Anti-Depressants

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Questions and Answers

Which of the following adverse effects is associated with increased serotonin (5-HT) levels in the gut, as seen with SSRI use?

  • Nausea and GI Upset (correct)
  • Hypersomnia
  • Sexual dysfunction
  • Headaches

Orthostatic hypotension is a common side effect associated with which class of antidepressants?

  • 5-HT2 Antagonists
  • SSRIs
  • Monoamine Oxidase Inhibitors (MAOIs) (correct)
  • Tricyclic Antidepressants (TCAs) (correct)

What is the primary mechanism by which TCAs can lead to cardiac toxicity in overdose situations?

  • Blockade of norepinephrine reuptake
  • Inhibition of monoamine oxidase
  • Direct blockade of cardiac sodium channels (correct)
  • Excessive increase in serotonin levels

Which CYP enzyme is potently inhibited by paroxetine and fluoxetine, leading to increased levels of TCAs when used concomitantly?

<p>CYP 2D6 (A)</p> Signup and view all the answers

What potentially fatal syndrome can occur when MAOIs are combined with SSRIs, SNRIs, or most TCAs?

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

Which of the following drugs primarily blocks the re-uptake of serotonin (5-HT) with minimal effect on norepinephrine (NE)?

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

Which of the following medications, once widely used for diabetic peripheral neuropathy, has largely been replaced by other treatments?

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

Which of the following is a common anticholinergic side effect associated with tricyclic antidepressants (TCAs)?

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

Which tetracyclic antidepressant is associated with Parkinsonism due to its D2 receptor-blocking activity?

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

Which mechanism of action is characteristic of second-generation antipsychotics?

<p>Stronger blockade of serotonin (5-HT) receptors compared to dopamine (D2) receptors. (D)</p> Signup and view all the answers

Which dietary component should be avoided by patients taking MAOIs to prevent malignant hypertension?

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

Which drug has variable actions at dopamine (DA), norepinephrine (NE), and serotonin (5-HT) receptors?

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

Why might bupropion be avoided in patients who are currently being treated with MAOIs?

<p>Increased risk of hypertensive crisis (B)</p> Signup and view all the answers

A patient with schizophrenia is prescribed an antipsychotic medication. If the goal is to primarily target dopamine (D2) receptors over serotonin (5-HT) receptors, which of the following medications would be most appropriate?

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

A patient taking fluvoxamine concurrently begins experiencing bradycardia and significant hypotension. Which medication, when combined with fluvoxamine, is most likely the cause?

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

Which medication's primary mechanism involves blocking 5HT2A receptors?

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

A researcher is investigating the effects of various antidepressants on neurotransmitter re-uptake. They discover a novel compound that inhibits both serotonin and norepinephrine transporters with equal potency. Based on this information, which existing class of antidepressants does this new compound most closely resemble?

<p>Serotonin-Norepinephrine Re-uptake Inhibitors (SNRIs) (C)</p> Signup and view all the answers

A patient presents with symptoms of psychosis and is being considered for antipsychotic treatment. Their clinical history reveals a high risk of extrapyramidal symptoms (EPS). Which of the following antipsychotics, known for a lower risk of EPS due to its preferential 5-HT2A receptor antagonism over D2 receptor antagonism, might be the MOST appropriate initial choice?

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

A patient has experienced a depressed mood and loss of interest in activities for the past three weeks, accompanied by changes in sleep and appetite. According to the criteria outlined, which condition is MOST likely?

<p>Major depressive disorder (MDD) (A)</p> Signup and view all the answers

Which of the following best describes the neuropathic hypothesis of major depressive disorder (MDD)?

<p>A deficiency in brain-derived neurotrophic factor (BDNF) impairs neural plasticity and neurogenesis. (B)</p> Signup and view all the answers

Reserpine, a drug known to deplete monoamines, has which effect?

<p>Leads to depression (A)</p> Signup and view all the answers

Dysregulation of the hypothalamic-pituitary-adrenal (HPA) axis, often observed in individuals with major depressive disorder (MDD), typically results in:

<p>Elevated cortisol levels (B)</p> Signup and view all the answers

Which of the following mechanisms of action is NOT typically associated with antidepressant drugs?

<p>Enhancing dopamine synthesis (C)</p> Signup and view all the answers

Which of the following statements accurately describes a key difference between selective serotonin reuptake inhibitors (SSRIs) and tricyclic antidepressants (TCAs)?

<p>SSRIs have a lower risk of lethal toxicity in overdose compared to TCAs. (C)</p> Signup and view all the answers

Which of the following is a potential consequence of combining a selective serotonin reuptake inhibitor (SSRI) with a monoamine oxidase inhibitor (MAOI)?

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

Why are tricyclic antidepressants (TCAs) typically administered at night?

<p>Due to their sedative effects (C)</p> Signup and view all the answers

Which receptor is antagonized by both nefazodone and trazodone?

<p>5HT2A receptor (B)</p> Signup and view all the answers

Bupropion's antidepressant effects are believed to be primarily mediated through which mechanism?

<p>Presynaptic release of catecholamines (B)</p> Signup and view all the answers

What is a primary reason MAOIs are seldom used?

<p>Potential for adverse reactions with certain foods (A)</p> Signup and view all the answers

Which statement accurately describes a key difference between selective serotonin-norepinephrine reuptake inhibitors (SNRIs) and tricyclic antidepressants (TCAs)?

<p>SNRIs are better tolerated because they have no effect on histamine, alpha adrenergic blocking, and antocholinergic effects compared to TCAs. (A)</p> Signup and view all the answers

Amoxapine, a tetracyclic antidepressant, possesses a unique property compared to other antidepressants due to its active metabolite. What is this unique property?

<p>Potent D2 receptor blocker, giving it antipsychotic effects (A)</p> Signup and view all the answers

A patient taking phenelzine needs to be counselled, what food should they avoid?

<p>Foods rich in Tyramine (C)</p> Signup and view all the answers

${5HT_{2A}}$ receptor activation has which effect when bound by LSD?

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

Which of the following best describes the primary mechanism of action of fluoxetine?

<p>Inhibiting serotonin reuptake in the CNS. (B)</p> Signup and view all the answers

What is a significant pharmacokinetic property of fluoxetine that distinguishes it from other SSRIs?

<p>It is biotransformed into norfluoxetine, an active metabolite with a long half-life. (B)</p> Signup and view all the answers

What is a crucial consideration when switching a patient from fluoxetine to another antidepressant that also raises serotonin levels?

<p>Fluoxetine's long half-life necessitates a washout period of several weeks to prevent serotonin syndrome. (B)</p> Signup and view all the answers

How does increased serotonin in the peripheral nervous system (PNS), due to fluoxetine, typically manifest?

<p>Nausea, GI upset, and diarrhea. (D)</p> Signup and view all the answers

Why is combining fluoxetine with a Monoamine Oxidase Inhibitor (MAOI) considered dangerous?

<p>The combination can result in serotonin syndrome. (D)</p> Signup and view all the answers

A patient taking fluoxetine reports a decreased interest in sexual activity. Which of the following is the most likely reason for this side effect?

<p>Increased serotonin levels in the spinal cord. (A)</p> Signup and view all the answers

Fluoxetine inhibits the CYP2D6 enzyme. Which of the following is a potential consequence of this inhibition?

<p>Decreased metabolism and increased plasma levels of drugs metabolized by CYP2D6. (B)</p> Signup and view all the answers

Given its wide therapeutic index, what implications does this have on the safety profile of Fluoxetine?

<p>Fluoxetine has a wide safety range, making overdose difficult. (D)</p> Signup and view all the answers

What are some of the common side effects (ADRs) of fluoxetine?

<p>Nausea (A), Dry mouth (B)</p> Signup and view all the answers

What is Serotonin Syndrome?

<p>A neurological disorder caused by excessive serotonin activity in the brain. (A)</p> Signup and view all the answers

What is the primary difference between Reactive Depression and Endogenous Depression?

<p>Reactive Depression is caused by external factors, while Endogenous Depression has biological causes. (A)</p> Signup and view all the answers

Which of the following hypotheses of depression is described: Loss of 5-HT and/or DA leads to MDD. Reserpine, which depletes monoamines, leads to depression?

<p>Monoamine Hypothesis of MDD (Biogenic Amine Hypothesis) (A)</p> Signup and view all the answers

All available antidepressant drugs affect the:

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

Which of the following drugs inhibit the serotonin transporter (SERT)?

<p>fluoxetine (A), paroxetine (B), fluvoxamine (C)</p> Signup and view all the answers

Which of the following are Selective Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs)?

<p>desvenlafaxine (B), duloxetine (C), venlafaxine (A)</p> Signup and view all the answers

Which of the following are 5-HT2 Antagonists? (Select all that apply)

<p>trazodone (A), nefazodone (B)</p> Signup and view all the answers

Which of the following is described: 1) differs from other SSRIs, 2) metabolized to the active metabolite, norfluoxetine, 3) an SSRI combined with an MAO inhibitor can cause serotonin syndrome?

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

Which of the following Serotonin Norepinephrine Reuptake Inhibitors is described as extensively metabolized in the liver and most tightly bound to protein (albumin)?

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

Which of the following antidepressants is described as dosed once per day, given at night due to sedative effects, and has serum levels useful for predicting toxicity and efficacy?

<p>Tetracyclic and Unicyclic Antidepressants (A)</p> Signup and view all the answers

What are bupropion, mirtazapine, amoxapine, and maprotiline?

<p>Tetracyclic and Unicyclic Antidepressants (B)</p> Signup and view all the answers

Which of the following, at lower doses, is used as a hypnotic for Major Depressive Disorder (MDD)?

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

Which of the following is described by: (a) binding presynaptic autoreceptors and (b) binding specific postsynaptic receptors like 5HT2 antagonists?

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

Which of the following is a 5HT2A agonist?

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

Which of the following are non-selective MAO inhibitors? (Select all that apply)

<p>tranylcypromine (A), phenelzine (B)</p> Signup and view all the answers

Which of the following is described as an irreversible MAO B inhibitor that becomes nonselective at higher doses, and is used in Parkinsonism?

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

Which of the following is used to treat insomnia?

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

A seven day supply of which of the following can be lethal?

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

Levels of which of the following increase when nefazodone inhibits CYP 3A4?

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

Which of the following was the most widely used drug in podiatric medicine to treat diabetic peripheral neuropathy?

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

Most SSRIs are FDA Pregnancy category C.

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

Flashcards

SSRIs

Block re-uptake of serotonin (5HT), with little effect on norepinephrine (NE).

SNRIs

Block re-uptake of both serotonin (5HT) and norepinephrine (NE).

TCAs

Variably block re-uptake of 5HT and/or NE; older class of antidepressants.

5-HT Antagonists

Block 5HT2A serotonin receptors.

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Tetracyclics and Unicyclics

Have variable actions at dopamine (DA), NE and 5HT receptors.

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Psychosis Cause Theory

Elevated levels of certain CNS neurotransmitters (NE, 5HT, DA).

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First Generation Antipsychotics

Stronger block of dopamine (D2) receptors than serotonin (5HT) receptors.

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Second Generation Antipsychotics

Stronger block of serotonin (5HT) receptors than dopamine (D2) receptors.

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SSRI ADR: GI Effects

Increased serotonin levels in the gut, leading to nausea, GI upset, and diarrhea.

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SSRI ADR: Sexual Dysfunction

Decreased libido and other sexual side effects reported by 30-40% of patients.

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TCA ADR: Anticholinergic Effects

Dry mouth, constipation, blurred vision, and confusion commonly caused by TCAs.

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TCA ADR: Orthostatic Hypotension

Drop in blood pressure upon standing, caused by TCAs blocking alpha receptors.

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TCA ADR: Weight Gain & Sedation

Weight gain and sedation resulting from TCAs blocking H1 receptors.

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5-HT2 Antagonist ADRs

Sedation and gastrointestinal disturbances are the most common side effects.

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MAOI ADRs

Weight gain and orthostatic hypotension are the most common adverse drug reactions.

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TCA Overdose Risk

TCAs can cause fatal cardiac toxicity in overdose situations.

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SSRIs as CYP 2D6 Inhibitors

Potent inhibitors of CYP 2D6, leading to increased levels of drugs like TCAs.

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Serotonin Syndrome

Potentially fatal reaction caused by combining MAOIs with SSRIs, SNRIs, TCAs, or meperidine.

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Major Depressive Disorder (MDD)

A mental disorder characterized by a persistent sad mood and loss of interest or pleasure.

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Brain-Derived Neurotrophic Factor (BDNF)

A protein that supports nerve cell survival and growth in the brain.

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Monoamine Hypothesis of MDD

This hypothesis suggests that a deficiency in serotonin (5-HT) and/or dopamine (DA) leads to depression.

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Selective Serotonin Reuptake Inhibitors (SSRIs)

SSRIs work by blocking the reuptake of serotonin, increasing its availability in the synapse.

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Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs)

SNRIs inhibit the reuptake of both serotonin and norepinephrine, increasing their availability in the synapse.

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Tricyclic Antidepressants (TCAs)

Older class of antidepressants that inhibits serotonin and norepinephrine reuptake, but have more side effects.

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Monoamine Oxidase Inhibitors (MAOIs)

A class of antidepressants that blocks monoamine oxidase, preventing the breakdown of monoamines.

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Trazodone

In lower doses it is used as a hypnotic to help with sleep.

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Bupropion

Increases catecholamine release, also used for smoking cessation.

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Mirtazapine

Blocks presynaptic alpha 2 autoreceptors, enhancing NE and 5HT release

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Amoxapine/Maprotiline

Inhibits the reuptake of norepinephrine and serotonin, similar to TCAs.

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Monoamine Oxidase (MAO)

Enzymes that break down monoamines; MAO-A acts on 5-HT, EPI, NE, and DA, while MAO-B acts on DA and some 5-HT.

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Phenelzine/Tranylcypromine

Non-selective MAOIs that inhibit both MAO-A and MAO-B.

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What are SSRIs?

A class of drugs that selectively blocks the reuptake of serotonin in the brain.

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What is Fluoxetine?

An SSRI used to treat depression, anxiety disorders, and other CNS conditions.

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How Fluoxetine Works

It binds to and inhibits SERT, increasing serotonin levels in the synapse.

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Fluoxetine's Mechanism

Raising serotonin levels in the CNS by blocking the serotonin reuptake pump.

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SSRI GI Side Effects

Nausea, GI upset, and diarrhea due to increased serotonin levels in the peripheral nervous system.

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Fluoxetine as CYP2D6 Inhibitor

Inhibits CYP2D6, potentially increasing levels of other drugs.

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What is Serotonin Syndrome?

A potentially fatal condition caused by excessive serotonin activity in the CNS and PNS.

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What is norfluoxetine?

Fluoxetine is metabolized into this active metabolite with a long half-life, potentially leading to accumulation.

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Study Notes

Antipsychotic Drugs

  • The operative theory links schizophrenia, bipolar disorder, and psychosis with elevated CNS neurotransmitters.
  • Reducing the activity of these neurotransmitters is a major goal in drug therapy for these conditions.
  • The neurotransmitters in excess include NE, 5HT, and DA.
  • The drugs used act by attaching to and blocking a specific receptor for one or more of these neurotransmitters.

First Generation Antipsychotics

  • First Generation Antipsychotics have a stronger block of dopamine receptors compared to 5HT (serotonin) receptors, D2 >>5HT.
  • First Generation Antipsychotics include: chlorpromazine, thiothixene, fluphenazine, thioridazine, haloperidol.

Second Generation Antipsychotics

  • Second Generation Antipsychotics exhibit a stronger block of 5HT receptors compared to dopamine receptors, 5HT > D2.
  • Second Generation Antipsychotics include: aripiprazole, lurasidone, ziprasidone, brexpiprazole, olanzapine, cariprazine, quetiapine, clozapine, risperidone.

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