

-tx with atropine or diazepam for cns effects

Front 35

toxicity of cholinomimetics: cholinesterase inhibitors

Back 35

-home pesticides = source
-tx- maintain vital signs, decontaminate, parenteral atropine in large doses and PAM to regenerate, benzodiazepines to prevent seizures