Anti-Depressants Flashcards
SSRI mechanism
inhibit presynaptic serotonin pumps –> increase availability of serotonin in synaptic cleft
Which SSRI has the longest half-life?
Fluoxetine (Prozac)
Which SSRI can be used in pregnancy and approved for use in children?
Fluoxetine (Prozac)
Fluoxetine (Prozac) specific concerns
- more common sleep changes and anxiety
- can elevate levels of neuroleptics, leading to inc side effects
Which SSRI has the highest risk for GI disturbances?
Sertraline (Zoloft)
Which SSRI is highly protein bound?
Proxetine (Paxil)
- causes several drug interactions
Paroxetine (Paxil) half-life?
Short–>leading to withdrawal phenomena if not taken consistently
Paroxetine (Paxil) specific side effects?
more anticholinergic effects (sedation, constipation, weight gain)
Which SSRI is the only one approved for OCD?
Fluvoxamine (Luvox)
Fluvoxamine (Luvox) common side effects?
Nausea and vomiting
Also has a lot of drug interactions
Which SSRI has the fewest drug-drug interactions?
Citalopram (Celexa)
Which SSRI has possibly fewer sexual side effects?
Citalopram (Celexa)
Compare escitalopram (Lexapro) and citalopram (Celexa)
levo-enantiomer
similar efficacy with possibly fewer side effects
more expensive!
In comparison to TCAs and MAOIs, what are the benefits to using an SSRI?
- serotonin selectivity (do not act on HAM)–>fewer side effects
- much safer in overdose
List side effects of SSRIs
- sexual dysfunction (dec interest, anorgasmia, delayed ejaculation)
- GI disturbance (nausea, diarrhea)
- insomnia, vivid dreams
- headache
- anorexia, weight loss
- restlessness (akathisia-like state at initiation and termination)
- seizures
- BLACK BOX WARNING: inc suicidal thinking and behavior especially in children/adolescents
Why should SSRIs not be used for at least 2 weeks prior to or after MAOIs?
Serotonin syndrome: fever, diaphoresis, shivering, tachycardia, HTN, delirium, neuromuscular excitability, hyperreflexia, potentially death
What drugs may help the sexual side effects of SSRIs?
buproprion, changing to a non-SSRI antidepressant, adding sildenafil for men
How do SSRIs interact with warfarin?
can inc levels, so must monitor!
Venlafaxine (Effexor) and Duloxetine (Cymbalta) are what type of antidepressant?
SNRIs
Venlafaxine (Effexor) is used for depression as well as…
anxiety disorders like GAD, some use in ADHD
Venlafaxine (Effexor) specific side effects?
similar to SSRIs
can also inc bp (do not use in patients with untreated or labile bp)
Duloxetine (Cymbalta) is used for depression as well as…
neuropathic pain or fibromyalgia
Duloxetine (Cymbalta) specific side effects?
similar to SSRIs, but more dry mouth and constipation (NE effects)
may be more liver side effects if have liver disease or heavy alc use
expensive!
Bupropion (Wellbutrin) mechanism?
NE-Dopamine reuptake inhibitor
Benefits of bupropion (Wellbutrin)?
lack of sexual side effects vs SSRIs
some efficacy in adult ADHD
Side effects and contraindications of bupropion (Wellbutrin)?
inc risk of seizures and psychosis at high doses; inc anxiety in some
contraindicated in patients with seizure (lower seizure threshold) or active eating disorders or those currently on an MAOI
Trazodone (Desyrel) mechanism?
Serotonin receptor antagonist and serotonin reuptake inhibitor
Trazodone (Desyrel) is used for…
refractory major depression, major depression with anxiety, insomnia (secondary to its sedative effects)
do not have the sexual side effects of SSRIs
Trazodone (Desyrel) specific side effects?
nausea, dizziness, orthostatic hypotension, cardiac arrhythmias, sedation, and priapism (painful erect penis that will not return to flaccid state… aka “trazondone will raise the bone”)
Mirtazapine (Remeron) is more useful for what population with depression?
elderly (helps with sleep and appetite)
refractory major depression (especially those who need to gain weight)
Mirtazapine (Remeron) side effects?
sedation, WEIGHT GAIN, dizziness, somnolence, tremor, dry mouth, constipation, rare agranulocytosis
TCAs mechanism?
inhibit reuptake of NE and serotonin
Why are TCAs rarely used as first-line?
higher incidence of side effects, inc monitoring of dosing, can be lethal in overdose
What is the difference between tertiary amines and secondary amines among the TCAs?
tertiary amines are highly anticholinergic–>more sedating, greater lethality in overdose
Amitriptyline (Elavil), Imipramine (Tofranil), Clomipramine (Anafranil), Doxepin (Sinequan) are tertiary or secondary amine TCAs?
tertiary
Nortriptyline (Pamelor, Aventyl) and Desipramine (Norpramin) are tertiary or secondary amine TCAs?
secondary
Amitriptyline (Elavil) are used for depression as well as…
chronic pain, migraines, insomnia
Imipramine (Tofranil) is used for depression as well as…
enuresis and panic disorder
also has a injectable IM form
Clomipramine (Anafranil) is used for depression as well as…
OCD
Doxepin (Sinequan) is used for depression as well as…
chronic pain, potentially as a sleep aid in low doses
Nortriptyline (Pamelor, Aventyl) is used for depression as well as…
chronic pain
Which TCA is least likely to cause orthostatic hypotension?
Nortriptyline
Which TCA is least anticholinergic?
Desipramine (Norpramin)–>more activating, least sedating
How much of a TCA can be lethal in overdose?
1 week supply (1-2 g)
What is the treatment for TCA overdose?
IV sodium bicarbonate
Amoxapine (Asendin) and Maprotiline (Ludiomil) are what type of antidepressants?
tetracyclic antidepressants
Amoxapine (Asendin) specific side effects?
metabolite of antipsychotic loxapine
may cause EPS and has similar side effect profile to typical antipsychotics
Maprotiline (Ludiomil) specific side effects?
higher rates of seizure, arrhythmia, and fatality on overdose
Why do TCAs have many drug interactions?
highly protein bound and lipid soluble
TCAs 3Cs in major complications?
Cardiotoxicity
Convulsions
Coma
List TCA side effects:
- HAM (antihistamine- sedation;
antiadrenergic- cardiovascular such as orthostatic hypotension, dizziness, reflex tachy, arrhythmias, widening QRS/OT/PR;
antimuscarinic/anticholinergic: dry mouth, constipation, urinary retention, blurred vision, tacky, exacerbation of narrow angle glaucoma) - weight gain
- seizures
- serotonergic effects (erectile/ejaculatory dysfunc, anorgasmia)
Symptoms of TCA overdose?
agitation, tremors, ataxia, delirium, hypoventilation from CNS depression, myoclonus, hyperreflexia, seizures, coma
MAOIs mechanism?
prevent inactivation of amines such as NE, serotonin, dopamine, and tyramine (intermediate from tyrosine–>NE) by irreversibly inhibiting enzymes MAO-A and -B
MAO-A affects what amines? MAO-B?
MAO-A serotonin
MAO-B NE/E
both dopamine and tyramine
When are MAOIs most effective?
refractory depression/atypical depression (hypersomnia, inc appetite, inc sensitivity to interpersonal rejection)
also refractory panic/anxiety disorder
Phenelzine (Nardil), Tranylcypromine (Parnate), Isocarboxazid (Marplan) are what group of antidepressants?
Selegiline (Deprenyl), Rasagiline (Azilect)?
all are MAOIs
Phenelzine (Nardil), Tranylcypromine (Parnate), Isocarboxazid (Marplan) are non-selective
Selegiline (Deprenyl), Rasagiline (Azilect) are MAO-B inhibitors
What two medical emergencies does one worry about with MAOIs?
Serotonin syndrome wait 2 weeks before switching from SSRI to MAOI and at least 5-6 weeks with fluoxetine
Hypertensive crisis, when taken with tyramine-rich foods or sympathomimetics
List side effects seen with MAOIs
- orthostatic hypotension
- drowsiness
- weight gain
- sexual dysfunc
- dry mouth
- sleep dysfunc
- if have pyridoxine deficiency–>paresthesias (treat with B6)
- rarely, liver toxicity, seizures, coma
Which MAOI does not require following the dietary restrictions?
Selegiline when used in low doses
must still avoid decongestants, opiates (Demerol) and serotonergic drugs
