Craviso: Antidepressants and Mood Stabilizers Flashcards
actions confined to blocking 5-HT reuptake (first-line drugs)
SSRIs
newer “selective” inhibitors – actions confined to blocking NE and 5-HT reuptake (first-line drugs);
older, less selective inhibitors - tricyclics (TCAs) that exert antagonist effects on a variety of receptors
SNRIs (serotonin-norepinephrine reuptake inhibitors)
inhibit the metabolism of NE and 5-HT
Monoamine oxidase inhibitors
What are these?
FLUOXETINE (Prozac; Prozac Weekly) SERTRALINE (Zoloft) PAROXETINE (Paxil) CITALOPRAM (Celexa) ESCITALOPRAM (Lexapro)
SSRIs
What is one major thing that you should consider when prescribing SSRIs?
SSRIs can be potent inhibitors of several cytop450’s (CYP2D6)
Which two SSRIs have high potential for inhibiting cytoP450s? Which two have low potential?
fluoxetine and paroxetine - high potential
citalopram and escitalopram - low potential
Adverse side effects of SSRIs?
significant sexual dysfunction, decreased libido
prominent GI disturbances
insomnia, restlessness
significant anorexia and weight loss with early treatment
significant weight gain with long-term use
This SSRI can cause QT prolongation
citalopram
This SSRI, if used during pregnancy, can be linked to an increase in cardiovascular malformations in the fetus
paroxetine
Two syndromes that you should be cautious of with patients taking SSRIs?
withdrawal syndrome after long-term use abruptly stopped;
5HT syndrome when used with MAO inhibitors or other drugs that increase 5HT
This is the only SSRI approved for use in children and adolescents
fluoxetine
SSRI approved for use in adolescence
escitalopram
SSRIs can be used for (blank) disorders
anxiety
What are two additional things that paroxetine can be used to treat?
seasonal affective disorder
PMS and PMDD, hot flashes
What are two additional things that fluoxetine can be used to treat?
bulimia nervosa
migraine prophylactic
This is a serotonin-norepinephrine reuptake inhibitor; blocks reuptake of both NE and 5HT and weakly DM
Venlafaxine
Adverse side effects of Venlafaxine?
similar to SSRI side effects;
can cause dose-related increase in blood pressure
Two additional uses for Venlafaxine?
anxiety disorders
treating neuropathic pain
This serotonin-norepinephrine reuptake inhibitor is contraindicated in those with chronic liver disease or hepatic insufficiency
Duloxetine
Additional uses for Duloxetine?
fibromyalgia
diabetic peripheral neuropathy
long-term treatment of generalized anxiety disorder
What are these? How do they work?
NORTRIPTYLINE (Aventyl, Pamelor)
IMIPRAMINE (Tofranil)
AMITRIPTYLINE (Elavil)
tricyclic antidepressants (TCAs); block the reuptake of both NE and 5HT
Nortriptyline mostly blocks the reuptake of (blank)
NE
Imipramine and amitriptyline mostly block the reuptake of (blank)
5HT
Major problems with TCAs?
Their use is confined to patients who do not respond or tolerate more widely-prescribed antidepressants
fatal if OD
cardiotoxic
lower seizure threshold
significant antagonist activity
Which 3 receptors do tricyclic antidepressants block? What effects does this cause?
- muscarinic ACh receptors - sedation, cognitive impairment, confusion, delirium, blurred vision, dry mouth, tachycardia
- alpha 1 adrenergic receptors - hypotension and sedation
- H1 receptors - sedation
Tricyclic antidepressants can cause what three adverse effects at therapeutic doses?
lower seizure threshold
sexual dysfunction
weight gain
Tricyclic antidepressants can cause what adverse effects at toxic doses?
cardiotoxicity (cardiac conduction delays, ventricular block, arrhythmias) **may occur at therapeutic dose
acute OD is often life-threatening due to hyperpyrexia, HTN, tachycardia, arrhythmias, etc
Adverse drug-drug interactions can occur when TCAs are taken with what?
Monoamine oxidase inhibitors
anticholinergics and antihistamines
CNS depressants
This is a dopamine reuptake inhibitor; also possibly blocks some reuptake of NE and 5HT
Bupropion
Adverse effects of Bupropion?
restlessness, insomnia, anxiety
risk of seizure activity *contraindicated in pts with seizures and eating disorders
may precipitate psychotic episodes
Bupropion is contraindicated in these patients…
pts with seizures and eating disorders
Sustained release formulation of bupropion which is used as an aid in smoking cessation
Zyban
antagonist of central presynaptic alpha2-adrenergic autoreceptors (receptors that mediate negative feedback for NE and 5-HT release);
blockade of 5-HT2 and 5-HT3 receptors
Mirtazapine
Side effects of Mirtazapine?
sedation
dizziness
stimulates appetite, weight gain
These two newer antidepressants are NOT commonly associated with sexual side effects
Mirtazapine
Bupropion
blocks 5-HT reuptake
also acts an antagonist at 5-HT2 receptors and as a partial agonist at 5-HT1A receptors
Trazodone
Adverse effects of Trazodone?
significant drowsiness and dizziness
GI upset
orthostatic hypotension
priapism
Is a SSRI and a partial agonist at 5-HT1A receptors
Vilazodone
Adverse effects of Vilazodone?
insomnia
GI disturbance
blocks MAO, the enzyme in nerve terminals that converts the monoamine neurotransmitters NE, 5-HT and dopamine into inactive products
Monoamine oxidase inhibitors
Why are MAOIs considered a last choice drug?
risk of hypertensive crisis in response to ingestion of certain foods containing tyramine
Foods containing tyramine can cause (blank) in patients taking MAOIs
hypertensive crisis
REVERSIBLE inhibitor of MAO;
available as a transdermal system (Ensam) - enables it to bypass the gut, thereby allowing inhibition of central MAO enzymes while reducing the chance of hypertensive reactions caused by tyramine
Selegiline
IRREVERSIBLE inhibitor of MAO
Phenelzine
Adverse effects of MAOIs?
sexual dysfunction CNS stimulation sleep disturbances weight gain orthostatic hypotension
MAOIs can cause drug interactions when taken with what?
indirect acting sympathomimetics
tyramine containing food
SSRIs and 5HT receptor agonists (too much 5HT –> 5HT syndrome)
characterized by:
exaggerated optimism and self-confidence
decreased sleep without experiencing fatigue
grandiose delusions, inflated sense of self-importance
excessive irritability; aggressive behavior
racing speech, flight of ideas
impulsiveness, poor judgment
easily distracted
reckless behavior
manic episodes
First line drug for acute mania, and long-term maintenance therapy to avert manic and depressive episodes in patients with bipolar disorder
Used to treat depression in an individual who has a history of bipolar disorder (better than antidepressants that can trigger mood swings)
Lithium
Why is lithium preferred over antidepressants for treating the depression involved in bipolar disorder?
antidepressants can trigger mood swings!
Is lithium effective for rapid cyclers? (>4 cycles of mania/depression in one year)
No!
How is lithium cleared? What drugs can decrease lithium clearance? What drugs increase lithium clearance?
via the kidney;
loop and thiazide diuretics, NSAIDs and ACE inhibitors;
osmotic diuretics, acetazolamide, caffeine, theophylline
Lithium can interfere with (blank) absorption and may promote (blank) depletion
Na+; Na+
What adverse effects can lithium cause at therapeutic doses?
drowsiness, slow mentation, forgetfulness
GI distrubance
polyuria and thirst (decreased response of kidney to ADH)
weight gain
mild tremor
What are two serious side effects with long-term use of Lithium?
degenerative changes in the kidney
depression of thyroid function
Lithium should not be used during (blank) or (blank)
pregnancy; breast feeding
Lithium has a (blank) therapeutic index so serum levels must be carefully monitored (always monitor for conditions that may decrease volume of distribution or renal clearance)
LOW
At what blood level of lithium would you notice ataxia, gross tremor, cardiac arrhythmias, coma and convulsions?
> 2.5mEq/L
What are these drugs used for?
Valproic Acid
Carbamazepine
antiepileptic drug (AED) for treating mania and mixed states
What are these? QUETIAPINE (Seroquel) OLANZAPINE (Zyprexa) RISPERIDONE (Risperdal) ARIPIPRAZOLE (Abilify) LURASIDONE (Latuda) – bipolar depression only ASENAPINE (Saphris)
atypical antipsychotics
What are these?
LORAZEPAM (Ativan) and CLONAZEPAM (Klonopin)
benzos
Newer AED used for bipolar depression
Lamotrigine
