Broad Class
Antisialagogue
Antivertigo
Pharm class
Anticholinergic / Antimuscarinic
Structural Considerations
Tertiary Amine
Naturally occuring belladonna alkaloid
MOA
Primary Action: Competetive antagonist of ACh at parasympathetic muscarinic receptors
Also antagonizes histamine and serotonin
Effects on vestibular apparatus
Indications / Clinical Uses
Decreases secretions
PONV
motion sickness/vertigo
dilate pupils and cycloplegia
unstable trauma pt
sedation/amnesia
Dosing IV/IM
0.3 - 0.65 mg (both)
Trandermal patch dosing
1 mg postauricular
IV onset
1-3 mins
IM onset
30-60 mins
Transdermal onset
2-3 hours
IV duration
30-60 mins
IM duration
4-6 hours
CV effects
Paradoxical: may decrease HR (especially low doses 0.1 - 0.2 mg)
CNS
Depressant effects
amnesia
toxic psychosis (especially in elderly)
dizziness
Mydriasis
blurred vision (cycloplegia)
anisocoria (different pupil sizes)
Patch teachings?
Take off patch in 24 hours, wash hands, and DO NOT touch eyes
Contraindications
Narrow-angle glaucoma
Population considerations: Elderly
Toxic psychosis
Primary Concern
Anticholinergic Syndrome (Treat with Physo)
Drug-Drug interactions
Opioids increase vestibular sensitvity thus counteracting therapeutic antivertigo effect
Metabolism
Primarily Liver
- hydrolysis and conjugation
Elimination
Primarily: Renal
- 90% in urine
- small amount excreted unchanged
minor biliary excretion
Elimination Half-life
2-4 hours
- CNS effects may persist longer due to central receptor binding and redistribution
Clearance Rate
1.2-1.5 L/min
High Hepatic ER