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Pharmacology Exam 2 > Autonomic Drugs > Flashcards

Autonomic Drugs Flashcards

1
Q

onabotulinumtoxinA (botox)

A 
Protein from C. botulinum
Blocks release of ACH (SNAP-25) 
Post-synaptic terminal cannot be stimulated 
= Flaccid paralysis 
Sprouting new nerve may take months

Tx: Blepharospasm, cosmetic, overactive bladder, hyperhydrosis

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2
Q

Muscarine

A

Amanaita muscarina mushroom

Selective agonist of muscarinic receptors

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3
Q

Atropine

A 
Atropa belladonna
Competitive antagonist of ALL muscarinic receptors equally
*block all PNS symptoms*
Low affinity for nicotinic
Cross BBB
Dose dependent response
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4
Q

Nicotine

A

Stimulates Nn, Nm (also blocks and stimulate)

Persistent stimulation leads to desensitization

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5
Q

d-Tubocurarine (curare)

A

Competitive agonist of Nm

Does not block Nn

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6
Q

Acetylcholinesterase (AChE)

A

Rapidly terminates cholinergic transmission by hydrolysis in the nerve terminal
Allow for depolarization

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7
Q

Butyrylcholinesterase

A

Pseudocholinesterase
Plasma, glial cells, liver
Drug metabolizing enzyme
Some patients may be deficient

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8
Q

Tyrosine hydroxylase

A

Rate limiting step of catecholamine neurotransmitter formation

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9
Q

Mitochondrial monoamine oxidase (MAO)

A

Degrades catecholamine storage vesicles
Deaminates catecholamines = inactivate!
Clears catecholamines from nerve terminal

MAOIs increase NT in nerve terminal

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10
Q

Vesicular membrane monoamine transporter-2 (VMAT-2)

A

Transports NTs to vesicles and concentrated

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11
Q

Reserpine

A

Antihypertensive, Antipsychotic
IRREVERSIBLE inhibitor of VMAT-2
= NTs are not stored in vesicle, degraded by MAO
Deplete catecholamine
Decrease SNS effects, non-selective side effects

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12
Q

Tyramine

A

Fermentation byproduct of tyrosine in protein rich food
CHEESE, wine, cured meats
Displaces NE from vesicles and causes non-vesicular release from nerve terminals by reverse transport of NET
High concentration of NE in synapse
Problematic with MAO Inhibitors - HTN crisis

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13
Q

Methyldopa

A

Antihypertensive
Can be used safely during pregnancy no birth defects
Can ONLY stimulate A-2 (autoregulator) to decrease NT release of NE

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14
Q

Cocaine

A

Block reuptake of NE everywhere

Block NET from reuptaking NE

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15
Q

Catechol-O-methyltransferase (COMT)

A

Cytosolic (liver, kidney)
Clearance of circulating catecholamines in blood

Inhibitors for Parkinsons

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16
Q

Vanillylmandelic acid (VMA)

A

Metabolite excreted in urine
Measure to determine how active SNS is

High levels - theochromocytoma
Low levels - deficit

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17
Q

Synthetic Choline Esters

A

Selective
Prolonged action to ACH
Do not penetrate BBB
PNS effects

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18
Q

Bethanechol (Urecholine)

A

Resistant to hydrolysis by cholinesterase
Increase bladder detrusor contraction and GI tract
Tx: postpartum urinary retention, GERD, gastric atony

19
Q

Pilocarpine

A

Prototype Cholinomimetic Alkaloid
Partial agonist of ALL muscarinic subtypes
Eyes miosis, blurred vision, decreased IOP
Tx: dry mouth, wide angle glaucoma

20
Q

Cervimeline

A 
Alkaloid selective agonist of M3
Sjogrens syndrome (stimulate remaining receptors)
Longer duration than pilocarpine w/ less side effects
21
Q

Physostigmine

A

Antidote to atropine

counteracts both CNS and peripheral effect by elevating synaptic concentration of ACH agonist

22
Q

Scopolamine

A

Muscarinic antagonist
Better CNS penetration
Sedation at low dose, suppress emesis, motion sickness block M receptor in vestibular
Prophylaxis motion sickness

23
Q

Ipratropium bromide (Atrovent)

A

Quaternary amine (does not cross membrane)
Bronchodilator (asthma/COPD)
Limited absorption when inhaled, minimal side effects

24
Q

Tropicamide

A

Mydriatic, cyclopegic
SHORTER DURATION (6 hours)!
Facilitates diagnosis and surgery of ophthalmic disorders
Blurred vision, photophobia common side effects

25
Q

Tolterodine (detrol)

A

Non-selective muscarinic antagonist
Tx: Overactive bladder/urge/incontinence
Improved capacity of bladder and decreased urgency sensation

26
Q

Neostigmine

A

Blocks acetylcholinesterase
Blocks ACH degradation (increases ACH effects)
Reversible inhibitor, but occupies active site for long time

27
Q

Phyostigmine

A

Not an agonist of Nicotinic
Same as Neostigmine but crosses the BBB
Tx: poisoning by atropine

28
Q

Donepezil (Aricept)

A

More selective inhibition of AChE isoform in CNS

Tx: Alzheimers cognitive decline

29
Q

Malathion

A

Irreversible Inhibitor of AchE
Insecticide
Highly lipid soluble
Accidental agricultural poisoning, warfare agent

30
Q

Pralidoxime (Protopam)

A

Reactivates AChE ONLY at NMJ, must be administered before aging occurs
Regenerate new enzyme to remove irreversibly bound organophosphate
Takes off organophosphate in AChE
Tx: Pesticide poisoning, warfare

31
Q

Catecholamines vs. Non-catecholamines

A

Catecholamine - no oral, short action, no BBB

Noncatecholamine - no catechol fxnl group, oral, long duration, cross BBB (CNS effects)

32
Q

Epinephrine

A

A1, A2, B1, B2, Non-selective

  • B1 cardiac effects
  • A1 vascular/skeletal muscle (high dose)
  • B2 vascular/skeletal muscle (low dose)
  • B2 respiratory effects

Uses/tx: in combo w/ anesthetics, anaphylactic shock/cardiac arrest, hemostasis

33
Q

Norepinephrine

A

A1, A2, B1 (lost B2 activity!)
B1 Cardio effects
Tx: hypotension, septic shock PREFERRED over EPI

34
Q

Isoproterenol

A

B1, B2 (non-selective B agonist)
B1 - cardio, AV block and cardiac arrest
B2 - bronchospasm during anesthesia (Rare)

35
Q

Dopamine

A

D1>B1>A1
Low dose - D1 (renal) - INCREASE RENAL BF
Medium Dose - B1 (some cardio not a lot increase in HR)
Large dose - A1 vasoconstriction

Tx: good for shock especially if trying to allow renal BF (NE and Epi constrict renal), maintains bp

36
Q

Dobutamine

A

B1 agonist
B1 cardiac effects - increase contractility, HR, conduction velocity
Less reflex tachycardia because no vascular involvement (B2) - but side effect is tachycardia
Good for shortterm management of CHF

37
Q

Phenylephrine (Sudafed)

A

A1 agonist
Nose - vasoconstriction, decongestion
Vasoconstriction, mydriasis, detmuescent

Toxicity in high dose = reflex brady, HTN, arrythmia, vomiting nausea

38
Q

Clonidine

A

A2 agonist
Autoregulators stimulated = decrease NE
Any NE effects decreased, reduce SNS outflow

Tx: HTN, Severe pain
S/E: Bradycardia, dry mouth, sedation
Must decrease dose slowly, reflex HTN on withdrawl

39
Q

Terbutaline

A

B2 agonist
Tx: Respiratory - reduces airway resistance in asthmatics
Tx: Suppresses premature labor by relaxing uterine smooth muscle contractions

SE: tremor, hyperglycemia, tachycardia (high dose), DEATH IN PREGNANT WOMEN

40
Q

Prazosin

A 
A1 blocker
Dilates arteries/veins, relax SMC of bladder (trigone and sphincter), prostate
Tx: HTN, urinary retention
S/E: Orthostatic Hypotension
Effect depend on activity of SNS
41
Q

Tamulosin (Flomax)

A

Selective A1a antagonist
Dilate the prostate arteries, urethra, bladder
Tx: BPH, urinary retention
S/E: Interacts with erectile dysfunction drugs, can lead to hypotension

42
Q

Propanolol

A 
Non-selective B1, B2 antagonist
Pure competitive antagonist
Inhibit B1 cardio (decrease HR, contractility)
B2 respiratory
B2 - kidney (no renin), liver (glycogen)
S/E: fatigue, lethargy
Contraindicated for DM, Cardiac
43
Q

Metoprolol

A

B1 antagonist selective
“CARDIOSELECTIVE”
No B2 side effects unless high dose
Tx: HTN, angina, CHF, MI

Pharmacology Exam 2 (4 decks)

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