Prototype drugs exam 2 Flashcards
Anticholinergic Agents/ Parasympatholytics
atropine
Indications for atropine
Decrease secretions, bradycardia, pylorospasm, ureteral colic, relaxing of bladder, emotional lability with head injuries, antidote for cholinergic drugs, pupil dilation
Actions of atropine
competitively blocks acetylcholine muscarinic receptor sites, blocking the effects of the parasympathetic nervous system.
Pharmacokinetics of atropine
Route- IM
Onset-10-15min
peak- 30min
Duration 4h
Route- IV
Onset- stat
Peak- 2-4 min
Duration- 4h
Route- SQ
Onset- varies
Peak- 1-2h
Duration- 4h
Route- topical
Onset- 5-10 min
Peak- 30-40 min
Duration- 7-14 day
Half-life of atropine
2.5 h, with metabolism in the liver and excretion in the urine
Adverse effects of atropine
blurred vision, mydriasis, cycloplegia, photophobia, palpitations, bradycardia, dry mouth, altered taste perception, urinary hesitancy &retention, decreased sweating, predisposition to heat prostration, (Flushed, hot, dry, mad as the hatter)
Direct-Acting cholinergic agonists
bethanechol (Duvoid, Urecholine)
Indications for bethanechol
Treatment of nonobstructive postoperative and postpartum urinary retention, neurogenic bladder atony in adults and children >8y; diagnosis and treatment of reflux esophagitis in adults and used orally in infants and children for treatment of esophageal reflux.
Action of bethanechol
Acts directly on cholinergic receptors to mimic the effects of Ach, increase tone of detrusor muscles and causes emptying of the bladder.
Pharmacokinetics of bethanechol
Route - oral
onset- 30-90min
peak- 60-90 min
duration- 1-6 h
half-life of bethanechol
metabolism and excretion unkonwn, though to be synaptic.
adverse effects of bethanechol
abdominal discomfort, salivation, nausea, vomiting, sweating, flushing.
Indirect-acting cholinergic agonists
pyridostigmine (Mestinon) & donezpezil (Aricept)
Indications for pyridostigmine
managment of myasthenia gravis; antidote to neuromuscular junction blockers; increases survival after exposure to nerve gas.
Indications for donepezil
management of Alzheimer’s dementia, including severe dementia.