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PDSA > Block 6 - literally just drugs > Flashcards

Block 6 - literally just drugs Flashcards

1
Q

list the following for narcan/naloxone

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

target - MOR

Gi (which doesn’t get activated by this drug)

antagonist (Mu Opioid Receptor blocker)

used to treat opioid overdose

can lead to dramatic withdrawal effects and diarrhea

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2
Q

list the following for fentanyl

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

target - MOR

Gi

Agonist

used to treat pain.

Comes in both fast acting and short acting. Used in anesthesia and as a dermal patch for cancer pain and other pain. is more potent than morphine.

side effects include addiction, constipation, cloudy mind, fatal overdose

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3
Q

list the following for oxycodone

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

MOR

Gi

analgesic

when combined with acetaminophen = percocet; when combined with aspirin = percodan

side effects include addiction, constipation, cloudy mind, fatal overdose

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4
Q

list the following for hydrocodone

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

MOR

Gi

Agonist

Analgesic

when combined with acetaminophen = vicodin, lortab, and norco

side effects include addiction, constipation, cloudy mind, fatal overdose

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5
Q

list the following for codeine

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

MOR

Gi

agonist

analgesic

depends on CYP2D6 metabolism to morphine. not oral but can be suppository

side effects include addiction, constipation, cloudy mind, fatal overdose (though less of a concern than others)

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6
Q

list the following for morphine

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

MOR

Gi

Agonist

Analgesic

same therapeutic action as other opioids

side effects include addictive and constipation

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7
Q

list the following for endomorphin

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
A

MOR

Gi

Agonist

in hypothalamus, it is found in histaminergic neurons, regulating sedative and arousal behaviors

in neurons of the dorsal horn of the spine it inhibits nociceptors

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8
Q

list the following for endorphin

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
A

MOR & DOR equally

Gi

Agonist

hormone and NT made in pituitary and hypothalamus

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9
Q

list the following for enkephalin

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
A

DOR > MOR

Gi

Agonist

Pain

NT of the brains pain center in the PNS and CNS.
binds to DOR more than MOR and seems to be the main nociceptor inhibitor.

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10
Q

list the following for local anesthetics

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
A

VGSCs

Na channel

Blocker (antagonist)

Anesthetic (apply at site or epidural near spine)

stops AP from signaling to spine
bind and block when activation gate is open.
voltage sensory is shifted from inside the cell.

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11
Q

list the following for thiopental

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
A

GABA-A & AMPA

Cl channel

Agonist of GABA-A, antagonist of AMPA

injectable anesthetic

short acting barbiturate

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12
Q

list the following for propofol

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

GABA-A

Cl channel

agonist

injectable anesthetic

GA used for surgeries, coma, SE, and lethal injection

lowers breathing and BP

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13
Q

list the following for ketamine

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

NMDA receptor

Ca and Na channels

blocker (antagonist)

dissociative anesthetic

dissociates mind from body. is much safer than other GA because it increases breathing, HR, and BP.
can be used at low doses for depression, PTSD, and pain

can cause hallucinations

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14
Q

list the following for carbamazepine

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
A

VGSCs

sodium

blocker

partial, tonic-clonic, SE seizures, and BPD

Class 1b anti-arrhythmic agent (local anesthetics) block VGSCs in the open state and leave the channels closed

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15
Q

list the following for phenytoin

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
A

VGSCs

sodium

blocker

partial, tonic-clonic, SE seizures, and BPD

Class 1b anti-arrhythmic agent (local anesthetics) block VGSCs in the open state and leave the channels closed

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16
Q

list the following for lamotrigine

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
A

VGSC and VGCC

both Na and Ca

blocker

partial, tonic-clonic, SE, and BPD

broad spectrum cation channel blocker; classified for blocking of Na but not same as class 1b b/c also blocks calcium channels

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17
Q

list the following for gabapentin and related

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

axonal Ca channel regulatory subunit

Ca channel

blocker

partial seizure

blocks axonal Ca channel regulation on glutamate neurons

can be used as a pain medication

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18
Q

list the following for levetiracetam

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
A

SV2A

synaptic vesicle protein

blocker

partial, tonic-clonic, and SE seizures

binds selectively to SV2A to prevent exocytosis.

19
Q

list the following for valproate

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

unknown

unknown

every kind of seizure

somehow hyperpolarizes neurons so may act on K channels or Cl channels (non-GABA)

known teratogen

20
Q

list the following for topiramate

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

unknown

unknown

mostly for partial seizures but can be used for all

diminishes depolarizations somehow

side effects include suicide risk

can be used for alcohol rehab, weight loss, and migraines

21
Q

list the following for T channel blockers

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

T-type calcium channel blocker

T-type calcium channel

blocker

absence seizures

block the T-type channels in the thalamus to prevent the brain from going into 15s “sleep-like mode” and prevents the 3 “spikes-slow waves/second” EEG

22
Q

list the following for tiagabine

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
A

GAT-1

transporter

blocker

epilepsy

transport inhibitor of GABA uptake transporter (GAT-1). GABA is not removed from the synapse into astrocytes or axonal bulb

23
Q

list the following for vigabatrin

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
A

GABA-T

GABA-T (enzyme)

blocker

epilepsy

irreversibly inhibits GABA transaminase (GABA-T), the enzyme that metabolizes GABA (meaning there’s more GABA in vesicles so GABA leaks into the synapse; then, there’s less drive to remove GABA from the synapse)

24
Q

list the following for BNZs

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

BNZ site of GABA-A

Cl channel

positive allosteric modulator

epilepsy, anxiety, insomnia, addition

positive allosteric modulator of GABA-A channels (induce IPSPs); do not directly activate GABA-A, but enhance its effect
increase the frequency of GABA opening to GABA-A because it increases the affinity

can help with calming anxiety and panic attacks, and insomnia

side effect = groggy mental state, lethargy, “hangover”, addictive, fatal overdoses with alcohol

25
Q

list the following for Z drugs

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

BNZ site with alpha-1 subunit

Cl channel

sleep

enhances hypothalamus sleep mechanism

less hangover than BNZs

ineffective for epilepsy or axiety

addictive

26
Q

list the following for barbiturates

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

GABA-A & AMPA

Cl channel (also blocks Na channel)

Antagonist of AMPA
Agonist/enhancer of GABA-A

GA and AED

low doses = positive allosteric modulator of GABA-A (holds channel open)
high doses = direct agonist of GABA-A
antagonist to AMPA

can help with epilepsy, anxiety, insomnia, and GA depending on dose and PK

can lead to fatal overdoses (with or without alcohol)

27
Q

list the following for buspirone

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

serotonin 5HT1A GPCR

Gi

agonist

anxiolytic

slow onset, can take 3-4 weeks; used in GAD, but less effective in panic disorders and not used for acute anxiety

lowers anxiety without marked sedative, hypnotic, or euphoric effects

28
Q

list the following for orexin antagonists

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

orexin receptor

Gs

antagonist

sleep

orexin A and B are excitatory neuropeptides for awakening that are silent during sleep.
loss of orexin is associated with narcolepsy and cataplexy

used for sleep but is not as effective as hoped

29
Q

list the following for alskirin

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

renin

protease blocker

JXG (juxtaglomerular cells)

treats high blood pressure (vasodilator/diuretic that blocks renin and decreases ANGII)

side effects - high potassium, renal impairment, potential teratogen

ANGII binding at AT1 inhibits renin release, so lowering ANGII will raise renin levels

30
Q

list the following for ACE inhibitors

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

ACE enzyme

blocker

antihypertensive (vasodilator and diuretic)

blocks ACE protease in the lung, leading to less ANGII but increased bradykinin.
results in vasodilation/diuretic effect

ACE inhibitor cough

“prils”

31
Q

list the following for “sartans”

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

AT1 GPCR ligand binding domain

Gq

blocks ANG2 binding (antagonist)

vascular smooth muscle

vasodilator

blocks GPCR coupled to Gq, thus blocking intracellular Ca increase (so no aldosterone and no vasoconstriction)
– diminished BP and volume

32
Q

list the following for spironolactone

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

MR

steroid hormone receptor

antagonist

lowers blood pressure by blocking aldosterone-induced expression of Na channels, Na/K ATPase, and K channels on the distal tubule

side effect - hyperkalemia

33
Q

list the following for nitroprusside

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

guanylyl cyclase (NO donor)

N/A

NO donor

used for hypertension; lowers BP second after IV infusion

possible cyanide poisoning if infusion lasts for more than an hour

34
Q

list the following for nitroglycerin

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

smooth muscle enzymes –> NO –> GC

N/A

NO donor (needs mtALD) for NO2 –> NO

used for relaxation of coronary arteries for angina pectoris

relaxes smooth muscle with no effect on cardiac or skeletal

DON’T USE WITH A PDE5 INHIBITOR

35
Q

list the following for -afil drugs

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

PDE-5 isozyme

^^^

PDE-5 inhibitor

used to treat ED, pulmonary hypertension, hypertension

retain cGMP in vascular smooth muscle, only enhances NO effect (doesn’t make more)

can cause severe hypotension if taken with an NO agonist

36
Q

list the following for class 0

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

HCN blocker

Na channel

Blocker

only targets pacemaker nodes

used for tachycardia that doesn’t involve contractility

causes bradycardia

37
Q

list the following for class 1a

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

VGSC

Na channel (and some K)

Blocker

sodium block decreases the rapid activation spike and potassium block prolongs the depolarization

the ECG shows a widened (slow) QRS wave and a long QT segment

ex. procainamide

38
Q

list the following for class 1b

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

VGSC

Na channel

blocker

used to treat ectopic heartbeat.

has no impact on conduction velocity, but shortens the QT segment because it only binds to hyper-active (already open) Na channels

39
Q

list the following for class 1c

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

VGSC

Na channel

blocker

slows conduction by blocking sodium channels (strongly), limiting the rapid activation spike

on an ECG shows a very wide QRS wave but repolarization should be about normal (does not affect Q-T)
actually INCREASES contractility (like class 1a)
40
Q

list the following for class 2

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

beta 1 or M2 or adenosine GPCR

Gs or Gi (depending)

blocker (for beta 1) or agonist (for M2 or adenosine)

decreases contractility and HR by decreasing cAMP

41
Q

list the following for class 3

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
A

K channels

K channels

blocker

conduction velocity is unaffected (QRS wave is normal), but contractility is increased. it takes longer for the cell to repolarize, so there is a longer QT segment

42
Q

list the following for class 4 (non-DHP like verapamil)

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

VGCC in cardiac cells

calcium channel

blocker

used to treat high CO and tachycardia

decreased AP (because less calcium) and shows a longer P-R segment on ECG
both contractility and HR decrease
– decreases contractility without causing vasodilation

43
Q

list the following for DHP-like class 4’s

  • target protein
  • G protein subunit/ion channel
  • agonist or antagonist?
  • what’s it used for?
  • therapeutic action?
  • side effects?
A

VGCCs for vascular muscles

Ca channel

blocker

preferentially binds to vascular smooth muscle VGCCs to cause vasodilation

most have ___dipine suffixes

blocks MLCK activation

PDSA (6 decks)

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