Pharmacology - Antidepressants - Oliver Brown Flashcards
T/F: Most antidepressant drugs block the reuptake of both NE and 5HT to varying degrees.
True
Give the class: Tranylcypromine
MAOI
Give the class: Fluoxetine
SSRI
Give the class: Citalopram
SSRI
Give the class: Duloxetine
SNRI
serotonin-norepi reuptake inhibitor
Give the class: Venlafaxine
SNRI
Give the mechanism:
Tranylcypromine
Phenelzine
Irreversibly inhibit both MAO-A and MAO-B
MAOI
Give the side effects: Tranylcypromine
Hypertensive crisis (with tyramine-rich foods); serotonin syndrome (MAOI + SSRI)
Anticholinergic, orthostatic hypotension, sexual dysfunction, weight gain, sedation, insomnia, dizziness
What is Tranylcypromine used for:
Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism
Give the mechanism: Fluoxetine Sertraline Citalopram Escitalopram Paroxetine
Inhibit reuptake of 5-HT (and NE to lesser extent)
SSRI
Give the indication: Fluoxetine Sertraline Citalopram Escitalopram Paroxetine
Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism; pre-menstrual dystrophic disorder
Give the side effects: Fluoxetine Sertraline Citalopram Escitalopram Paroxetine
Serotonin syndrom (with MAOIs)
Fewer than tricyclics; mostly nausea, decreased sexual function
What is unique about Fluoxetine and Paroxetine as SSRIs?
They are Potent P450 inhibitors; form active metabolite (norfluoxetine)
Specifically CYP2D, CYP2C, CYP2A
Give the class: Venlafaxine (Effexor)
SNRI
Give the mechanism:
Duloxetine (Cymbalta)
Venlafaxine (Effexor)
Inhibits reuptake of 5-HT and NE
Give the indication:
Duloxetine (Cymbalta)
Venlafaxine (Effexor)
Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism
Give the class: Buproprion
Atypical antidepressant
Give the class: Mirtazapine
Atypical antidepressant
Give the mechanism: Mirtazapine
5HT2a antagonist; also inhibits 5HT reuptake
Give the indication: Buprioprion
Depression, weight loss, smoking cessation (my answer)
Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism; maintain nicotine abstinence in quitting smokers (their answer)
Give the indication: Mirtazapine
Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism
Give the important side effect of Buproprion
It lowers the seizure threshold
Give the class:
Trazodone
Nefazodone
5HT2A antagonist
also inhibits serotonin reuptake
use for depression esp when coupled with insomnia
Side effects include drowsiness (major)
What are some miscellaneous antidepressant treatments?
Lithium salts St. John's Wort ECT TMS (transcranial magnetic stimulation) - like ECT but w/o the siezure NRIs Ketamine
Give the class: Phenelzine
MAOI
MAO-A oxidizes mainly:
NE, 5HT, tyramine
MAO-B oxidizes mainly:
DA, phenylethylamine
What is serotonin syndrome?
When a pt is on MAOI and SSRI (or other drugs)
potentially lethal
Hyperthermia, Muscle rigidity, Myoclonus, Rapid changes in mental status and vital signs
Give the class: Desipramine Imipramine Amitriptyline Nortriptyline
Tricyclics
Give the mechanism: Desipramine Imipramine Amitriptyline Nortriptyline
Block reuptake of NE or 5-HT at varying potencies and selectivity; also variably block muscarinic, a-adrenergic, dopamine, and histamine receptors
Give the indication: Desipramine Imipramine Amitriptyline Nortriptyline
Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism
What is the added unique indication of Amitriptyline?
prevention of tension headaches, migraines
Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism;
Give the side effects: Desipramine Imipramine Amitriptyline Nortriptyline
Sympathomimetic (cardiac arrhythmias and conduction defects, especially at OD)
Antimuscarinic, orthostatic hypotension, sedation (additive with alcohol), seizures
Are the tricyclics used often to treat depression?
No
Not very safe; rarely used anymore
Overdose of tricylcics may cause what serious adverse effect?
cardiac arrhythmias
conduction defects
Main complaints patients give when taking SSRIs are:
Nausea
Sexual dysfunction
What is the only atypical antidepressant that is selective for dopamine uptake transporter?
Buproprion
Give the mechanism: Ketamine
NMDA receptor antagonist
produces rapid antidepressant response - rapidly increases synaptogenesis in mice
What is enuresis?
Institutionalized elderly patients who have incontinence
An indication for antidepressant use
T/F: SSRIs are more effective antidepressants than tricyclics.
False
They have the same efficacy but are better tolerated.
What anticonvulsants are used to treat bipolar depression?
Carbamazepine
Valproate
What class of drugs are indicated for severe bipolar disorder?
The antipsychotics:
Olanzapine (Zyprexa)
Risperidone (Risperdal)
Aripiprazole (Abilify)
Give the side effects: Lithium
Drowsiness, weight gain, tremor, polydipsia, polyuria
Neurotoxicity, Cardiac toxicity, renal dysfunction with elevated levels
Give the mechanism: Lithium
Lithium causes depletion of inositol phosphate second messengers (IP3 and DAG depleted)
What is the bioamine hypothesis of depression?
Too little CNS NE and or 5HT (amount or activity)
