Exam 5 - Lec 67-68 Antidepressants Watt Flashcards
1st antidepressant drug
a. isoniazid
b. reserpine
c. imipramine
d. selegiline
c. imipramine
(also first TCA)
3 types of depression; what percent are they among depression cases?
reactive (60%)
major depressive disorder (25%)
bipolar affective (15%)
decreased sleep, appetite changes, fatigue, psychomotor dysfunctions, menstrual irregularities, palpitations, constipation, headaches, non-specific body aches
a. physiological features of depression
b. psychological features of depression
c. cognitive features of depression
a. physiological features of depression
dysphoric mood, worthlessness, excessive guilt, loss of interest/pleasure in all or most activities
a. physiological features of depression
b. psychological features of depression
c. cognitive features of depression
b. psychological features of depression
decreased concentration, suicidal ideation
a. physiological features of depression
b. psychological features of depression
c. cognitive features of depression
c. cognitive features of depression
look at slide 6 for drug-induced depression examples
fo sho
what are the 3 hypotheses of depression?
biogenic amine
neuroendocrine
neurotrophic
which is NOT part of the “biogenic amine” hypothesis of depression?
a. Reserpine causes depression by depleting NE and 5HT from vesicles
b. Agents that increase 5HT and NE are effective for treating depression
c. Depressed patients have reduced BDNF levels
d. Genetic polymorphisms in SERT promoter
(s = short vs l = long allele)
e. alterations in 5HT1A/2C and alpha 2 receptors
c. Depressed patients have reduced BDNF levels (this is part of neutrophic hypothesis)
what is the neuroendocrine hypothesis of depression? (from internet)
depression is tied to neuroendocrine dysregulation; changes in HPA axis leads to increased levels of stress hormones
arousal, anxiety-like behavior, disruption of sexual behaviors, and disruption of sleep is involved with
a. CRF1
b. CRF2
a. CRF1
slow adaptive recovery and appetite suppression are involved with
a. CRF1
b. CRF2
b. CRF2
activation of the HPA axis is done by
a. CRF1
b. CRF2
a. CRF1
the HPA axis and CRF is involved in which hypothesis of depression?
a. biogenic amine hypothesis
b. neuroendocrine hypothesis
c. neurotrophic hypothesis
b. neuroendocrine hypothesis
which hypothesis of depression involves BDNF?
a. biogenic amine hypothesis
b. neuroendocrine hypothesis
c. neurotrophic hypothesis
c. neurotrophic hypothesis
explain how BDNF affects dendritic sprouts
more BDNF leads to more sprouting; loss of sprouts leads to depressed state
hippocampal glucocorticoid receptors are activated by cortisol during stress, which _______ BDNF
a. inc
b. dec
b. dec
how long does it take antidepressants to start working? (range)
2-3 weeks
how do MAO inhibitors work?
NE and serotonin are normally degraded by monoamine oxidase (MAO), so by inhibiting MAO, there is an inc amount of NE and serotonin packaged into vesicles and released into the synapse
two non-selective MAO inhibitors
a. phenelzine
b. selegiline
c. moclobemide
d. tranylcypromine
a, d
MAO-B selective
a. phenelzine
b. selegiline
c. moclobemide
d. tranylcypromine
b. selegiline
MAO-A selective
a. phenelzine
b. selegiline
c. moclobemide
d. tranylcypromine
c. moclobemide
what herbal product for depression has MAOI activity?
St. John’s Wort
pts on MAO inhibitors should avoid foods with
a. tyrosine
b. tryptophan
c. tyramine
d. high salt
c. tyramine
(MAO breaks down tyramine)
indications for TCAs (4)
depression
panic disorder
chronic pain
enuresis (bedwetting)
why are patients more likely to commit self-harm or suicide 2 weeks into tx?
when ppl are depressed, they don’t have the energy to take their lives, but when on an antidepressant they have more energy to commit self-harm before the actual therapeutic effects kick in
tertiary amines do not act on which transporter/receptor?
a. NET
b. SERT
c. H1
d. antimuscarinic receptors
e. alpha 1
f. beta 1
f. beta 1
what are the side effects of tertiary amines?
they cause the most sedation, weight gain, autonomic SE; also conduction disturbances of the heart
which tertiary amine is metabolized to desipramine?
a. imipramine
b. amitriptyline
c. clomipramine
d. doxepin
a. imipramine
which tertiary amine is metabolized to nortiptyline?
a. imipramine
b. amitriptyline
c. clomipramine
d. doxepin
b. amitriptyline
which tertiary amine is used for OCD?
a. imipramine
b. amitriptyline
c. clomipramine
d. doxepin
c. clomipramine
which drug can cause orgasm when yawning?
a. imipramine
b. amitriptyline
c. clomipramine
d. doxepin
c. clomipramine
which has less SE, tertiary or secondary amines?
secondary amines
3 secondary amines to know
desipramine
nortiptyline
maprotiline (also a tetracyclic)
mechanism of SSRIs
they block serotonin transporter pumps, inc serotonin in synapse
why are there so many uses for SSRIs?
bc there are 14 serotonin receptors involved in a lot of different things (13 GPCR, 1 ionotropic)
6 SSRIs to know
fluoxetine
fluvoxamine
paroxetine
sertraline
citalopram
escitalopram
which SSRI has little autonomic SE, no sedation?
a. sertraline
b. escitalopram
c. paroxetine
d. fluoxetine
d. fluoxetine
SE of SSRIs (6 of them; slide 36)
N/V
headache
sexual dysfunction
anxiety
insomnia
tremor
what syndrome makes pts feel brain zaps, confusion, and some other SE?
SSRI discontinuation syndrome
what syndrome can occur when giving SSRis with MAOIs, or TCAs?
serotonin syndrome
when given with SSRIs, which drug does NOT increase risk for serotonin syndrome?
a. MAOIs
b. St. John’s Wort
c. TCAs
d. tramadol
e. aspirin
f. triptans
g. metoclopramide
e. aspirin
2 SSRI + 5HT1A partial agonists to know
vilazodone (Viibryd)
vortioxetine (Brintellix)
which drug is both tetracyclic and a secondary amine?
maprotiline
which is FALSE about mirtazapine?
a. NET inhibitor
b. tetracyclic structure
c. alpha 2 antag
d. 5HT2 and 5HT3 antag
e. H1 antag
a. NET inhibitor
(it is a receptor antagonist, doesn’t hit transporters)
2 tetracyclic drugs to know
maprotiline
mirtazapine
which drug is unicyclic?
a. maprotiline
b. mirtazapine
c. bupropion
c. bupropion
which is FALSE about bupropion?
a. DAT, NET, SERT inhibitor
b. H1 antagonism
c. treats GAD
d. unicyclic
e. Zyban for smoking cessation
b. H1 antagonism
which drug is described below?
-5HT2A antag
-weak SERT inhibitor
-off label use as hypnotic
-pts generall wake up refreshed, usually no morning hangover
trazodone
which drug is a 5HT2A antagonist/SERT inhibitor?
a. trazodone
b. bupropion
c. mirtazapine
d. amitriptyline
a. trazodone
5 SNRIs to know
venlafaxine
desvenlafaxine
duloxetine
milnacipran
levomilnacipran
which SNRI is used for GAD, panic disorder, diabetic neuropathy, and migraine prophylaxis?
a. venlafaxine
b. desvenlafaxine
c. duloxetine
d. milnacipran
e. levomilnacipran
a. venlafaxine
which SNRI can be used for treatment of vasomotor symptoms associated with menopause?
a. venlafaxine
b. desvenlafaxine
c. duloxetine
d. milnacipran
e. levomilnacipran
b. desvenlafaxine
which SNRI treats GAD and peripheral neuropathy?
a. venlafaxine
b. desvenlafaxine
c. duloxetine
d. milnacipran
e. levomilnacipran
c. duloxetine
which SNRI is approved for fibromyalgia?
a. venlafaxine
b. desvenlafaxine
c. duloxetine
d. milnacipran
e. levomilnacipran
d. milnacipran
which SNRI is the active enantiomer of milnacipran and was approved in 2013?
a. venlafaxine
b. desvenlafaxine
c. duloxetine
d. milnacipran
e. levomilnacipran
e. levomilnacipran
2 NSRI drugs to know (NE selective reuptake inhibitors)
reboxetine
atomoxetine
which NSRI is not used in the USA?
a. reboxetine
b. atomoxetine
a. reboxetine
which NSRI was originally intended to be an antidepressant drug and was not approved, so it is used for ADHD?
a. reboxetine
b. atomoxetine
b. atomoxetine
clomipramine selectivity for 5-HT:NE
a. 1:136
b. 1:7
c. 8:1
d. 523:1
a. 1:136 (SERT selective)
amitriptyline selectivity for 5-HT:NE
a. 1:136
b. 1:7
c. 8:1
d. 523:1
b. 1:7
nortriptyline selectivity for 5-HT:NE
a. 1:136
b. 1:7
c. 8:1
d. 523:1
d. 8:1 (NE selective)
maprotiline selectivity for 5-HT:NE
a. 1:136
b. 1:7
c. 8:1
d. 523:1
d. 523:1 (NET selective)
what drugs block serotonin, NE, and dopamine reuptake?
SNDRIs aka “triple blockers”
what drug class are the rapidly acting antidepressants?
NMDA antagonists
2 clinically used NMDA antagonists
ketamine and esketamine
which should be given at subanesthetic doses?
a. ketamine
b. esketamine
a. ketamine
which is intranasally and available only through REMS?
a. ketamine
b. esketamine
b. esketamine
T or F: esketamine is used in conjunction with an oral antidepressant
T
FDA-approved drug for postpartum depression
brexanolone
two SSRIs for postpartum depression
fluoxetine and paroxetine
SNRI for postpartum depression
venlafaxine
T or F: antidepressants can be used for pain
T
drug for hypoactive sexual desire disorder
filbanserin (Addyi)
(“female Viagra”)
approx ___-___% of Americans have bipolar disorder; onset is < ____ years old
1.5-3%
< 30
5 types of bipolar disorder
bipolar I
bipolar II
cyclothymia disorder
unspecified bipolar and related disorder
substance-induced mood disorder
what two CCBs can be used for the treatment of bipolar?
verapamil, nimodipine
mechanism of lithium (2 things; look at slide 61)
-depletion of PIP2 and signaling (IP3 and PKC)
-modulate GSK3 (phosphorylation and binding partners)
valproate MOA (4 things on slide)
-inc GABA activity, inhibit GABA transaminase
-block Na+ channels
-block T-type Ca2+ channels
-inhibits histone deacetylase (HDAC5)
T or F: lithium has a small therapeutic index
T (so it has lots of SE)
3 mood stabilizers (one is a drug, two are drug classes)
lithium
anticonvulsants
atypical antipsychotics
how does carbamazepine/oxcarbazepine work for bipolar disorder? (from internet)
they inhibit sodium channels, which reduces the excitability of neurons and can help stabilize mood and bipolar sx
which anticonvulsant acts on sodium and calcium channels?
a. carbamazepine
b. lamotrigine
c. topiramate
b. lamotrigine
which anticonvulsant acts on sodium channels and also may enhance GABA at receptor and blocks excitatory AA receptors?
a. carbamazepine
b. lamotrigine
c. topiramate
c. topiramate
look at slide 64 for atypical antipsychotics for bipolar disorder
sure thing
