Flashcards in Antidepressants and Mood Stabilizers Deck (30)
Serotonin-Selective Reuptake Inhibitor MOA - ___ inhibit the ___‐synaptic reuptake of serotonin (via ___)
Selectively inhibit the pre‐synaptic reuptake of serotonin (via SERT)
o results in enhanced, prolonged serotonergic neurotransmission to post‐synaptic receptors
As a class, why do SSRI's have fewer side effects than TCA's?
As a class, much less impact on
-histamine receptors (CNS)
-muscarinic receptors (anticholingergic)
-adrenergic receptors (CV)
Minor/infrequent side effects of SSRI's (five areas).
What other class subset has this?
o Sexual dysfunction
o GI (N/V/dyspepsia)
o CNS (sedation or insomnia/agitation)
o Weight gain
o QT prolongation
Non-TCA SNRI's have similar side effects.
**What drug in the SSRI class has highest risk of drug-drug interaction?
**Fluoxetine (strong CYP450 inhibitor)
What two drugs in the SSRI class has least risk of drug-drug interaction?
Citalopram and sertraline (mild CYP450 inhibitor)
Sweating, hyperreflexia, akathisia/myoclonus, shivering/tremors - What state is this and what causes it?
Increased risk of this when given in combo with other serotonin-affecting (i.e. SSRI's) agents.
What drug class includes TCA's?
Difference in MOA between tertiary and secondary amine TCA's.
Tertiary - inhibit both NE/5‐HT relatively equally.
Secondary - inhibit NE more than 5‐HT.
What three receptors do TCA-based SNRI's impact?
alpha adrenergic - CV
muscarinic - anticholinergic
Histamine - CNS
Symptoms indicating a toxic TCA overdose?
3 C's (Tri C): Coma, Cardiotoxicity (Conduction abnormalities - CoD), Convulsions
What is the "Quinidine-like" effect that results from toxic TCA overdose?
Class 1A Antiarrhythmic:
-Slows Conduction - In Ventricular cells: Slows phase 0 depolarization & conduction velocity
- Na channel blockade
What Serotonin-Adrenergic Receptor Antagonists (SARA's) has sleep assistance?
What Serotonin-Adrenergic Receptor Antagonists (SARA's) selectively block pre‐synaptic 5‐HT2A and block α1 post‐synaptic adrenergic receptors?
Trazodone and nefazodone
What Serotonin-Adrenergic Receptor Antagonists (SARA's) selectively blocks pre‐synaptic α2 adrenergic
receptors & on serotonergic neurons?
Common SE of Serotonin-Adrenergic Receptor Antagonists (SARA's)
o CNS (sedation) - H1 and/or alpha1
o Weight gain
o Dry mouth
A depressed smoker who needs meds for both depression and smoking cessation.
Bupropion, which is a Noradrenergic-Dopamine Reuptake Inhibitors (NDRI) - inhibit the pre‐synaptic reuptake of serotonin norepinephrine (via NET) & dopamine (via DAT)
MOA of Bupropion?
(An NDRI) Selectively inhibit the pre‐synaptic reuptake of
serotonin norepinephrine (via NET) & dopamine
Unique side effect of Noradrenergic-Dopamine Reuptake Inhibitors
agitation/insomnia - stimulating property
What three amine neurotransmitters do do MAOI's increase levels of?
NE, 5-HT, DA (they inhibit both MAO A and B)
What is the only B-selective MAOI is NOT irreversible?
Selegiline (B-selective, non-selective at high doses)
Cheese and wine :)
MAOI hypertensive crisis
What is the biggest limiting factor of MAOI's?
What MAOI would not have this effect?
Hypertensive crisis - because MAOI's inhibit MAO-A, which is necessary for Tyramine metabolism.
What drug can reduce risk of suicide in bipolar patients?
Three classic drug-drug interaction with lithium.
Any drug that increases Na excretion **(NSAIDs, ACE inhibitor lisinopril, diuretic thiazides)** will increase reabsorption of lithium.
***What drug causes nephrogenic diabetes insipidus?
***Lithium (see polyuria/polydipsia).
Due to the renal impact Na/K/lithium.
***What antiseizure/bipolar medication is a major CYP450 inducer?
***carbamazepine (esp drugs metab by CYP3A4)
used for actue and maintenance treatment
Which mood stabilizer is used for acute bipolar with or w/o psychotic features?
***What anti-seizure/bipolar medication is a major CYP450 inhibitor?
When taking SSRI's, TCA's, SNRI's, sympathomimetics, antihypertensives, or any 5-HT/NE affecting drugs, what is contraindicated in tx of depression/anxiety?