antidepressants Flashcards by Darian Wilson

gepirone (trade name) is….

drug class?

Exxua

serotonin modulators?

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escitalopram (trade name) is….

drug class?

Lexapro

SSRI

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paroxetine (trade name) is….

drug class?

Paxil

SSRI

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esketamine (trade name) is….

drug class?

Spravato

NMDA receptor antagonists

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monoamine theory of depression

depression is due to monoamine deficiency

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NTs involved in depression

DA, 5HT, NE, E

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DA, 5HT, NE, E are all …

monoamines

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second messanger systems in depression

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types of antidepressants

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MAOIs

Reduce enzymatic deactivation of monoamines

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tricyclics

imipramine (Tofranil)
desipramine (Norpramin; active metabolite of Imipramine)
trimipramine (Surmontil)
protriptyline (Vivactil)
amitriptyline (Elavil)
nortriptyline (Pamelor, Aventil; active metabolite of amitriptyline)
doxepin (Adapin, Sinequan)
clomipramine (Anafranil)

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how do TCAs work?

Block reuptake of 5-HT, NE

Block post-synaptic H, AChM, NE

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what does blockage of H do?

Blockade of H = drowsiness, sedation

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what does blockage of AChM do?

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SE profiles for TCAs

Blockade of H = drowsiness, sedation

– Blockade of AChM = confusion, memory & cognitive impairment (hippocampus), dry mouth, blurred vision, tachycardia, urinary retention (ANS)

– Blockade of NE receptors = orthostatic hypotension (PNS)

Side effect profiles vary, depending on affinity for H, AChM,
NE

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issues with TCAs

Cardiotoxic in large doses
Risk of OD

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what drugs are good for pts w depression and chronic pain? why?

TCAs; analgesic properties

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TCAs absorption

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MAOIs inhibit ______?

MAOa; Most bind irreversibly to MAOA

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issues with MAOIs

Consumption of foods containing high levels of tyramine is problematic
Product of fermentation
“Wine and Cheese Effect”
Increases blood pressure
Adherence to a strict diet eliminates danger

Low TI, so OD is possible

Side Effects

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MAOI SE profile?

Sedation
Orthostatic hypotension
Dry mouth
Nervousness
Muscle ache
Paresthesia (pricking or tingling sensation)—usually in extremities
may be from the MAOI’s interference with vitamin B6 metabolism
100 mg of vitamin B6 daily may reduce or eliminate these symptoms
Insomnia
Weight gain
Sexual dysfunction
Anorgasmia (inability to achieve orgasm)
Impotency
Urinary difficulty

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selegiline is a _____; it is different than others because _____

MAOI; it is transdermally applied so no issues w GI tract

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SSRIs
(common ones and their trade names)

Fluoxetine (Prozac)
Sertraline (Zoloft)
Fluvoxamine (Luvox)
Citalopram (Celexa)
Escitalopram (Lexapro)

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how do SSRIs work?

Do not bind to 5-HT receptors, rather make 5-HT more available to
bind with receptors

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side effects of SSRIs

withdrawal syndrome sexual dysfunction serotonin syndrome

what is serotonin syndrome? what causes it ?

High doses, combination of SSRI with another 5-HT agonist Cognitive disturbances, agitation, ANS dysfunction (like high fevers) motor problems, hallucinations

acronym for SSRI withdrawal syndrome

FINISH: Flu-like symptoms, Insomnia, Nausea, Imbalance, Sensory disturbances, Hyperarousal (FINISH)

fluoxetine trade name

Prozac

what was the first SSRI

prozac

sertraline (trade name)

zoloft

issue w zoloft

Higher risk of serotonin syndrome and withdrawal syndrome

fluvoxamine (trade name)

Luvox

what drug has the shortest half life of all SSRIs?

fluvoxamine (Luvox)

what is Luvox best used for? why?

High affinity for NE α1, which produces anxiolytic effects Often used to treat anxiety disorders

SNRIs

Highly selective for NT and 5-HT, with little binding to other receptors Fewer side effects, particularly ones related to increased serotonergic tone Analgesic

issues of nefazodone

Increased risk for severe liver damage

nefazodone (trade name)

Serzone

what 2 SNRIs are approved for tmt of fibromyalgia

milnacipran (Savella) duloxetine (Cymbalta)

milnacipran (trade name) class of drug

Savella SNRI not approved for depression

issues w duloxetine (Cymbalta)

Not recommended for bipolar pxts; may induce mania

duloxetine (trade name) drug class?

cymbalta SNRI

venlafaxine (Effexor) is used off label for

cocaine dependence

issues w venlafaxine (Effexor)

inc liability for suicide

tetracyclics (common ones, how do they work?) used for?

mirtazepine (Remeron) Does not block reuptake transporters Increases release of 5-HT and NE

pros of mirtazepine (Remeron)?

Increased appetite/weight gain Good for txting pxts with eating or wasting disorders, and elderly pxts Very few sexual side effects

STARD study? conclusions?

Sequenced Treatment Alternatives to Relieve Depression ~2/3 pxts achieved remission Substantial participation withdrawal after each phase: 21% phase 1, 30% phase 2, 42% phase 3 Before giving up on antidepressants Try 2 or 3 Give them at least 12 weeks (3 months) It may be that antidepressant therapy works better in more severely depressed pxts (HAM-D >25)

why is gepirone special?

The neurogenic theory of depression stems from recent findings that in the mature brain

Neurons are capable of being repaired and produced

First-generation tricyclic antidepressants are defined by a commonality in basic

Molecular structure

Which statement below best describes the pharmacodynamics of Escitalopram It primarily effects ____ systems with minimal effects on ___, ___ , & ___ systems

It primarily effects 5-HT systems with minimal effects on NE/DA/ACh systems

Orthostatic hypotension is a common side effect of

TCAs and MAOIs

What is the pharmacodynamic mechanism of bupropion? (trade name of buproprion?)

it blocks DA & NE reuptake wellbutrin

An SNRI would be a good treatment choice for someone

with MDD and pain

The tricyclic antidepressants differ from Prozac and Zoloft in that they also have major effects on ________________.

norepinephrine

maprotiline (trade name, class of drug?)

(Ludiomil) – Modified TCA

amoxapine (trade name, class of drug?)

(Ascendin) – NET antagonist

trazodone (trade name, class of drug?)

(Desyrel) – Weak NET, SERT antagonist – Blocks 5-HT2A

clomipramine (trade name, class of drug?)

(Anafranil) – NET, SERT antagonist, with higher affinity for SERT

issues with maprotiline (Ludiomil)?

epileptogenic (can cause seizures)

issues w amoxapine (Ascendin) ; why?

Blocks DA receptors – can induce Parkinsonian-like EPS

________ is better than TCAs at relieving anxiety and behavioral agitation

amoxapine (Ascendin)

trazodone (Desryl) has heavy _______ effects, therefore it is primarily used as a _______

sedative ; hypnotic

clomipramine (Anafranil) is used to treat ________ , _________, & _________. Particularly _______ & ______

Used to treat anxiety and pain as well as depression, particularly OCD and Panic Disorder

how does clomipramine (Anafranil) work?

NET, SERT antagonist, with higher affinity for SERT

SSRIs are recommended to be dosed at ________? why?

nighttime; they can be sedating

SSRIs are more _________ than TCAs; why?

safe ; no cardiac effects

Luvox (fluvoxatine) has a high affinity for ______, which makes it helpful for tmt of ________

NE a1 ; anxiety

antidepressants Flashcards

(67 cards)