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87 Cards in this Set

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Most adrenergically active SNRI?
levomilnacipran [Fetzima]
Max dose of desvenlafaxine [Pristiq] for MDD?
50 mg/day
SNRI that binds to both 5-HT and NE at lowest dose?
duloxetine [Cymbalta]
Dr. Ehret's favorite antidepressant?
duloxetine [Cymbalta]

- also indicated for pain, fibromyalgia
- weight loss can be a "good" side effect
Target dose for duloxetine [Cymbalta] for MDD?
60 mg/day
Of the 4 SNRI's approved for MDD, which is the only one that has an effect on CYP?
duloxetine [Cymbalta]

- moderate inhibitor of 2D6
SSRI with the longest half-life?
fluoxetine [Prozac]

- 96-144 h for fluoxetine
- 96-384 h for active metabolite (norfluoxetine)
In general, are SSRIs "activating"?
Yes. They can cause insomnia. This is why SSRIs are usually taken in the morning.
Fluoxetine is a potent inhibitor of which CYP?
2D6
Which SSRI is most likely to cause diarrhea?
sertraline [Zoloft]

(Take with food.)
SSRI that is not FDA-approved for MDD but is as effective as other SSRIs for treating MDD?
fluvoxamine [Luvox]

(OCD is the only FDA-approved indication.)
SSRI with the shortest half-life?
fluvoxamine [Luvox]

15 h
Fluvoxamine [Luvox] is a strong inhibitor of which CYPs?
1A2, 3A4

(also 2C19 to a lesser extent)
Max dose of sertraline [Zoloft]?
200 mg/day
Max dose of fluvoxamine [Luvox]?
300 mg/day
Effective dosing ranges for sertraline and fluvoxamine?
100-200 mg/day for both
The only SSRI that is Pregnancy Category D?
paroxetine [Paxil]

- causes pulmonary HTN in infants
Paroxetine is a potent inhibitor of which CYP?
2D6
SSRI with mild anticholinergic effects?
paroxetine [Paxil]
The most CELEctive SSRIs?
RS-citalopram [CELExa]
S-citalopram [Lexapro]

= less likelihood of sexual dysfunction due to greater selectivity
Max dose of citalopram [Celexa] for MDD?
40 mg/day

- anything higher may cause QTc prolongation
Max dose of escitalopram [Lexapro]?
20 mg/day
Which are more likely to cause HTN: SSRIs or SNRIs?
SNRIs

(increased NE = adrenergic effects)
Max dose of desvenlafaxine [Pristiq] for MDD?
50 mg/day

50 mg QOD for ESRD since it's metabolized by UGT and excreted renally
SNRI that may cause dose-related MINOR elevations in BP?
venlafaxine [Effexor]
SNRI that may cause SIGNIFICANT elevations in BP?
levomilnacipran [Fetzima]

(= the most adrenergically active SNRI)
Newest SNRI on the market?
levomilnacipran [Fetzima]
The one SNRI that is NOT a CYP substrate?
levomilnacipran [Fetzima]

(It's renally excreted.)
Can levomilnacipran [Fetzima] ER capsules be crushed or opened?
No.
Dosing range for levomilnacipran [Fetzima]?
40-120 mg/day
If you have "ants in your pants," what condition are you experiencing?
Akathisia

(= internal restlessness)
The mildest symptom in serotonin sydrome?
Akathisia
The most severe/life-threatening symptom in serotonin syndrome?
Hyperthermia
Is it a good idea to give a SSRI to someone with a GI bleed risk?
No. SSRIs decrease 5-HT uptake from the blood to platelets.

Think about it:

- 5-HT2A receptors are found on platelets, smooth muscle and the cerebral cortex
- Activation of 5-HT2A on platelets leads to platelet aggregation

- SSRIs block the uptake of 5-HT by platelets from the blood-- platelets do not synthesize 5-HT, so 5-HT must come from somewhere else.

- Thus, SSRIs cause less 5-HT to be taken up by platelets from the blood. In effect, there is less aggregation of platelets, leading to bleeding. This is more likely to occur in the GI than in the skin.
What are the two hormones that are stored in/released from the posterior pituitary "gland"?
antidiuretic hormone; aka vasopressin, aka arginine vasopressin (AVP)

oxytocin
Does hyponatremia occur because a person has a deficiency in sodium or because a person is retaining excess water?
Hyponatremia results from an excess of water, not a deficiency in sodium. It may result from an inappropriate secretion of antidiuretic hormone (SIADH), which results in water retention.
Clinical presentation of SIADH?
Confusion
Lethargy
Dizziness
Delirium
Fatigue
Anorexia
Onset of SIADH?
3 days to 4 months
How long does it take for hyponatremia to resolve after d/c the offending agent?
2 weeks
Discontinuation syndrome is aka what?

Least likely to occur with the SSRI ____ and most likely to occur with the SSRI _____ due to the drug's long and short half-life, respectively.
Withdrawal

fluoxetine
fluvoxamine, paroxetine
Symptoms of d/c syndrome mimic symptoms of what illness?
Flu
Sexual dysfunction is most likely to occur with increased activity of what NT/type of neuron?
5-HT/serotonergic neurons
Pharmacologic class of bupropion [Wellbutrin]?
NDRI

(= NE/DA reuptake inhibitor)
Best times to dose bupropion [Wellbutrin] if giving BID?
7 am and 1 pm

(NOT q 12 h due to activating effects!)
Is it a good idea to give bupropion [Wellbutrin] to someone who suffers from anorexia, bulimia or epilepsy?
No. Bupropion may LOWER seizure thresholds.
Psychosis is a side effect of bupropion. Why do you think this occurs?
Bupropion is a NDRI. Increasing DA in the limbic system may cause psychosis. Think about the pathophys. of schizophrenia-- DA hyperactivity in the mesolimbic pathway.
Bupropion inhibits which CYP?
2D6
T/F? Bupropion may be useful for treating ADHD since it is a stimulating drug.
True.
Pharmacologic class of mirtazapine [Remeron]?
alpha-2 antagonist

(aka SNDI = "serotonin and NE disinhibitor")
Antidepressant that may be useful for an elderly patient who has a decreased appetite and trouble sleeping?
mirtazapine [Remeron]

Potent antagonist of:
- central H1 = sedation; inc. appetite
- 5-HT2 (5-HT2C, which is in the hypothalamus) = inc. appetite
- 5-HT3, which is on parasympathetic nerves = sympathetic-type effects, such as dry mouth, constipation

Moderate antagonism of:
- peripheral alpha-1-adrenergic receptors
- peripheral muscarinic receptors
Starting dose of mirtazapine?
7.5-15 mg qhs
Effective dose range of mirtazapine?
15-45 mg
Max dose of mirtazapine?
60 mg
2 MAOIs that Dr. Ehret mentioned?
- phenelzine [Nardil]
- tranylcypromine [Parnate]
- phenelzine [Nardil]
- tranylcypromine [Parnate]
Class of antidepressants that have the highest rate of switching from depression to mania?
MAOIs
CV effects of MAOIs?
- Decreased QTc interval
- Decreased HR
- HYPOtension
2 things that can cause hypertensive crisis-- a concern in patients taking MAOI?
- tyramine-containing foods
- concomitant use of sympathomimetics
Tyramine increases the release of which NT in the periphery?
NE

(Tyramine is a naturally occurring monoamine that is derived from tyrosine. It cannot cross the BBB.)
If switching from a MAOI to an SSRI, how long must you wait before starting the SSRI?
2 weeks

(This is how long if takes for MAO to regenerate.)
If switching from an SSRI to a MAOI, how long must you wait before starting the MAOI?
Wash-out period of SSRI depends on its half-life.

(Fluoxetine has a long half-life, so wait 5 weeks.)
Drugs to avoid while taking MAOI?
- Indirect/direct sympathomimetics
- Other antidepressants
- Buspirone
- Meperidine
- Dextromethorphan
- Cocaine
The name "TCA" reflects the structure of the drug class. What is the actual pharmacologic class?
SNRI
Antidepressant drug class that is used mostly for treating pain and not depression?
TCA
Antidepressant drug class with the most anticholinergic effects?
TCA
Common AEs of TCAs?
- sedation
- orthostatic hypotension
- anticholinergic effects
Serious AEs of TCAs?
- switching
- arrhythmias
- seizures
- death
Plasma concentration monitoring is (RARELY) done for which 2 TCAs?
- nortriptyline: 50-150 ng/mL
- desipramine: 125-300 ng/mL

(These two are secondary amines, metabolites of tertiary amines that are also commercially available.)
Which antidepressant drug class has lots of drug-drug interactions, i.e. things that can either increase or decrease levels of antidepressant?
TCA
Antidepressant that has black box warning for potential to cause hepatic failure?
nefazodone
Nefazodone inhibits which CYP?
3A4
Rare but serious AE of nefazodone?
Priapism

("nefazoBONE")
Rare but serious AE of trazodone?
Priapism

("trazoBONE")
Pharmacologic class of trazodone?
SARI with strong antihistamine effects

(= serotonin antagonist and reuptake inhibitor)
Dosing for trazodone ER for treating depression?
150 or 300 mg ER tab hs on empty stomach
MOA of vilazodone [ViiBRYD]?
It's a HYBRID: SSRI and partial 5-HT1A agonist
Newest SSRI on the market?
vortioxetine [Brintellix]
MAO of vortioxetine [Brintellix]?
- SSRI
- agonist at 5-­HT1A receptor
- partial agonist at 5-­HT1B receptors
- antagonist 5-HT3, 5-HT1D, 5-HT7 receptors
Can ECT be used in pregnant women?
Yes.

(GA's are flushed out of the body quickly.)
MOA of lithium?
Increases presynaptic transmission of 5-HT
Therapeutic level of lithium?
> 0.5 mEq/L
When is lithium used?
Bipolar disorder
Augmentation strategy in resistant depression
Which is more effective as an augmentation strategy in resistant depression: T3 or lithium?
T3

(also has less side effects)
The two atypical antipsychotics that may be used as adjunctive therapies in resistant MDD?
- aripiprazole (preferred), (15 mg/day)
- quetiapine XR (150-300 mg/day)
Efficacy of ECT in MDD?
80-90%!
MOA of St. John's Wort?
- "affinity for" GABA-A, GABA-B, 5-HT1, 3, 4
- SRI
- mild MAOI
Effective dose of St. John's Wort?
300 mg TID
What does "SAMe" stand for and what does it do?
S-adenosyl methionine

Serves as a methyl donor in the synthesis of phospholipids, catecholamines, serotonin.