What do anticholinergic do?
Antagonize effects of ACh at muscarinic receptors
Where do anticholinergic drugs mainly work?
- Heart
- Salivary glands
- GI
- GU
anticholinergic drugs can be classified as what 2 things? and name the main drugs in the class.
- Natural tertiary amines (Atropine & Scopalamine)
- semisynthetic quarternary amines (Glycopyrrolate)
Tertiary amines have what characteristics? Quaternary amines?
- Neutral charge will cross BBB and Placenta
- Positive charge will not cross BBB and placenta
How do anticholinergic drugs work?
- Competitive agonists
- Reversibly bind with muscarinic receptor and prevents ACh from binding
Muscarinic cholinergic receptors have 5 subtypes, what are they?
- M1 = CNS and stomach
- M2 = Lungs and Heart
- M3 = CNS, airway, smooth muscle, glandular tissue
- M4 = CNS
- M5 = CNS
How do you overcome the effect of anticholinergic drugs?
-Increase ACh
Which of the muscarinic receptors are most sensitive?
=M3>M2>M1
= A dose to affect M1 will also affect M2/3
At small doses all anticholinergic drugs can produce what and why?
- Decreased HR
- Direct agonist effects
Out of all the anticholinergics, scopolamine has the greatest effect on what 4 things.
- Sedation
- Antisialagogue
- Mydrasis (pupil dilation)
- Prevent motion induced nausea.
Which anticholinergic drug has the greatest effect to increase HR?
-Atropine
What type of anticholinergic can be used in the oral form?
-Tertiary (atropine & scopolamine)
What is the onset time and duration of action for atropine and glycopylorate?
- Atropine onset = 1 minute
- Glycopyrrolate onset = 2-3 minutes
- Both of duration of 30-60 minutes
Because they are lipid soluble _______ amines will penetrate the CNS while _______ will not.
- Tertiarry (atropine & scopolamine)
- Quarternary (glycopyrrolate)
How does scopolamine produce sedation? and how is it different than versed?
- Decrease activity to the RAS
- Has retrograde amnestic properties
Which anticholinergic can cause delayed arousal in the 1st 30 minutes after anesthesia?
-Atropine
What problems can anticholinergic cause when used as a sedative?
- Restlessness to somnolence
- Delayed awakening w/ elderly
- Inhaled anesthetics can potentate CNS effects
How do you reverse the sedative effects of anticholinergics?
Physostigmine
anticholinergic should be used with caution in which two patient types?
- Glaucoma (Icrease IOP)
- Preggos (cross placenta)
Put the 3 anticholinergic drugs in order of potency for antisialagogues?
- Scopolamine 3x more potent than atropine
- Glyco - 2x more potent than atropine
What drug should be used if you want antisialagogue and sedation? Just antisialagogue?
- Scopoalmine
- Glycopyrrolate
What drug is used to blunt vagal response in pediatric patients upon intubation?
-Atropine
What is the drug of choice for intraop bradycardia? and how does it work?
- Atropine
- Blocks ACh on SA node
How do anticholinergic drugs bronchodilate? and how is it given?
- mostly medium/large airways
- Antagonism of ACh effects on airway smooth muscle
- Given via aerosol
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