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29 Cards in this Set
- Front
- Back
Which drugs are more selective for 5HT1 reuptake inhibition?
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Fluoxetine (prototype SSRI) & Setraline (SSRIs)
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Which drug is most selective for NE reuptake inhibition?
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Maprotiline (Tricyclic)
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Which drugs are between selectivity/non-selective for NE & 5HT1 reuptake inhibition?
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Amitryptiline (Tricyclic) & Clomipramine (Tricyclic)
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What are the first line drugs for depression?
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SSRIs (safe, well tolerated, compliance, effective for OCD/PTSD/Bulimia, blah blah blah)
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What is the MOA of SSRIs?
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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!)
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Kinetics of SSRIs (Fluoxetine)?
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- Well absorbed
- Inhibitors of P450 (esp. 2D6) - Significant first pass metabolism --> lingering active metabolites - Long t1/2 (120-150 hrs) |
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What are the adverse effects of SSRIs?
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- Mostly due to increased serotonin action of unwanted 5HT1 receptors
- Tolerance develops to most SE |
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5HT1 action?
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Therapeutic effect of SSRIs
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5HT2 side effects?
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- Agitation/Akathesia
- Insomnia - Anxiety/Panic Attacks - Sexual dysfunction (does not help to switch within SSRI class to alleviate) |
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5HT3 action?
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- Nausea/Vomit/Wt.loss
- GI cramps/diarrhea |
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Other adverse effects of SSRIs?
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- Rebound
- Efficacy wear off w/ long course - Toxicity - not a big issue (agitation, vomit, seizure, death) |
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Contraindication/Drug interactions in SSRIs?
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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 |
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Clinical use of SSRIs?
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First line depression
*Other disorders too |
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Least preferred uses of SSRIs? (Don't start on or remove if...)
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- Sexual dysfunction
- Loss of efficacy - Nocturnal myoclonus - Insomnia |
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What are atypical anti-depressants?
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Do not effect re-uptake or metabolism of 5HT1 or NE specifically
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Two classes of atypicals?
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1. Re-uptake inhibitors of NE, DA, 5HT
2. Direct receptor antagonists |
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What is MOA of Buproprion?
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Re-uptake inhibitor of strong NE and moderate DA
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Side effects of Buproprion?
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Seizures (dose-related), Sitmulation
Agitation, nausea, insomnia |
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When is Buproprion preferred in depression?
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Retarded depression
Hypersomnia SSRI non-responders/non-tolerant Cognitive slowing |
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Least preferred uses of Buproprion?
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Seizures
Non-compliance Agitated/Insomniac patients |
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Other uses of Buproprion?
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Add w/ SSRI
ADD Smoking cessation |
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What is MOA of Venlafaxine?
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Combo (three drugs in one)
Strong 5HT reuptake inhibitor Moderate NE reuptake inhibitor Weak DA reuptake inhibitor |
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Side effects of Venlafaxine?
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Nausea
Insomnia |
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Factoid: At low dose, look similar to SSRIs. At high dose, start seeing NE & DA effects.
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Ok
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When is Venlafaxine preferred clinically?
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Melancholy
Severe depression Refractory to other anti-depressants Has a rapid onset |
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What else is Venlafaxine also approved for?
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GAD
Panic Disorder *Do not use as an anorexic!!! *Bipolar? |
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What is MOA of Mirtazapine?
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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 |
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Uses of Mirtazapine?
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Depression (w/ anxiety, w/ panic, severe, loss of SSRI efficacy)
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Don't use for...?
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Immunocompromised due to neurtopenia b/c can potentiate
Hypersomnia, overweight, ... |