Phramacology Cholinergic Antagonists

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cholinergic antagonists

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block the action of Ach at muscarinic receptors

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tertiary agents

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lipid soluble
penetrates CNS better

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quarternary agents

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positive charge
water soluble
have higher ganglionic blocking to antimuscarinic activity ratio

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Atropine

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tertiary, but penetrates CNS poorly

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Scopolamine

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tertiary, penetrates CNS better than Atropine

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Ipratropium

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Quat, little CNS activity

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drug classes with anticholinergic effects

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H1-blockers
phenothiazines
TCA's
carbamazepine (Tegretol)

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anticholinergic toxicity symptoms

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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)

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other anticholinergic Side effects

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tachycardia
constipation
mental confusion
urinary retention

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cholinergic antagonists
tertiary agents

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1) Atropine
2) Scopolamine
3) Benztropine mesylate
4) Trihexyphenidyl
5) Dicyclomine
6) Darifenicin
7) Homatropine
8) Cyclopentolate
9) Tropicamide

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Atropine

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from belladonna plant
prototype of its class

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L-hyoscyamine

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active form

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d-hyocyamine

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non-active form

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use of Atropine

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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**

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action of Atropine

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competitive inhibitor at autonomic postgang. cholinergic receptors (muscarinic) even in sympathetic systems at sweat glands

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Atropine at low doses

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paradoxical decrease in HR

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Atropine at higher doses

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restlessness
hallucinations
disorientation

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Scopolamine

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Transderm Scop
L-hyoscine
(tertiary cholinergic antagonist)

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Scopolamine vs Atropine

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Scopolamine: more potent than Atropine on iris, ciliary body, secretions
less potent: at heart, bronchial & GI smooth muscles

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Scopolamine at therapeutic doses

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high incidence of CNS depression

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use of Scopolamine

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to prevent motion sickness (most common)
treatment for Parkinsonism

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Scopolamine in WW2

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twilight sleep and lowers inhibitions

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Benztropine mesylate

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Cogentin
synthetic muscarinic antagonists (structure similar to Atropine
tertiary agent

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use of Benztropine mesylate

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used to treat Parkinsonian syndromes
extrapyramidal symptoms
antihistaminic
local anesthetic effects

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Benztropine mesylate blocks?

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blocks CNS muscarinic receptors (M1) and dopamine reuptake

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Trihexyphenidyl

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Artane
synthetic antimuscarinic
tertiary agents

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use of Trihexyphenidyl

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for Parkinsonism
blocks dopamine reuptake
direct antispasmodic action on smooth muscles

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Dicyclomine

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Bentyl
cholinergic antagonist
tertiary agents (but little CNS activity)

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use of Dicyclomine

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antispasmodic in Tx of IBS

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Darifenicin

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Enablex
cholinergic antagonists
tertiary agents

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use of Darifenicin

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used to tx overactive bladder and urgency

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Darifenicin

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competitive agent
more potent at M3 receptors

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Darifenicin bind to?

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alpha-1-acid glycoprotein
98% plasma protein bound

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major eliminate route of Darifenicin?

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P-450 metabolism (CYP2D6 & CYP 3A4)
**caution in hepatic insufficiency or with P-450 inhibitors**

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mojor SE of Darifenicin

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dry mouth
dry eyes
constipation
UTI's

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Homatropine

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Isopto Homatropine
cholinergic antagonist
tertiary agent

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use of Homatropine

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opthalmic to produce mydriasis and cycloplegia for Dx

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contraindication of Homatropine

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pt with glaucoma or sensitivity to anticholinergics

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Cyclopentolate

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Cyclogyl
cholinergic antagonist
tertiary agent

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use of Cyclopentolate

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ophthalmic to produce mydriasis and cycloplegia for dx

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Tropicamide

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Mydriacyl
cholinergic antagonist
tertiary agent

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use of Tropicamide

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opthalmic to produce mydriasis and cycloplegia for dx

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contraindication of Tropicamide

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pt with glaucoma or a sensitivity to anticholinergics

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Homatropine
Cyclopentolate
Tropicamide

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may cause temporary stinging/burning on application, and increase IOP

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cholinergic antagonists
quaternary agents

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1) Glycopyrrolate
2) Ipratropium
3) Propantheline

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Glycopyrrolate

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Robinal
quaternary agent
cholinergic antagonist

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use of Glycopyrrolate

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GI antispasmotic
tx of bronchospasm
pre-op med to decrease salivary, GI, & pulmonary secretions
to decrease risk of acid aspiration during sx

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use of Glycopyrrolate during sx

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to block the effect of vagal stimulation
to block the muscarinic stimulation seen when anticholinesterase are used as reversal agents

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Glycopyrrolate, any CNS effects?

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No CNS effects
should not be used to tx OP toxicity

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Ipratropium

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Atrovent
structually similar to Atropine, but its quat

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use of Ipratropium

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bronchodialator for COPD
for acute asthma attacks
rinorrhea

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Proantheline

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Pro-Banthine
quat
older drug, used infrequently now

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use of Proantheline

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duodenal ulcers and IBS

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absorption of Proantheline

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absorption incomplete (10-25%) and variable
food further decreases absorption