Autonomic Pharmacology

Front 1

What are the symptoms of too much (endogenous) AcH?

Back 1

DUMBBELSS

Diarrhea
Urination
Miosis
Bronchospasm
Bradycardia
Excitation of skeletal muscle/CNS
Lacrimation
Sweating
Salivation
*In general, you are putting out liquids (sweating, diarrhea, lacrimation, etc.)

Front 2

What are the effects (general) of organophosphate (parathion) poisoning?

Why (mechanism)?

Back 2

Effects are the same as too much AcH (DUMBBELSS).
This is because organophosphates are irreversible acetylcholinesterase inhibitors.

*On boards, the scenario would probably be a farmer who gets poisoned.

Front 3

Which cholinomimetic activates bowel & bladder (post-op/neurogenic ileus)?

Back 3

Bethanechol

Front 4

Which cholinomimetics (2) are used to treat glaucoma?

Back 4

carbachol, pilocarpine

Front 5

Which cholinomimetic is used as a challenge test for the diagnosis of asthma?

Back 5

methacholine

Front 6

What is the mechanism of action + 3 uses of neostigmine?

Back 6

MOA- anticholinesterase

3 uses:
1) Myasthenia gravis,
2) postop/neurogenic ileus, and 3)reversal of neuromuscular blockade (post-up)

Front 7

What is mechanism of action and 1 use for pyridostigmine?

Back 7

Anticholinesterase = MOA

used for treatment of myasthenia gravis (long-acting, does not penetrate CNS)

pyRIDostigmine gets RID of myasthenia gravis

Front 8

What is the MOA and use for edrophonium?

Back 8

Extremely short-acting anticholinesterase, used in diagnosis of myasthenia gravis

Front 9

Which two anticholinesterases can be used to treat glaucoma?

Back 9

Physostigmine and Echothiophate

Front 10

Which anticholinesterase can cross the blood brain barrier and be used to treat atropine overdose?

Back 10

Physostigmine

FIXES atropine overdose

Front 11

Which three anticholinesterases are given to Alzheimer's patients?

Back 11

Donepezil, Galantamine, Rivastigmine

Front 12

What is the treatment for organophosphate poisoning?

Back 12

1) atropine + pralidoxime

Atropine is a muscarinic antagonist and pralidoxine helps regenerate active AchE

Front 13

What is the mechanism of action of atropine?

Back 13

Muscarinic antagonist- blocks AcH

Front 14

What are two uses for atropine?

Back 14

eye- used to dilate eyes for eye exam
bronchial- used to decrease secretions when someone is intubated

Front 15

What are the Anti-cholinergic side effects?

Back 15

Hot as a Hare (increased body temp)
Dry as a Bone (dry mouth, skin)
Red as a Beet (flushing)
Blind as a Bat (cycloplegia --> blurry near vision)
Mad as a Hatter (CNS effects, delirium)
Bloated as Toad (constipation/urinary retention)

Front 16

Which two muscarinic antagonist drugs have the same use as atropine?

Back 16

homatropine and tropicamide

Front 17

Which muscarinic antagonist drug is used to treat Parkinson's disease?

Back 17

Benztropine

"PARK my BENZ"

Front 18

What is the MOA and use for scopolamine?

Back 18

MOA- muscarinic antagonist with CNS effects (blocks emesis)

Use- to treat motion sickness/post-surgical/end of life nausea/secretions

Front 19

What is the MOA and use for ipratropium?

Back 19

MOA- muscarinic antagonist with respiratory effects

Used to cause smooth muscle relaxation and treat COPD/Asthma

Front 20

What is the MOA and use for oxybutinin?

Back 20

MOA- muscarinic antagonist with smooth muscle effects (will relax smooth muscle)

Used to reduce urgency in mild cystitis and reduce bladder spasms (because remember that bladder muscle CONTRACTION will push urine out)

Front 21

Tolterodine, darifenacin, solifenacin, and trospium are what kind of drugs?

What are they used to treat?

Back 21

Muscarinic antagonists

Used to treat urge-type urinary incontinence

Front 22

What is the MOA and use of glycopyrrolate?

Back 22

MOA- muscarinic antagonist

Use? Decrease airway secretions

Front 23

What is the MOA and use for methscopolamine?

Back 23

MOA- muscarinic antagonist that works in the GI tract

Use- peptic ulcer treatment (decreases gastric acid secretion)

Front 24

Name a muscarinic antagonist other than methscopolamine that has primarily GI uses?

Back 24

Propantheline

Front 25

Who would you NOT want to give a muscarinic antagonist to?

Back 25

Anyone with glaucoma, BPH or urinary retention, GI obstruction, dementia, or an infant with fever

Front 26

What is the mechanism of action of hexemethonium?

Back 26

Nicotinic antagonist, works at the ganlionic level and so it inhibits both sympathetic and parasympathetic actions

Front 27

What is the net effect of hexamethonium regarding?
BP, HR, CO, urine output, GI motility, the eye

Back 27

BP - decreased bc there is more sympathetic innervation at vessels
At all other places (in question), parasympathetic tone dominates, so hexamethonium looks like a parasympathetic antagonist:

Increases HR, decreases CO-don't totally get?, Decreases urine, decreases GI motility, and causes mydriasis.

Front 28

What is the mechanism of action of hemicholinium?

Back 28

Blocks uptake of choline into presynaptic cholinergic neuron

Front 29

What is combined with Acetyl-co A to make acetylcholine?

Back 29

choline!

Front 30

What substance inhibits the production of AcH in the presynaptic cell?

Back 30

Vesamicol

Front 31

Name one toxin that blocks AcH release and one toxin that increases AcH release from the presynaptic cell.

Back 31

Blocks- botulinum toxin

Increases- black widow spider toxin

Front 32

What is the amino acid precurser of norepinephrine?

Back 32

Phenyalanine/tyrosine (Phe --> Tyr --> DOPA --> dopamine --> NE)

Front 33

What substance blocks tyrosine --> DOPA?

Back 33

Metyrosine

Front 34

What substance blocks dopamine --> NE?

Back 34

Reserpine

Front 35

What ion initiates AcH AND NE release from the presynaptic cell?

Back 35

Ca2+

Front 36

Name 4 substances that would decrease the release of NE from the presynaptic terminal.

Back 36

1) NE itself, acting on alpha 2 pre-synaptic receptors
2) Acetylcholine, acting on M2 receptors
3) Guanethidine
4) Bretylium

Front 37

Name 4 substances that would increase the release of NE from the presynaptic nerve terminal.

Back 37

1) angiotensin II acting on an angiotensin II receptor
2) Amphetamines
3) Ephedrine (stimulant)
4) Tyramine

Front 38

Name 5 drugs or drug categories that inhibit NE reuptake.

Back 38

1) SNRIs
2) TCAs
3) Cocaine
4) Amphetamines
5) Maprotiline

Front 39

Both AcH and NE can bind pre-synaptic receptors, bind post-synaptic receptors, and be degraded. Which one can also be taken back up by the pre-synaptic cell?

Back 39

NE

Front 40

Which sympathomimetic would you use to treat anaphylaxis?

Back 40

Epinephrine

Front 41

Which sympathomimetic would you use to treat open angle glaucoma?

Back 41

Epinephrine

Front 42

Which sympathomimetic activates all four sympathetic receptors?

Back 42

Epinephrine

Front 43

What does giving Epinephrine at low doses preferentially activate?

Back 43

B2 receptors --> vasodilation

Front 44

Name three things that epinephrine might be used to treat.

Back 44

1) Anaphylactic shock
2) open angle glaucoma
3) asthma (low dose to activate beta 2 Rs)
4) hypotension

Front 45

Which sympathomimetic could be used to treat hypotension (alpha 1 effects) but might decrease renal perfusion?

Back 45

Norepinephrine

Front 46

Which sympathomimetic might be used to treat AV block? On which receptor does it act?

Back 46

Isoproterenol, Acts on B1=B2 receptors

Front 47

Which sympathomimetic could be given in shock to increase rental perfusion (theoretically) and in heart failure?

Back 47

Dopamine (D1 = D2 > beta > alpha)

Ideally, the dopamine increases renal perfusion, and then the beta effects kick start the heart. Would give this along with NE.

Front 48

Which sympathomimetic would you use to treat septic shock?

Back 48

NE

Front 49

Which sympathomimetic would you give in heart failure or during cardiac stress testing (or for cardiogenic shock)?

Back 49

Dobutamine, which has beta 1 > beta 2 effects.

So beta 1 - increase hr and contractility, beta 2- vasodilation

Front 50

Which sympathomimetics would you reach for (2) for short-term treatment of asthma?

Back 50

1) Albuterol
2) Metaproterenol

B2 > B1 effects (but they still have beta 1 effects)

Front 51

Which sympathomimetic would you use to treat long-term asthma?

Back 51

Salmeterol

Front 52

Which sympathomimetics would you use to reduce premature uterine contractions?

Back 52

1) Terbutaline
2) Ritodrine

Front 53

Which sympathomimetic would you use to treat epistaxis or for nasal decongestion?

Back 53

phenylephrine (alpha > allpha 2)

Front 54

What is the MOA and 4 uses for amphetamines?

Back 54

MOA- indirect sympathetic agonist by causing more release of stored catecholamines

4 uses-
1) major depressive disorder (while waiting for anti-depressant to start working)
2) narcolepsy
3) obesity
4) ADD

Front 55

What is the MOA and three uses for ephedrine?

Back 55

MOA- indirect sympathetic agonist, causes release of stored catecholamines

Uses-
Nasal decongestion, urinary incontinence, hypotension, and in otolaryngology surgery to stop bleeding

Front 56

What is the MOA and use for cocaine?

Back 56

Cocaine is a sympathetic agonist (indirect)- inhibits NE uptake

Used as local anesthetic bc it takes away pain & vasoconstricts to keep effect local. Cocaine blocks sodium channels which is why it is an anesthetic.

Front 57

What is the MOA of clonidine/alpha methyldopa? What are they used to treat?

Back 57

MOA- they are alpha 2 agonists so they act centrally, causing inhibition of NE release and thus leading to decreased BP.

Used to treat high BP in renal failure (clonidine) & high BP in pregnancy (alpha methyl dopa)

Front 58

What is the net effect of NE on blood pressure and heart rate?

Back 58

NE - increases blood pressure (vasoconstriction) and decreases heart rate (reflex bradycardia)

Front 59

What is the net effect of isopoterenol on BP and heart rate?

Back 59

Isoproterenol decreases BP (beta 2 effect) and increase HR (reflex tachycardia + beta 1 effects)

Front 60

What type of receptor is a nicotinic ACh receptor?

Back 60

ligand gated

Front 61

What type of receptor is a muscarinic AcH receptor?

Back 61

G protein coupled

Front 62

What is the action of beta blockers on the kidney?

Back 62

Decreased renin secretion due to beta receptor blockate on JGA cells

Front 63

Why do beta blockers work to treat angina?

Back 63

They decrease heart rate and contractility, leading to reduced oxygen need by coronary arteries

Front 64

Which beta blockers dec. MI mortaility?

Back 64

metoprolol & carvedolol

Front 65

How do beta blockers act to treat SVT?

Back 65

They slow AV conduction velocity

Front 66

Which beta blockers are used to treat SVT?

Back 66

propranolol, esmolol (IV, short acting)

Front 67

Which beta blockers are used to treat glaucoma and how do they work?

Back 67

timolol

decreases secretion of aqueous humor

Front 68

Why should beta blockers be used with caution in diabetics?

Back 68

bc they won't experience the normal effects of hypoglycemia due to the beta blockade

Front 69

What is the sexual side effect of beta blockers?

Back 69

impotence

Front 70

Why might a beta blocker exacerbate asthma?

Back 70

because you are blocking beta two agonism which leads to bronchodilation

Front 71

Which type of beta blocker would be less likely to cause asthma exacerbation?

Back 71

b1 selective

Front 72

How do you recognize the non-selective beta blockers?

Back 72

They start with P- N (end of the alphabet)

Front 73

How do you recognize the beta 1 selective antagonists?

Back 73

They start with A-M

Front 74

Name two nonselective alpha/beta antagonists

Back 74

carvedilol, labetalol

Front 75

Name two partial beta agonists

Back 75

pindolol, acebutolol

Front 76

Why don't you give a beta blocker with cocaine?

Back 76

bc cocaine has some beta 2 (vasodilatory) effects that you will block if you give a beta blocker to slow the heart rate

Front 77

What drug is a non-selective, irreversible alpha blocker used to treat pheochromocytoma?

Back 77

phenoxybenzamine

Front 78

Which drug is a reversible non-selective alpha blocker?

Back 78

phentolamine

Front 79

What are the side effects of alpha blockers (non-selective)

Back 79

orthostatic hypOtension, reflex tachycardia

Front 80

What type of drug as prazosin, terazosin, and doxazosin?

Back 80

alpha 1 selective blockers

Front 81

What can alpha 1 selective blockers be used to treat (2)?

Back 81

BPH, hypertension

Front 82

Toxicity of alpha 1 blockers?

Back 82

1st dose orthostatic hypertension, dizziness, headache

Front 83

What is the alpha 2 selective blocker?

Back 83

mirtazapine

Front 84

What's the difference between phenylephrine, phenoxybenzamine, and phentolamine?

Back 84

phenylephrine- alpha 1 > alpha 2 agonist

Phenoxybenzamine- irreversible alpha (1 & 2) blocker

Phentolamine - reversible alpha (1&2) blocker