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54 Cards in this Set

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cholinergic antagonists
block the action of Ach at muscarinic receptors
tertiary agents
lipid soluble
penetrates CNS better
quarternary agents
positive charge
water soluble
have higher ganglionic blocking to antimuscarinic activity ratio
Atropine
tertiary, but penetrates CNS poorly
Scopolamine
tertiary, penetrates CNS better than Atropine
Ipratropium
Quat, little CNS activity
drug classes with anticholinergic effects
H1-blockers
phenothiazines
TCA's
carbamazepine (Tegretol)
anticholinergic toxicity symptoms
1) hot as a hare, hyperthermia
2) blind as a bat (mydriasis & cycloplegia)
3) mad as a hatter (CNS stimulation)
4) dry as a bone (xerostomia)
other anticholinergic Side effects
tachycardia
constipation
mental confusion
urinary retention
cholinergic antagonists
tertiary agents
1) Atropine
2) Scopolamine
3) Benztropine mesylate
4) Trihexyphenidyl
5) Dicyclomine
6) Darifenicin
7) Homatropine
8) Cyclopentolate
9) Tropicamide
Atropine
from belladonna plant
prototype of its class
L-hyoscyamine
active form
d-hyocyamine
non-active form
use of Atropine
1) treat bradycardia
2) pre-op to decrease secretions
3) mydriatic for eye exam
4) counteraction for AchE-I toxicity
** No longer used for Parkinson's**
action of Atropine
competitive inhibitor at autonomic postgang. cholinergic receptors (muscarinic) even in sympathetic systems at sweat glands
Atropine at low doses
paradoxical decrease in HR
Atropine at higher doses
restlessness
hallucinations
disorientation
Scopolamine
Transderm Scop
L-hyoscine
(tertiary cholinergic antagonist)
Scopolamine vs Atropine
Scopolamine: more potent than Atropine on iris, ciliary body, secretions
less potent: at heart, bronchial & GI smooth muscles
Scopolamine at therapeutic doses
high incidence of CNS depression
use of Scopolamine
to prevent motion sickness (most common)
treatment for Parkinsonism
Scopolamine in WW2
twilight sleep and lowers inhibitions
Benztropine mesylate
Cogentin
synthetic muscarinic antagonists (structure similar to Atropine
tertiary agent
use of Benztropine mesylate
used to treat Parkinsonian syndromes
extrapyramidal symptoms
antihistaminic
local anesthetic effects
Benztropine mesylate blocks?
blocks CNS muscarinic receptors (M1) and dopamine reuptake
Trihexyphenidyl
Artane
synthetic antimuscarinic
tertiary agents
use of Trihexyphenidyl
for Parkinsonism
blocks dopamine reuptake
direct antispasmodic action on smooth muscles
Dicyclomine
Bentyl
cholinergic antagonist
tertiary agents (but little CNS activity)
use of Dicyclomine
antispasmodic in Tx of IBS
Darifenicin
Enablex
cholinergic antagonists
tertiary agents
use of Darifenicin
used to tx overactive bladder and urgency
Darifenicin
competitive agent
more potent at M3 receptors
Darifenicin bind to?
alpha-1-acid glycoprotein
98% plasma protein bound
major eliminate route of Darifenicin?
P-450 metabolism (CYP2D6 & CYP 3A4)
**caution in hepatic insufficiency or with P-450 inhibitors**
mojor SE of Darifenicin
dry mouth
dry eyes
constipation
UTI's
Homatropine
Isopto Homatropine
cholinergic antagonist
tertiary agent
use of Homatropine
opthalmic to produce mydriasis and cycloplegia for Dx
contraindication of Homatropine
pt with glaucoma or sensitivity to anticholinergics
Cyclopentolate
Cyclogyl
cholinergic antagonist
tertiary agent
use of Cyclopentolate
ophthalmic to produce mydriasis and cycloplegia for dx
Tropicamide
Mydriacyl
cholinergic antagonist
tertiary agent
use of Tropicamide
opthalmic to produce mydriasis and cycloplegia for dx
contraindication of Tropicamide
pt with glaucoma or a sensitivity to anticholinergics
Homatropine
Cyclopentolate
Tropicamide
may cause temporary stinging/burning on application, and increase IOP
cholinergic antagonists
quaternary agents
1) Glycopyrrolate
2) Ipratropium
3) Propantheline
Glycopyrrolate
Robinal
quaternary agent
cholinergic antagonist
use of Glycopyrrolate
GI antispasmotic
tx of bronchospasm
pre-op med to decrease salivary, GI, & pulmonary secretions
to decrease risk of acid aspiration during sx
use of Glycopyrrolate during sx
to block the effect of vagal stimulation
to block the muscarinic stimulation seen when anticholinesterase are used as reversal agents
Glycopyrrolate, any CNS effects?
No CNS effects
should not be used to tx OP toxicity
Ipratropium
Atrovent
structually similar to Atropine, but its quat
use of Ipratropium
bronchodialator for COPD
for acute asthma attacks
rinorrhea
Proantheline
Pro-Banthine
quat
older drug, used infrequently now
use of Proantheline
duodenal ulcers and IBS
absorption of Proantheline
absorption incomplete (10-25%) and variable
food further decreases absorption