Autonomic Parasymathetic Drugs: Muscarinic Antagonists Flashcards
muscarinic antagonists reversibly block
muscarinic receptors
antimuscarinics block the muscarinic effects of
antimuscarinics block the muscarinic effects of diarrhea, urination, miosis, bronchospasm, bradycardia, lacrimation, salivation
antimuscarinics block the action of
antimuscarinics block the action of acetylcholine at M receptors
Atropine is an
antimuscarinic
Atropine and related antimuscarinic alkaloids are found in
- the flower Atropa belladonna (‘Deadly Nightshade’)
2. the plant Datura stramonium (‘Jimsonweed’)
antimuscarinics cause
pupillary dilation (mydriasis) and cycloplegia (inability to accommodate the lens for near vision)
Antimuscarinics include
- scopolamine
2. atropine
scopolamine is used to treat
motion sickness (vestibular nausea)
scopolamine transdermal patch is used to treat
motion sickness
antimuscarinics (e.g. scopolamine) cross
antimuscarinics (e.g. scopolamine) cross the blood-brain barrier and inhibits central M1 receptors
antimuscarinics block parasympathetic activation of M2
antimuscarinics block parasympathetic activation of M2 receptors on the SA and AV nodes (increased heart rate, increased AV conduction)
antimuscarinics block parasympathetic activation of __________ receptors on the SA and AV nodes (increased heart rate, increased AV conduction)
M2
antimuscarinics (e.g. atropine) increase
- heart rate
2. AV conduction
antimuscarinics are used to treat
- Bradycardia
2. Heart Block
ipratropium and tiotropium are useful in the management of
COPD (antagonize M3 receptors → bronchodilation, decreased secretions)
ipratropium and tiotropium are ________ antimuscarinic bronchodilators
inhaled antimuscarinic bronchodilators
_______ dissociates more slowly from the M3 receptor (longer bronchodilator action)
tiotropium
M3 muscarinic antagonist
- oxybutynin
- ipratropium
- tiotropium
- Tolterodine
oxybutynin and tolterodine treat
oxybutynin and tolterodine treat incontinence (antagonize M3 receptors → relax smooth muscle in ureters and bladder wall)
M1 muscarinic receptors are found in the
CNS
M1 receptor antagonists can reduce
M1 receptor antagonists can reduce tremors and rigidity in Parkinson’s disease
centrally acting M1 muscarinic antagonist
- benztropine
2. trihexyphenidyl
centrally acting antimuscarinics (e.g. benztropine, trihexyphenidyl) treat
centrally acting antimuscarinics (e.g. benztropine, trihexyphenidyl) treat tremor and rigidity in Parkinson’s (block excess cholinergic activity)
excessive M1 activation is associated with
cogwheel rigidity in Parkinson’s disease
antimuscarinics treat
extrapyramidal side effects caused by antipsychotics: e.g. dystonia, akathisia, parkinsonism (re-establish dopaminergic- cholinergic balance)
antimuscarinics inhibit M3 receptors on
antimuscarinics inhibit M3 receptors on sweat glands → decreased sweating → hyperthermia
antimuscarinics decrease
antimuscarinics decrease salivation and lacrimation → dry mouth and eyes
antimuscarinics cause
antimuscarinics cause mydriasis and cycloplegia → blurred vision
antimuscarinics cause mydriasis
antimuscarinics cause mydriasis → decreased outflow of aqueous humor → acute angle closure glaucoma
antimuscarinics cross
antimuscarinics cross the BBB and antagonize central M1 receptors → sedation, agitation, hallucination, coma (especially in elderly patients)