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29 Cards in this Set

  • Front
  • Back
Which drugs are more selective for 5HT1 reuptake inhibition?
Fluoxetine (prototype SSRI) & Setraline (SSRIs)
Which drug is most selective for NE reuptake inhibition?
Maprotiline (Tricyclic)
Which drugs are between selectivity/non-selective for NE & 5HT1 reuptake inhibition?
Amitryptiline (Tricyclic) & Clomipramine (Tricyclic)
What are the first line drugs for depression?
SSRIs (safe, well tolerated, compliance, effective for OCD/PTSD/Bulimia, blah blah blah)
What is the MOA of SSRIs?
Block autoreceptors --> downregulation of autoreceptors --> Increase serotonin production --> too much serotonin in cleft --> downregulation of post-synaptic receptors (THIS IS WHY THE DRUGS TAKE SO LONG TO WORK!)
Kinetics of SSRIs (Fluoxetine)?
- Well absorbed
- Inhibitors of P450 (esp. 2D6)
- Significant first pass metabolism --> lingering active metabolites
- Long t1/2 (120-150 hrs)
What are the adverse effects of SSRIs?
- Mostly due to increased serotonin action of unwanted 5HT1 receptors
- Tolerance develops to most SE
5HT1 action?
Therapeutic effect of SSRIs
5HT2 side effects?
- Agitation/Akathesia
- Insomnia
- Anxiety/Panic Attacks
- Sexual dysfunction (does not help to switch within SSRI class to alleviate)
5HT3 action?
- Nausea/Vomit/Wt.loss
- GI cramps/diarrhea
Other adverse effects of SSRIs?
- Rebound
- Efficacy wear off w/ long course
- Toxicity - not a big issue (agitation, vomit, seizure, death)
Contraindication/Drug interactions in SSRIs?
1. Serotonin Syndrome (interactions w/ MAOIs, other drugs that elevate 5HT)
Sx: Hyperthermia, Muscle rigid, myoclonus, tremor, shivering, mental status change & vital sign change

DO NOT GIVE A MAOI w/ SSRI

2. Patients w/out cytochrome P4502D6
Clinical use of SSRIs?
First line depression

*Other disorders too
Least preferred uses of SSRIs? (Don't start on or remove if...)
- Sexual dysfunction
- Loss of efficacy
- Nocturnal myoclonus
- Insomnia
What are atypical anti-depressants?
Do not effect re-uptake or metabolism of 5HT1 or NE specifically
Two classes of atypicals?
1. Re-uptake inhibitors of NE, DA, 5HT
2. Direct receptor antagonists
What is MOA of Buproprion?
Re-uptake inhibitor of strong NE and moderate DA
Side effects of Buproprion?
Seizures (dose-related), Sitmulation

Agitation, nausea, insomnia
When is Buproprion preferred in depression?
Retarded depression
Hypersomnia
SSRI non-responders/non-tolerant
Cognitive slowing
Least preferred uses of Buproprion?
Seizures
Non-compliance
Agitated/Insomniac patients
Other uses of Buproprion?
Add w/ SSRI
ADD
Smoking cessation
What is MOA of Venlafaxine?
Combo (three drugs in one)

Strong 5HT reuptake inhibitor
Moderate NE reuptake inhibitor
Weak DA reuptake inhibitor
Side effects of Venlafaxine?
Nausea
Insomnia
Factoid: At low dose, look similar to SSRIs. At high dose, start seeing NE & DA effects.
Ok
When is Venlafaxine preferred clinically?
Melancholy
Severe depression
Refractory to other anti-depressants
Has a rapid onset
What else is Venlafaxine also approved for?
GAD
Panic Disorder

*Do not use as an anorexic!!!
*Bipolar?
What is MOA of Mirtazapine?
Alpha 2 adrenergic antagonist (b/c these block 5HT & NE release --> if you block 5HT & NE levels increase)
(Also 5HT2, 5HT3, H1)

*No alpha 1 action
*Prevent SSRI side effects (by blocking 5HT2 & 5HT3)
*H1 causes sedation & wt. gain
Uses of Mirtazapine?
Depression (w/ anxiety, w/ panic, severe, loss of SSRI efficacy)
Don't use for...?
Immunocompromised due to neurtopenia b/c can potentiate

Hypersomnia, overweight, ...