Anti-Cholinergics Flashcards
Atropine
Atropine
Class:
anticholinergic, also a tertiary amine so it does cross the BBB
MOA:
Competitive agonist for acetylcholine at muscarinic receptors, blocking acetylcholine and leading to its effects.
@M1 It increases HR
@M2 it bronchodilates, decreases secretions
@M3 decreases GI secretions
Uses:
- Increases HR, best-anticholinergic for bradycardia
- Tx PONV by blocking ach at CRTZ
- Tx biliary spasm r/t opioids
- Used with edrophonium for reversing NMB
Pk:
onset: Immediate, 1 min
Peak action within 1-2 minutes
DOA: 1 hours
E1/2t 1-2 hours
Hydrolyzed to tropine and atropic acid, excreted 18% unchanged in urine
Dose:
- 01 mg/kg with edrophonium for reversal of NMB
- 04 to 1 mg/kg for bradycardia
SE:
Increase HR, bronchodilation, decrease secretions
sedation/restlessness/confusion
central anti-cholinergic syndrome
Urinary retention / constipation / decrease GI motility
Xerostomia / mydriasis
can inhibit sweating
C/I
- Glaucoma
- Mobitz II / HB
- caution in CAD
- fever
- myasthenia gravis
- careful with concurrent administartion of other drugs with anti-cholinergic properties such as:
- butyrphenones
- phenothiazines
- TCAs
Glycopyrolate
Glycopyrolate
Class:
anti-cholinergic, also a quartenary ammonium compound, does NOT cross BBB
MOA:
Competitive antagonist for acetylcholine at muscarinic receptors. Blocks the action acetylchline at muscarinic receptors
@M1 leads to increase in HR
@M2 leads to bronchodilation and decrease secretions
@M3 leads to decrease in gastric secretions
Uses:
- Tx bradycardia
- Anti-sialogogue
- Reversing NMB with neostigmine
- Tx PONV via decreasing of gastric secretions
- Tx bronchoconstriction
- Best choice for elderly r/t decrease r/f central anti-cholinergic syndrome.
Pk:
Onset: 3 minute
Peak action reached within 3-5 minutes
DOA: 2 hours
E1/2T: 1 hour
VD: 0.4 L/kg
PB: 40%
Liver metabolism and 85% excreted unchanged in urine
Dose:
with neostigmine, 0.01 mg/kg
bradycardia/anti-sialogogue: 0.1 mg/kg.
SE:
- increased HR, bronchodilation.
- urinary retention/ xerostomia/ constipation
- decrease GI motility
C/I:
- glaucoma
- caution in CAD/HTN/CHF
- caution in renal failure , caution in elderly
- Myasthenia gravis
- avoid concurrent use with drugs that have other anti-cholinergic effects (phenothiazine, butyphenones, TCAs)
Scopalamine
Scopalamine
Class:
anticholinergic, also tertiary amine so it crosses BBB
MOA:
Competitive antagonist for acetylcholine at muscarinic receptors, decreases PSNS tone.
@M1 increase HR
@M2 decrease secretions, bronchodilation
@M3 decrease gastric acid secretions
Used:
as an anti-sialogogue
for motion sickness
potent anti-emetic
sedation
bronchodilation
biliary spasm
Pk:
onset: 10 minutes
DOA: 2 hours
E1/2T: 4 hours, may least 3-7 days
PB: 40%
Vd: 0.4 l/kg
metabolized in liver, excreted less than 1% in urine
Dose:
0.3 to 0.6 mg IV q4-6 hours
SE:
Increase hR/BRonchodilation
Urinary retention/constipation/xerostomia/decrease GI motility
Sedation/confusion/restlessness
central anti-cholinergic syndrome
orthostatic hypotension
mydraisis, increase IOP
C/I
glaucoma
HTN/CAD/CHF
Gi/Gu obstruction
caution in MG
decreases the effect of levodopa/acetaminophen.
Avoid concurrent use with other drugs with anti-cholinergic properties such as TCAs, phenthiazines, buytyrphenones.
