Drugs Acting On The Autonomic Nervous System Flashcards

1
Q

TRUE OR FALSE?
ANS CAN ACT ON DIFFERENT SYSTEMS?

A

TRUE

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2
Q

Cholinergic Pharmacology

A

~Cholinergic Drugs
~Anticholinegernic Drugs

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3
Q

Adrenergic Pharmacology

A

~ Adrenergic Drugs
~ Anti Adrenergic Drugs

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4
Q

Is the major involuntary, unconscious, automatic portion of the nervous system and contrasts in many several ways with the somatic (Voluntary nervous system)

A

Autonomic nervous System

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5
Q

The ANS is divided into 2 parts:

A

~ Parasympathetic Nervous System
~ Sympathetic Nervous System

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6
Q

1.) Cardiac and smooth muscle, gland cells, nerve terminalis
2.) Sweat Glands
3.) Renal Vascular smooth muscle
4.) Skeletal Muscle

A

1.) Parasympathetic / Sympathetic
2.) Sympathetic
3.) Sympathetic
4.) Somatic

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7
Q

TRUE or FALSE?
The parasympathetic and Sympathetic nervous system predominate effect on the body one at a time only?

A

TRUE
Can’t be at the same time due to it wasting energy

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8
Q

Thoracolumbar area

A

Sympathetic

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9
Q

Acts on parasympathetic

A

Cholinergic Pharmacology

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9
Q

Cholinergic drugs

A

Hemicholinium

Vesamicol

Botulinum

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9
Q

Brain and skeletal

A

Nicotinic

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10
Q

prevent uptake of choline

A

Hemicholinium

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11
Q

prevents the release of the ach to the postsynaptic cleft
Anticholinergic drugs

A

Botulinum

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12
Q

prevent ach to form vesicle

A

Vesamicol

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13
Q

N erase just diffusion metabolism
~Can be reuptake Cocaine
TCA- prevents reuptake therefore prolongs the effect

A

Norepinephrine

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14
Q

Anticholinergic drugs

A

~Metyrosine
~Reserpine
~Guanethidine

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15
Q

Acts on the sympathetic

A

Adrenergic

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16
Q

PROCESS:
Synthesis

CHOLINERGIC:
ADRENERGIC:

A

CHOLINERGIC: hemicholinium
ADRENERGIC: metyrosine

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17
Q

PROCESS:
Release

CHOLINERGIC:
ADRENERGIC:

A

CHOLINERGIC: Botulinum toxin
ADRENERGIC: Guanethidine

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18
Q

PROCESS:
Termination of action

CHOLINERGIC:
ADRENERGIC:

A

CHOLINERGIC: AChesterase
ADRENERGIC: Cocaine, TCA

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19
Q

Receptor characteristics:

A

Muscarinic
Nicotinic

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19
Q

Receptor characteristics:
Cholinoceptors
~ Muscarinic
M1, M2, M3, M4, M5

A

M1: BRAIN
M2: HEART
M3: SMOOTH MUSCLES, BLOOD VESSELS OTHER ORGANS PRESENT IN THE BODY (EVERYTHING ELSE)
M4: CNS
M5: CNS

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20
Q

Receptor characteristics:
Adrenoreceptors
~Alpha Receptors
~Beta Receptors

A

Alpha 1: Stimulatory (general muscles)
Alpha 2: Inhibitory
Beta 1: Heart
Beta 2: Lungs

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21
Q

Receptor characteristics:
Adrenoreceptors

A

Alpha Receptors
Beta Receptors

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22
Q

muscarinic nicotinic (ache)

choline esters alkaloids

A

Direct acting

Muscarinic

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23
Q

Indirect acting (breakdowns ACH)

A

Edrophonium - short acting

Carbamates - intermediate to long acting

Organophosphates - very long acting

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24
Q

Muscarinic receptors:
Eye

Target:
Receptor:
Response:

A

Target: Sphincter ciliary muscle
Receptor: M3
Response: Miosis Accommodation (Near vision)

25
Q

Muscarinic receptors:
Heart

Target:
Receptor:
Response:

A

Target: Sa node Av node
Receptor: M2
Response: Decrease heart rate Decrease conduction velocity

26
Q

Muscarinic receptors:
Lungs

Target:
Receptor:
Response:

A

Target: Bronchioles Glands
Receptor: M3
Response: Bronchospasm Increase secretion

27
Q

Drug:
ACH

Receptor:

Hydrolysis by ACHesterase:

Indication:

A

Receptor: Muscarinic and nicotinic

Hydrolysis by ACHesterase: +++

Indication: Short half life

28
Q

Muscarinic receptors:
GIT

Target:
Receptor:
Response:

A

Target: Glands Stomach Intestine

Receptor: M1, M2, M3

Response: Increase secretion, Increase motility, Increase contraction

29
Q

Drug:
bethanechol

Receptor:

Hydrolysis by ACHesterase:

Indication:

A

Receptor: muscarinic

Hydrolysis by ACHesterase: (-)

Indication: Postoperative ileus and urinary retention

30
Q

Drug:
methacholine

Receptor:

Hydrolysis by ACHesterase:

Indication:

A

Receptor: muscarinic> nicotinic

Hydrolysis by ACHesterase: (+)

Indication: Diagnosis of bronchial hyperreactivity

31
Q

Drug:
pilocarpine

Receptor:

Hydrolysis by ACHesterase:

Indication:

A

Receptor: muscarinic

Hydrolysis by ACHesterase: (-)

Indication: Xerostomia, glaucoma

32
Q

Indirect acting: anticholinesterase inhibitors:
DRUG: Neostigmine

Characteristics:

Clinical Use:

A

Characteristics: Long acting - quaternary Amine (No CNS entry)

Clinical Use: Treatment of myasthenia Gravis

32
Q

Indirect acting: anticholinesterase inhibitors:
DRUG: Edrophonium

Characteristics:

Clinical Use:

A

Characteristics: Ultra-short acting

Clinical Use: Differentiate myasthenic crisis and cholinergic crisis

33
Q

Indirect acting: anticholinesterase inhibitors:
DRUG: Pyridostigmine

Characteristics:

Clinical Use:

A

Characteristics: Long acting - quaternary Amine (No CNS entry)

Clinical Use: Reversal of nondepolarizing neuromuscular blockade

34
Q

Indirect acting: anticholinesterase inhibitors:
DRUG: Physostigmine

Characteristics:

Clinical Use:

A

Characteristics: Tertiary amine (Cross cns)

Clinical Use: Antidote for atropine, treatment for glaucoma

35
Q

Indirect acting: anticholinesterase inhibitors:
DRUG: Donepezil, tacrine

Characteristics:

Clinical Use:

A

Characteristics: Lipid soluble (cross cns)

Clinical Use: Alzheimer disease

35
Q

Indirect acting: anticholinesterase inhibitors:
DRUG: Organophosphates

Characteristics:

Clinical Use:

A

Characteristics: Irreversible noncompetitive ACHesterase inhibitor

Clinical Use: Insecticide (malathion, Parathion) Nerve gas (Sarin)

36
Q

Organophosphate poisoning antidote:

A

Pralidoxime

37
Q

Organophosphate poisoning
D
U
M
B
E
L
S
S

A

DIARRHEA
URINATION
MIOSIS
BRADYCARDIA
EMESIS
LACRIMATION
SALIVATION
SWEATING

38
Q

Irreversibly acting cholinomimetics:

These compounds phosphorylate the esteratic site on ACHE at __________________________

A

Serine hydroxyl groups

39
Q

reversible by pralidoxime (2-PAM)

A

phosphorylation

40
Q

Anticholinergic drugs Muscarinic receptor antagonist:

Atropine

Pharmacological Effects:

A

~Decreased Secretions

~Mydriasis, Cycloplegia

~Hyperthermia

~Tachycardia

~Sedation

~ Urinary Retention and Constipation

41
Q

Anticholinergic drugs Muscarinic receptor antagonist:

Atropine

Side Effects:

A

Hot as a hare

Dry as a bone

Blind as a bat

Red as a beet

Mad as a hatter

41
Q

Adrenoreceptors
A2

G Protein Class:

Target:

Responses:

A

G Protein Class: Gi

Target: Prejunctional nerve terminalis
*pancreas
*platelets

Responses:
Decrease sympathetic outflow
Decrease insulin release
Increase platelet aggregation

42
Q

Atropine Antidote:

A

Physostigmine; Used for glaucoma

43
Q

Adrenoreceptors
A1

G Protein Class:

Target:

Responses:

A

G Protein Class: GQ

Target: *eye: radial Arterioles
*veins
*bladder
*liver
*kidneys

Responses: Mydriasis (pupillary dilation Increase vascular smooth muscle coontraction

44
Q

Adrenoreceptors
B1

G Protein Class:

Target:

Responses:

A

G Protein Class: GS

Target: Heart

Responses:
Increase: Heart rate
Conduction velocity
Renin release

45
Q

Adrenoreceptors
B2

G Protein Class:

Target:

Responses:

A

G Protein Class: GS

Target:
Lungs
Blood vessels
Uterus
Skeletal muscle
Liver
pancreas

Responses:
Bronchodilation Vasodilation
Uterine relaxation

45
Q

Alpha agonists:
Phenylephrine methoxamine

Receptor Affinity Site:

Clinical Use:

A

Receptor Affinity Site: A1>A2

Clinical Use: Nasal decongestant

46
Q

Alpha agonists:
Clonidine, methylnorepinephrine

Receptor Affinity Site:

Clinical Use:

A

Receptor Affinity Site: A2>A1

Clinical Use: Hypertensive Urgency

47
Q

Mixed alpha and beta agonist:
norepinephrine

Receptor Affinity Site:

Clinical Use:

A

Receptor Affinity Site: A1>A2>B1

Clinical Use: Septic Shock

48
Q

Mixed alpha and beta agonist:
Epinephrine

Receptor Affinity Site:

Clinical Use:

A

Receptor Affinity Site: B>A

Clinical Use: Anaphylaxis and asthma

49
Q

Beta agonists
Isoproterenol

Receptor Affinity Site:

Clinical Use:

A

Receptor Affinity Site: B1=B2

Clinical Use: Electrophysiologic evaluation of tachyarrhythmias

49
Q

Beta agonists
Dobutamine

Receptor Affinity Site:

Clinical Use:

A

Receptor Affinity Site: B1>B2

Clinical Use: Cardiogenic shock

50
Q

Beta agonists
Albuterol, salmeterol, terbutaline, metaproterenol, ritodrine

Receptor Affinity Site:

Clinical Use:

A

Receptor Affinity Site: B2>B1

Clinical Use: Asthma

51
Q

Dopamine agonist:
dopamine

Receptor Affinity Site:

Clinical Use:

A

Receptor Affinity Site: D1=D2>B>A

Clinical Use: Shock , heart failure

52
Q

Dopamine agonist:
FENOLDOPAM

Receptor Affinity Site:

Clinical Use:

A

Receptor Affinity Site: D1>D2

Clinical Use: POSTOPERATIVE hypertension, hypertensive crisis/ emergency with impaired renal function

53
Q

Increase mean bp through vasoconstriction

Increase bp > reflex bradycardia ( may decrease cardiac output but offset by increase venous return)

A

Direct acting adrenoceptor agonists:
Alpha 1 agonists

54
Q

Stimulate prejunctional in the cns to decrease sympathetic outflow

Clinical use: mild to moderate hypertension

A

Alpha 2 agonists (clonidine and methyldopa)

54
Q

Epinephrine activates…

A

A1, A2, B1 and B2

55
Q

Norepinephrine activates…

A

A1, A2 and B1

56
Q

Decrease total peripheral resistance and decrease bp

Clinical use: hypertension

A

Alpha receptor antagonist

57
Q

Decrease heart rate stroke volume renin release

A

B1 antagonist

58
Q

Shortest acting beta blocker:

A

Esmolol