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Anticholinergic drugs - Coggle Diagram
Anticholinergic drugs
in general
Anticholinergic drugs (also called cholinergic blockers) are drugs that oppose the
physiological action of the neurotransmitter acetylcholine
also called parasympatholytic agents, are substances that reduce
the activity of the parasympathetic nervous system.
Because of the wide distribution of parasympathetic nerves, these drugs affect
many organs and structures of the body
including the eyes, the respiratory and
gastrointestinal tracts, the heart and the bladder
first type
Cholinoceptor blockers
Are antagonists or inverse agonists that bind to muscarinic or nicotinic receptors and prevent the effects of ACh and other cholinergic agonists
has two types
Antimuscarinic agents
Muscarinic receptors
Five subtypes (M1 to M5 )
ligand binding pocket are conserved among all muscarinic receptor subtypes.
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types
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Mechanism of Action
a nonselective, reversible and competitive antagonist that binds with high affinity to of all five known (M1 to M5) muscarinic receptors
s lipid-soluble and readily crosses membrane barriers
… so gets well distributed into the CNS, the eye, and other organs
an effective antidote used in the treatment of organophosphate anticholinesterase poisoning, overdose by a muscarinic agonist
Side effects
Dry mouth, urinary retention, blurred vision,
tachycardia and constipation
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It is a short acting antimuscarinic drug commonly applied as eye drops (ophthalmic
solution) prior to retinal exams
It produces mydriasis (dilation of the pupil) for 6h by inhibiting the contraction of the
iris sphincter muscles
- Darifenacin and oxybutynin
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Is an M1 selective antagonist, is used in the treatment of peptic ulcers, as it
reduces gastric acid secretion and reduces muscle spasm
has another divided
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Absorption
Distribution
Metabolism and Excretion
Contraindications
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only 10–30% of a quaternary antimuscarinic drug is absorbed after oral administration and decreased lipid solubility
antinicotinic
Neuromuscular blockers
useful during surgery to provide complete muscle relaxation at lower anesthetic doses, allowing for more rapid recovery from anesthesia and reducing postoperative respiratory depression
has two types
Nondepolarizing
Mechanism of action
competitively block ACh transmission at the nicotinic receptors … By doing so, they prevent depolarization at the muscle cell membrane and inhibit muscular contraction
Pharmacokinetics
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Drugs that are eliminated in the bile have shorter durations of action than those eliminated by the kidney
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Depolarizing
Succinylcholine
Mechanism of action
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Drug interactions
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Pharmacokinetics
Succinylcholine is injected intravenously. Its duration of action is longer than that of ACh (5–30 s), but it’s also brief (few min) which results from redistribution and rapid hydrolysis by plasma pseudocholinesterase … Therefore, drug effects rapidly disappear upon discontinuation
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