Anticholinergics Flashcards
brand name of atropine
atropine
how is atropine supplied
- 4 mg/mL (vial)
0. 1 mg/mL (1mg ER injector)
classification of atropine
tertiary amine
alkaloid of belladonna plant
MOA of atropine
Competitive antagonist
Combines reversibly with muscarinic cholinergic receptors to block the action of Ach at parasympathetic postganglionic sites.
*crosses BBB easilty
*combines to receptor without leading to the cell membrane permeability, inhibition of adenylate cyclase and alteration in calcium response that would normally lead to a cholinergic response in the presence of Ach.
Little effect at nicotinic cholinergic receptos
Weak analgesic action
M1 receptor function
M1- CNS stomach
M2 receptor function
M2- airway smooth muscle and the heart
M3 receptor function
M3- CNS, airway smooth muscle, glandular tissues and vascular endothelial cells.
M4 receptor function
M4- CNS
M5 receptor function
M5- CNS
uses of atropine
preopmedication to inhibit salivation and secretions
treatment of symptomatic sinus bradycardia
AV block
antidote for anticholinesterase poisoning, organophosphate insecticides
decrease side effects of anticholinesterases (edrophonium and neostigmine)
ophthalmic- mydrasis and cycloplegia for examination
dose of atropine for neuromuscular blockage reversal
IV 25-30 mcg/kg 30-60 seconds before neostigmine or 7-10 mcg/kg 30-60 seconds before edrophonium
is atropine effective with heart transplant patients for increasing the HR
NO- bradycardia may unresponsive
dose of atropine for treating bradycardia
IV 0.5 mg q 3-5 minutes
not to exceed a total of 3 mg
max dose of atropine for bradycardia
3 mg or 0.4 mg/kg
dose of atropine for salivation inhibition preanesthesia
IM IV Subq
0.4-0.6 mg 30-60 minutes preop
q4-6 hours
what effect can doses of less than 0.5 mg of atropine have on the bradycardic patient
paradoxical bradycardia
what is given along with atropine during organophosphate poisoning to decrease secretions
pralidoxime
cholinesterase reactivator
what actions does atropine reverse?
muscarinic but NOT nicotinic effects of organophosphate poisoning
onset of atropine
about 1 minute
peak of atropine
?
duration of atropine
30-60 minutes IV
2-4 hours IM
metabolism of atropine
hepatic via enzymatic hydrolysis to inactive metabolites
effects may be prolonged with severe hepatic impairment
half life of atropine
2-3 hours
much longer in children
elimination of atropine
renal (30-50%)
unchanged drug and metabolites
adverse CV effects of atropine
Cardiac arrhythmias, flushing, hypotension, palpitations, tachycardia.
(not for 2degree type 2 or 3degree AV block). Caution with HF, CAD, tachyarrhythmias, → MI
low doses can cause transit decrease in HR mediated through an unkown mech
Larger doses increase HR by blocking bagal effects on M2 receptors on the SA node. High doses of atropine cause skin vasodilation.
adverse CNS effects of atropine
ataxia, coma, delirium, disorientation, dizziness, drowseiness, excitement, hallucination, HA, insomnia, nervousness (treat with physostigmeine)
adverse derm effects of atropine
anhydrosis, scarlatiniform rash, skin rash, urticarial,
adverse GI effects of atropine
decreased motility from esophagus to colon,
Ageusia loss of taste,
bloating constipation, delayed gastric emptying, nausea, paralytic ileus, vomiting, zerostomia,
LES sphincter relaxation, decreased barrier pressure and an increased in incidence of reflux from stomach to esophagus
adverse GU effects of atropine
urinary hesitancy
urinary retention
NMS adverse effects of atropine
laryngospasm
weakness
adverse respiratory effects of atropine
decreased volume of secretions from the nose, mouth, pharynx, and bronchi, decreases airway resistance via relaxation of bronchi and bronchiolar smooth muscle.