Final Exam Review Flashcards
direct acting cholinomimetics
-drug binds and activates muscarinic or nicotinic receptors
-mimics effects of ACh on peripheral organs
Indirect-acting cholinomimetics
-inhibits AChE
-drug that amplifies the effects of endogenous ACh
Nicotine
nicotinic receptor
varenicline
nicotinic receptor
Bethanechol
-muscarinic agonist
-treats atony and urinary retention
-side effects: diarrhea and urinary urgency
Carbachol
-nicotinic and muscarinic agonist
-glaucoma
pilocarpine
-muscarinic agonist
-glaucoma
-increase salivary secretion
CEVIMELINE
-muscarinic agonist
-for dry mouth associated with Sjogren syndrome or radiation damage
organophosphates
-indirect acting cholinomimetics
-very long acting
Pyridostigmine
-indirect acting cholinomimetics
-intermediate to long acting
Edrophonium
-indirect acting cholinomimetics
-short acting
Muscarinic agonists
-act at M2 and M3 receptors
-parasympathetic
M3 receptor activation
-stimulates smooth muscle contraction
-gland secretion
M2 receptor activation
decreases heart rate
effects of muscarinic agonists in glaucoma
-pupillary circular and ciliary muscle contraction
(miosis and cyclospasm)
-open angle of the anterior chamber
-facilitate outflow of aq humor
-reduce IOP
Physostigmine
-indirect acting cholinomimetics
-intermediate to long acting
-glaucoma
Atony
-paralysis of the stomach, bowel, bladder following surgery
Urinary retention
postoperative or postpartum or secondary to spinal
cord injury or disease (neurogenic bladder)
Neostigmine
-indirect acting cholinomimetics
-intermediate to long acting
-treats atony and urinary retention
-side effects: diarrhea and urinary urgency
Sjögren syndrome
-autoimmune disease where glands are attacked by antibodies
-causes dry mouth and dry eyes
toxicity of muscarinic agonists
-cyclopsam of accommodation
-bronchospasm in asthmatics
-diarrhea
0urinary urgency
0sweating
-vasodilation (hypotension: M3 activation)
-reflex tachycardia
-bradycardia (large dose, direct M2 activation)
AChE inhibitors MOA
-increase levels of AChE at synaptic cleft and neuroeffector junctions
-Enhance responses in organs
innervated by parasympathetic
nerves
how do cholinesterase inhibitors treat glaucoma?
-contract ciliary body
-facilitate outflow of aq humor
-reduce IOP
Edrophonium
diagnostic test for myasthenia gravis
long term therapy treatments for myasthenia gravis
-pyridostigmine
-neostigmine is an alternative
neuromuscular blockade
-produced as an adjunct to surgical anesthesia
-using NONDEPOLARIZING neuromuscular relaxants such as PANCURONIUM
pancuronium
-NONDEPOLARIZING neuromuscular relaxant used in surgery
-form of paralaysis
how do you reverse neuromuscular blockade(surgical paralysis)?
-with cholinesterase inhibitors
-neostigmine and edrophonium
treatment for antimuscarinic (atropine) poisoning
-physostigmine (AChE inhibitor)
-works in CNS and peripheral
-reverses signs of muscarinic blockade
Anti-cholinesterase toxicity: muscarinic excess
-miosis
-salivation
-bronchial constriction
-vomiting
-diarrhea
Anti-cholinesterase toxicity: depolarizing neuromuscular blockade
respiratory arrest
Anti-cholinesterase toxicity: CNS involvement
-cognitive disturbances
-convulsions
-coma
Anti-cholinesterase toxicity: cause of death
respiratory failure
treatment of AChE toxicity
-atropine: antagonizes muscarinic receptor sites in both CNS and peripheral organs
-Pralidoxime(2-PAM): cholinesterase regenerator (prevent aging)
Therapy considerations for AChE toxicity
-early treatment is important
-continue drug therapy fir a week or longer
Anticholinesterases for myasthenia gravis testing
Edrophonium (short acting)
Anticholinesterases for myasthenia gravis therapy
-neostigmine: intermediate
-pyridostigmine: long acting
Anticholinesterases for reversal of NM blockade of nondepolarizing neuromuscular relaxants
-edrophonium
-neostigmine
-pyridostigmine
Anticholinesterases for reversal atropine (antimuscarinic) poisoning
-Physostigmine
-lipid soluble
-reverse both central and peripheral muscarinic blockade
Anticholinesterases for glaucoma
-Physostigmine
-lipid soluble
Anticholinesterases for bowel and urinary atony(after surgery or spinal cord injury)
-Neostigmine
Anticholinesterase effects on Neuromuscular junction
-stimulate skeletal muscle contraction
-low dose: prolong and intensity contraction
-high dose: FASCICULATION
-toxic dose: muscle paralysis
Anticholinesterase effects on the eye
-miosis (pupillary circular Ms. Contraction)
-cyclopsam( due to contraction)
-decrease IOP
-
Anticholinesterase effects on the GI
-Increase GI motility: relax sphincter
-increase GI secreation
-side effects: DIARRHEA
Anticholinesterase effects on the genitoururinary tract
-increase detrusor contraction
-relax sphincter
-side effects: URINARY URGENCY
Anticholinesterase effects on the heart/blood vessel
-Side effect: bradycardia(M2 activation)
-no effect on blood vessel
antimuscarinic MOA
-reversible blockade of cholinomimetic action at muscarinic receptors
-m1-m5
anti-muscarinics for motion sickness
Scopolamine
-lipid soluble
anti-muscarinics for retina examination and how long they last
-atropine: long
-scopolamine: long
-homatropine: short
-cyclopentolate: short
-tropicamide: SHORTEST PREFERRED IN PATIENTS WITH NARROE ANTERIOR CHAMBER
anti-muscarinics to prevent synechia formation (tissue adhesion)
-homatropine
-long acting
anti-muscarinics for asthma and COPD
-ipratropium: short
-tiotropium: longer
-aclidinium: longer
-umeclidium: longer
anti-muscarinics for routine preoperative medications (Prevent laryngospasm and
bronchial secretion caused by
inhaled anesthetics)
-atropine
-scopolamine: also has sedative effect
anti-muscarinic effects on the eye
-Mydriasis: pupil dilation
-cycloplegia: relaxation of cilliary muscle
-SIDE EFFECTS: BLURRED VISION (BLIND AS A BAT), INCREASED IOP, DRY EYES
anti-muscarinic effects on the respiratory system
-bronchodilation
-reduce bronchial secretion
anti-muscarinic effects on the GI tract
-reduced motility
-reduced salivation
CONSTIPATION
anti-muscarinic effects on the urinary tract
-relax bladder wall
-side effects: URINARY RETENTION IN BPH PATIENTS
anti-muscarinic effects on the heart
-TACHYCARDIA (due to block of M2 activation in the SA node)
anti-muscarinic effects on the glands (sweat, salivary, lacimal…)
-reduced secretions
-HYPERTHERMERIA(atropine fever in children, hot as hare)
-dry as bone