Parasympathomimetics Flashcards
Cholinergic agonist
Pupil constrict, heart decrease, vasodilation, bronchoconstriction, increase GI, urinary bladder constriction
Cholinergic receptor agonists chemicals
Acetylcholine, methacholine, carbachol, pilocarpine, betanechol
Acetylcholinesterase inhibitors
Edrophonium (tensilon), Physostigmine (Eserine), Neostigmine (prostigmin), Pyridostigmine (mestinon), Rivastigmine (excelon), Donepezil (aricept), Galantamine (razadyne), insecticides, nerve gases
Cholinergic receptor agonists info
Drugs that directly activate either nicotinic or muscarinic receptors
Many drugs that have anticholinergic activity effect?
patients with glaucoma, BPH, Alzheimer’s
Clinical uses of cholinergic receptor agonists
Very limited because of side effects
Open angle glaucoma
permits opening of canal of schlemm when ciliary muscle constricts for aqueous drainage, most common form, responds to therapy
Closed angle glaucoma
a physical obstruction of the canal, even muscle contraction the canal cannot be opened, does not respond to medication, can be emergency
Acetylcholinesterase Inhibitors
Blocks acetylcholinesterase will increase concentration of ACH in synapse, similar result of receptor agonist; increase GI, relax bladder sphincter
Adverse drug reactions of acetylcholinesterase inhibitors
SLUD; salivation, lacrimation, urination, defecation; increase sweating, bradycardia, hypotension, miosis
Adverse drug reactions of acetylcholinesterase inhibitors
SLUD; salivation, lacrimation, urination, defecation; increase sweating, bradycardia, hypotension, miosis
Eprophonium (tensilon)
rare, primarily used for diagnosis myasthenia gravis, given IV, short acting, pt with mg will have improvement when given this drug
pyridostigmine (Mestinon)
Reversible, for treatment of myasthenia gravis, PO
Neostigmine, Physostigmine
Used by anesthesiologists for reversal of neuromuscular blockers, IV or IM; reverse paraysis
Pralidoxime (Protam)
a cholinesterase reactivator, used for pesticide or nerve gas poisoning, most effective if given within hours of exposure, rarely used
Atropine
Given IV, can be used for reversal of any AchE inhibitor
Alzheimer’s disease
loss of cholinergic neuronal activity has been identified as a contributable cause of cognitive decline, AchE have become mainstay in therapy, hope to slow progression
Tacrine (Cognex)
first AchE inhibitor available, still on market but never used; causes liver damage
Tacrine (Cognex)
first AchE inhibitor available, still on market but never used; causes liver damage
Donepezil (aricept)
mild-severe alzheimer’s (dif dose), no dose adjust for hepatic or renal, ADR’s: incomnia, weight loss
Galantamine (Razadyne)
mild to moderate Alzheimer’s, PO only, dose adjust for renal and hepatic, Drug Interaction increase activity of galantamine
Rivastigmine (Exelon)
Mild-severe Alzheimer’s (same dose), Parkinson’s dementia (same dose), adjust for renal and hepatic; transdermal thought to be beneficial for compliance and less adr’s
Parasympatholytics are more commonly called
anticholinergics, very common
Action of anticholinergics
act as competitive antagonists at muscarinic receptor site on post ganglionic neurons
Types of parasympatholytics
Atropine, scopolamine (Transderm), Dicyclomine (bentyl), hyoscyamine, Glycopyrrolate (Robinul)
Anticholinergic eye medications
Atropiine, cyclopentolate, phenylephrine (cyclomydril), tropicamide (Midriacyl)
Anticholinergic heart uses and medications
For short term management of bradycardia; Atropineand glycoprrrolate (Robinul)
There are no clinical uses for which anticholinergic
Sweat gland and blood vessels
Anticholinergic salivary gland uses and medication
inhibits secretion of saliva; Atropine and glycopyrrolate
Anticholinergic urologic use
Urinary incontinence; Tolterodine, Oxybutynin, solifenacin, darifenacin, trospium, fesoterodine
Oxybutynin (ditropan)
manage overactive bladder, no dose adjust for hepatic or renal, ADR: dry moouth, dizziness, constipation
Oxybutynin (ditropan)
manage overactive bladder, no dose adjust for hepatic or renal, ADR: dry mouth, dizziness, constipation
Tolterodine (Detrol)
long acting, overactive bladder, adjust for renal and hepatic; ADR: dry mouth, HA, constipation; some drug reaction
Solifenacin (Vesicare)
overactive bladder, caution with renal and hepatic, ADR: dry mouth, constipation; DI: grapefruit juice; appealing for dementia pts
Darifenacin (Enablex)
overactive bladder; no adjust for renal, adjust for hepatic; ADRs: dry moouth, HA, constipation; preferred with dementia
Trospium (sanctura)
Overactive bladder, adjust renal, none for hepatic; ADR: dry mouth; VERY expensive
Fesoterodine (Toviaz)
Overactive bladder; adjust renal and liver; ADR: dry mouth; some DI, Very expensive
Anticholinergic respiratory use and medication
use for asthma, COPD; atropine, glycopyrrolate
Ipratropium (atrovent)
asthma, COPD; inhaler or nebulizer; no renal or hepatic, no DIs, no ADRs; Frequent dosing because of short half life
Tiotropium (spiriva)
Long acting, COPD only, once daily, dry powder inhaler; new to market, $$
Aclidinium (Tudorza)
Only COPD, twice daily, new product $$
Aclidinium (Tudorza)
Only COPD, twice daily, new product $$
Anticholinergic GI uses and medication
cramping, diarrhea, IBS; dicyclomine, hyoscyamine
Dicyclomine (Bentyl)
Antispasmodic, IBS and cramping; Adr: drowsiness, dizziness, dry mouth, blurred vision; old drug, cheap
Hyoscyamine (anaspaz, Levsin)
GI, preferred for peds, common adrs, old, cheap
Anticholinergic CNS uses
restores balance of neurotransmitters, Parkinson’s, prevent motion sickness
Benztropine (Cogentin)
use for EPS, anti-psychotics, ADR: agitation, HA, constipation, dry mouth, Tachycardia etc, old cheap
Trihexyphenidyl (artane)
CNS, ADRs: significant constipation, tachy, etc, old, cheap
Scopolamine (transderm)
Motion sickness, patch, OTC, ADRs: drowsiness, blurred vision
Glycopyrrolate (Robinul)
Neuromuscular, IV ADR: HA, vomiting, dry mouth, constipation
