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74 Cards in this Set

  • Front
  • Back
scopalamine origin
atropine/belladonna found in
Datura plant (jimson)
anticholinergic effect?
Lowers the “rest and digest” of the parasympathetic by antagonizing acetylcholine receptor

acetylcholinesterase inhibitors.
anticholinergic uses?
Treatment for reflex-mediated bradycardia
Prophylaxis against anticholinesterase toxicity,(treatment for cholinergic crisis, cholinergic adjunct for curariform block)
Antisialagogue preanesthetic medication (not atropine)
Prophylaxis against arrhythmias induced by succinylcholine for intubation
Anesthesia adjunct (preanethesia) with an opioid
reduce excitement,
produce amnesia
protect against opioid-induced respiratory depression.
Prophylaxis against aspiration
Postoperative nausea and vomiting
local anesthetics block the?
Na channel
Parenteral ___________ is also indicated in conjunction with analgesics in cardiopulmonary bypass patients who cannot be deeply anesthetized because of the risk of severe hypotension or circulatory collapse
Other anticholinergic uses...
Anticholiesterase (cholinergic crisis), muscarine, organophosphate overdose
Opthalmic (mydriasis/cycloplegia)
Urinary Incontinence treatment - Darifenacin, M2 antagonist
Peptic Ulcer Treatment Adjunct
Irritable bowel syndrome
Motion Sickness
Asthma - ipratropium and tiotropium
Antidiarrheal (constituent of Lomotil)
Allergies (better options)
Constituent of nonprescription cold remedies
Management of Parkinson's Disease – Benzotropine
Treat antidopaminergic effects of metoclopramide
what causes mydriasis/cycloplegia?
anticholinergic for asthma?
ipratropium and tiotropium
anticholinergic for Management of Parkinson's Disease –
what can treat the antidopaminergic effects of metoclopramide?
Metoclopramide is a dopamine _____?
anticholinergics effect on lactation
Parasympathetic Effects of anticholinergics on eye, salivary gland, heart, lungs, pancreas, intestine and bladder
Eye: Contraction to give miosis and near vision
Salivary Glands: Secretion
Heart: Decreased HR, conduction velocity, contraction
Lungs: Bronchoconstriction
Pancreas: Increased insulin secretion
Intestine: Increased Motility and tone
Bladder: Sphincter relaxation and Detrosor contraction
Anti-cholinergic vs. Antimuscarinic?
The anticholinergics are anti-muscarinics more specifically
anticholinergic for COPD
Ipratropium – isopropyl atropine analog
The _____ is the natural occurring and the active compound but given as racemic mixture
anticholinergic SAR facts
These have the ester again – recognized by the acetylcholine receptor. Not recognized by acetylcholinesterase or any other esterase.
These structures have a chiral carbon.
tropic acid is in?
atropine (hyoscyamine) pka 9.9
mandelic acid is in?
glycopyrolate (robinul)
scopolamine pka
2 naturally occurring anticholinergics
scopolaine and atropine
2 synthetic anticholinergics
glycoryrrolate and ipratropium
are anticholinergis acids?
NO, even though they have an acidic portion
As bases, _________ are often formulated as water soluble conjugate acids at slightly acidic pHs.
Parasympathetic Muscarinic Postganglionic (effector) receptor sites: [4]
autonomic effector cells (smooth muscle)
cardiac muscle
Sinoatrial/atrioventricular nodes
exocrine glands.

non-comp or comp?
Competitive antagonists

Block acetylcholine from binding.

G- protein will not be released and will not activiate second messenger
anticholinergic effect on pre synaptic neruon...
Have no effect on the pre-synaptic neuron. Acetylcholine will continue to be released
M1 receptor....
2nd messenger effect
clinical effect
clinically selective drug?
Phospholipase C Stimulation
H+ secretion
M2 receptor....
2nd messenger effect
clinical effect
clinically selective drug?
Heart,CNS,Airway Smooth Muscle
Adenylate Cyclase Inhibition
M3 receptor....
2nd messenger effect
clinical effect
clinically selective drug?
Salivary Glands
Airway Smooth Muscle
Vascular Endothelial Cells
Phospholipase C Stimulation,Salivation
M4 receptor....
2nd messenger effect
clinical effect
clinically selective drug?
CNS, Heart

Adenylate Cyclase Inhibition
M5 receptor....
2nd messenger effect
clinical effect
clinically selective drug?
Phospholipase C Stimulation
the anticholinergic/antimuscarinics that we use affect what M recoptors?
all M types
Dose variability
Lower dose

Bronchial/salivary secretions (M3)
heart and eye effects (M2)
control GI and genitourinary tract
inhibition of H+ secretions (M1)

Higher dose

So If giving higher doses to control H+ then will have side effects of the other lower concentrations. If giving low dose to minimize salivary secretions, might not see other effects
Atropine dose variablity examples.....from low to high dosage

same trend with all 3 compounds
0.5 mg slight cardiac slowing/some dryness of mouth/inhibition of sweating
1.0 mg dryness of mouth/thirst/acceleration of heart/mild dilation of pupils
2.0 mg rapid heart rate/palpitation/marked dryness of mouth/dilated pupils/blurring of near vision
5.0 mg all above worse/difficulty is speaking and swallowing/restlessness and fatigue/headache/dry and hot skin/ reduced intestinal peristalsis
10+ mg all above worse/ pulse rapid and weak/iris obliterated/vision very blurred/skin flushed, hot and dry and scarlet/ataxia/restlessness and excitement/hallucinations/delirium
What would govern between atropine, glycopyrolate or scopolamine?
unwanted side effect or speed of onset
most sedative

most scopalamine

no sedative effects with glycopyrolate
most antisialogogue?

most scopolamine

least atropine
most HR effect?


least scoplomine
most smooth muscle relaxation?

most atropine/glycopyrolate

least glycopyrolate
most mydriasis/cycloplegia?


least-non with glycopyrolate
motion sickness tx most?


least-none with glycopyrolate
gastric acid reduction-most?

all equal
agent with fetal HR effect
maybe scopolamine- only
agent for glaucoma patient?
must be careful with scopolamine dosage so atropine maybe better choice
agent for pregnant pt?
Although atropine and scopolamine can both cross placenta, no change for atropine (scopolamine has not been tested) also no change for glycopyrrolate – expected since not very lipophylic.
why does scopolamine have more sedative effects?
higher PKA

Although scop and atropine are tertiary amines, at physiological pH, more of atropine is ionized so less concentration to CNS.
agent for bradycardia tx?
atropine because faster onset.

This increased heart rate is an anticholinergic effects but remember for later chapters, this is also an adrenergic agonist effect (same effect observed for epinephrine)
what causes scopolamine/MS sedative effects?
Depress RAS to give sedation
Depress other areas of brain to give amnesia
Antisialagogue effects
Scopalamine w/ sedation Glycopyrrolate w/o
Added to nonprescription cold remedies to stop upper airway secretions
Increased Heart Rate, Tachycardia (Atropine-fast onset))
Treatment for reflex-mediated bradycardia
Effect primarily at sinoatrial node
Less change at extremes of age
Lower dose with volatile anesthetic
Glycopyrrolate may be best choice for patients at risk for cardiovascular complications (faster offset)
most potent?
scopolamine, then glyco
how does atropine the HR?
Block Ach binding at sinoatrial node. Higher doses for those with lower vagal tone. Young adults with high vagal tone show most effect. Volatile anestheics depress vagal center so need less drug
Relax Smooth Muscle (Glycopyrrolate)
Decrease airway resistance/increase dead space
Biliary and ureteral Smooth Muscle Relaxation
Modest antispasmodic
wont overcome opioid effects on sphincter of Oddi but will on ureteral contraction.
Reduces tone of funcus of bladder giving urinary retention
Gastrointestinal Tract
Descrease peristalsis increases transit time
High drug concentration required
Mydriasis /Cycloplegia
Block constriction of pupil and contraction of ciliary muscles.
7-14 day recovery time
Care must be taken with Glaucoma patients (acute angle effects)

End result is dilated pupils – reputed to be why Cleopatra and Renaissance women used belladonna on their eyes to look more alluring. I was give Ipratropim bromide and instructed to thoroughly wash my hands after using inhaler because if I touched by eyes, I would be unable to see clearly for a week.
choice for NO CNS effects?

no cardiac effects if arelolized
Alternative is Ipratropium bromine (N-isopropyl derivative) which is often used for COPD. Ipratropium could also be used against brochoconstriction due to tracheal intubation since this seems to be an acetylcholine mediated response. Ipratropium and a b-agonuist such as albuterol is good treatment for COPD
Gastric H+ Secretion notes
Requires high doses and will see other effects
Prevention of Motion Sickness
best choice?
Transdermal scopalamine is best choice

Transdermal – low dose minimizes other effects that might see like sedation. Must apply at least 4 hours ahead of time. Blocks trasmission of signals to the medulla that come from overstimulation of the vestibular apparatus. Some say because lowers salivation. Need again be careful of any transfer to eye after handeling of the patch
Presynaptic inhibitory M1 receptor (feedback blocker) (antagonistic effect)
vagal nerve endings
Sympathetic effects (allows more ach to be released)
Adrenergic neurons
Sympathomimetic effects (we can cause the release of nor-epi, which is the natural ligand for adrenergic neurons)

Inhibition of this presynaptic receptor prevents the feedback inhibition of acetylcholine release. More acetylcholine is released and my in fact see paradoxical slowing of the heart rate.

Also can cause release of norepiniphrine so can get sympathetic effects (fight and flight)

This response can happen with low doses (parasympathetci) paradoxical lowering
Tertiary amines rapidly absorbed/distributed
shown to cross placenta (tachycardia in fetus)
Can cross BBB (CNS effects)
Quaternary amines poor absorption/distribution

Tertiary amines oral absorption in GI (not stomach why?) can be absorbed through mucosa
Quat amines (glycopyrrolate) – if given orally, only about 10 – 25% absorbed

Quaternary amines do not cross BBB but tertiary can. This means the teriary amines can have some CNS activity. At different doses see sedation and excitation.
Protein Binding
Atropine - Moderate (
Scopalamine – Low (BEST DISTRIBUTED)
Glycopryrolate - (worst distributed/absorbed)
% ionization of Glycopyrolate?
100% ionized at ANY ph

Scop is more unionized at phys PH, therfore more will cross the BBB.
Glyco 15-20% bioavail with PO
99% Scopalamine/80% Atropine/20% Glycopyrolate
Hepatic Metabolism
Atropine hydrolyzed to Tropine and Tropic Acid (ester bond-hydrolysis in liver)

Although atropine is hydrolyzed, this cannot be done with plasma esterases in humans though animals have the correct esterase.
Scopolamine is the least ionized

The purpose of metabolism is to make things more water soluble
The dose of glycopyrolate is about ______ that of atropine and scopolamine
Atropine facts
dose 0.01 – 0.02

onset comparable to Glycopyrollate

duration Oral: 4–6 hr Parenteral: Brief

elimination 2.5 hr
(~20% unchanged)
scopolamine facts
dose 0.01 – 0.02

onset Oral: 30–60 Parenteral: 30

duration Oral: 4–6 hr Parenteral: 4 hr 8 hr

elimination Renal
(1% unchanged)
glycopyrolate facts
dose 0.005-0.001
*about _

onset IM/SC: 14-30 IV: 1
Duration Antisialagogue:
Up to 7 hr Vagal blocking:
2–3 hr

elimnation 1.7 hr
(80% unchanged)
Side Effects
CNS – Central Anticholinergic Syndrome
Low doses atropine mild stimulating
Higher doses are depressant
Gastroesophageal Reflux
Decreasing tone of lower esophageal sphincter decreases barrier.

Sopalamine>atropine have seen glycopyrrolate with IV before induction of anesthesia
Restlessness, confusion, hallucinations, combative (children), somnolence, unconsciousness especially in elderly but also those under age 13
Overdose (Central and Peripheral Anticholinergic Syndrome)

mostly seen in extremes of age
Blurred vision, continuing, or changes in near vision clumsiness or unsteadiness confusion difficulty in breathing dizziness drowsiness, severe dryness of mouth, nose, or throat, severe fast heartbeat fever “atropine fever” (sweat inhibition) hallucinations muscle weakness, severe Seizures slurred speech tiredness, severe unusual excitement, nervousness, restlessness, or irritability unusual warmth, dryness, and flushing of skin
Respiratory paralysis with quaternary compounds due to curare-like effects
atropine fever from?
inhibition of sweating
Overdose Treatment
Physostigmine (Antilirium)
sometimes Neostigmine

Physostigmine/neostigmine – these acetylcholinesterase inhibitors will allow for the increase of acetylcholine at the receptor sites. This will increase concentration at the muscaric receptor and cause a reversal.
Physostigmine best for CNS effects because physo can cross BBB. Neostigmine cannot as well.
Low dose IV and repeated doses since pysostigmine is metabolized fairly rapidly

Barb or benzo for the delirium
Norepinephrine for increasiing blood pressure
Other Drugs/same receptor
Edrophonium – M2/M3 competitive antagonist

* Remember, the depolarizing and non-depolarizing muscle relaxants do block acetylcholine receptors but the nicotinic receptors

Edrophonium was acetylcholinesterase inhibitor but also seems to have some mild anti-muscarinic effects as well.

Antihistimines have anticholinergic and that is why helpful in cold remedies.