Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
38 Cards in this Set
- Front
- Back
|
What are the four classes of antidepressant medications?
|
SSRI
Tricyclics Heterocyclics MAOI |
|
|
What are the principal members of the SSRI antidepressant class?
|
fluoxetine, citalopram, paroxetine, sertraline. escitalopram, fluvoxamine
|
|
|
What are the principal members of the Tricyclic antidepressant class?
|
nortriptyline, imipramine, amytriptyline, desipramine, doxepin
|
|
|
What are the principal members of the Heterocyclic antidepressant class?
|
bupropion, mirtazepine, nefazadone, venlafaxine, duloxetine, desvenlafaxine
|
|
|
What are the principal members of the MAO-I’s antidepressant class?
|
phenylzine, tranylcypromine, isocarboxazid, selegiline patch
|
|
|
What are the acute mechanisms of SSRI antidepressant action?
|
selective inhibition of the plasma membrane 5HT transporter
|
|
|
What are the acute mechanisms of Tricyclic antidepressant action?
|
less-selective inhibition of NE and 5HT plasma membrane transporters
|
|
|
What are the acute mechanisms of Heterocyclic antidepressant action?
|
have varied effects:
duloxetine, venlafaxine, desvenlafaxine: potently inhibit both 5HT and NE reuptake (sometimes called SNRIS) mirtazapine: blocks presynaptic a2 adrenoceptors (promotes NE release by blocking auto-inhibition). also block 5-HT2 and 5-HT3 receptors bupropion, MOA unclear, but has mild amphetamine-like effects nefazadone, is a 5HT2A and 5HT2C antagonist and a weak 5HT reuptake blocker |
|
|
What are the acute mechanisms of MAO-I antidepressant action?
|
increase monoamine levels by inhibiting both MAO-A and MAO-B (selegiline, selective inhibitor of MAO-B)
|
|
|
Why is the onset of antidepressant effect is delayed?
|
probably because it takes time for the brain plasticity involved in depression to be reversed. e.g. the BDNF increased by monoamines takes weeks to fully induce hippocampal neurogenesis.
|
|
|
What are the principal adverse effects of Tricyclics?
|
anticholinergic, orthostatic hypotension, arrhythmias, sexual dysfunction, weight gain, seizures (can be lethal: cardiac arrhythmias, hypotension, uncontrollable seizures)
|
|
|
What are the principal adverse effects of SSRIs?
|
headache, CNS arousal, GI, sexual, Bleeding, weight gain, Serotonin Syndrome
|
|
|
What are the principal adverse effects of Heterocyclic antidepressants?
|
Venlafaxine and duloxetine nausea, sedation, dry mouth, sweating
Bupropion: seizures, amphetamine-like anorexia, insomnia, agitation, tremor Mirtazepine: mild anticholinergic & antihistaminergic effects (hypotension, sedation, dry mouth, constipation, weight gain). possible agranulocytosis and neutropenia |
|
|
What are the principal adverse effects of MAO-I?
|
tyramine induced hypertension. sedation, hypotension, sexual, weight gain, rare psychosis, Serotonin Syndrome
|
|
|
What are the signs/syptoms of Serotonin syndrome?
|
muscle rigidity, myoclonus, hyperthermia, CV instability, CNS excitation
|
|
|
What are the signs/symptoms of antidepressant discontinuation syndrome?
|
flu-like symptoms, rebound symptoms of anxiety/depression, paraesthesias, confusion, irritability/agitation
|
|
|
What is the strategy for treating resistant depression?
|
involves reappraising the diagnosis, and adequate trial of maximal tolerated [and safe] dose, augmentation of antidepressant with a second antidepressant, lithium, T3, atypical antipsychotic, addition of psychotherapy, consideration of electroconvulsive therapy
|
|
|
What is the mechanism of action of Phenelzine? What are its uses? What are the risks/benefits and contraindications?
|
MAOI nonselective
Typical, Atypical depression, nearly obsolete Irreversible/long-lasting centrally mediated: agitation, delirium, confusion, psychosis Autonomic: OH, tachycardia, constipation, urination difficulties, impotenance Contraindications: SSRIs, meperidine→life threatening. cheese→HTN crisis Potentiates: antihistamines, amphetamines, barbiturates Similar to Tranylcypromine |
|
|
What is the mechanism of action of Tranylcypromine? What are its uses? What are the risks/benefits and contraindications?
|
MAOI nonselective
Typical, Atypical depression, nearly obsolete Irreversible/long-lasting centrally mediated: agitation, delirium, confusion, psychosis Autonomic: OH, tachycardia, constipation, urination difficulties, impotenance Contraindications: SSRIs, meperidine→life threatening. cheese→HTN crisis Potentiates: antihistamines, amphetamines, barbiturates Similar to Phenelzine |
|
|
What is the mechanism of action of selegeline patch? What are its uses? What are the risks/benefits and contraindications?
|
MAOI (modestly selective for MAO-B)
Typical and Atypical depression Reversible, reduced risk of tyramine reactuib Centrally mediated: agitation, delirium, confusion, psychosis autonomic: OH, tachycardia, constipation, urination difficulties, impotence Contraindications: SSRIs, meperidine→life threatening. cheese→HTN crisis local skin irritation at patch site, low tyramine diet at > 9 mg |
|
|
What is the mechanism of action of Imipramine? What are its uses? How long does it take to kick in? How many people respond? What are the risks/benefits and contraindications?
|
TCA (moderate NE and 5HT)
typical depression (migraine, anxiety, and enuresis) Sedation Requires several weeks, 70-80% respond cardiac conduction abnormalities, lethal in OD, confusion, OH, dizziness, blurred vision, mouth dryness, urinary retention, constipation, weight gain, delirium, sexual dysfunction Interactions: guanethedine, MAOIs |
|
|
What is the mechanism of action of Desipramine? What is its use? Risks/Benefits?
|
TCA (High NE, Low 5HT)
Typical Depression, Chronic Pain (migraine, anxiety, enuresis) Least sedative, w/lease central ACh activity Same Risks/Benefits as Imipramine: cardiac conduction abnormalities, lethal in OD, confusion, OH, dizziness, blurred vision, mouth dryness, urinary retention, constipation, weight gain, delirium, sexual dysfunction Interactions: guanethedine, MAOIs |
|
|
What is the mechanism of action of Amitriptyline? What are its uses? Risks/Benefits?
|
TCA (Moderate NE, and 5HT effects)
Typical Depression (migraine, anxiety, enuresis) High sedation with most central ACh activity Same Risks/Benefits as Imipramine: cardiac conduction abnormalities, lethal in OD, confusion, OH, dizziness, blurred vision, mouth dryness, urinary retention, constipation, weight gain, delirium, sexual dysfunction Interactions: guanethedine, MAOIs |
|
|
What is the mechanism of action of nortriptyline? What are its uses? Risks/Benefits?
|
TCA (High NE, Low 5HT)
Typical depression, Chronic Pain (migraine, anxiety, enuresis) median level of sedation Same Risks/Benefits as Imipramine: cardiac conduction abnormalities, lethal in OD, confusion, OH, dizziness, blurred vision, mouth dryness, urinary retention, constipation, weight gain, delirium, sexual dysfunction Interactions: guanethedine, MAOIs |
|
|
What is the mechanism of actin of Doxepin? What are its uses? Risks/Beneftis?
|
TCA
Typical depression (migraine, anxiety, enuresis) High Level of Sedation Same Risks/Benefits as imipramine: cardiac conduction abnormalities, lethal in OD, confusion, OH, dizziness, blurred vision, mouth dryness, urinary retention, constipation, weight gain, delirium, sexual dysfunction Interactions: guanethedine, MAOIs |
|
|
Out of all the tricyclic antidepressants, which one is the least sedative? What one is the most?
|
most: amitriptyline
least: desipramine |
|
|
What two tricyclic antidepressants are helpful in chronic pain management?
|
desipramine and nortriptyline
|
|
|
What is the mechanism of action of Bupropion? What are its uses? Risks/Benefits?
|
dopamanergic and norepinephrine re-uptake inhibitors (NOT 5HT)
Typical and Atypical Depression Smoking Cessation More rapid onset of action Add to Treat Sexual Side Effects of SSRI Seizure, Side effects like amphetamines - anorexia, insomnia, and tremor Contraindicated in bulemia, anorexia |
|
|
What is the mechanism of action of Fluoxetine? What are its uses? Risks/Benefits?
|
SSRI
Typical and Atypical depression Panic, OCD, SAD, PTSD, GAD Doubling the dose quadruples the blood level, long T1/2, non-linear kinetics, agitation, anxiey Good for anxiety. but can induce anxiety in some pts Over 50% do not experience SE Nausea, activation, diarrhea, sexual SE, (rare EPS, elderly SIADH) Inhibit P450 isoenzymes |
|
|
What are the symptoms/signs of Serotonin syndrome?
|
mental status, myoclonus, hyperreflexia, HTN, diarrhea, fever, tremor
|
|
|
What is the mechanism of action of Sertraline? What are its uses? Risks/Benefits?
|
SSRI
Typical/atypical depression Panic, OCD, SAD, PTSD, GAD Lower activation, no P450, more diarrhea _ Nausea, activation, diarrhea, sexual SE, (rare EPS, elderly SIADH) |
|
|
What is the mechanism of action of Paroxetine? What are its uses? Risks/Benefits?
|
SSRI
Typical/atypical depression Panic, OCD, SAD, PTSD, GAD Doubling the dose quadruples the blood level, nonlinear kinetics, sedation, less diarrhea Nausea, activation, diarrhea, sexual SE, (rare EPS, elderly SIADH) Inhibit P450 isoenzymes |
|
|
What is the mechanism of action of Citalopram? What are its uses? Risks/Beneftis?
|
SSRI
Typical/atypical depression Panic, OCD, SAD, PTSD, GAD Most selective, no P450, linear kinetics, lo sexual dysfx, lo anxiety, nausea main SE Nausea, activation, diarrhea, sexual SE, (rare EPS, elderly SIADH) Inhibit P450 isoenzymes |
|
|
What is the mechanism of action Trazodone? What are its uses? Risks/Beneftis?
|
5HT agonist/antagonist
Insomnia Too sedating at AD dose Lower CV/anti-ACh effects than TCA Used for insomnia and agitation Sedation, priapism, OH, arrhythmias |
|
|
What is the mechanism of action of Nefazodone? What are its uses? Risks/Benefits?
|
5HT agonist/antagonist
Typical/atypical depression Insomnia, anxiolitic Don’t combine with new antihistamines Minimal sexual SE Potent P450 inhibitor Less sedating, less hypoTN than trazodone Less toxic than TCA |
|
|
What is the mechanism of action of Venlafaxine? What are its uses? Risks/Beneftis?
|
5HT/NE-RI
Typical/atypical depression At lo dose like SSRI, at med dose 5HT/NE Higher rates of nausea than SSRI Increases in BP at higher doses Low medication interactions |
|
|
What is the mechanism of action of Duloxetine?
|
5-HT/NE-RI
Depression, Chronic Pain, Generalized Anxiety Good for chronic pain Higher rates of nausea than SSRI Moderate P450 inhibitor |
|
|
What is the mechanism of action of Mirtazapine (Remeron)? What are its uses? Risks/Benefits?
|
α-2 antagonist (increased NE)
also 5HT1/2, H1 antagonist Typical/atypical depression Sedation, hypoTN, appetite, weight gain, constipation Don’t use with MAO-I Minimal sexual SE |
