Anti-depressants 2 Flashcards by K Medina

SNRIs do NOT have affect upon

Alpha-1 adrenergic, cholinergic, dopaminergic, or histaminergic receptors

(less side effects, but unique side effects)

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Unique side effects of SNRI

Pseudocholinergic effects by stimulating NE or receptors in the SNS

(decrease parasympathetic tone)

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Duloxetine inhibits _____ (enzyme)

CYP2D6

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SNRI adverse effects (class effects) (5)

Nausea, dizziness, diaphoresis
Blood pressure increase
Headaches
Sexual dysfunction
Hyponatremia

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In addition to treating depression Duloxetine also treats _____(4)

Generalized anxiety disorder
Diabetic peripheral neuropathic pain
Fibromyalgia
Chronic musculoskeletal pain

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In addition to treating depression, Milnacipran also treats ______

Fibromyalgia

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Venlafaxine side effects

sexual dysfunction

(Most likely SNRI to cause this)

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Two types of Tricyclic antidepressants

Tertiary or secondary amines

(tertiary has the methyl group)

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Tertiary amines effects (2)

Highly anticholinergic
Strong serotonin and norepinephrine reuptake inhibitor

(if this becomes too much, try the secondary Amine TCA)

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Secondary amine effects (3)

less anticholinergic
More potent
More selective norepinephrine reuptake inhibitor

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Tricyclic antidepressant MOA

Serotonin and norepinephrine reuptake inhibitor

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TCAs block: (4)

Blockade of muscarinic M1, H1, alpha-adrenergic 1 receptors
fast Na Channel in cardiac cells

(they bind to everyhing!)

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Which Tri cyclic antidepressants have the best overall tolerability (2)?

Notriptlyin
Desipramine

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All cyclic antidepressants are potentially _____ toxic

cardio

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________ may treat childhood enuresis (bed-wetting)

Imipramine

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What are the three C’s of Tri cyclic antidepressants poisoning

Convulsion
Cardiac arrest
Coma

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Two types of monoamine oxidase inhibitors

Hydrazine
Non hydrazine

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Monoamine oxidase is responsible for _____(2)

Breakdown of Serotonin and norepinephrine

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The blockade of monoamine oxidase a in the gastrointestinal tract is responsible for the ______ reaction associated w/MOAIs

“cheese reaction” = hypertensive crisis

(A patient taking MOAIs and just foods containing the sympathomimetics tyramine)

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MOAIs are metabolized by ______ (process).

acetylation

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MOAIs can also be effective in treating ______.

resistant depression

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MOAIs have potent ____ effects

hypotensive (leading to dizziness)→risk in treating elderly

(also causes urinary hesitancy, headache and myoclonic jerks)

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What is the only antidepressant that is available in a patch?

MAOIs

(Also available sublingually)

Indication of nefazodone

depression

Nefazodone MOA

Antagonize and down regulates postsynaptic serotonin 5-HT2A

Trazodone pharmacokinetics

The table is by CYPT3A4

Trazodone adverse effects

1. priapism 2. sedation (dizziness, dry mouth, nausea)

Vilazodone MOA

1. Serotonin reuptake inhibitor 2. Partial Agonist of 5-HT1A receptor (side effects: diarrhea, sexual dysfunction)

Vilazodone is metabolized by

CYP3A4

Vilazodone adverse effects

sexual dysfunction (diarrhea, N/V)

Vortioxetine indications (2)

1. Treatment for major depression 2. Cognitive dysfunction associated with depression (metabolized by CYP2D6)

Ketamine MOA

NMDA ***_noncompetitve_*** antagonist → releases BDNF

Ketamine indication

Suicide prevention (when the patient is on the brink; must be given at the doctor's office); not for regular depression tx (rapid effect)

Brexanolone indication

Postpartum depression → due to the drop in alopregnenalone (effect lasts for ***_30 days,_*** no dissociateive symptoms or risk of abuse)

Brexanalone

1. Sedation / somnolence 2. Dry mouth 3. Loss of consciousness

Duloxetine should be prescribed with caution to patients with the following conditions (4).

1. Severe kidney impairment 2. Hepatic impairment 3. Angle closure glaucoma 4. Alcohol abuse

Levomilnacipran side effects

1. Not recommended for patients with kidney disease 2. Caution with angle closure glaucoma, hypertension or cardiovascular conditions (at low dose blocks reuptake of NE 2xs more potently than 5-HT)

Milnacipran should be avoided in patients with the following conditions

1. End stage kidney disease 2. Angle closure glaucoma 3. Chronic liver disease 4. Alcohol abuse

Venlafaxine should be avoided in patients with the following conditions

1. angle closure glaucoma 2. patients at risk for bleeding (anticoagulants)

TCA Metabolism & elimination occurs largely in the liver by which enzymes (4)?

1. 1A2 2. 1C19 3. 2D6 4. 3A4

Many of the TCA metabolites have \_\_\_\_\_a ctivity. Desipramine is the active (demethylated) metabolite of \_\_\_\_\_, and nortriptyline is the active (demethylated) metabolite of \_\_\_\_\_\_.

* antidepressant * imipramine * amitriptyline

Trazadone use other than antidepressant:

* dyspepsia * hypnotic

Nefazodone adverse effects is mainly \_\_\_\_\_\_\_\_.

Acute liver failure Patients receiving the drug should be monitored for signs and symptoms of liver failure (nausea, abdominal pain, jaundice, impaired synthetic function, coagulopathy, and delirium)

TCA: adverse effects (5)

1. Prolonged QT interval 2. Tremor 3. Bone fracture 4. Neuroleptic malignant syndrome (amoxapine) 5. Tardive dyskinesia (amoxapine)

Tricyclic antidepressant poisoning: treatment of hypotension

Isotonic crystalloid (vasopressor if necessary, i.e. neosynephrine or norepinephrine are preferred)

Tricyclic antidepressant poisoning: treatment of conduction disturbances

1. Challenge with intravenous sodium bicarbonate 2. If QRS Narrows, begin continuous infusion (150 mEq of sodium bicarbonate in 1 liter of D5W to run at 250 mL/hour in adults or twice the maintenance fluid rate in children)

Tricyclic antidepressant poisoning: treatment of gastrointestinal issues

Administer activated charcoal if patient presents within 2 hours of ingestion (1 g/kg. maximum dose 50 g)

Tricyclic antidepressant poisoning: treatment of seizures

Benzodiazepine (**do not** treat with phenytoin)

Tranylcypromine predominantly an irreversible inhibitor of \_\_\_\_\_, but also irreversibly inhibits \_\_\_\_to a degree; It also appears to block reuptake of ______ (2).

* MAO A * MAO B * erotonin and catecholamines

Tranylcypromine: drug interactions (2)

1. interact with sympathomimetics → hypertensive crisis 2. interact with serotonin syndrome medications → serotonin syndrome

Phenelzine irreversibly inhibits \_\_\_\_\_(2).

1. MAO A 2. MAO B

Phenelzine side effects (3)

1. Weight gain 2. Sedation 3. **Sexual dysfunction** 4. (rarely hepatotoxicity, all MAO-Is cause sexual dysfunction, except for selegiline)

All MAO-Is cause sexual dysfunction, except for \_\_\_\_\_\_.

Selegiline

Selegiline mechanism of action

Selective MAO B inhibitor; non-selective at higher doses

EMSAM is FDSA approved for use in the treatment of depression. Also available in \_\_\_\_\_\_

sublingual forms that bypass both gut and liver metabolism (this is a form of selegeline; which also comes as a transdermal patch)