CNS Drugs 1 Flashcards by Jocelyn s

What are the 4 binding sites of GABA receptors?

GABA, benzodiazepine, barbiturate, and ethanol binding site

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What is the role of the GABA neurotransmitter and receptor?

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

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Name 4 Benzodiazepines

Hint: suffix -am

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

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Name the barbiturate used primarily for seizure treatment and its MOA

Phenobarbital, enhances GABA effects to inhibit neurotransmission

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What are adverse effects of benzodiazepines?

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

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Adverse effects of barbiturate drugs

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

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

ethanol & barbiturates= Zero-order

Benzos=First order

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Which CNS drugs are lethal at high doses?

ethanol, barbiturates

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

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

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What do zolpidem & eszopiclone (GABA agonists) treat?

insomnia (short duration of action)

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Side effects of non-benzo/barbiturate GABA agonists?

zolpidem & lunesta

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

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

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

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Adverse effects of SSRIs

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

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

venlafaxine & duloxetine

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Side effects of SNRIs (venlafaxine & duloxetine)

same as SSRIs + raised BP

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MOA of TCAs amitriptyline & imipramine

same as SNRIs

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Side effects of TCAs amitriptyline & imipramine

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

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Why is phenelzine (MAOI) rarely used?

food, drink, and drug interactions

What is the MOA of phenelzine? Hint: MAOI

inhibits monoamine oxidase to increase norepinephrine, serotonin, and dopamine

Adverse effects of phenelzine (MAOI)

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

MOA of the muscle relaxant cyclobenzaprine

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

SIde effects of the muscle relaxant cyclobenzaprine

sedation and STRONG anti-cholinergic effects

Name the (2) serotonin receptor agonists used for migraine

sumatriptan and zolmitriptan

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

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

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

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

MOA of bupropion (Wellbutrin; Zyban)

increases norepinephrine & dopamine levels by inhibiting their reuptake

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

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

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

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

Mirtazapine MOA

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

Trazodone MOA

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

Adverse effects of lithium

increased IOP and anticholinergic effects

MOA of lithium

reduces norepinephrine and dopamine, narrow therapeutic index

List 4 dopamine pathways in the brain

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

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

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

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

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

Side effects of ALL Typical antipsychotics (dopa antagonists)

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

Side effects of Atypical antipsychotics

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

Side effects of drugs that increase dopamine

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

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

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

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

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

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

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

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??

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

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

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

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

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

CNS Drugs 1 Flashcards

Intro to drugs of the CNS