CNS Drugs 1

Question 1

What are the 4 binding sites of GABA receptors?

Answer 1

GABA, benzodiazepine, barbiturate, and ethanol binding site

Question 2

What is the role of the GABA neurotransmitter and receptor?

Answer 2

INHIBIT neurons from firing (Cl- influx causes hyperpolarization, prevents AP)

Question 3

Name 4 Benzodiazepines

Hint: suffix -am

Answer 3

Diazepam (Valium), alprazolam (Xanax), Lorazepam (Ativan), and clonazepam (Klonopin)

Question 4

Name the barbiturate used primarily for seizure treatment and its MOA

Answer 4

Phenobarbital, enhances GABA effects to inhibit neurotransmission

Question 5

What are adverse effects of benzodiazepines?

Answer 5

Fatal with alcohol/opioids, reduced coordination (risk of falls), dependence, addiction and withdrawal, mild anti-cholinergic effects

Question 6

Adverse effects of barbiturate drugs

Answer 6

Over sedation/fatal OD, respiratory depression, fatal when combined with opioids, alcohol, or benzodiazepines

Question 7

What order of kinetics do alcochol, barbiturates, and benzodiazepines follow?

Answer 7

ethanol & barbiturates= Zero-order

Benzos=First order

Question 8

Which CNS drugs are lethal at high doses?

Answer 8

ethanol, barbiturates

Question 9

What is the MOA of zolpidem (Ambien) & eszopiclone (Lunesta)?
Hint: GABA agonists

Answer 9

Bind to benzodiazepine site on GABA receptor, but have different chemical structure

Question 10

What do zolpidem & eszopiclone (GABA agonists) treat?

Answer 10

insomnia (short duration of action)

Question 11

Side effects of non-benzo/barbiturate GABA agonists?

zolpidem & lunesta

Answer 11

sleep disorders (sleepwalking), visual hallucinations, & some anti-cholinergic effects

Question 12

Which (6) drugs increase serotonin by inhibiting reuptake in neurons? (SSRIs)

Answer 12

citalopram, escitalopram, fluoxetine (Prozac), fluvoxamine, paroxetine, & sertraline

Question 13

Adverse effects of SSRIs

Answer 13

sexual dysfunction, platelet inhibition (easy bruising/bleeding), serotonin syndrome, & mild anti-cholinergic effects

Question 14

Name of (2) drugs that increase norepinephrine and serotonin by inhibiting their reuptake (SNRIs)

Answer 14

venlafaxine & duloxetine

Question 15

Side effects of SNRIs (venlafaxine & duloxetine)

Answer 15

same as SSRIs + raised BP

Question 16

MOA of TCAs amitriptyline & imipramine

Answer 16

same as SNRIs

Question 17

Side effects of TCAs amitriptyline & imipramine

Answer 17

Same as SNRIs + sedation and OD fatal (1 pill can kill a toddler), and anticholinergic effects are STRONG

Question 18

Why is phenelzine (MAOI) rarely used?

Answer 18

food, drink, and drug interactions

Question 19

What is the MOA of phenelzine? Hint: MAOI

Answer 19

inhibits monoamine oxidase to increase norepinephrine, serotonin, and dopamine

Question 20

Adverse effects of phenelzine (MAOI)

Answer 20

nystagmus, mild anticholinergic effects, and hypertension that can be lethal with food/drinks that contain tyramine

Question 21

MOA of the muscle relaxant cyclobenzaprine

Answer 21

somehow increases norepinephrine in the brain causing skeletal muscles to relax, similar chemical structure to TCAs

Question 22

SIde effects of the muscle relaxant cyclobenzaprine

Answer 22

sedation and STRONG anti-cholinergic effects

Question 23

Name the (2) serotonin receptor agonists used for migraine

Answer 23

sumatriptan and zolmitriptan

Question 24

side effects of sumatriptan and zolmitriptan (serotonin receptor agonists used for migraine)

Answer 24

non-arteritic ischemic optic neuropathy (NAION), retinal artery & vein occlusions, heart attack and stroke

Question 25

MOA of sumatriptan and zolmitriptan (serotonin receptor agonists for migraine)

Answer 25

increases effect of serotonin in CNS blood vessels, causing vasoconstriction and reduced inflammation

Question 26

MOA of bupropion (Wellbutrin; Zyban)

Answer 26

increases norepinephrine & dopamine levels by inhibiting their reuptake

Question 27

What else is the antidepressant bupropion used for and what are its side effects?

Answer 27

smoking cessation treatment (Zyban), strong sedation and anticholinergic effects

Question 28

Side effects of mirtazapine and trazodone. | What are they most used for?

Answer 28

strong sedatives, used more as a sleep air, and anticholinergic effects

Question 29

Mirtazapine MOA

Answer 29

somehow increases norepinephrine & serotonin release from neurons, blocks histamine binding

Question 30

Trazodone MOA

Answer 30

blocks serotonin reuptake/binding to 5HT receptors, blocks histamine binding

Question 31

Adverse effects of lithium

Answer 31

increased IOP and anticholinergic effects

Question 32

MOA of lithium

Answer 32

reduces norepinephrine and dopamine, narrow therapeutic index

Question 33

List 4 dopamine pathways in the brain

Answer 33

1.nigrostriatal 2. mesolimbic, and 3. tuberoinfundibular systems 4. chemoreceptor trigger zone in medulla (vomiting center)

Question 34

Name (3) typical and (1) atypical anti-psychotics and their MOA. (dopamine receptor antagonists)

Answer 34

(haloperidol, thioridazine, chlorpromazine, aripiprazole) Block dopamine from binding to its receptor, reducing effects of dopamine pathways

Question 35

Ocular side effects of the phenothiazines thioridazine & chlorpromazine. (Typical antipsychotics, dopa antagonists)

Answer 35

pigmentation on cornea, anterior stellate cataracts, pigment disruption of RPE, and oculogyric crisis, retinal toxicity

Question 36

Side effects of ALL Typical antipsychotics (dopa antagonists)

Answer 36

Parkinson's-like movement disorders & anti-cholinergic effects

Question 37

Side effects of Atypical antipsychotics

Answer 37

Metabolic disorder (DM, weight gain) & mild movement disorders

Question 38

Side effects of drugs that increase dopamine

Answer 38

Adrenergic agonist effects and mydriasis (a1 stimulation iris dilator), cardiovascular issues. nausea, vivid dreams, addictive, hallucinogen/psychotic behaviors

Question 39

MOA and side effects of donepezil (Aricept) used for Alzheimer's Hint: acetylcholinesterase inhibitor

Answer 39

(Indirect cholinergic agonist) reversible, inhibits acetylcholinesterase-->increases ACh effects & parasympathetic response (miosis, lower BP, sweating...)

Question 40

MOA and side effects of the anti-convulsant phenytoin (Dilantin)

Answer 40

blocks Na channels in neurons to decrease firing rate; causes nystagmus, diplopia, EOM palsies, gingival hyperplasia, hirsutism & sedation

Question 41

MOA and side effects of the anti-convulsant divalproex (Depakote) also used as an anti-mania drug

Answer 41

Inhibits Na channels to reduce firing rate; | causes sedation & low platelets/ increased bleeding

Question 42

What is the name of the anti-seizure drug that is also used for migraine, weight loss, and more, and what are its 3 MOAs??

Answer 42

topiramate (Topamax) 1. Blocks Na channels 2. increases GABA and 3.blocks glutamate receptors, all to decrease neuron firing rate

Question 43

Topiramate causes dizziness, sedation, loss of appetite & weight, diplopia, nystagmus, &idiosyncratic drug reaction. Define idiosyncratic drug reaction

Answer 43

A bilateral transient myopic shift that can lead to bilateral angle closure (choroidal swelling pushes everything fwd.

Question 44

List the uses of gabapentin & pregabalin, their MOA, and side effects.

Answer 44

Nerve pain due to diabetic neuropathy or postherpetic neuralgia (after shingles), anti-convulsant, psychiatric disorders. Binds to Ca channels to reduce excitatory neurotransmitters like glutamate & norepinephrine; causes sedation & dizziness