2008 M1-C2-L44 (Pharm) --> Cholinergic Drugs Ii

Front 1

Acetylcholine Blocking Agent

List the four types

Back 1

Cholinergic Neuron Blockers

Anti-muscarinic drugs

Ganglionic blockers

Neuromuscular Blockers

Front 2

Acetylcholine Blocking Agent

List two Cholinergic Neuron blockers.

Back 2

Hemicholinium

Botulinium toxin

Front 3

Acetylcholine Blocking Agent

What are the effects of Hemicholinium?

Back 3

Blocks transport of CHOLINE into neuron.

Thus, decrease in ACh release

Front 4

Acetylcholine Blocking Agent

What are the effects of botulinium toxin?
(food poisoning)

Back 4

Blocks the nerve stimulated release of ACETYLCHOLINE

Front 5

Acetylcholine Blocking Agent

Antimuscarinic drugs block muscarinic receptors how?

with what kind of activities?

Back 5

COMPETITIVELY

with

high affinity
&
NO intrinsic activity

Front 6

Acetylcholine Blocking Agent

Antimuscarinic Drugs

Which receptors of the body are affected? x2

Back 6

Receptors innervated by
Post-ganglionic Parasympathetic fibers

Receptors in sweat glands
(Post-ganglionic Sympathetic)

Front 7

Acetylcholine Blocking Agent

Ganglionic Blockers block which type of receptors?

Where are these receptors in the body?

Back 7

Nicotinic receptors

of

Autonomic Ganglia
&
Adrenal Medulla

Front 8

Acetylcholine Blocking Agent

Neuromuscular blockers block which type of receptors?

Where are these receptors in the body?

Back 8

Nicotinic receptors

Motor-end plate
of
Skeletal muscle

Front 9

Acetylcholine Blocking Agent

Belladonna Alkaloids are a kind of what type of anticholinergic drug?

Back 9

Antimuscarinic drug

Front 10

Acetylcholine Blocking Agent

Belladonna Alkaloids are effective through what mechanism of action? x2

Back 10

COMPETITIVE Antagonist

of

Acetylcholine
&
other muscarinic receptor agonists

Front 11

Acetylcholine Blocking Agent

Belladonna Alkaloids effects on nicotinic receptors?

Back 11

Little or no effect

Front 12

Acetylcholine Blocking Agent

Belladonna Alkaloids

Discuss the quantitative effect on muscarinic receptors.

Back 12

Muscarinic receptors are NOT equally sensitive to the effect of Belladonna alkaloids.

(may be due to high and low affinity binding sites)

Front 13

Acetylcholine Blocking Agent

The __________ are NOT equally sensitive to antimuscarinic agents.

Back 13

Parasympathetic neuro-effector junctions

Front 14

Acetylcholine Blocking Agent

Antimuscarinic Drugs

Example of prototype drug

Back 14

Atropine

Front 15

Acetylcholine Blocking Agent

List the tissues affected by Antimuscarinic Drugs in order from most to least sensitive. x8

Back 15

Salivary glands

Sweat glands
Eyes
(Cardiovascular) Heart
(Cardiovascular) Circulation

Respiratory Tract
Gi Tract
Urinary Tract

Front 16

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Salivary Glands

Why give a low dose?

Low does causes what symptoms? x3

Back 16

B/c highly sensitive

Dry mouth
Difficulty swallowing
Difficulty speaking

Front 17

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Salivary Glands

What does it do to the secretion rate?

Back 17

Completely abolish

PS - induced secretions

Front 18

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Sweat Glands

Effects of antimuscarinics @ low dose?

What about at toxic doses?

Back 18

Skin becomes HOT and DRY

Temperature may rise

Front 19

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Sweat Glands

Clinical danger in infants?

Back 19

"Atropine" fever can be induced in infants

(termperature may reach 43 C)

Front 20

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Sweat Glands

Why is the cholinergic effect of antimuscarinics on sweat glands unique?

Back 20

Because the sweat glands are actually part of the sympathetics.

Front 21

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Eyes

Antimuscarinics block effects of ACh where? x2

Back 21

Sphincter (iris)

Ciliary muscles

Front 22

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Eyes

What happens at the iris?

Resulting symptoms. x2

Back 22

Dilation of circular muscles.

Mydriasis

Photophobia

Front 23

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Eyes

What happens at the ciliary muscles?

This leads to what physiological symptoms? x2

Back 23

Relaxation of ciliary muscle

Paralysis of accomodation (cycloplegia)

Loss of pupillary response to light

Front 24

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Eyes

What is the effect of cycloplegia?

Back 24

Lens if fixed for far vision

Near objects are blurred

Front 25

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Eyes

Antimuscarinics have little or no effect on?

Except in?

Because?

Back 25

Intraocular pressure

Narrow angle glaucoma

Increase in aqueous outflow resistance

Front 26

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Heart

Main effect is on?

Back 26

Heart RATE

Front 27

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Heart

@ low doses do what?

Mechanism?

Significant in?

Back 27

Decrease heart rate

Stimulation of vagal nerve

Rarely a significant effect
(decrease 4-8 beats/min)

Front 28

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Heart

@ high doses do what?

Mechanism?

Significant in?

Back 28

Increasing tachycardia

Blocks vagal effect on SA node pacemaker

More apparent in young adults with increased vagal tone.
(increase 35-40 beats/min at rest)

Front 29

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Circulation

Regular dosages do what?

Why is this?

Back 29

little effect or none when given alone

b/c no cholinergic innervations in blood vessels

Front 30

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Circulation

At toxic doses, what happens?

This symptom called?

Mistaken for?

Back 30

Dilation of cutaneous blood vessels

Atropine flush

Scarlet fever

Front 31

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Circulation

Useful for what action?

Back 31

To COUNTERACT the peripheral vasodilation and sharp fall in BP caused by choline esters.

Front 32

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Respiratory Tract

Antimuscarinic effects? x5

Back 32

Mucus membrane dryness

Respiration stimulation

Smooth muscle relaxation

Bronchodilation

Secretion inhibition

Front 33

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
GI Tract


Antimuscarinic effects? x2

What doses give these effects?

Back 33

Reduction of gastric secretions

Inhibition of gastric motility

Only with high doses

Front 34

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
Urinary Tract


Antimuscarinic effect? x1

Due to what effect? x2

Back 34

Urinary retention

Relaxation of ureter

Relaxation of detrusor muscle

Front 35

Pharmacological Effects
of
Antimuscarinic Drugs
on
Parasympathetic Nervous System
for
CNS

Antimuscarinic effects? x6

Which one only occurs at really high doses?

Back 35

Memory & Concentration decrease

Drowsiness & Sedation

Ataxia

Coma

Hallucinations

Excitation
(only in really high doses)

Front 36

Poisoning
due to
Ingestion
of
Antimuscarinic Drugs

Ingestion of what drugs (x2) are the major cause of poisoning?

Back 36

Belladonna alkaloids

Drugs with "atropine-like" properties

Front 37

Poisoning
due to
Ingestion
of
Antimuscarinic Drugs

Most susceptible?

Danger?

Back 37

infants and small children

can be fatal

Front 38

Poisoning
due to
Ingestion
of
Antimuscarinic Drugs

Fatality caused by? x2

Fatal dose in children?

Back 38

respiratory arrest

circulatory arrest

10 mg or less in children

Front 39

Poisoning
due to
Ingestion
of
Antimuscarinic Drugs

How do you diagnose poisoning?

Back 39

Administeration an AChE inhibitor

Front 40

Other drugs with antimuscarinic properties.

There are 4

Back 40

Antiparkisonian agents (benztropine)

Antihistamines

Antidepressants (tricyclics)

Antipsychotics (chlorpromazine)

Front 41

What is a synthetic substitute for belladonna alkaloids?

Back 41

Quaternary Ammonium Compounds

Front 42

Quaternary Ammonium Compounds

Why good?
Why bad?

Back 42

Does not cross BBB. (less side effects)

Poorly and unreliably absorbed PO

Front 43

Quaternary Ammonium Compounds

Greater potency for what receptor?

in comparison to?

Back 43

Nicotinic receptors

tertiary amines

Front 44

Antimuscarinic Drugs
in
Therapeutic Uses

Name 10

Back 44

Pre-anesthetic medicaiton

Ophthalmologic exam

Respiratory tract infection

Toxicity treatments

Obstetrical sedation

Motion sickness

Parkinsonism-like symptoms

Sleeping pills (OTC)

Peptic ulcers

Spasticity of GI tract

Front 45

Antimuscarinic Drugs
in
Therapeutic Uses

Why is antimuscarinics good for pre-anesthetic medication? x3

Back 45

salivation/secretion inhibition

bronchodilation

sedation
(amnesia & tranquilization)

Front 46

Antimuscarinic Drugs
in
Therapeutic Uses

Benefits of using antimuscarinics in ophthalmological exams. x3

Back 46

local administration

mydriasis

cycloplegia

Front 47

Antimuscarinic Drugs
in
Therapeutic Uses

How does mydriasis caused by antimuscarinics help in eye exams?

Back 47

Dilation of pupil allows thorough exam of:

retina
&
optic disk

Front 48

Antimuscarinic Drugs
in
Therapeutic Uses

How does cycloplegia caused by antimuscarinics help in eye exams?

Back 48

Refractive index of eye

can be measured

Front 49

Antimuscarinic Drugs
in
Therapeutic Uses

What condition is contraindicated with antimuscarinics for use in eye exams?

Back 49

Narrow angle glaucoma

Front 50

Antimuscarinic Drugs
in
Therapeutic Uses

In treatment of peptic ulcers, what is the problem?

Back 50

Patient compliance

b/c of side effects
(dry mouth, blurriness, etc)

Front 51

Antimuscarinic Drugs
in
Therapeutic Uses

In treatment of spasticity in the GI, the conditions are best if the cause of GI spasticity is?

Back 51

Excessive PS stimulation

Front 52

Antimuscarinic Drugs
in
Therapeutic Uses

Parkinsonism-like symptoms are sometimes induced by?

Back 52

Antipsychotic therapy (benztopine)

Front 53

Antimuscarinic Drugs
in
Therapeutic Uses

In treating respiratory tract infections, antimuscarinics work well in treating the symptomatic relief of?

How does this affect the natural course of the condition?

Back 53

acute rhinitis

associated with

hay fever

Does NOT affect the natural course of the condition

Front 54

Antimuscarinic Drugs
in
Therapeutic Uses

In the treatment of toxic effects, poisoning of what (x2) can be treated?

Can be treated how?

Back 54

AChE inhibitor poisoning

Mushroom poisoning

Administer LARGE doses
of
Atropine