Autonomic Nervous System

Front 1

Cholinergic Agonists - Direct acting

Back 1

Acetylcholine
Bethanachol
Carbachol
Pilocarpine

Front 2

Cholinergic Agonists - Indirect acting

Back 2

REVERSIBLE
Edrophonium
Neo-, Physo-, Pyrido-stigmine
IRREVERSIBLE
Echothiphate
Isoflurophate

Front 3

Cholinergic Agonists - Reactivation of acetylcholine esterase

Back 3

Pralidoxime

Front 4

Hemicholinium

Back 4

Inhibits choline transport into cells.

Hint 4

ACh synthesis

Front 5

Choline acyteltransferase (ChAT)

Back 5

Catalyzes reaction of choline with acetyl CoA to make ACh

Hint 5

ACh synthesis

Front 6

Vesamicol

Back 6

Inhibits ACh packaging into vesicles

Hint 6

ACh synthesis

Front 7

Botulinum

Back 7

Blocks release ACh into synapse

Hint 7

ACh transmission

Front 8

Acetylcholine esterase (AChE)

Back 8

Degrades ACh in synapse to choline and acetate

Hint 8

ACh transmission

Front 9

Acetylcholine

Back 9

Cholinergic Agonist - Direct
Not important therapeutically
-Decrease HR and CO
-Decrease BP (vasodilation, NO)
-Parasympathetic actions

Hint 9

Cholinergic Agonist - Direct

Front 10

Bethanechol

Back 10

Cholinergic Agonist - Direct
Ap: Postop and neurogenic ileus and urinary retention
-Stimulates muscarinic: Bowel and Bladder
-Resistant to AChE

Hint 10

Cholinergic Agonist - Direct

Front 11

Carbachol

Back 11

Cholinergic Agonist - Direct
Ap: Glaucoma, pup. constriction, release of intraocular pressure
-Resistant to AChE
-Long duration of action

Hint 11

Cholinergic Agonist - Direct

Front 12

Pilocarpine

Back 12

Cholinergic Agonist - Direct
Ap: Glaucoma
-Less potent than ACh derivatives
Sfx: Can cross BBB and cause CNS disturbances; stimulates sweat, tears and saliva

Hint 12

Cholinergic Agonist - Direct

Front 13

Methacholine

Back 13

Cholinergic Agonist - Direct
Ap: Challenge test for diagnosis of asthma
-Stimulates musc receptors in airway -> constriction

Hint 13

Cholinergic Agonist - Direct

Front 14

Physostigmine

Back 14

Cholinergic Agonist - Anticholinesterase
Ap: Glaucoma; atropine overdose; bowel/bladder atony
- Increases endogenous ACh
- Crosses BBB (convulsions)

Hint 14

Cholinergic Agonist - Anticholinesterase

Front 15

Neostigmine

Back 15

Cholinergic Agonist - Anticholinesterase
Ap: Postop and neurogenic ileus and urinary retention; Myasthenia Gravis; antidote to neuromusc blockers
- Increases endogenous ACh
- No CNS penetration

Hint 15

Cholinergic Agonist - Anticholinesterase

Front 16

Pyridostigmine

Back 16

Cholinergic Agonist - Anticholinesterase
Ap: Myasthenia Gravis (increases strength)
- Increases endogenous ACh
- Crosses BBB

Hint 16

Cholinergic Agonist - Anticholinesterase

Front 17

Edrophonium

Back 17

Cholinergic Agonist - Anticholinesterase
Ap: Diagnosis of Myasthenia Gravis (short -acting)
- Increases endogenous ACh

Hint 17

Cholinergic Agonist - Anticholinesterase

Front 18

Echothiophate

Back 18

Cholinergic Agonist - Anticholinesterase
Irreversible
Ap: Glaucoma (increases aqueous humor outflow)
- Increases endogenous ACh

Hint 18

Cholinergic Agonist - Anticholinesterase

Front 19

Pralidoxime (PAM)

Back 19

Reactivates inhibited AChE
Ap: Antidote to irreversible AChE inhibitors such as echothiophate

Front 20

AChE Inhibitor poisoning - symptoms and treatment

Back 20

Symptoms: Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, Salivation
Treatment: atropine and pralidoxime

Front 21

Hexamethonium

Back 21

Nicotinic ACh receptor antagonist - Ganglionic Blocker
Ap: antiHTN; used experimentally to prevent vagal reflex to BP change
TOX: orthostatic hypotension, blurred vision, constipation, sexual dysfxn

Hint 21

Ganglionic Blocker

Front 22

Nicotine

Back 22

Nicotinic ACh receptor antagonist - Ganglionic Blocker

Hint 22

Ganglionic Blocker

Front 23

Trimethaphan, mecamylamine

Back 23

Nicotinic ACh receptor antagonist - Ganglionic Blocker
Ap: emergency BP lowering

Hint 23

Ganglionic Blocker

Front 24

Tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rapacuronium

Back 24

Nondepolarizing neuromuscular blockers
Competitive inhibitors of motor nicotinic receptors
Ap: Muscle paralysis in sx or mech. vent

Hint 24

Neuromuscular Blockers

Front 25

Succinylcholine

Back 25

Depolarizing neuromuscular blocker
Phase I: prolonged depol - no antidote
Phase II: repolarized, resistant to depol - antidote is AChE inhibitors
Ap: Muscle paralysis in sx or mech. vent

Hint 25

Neuromuscular Blocker

Front 26

Metyrosine

Back 26

Blocks tyrosine -> DOPA
Ap: lower catecholamines produced with pheochomocytoma

Hint 26

Adrenergic nt synthesis

Front 27

Reserpine

Back 27

MECH: Blocks packaging of DA into vesicles
USE: antiHTN
TOX: sedation, depression, nasal stuffiness, diarrhea

Hint 27

Adrenergic nt synthesis

Front 28

Guanethidine, bretylium

Back 28

MECH: Blocks release of catecholamines from vesicle
USE: antiHTN
TOX: orthostatic/exercise hypotension, sexual dysfxn, diarrhea

Hint 28

Adrenergic nt release

Front 29

Amphetamine

Back 29

Sympathomimetic - indirect, general
- Increases release of stored catecholamines from vesicles
Ap: Narcolepsy, obesity, ADD

Hint 29

Sympathomimetic

Front 30

Monoamine Oxidase (MAO)

Back 30

Oxidizes/metabolizes NE and DA

Hint 30

Catecholamine metabolism

Front 31

Catechol O-methyltransferase (COMT)

Back 31

Oxidizes/metabolizes NE and DA

Hint 31

Catecholamine metabolism

Front 32

Phenylephrine

Back 32

Direct-acting adrenergic agonist
Selectivity: α1 > α2

USE: dilates pupil, vasoconstrictor, nasal decongestant
TOX: hypertensive headache, cardiac irregularities

Hint 32

sympathomimetic

Front 33

Cocaine

Back 33

Sympathomimetic - indirect general
- Blocks reuptake of norepi
-> vasoconstriction, local anesthesia

Hint 33

Sympathomimetic

Front 34

Epinephrine

Back 34

Direct-acting adrenergic agonist
Selectivity: all; low doses -> β
MECH:
Resp: bronchodilation (β2); used for asthma and anaphylactic shock
Eye: reduces production of aqueous humor; used for open-angle glaucoma
CV: increases contractility & HR (β1); constricts vessels to skin, mucous membranes, viscera (α); dilates vessels to liver and skel. m.(β2); overall ↓DBP & ↑SBP
Hyperglycemia: increased glycogenolysis (β2); decreased insulin (α2)
Lipolysis: stimulates hormone-sens lipase (β)
Anesthetics: very small amount vasoconstricts site of injection to slow release

TOX: CNS disturbances; cerebral hemorrhage due to high BP; cardiac arrhythmias; pulmonary edema

Hint 34

Sympathomimetic

Front 35

Methoxamine

Back 35

Direct-acting adrenergic agonist
Selectivity: α1 > α2

USE: paroxysmal supraventricular tachycardia (vagal effects); sx hypotension (vasoconstriction → ↑total peripheral resistance)
TOX: hypertensive headache, cardiac irregularities

Hint 35

sympathomimetic

Front 36

Norepinephrine

Back 36

Direct-acting adrenergic agonist
Selectivity: α1, α2 > β1
MECH:
CV - vasoconstriction → ↑DBP (preload) & ↑SBP (resistance)
↑ contractility, but baroreceptor reflex counteracts HR (given after atroprine, tachycardia develops)
USE: shock
TOX: ↓ renal perfusion

Hint 36

Sympathomimetic

Front 37

Isoproterenol

Back 37

Direct-acting adrenergic agonist
Selectivity: β1 = β2
MECH:
CV - increases contractility & HR (β1); dilates vessels to liver and skel. m.(β2) (decreases DBP)
Resp - bronchodilation
USE: AV block, bronchodilator
TOX: CNS disturbances; cerebral hemorrhage due to high BP; cardiac arrhythmias; pulmonary edema

Hint 37

Sympathomimetic

Front 38

Clonidine

Back 38

Direct-acting adrenergic agonist
Selectivity: α2, acts central to ↓ adrenergic outflow
USE: essential hypertension, esp. with renal dz (no decrease in renal blood flow)
TOX: dry mouth, sedation, severe rebound HTN

Hint 38

sympathomimetic

Front 39

Dopamine

Back 39

Direct-acting adrenergic agonist
Selectivity: D1=D2 > β > α

MECH:
CV - increases contractility & HR (β1); constricts vasculature (α)
Renal/visceral - dilates renal & splanchnic arterioles (D)
USE: Shock (drug of choice), heart failure
TOX: nausea, HTN, arrhythmias (short-lived)

Hint 39

Sympathomimetic

Front 40

Dobutamine

Back 40

Direct-acting adrenergic agonist
Selectivity: β1 > β2

MECH: increases contractility & HR (β1)
USE: Congestive HF, shock, cardiac stress testing

Hint 40

Sympathomimetic

Front 41

Terbutaline

Back 41

Direct-acting adrenergic agonist
Selectivity: β2

Ap: bronchodilation, ↓ uterine contractions

Front 42

Albuterol

Back 42

Direct-acting adrenergic agonist
Selectivity: β2

Ap: bronchodilation (inhalant)

Front 43

Ephedrine

Back 43

Mixed-action adrenergic agonist
MECH:
-Releases stored catecholamines
-Directly stimulates receptors
- Not a catechol → long duration
USE: nasal decongestion, urinary incontinence, hypotension
TOX: CNS and CV stimulation; arrhythmias, stroke, seizures (high dose)

Hint 43

sypathomimetic

Front 44

α1 actions

Back 44

G-protein → PLC →PIP & IP3 → Ca++ →
- Vasoconstriction
- ↑ peripheral resistance
- ↑ BP
- Mydriasis (pupil dilation)
- ↑ closure of bladder internal sphincter

Front 45

α2 actions

Back 45

Gi → ↓cAMP →
- inhibition of norepi release
- inhibition of insulin release

Front 46

β1 actions

Back 46

Gs → ↑cAMP →
-Tachycardia
- ↑ lipolysis
- ↑ inotropy

Front 47

β2 actions

Back 47

Gs → ↑cAMP →
- Vasodilation
- ↓ peripheral resistance (slight)
- Bronchodilation
- ↑ muscle and liver glycogenolysis
- ↑ release of glucagon
- Relaxed uterine smooth muscle

Front 48

Phenoxybenzamine

Back 48

α-blocker, nonselective, irreversible, non-competitive
MECH: prevents vasoconstriction → reflex tachycardia, orthostatic hypotension
Epinephrine reversal
USE: pheochromocytoma

Hint 48

Adrenergic antagonist

Front 49

Phentolamine

Back 49

α-blocker, nonselective, reversible

CV: prevents vasoconstriction → reflex tachycardia, orthostatic hypotension

Ap: diagnosis of pheochromocytoma (short-acting)

Hint 49

Adrenergic antagonist

Front 50

Pra-, tera-, doxa-ZOSIN

Back 50

α1-blockers, competitive
MECH: ↓peripheral vasc resistance without fx on CO or renal blood flow
USE: Hypertension, urinary retention in BPH
TOX: First-dose effect (syncope); dizziness, lethargy, HA, drowsiness

Hint 50

Adrenergic antagonist

Front 51

β-blocker effects

Back 51

CV: ↓CO; ↓renin secretion; peripheral vasoconstriction
Resp: bronchoconstriciton
Renal: ↓renal perfusion → Na retention
Glucose metabolism: ↓glycogenolysis; ↓glucagon
Eye: ↓secretion of aqueous humor

Ap: HTN, Angina pectoris, MI, SVT (↓AV conduction velocity), CHF

β1-selective: less bronchoconstriction at low doses, good for asthmatics
partial agonist: less carbohydate metabolism effects, good for diabetics

Front 52

Timolol

Back 52

β-blocker, non-selective

MECH: ↓secretion of aqueous humor w/o pupillary or vision changes
USE: glaucoma

Front 53

Propranolol

Back 53

β-blocker, non-selective

Front 54

Nadalol

Back 54

β-blocker, non-selective, long-acting

Front 55

Acebutolol

Back 55

β-blocker, β1-selective, partial agonist

Front 56

Pindolol

Back 56

β-blocker, non-selective, partial agonist

Front 57

Metoprolol

Back 57

β-blocker, β1-selective

Front 58

Atenolol

Back 58

β-blocker, β1-selective

Front 59

Esmolol

Back 59

β-blocker, β1-selective

Front 60

Labetolol

Back 60

β-blocker, non-selective, concurrent alpha1 blocking

Ap: Good for patients for whom increased peripheral vasc resistance is bad

Front 61

Atropine

Back 61

Muscarinic antagonist
MECH: competitive inhibitor of muscarinic receptor
USE/FX:
Eye - mydriasis (dilation), cycloplegia (inability to focus)
GI - antispasmodic, reduced motility
Stomach - ↓ acid secretion
Airway - ↓ secretions, used prior to sx
Bladder - ↓ urgency in cystitis
TOX:
Hot as a hare - ↑ bod temperature, rapid pulse - hyperthermia in infants
Dry as a bone - dry mouth, skin, and eyes
Red as a beet - flushed skin
Blind as a bat - cycloplegia - acute angle-closure glaucoma in elderly
Mad as a hatter - disorientation, constipation - urinary retention w/ prostatic hypertrophy

Hint 61

Cholinoreceptor blocker

Front 62

Tropicamide

Back 62

MECH: competitive inhibitor of muscarinic receptor
USE/FX:
Eye - mydriasis (dilation), cycloplegia (inability to focus)

Hint 62

Cholinoreceptor blocker

Front 63

Methscopolamine

Back 63

MECH: competitive inhibitor of muscarinic receptor
USE/FX:
GU - ↓ urgency in mild cystits; ↓ bladder spasms

Hint 63

Cholinoreceptor blocker

Front 64

Scopolamine

Back 64

MECH: competitive inhibitor of muscarinic receptor
USE/FX:
CNS - prevent motion sickness; block short-term memory
TOX: same as atropine (blurred vision, confusion, mydriasis, constipation, urinary retention, dry mouth and skin, etc)

Hint 64

cholinoreceptor blocker

Front 65

Ipratropium

Back 65

MECH: competitive inhibitor of muscarinic receptor
USE/FX: Respiratory - management of COPD and asthma

Front 66

Methyldopa

Back 66

MECH: activates alpha2 to reduce sympathetic outflow → ↓TPR
USE: antiHTN
TOX: sedation, positive Coomb's test

Hint 66

sympathomimetic

Front 67

Oxybutin

Back 67

MECH: competitive inhibitor of muscarinic receptor
USE/FX:
GU - ↓ urgency in mild cystits; ↓ bladder spasms

Hint 67

Cholinoreceptor blocker

Front 68

Glycopyrrolate

Back 68

MECH: competitive inhibitor of muscarinic receptor
USE/FX:
GU - ↓ urgency in mild cystits; ↓ bladder spasms

Hint 68

Cholinoreceptor blocker