SSRIs: Citalopram, Escitalopram, and Fluoxetine
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Questions and Answers

Which SSRI is noted for potentially suppressing nitric oxide synthase at higher doses?

  • Fluoxetine
  • Paroxetine (correct)
  • Sertraline
  • Vortioxetine

Which formulation of paroxetine is designed to minimize gastrointestinal side effects?

  • Oral Concentrate Solution
  • Controlled Release (CR) (correct)
  • Immediate Release
  • Suspension

A patient reports experiencing nausea and diarrhea after starting an SSRI. Which of the following medications is MOST likely the cause, based solely on its common side effects?

  • Sertraline (correct)
  • Lithium
  • Amitriptyline
  • Haloperidol

Which SSRI is also available as an oral concentrate solution?

<p>Sertraline (C)</p> Signup and view all the answers

A clinician is considering prescribing an antidepressant that acts as an SSRI and also has agonist activity at the 5-HT1A receptor. Which of the following medications fits this profile?

<p>Vortioxetine (B)</p> Signup and view all the answers

Which medication's multimodal mechanism of action is thought to confer potential cognitive benefits for some patients?

<p>Vortioxetine (C)</p> Signup and view all the answers

Which of the following is a contraindication for venlafaxine?

<p>Known hypersensitivity (C)</p> Signup and view all the answers

At lower doses, venlafaxine primarily affects which neurotransmitter system?

<p>Serotonin (B)</p> Signup and view all the answers

Which of the following side effects is most closely associated with higher doses of venlafaxine, differentiating it from typical SSRI side effect profiles?

<p>Dose-related increases in blood pressure (A)</p> Signup and view all the answers

A patient taking an antidepressant is experiencing significant nausea, sexual dysfunction, and insomnia. If sertraline and vortioxetine are known to have these side effects, what differentiates them based on their mechanisms of action?

<p>Sertraline acts solely as an SSRI, whereas vortioxetine has additional receptor activity. (C)</p> Signup and view all the answers

Which of the following best describes the primary mechanism of action shared by all listed SSRIs?

<p>Selectively inhibiting presynaptic serotonin reuptake. (C)</p> Signup and view all the answers

A patient reports experiencing dry mouth and constipation after starting an SSRI. Which of the following is the MOST likely cause?

<p>Paroxetine (Paxil) (A)</p> Signup and view all the answers

Which SSRI has a once-weekly formulation?

<p>Fluoxetine (Prozac) (D)</p> Signup and view all the answers

A patient is being switched from fluoxetine to a monoamine oxidase inhibitor (MAOI). What is the recommended minimum washout period before starting the MAOI?

<p>5 weeks (D)</p> Signup and view all the answers

Which of the following SSRIs is MOST commonly used for obsessive-compulsive disorder (OCD) and social anxiety disorder?

<p>Fluvoxamine (Luvox) (C)</p> Signup and view all the answers

Which SSRI is available under the brand name Serafem?

<p>Fluoxetine (D)</p> Signup and view all the answers

Which SSRI is associated with QTc prolongation at higher doses, necessitating caution and a maximum recommended daily dose?

<p>Citalopram (Celexa) (B)</p> Signup and view all the answers

Which SSRI is considered the most 'activating,' potentially leading to insomnia in some patients?

<p>Fluoxetine (Prozac) (D)</p> Signup and view all the answers

A patient abruptly discontinues paroxetine after several months of treatment. Which of the following is the MOST likely reason for experiencing significant withdrawal symptoms compared to other SSRIs?

<p>Paroxetine has one of the shortest half-lives in the SSRI class (B)</p> Signup and view all the answers

Which of the following statements about enantiomers of SSRIs is true?

<p>Escitalopram consists only of the S-enantiomer; citalopram is a racemic mixture. (A)</p> Signup and view all the answers

Which of the following SSRIs is available in a controlled-release formulation?

<p>Paroxetine (Paxil CR) (A)</p> Signup and view all the answers

A patient with PMDD may be prescribed which brand name of fluoxetine?

<p>Serafem (A)</p> Signup and view all the answers

Which SSRI is most likely to cause significant withdrawal symptoms upon abrupt discontinuation due to its short half-life?

<p>Paroxetine (A)</p> Signup and view all the answers

Which SSRI is primarily used for obsessive-compulsive disorder (OCD) and social anxiety disorder, and is not typically used for major depressive disorder (MDD) in the U.S.?

<p>Fluvoxamine (D)</p> Signup and view all the answers

Which of the following side effects is most associated with paroxetine compared to other SSRIs?

<p>Anticholinergic effects (B)</p> Signup and view all the answers

Which SSRI requires a 5-week washout period when switching to or from a monoamine oxidase inhibitor (MAOI)?

<p>Fluoxetine (B)</p> Signup and view all the answers

Which SSRI, when administered at doses exceeding 40 mg/day, poses an elevated risk of QTc prolongation?

<p>Citalopram (A)</p> Signup and view all the answers

How does the mechanism of action of escitalopram differ from that of citalopram?

<p>Escitalopram is the S-enantiomer of citalopram, making it enantiomerically pure. (B)</p> Signup and view all the answers

Which statement accurately describes the relative likelihood of insomnia as a side effect among the listed SSRIs?

<p>Fluoxetine is the most likely to cause insomnia due to its activating properties. (B)</p> Signup and view all the answers

A cytochrome P450 (CYP450) inhibition profile for an SSRI reveals significant inhibition of CYP2D6. This characteristic would be most relevant when considering potential drug interactions with which of the following?

<p>A prodrug activated by CYP2D6 into its active form. (B)</p> Signup and view all the answers

Which of the following SSRIs is known for its relatively high anticholinergic activity?

<p>Paroxetine (D)</p> Signup and view all the answers

Which of the following is an important consideration when prescribing venlafaxine, particularly at higher dosages?

<p>Dose-related increases in blood pressure (D)</p> Signup and view all the answers

A patient experiences significant nausea and diarrhea after starting an antidepressant. If sertraline and vortioxetine are known to cause these side effects, which of the following differentiates them based on their mechanisms of action?

<p>Vortioxetine also acts as an agonist at the 5-HT1A receptor and antagonist at the 5-HT3 receptor. (A)</p> Signup and view all the answers

Which antidepressant has a mechanism of action that includes both serotonin reuptake inhibition and direct agonism of the 5-HT1A receptor?

<p>Vortioxetine (A)</p> Signup and view all the answers

What is a key consideration to keep in mind while prescribing sertraline?

<p>It is available as an oral concentrate solution. (A)</p> Signup and view all the answers

Which of the following antidepressants is LEAST likely to cause a significant increase in blood pressure, even at higher doses?

<p>Sertraline (A)</p> Signup and view all the answers

Which antidepressant is most likely to be considered as a first-line treatment option because of its balanced side effect profile?

<p>Sertraline (C)</p> Signup and view all the answers

Which of the following side effects is most associated with venlafaxine?

<p>Dose-dependent hypertension (C)</p> Signup and view all the answers

Which antidepressant's prescribing information specifically advises caution in patients with uncontrolled hypertension due to its potential to increase blood pressure?

<p>Venlafaxine (C)</p> Signup and view all the answers

A patient on venlafaxine develops a blood pressure of 160/100 mmHg. What is the MOST appropriate initial step?

<p>Reduce the dose of venlafaxine and monitor blood pressure. (C)</p> Signup and view all the answers

Which of the following antidepressants is available in both immediate-release and extended-release formulations, potentially affecting its dosing schedule and side effect profile?

<p>Bupropion (A)</p> Signup and view all the answers

A patient is currently taking an antidepressant that inhibits both serotonin and norepinephrine reuptake. To what class of medications does this antidepressant belong?

<p>Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) (A)</p> Signup and view all the answers

Considering the listed medications, which of the following requires monitoring of blood pressure, especially at higher doses, due to its pharmacological action?

<p>Venlafaxine (A)</p> Signup and view all the answers

A clinician is looking for an antidepressant option that has a multimodal mechanism including 5-HT modulation but is NOT classified as either an SSRI or SNRI. Which of the following would be the MOST appropriate choice?

<p>Vortioxetine (B)</p> Signup and view all the answers

Which of the following medications comes in a transdermal form?

<p>Selegiline (D)</p> Signup and view all the answers

A patient who is CYP2D6 poor metabolizer is prescribed a moderate dose of desvenlafaxine. Which of the following outcomes is MOST likely?

<p>The patient will experience an increased risk of adverse effects due to elevated desvenlafaxine levels. (C)</p> Signup and view all the answers

A patient on tranylcypromine starts taking an herbal supplement containing tyramine. Which of the following physiological responses is MOST likely to occur?

<p>Hypertensive crisis due to accumulation of tyramine. (B)</p> Signup and view all the answers

Which of the following strategies is MOST appropriate to mitigate the risk of serotonin syndrome when switching from fluoxetine to tranylcypromine?

<p>Implement a 5-week washout period after discontinuing fluoxetine before starting tranylcypromine. (D)</p> Signup and view all the answers

A patient is started on phenelzine for treatment-resistant depression. What dietary modification is MOST crucial to educate the patient about?

<p>Avoiding foods high in tyramine to prevent hypertensive crisis. (C)</p> Signup and view all the answers

A patient is being treated with levomilnacipran. Which of the following pre-existing conditions would warrant the MOST caution when prescribing this medication?

<p>Narrow-angle glaucoma (C)</p> Signup and view all the answers

A patient taking an antidepressant is scheduled for elective surgery requiring anesthesia. Which antidepressant poses the GREATEST risk of interaction with anesthetic agents, potentially leading to cardiovascular instability?

<p>Amitriptyline (C)</p> Signup and view all the answers

Which of the following best explains why trazodone is often prescribed at lower doses for insomnia compared to its antidepressant dosages?

<p>Trazodone's antihistaminic effects are more pronounced at lower doses, promoting sedation. (C)</p> Signup and view all the answers

A patient on mirtazapine reports significant weight gain and daytime sedation. Which of the following strategies is the MOST appropriate initial step?

<p>Lower the dose of mirtazapine, if clinically appropriate, to minimize antihistaminic effects. (A)</p> Signup and view all the answers

A patient with depression and comorbid neuropathic pain might benefit MOST from which of the following antidepressants?

<p>Duloxetine (C)</p> Signup and view all the answers

A patient presents with depressive symptoms and significant fatigue. After ruling out medical causes, which antidepressant would be the LEAST likely choice due to its potential to exacerbate fatigue?

<p>Mirtazapine (D)</p> Signup and view all the answers

Flashcards

SSRIs: Mechanism

Selectively inhibit presynaptic reuptake of serotonin (5-HT), increasing serotonin levels in the synaptic cleft.

Citalopram (Celexa®): Side Effects

Nausea, sexual dysfunction, potential sedation or insomnia, initial anxiety increase, QTc prolongation risk.

Escitalopram (Lexapro®)

Selectively inhibits presynaptic serotonin reuptake; S-enantiomer only.

Escitalopram (Lexapro®): Side Effects

Nausea, insomnia or sedation, headache, and sexual dysfunction.

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Fluoxetine (Prozac®): Side Effects

Nausea, sexual dysfunction, insomnia (most 'activating' SSRI), and can increase anxiety.

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Fluoxetine (Prozac®): Half-life

Long half-life (and even longer for its active metabolite, norfluoxetine).

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Fluvoxamine (Luvox®): Side Effects

Nausea, sedation, sexual dysfunction, and GI upset.

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Fluvoxamine (Luvox®): Uses

Primarily FDA-approved for obsessive-compulsive disorder (OCD) and social anxiety disorder.

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Paroxetine (Paxil®): Side Effects

Notable anticholinergic effects, sedation, weight gain, sexual dysfunction, significant withdrawal.

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Paroxetine (Paxil®): Discontinuation

Significant withdrawal symptoms if abruptly discontinued (shortest half-life in SSRI class).

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Paroxetine's Key Traits

An SSRI with anticholinergic properties; may suppress nitric oxide synthase at higher doses.

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Sertraline's Action

Selectively inhibits presynaptic serotonin reuptake.

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Sertraline's Side Effects

Nausea, diarrhea, sexual dysfunction, insomnia or sedation (varies by patient).

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Vortioxetine's Mechanism

SSRI plus 5‐HT1A agonist and 5‐HT3 antagonist activity.

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Vortioxetine's Side Effects

Nausea, diarrhea, dizziness, possible sexual dysfunction.

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Venlafaxine's Action

Inhibits presynaptic reuptake of serotonin and norepinephrine.

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Venlafaxine's Side Effects

Nausea, sexual dysfunction, dose‐related increases in blood pressure, insomnia, and increased sweating.

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Venlafaxine Contraindication

Caution advised due to potential blood pressure elevations.

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Paroxetine CR benefit

An approved extended-release formulation of Paroxetine to reduce the side effects.

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Sertraline's Usage

Often a first‐line SSRI due to a balanced side effect profile.

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Sertraline's (Zoloft®) Action

Selectively inhibits presynaptic serotonin reuptake.

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Vortioxetine (Trintellix®) Mechanism

Functions as an SSRI with additional receptor activity (agonist at 5‐HT1A, antagonist at 5‐HT3).

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Vortioxetine's Benefit

May offer cognitive benefits for some patients due to its multimodal mechanism.

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Venlafaxine's (Effexor®) Action

Inhibits presynaptic reuptake of serotonin and norepinephrine.

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Vortioxetine's (Trintellix®) Side Effects

Nausea, diarrhea, dizziness, possible sexual dysfunction.

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Sertraline Contraindication

Known hypersensitivity to sertraline.

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Venlafaxine's (Effexor ®) Side Effects

Nausea, sexual dysfunction, dose‐related increases in blood pressure, insomnia, and increased sweating.

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Vortioxetine Contraindication

Known hypersensitivity to vortioxetine.

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Citalopram (Celexa®): Action

Selectively inhibits presynaptic reuptake of serotonin (5-HT), increasing serotonin levels.

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Venlafaxine Dosage Effect

Has more of an SSRI effect at lower doses.

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Citalopram (Celexa®): Contraindication

Hypersensitivity to citalopram.

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Escitalopram (Lexapro®): Action

S-enantiomer of citalopram; inhibits presynaptic serotonin reuptake.

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Escitalopram (Lexapro®): Contraindication

Hypersensitivity to escitalopram.

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Fluoxetine (Prozac®): Action

Selectively inhibits presynaptic serotonin reuptake.

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Fluoxetine (Prozac®): Contraindication

Hypersensitivity to fluoxetine; caution with MAOIs.

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Fluvoxamine (Luvox®): Action

Selectively inhibits presynaptic serotonin reuptake.

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Fluvoxamine (Luvox®): Contraindication

Hypersensitivity to fluvoxamine.

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Paroxetine (Paxil®): Action

Selectively inhibits presynaptic serotonin reuptake.

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Paroxetine (Paxil®): Contraindication

Hypersensitivity to paroxetine; caution with abrupt stop.

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TCAs: Mechanism

Block reuptake of serotonin and norepinephrine, but act on other receptors too, leading to more side effects.

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MAOIs: Mechanism

Inhibit monoamine oxidase, preventing breakdown of neurotransmitters like serotonin, norepinephrine, and dopamine.

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Bupropion: Class

An antidepressant that inhibits the reuptake of dopamine and norepinephrine.

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Mirtazapine: Action

Block serotonin reuptake and antagonizes certain serotonin receptors.

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Venlafaxine (Effexor®)

A SNRI antidepressant.

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Bupropion (Wellbutrin®)

An atypical antidepressant that primarily affects dopamine and norepinephrine.

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Mirtazapine (Remeron®)

Blocks certain serotonin receptors and also blocks serotonin reuptake.

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Amitriptyline (Elavil®)

Tertiary amine TCA.

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Nortriptyline (Pamelor®)

A secondary amine TCA.

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Maprotiline (Ludiomil®)

Blocks norepinephrine and, to a lesser extent, dopamine reuptake.

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MAOIs: Dietary restriction

Must avoid tyramine-rich foods.

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Study Notes

  • Selective Serotonin Reuptake Inhibitors (SSRIs) increase serotonin levels in the synaptic cleft by selectively inhibiting presynaptic reuptake of serotonin (5-HT).

Citalopram (Celexa®)

  • Selectively inhibits presynaptic reuptake of serotonin (5-HT).
  • Increases serotonin levels in the synaptic cleft.
  • Key side effects include nausea, sexual dysfunction, potential sedation or insomnia, an initial increase in anxiety, and risk of QTc prolongation at doses greater than 40 mg/day.
  • Should not be taken by individuals with known hypersensitivity.
  • A maximum daily dose of 40 mg is advised to reduce QT prolongation risk.
  • Typically, the maximum recommended daily dose is 40 mg/day to reduce QT prolongation risk.

Escitalopram (Lexapro®)

  • Selectively inhibits presynaptic serotonin reuptake.
  • Consists only of the S-enantiomer (enantiomerically pure).
  • Key side effects are nausea, insomnia or sedation, headache, and sexual dysfunction.
  • Should not be taken by individuals with known hypersensitivity.
  • Thought to have a slightly better side effect profile than citalopram.
  • Similar to citalopram but consists only of the S-enantiomer (making it enantiomerically pure).

Fluoxetine (Prozac®, Prozac Weekly®, Serafem®, Selfemra®)

  • Selectively inhibits presynaptic serotonin reuptake.
  • Key side effects include nausea, sexual dysfunction, and insomnia; can initially increase anxiety.
  • Should not be taken by individuals with known hypersensitivity to fluoxetine; caution with concurrent MAOI use (requires a 5-week washout).
  • The SSRI which is the most “activating".
  • Has a long half-life, and its active metabolite, norfluoxetine, has an even longer half-life.
  • Prozac Weekly® is for once-weekly usage.
  • Serafem® is a brand name typically used for PMDD.
  • Considered the most "activating" SSRI.

Fluvoxamine (Luvox®)

  • Selectively inhibits presynaptic serotonin reuptake.
  • Key side effects are nausea, sedation, sexual dysfunction, and GI upset.
  • Should not be taken by individuals with known hypersensitivity to fluvoxamine.
  • Primarily FDA-approved for obsessive–compulsive disorder (OCD) and social anxiety disorder.
  • Not typically used for MDD in the U.S., though may be used off-label.

Paroxetine (Paxil®, Pexeva®, Paxil CR®)

  • Selectively inhibits presynaptic serotonin reuptake.
  • Key side effects include anticholinergic effects (e.g., dry mouth, constipation), sedation, weight gain, increased risk of sexual dysfunction, and significant withdrawal symptoms if abruptly discontinued because it has one of the shortest half‐lives in the SSRI class.
  • Should not be taken by individuals with known hypersensitivity to paroxetine; caution with abrupt discontinuation.
  • Considered the most anticholinergic SSRI.
  • Higher dosages could reduce nitric oxide synthase, which could lead to erectile dysfunction.
  • The CR formulation can help reduce GI side effects.
  • May suppress nitric oxide synthase at higher doses, possibly contributing to erectile dysfunction.

Sertraline (Zoloft®)

  • Selectively inhibits presynaptic serotonin reuptake.
  • Key side effects are nausea, diarrhea, sexual dysfunction, insomnia or sedation (varies by patient).
  • Should not be taken by individuals with known hypersensitivity to sertraline.
  • Often a first-line SSRI is due to a balanced side effect profile.
  • Also available as an oral concentrate solution.

Vortioxetine (Trintellix®)

  • Functions as an SSRI plus additional receptor activity (agonist at 5-HT1A, antagonist at 5-HT3).
  • Key side effects are nausea, diarrhea, dizziness, and possible sexual dysfunction.
  • Should not be taken by individuals with known hypersensitivity to vortioxetine.
  • The multimodal mechanism may offer cognitive benefits for some patients.

Serotonin–Norepinephrine Reuptake Inhibitors (SNRIs)

  • SNRIs inhibit presynaptic reuptake of serotonin and norepinephrine.

Venlafaxine (Effexor®, Effexor XR®)

  • Inhibits presynaptic reuptake of serotonin and norepinephrine.
  • Key side effects are nausea, sexual dysfunction, dose-related increases in blood pressure (especially at higher doses), insomnia, and increased sweating.
  • Should not be taken by individuals with known hypersensitivity; caution in uncontrolled hypertension.
  • Has more of an SSRI effect at lower doses.

Desvenlafaxine – Pristiq®, Khedezla®

  • Inhibits presynaptic reuptake of serotonin and norepinephrine.

Duloxetine – Cymbalta®

  • Inhibits presynaptic reuptake of serotonin and norepinephrine.

Levomilnacipran – Fetzima®

  • Inhibits presynaptic reuptake of serotonin and norepinephrine.

Tricyclic Antidepressants (TCAs)

Tertiary Amines

  • Amitriptyline – Elavil®
  • Clomipramine – Anafranil®
  • Doxepin – Sinequan®, Silenor®
  • Imipramine – Tofranil®, Tofranil-PM®
  • Trimipramine – Surmontil®

Secondary Amines

  • Desipramine – Norpramin®
  • Nortriptyline – Pamelor®
  • Protriptyline – Vivactil®
  • Amoxapine – Asendin® (discontinued)

Tetracyclic (sometimes classed as “heterocyclic”)

  • Maprotiline – Ludiomil®

Monoamine Oxidase Inhibitors (MAOIs)

  • Isocarboxazid – Marplan®
  • Phenelzine – Nardil®
  • Selegiline (transdermal) – Emsam®
  • Tranylcypromine – Parnate®

Other (Atypical) Antidepressants / Miscellaneous

  • Bupropion hydrochloride – Wellbutrin®, Wellbutrin-SR®, Wellbutrin-XL®
  • Bupropion hydrobromide – Aplenzin®
  • Dextromethorphan / Bupropion – Auvelity®
  • Mirtazapine – Remeron®, Remeron SolTab®
  • Vilazodone – Viibryd®
  • Trazodone – Oleptro®, Desyrel®
  • Nefazodone – Serzone® (brand discontinued in many places)
  • Ketamine / Esketamine – Spravato® (esketamine)
  • Brexanolone – Zulresso®
  • Zuranolone – Zurzuvae®
  • Gepirone – Exxua®
  • Note: Some of the brand names may be discontinued or less commonly used in certain regions, but they are listed here as they appear in the document.

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Description

This note discusses Selective Serotonin Reuptake Inhibitors (SSRIs) like Citalopram, Escitalopram, and Fluoxetine. It inhibits presynaptic reuptake of serotonin (5-HT), increasing serotonin levels in the synaptic cleft. The note also outlines key side effects and contraindications for each medication.

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