Pharm, antidepressants, Linger Flashcards
What are the sSRIs
citalopram escitalopram fluoxetine fluvoxamine paroxetine setraline
what are the Selective serotonin NE reuptake inhibitors
duloxetine
venlafaxine
what tricyclic antideppressants are used in depression
amitriptyline
desipramine
imipramine
nortriptyline
what is the 5-HT2 antagonist used in depression
tazodone
what are the tetracyclic and unicyclic agents
buproprion
mirtazapine
what MAOI is used in depression
selegiline
forms MAOI selegiline is available in
transdermal patch
sublingual
bypass gut and liver for increased bioavialability
MOA SSRI
allosterically inhibit serotonin transporter to increase [ ] in cleft
80% SET blocked at therapeutic dose
what is MOA proposed for chronic use SSRI
down regulation post synaptic %-HT2a R density
SNRIs and tricyclic antidepressant MOA
inhibit SERT and NET increasing NT [ ]
affinity of tricyclic antidepressants for R
muscarinic too, Histamine and alpha adrenergic
5-HT2 antagonist MOA
trazodone and nefazodone
antagonize postsynaptic R to enhance tone
MOA Bupropion
selective inhibitor of dopamine transporter stimulates release NE and DA
no direct effect on serotonin reuptake or R
MAOI MOA
cause accumulation NE 5-HT and DA in vesiicles at nerve endings
MOA selefiline
selective irreversible MAO-B inhibitor at low doses
nonselective MAOA/B inhibitor at high dosese (depression)
MOA phenelzine and tranylcypromine
nonselective irreversible MAOIs
which tricyclic antidepressants stimulate muscarinic R the most
amitriptyline
protriptyline
which antidepressants work on SERT the most
citalopram clomipramine fluoxetine flucoxamine parozetine sertraline
which antidepressants have highest affinity for NET
despramine
protriptyline
70-80% depressino patients achieve remission via what
switching to another agent or augmentation by addition of another drug
When adequate response for depression achieved, what is therapy recommendation
minimum 6-12 mo to reduce risk of relapse
patients considered for long term maintenance when
> 2 MDD episodes in previous 5 years or >3 in lifetime
second most common use antidepressants
anxiety disorders
PTSD, OCD, social anxiety, generalized anxiety and panic disorder
OCD is known to respond to what agents
serotonergic agents like fluoxetine and fluvoxamine, paroxetine and clompramine
what antidepressants are used in pain disorders
TCA and SSRI
What antidepressants are used for premenstrual dysphoric disorder
SSRIs
fluoxetine
setraline
Tx schedule for premenstrual dysphoric disorder
2 weeks during luteal phase
which antidepressants are used in eatind disorders
fluoxetine and others
bulimia not anorexia
what antidepressants are used for insomina
amitriptyline and trazodone
Which TCA is used for pruritis
doxepin because works on histamine R
first line for Tx MDD and anxiety
SSRIs because fewer antimuscarinic effects and less cardiotoxic in overdose
What is a drug for depression in patients who cannot tolerate sexual dysfunction, weight gain and sedation
bupropion
2nd 3rd line agents for MDD
TCAs and MAOIs because potentially lethal in overdose
need titration to achieve therapeutic dose
serious effects and interactions
Adverse effects of all antidepressants
increased suicidality in patients under age 25
side effects SSRIs
mild sedation and antimuscarinic effects
GI: nuasea, vomiting, upset stomach, constipation
diminished sexual function libido delayed orgasm, diminished arousal
HA, insomnia, hypersomnia and weight gain
What is discontinuation syndrome
dizziness and paresthesia after sudden discontinuation
seen with SSRI and SNRI and TCA
Serotonin syndrome
overdose SSRI or concurrent MAOI use
CI to SSRI
patients displaying active manic Sx
paroxetine CI in pregnant patients
Adverse effects to SNRIs
serotonergic effects and! noradrenergic like insomnia, anxiety and agitation
inc BP and HR
venlafaxine inc bleeding risk and related with cardiac toxicity in overdose
adverse effects TCA
anticholinergic: dry mouth, constipation urinary retention, blurred vision and confusion orthostatic hypotension weight gain and sedation cardiotoxicity arrhythmias and heart block hepatic dysfunction hyponatremima hematologic abnormalities sexual side effects like sSRI
which TCA exhibit marked antimuscarinic and cardiac side effects
imipramine and amitriptyline
CI to TCA
arrhythmias, recent MI, liver disease, glaucoma, mania
adverse effects 5-HT2 antagonist
sedation and GI disturbances
orthostatic hypotension
black box warning nefazodone
hepatotoxicity and potentially lethal hepatic failure
adverse effects bupropion
agitation and insomnia and anorexia
which antidepressants do not have significant sexual side effects
5-HT2 antagonists
bupropion and mirtazapine
adverse effects MAOIs
orthostatic hypotension and weight gain
highest rate sexual side effects!!!!!!!!
discontinuation syndrome in MAOI
delirium like presentation with psychosis, excitement and confusion
amitriptyline overdose
arrhythmia, altered mental status and seizures
amitriptyline overdose
arrhythmia, altered mental status and seizures
gastric decontamination is helpful up to 8 hr post ingestion
MAOI overdose
autonomic instability hyperadrenergic Sx psychotic Sx confusion delirium, fever and seizures
pharmokinetics of antidepressants
inhibitors of CYP450 or substrates
St Johns wort PK
herbal med that induces CYP450
used to Tx depression
Sx serotonin syndrome
cognitive: delirium, agitation coma
ANS: HTN, tachy, hyperthermia, diaphoreses
somatic: myoclonus, hyperreflexia, tremor
switching between SSRI and MAOI
current therapy needs to be discontinued for at least 2 weeks
6 weeks for fluoxetine because longer half life
Tx serotonin syndrome
withdraw offending drug, sedation with benzo, paralysis, intubation, ventilation
consider 5-HT2 block with cyproheptadine or clorpromazine
Foods with significant amounts tyramine
pickled, aged, smoked, marinated, meats (spoiled), chocolate, alcoholic beverages, fermented foods like cheese
CI with tyramine food
MAOI because normally metabolized by MAO so with large amounts leads to HTN crisis
NE release from peripheral nerves and inc HR and BP (potentially fatal!*)
