jacob hummel m.d. tulane university anesthesiology
TRANSCRIPT
*Objectives
*Know the different mechanisms of action for atropine, scopolamine and glycopyrrolate
*Clinical use of each of these drugs
*Effects on the cardiovascular, respiratory, cerebral, G.I. and other organ systems
*Disclosures
*This is a really short lecture but its brevity does not reflect the value of its content
*Antimuscarinics
*This term is more indicative of what these drugs accomplish as they are primarily blocking the effects of acetylcholine at the muscarinic receptors
*Antimuscarinics
*Primary use is prior or concomitant administration with anticholinesterases
*Crucial in the treatment of bradycardia
*Beneficial in the prevention of PONV
*Antisialogogues
*Structure and Binding
*Ester linkage essential for effective binding to the acetylcholine receptors, competitively inhibiting the binding of acetylcholine
*Different types of muscarinic receptors: neuronal (M1), cardiac (M2), and glandular (M3)
*Systemic Effects
*CARDIOVASCULAR
*Blockade of the muscarinic receptors in the sinoatrial node results in tachycardia
*Useful for reversing vagal reflexes
*Systemic Effects
*RESPIRATORY
*Inhibit secretions along the respiratory tract
*Relaxes bronchial smooth muscle ->
decreased airway resistance but increased dead space
*Systemic Effects
*CEREBRAL
*Range of effects, stimulation to depression
*Physostigmine reverses these occurrences
*Systemic Effects
*G.I.
*Decreased secretions and salivation
*Decreased peristalsis
*Lower esophageal sphincter pressure reduced
…better view, but more at risk for aspiration
*Atropine
*Potent effects on the heart and lungs
*Most efficacious for treating bradycardia
*Tertiary amine allows it to cross blood-brain barrier
*Derivative is ipratropium bromide and used to treat bronchospasm
*Use cautiously with heart disease, narrow angle glaucoma, BPH and bladder-neck obstruction
Give me the atropine, NOW!
*Scopolamine
*Similar dosing to atropine, 0.01-0.02 mg/kg with adult dose around 0.4 - 0.6 mg
*More potent antisialogogue than atropine
*Greater CNS effects
*Lipid solubility allows for the transdermal patch
*Don’t touch your eyes after you put a patch on someone!
*Glycopyrrolate
*Contains mandelic acid in place of the tropic acid seen in atropine
*Dosing is usually half of the atropine dosing and used for similar effects (bradycardia, antisialogogue, etc.)
*Quaternary structure prevents crossing of the blood-brain barrier
*No ophthalmic activity
*Potent antisialogogue
*Longer duration of action than atropine (2-4 hrs. vs 30 minutes)
*Case Discussion
*An elderly patient is scheduled for enucleation of a blind, painful eye. Scopolamine, 0.4 mg intramuscularly, is administered as premedication. In the preoperative holding area, the patient becomes agitated and disoriented
The only other medication the patient has received is 1% atropine eye drops
*…how do you treat and would you proceed with the case?
*Anticholinergic Poisoning
*Signs and Symptoms
*Agitation, delirium, unconsciousness
*dry mouth, tachycardia, atropine flush, atropine fever, and impaired vision
…antidote is physostigmine as it is the only anticholinesterase to cross the blood-brain barrier
*Proceed with the case?
*Elective Procedure
*Is patient optimally medically managed?
*Do symptoms resolve with intervention?