1. Anti-Depressant Drugs Flashcards
*All antidepressants either are known to be or can be associated with what, in which a slow titrattion downward is recommended, aka as deprescribing?
Withdrawal Syndrome
Withdrawal Syndrome has symptoms of the acronym FINISH, which include flu like symptoms, insomnia, nausea, imbalance, sensory distrubances and?
Hyperarousal
Antidepressants are used for other indications as well, including nicotine withdrawal (bupropion), enuresis (imipramine) and diabetic peripheral neuropathy, fibromyalgia, chronic MSK pain, and stress incontinence see with what medication?
Duloxetine
The following drugs are what kind of antidepressants? TCAs Desvenlafaxine Duloxetine Venlafaxine Levomilnacipran
SNRI (serotonin-norepinephrine reuptake inhibitors)
The following drugs are what kind of antidepressants?
Amoxapine
SNRI + DA (serotonin norepinephrine reuptake inhibitor + dopamine antagonist)
The following drugs are what kind of antidepressants? Citalopram Escitalopram Fluoxetine Paroxetine Sertaline Vilazodone* Vortioxetine*
SSRIs (selective serotonin reuptake inhibitor)
The following drugs are what kind of antidepressants?
Buproprion
NDRI (noradrenergi-dopamine reuptake inhibitor)
The following drugs are what kind of antidepressants? Mirtazapine Nefazodone Trazodone (odones are also SSRIs)
SARAs (serotonin adrenergic receptor antagonists)
The following drugs are what kind of antidepressants? Isocarboxazid Phenelzine Selegiline Tranylcypromide
MAOIs (monoamine oxidase inhibitors)
What drug is an SSRI and also a partial agonist on 5HT1a?
Vilazodone
What drug is an SSRI and also a partial agonist on 5HT1b and full agonist on 5HT1a, and full antagonist on 5HT1d,3,7?
Vortioxetine
What drug is a noradrenergic dopamine reuptake inhibitor NDRI and also shown to increase NE/DA presynaptic release?
Bupropion
What drug is a MAOI and also a selective agent at low/moderate doses (higher doses are non-selective)?
Selegiline
SSRIs inhibit presynaptic reuptake of serotonin via SERT, resulting in increased/prolonged neurotransmission at post synaptic receptors, what are two SSRIs that have additional MOAs?
Vilazodone
Vortioxetine
*sometimes used as an ‘extra kick’
SSRIs have less impact on histamine, muscarinic and adrenergic receptors as compared to TCAs. There are less SE, which include CNS (sedation or insomnia), sexual dysfunction (all anti-d), weight gain or loss, and what?*
Acute withdrawal reactions *star
SSRIs have SE that include QT prolongation on high doses or in cardiac patients, hyponatremia, (serious)- suicidality, and what-which is seen when given with multiple serotonin affecting agents, and seen as sweating, hyperreflexia, akathisia/myoclonus, and shivering/tremors?
Serotonin Syndrome (multiple serotonin affecting drugs only)
CLONUS
There is variable risk of drug drug interactions (CYP450), with vortioxetine and escitalopram being the least likely to cause interactions, and what is the most likely to inhibit CYP450?
Fluoxetine
SNRIs (which include TCAs) inhibit presynaptic reuptake of serotonin via SERT and NE via NET, tertiary amine TCAs inhibit both equally, secondary amine TCAs inhibit NE more than 5HT, and all other SNRIs inhibit what more than the other?
Inhibit 5HT > NE
What is an SNRI that also is a dopamine antagnoist?
Amoxapine (one of the two that affects dopamine)
Tertiary amine TCA amitriptyline is metabolized in the body to nortriptyline, and tertiary amine TCA imipramine is metabolized in the body to?
Desipramine
TCAs along with SNRI (serotonin norepinephrine via SERT/NET reuptake inhibitor), they also have impact on 3 key non-efficacy related receptors including: histamine (H1), muscarinic (cholinergic), and what?
a1 (adrenergic)
Since TCAs (tri-cyclic agents) also affect alpha, muscarinic and histamine receptors, there are additional SE, including anticholinergic dry mouth/urinary retention/ blurred vision, CNS (histamine) sedation fatigue dizziness seizures and what- which is the most important?
due to A1 adrenergic receptor agonism you see cardiovascular effects including…
tachycardia
orthostatic hypotension
dysrhythmias*
Sort the following TCAs into tertiary and secondary amines... Amoxapine clomipramine Desipramine doxepin nortriptyline imipramine amitriptyline
Tertiary Amine TCA amitriptyline clomipramine doxepin imipramine Secondary Amine TCAs Amoxapine nortriptyline Desipramine
Toxic ingestion of TCAs (over dose) leads to 3 C’s, including coma, convulsions and ?
cardiotoxicity such as conduction abnormalities
quinidine-like effect-slow conduction via Na blockade
Non-TCA SNRIs have SE relatively similar to SSRIs with LESS risk of sexual dysfunction, these drugs include desvenlafaxine, duloxetine, venlafaxine, and ?
levomilnacipran
also amoxapine but has DA
What two agents are SARAs, which act like SSRIs, and which block post synaptic a1 receptors on noradrenergic neurons (NE) and post synpatic 5-HT2 receptors, sometimes also a H1 blockade causing sedation?
Trazodone and Nefazodone
What agent is a SARA, which blocks presynaptic a2 receptors on noradrenergic (NE) and serotonergic (5HT) neurons and blocks post-synaptic 5HT2/3 receptors, with no SERT/NET activity and also blocks H1 (sedation), is the MC used med in depression(?) ?
Mirtazapine
SARAs has SE due to H1/a1… sedation is seen with trazodone and mirtazapine, orthostatic hypotension with trazodone and what med causes weight gain?
Mirtazapine
NDRIs selectively inhibits presynaptic reuptake of NE via NET, and dopamine via DAT, as well as enhanced presynaptic release of NE and DA, which is done via VMAT2… which is the only drug that is in this category?
Bupropion
and amoxipine are the only two that affect dopamine
NDRIs have SE that include agitation and insomnia, weight loss, and are given in the morning as a pick me up since they are stimulation, what is the worst major SE which is seen with high doses or with a history?
Seizures (bupropion)
MAOIs inhibit MAO (A/B) which increases levels of monoamines in neuronal vesicles and increase amounts of NE, 5HT, and DA released, uncommonly used but may be used in treament resistant depression, drugs include isocarboazid, tranylcypromide, Selegiline and?
phenelzine
All oral agents are considered irreversible MAOIs, take 14 days to recover, all agents are non selective, except which MAOI which is B selective?
Selegiline (in a PATCH form)-not oral
MAOI tranylcypromide is a stimulant analog used in ADHD as well shown to increase transmitter release, it is irreversible like the others, but also has the shortest recovery time which is around?
3-5 days, compared to the avg. 14 days
SE of MAOIs include sexual dysfunction, weight gain, and insomnia/agitation/nervousness (like all antidepressants), and orthostatic hypotension is the MC… There are common drug interactions with 5HT/NE affecting drugs, anti-HTNs, amphetamines, SSRIs, TCAs, SNRIs, so remember what?
there is a 2 week wash-out period (fluoxetine is 5 weeks)
There is major concern with MAOIs which is hypertensive crisis*, nonselective MAOIs inhibit MAO-A necessary for GI tyramine metabolism, inc tyramine can induce significant catecholamine release- causing HTNsive crisis, however there is low risk of this occuring with?
Selegiline patch/topical (since it only affects MOA B)
All of the following are signs and symptoms of what? severe headache N/V sweating/anxiety nosebleeds tachycardia chest pain changes in vision shortness of breath confusion
Hypertensive Crisis seen with MOAIs
Note: tyramines found in aged cheese, fermented things, red wine… etc
What is a new miscellaneous antidepressant, an s-isomer of ketamine, NMDA receptor (glutamate) antagonist, indicated for treatment resisitant depression in conjucntion with ongoing anti-d therapy, administer nasally by authorzed physicians, pt observed 2 hours post via BP and sedation?
Esketamine
treatment resistant depression
What is a new miscellaneous antidepressant which is a GABAa receptor positive allosteric modulator, which is identical to endogenous allopregnanolone- levels of which increase during pregnancy and decrease post delivery, therefore used for POST PARTUM DEPRESSION?
Brexanolone
Brexanolone used for postpartum depression is given via 60 hour IV by authorized physician, and observed during infusion q2hr for somnolence and loss of consciousness, with superior efficacy compared to placebo post 60 hr infusion and the efficacy lasts up to?
30 days post-dose
*v expensive– 35k/infusion
Lithium is used as a mood stabilizer because it has effects on brain structure and neurotransmitter modulation… Its effect on brain structures- including anterior cingulate cortex, superior temporal gyrus, ventral prefrontal cortex and hippocampus, are what?
Neuroprotective/Neuroproliferative
Lithium also modulates neurotransmitters, including inhibiting DA during mania (increased DA), downregulates NMDA receptor, and lastly it promotes what?
GABAergic neurotransmission - increasing levels of GABA in CSF
Lithium is a monovalent ion handled by kidneys similarly to Na/K and competes with Na for Kidney reabsorption. Li enters the principal cell in collecting duct via Na channels and interferes with ADH mediated effects with can lead to ADH resistance which results in? (2)
Polyuria/Polydipsia
Nephrogenic Diabetes Insipidus but with mental issues*
Lithium interacts with diuretics (thiazides), ACEIs (lisinopril), and NSAIDs, and is checked via blood levels in which there is a narrow range in which the lithium must be at. MC tested SE of lithium on boards is?
Thyroid Goiter (hypothyroid) because Li inhibits iodination of thyroid hormone
Antiseizure agents (mood stabilizers) such as valproic acid and divalproex are used for ACUTE bipolar I, lamotrigine for maintenance of bipolar disorder (I & II), and carbamazepine is used for acute and maintenance treatment of acute mania and mixed episodes (bipolar I), and it is the only one which is a major?
CYP450 inhibitor
