Musarinic agonist/antagonist

• What transmitter does cholinergic drugs mimic or block?

  Acetylcholine
• what are the muscarinic agonist (cholinergic) drugs?

  Bethanechol

  Cevimeline

  Pilocarpine

  acetylcholine
• What is Bethanechol MOA?

  bindes reversibly to muscarinic cholinergic receptors
• what are the effects of Bethanechol?

  Bradycardia

  Lung constriction of bronchi

  GI: increase tone and motility

  Bladder: contraction of detrusor muscle and relaxation of trigone sphincter

  increase sweating, salivation, bronchial secretions and gastric acid

  Eye: Miosis and contraction of ciliary muscle
• What is Bethanechol used for?

  urinary retention

  investigational gastro uses

  off label GI reflux
• what are side effects of Bethanechol?

  hypotension

  abdominal cramps and diarrhea

  increase salivation

  exacerbation of asthma

  dysrhythmias in pts with hyperthyroidism
• what disease would you not give Bethanechol to?

  hyperthyroidism
• What does Cevimeline treat?

  dry mouth of SJS
• what does Pilocarpine treat?

  topical therapy for glucoma

  dry mouth SJS
• what does acetylcholine treat?

  rapid miosis (constriction) after cataract surgery
• What sources are Muscarinic poisoning?

  ingestion of mushrooms

  direct-acting muscarinic agonists

  cholinesterst inhibitors
• What is the monogram to remember when too much cholinergic acetylcholine is given?

  SLUDGE

  Salivation

  Lacrimation

  Urination

  Defecation

  GI upset

  Emesis
• What is the treatment for muscarinic poisoning?

  Atropine and supportive therapy
• What medications are given for overactive bladder?

  Anticholinergic drugs

  Atropine

  Oxybutynin

  Darifencacin

  Solifenacin

  Tolterodine

  Fesoterdodine

  Trospium
• What can be given if anticholinergic drugs do not work for overactive bladder?

  Percutaneous Tibial nerve stimulation
• what certain drugs have antimuscarinic (anticholinergic) actions?

  antihistamines

  TCA

  phenothiazine antipyschotics

  use with caution or not at all with other anticholinergic drugs
• What are the effects of atropine?


  increase HR

  decrease secretions

  relax bronchi, decrease tone of urinary bladder

  decrease tone and motility of GI

  mydriasis and cycloplegia

  mild excitation to hallucinations and delirium
• what is atropine used for?

  preanesthetic

  disorders of the eye

  bradycardia

  intestinal hypertoncity and hypermotility

  muscarinic agonist poisoning

  PUD

  asthma

  biliary coilic
• what are the adverse effects of atropine?

  xerostomia

  blurred vision and photophobia

  elevation of intraocular pressure

  urinary retention

  constipation

  anhidrosis

  tachycardia

  asthma
• what anticholinergic side effects does oxybutynin have?

  dry mouth, constipation, increased HR

  urinary hesitation/retention

  mydriasis

  dry eyes

  hallucinations and agitation - elderly and peds populatin
• what enzyme to avoid with CYP34A with oxybutynin that alter levels?

  CYP34A
• Darifenacin has the greatest degree for what M selectivity?

  M3

  does not have effect on M1 and M2
• Solifenacin has what adverse effects?

  dry mouth

  blurred vision

  in high doses prolongs QT
• Tolterodine selective muscarinic antagonist? side effects?

  nonselective muscarinic antagonist

  fewer side effects

  prolong QT
• Fesoterodine selectivity? drug interactions?

  nonselective muscarinic anatgonist

  substrate for CYP2D6 and CYP34A
• What is Mirabegron and Vibegron MOA of overactive bladder?

  promotes relaxation during filling to increase bladder capacity. Decreased urination frequency with impacting pressure or residual volume

  Detrusor relaxation through norepi activating Beta 3 adrenoreceptors
• What medications do not involve muscarinic receptors and do not produce anticholinergic effects?

  Mirabegron and Vibegron
• What are Mirabegron drug interactions? and adverse effects?

  substrate for CYP2D6 and CYP3A4

  moderate inhibitor for CYP26D

  minor inhibitor for CYP34A

  cause QT prolong and increase BP

  do not give to pts with renal disease or HTN
• what substrate is Vibegron of?

  CYP3A4
• What is Onabotulinumtoxina Botox MOA? side effects? line in OAB?

  3rd line in OAB

  injected into detrusor muscle

  motor endplate units regenerate after 3-24 months

  side effects - voiding dysfunction and UTI
• What are non-traditional therapies for OAB? MOA?

  SNRIs - Venlafaxine and duloxetine

  serotonin facilitates urine storage

  inhibit Sympatheitc innervation to the bladder
• what are duloxetine drug interactions?

  do not give with MAOIs

  metabolized by CYP3A4 and CYP2D6
• what is the difference between Atropine and Scopolamine?

  atropine - mild CNS excitation

  Scopolamine - produce sedation, suppress emesis and motion sickness
• what is scopolamine used for?

  motion sickness

  production of cycloplegia and mydriasis for ophthalmic procedures

  preanesthetic sedation

  obstetric amnesia
• What is not an adverse effect for Ipratropium bromide that is common with anticholinergics?

  dry mouth, blurred vision urinary hesitancy, constipation
• what medications are used for antisecretory anticholinergics?

  Glycopyrrolate

  mepenzolate

  Methscopolamine

  Propantheline
• what medications are used for mydriatic-cycloplegics (dilate eyes)(anticholinergics)

  atropine, homatropine, scoplamine, cyclopentolate, tropicamide
• what drugs cause central acting anticholinergics/drug induced parkinsonism?

  Benzotropine and Trihexphenidyl

  blocks the muscarinic receptors in the CNS
• what are symptoms of muscarinic antagoinst (anticholinergic) poisioning?

  dry mouth, blurred vision, photophobia

  hyperthermia,

  hot, dry, flushed skin

  resp depression - death
• What are sources of muscarinic antagoinst (anticholinergic) poisoning?

  belladonna

  antimuscarinic drugs: atropine, scopolamine

  antimuscarinic properties: antihistamines, TCA, phenothiazines