Cholinergic Agonists and Anticholinergic Flashcards

1
Q

AUTONOMIC NERVOUS SYSTEM

A
SympatheticAdrenergic 
Neurotransmitter
Norepinephrine
Epinephrine
Dopamine

Fight & Flight

ParasympatheticCholinergic
Neurotransmitter
Acetylcholine

Rest & Digest

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2
Q

Sleepy chicken

A

Sleepy chicken
Cholinergic
Cholinergic agonist
Parasympathomimetic

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3
Q

Bear

A

Bear
anticholinergic
Parasympatholytic

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4
Q

Negative feedback loop

A

natural process
fight of flight stimuli=> release of catecholamines

activates adrenergic receptors
a1
b1
b2

high level of catecholamines activating a2=>
stops adrenergic system

rest and digest stimuli=> release of acetycholine

activates muscarinic receptors

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5
Q

Drugs

A

adrenergic agonists BEAR

adrenergic antagonists CHICKEN

cholinergic CHICKEN

anticholinergic BEAR

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6
Q

Source of side effects:

A

ACh works in the parasympathetic system as well as in the somatic (efferent) receptors

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7
Q

Cholinergic Agonists(Parasympathomimetics)

A

Drugs that stimulate Parasympathetic NS

Mimic parasympathetic neurotransmitter acetylcholine (ACh)

Cholinergic receptors
are not just in autonomic NS;
they are also in somatic NS (see previous slide)

Muscarinic
Nicotinic

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8
Q

Muscarinic receptors

A

Located on smooth muscles and myocardium
(autonomic or involuntary muscles/glands)

Stimulated by ACh

Muscarinic receptors affect smooth muscle and cardiac muscle

Muscarinic
(smooth muscle and heart are suppressed by ACh)

CNS (is stimulated by ACh)

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9
Q

Nicotinic Receptors

A

Located on skeletal muscles
(somatic or voluntary muscles)

Stimulated by ACh

We need to know this to understand side-effects and drugs used for MG

Nicotinic receptors affect skeletal muscles contraction

Nicotinic (MS voluntary muscles is stimulated by ACh)

CNS (is stimulated by ACh)

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10
Q

Ach=

A

Acetylcholine (Ach) is a neurotransmitter activating parasympathetic nervous system (receptor sites on organs, tissues, and glands)

Muscarinic receptors affect smooth muscle and cardiac muscle

Nicotinic receptors affect skeletal muscles contraction

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11
Q

bethanechol

A

urinary retention

Direct acting

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12
Q

donepezil

memantine

A

Alzheimer’s disease

Indirect acting (AchE inhibitor)

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13
Q

neostigmine

A

MG,

retention,

ileus,

to reverse nondepolarizing neuromuscular block

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14
Q

pyridostigmine

A

MG,

to reverse nondepolarizing neuromuscular block

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15
Q

edrophonium

A

MG

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16
Q

Neuromuscular blockers:

A

depolarizing agents

non-depolarizing agents

17
Q

non-depolarizing agents

A

(doxacurium or pancuronium)

cholinesterase inhibitors reverse non-depolarizing neuromuscular blockers,

need for reversal for longer duration of action and very slowly metabolized

(slow redistribution or renal excretion)

18
Q

depolarizing agents

A

(succinylcholine)

cholinesterase inhibitors increase the neuromuscular blockage of depolarizing agents

(must NOT take cholinesterase inhibitors with depolarizing neuromuscular blockers),

no need for reversal
(short duration of action and metabolized)

19
Q

Page 91 of ATI mentions the use of donepezil for Parkinson’s;

A

it was meant that this drug may be used to treat dementia (Alzheimer)
in patients with Parkinson and it is known to be safe although there
is a risk of worsening PD because PD is treated with anticholinergics.

20
Q

Cholinergic side-effectsCholinergic crisis (OD)

A

excessive muscarinic stimulation

General:
HA, dizziness (poor perfusion to the brain due to low BP)

Eye: blurred vision (FALL) due to miosis and loss of accommodation (poor vision) in dim light

Lung: SOB due to bronchoconstriction, ↑ bronchial secretions

CV: bradycardia, dysrhythmias => low BP => dizziness and fall

GI: increased gastric secretions, motility (D/cramps, hyperactive bowel sounds)

GU: urgency, frequency, stress incontinence

Exocrine glands: hypersalivation, lachrimation

21
Q

Cholinergic side-effectsCholinergic crisis (OD)

A

Excessive nicotinic stimulation by
indirect-acting drugs

muscle cramps, fasciculation (muscle twitching)

Excessive ACh in CNS => excitation, seizure

Reversal agent: atropine (anticholinergic)

22
Q

Cholinergic side-effectsCholinergic crisis (OD)

NOTES

A

Muscarinic (smooth muscle and heart are suppressed by ACh)
Nicotinic (MS voluntary muscles is stimulated by ACh)
CNS (is stimulated by ACh)
SOB: shortness of breath
Lachrimation: too much tear production
Epiphora: inflammatory prevents tear drainage (superior/inferior puncta, canaliculi, lacrimal sac, nasolacrimal duct) noraml tear production

23
Q

Cholinergic Agonist

Contraindication

A

Pregnancy/lactation

GI obstruction (abdominal pain)

GU obstruction (Ureter/urethra stone)

24
Q

Cholinergic Agonist

Caution

A

Seizure

PUD

Asthma

Bradycardia & Low BP

PUD: peptic ulcer disease

25
Q

Anticholinergic (Parasympatholytics)

Action

A

Inhibit action of ACh by occupying ACh receptors

Blocking parasympathetic nerves => sympathetic domination

Anticholinergic = anti-rest/digest = adrenergic

competitive antagonist (bind to ACh receptors with no effects) hence a blocker

26
Q

Anticholinergics

Effects of anticholinergics (very similar to adrenergic)

A

GI:
↓ peristalsis/hypoactive bowel sounds,
↓ gastric secretions & salivation,
constipation

Eye:
mydriasis,
decrease accommodation in bright light
(photophobia)

Heart:
increase
HR,
BP

Lungs:
bronchodilation,
decrease bronchial secretions

GU:
relax detrusor muscle,
increase sphincter constriction (urinary retention)

CNS:
drowsiness,
decrease tremors and rigidity (used for PD)

Used to reverse cholinergic drugs

27
Q

Anticholinergics

DRUGS

A

Atropine

28
Q

Atropine

ROUTES

A

IV:
for symptomatic bradycardia

PO drop:
to reduce saliva (pre-op, palliative)
Ophthalmic drop: to produce mydriasis
& cycloplegia (pre-op)

IM:
for reversal for cholinergic OD
(OD with MG drugs)

29
Q

Atropine

SIDE EFFECTS ADVERSE REACTIONS

A
Tachycardia, 
palpitations, 
nasal congestion, 
photophobia, 
blurred vision, 
dry mouth and skin, 
constipation, 
urinary retention, 
impotence, 
memory impairment, coma

cycloplegia (paralysis of the ciliary muscle hence prevent lens adjustment)

30
Q

Atropine

CONTRAINDICATIONS

A

Contraindicated in glaucoma, BPH, MG

31
Q

ATROPINE CHART

EYE

A

Ophthalmic drop

to produce mydriasis & cycloplegia

32
Q

ATROPINE CHART
GI
ETC.

A

IV:
for symptomatic bradycardia

PO drop:
to dry up oral secretions

IM:
For reversal of cholinergic crisis

33
Q

benztropin

A

anticholinergic that in combination with
dopaminergic,
inhibits the release of ACh in

CNS for Parkinsonism
(uninhibited ACh)

and for EPS (extrapyramidal syndrome)

34
Q

CHART words

A

CP: cerebral palsy
IBS: irritable bowel syndrome
PUD: peptic ulcer disease
EPS: extrapyramidal syndrome