Depression Flashcards
Floxetine Citalopram Escitalopram Paroxetine Sertraline
SSRI’s
SSRI
MOA
- Block re-uptake of serotonin only
When do SSRIs peak in the body?
2-8 hrs
SSRI where food increases its absorption
Sertraline
sertraline is SO delicious
SSRI with LONGEST 1/2 life
Fluoxetine
→50 hrs
→Active metabolites in body for 10 days
SSRI that is a POTENT inhibitor of CYP-2D6
- Fluoxetine
- Paroxetine
(interaction occurs w/ TCAs, antipsychotics, antiarrhythmics)
Hepatic impairment & SSRIs
Reduce dose of SSRI
Only SSRI approved for bulimia
Fluoxetine
Memorize the cart with the clinical utilities
Do it.
“Very important according to Dom”
2 SSRIs that are more sedating
- Paroxetine
2. Fluvoxamine
2 SSRIs that are more activating
- Fluoxetine
2. Sertraline
Loss of libido, delayed ejaculation, and anorgasmia, is common w/ ….
SSRI
ADR
(*consider switch to bupropion)
SSRI
Caution in children
Suicide
SSRIs approved in children to tx OCD
- Fluoxetine
- Sertraline
- Fluvoxamine
SSRIs approved in children to tx Depression
- Fluoxetine
2. Escitalopram
Does an SSRI overdose cause a cardiac arrythmia?
Nope
but can cause a QT prolongation
Seizures and SSRIs
SSRI can lower the seizure threshold
SSRI + MAOI or other serotonergic drug can cause…
Serotonin Syndrome
Hyperthermia, muscle rigidity, sweating, myoclonus (clonic muscle twitching), and changes in MS and VS
Sx of Serotonin Syndrome
SSRIs are contraidicated…
In presence of an MAOI
How do you stop an SSRI?
TAPER
Venlafaxine
Desvenlafaxine
Duloxetine
Levomilnacipran
SNRI
Block reuptake of both 5-HT and NE in CNS
SNRI
MOA
SNRI that is an active demethylated metabolite of another SNRI
Active metabolite: Desvenlafaxine
of Venlafaxine
SNRI that is a moderate inhibitor of CYP 2D6?
Duloxetine
*gets metabolized in liver into inactive metabolites
SNRI Use:
Block reuptake of both 5-HT and NE in CNS
Duloxetine
SNRI Use:
GAD, panic disorder, social phobia
Venlafaxine
SNRI Use of all
Depression
SNRIs MOST likely to have more sexual dysfunction
Venlafaxine
Desvenlafaxine
SNRI to avoid in liver dysfunction
Duloxetine
Imipramine
Desipramine
Amitriptyline
Doxepin
TCA’s
Potent inhibitors of NE and serotonin reuptake into presynaptic nerve terminals
Also block serotonergic, α-adrenergic, histaminia, and muscarinic receptors
Desipramine: more selective for NE reuptake
TCA’s
MOA
Low & inconsistent bioavailability d/t variable 1st pass meatabolism
TCA’s
Highly lipophilic/extreme fat solubility allows for easy penetration int CNS + has a long half life
TCA’s
TCA
Metabolism
Elimination
Liver
Urine (inactive)
No longer used to control bed wetting in children < 6 yo
Imipramine (a TCA)
Use
Prevent migranes & tx chronic pain syndromes
Amitriptyline (a TCA)
Use
Low dose to tx insominia
Doxepin (a TCA)
Use
TCA
General use
- Mod-severe depression
2. Panic disorder
ADR:
sudden death in children and adolescents (get EKG 1st)
Despiramine (a TCA)
Orthostatic hypertension Tachycardia Arrhythmias Nausea Drowsiness Decreased sexual desire and inhibited ejaculation Resting tremor Manic episodes
TCA
ADR
TCAs have a narrow _________ __________.
Therapeutic Dose
*can be deadly
Isocarboxazid
Phenelzine
Tranylcypromine
Selegiline
MAOI
Prevent inactivation of MAO-A and B in neuron→ excess NE, 5-HT, Dopamine in synapse
MAOI
MOA
Length of MAOI washout
→When is it used ?
2 weeks
Used when switching from MAOI to another antidepressant
MAOI
Utility
- Major depression unresponsive to drugs
2. Selegiline: Parkingson’s
MAOI + Tyramine containing foods
AVOID b/c can lead to a HTN crisis
example: aged cheese, wine, fish or shrimp sauce etc
Orthostatic hypotension Restlessness, drowsiness, dizziness HA, constipation, N/V Joint pain, dry mouth, peripheral edema Rash, skin/mucous membrane hemorrhage
MAOI
ADR
↑ norepinephrine and dopamine activity→ presynaptic release of catecholamines
& can also affect nicotinic receptors
Bupropion
MOA
Bupropion
Use
- Major depresson
2. Smoking cessation
Bupropion
ADR
- Lowers seizure threshold
2. CYP 2D6 inhibitor
N/V Diarrhea Diaphoresis Hyperreflexia Bruxism Sweat Cogwheel rigidity Tachycardia
Serotonin Syndrome Sx
Serotonin Syndrome Tx
- Discontinue serotonergic agents
- Supportive care
- +/- use of benzo
- +/- Cyproheptadine serotonin antagonist
Cyproheptadine
→Use
→Administration
Use: serotonin & histamine receptor antagonist
Admin: PO only
Nefazodone
Trazodone
Vortioxetine
Serotonin Receptor Modulators
Serotonin Receptor Modulators
Trazodone
Use
Major depression
Sedation
Hypnosis
Serotonin Receptor Modulators
Vortioxetine
Use
Major depression
Serotonin Receptor Modulators
ADR
Vortioxetine: GI, sexual dysfunction, careful with additive SERT agents
Serotonin syndrome
Serotonin Receptor Modulators
Metabolism
→Trazodone and Nefazodone: short half lives, active metabolites
→Nefazodone: inhibits CYP3A4
→Vortioxetine: CYP2D6 metabolization and glucuronic acid conjugation
