Chapter 35 - Antidepressants Flashcards
What is the most common psychiatric disorder?
depression
What are the clinical features of depression?
-depressed mood
-loss of pleasure or interest
-insomnia
-anorexia
-loss of concentration
-feelings of guilt, worthlessness, helplessness
-suicidal thoughts
How long do symptoms need to last to be considered depression?
present most of the day, nearly every day, for at least 2 weeks
What are possible factors that contribute to depression?
-genetics
-childhood (ACEs)
-low self-esteem
-life stress
The monoamine hypothesis of depression says…
depression is thought to be caused by functional insufficiency of monoamine NTs
When we say depression is complex we mean…
there is likely no ‘one’ cause
Explain the association between inflammation and depression:
-activation of immune system and inflammation change BBB
-BBB allows entry of pro-inflammatory proteins that change brain and cause depression
When is electroconvulsive therapy used?
-when drugs and psychotherapy don’t work
-rapid response needed
-severe depression
-suicidal patients
-elderly patients at risk of starving
What is TMS?
transcranial magnetic stimulation
When do initial responses to antidepressants begin?
1-3 weeks after starting therapy
Maximal responses of antidepressants may not be seen for ___ weeks
12
What is considered a failed response to antidepressants?
drugs taken for 1 month with no success
How does efficacy of antidepressants vary?
it doesn’t they are nearly all equal
How do antidepressants affect suicidal tendencies?
-may increase them during early treatment
-especially in young adults
What changes should patients starting antidepressants be watched for?
-suicidal behaviour
-worsening mood
-behaviour changes
What does SSRI stand for?
selective serotonin reuptake inhibitor
When were SSRIs introduced?
1987
What is the most commonly prescribed antidepressant?
SSRIs
SSRIs are as effective as ________________ but don’t cause…
tricyclic antidepressants; SSRIs don’t cause hypotension, sedation, anticholinergic effects
Does overdose on SSRIs cause cardiac toxicity?
no
How common is death by SSRI overdose?
not common
How do SSRIs act?
blocking neuronal 5-HT reuptake
What was once the most widely prescribed SSRI in the world?
Fluoxetine (Prozac)
What is Fluoxetine (Prozac) used for?
-bipolar disorder
-OCD
-panic disorder
-bulimia nervosa
-premenstrual dysphoric disorder
-GAD
-PTSD
-social anxiety
-ADHD
-tourettes
What are the adverse effects of Fluoxetine (Prozac)?
-serotonin syndrome
-teratogenesis
-bleeding disorders
-sexual dysfunction
-weight gain
-hyponatremia (older adults)
-withdrawal syndrome
When does serotonin syndrome start?
2-72 hours after treatment
What does serotonin syndrome involve?
-agitation
-confusion
-disorientation
-anxiety
-hallucinations
-poor concentration
-incoordination
-myoclonus
-hyperreflexia
-excessive sweating
-tremor
-fever
-death
How do you stop serotonin syndrome?
discontinuation of the drug
What increases the risk of serotonin syndrome?
concurrent use of MAOIs and other drugs that affect 5-HT
What does fluoxetine (prozac) interact with?
-monoamine oxidase inhibitors (MAOIs)
-antiplatelets
-anticoagulants
-other drugs that work on 5-HT
What does SNRI stand for?
serotonin/norepinephrine reuptake inhibitor
What group of antidepressant is Venlafaxine (Effexor)?
SNRI
What are SNRIs used for?
-major depression
-GAD
-social anxiety disorder
-neuropathic pain
SNRIs block the reuptake of…
NE and 5-HT
What are the side effects of SNRIs?
-nausea
-headache
-anorexia
-nervousness
-sweating
-somnolence
-insomnia
-weight loss
-diastolic hypertension
-sexual dysfunction
-hyponatremia (older adults)
-neonatal withdrawal syndrome
-withdrawal syndrome
Desvenlafaxine, Duloxetine, Levomilnacipran, and Venlafaxine are all ________
SNRIs
What is a special consideration of the absorption of Duloxetine?
food reduces rate of absorption
How does Duloextine travel in the bloodstream?
bound to albumin
How is Venlafaxine administered?
XR capsules
With Venladaxine and Levomilnacipran, the dose must be decreased when…
the patient has liver or kidney dysfunction
What does SPARI stand for?
serotonin-1A partial agonist/serotonin reuptake inhibitor
What group of antidepressant is Vilazodone (Viibryd)?
SPARI
How does Vilazodone act?
ssri and partial agonist of 5-HT1A
What is Vilazodone used for?
manic depressive disorder and generalized anxiety disorder
Vilazodone should be administered with or without food?
with food
Vilazodone should not be administered with food or meds with _____________ properties such as…
anticoagulant; ginko, ginger, garlic, licorice
What are side effects of Vilazodone?
-headache
-diarrhea
-nausea
Do symptoms stop suddenly when Vilazodone is discontinued?
no
How long does it take for Vilazodone to take effect?
up to 28 days
What does SARI stand for?
serotonin antagonist receptor inhibitor
What drug class is Vortioxetine (Trintellix)?
SARI
How does Vortioxetine work?
-inhibit 5-HT reuptake
-stimulate 5-HT1A receptors
-block 5-HT3, 5-HT1D, 5-HT7 receptors
-partial agonist of 5-HT1B receptors
What is Vortioxetine used for?
major depression in adults
When does Vortioxetine require a 50% dose reduction?
when taken with CYP2D6 inhibitors
How is Vortioxetine transported in blood?
higly protein bound
What are the adverse effects of Vortioxetine?
-nausea
-constipation
-suicide
-agitation
-NMS
-serotonin syndrome
-hyponatremia
-pregnancy
-bone fracture risk
What antidepressant group is Trazodone?
SARI
How does Trazodone act at high doses?
-bind to 5-HT2 receptors and acts as a 5-HT agonist
How does Trazodone act at low doses?
-bind to 5-HT2 receptors and acts as a 5-HT antagonist, like SSRIs
What receptor subtypes does SARI act on?
H1, A1, and A2
What is Trazodone used for?
as a sedative, even in people without depression
What are the adverse effects of Trazodone?
-anticholinergic
-priapism (erection)
How do tricyclic antidepressants act?
by blocked reuptake of NE and 5-HT
What is the most dangerous AE of TCAs?
cardiotoxic in OD
Amitrityline along with Clomipramine, Doxepin, Imipramine, Nortriptyline are all…
TCAs
What are TCAs used for?
-depression
-fibromyalgia syndrome
-neuropathic pain
-chronic insomnia
-ADHD
-panic disorder
-OCD
-nocturnal enuresis
What are the adverse effects of TCAs?
-orthostatic hypotension
-anticholinergic effects!!
-diaphoresis (sweating)
-sedation
-cardiac toxicicty
-seizures
TCA toxicity (anticholinergic and cardiotoxic) manifests as:
-dysrhythmias
-tachycardia
-intraventricular blocks
-complete AV block
-ventricular tachycardia
-V fib
How is TCA toxicity treated?
-gastric lavage
-charcoal ingestion
-IV sodium bicarbonate (dysrhythmias)
MAOIs are the ________ or ________ choice antidepressants for most patients.
second or third
How do MAOIs compare to TCAs and SSRIs?
-equally effective
-MAOIs are more hazardous
Eating foods rich in ___________ risk triggering hypertensive crisis in patients taking MAOIs.
tyramine
MAOIs are the drug of choice for _________ depression
atypical
Phenelzine (Nardil) is a _______
MAOI
How do MAOIs act?
-convert monoamine NTs (NE, serotonin, and dopamine) into active products
-inactivate tyramine and biogenic amines
What are the two forms of MAO in the body?
MAO-A
MAO-B
Reversible MAOI action lasts ________
3-5 days
Irreversible MAOI action lasts _________
~2 weeks
What are MAOIs used for?
-depression
-bulimia nervosa
-agoraphobia
-ADHD
-OCD
-panic attacks
What are the AEs of MAOIs?
-CNS stimulation
-orthostatic hypotension
-hypertensive crisis (via dietary tyramine)
How does tyramine promote hypertensive crisis?
tyramine promotes the release of NE from sympathetic neurons
What are the symptoms of a hypertensive crisis?
-headache
-tachycardia
-hypertension
-N&V
-confusion
-sweating
-stroke
-death
What foods should not be eaten when taking MAOIs?
cheese, salami, wine, beer
What is the treatment for hypertensive crisis?
-IV vasodilator
-sodium nitroprusside
-phentolamine (alpha antagonist)
-labetalol (A/B antagonist)
What does RIMA stand for?
reversible inhibitor of monoamine oxidase
What class of antidepressant is Moclobemide?
RIMA
How does Moclobemide act?
by reversibly inhibiting monoamine oxidase
What are the adverse effects of Moclobemide?
-dry mouth
-dizziness
-tremor
-headache
-restlessness
What is Moclobemide used for?
-anxiety
-phobias
-atypical depression
When is Moclobemide administered?
after meals
Can people on Moclobemide eat tyramine?
yes but not in excessive amounts
What does Moclobemide interact with?
-St. John’s wort
-many others
What antidepressant class is Bupropion (Wellbutrin)?
norepinephrine and dopamine reuptake inhibitor
In what cases should the dose of Bupropion be decreased?
renal dysfunction
How does Bupropion differ from the rest of the drugs?
-no weight gain
-no sexual dysfunction
-increased seizure risk
-Zyban brand used for smoking cessation
-SR and XL tabs
What are the adverse effects of Bupropion?
-seizures
-agitation
-tremor
-tachycardia
-blurred vision
-dizziness
-headache
-insomnia
-dry mouth
-GI upset
What does Bupropion interact with?
MAOIs
How does Mirtazapine (Remeron) act?
-block 5-HT2, 5-HT3 & H1 receptors
-moderate blockade of A1 and muscarinic receptors
What are the adverse effects of Mirtazapine?
-anticholinergic (dry mouth, sedation)
-edema
-dizziness
-arthralgias (joint stiffness)
-nightmares
-weight gain
-increased QT interval
What is Mirtazapine used for?
-anxiety
-somatization
-depression
How does Mirtazapine differ from other drugs?
less sexual dysfunction
What antidepressant class is Esketamine (Spravato)?
glutamate receptor modulator (NMDA receptor antagonist)
How does Esketamine act?
non-selective, non-competitive blockade of NMDA (glutamate) receptors
What is Esketamine used for?
-MDD
-combined with SSRI and SNRI when no response to 2 courses of current treatment
WARNINGS of Esketamine:
-assess BP before and after (will peak 40min post dose, monitor till normal)
-dissociative sedation
-respiratory depress
-signs of abuse or misuse
-suicidal ideation
-CV risk (resuscitation equip avail!!!)
How is esketamine given?
-2 sprays intranasally
-single use
Esketamine isn’t used or people older than ______
age 65
People of ___________ ancestry should have a reduced dose of Esketamine
Japanese
What are the side effects of esketamine?
-increased BP
-sedation
-dissociation
-headache
-vertigo
Esketamine administration requires:
-direct HCP supervision
-2 hr observation
Electroconvulsive therapy is effective and ________
rapid
What is an adverse effect of ECT?
memory loss of immediate events
Where does transcranial magnetic therapy deliver magnetic fields?
left dorsolateral prefrontal cortex
TMT lasts ____ sessions every ___ weeks
40 min; every 6 weeks
What are the adverse effects of TMT?
-transient headaches
-scalp discomfort
-eye pain
-toothache
-muscle twitching
-seizures
When is vagus nerve stimulation used?
long-term therapy of treatment-resistant depression - when at least 4 drugs have failed
What is vagus nerve stimulation?
implanted device that delivers electrical pulses to the vagus nerve
What are the side effects of vagus nerve stimulation?
-hoarseness
-voice alteration
-cough
-dyspnea
What is light therapy used for?
treatment of seasonal affective disorder and nonseasonal major depression
What is Psilocybin?
a 5-HT2A receptor agonist that is used for therapy in opioid addiction and mental heath conditions
