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Reversal of anticholinergic induced CNS toxicity cholinergic drugs
- Drugs that block skeletal neuromuscular junction are often used during general anesthesia to maintain SM paralysis during surgery
- Indirect acting cholinergic stimulants inhibit cholinesterase enzyme at neuromuscular junction allowing endogenously released Ach to remain active at the synaptic site and overcome the neuromuscular blockade until the curarelike agents have metabolized
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Reversal of neuromuscular blockage
- Indirect acting cholinergic stimulants
- ----Reverse toxic effects of anticholinergic drugs
- Inhibit Ach breakdown allowing endogenously released Ach to overcome anticholinergic drugs
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Adverse Effects Cholinergic Drugs
- GI distress
- Increased salivation
- Bronchoconstriction
- Bradycardia
- Visual problems
- Exaggerated during parasymp activity
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Anticholinergic Drugs
- Attempt to diminish response to cholinergic stimulation
- Competitive antagonists of the postsynaptic cholinergic receptor but doesn’t activate it
- ----Binding blocks the receptor from the effects of the endogenous Ach, diminishing the cellular response to cholinergic stimulation
- Categories
- ----Antimuscarinic and antinicotinic agents
- --------Most common: atropine
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Anticholinergic drugs Mechanism of Action
- Preferential for certain muscarinic receptors
- Specificity is not exclusive therefore other tissues affected as well
- Antagonize GI muscarinic receptors
- Other drugs work on the ENS cholinergic synapses
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GI disorders anticholinergic drugs
- Blocks effects of endogenous Ach release
- Antispasmodic drugs: Decrease GI smooth muscle tone or spasms
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Parkinson disease
- Caused by deficiency in dopamine in basal ganglia
- Leads to overactivity of ventral cholinergic synapses
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Cardiovascular system
- Block effects of vagus nerve on myocardium
- Ach slows HR and conduction of action potentials
- ----Atropine reverses these effects
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Cholinergic poisoning
Inhibit the Ach-e enzyme throughout the body causing overstimulation of nicotinic and muscarinic receptors inf organs
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Eye
Block ach mediated contraction of pupillary sphincter muscle causing dilatation (mydriasis)
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Motion sickness
- Block cholinergic transmission from the brain and brainstem related nausea and vomiting
- Administered trans dermally via patches
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Preoperative med
- Decrease respiratory secretions during general anesthesia
- Respiratory tract
- Vagus nerve causes bronchoconstriction
- Anticholinergic drug blocks effects of vagal releases Ach and relax smooth muscle
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Urinary tract
- Atropine
- Elevate urinary frequency and incontinence by causing hypertonicity of bladder reducing contraction of the bladder detrusor muscle; allowing the bladder to fill more normally
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Adverse Effects anticholinergic drugs
- Cant be targeted for one specific organ without also achieving response in other tissue
- Dryness of mouth
- Blurred vision
- Urinary retention
- Constipation
- Tachycardia
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