Block 6 - literally just drugs Flashcards by Kate Ball

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?

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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list the following for fentanyl

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

target - MOR

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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list the following for oxycodone

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

MOR

analgesic

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

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

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list the following for hydrocodone

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

MOR

Agonist

Analgesic

when combined with acetaminophen = vicodin, lortab, and norco

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

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list the following for codeine

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

MOR

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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list the following for morphine

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

MOR

Agonist

Analgesic

same therapeutic action as other opioids

side effects include addictive and constipation

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list the following for endomorphin

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

MOR

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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list the following for endorphin

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

MOR & DOR equally

Agonist

hormone and NT made in pituitary and hypothalamus

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list the following for enkephalin

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

DOR > MOR

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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list the following for local anesthetics

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

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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list the following for thiopental

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

GABA-A & AMPA

Cl channel

Agonist of GABA-A, antagonist of AMPA

injectable anesthetic

short acting barbiturate

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list the following for propofol

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

GABA-A

Cl channel

agonist

injectable anesthetic

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

lowers breathing and BP

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list the following for ketamine

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

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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list the following for carbamazepine

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

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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list the following for phenytoin

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

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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list the following for lamotrigine

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

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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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?

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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list the following for levetiracetam

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

SV2A

synaptic vesicle protein

blocker

partial, tonic-clonic, and SE seizures

binds selectively to SV2A to prevent exocytosis.

list the following for valproate

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

unknown

every kind of seizure

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

known teratogen

list the following for topiramate

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

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

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?

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

list the following for tiagabine

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

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

list the following for vigabatrin

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

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)

list the following for BNZs

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

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

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?

BNZ site with alpha-1 subunit Cl channel sleep enhances hypothalamus sleep mechanism less hangover than BNZs ineffective for epilepsy or axiety addictive

list the following for barbiturates - target protein - G protein subunit/ion channel - agonist or antagonist? - what's it used for? - therapeutic action? - side effects?

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)

list the following for buspirone - target protein - G protein subunit/ion channel - agonist or antagonist? - what's it used for? - therapeutic action? - side effects?

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

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?

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

list the following for alskirin - target protein - G protein subunit/ion channel - agonist or antagonist? - what's it used for? - therapeutic action? - side effects?

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

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?

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"

list the following for "sartans" - target protein - G protein subunit/ion channel - agonist or antagonist? - what's it used for? - therapeutic action? - side effects?

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

list the following for spironolactone - target protein - G protein subunit/ion channel - agonist or antagonist? - what's it used for? - therapeutic action? - side effects?

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

list the following for nitroprusside - target protein - G protein subunit/ion channel - agonist or antagonist? - what's it used for? - therapeutic action? - side effects?

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

list the following for nitroglycerin - target protein - G protein subunit/ion channel - agonist or antagonist? - what's it used for? - therapeutic action? - side effects?

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

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?

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

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?

HCN blocker Na channel Blocker only targets pacemaker nodes used for tachycardia that doesn't involve contractility causes bradycardia

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?

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

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?

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

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?

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) ```

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?

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

list the following for class 3 - target protein - G protein subunit/ion channel - agonist or antagonist? - what's it used for? - therapeutic action?

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

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?

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

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?

VGCCs for vascular muscles Ca channel blocker preferentially binds to vascular smooth muscle VGCCs to cause vasodilation most have ___dipine suffixes blocks MLCK activation