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Systemic Pharmacology OPTM 5133 > CNS Drugs 1 > Flashcards

CNS Drugs 1 Flashcards

Intro to drugs of the CNS

1
Q

What are the 4 binding sites of GABA receptors?

A

GABA, benzodiazepine, barbiturate, and ethanol binding site

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2
Q

What is the role of the GABA neurotransmitter and receptor?

A

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

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3
Q

Name 4 Benzodiazepines

Hint: suffix -am

A

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

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4
Q

Name the barbiturate used primarily for seizure treatment and its MOA

A

Phenobarbital, enhances GABA effects to inhibit neurotransmission

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5
Q

What are adverse effects of benzodiazepines?

A

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

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6
Q

Adverse effects of barbiturate drugs

A

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

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7
Q

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

A

ethanol & barbiturates= Zero-order

Benzos=First order

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8
Q

Which CNS drugs are lethal at high doses?

A

ethanol, barbiturates

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9
Q

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

A

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

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10
Q

What do zolpidem & eszopiclone (GABA agonists) treat?

A

insomnia (short duration of action)

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11
Q

Side effects of non-benzo/barbiturate GABA agonists?

zolpidem & lunesta

A

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

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12
Q

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

A

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

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13
Q

Adverse effects of SSRIs

A

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

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14
Q

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

A

venlafaxine & duloxetine

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15
Q

Side effects of SNRIs (venlafaxine & duloxetine)

A

same as SSRIs + raised BP

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16
Q

MOA of TCAs amitriptyline & imipramine

A

same as SNRIs

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17
Q

Side effects of TCAs amitriptyline & imipramine

A

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

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18
Q

Why is phenelzine (MAOI) rarely used?

A

food, drink, and drug interactions

19
Q

What is the MOA of phenelzine? Hint: MAOI

A

inhibits monoamine oxidase to increase norepinephrine, serotonin, and dopamine

20
Q

Adverse effects of phenelzine (MAOI)

A

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

21
Q

MOA of the muscle relaxant cyclobenzaprine

A

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

22
Q

SIde effects of the muscle relaxant cyclobenzaprine

A

sedation and STRONG anti-cholinergic effects

23
Q

Name the (2) serotonin receptor agonists used for migraine

A

sumatriptan and zolmitriptan

24
Q

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

A

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

25
Q

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

A

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

26
Q

MOA of bupropion (Wellbutrin; Zyban)

A

increases norepinephrine & dopamine levels by inhibiting their reuptake

27
Q

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

A

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

28
Q

Side effects of mirtazapine and trazodone.

What are they most used for?

A

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

29
Q

Mirtazapine MOA

A

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

30
Q

Trazodone MOA

A

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

31
Q

Adverse effects of lithium

A

increased IOP and anticholinergic effects

32
Q

MOA of lithium

A

reduces norepinephrine and dopamine, narrow therapeutic index

33
Q

List 4 dopamine pathways in the brain

A

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

34
Q

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

A

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

35
Q

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

A

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

36
Q

Side effects of ALL Typical antipsychotics (dopa antagonists)

A

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

37
Q

Side effects of Atypical antipsychotics

A

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

38
Q

Side effects of drugs that increase dopamine

A

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

39
Q

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

A

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

40
Q

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

A

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

41
Q

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

A

Inhibits Na channels to reduce firing rate;

causes sedation & low platelets/ increased bleeding

42
Q

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??

A

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

43
Q

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

A

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

44
Q

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

A

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

Systemic Pharmacology OPTM 5133 (8 decks)

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