Anti-Depressant

Question 0

SNRI (Venlafaxine, Effexor, Duloxetine)

Answer 0

Action: serotonin reuptake and norepinephrine reuptake portion of molecule block respective pumps. Dual action anti-depressant
Indication: Depression, with or without pain, ache.
Dose: 75-375mg qd, short half life
Side effects: GI, sexual, sweat, Na, sleep, mania, diastolic BP increases
Black box: increased suicidal ideation up to 25yo
Interactions: very weak 2D6 inhibitor, increased levels of MAOI and TCA
Special: dual re-uptake >225mg qd, discontinuation sx can be bad

Question 1

SSRI (Citalopram, Sertraline, Celexa, Escitalopram, Fluoxetine, Paroxetine, Fluvoxamine, Prozac, Zoloft)

Answer 1

Action: selective serotonin reuptake inhibitor, increase levels of serotonin in synapse
Dose- 20-40mg qd
Side Effects: GI, sexual, sleep, sweating, hyponatremia, mania
Black box: increase in suicidal thinking up to 25yo
Interactions: weak 2D6 inhibition, can increase MAOI and TCA levels
Special: first-line anti-depressant
QTc prolongation avg 18msec at 60mg qd (>480msec risk of Torsade’s)

Question 2

TCA (Nortriptyline, Pamelor, Chlomipramine, Anafranil, Imipramine, Amitriptyline)

Answer 2

Tertiary amine
Serotonergic > norepinephrine
Secondary amine (Nortriptyline)
Norepinephrine > serotonergic
Action: dual antagonist at Serotonin reuptaker and norepinephrine reuptaker. Also antagonizes Histaminic, cholinergic, a1 receptors
ADR: wt gain, sedation, ach crisis, hypotension, arrhythmia, sexual, sweat, delirium–contraindicated in Alzheimer’s pt
Interaction: inhibit 2D6, increase levels of MAOI and TCA
Special: lethal in overdose (LD50 is 2000-3000mg), not first-line antidepressant due to ADR

Question 3

NDRI (Bupropion, Wellbutrin, Zyban)

Answer 3

Action: reuptake inhibitor for norepinephrine and dopamine
Dose: XL 150-450mg qd
Side effect: good safety profile, insomina, tremor, tinnitus, seizures
Interactions: 2d6 inhibition, increase levels of MAOI, TCA, tramado, levodopa
Special: avoid in eating d/o and seizure d/o, least likely to cause mania, may reduce sexual ADR in AD

Question 4

MAO-I (Phenelzine, Nardil, Tranylcypromine, Parnate)

Answer 4

Action: “The Big Kahuna” inhibit degradation of monoamines
Phenelzine (sedating, originally developed as TB drug), Tranylcypromine (stimulating, developed as amphetamine)
Side effects: serotonin syndrome (MS changes, autonomic instability, neuromuscular signs), hypertensive crisis (“cheese syndrome”)
Interaction: methadone (act as SSRI),
Special: third line anti-depressant

Question 5

NaSSA (Mirtazapine, Remeron)

Answer 5

Action: noradrenergic and specific serotonergic antidepressants (NaSSA), antagonizes a2, blocks serotonergic receptors in unwanted areas of brain, also blocks histamine
Dose: 15-45mg qd
ADR: sedating, wt gain (histamine), low sexual ADR
Interaction: no P450, do not combine with MAOI

Question 6

SARI (Trazodone, Nefazodone)

Answer 6

Class: serotonin 2A antagonists and reuptake inhibitors, dual action but different mechanism from SNRI, TCA, and MAOI

Question 7

Benzodiazepine (Diazepem, Valium, Xanax)

Answer 7

Drug class: GABA receptor agonist
Indications: anxiolytic, sedative, anti-epileptic, muscle relaxant, anterograde amnesia
Dose: 4-40mg qd
Half life: 20-50hrs, very long
Interaction: with CNS depressant, opiates, cimetidine
Special: diazepem is non-selective, valium for alcohol withdrawal seizure/same receptor, hepatically cleared, give renally-clearing bzd for alcoholic/cirrhosis
Zolpidem: preferential affinity for a subunit (Zzzzz)

Question 8

Buspirone (BuSpar)

Answer 8

Class: 5HT-1A partial agonist
Indication: GAD, Augment MDD
Dose: 15-45mg bid
ADR: dizziness, h/a, sedation, nervous/restless
Interactions: with MAOI
Special: no sexual side effects, no dependence, no withdrawal, takes 4wks+ to work