Direct-Acting Cholinergic Agonists

  • Chemicals that act at the same site as the neurotransmitter acetylcholine (ACh)
  • Similar response as parasympathetic system activation - Effects are widespread
  • These drugs usually stimulate muscarinic receptors in PNS 
  • used as systemic agents used to:
        - ↑ bladder tone, urinary excretion, & GI secretions
        - also used as ophthalmic agents to induce miosis to relieve ↑ IOP of glaucoma via pupil constriction (not systemic when used ophthalmically)
        - ↓ HR, ↓ myocardial contractility, bronchoconstriction & ↑ bronchial mucous secretion

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Contraindications:
  • Any condition that would be exacerbated by parasympathetic effects—bradycardia, hypotension, CAD
  • PUD, intestinal obstruction or recent GI surgery  
  • Asthma 
  • Bladder obstruction 
  • Epilepsy & parkinsonism

Caution:
  • pregnancy / lactation

Adverse Reactions:
  • N/V, diarrhea, cramps, involuntary defecation 
  • Bradycardia, heart block, hypotension 
  • Urinary urgency 
  • Flushing, ↑ sweating & salivation, swallowing difficulty

Interactions:
  • ↑ risk of cholinergic effects if these drugs are combined or given with acetylcholinesterase inhibitors 

Kinetics:
  • Well absorbed and have relatively short half-life (1-6 hr) 
  • Metabolized; excretion of these drugs is not known

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Drugs:

1. Bethanechol (Duvoid, Urecholine)
   - urinary retention
   - urogenic bladder
   - esophageal reflux in infants/kids

Mgmt:
  • Produces muscarinic effects primarily on GI tract & urinary bladder
    •     ↑ tone & peristaltic activity of esophagus, stomach, and intestine
    •     contracts detrusor muscle of urinary bladder, usually enough to initiate micturition.
    •     cant help if obstructed 
  • must monitor for effectiveness - i.e are they having problem still w/ urinary retention? (relief should be quick)
  • if not working, could be structural problem (BUN & Cr will go way up)



2. Carbachol (Miostat)
- induces miosis to ↓ IOP


3. Cevimiline (Exovac)
- Tx dry mouth


4. Pilocarpine (Salagen)
- Tx dry mouth (xerostomia) s/p radiation therapy of head & neck tumor 
- glaucoma (constricts pupil & ↓ IOP)

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Nursing Mgmt
Baseline Assessment
  • Cardiovascular  - HR, BP CAD 
  • GI - Bleeding, ulcer disease, obstruction, dehydration 
  • Respiratory assessment  - Asthma 
  • GU - Recent bladder surgery or obstruction 
  • CNS - Parkinson’s and/or epilepsy



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