antidepressants Flashcards
gepirone (trade name) is….
drug class?
Exxua
serotonin modulators?
escitalopram (trade name) is….
drug class?
Lexapro
SSRI
paroxetine (trade name) is….
drug class?
Paxil
SSRI
esketamine (trade name) is….
drug class?
Spravato
NMDA receptor antagonists
monoamine theory of depression
depression is due to monoamine deficiency
NTs involved in depression
DA, 5HT, NE, E
DA, 5HT, NE, E are all …
monoamines
second messanger systems in depression
types of antidepressants
MAOIs
Reduce enzymatic deactivation of monoamines
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)
how do TCAs work?
Block reuptake of 5-HT, NE
Block post-synaptic H, AChM, NE
what does blockage of H do?
Blockade of H = drowsiness, sedation
what does blockage of AChM do?
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
issues with TCAs
Cardiotoxic in large doses
Risk of OD
what drugs are good for pts w depression and chronic pain? why?
TCAs; analgesic properties
TCAs absorption
MAOIs inhibit ______?
MAOa; Most bind irreversibly to MAOA
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
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
selegiline is a _____; it is different than others because _____
MAOI; it is transdermally applied so no issues w GI tract
SSRIs
(common ones and their trade names)
Fluoxetine (Prozac)
Sertraline (Zoloft)
Fluvoxamine (Luvox)
Citalopram (Celexa)
Escitalopram (Lexapro)
how do SSRIs work?
Do not bind to 5-HT receptors, rather make 5-HT more available to
bind with receptors
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
