Antidepressants and Mood Stabilizers - Craviso Flashcards
currently available drugs to treat depression are based on what theory of depression?
monoamine theory
T/F: all antidepressants cause immediate effects on synaptic monoamine levels
true
Despite an immediate increase in synaptic monoamine levels, why is there a delay of several weeks for antidepressants to have the desired effect?
slow increase in the expression of BDNF that promotes synaptogenesis
What percent of patients are refractory to multiple different antidepressants?
20%
What are the four major classes of antidpressants?
- SSRIs
- SNRIs
- Other new antidpressants
- MAOIs
SNRI block the uptake of what two amines?
5HT and NE
older tricyclic antidepressants are antagonists against (one/several) receptors
several
Newer antidepressants inhibit reuptake of what amine?
dopamine
MAOIs inhibit the metabolism of what two amines?
5-ht and NE
What are the firstline SSRIs?
FLUOXETINE (Prozac; Prozac Weekly) SERTRALINE (Zoloft) PAROXETINE (Paxil) CITALOPRAM (Celexa) ESCITALOPRAM (Lexapro)
how are SSRIs metabolized?
CYP450 in the liver
which SSRIs are the potent inhibitors of CYP2D6?
fluoxetine and paroxetine
which SSRIs are the low level inhibitors of CYP2D6?
citalopram and escitalopram
What are the major SE of taking SSRIs?
significant sexual dysfunction GI disturbances insomnia, restlessness anorexia or wt. loss early on or wt. gain with long term use QT prolongation with citalopram
T/F; SSRIs have a withdrawal syndrome
true; nausea, dizziness, anxiety, tremor, and palpiations
Use of which SSRI during pregnancy is linked to an increased risk of cardiovascular malformations in the fetus?
paroxetine
5-HT syndrome is seen with (SSRIs/MAOIs) that enhane 5-HT transmission
MAOIs
What is the only antidepressant approved for use in children?
fluoxetine
which SSRI is approved for use in adolescents?
escitalopram
why is the use of antidepressants limited in children?
risk of increasing SI
Which SSRI is sued for SAD?
paroxetine
Which SSRI is used as a migraine prophylactic?
fluoxetine
Which SSRI is used for PMS and PMDD and hot flashes?
paroxetine
Which SSRI is used for bulimia nervosa?
fluoxextine
Which newer, selective SNRI is the firstline druge that blocks NE and 5ht reuptake as well as weakly blocking DM reuptake?
Effexor
What are the side effects of SNRIs?
same as SSRIs;
dose related increase in BP
What are the additional uses of SNRIs?
Tx of neuropathic pain
anxiety disorders
Pristiq is a metabolite of which SNRI?
Effexor
Cymbalta is contraindicated in pts with what dz?
chronic liver disease or hepatic insufficiency
What are the additional uses of cymbalta?
fibromyalgia
Diabetic peripheral neuropathy
long term Tx of GAD
What are the common TCA’s?
Nortriptyline
Imipramine
Amitriptyline
Why are TCAs no longer used?
- can be fatal in overdose
- are cardiotoxic
- have a propensity to lower seizure threshold
- have significant antagonist activity at several types of neurotransmitter receptors
WHich TCA is a migraine prophylactic?
amitriptyline
When do you use TCAs?
pt is refractory to common antidepressants
What are the three receptor types that TCAs block?
- mACh
- a 1
- H1
what are the SE associated with blocking mACh receptors?
sedation, cognitive impairment, confusion, delirium, blurred
vision, dry mouth, tachycardia, urinary retention
what are the SE associated with blocking a1 receptors?
orthostatic hypotension, sedation
what are the side effects associated with blocking H1 receptors?
sedation
At therapeutic doses all TCAs can cause what SE?
lowering of seizure threshold
sexual dysfunction
weight gain
T/F: at toxic doses, ALL TCAs are cardiotoxic and OD is fatal
true
T/F: some pts develop cardiotoxicity to TCAs at therapeutic doses
true
what are the mechanisms of TCAs being cardiotoxic?
QT prolongation
ventricular block
arrhythmias
ventricular tachycardia
What is the MOA of TCA causing death via OD?
hyperpyrexia, hypertension and tachycardia, arrhythmias, severe anticholinergic effects and convulsions
What types of drugs have interactions with TCAs?
MAOIs
Anticholinergics and antihistamines
CNS depressants
what happens when you take MAOIs with tCAs?
severe HTN, serotonin syndrome
what happens when you take anticholinergics or antihistamines with TCAs?
additive effects due to blockade of mACh and H1 receptors
What happens when you take CNS depressants with TCAs?
more sedation
what is the only antidepressant that works by blocking dopamine reuptake?
Buproprion (wellbutrin)
What are some of the SE of wellbutrin?
insomnia
dose related seizure
contraindicated in seizure and eating disorders (electrolyte imbalance)
precipitate psychotic episodes`
T/F: wellbutrin has fewer sexual SE
true
What is the sustained release formula of wellbutrin used in smoking cessation>
Zyban
Remeron is an antagonist of (a1/a2) receptors that mediate negative feedback for NE and 5ht release
a2
T/F: remeron has sexual SE equal to SSRIs
false, like wellbutrin
Trazodone blocks 5ht reuptake by blcoking 5ht2 receptors and 5ht1(a/b) partially
5ht1a
What are the strange side effects of trazodone?
sig. drowsiness
GI upset
orthostatic htn
PRIAPISM
Vibryd is a hydbrid SSRI and partial agonist of (blank) receptor
5ht1a
no wt. gain
no sexual side effects
MAO-a metabolizes (NE and 5-ht / Dopamine)
MAO-a = 5-ht and NE
MAO-b metabolizes (NE and 5-ht / Dopamine)
dopamine
Why are MAOIs a last choice?
risk of hypertensive crisis
What degenerative disease do you use MAOIs to treat?
parkinsons
Selegeline is a (reversible/irreversible) MAOI
reversible
Phenelzine is a (reversible/irreversible) MAOI
irreversible
why is selegiline given as a transdermal patch?
bypasses the gut and lowers the risk of HTN crisis via tyramine
MAOI’s have side effects with what drugs?
- indirect acting sympathomimetics and tyramine coantianing foods
- SSRIs and 5 ht- receptor agonists causing serotonin sydrome
What are the characteristics of a manic episode?
1.exaggerated optimism and self-confidence
2. decreased sleep without experiencing fatigue
3. grandiose delusions, inflated sense of self-importance
4. excessive irritability; aggressive behavior
5. racing speech, flight of ideas
impulsiveness, poor judgment
6. easily distracted
7. reckless behavior
How many full cycles is considered rapid cycling in bipolar?
4 full cycles
Eskalith is lithium (carbonate/citrate)
carbonate
Cibalith is lithium (carbonate/citrate)
citrate
What is the firstline drug for mania?
lithium
Pts with bipolar disorder can experience what when taking SSRIs?
mood swings
T/F: pts with bipolar disorder may initially need an SSRI along with their lithium
true
T/F: lithium is not effective for rapid cyclers
true
Lithium effects are (immediate/build over time)
build over time
This drug causes the inhibition of recycling of inositol substrates
lithium
This drug alters the function of GPCRs assc’d with B-adrenergic and M1ACh receptors
lithium
Lithium distributes into (blood volume/total body water volume)
total body water
How soon does normal lithium reach peak plasma? Slow release?
Normal; 1-2 hours
slow release: 4 hours
How is lithium eliminated?
via the kidney; half life of 20-24 hours
Renal clearance of lithium is proportional to (blank)
plasma concentration
Dehydration, CHF, renal dz, old age can all (inc/dec) lithium levels
increase
Na depletion may cause sig. lithium (excretion/retention)
retention
Lithium clearance is (inc/dec) by loop and thiazide diuretics, NSAIDS, and ACE inhibitors
decreased
lithium clearance is (inc/dec) by osmotic diuretics, acetazolamide, caffeine, and theophylline
increased
What are the SE of lithium?
drowsiness, slowed mentation, forgetfulness GI distrubances Polyuria and thirst wt. gain mild tremor in fingers
What are the major complications of long term lithium use?
interstitial nephritis
depression of thyroid function (via iodine interference)
Can lithium be used during pregnancy?
not during first trimester or during breastfeeding
lithium has a (high/low) therapeutic index
low
Above 2.5 mEq/L lithium SE inlcude….
ataxia
gross tremor
cardiac arrhythmias
coma and convulsion
T/F: lithium tox can be seen at any blood levels
true
What is an anti-epileptic drug that is first line for mania and mixed states?
valproic acid (depakote) or carbamazepine (tegretol) or lamotrigine
What are the atypical antipsychotics?
QUETIAPINE (Seroquel) OLANZAPINE (Zyprexa) RISPERIDONE (Risperdal) ARIPIPRAZOLE (Abilify) LURASIDONE (Latuda) – bipolar depression only ASENAPINE (Saphris)
T/F: lorazepam and clonazepam can be used for treating acute mania
true