Drugs Used in Mood Disorders

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Questions and Answers

Which neurotransmitter is NOT primarily involved in the pathophysiology of depression?

Serotonin

Norepinephrine

GABA (correct)

Dopamine

Which of the following drugs is NOT typically used to treat bipolar disorder?

Fluoxetine (correct)

Paroxetine (correct)

Lithium

Sertraline (correct)

What is the typical duration before patients can expect clinical improvement from antidepressant therapy?

2-3 months

1-2 days

2-4 weeks (correct)

1-2 weeks

According to DSM-5 criteria, which of the following is NOT considered a core symptom for diagnosing depression?

Increased energy Signup and view all the answers

For a depression diagnosis, what is the minimum number of symptoms that must be present?

5 or more Signup and view all the answers

Which hypothesis posits a deficiency of neurotransmitters as a key factor in depression?

Monoamine hypothesis Signup and view all the answers

Which of the following factors is associated with an increase in brain-derived neurotrophic factor (BDNF) in patients with depression?

Regular physical exercise Signup and view all the answers

According to studies, which hormone is often found to be dysregulated in individuals with depression?

Cortisol Signup and view all the answers

Which symptom in the mnemonic for depression symptoms is represented by the letter 'I'?

Interest loss Signup and view all the answers

What role does serotonin play in brain physiology related to mood and sleep?

Regulates mood and sleep Signup and view all the answers

Which factor is known to NOT contribute to reduced brain-derived neurotrophic factor (BDNF) levels?

Increased norepinephrine Signup and view all the answers

What enzyme is responsible for the degradation of serotonin and norepinephrine in the synaptic cleft?

Monoamine oxidase (MAO) Signup and view all the answers

Which neurotransmitter is primarily associated with cognitive functions like memory and learning?

Norepinephrine Signup and view all the answers

What is the primary effect of antidepressants on brain-derived neurotrophic factor (BDNF) levels?

Increase BDNF levels Signup and view all the answers

Which hormone is typically elevated in depressive disorders according to neuroendocrine theories?

Cortisol Signup and view all the answers

Which symptom related to appetite is indicated in the depression mnemonic?

Appetite changes Signup and view all the answers

What percentage of patients with depression is typically affected by thyroid dysregulation?

25% Signup and view all the answers

Which neuroendocrine factor is believed to influence mood symptoms in postpartum depression?

Estrogen deficiency Signup and view all the answers

Which class of drugs is known to increase serotonin and norepinephrine levels, thus supporting the monoamine hypothesis?

SSRIs and SNRIs Signup and view all the answers

According to the monoamine hypothesis, which neurotransmitter is least likely to be implicated in the condition of depression?

Acetylcholine Signup and view all the answers

What is the primary function of brain-derived neurotrophic factor (BDNF) in the central nervous system?

Promoting neural plasticity and neurogenesis Signup and view all the answers

What relationship between BDNF levels and antidepressant therapy supports the neurotrophic hypothesis?

Increased BDNF levels with antidepressant therapy Signup and view all the answers

Which mechanism is likely responsible for the reduction of BDNF synthesis in the brain?

Glucocorticoid receptor binding Signup and view all the answers

Which of the following drugs is known to block central monoamine activity and could potentially lead to depression in some patients?

Propranolol Signup and view all the answers

Which type of antidepressant is associated with an increased risk of serotonin syndrome when combined with MAO inhibitors?

Selective serotonin reuptake inhibitors (SSRIs) Signup and view all the answers

What class of medications primarily blocks the reuptake of norepinephrine and serotonin?

Serotonin-norepinephrine reuptake inhibitors (SNRIs) Signup and view all the answers

Duloxetine is commonly prescribed for which of the following conditions?

Neuropathic pain Signup and view all the answers

Which side effect occurs frequently with high doses of SNRIs?

Hypertension Signup and view all the answers

Which of the following is NOT associated with serotonin syndrome?

Anticholinergics Signup and view all the answers

What is the primary method through which most antidepressants exert their effects on neurotransmitters?

Increasing the concentration of neurotransmitters in the synaptic cleft Signup and view all the answers

What specific action do selective serotonin reuptake inhibitors (SSRIs) perform within the synaptic cleft?

Block the uptake of serotonin into the presynaptic neuron Signup and view all the answers

Which biological process associated with antidepressant efficacy requires an extended period before improvements are noted?

Synthesis and release of BDNF Signup and view all the answers

What potential risk has been identified by the FDA in patients under 25 using antidepressants?

Elevated risk of suicidality Signup and view all the answers

Which trimester of pregnancy shows a potential correlation with low birth weight and premature delivery due to antidepressant use?

Third trimester Signup and view all the answers

What is the recommended approach for lactating mothers who are prescribed antidepressants?

Continue medication while evaluating risks and benefits Signup and view all the answers

Which transporter is primarily targeted by selective serotonin reuptake inhibitors (SSRIs)?

Serotonin transporter (SERT) Signup and view all the answers

What compounding factor may contribute to delayed antidepressant effects?

Changes in serotonin receptor density Signup and view all the answers

Which of the following neurotransmitter deficiencies is primarily associated with the monoamine hypothesis of depression?

Serotonin, norepinephrine, and dopamine Signup and view all the answers

What impact does reserpine, a drug that depletes monoamines, have on patients?

It has been associated with causing depression Signup and view all the answers

What relationship does glutamate have with depression according to the provided hypotheses?

It is elevated in the cerebrospinal fluid of depressed patients Signup and view all the answers

Which growth factor is shown to have reduced levels in depression according to the neurotrophic hypothesis?

Brain-derived neurotrophic factor (BDNF) Signup and view all the answers

How do antidepressants function in relation to BDNF levels according to the neurotrophic hypothesis?

They enhance BDNF levels, promoting neurogenesis Signup and view all the answers

What distinctive hormonal dysregulation is often found in patients suffering from depression as per the neuroendocrine hypothesis?

Elevated cortisol levels Signup and view all the answers

What evidence suggests a link between serotonin levels and mood disorders?

Deficiency in serotonin has been clinically observed in depression Signup and view all the answers

Which of the following statements about the effects of BDNF in the brain is accurate?

BDNF promotes neurogenesis and synaptic growth Signup and view all the answers

What is the primary purpose of prescribing selective serotonin reuptake inhibitors (SSRIs)?

Major depressive disorder (MDD) Signup and view all the answers

Which SSRI is recognized for its potential to be 'activating' due to its long half-life?

Fluoxetine Signup and view all the answers

Which enzyme system is primarily responsible for the metabolism of SSRIs?

Cytochrome P450 (CYP) enzymes Signup and view all the answers

Why is it advisable to administer SSRIs as a once-daily dosage?

They have long half-lives that allow for once-daily dosing Signup and view all the answers

Which side effect is most commonly associated with increased serotonergic activity when taking SSRIs?

Sexual dysfunction Signup and view all the answers

What is a notable risk associated with the abrupt discontinuation of SSRIs?

Discontinuation syndrome with dizziness and paresthesias Signup and view all the answers

What is a common clinical sign of serotonin syndrome?

Autonomic instability (hyperthermia, hypertension) Signup and view all the answers

Which medication is commonly used to treat serotonin syndrome by blocking serotonin receptors?

Cyproheptadine Signup and view all the answers

Which receptor's antagonism leads to the increase of norepinephrine and serotonin levels by mirtazapine?

Alpha-2 adrenergic receptor Signup and view all the answers

What is a significant side effect of esketamine therapy?

Dissociation Signup and view all the answers

Why should patients on MAOIs avoid certain foods?

To avoid hypertensive crisis Signup and view all the answers

Which neurotransmitter system do NMDA receptor antagonists primarily modulate in relation to depression treatment?

Glutamate Signup and view all the answers

Combining MAOIs with SSRIs can lead to what critical medical condition?

Serotonin syndrome Signup and view all the answers

Which of the following is an expected effect of mirtazapine at lower doses?

Weight gain Signup and view all the answers

Which food category poses a dietary risk for patients taking MAOIs?

Aged cheeses Signup and view all the answers

Which drug is recognized as a treatment option for resistant depression due to its NMDA receptor antagonist properties?

Ketamine Signup and view all the answers

What serious interaction can occur when MAOIs are combined with sympathomimetics?

Hypertensive crisis Signup and view all the answers

What is a primary cause of death in TCA overdose?

Cardiovascular toxicity (arrhythmias) Signup and view all the answers

Which neurotransmitters are primarily blocked by tricyclic antidepressants (TCAs)?

Serotonin and norepinephrine Signup and view all the answers

Which side effect is linked to the anticholinergic properties of TCAs?

Urinary retention Signup and view all the answers

Which TCA is most commonly prescribed for obsessive-compulsive disorder (OCD)?

Clomipramine Signup and view all the answers

What common central nervous system (CNS) side effect is seen with TCAs?

Sedation Signup and view all the answers

Which receptor blockade is primarily responsible for the fall risk associated with TCAs?

Alpha-1 adrenergic receptor blockade Signup and view all the answers

What electrolyte imbalance is frequently found in TCA overdose cases?

Hyponatremia Signup and view all the answers

What is the primary mechanism of action of bupropion (Wellbutrin)?

Norepinephrine and dopamine reuptake inhibitor Signup and view all the answers

In which of the following conditions is bupropion contraindicated?

Seizure disorders Signup and view all the answers

What is a significant risk when combining dextromethorphan with serotonergic medications?

Serotonin syndrome Signup and view all the answers

Which medication is utilized along with dextromethorphan in Auvelity to enhance its antidepressant effects?

Bupropion Signup and view all the answers

What is the primary mechanism of action of trazodone at low doses?

Alpha-1 receptor antagonist and 5-HT2A receptor antagonist Signup and view all the answers

Trazodone is often prescribed at low doses primarily for which condition?

Insomnia Signup and view all the answers

Which of the following is a rare but serious side effect of trazodone requiring immediate medical attention?

Priapism Signup and view all the answers

Which of these conditions is NOT a typical benefit associated with bupropion compared to SSRIs?

Increased serotonin reuptake Signup and view all the answers

Which enzyme is crucial for the metabolism of SNRIs like duloxetine?

Cytochrome P450 1A2 and 2D6 Signup and view all the answers

What adjustment is typically recommended for SNRI dosing in patients with renal insufficiency?

Reduce the dose Signup and view all the answers

Which pharmacokinetic characteristic of SNRIs is linked to potential side effects like hypertension?

Rapid metabolism through the kidneys Signup and view all the answers

What is a notable cardiovascular effect that can occur with high doses of SNRIs?

Hypertension Signup and view all the answers

Which symptom is associated with the discontinuation syndrome of SNRIs?

Dizziness and somnolence Signup and view all the answers

What is a significant risk factor for increased TCA toxicity related to metabolism?

Genetic variations in drug metabolism Signup and view all the answers

Which of the following is a potential pharmacological action of clomipramine aside from treating OCD?

Inhibiting norepinephrine reuptake Signup and view all the answers

Which characteristic makes MAOIs particularly significant in dietary restrictions?

Inhibition of tyramine breakdown Signup and view all the answers

In TCA overdose, which of the following symptoms is most likely to precede cardiac complications?

Dilated pupils Signup and view all the answers

What is a primary reason for the recommendation to administer TCAs at night?

To minimize CNS stimulation throughout the day Signup and view all the answers

Which finding is typically observed in the EKG of a patient who has overdosed on a TCA?

Wide QRS complex Signup and view all the answers

What is a key consideration when treating TCA-induced arrhythmias?

Avoiding Class I antiarrhythmic drugs Signup and view all the answers

In patients over 65 years old, which risk associated with TCAs is most concerning?

Increased susceptibility to falls Signup and view all the answers

What life-threatening condition is associated with the sudden discontinuation of MAOIs?

Discontinuation syndrome with psychosis and confusion Signup and view all the answers

What is the primary reason MAOIs are not often used as first-line therapy for depression?

High risk of drug and food interactions Signup and view all the answers

Which type of foods are contraindicated for patients taking MAOIs due to the risk of hypertensive crisis?

Tyramine-rich foods Signup and view all the answers

Bupropion is primarily effective in inhibiting the reuptake of which neurotransmitters?

Norepinephrine and dopamine Signup and view all the answers

What serious risk is associated with combining MAOIs and SSRIs?

Serotonin syndrome Signup and view all the answers

What common side effect can result from the use of MAOIs?

Weight gain Signup and view all the answers

Which medication should be avoided when a patient is on MAOIs due to possible hypertensive crisis?

Pseudoephedrine Signup and view all the answers

Bupropion is particularly chosen over SSRIs for certain patients because of its?

Lower risk of sexual side effects Signup and view all the answers

What is the main therapeutic use of Duloxetine (Cymbalta)?

For both depression and neuropathic pain Signup and view all the answers

What is the primary risk associated with combining SNRIs with MAOIs?

Risk of serotonin syndrome Signup and view all the answers

Which of the following enzymes is primarily involved in the metabolism of SNRIs?

Cytochrome P450 Signup and view all the answers

Which side effect is characterized by an increase in blood pressure and is typically seen in SNRIs?

Hypertension Signup and view all the answers

For a patient with renal insufficiency, how should the dose of SNRIs be managed?

Reduce the dose Signup and view all the answers

Which SNRI is utilized for treating social anxiety disorder in addition to its use for depression?

Venlafaxine (Effexor) Signup and view all the answers

Which symptom is a common side effect seen with both SSRIs and SNRIs?

Increased sweating Signup and view all the answers

What is a notable dose-dependent side effect of SNRIs?

Hypertension Signup and view all the answers

What is the primary mechanism of action of mirtazapine?

Alpha-2 receptor antagonist Signup and view all the answers

Which side effect is most commonly reported with the use of vortioxetine?

Headache Signup and view all the answers

Compared to SSRIs, mirtazapine is less likely to cause which side effect?

Sexual dysfunction Signup and view all the answers

What transporter does vortioxetine primarily inhibit in treating depression?

SERT (Serotonin transporter) Signup and view all the answers

Which receptor does vortioxetine partially act upon as an agonist?

5-HT1A Signup and view all the answers

What is the primary function of bupropion compared to SSRIs?

Lower risk of sexual side effects Signup and view all the answers

Dextromethorphan in Auvelity primarily acts as an antagonist of which receptor?

NMDA receptor Signup and view all the answers

What serious risk is associated with combining dextromethorphan with other serotonergic medications?

Serotonin syndrome Signup and view all the answers

What is the primary intended use of trazodone at low doses?

Treatment of insomnia Signup and view all the answers

Which receptor's blockade is linked to the sedative effects of trazodone?

Histamine H1 receptor Signup and view all the answers

Why has nefazodone fallen out of common use?

Potential for hepatotoxicity Signup and view all the answers

Nefazodone's antidepressant effects are mainly attributed to its blockade of which receptor?

5-HT2A receptor Signup and view all the answers

What unique side effect is associated with trazodone usage?

Priapism Signup and view all the answers

What specific neurotransmitter breakdown is primarily inhibited by MAO-A?

Serotonin, norepinephrine, and dopamine Signup and view all the answers

Which dietary component should be strictly avoided to prevent dangerous interactions while on MAOIs?

Tyramine-rich foods Signup and view all the answers

What mechanism does bupropion use to influence neurotransmitter levels in the brain?

Inhibits norepinephrine and dopamine reuptake Signup and view all the answers

Which of the following side effects is commonly experienced by patients on MAOIs?

Orthostatic hypotension Signup and view all the answers

What is a potential consequence of abruptly discontinuing MAOIs?

Psychosis, excitement, and confusion Signup and view all the answers

In which condition is bupropion contraindicated due to heightened risk?

History of seizure disorder Signup and view all the answers

Which side effect is noted for having the highest incidence among MAOI users?

Sexual dysfunction Signup and view all the answers

Which outcome reflects a significant risk for patients on MAOIs if they consume certain foods?

Hypertensive crisis Signup and view all the answers

What serious risk is associated with nefazodone that limits its clinical use?

Hepatotoxicity Signup and view all the answers

Which enzyme does nefazodone inhibit, contributing to potential drug interactions?

CYP3A4 Signup and view all the answers

What mechanism of action does mirtazapine utilize?

Alpha-2 adrenergic receptor antagonist Signup and view all the answers

What is the primary enzyme responsible for the metabolism of bupropion?

CYP2D6 Signup and view all the answers

Bupropion is contraindicated in patients with a history of which condition?

Seizure disorder Signup and view all the answers

Mirtazapine is less likely to cause which adverse effect compared to serotonin reuptake inhibitors?

Sexual dysfunction Signup and view all the answers

What mechanism of action does dextromethorphan exhibit in Auvelity?

NMDA receptor antagonist Signup and view all the answers

What is the primary action of vortioxetine in the treatment of depression?

Inhibition of the serotonin transporter (SERT) Signup and view all the answers

Which receptor does vortioxetine partially agonize?

5-HT1A Signup and view all the answers

What is a potential adverse reaction when combining dextromethorphan with other serotonergic medications?

Serotonin syndrome Signup and view all the answers

Which significant adverse effect is associated with vilazodone that necessitates monitoring?

Long QT syndrome Signup and view all the answers

What receptor does trazodone antagonize that contributes to its sedative effects?

Histamine H1 receptor Signup and view all the answers

Vilazodone enhances serotonergic activity by inhibiting which specific transporter?

Serotonin transporter (SERT) Signup and view all the answers

What is a rare but serious side effect associated with trazodone?

Priapism Signup and view all the answers

Nefazodone is chemically related to which other antidepressant?

Trazodone Signup and view all the answers

How soon can symptom improvement begin after starting Auvelity for depression?

1 week Signup and view all the answers

What is the primary mechanism of action of NMDA receptor antagonists like ketamine in treating depression?

NMDA receptor antagonism Signup and view all the answers

Esketamine (Spravato) is specifically indicated for what condition?

Treatment-resistant depression and acute suicidal ideation Signup and view all the answers

Which concern is significant regarding the use of ketamine for depression treatment?

Risk of dissociative symptoms and abuse potential Signup and view all the answers

Which antidepressant class is the first-line choice for major depressive disorder (MDD)?

Selective serotonin reuptake inhibitors (SSRIs) Signup and view all the answers

What is a critical aspect to consider while selecting an antidepressant for a patient?

Indication, cost, availability, adverse effects, drug interactions, and history of response Signup and view all the answers

What is the objective of acute treatment using antidepressants for depression?

Achieve full remission of depressive symptoms Signup and view all the answers

Which antidepressant is least likely to cause sexual side effects?

Bupropion Signup and view all the answers

What should be prioritized when choosing an antidepressant?

Patient's prior treatment history and response Signup and view all the answers

What is the recommended duration for a trial of antidepressant therapy to determine efficacy?

8-12 weeks Signup and view all the answers

What approach is recommended for patients with two or more serious episodes of major depressive disorder in the last 5 years?

Long-term antidepressant therapy Signup and view all the answers

Which antidepressant class has the highest risk associated with fatal overdose?

Tricyclic antidepressants (TCAs) Signup and view all the answers

What common symptom indicates antidepressant discontinuation syndrome?

Dizziness and paresthesias Signup and view all the answers

Which type of antidepressants is likely to cause severe withdrawal symptoms if discontinued abruptly?

Short half-life SSRIs (e.g., paroxetine, sertraline) Signup and view all the answers

What impact do paroxetine and fluoxetine have on the cytochrome P450 (CYP) enzyme system?

They are potent CYP2D6 inhibitors Signup and view all the answers

Which antidepressants are considered relatively free from significant drug interactions?

Citalopram and sertraline Signup and view all the answers

What is contraindicated with SSRIs due to the risk of serotonin syndrome?

MAOIs Signup and view all the answers

Which of the following pairs of medications are relatively free from significant drug interactions?

Citalopram and sertraline Signup and view all the answers

What serious contraindication must be considered when using SSRIs due to the risk of serotonin syndrome?

Use with MAOIs Signup and view all the answers

Which of the following symptoms is a hallmark of serotonin syndrome?

Hyperthermia, autonomic instability, and neuromuscular abnormalities Signup and view all the answers

Which medication is primarily used to treat serotonin syndrome by blocking serotonin receptors?

Cyproheptadine Signup and view all the answers

Which class of drugs is most frequently associated with the development of serotonin syndrome?

Antidepressants (SSRIs, SNRIs) Signup and view all the answers

What factors should be considered when selecting an antidepressant for a patient?

Indication, cost, availability, adverse effects, drug interactions, and history of response Signup and view all the answers

Which class of antidepressants is primarily associated with a higher incidence of sexual side effects?

Selective serotonin reuptake inhibitors (SSRIs) Signup and view all the answers

What is the main objective of acute treatment with antidepressants for patients experiencing depression?

Achieve full remission of depressive symptoms Signup and view all the answers

What is the duration typically expected before patients experience maximum benefits from antidepressants?

1-2 months Signup and view all the answers

For patients with a history of two or more serious episodes of major depressive disorder (MDD) in the last 5 years, what is the recommended course of action?

Long-term antidepressant therapy Signup and view all the answers

Which antidepressants are identified as potent inhibitors of CYP2D6 and are thus associated with significant drug interactions?

Paroxetine and fluoxetine Signup and view all the answers

Which antidepressants are commonly prescribed for managing both major depressive disorder (MDD) and anxiety disorders?

Selective serotonin reuptake inhibitors (SSRIs) Signup and view all the answers

What is commonly regarded as the initial goal when treating depression with antidepressants?

Achieve full remission of depressive symptoms Signup and view all the answers

Study Notes

Overview of Drugs Used in Mood Disorders

Key neurotransmitters in depression include serotonin, norepinephrine, and dopamine.
Lithium is indicated for the treatment of bipolar disorder.
Antidepressants typically show clinical improvement in 2-4 weeks.

Depression - DSM-5 Criteria

A diagnosis of depression requires at least 5 symptoms.
Depressed mood is one of the two mandatory symptoms for depression diagnosis.
Weight gain due to a medical condition should not be included when diagnosing depression.

Pathophysiology of Depression

The monoamine hypothesis links depression to deficiencies in serotonin, norepinephrine, and dopamine.
Glucocorticoid receptor binding is associated with decreased brain-derived neurotrophic factor (BDNF) in depression.
Cortisol dysregulation is commonly observed in depressed patients.

Depression Symptom Mnemonic

"I" in the mnemonic stands for interest loss.
"S" represents sleep disturbance within the mnemonic for depression symptoms.
Appetite changes in the mnemonic indicate potential weight fluctuations.

Normal Brain Physiology

Serotonin regulates mood, appetite, and sleep.
Monoamine oxidase (MAO) degrades serotonin and norepinephrine in the synaptic cleft.
Norepinephrine is crucial for mood regulation and cognitive functions such as memory and learning.

Neurotrophic Hypothesis

Brain-derived neurotrophic factor (BDNF) is vital for neural plasticity and resilience.
Antidepressants are known to increase BDNF levels.
Increased norepinephrine is not typically associated with reduced BDNF levels in depression.

Neuroendocrine Hypothesis

Elevated cortisol levels are commonly seen in depressed patients.
Thyroid dysregulation affects approximately 25% of patients with depression.
Estrogen deficiency may contribute to mood symptoms in postpartum depression.

Monoamine Hypothesis

SSRIs and SNRIs increase levels of serotonin and norepinephrine, supporting the monoamine hypothesis.
Acetylcholine is not typically implicated in depression according to this hypothesis.
Propranolol, a drug that blocks central monoamine activity, can potentially cause depression.

Neurotrophic Hypothesis (Continued)

BDNF promotes neural plasticity and neurogenesis in the brain.
Increased BDNF levels following antidepressant therapy support the neurotrophic hypothesis in depression.
Glucocorticoid receptor binding is associated with reduced BDNF synthesis in the brain.

Mechanism of Antidepressants

Most antidepressants alleviate depression symptoms by enhancing neurotransmitter levels in the brain (details on mechanism were not provided in the text).

Monoamine Hypothesis

Depression is linked to a deficiency of serotonin, norepinephrine, and dopamine.
Evidence: Reserpine, known to deplete monoamines, can induce depression in some individuals.
Glutamate levels are elevated in the cerebrospinal fluid of depressed patients.

Neurotrophic Hypothesis

Depression correlates with reduced levels of Brain-Derived Neurotrophic Factor (BDNF).
Antidepressants increase BDNF levels, facilitating neurogenesis.
Patients with depression often exhibit elevated cortisol levels, indicating hormonal dysregulation.

Antidepressant Mechanisms

Most antidepressants work by increasing serotonin and norepinephrine concentrations in the synaptic cleft.
Selective serotonin reuptake inhibitors (SSRIs) relieve depression symptoms by blocking serotonin reuptake into presynaptic neurons.
Antidepressants typically require several weeks for clinical effects due to the time needed for BDNF synthesis.

FDA Warning on Antidepressants

Patients under 25 face an increased risk of suicidality when using antidepressants.
Antidepressant use during the third trimester of pregnancy is associated with low birth weight and premature delivery.
In lactating mothers, weighing risks and benefits of continuing medication is recommended.

Selective Serotonin Reuptake Inhibitors (SSRIs)

SSRIs primarily target the serotonin transporter (SERT).
They are primarily prescribed for Major Depressive Disorder (MDD).
Fluoxetine is notable for its long half-life and potential activating effects.

SSRI Pharmacokinetics

Fluoxetine has the longest half-life among SSRIs, allowing for once-daily dosing.
SSRIs are predominantly metabolized by Cytochrome P450 (CYP) enzymes.
Their long half-lives permit less frequent dosing.

SSRI Side Effects

The most prevalent side effect of SSRIs is sexual dysfunction due to increased serotonergic activity.
Paroxetine is associated with a higher risk of weight gain compared to other SSRIs.
Abrupt discontinuation can result in dizziness and paresthesias, termed discontinuation syndrome.

Serotonin Syndrome

A common sign of serotonin syndrome includes autonomic instability, characterized by hyperthermia and hypertension.
Cyproheptadine is used to treat serotonin syndrome by blocking serotonin receptors.
Anticholinergics are not typical causes of serotonin syndrome, which is primarily caused by SSRIs, SNRIs, and MAO inhibitors.

SNRI Mechanism and Indications

SNRIs inhibit the reuptake of serotonin and norepinephrine.
In addition to depression, SNRIs are effective in treating neuropathic pain.
Duloxetine is frequently prescribed for generalized anxiety disorder (GAD) and chronic pain conditions like fibromyalgia.

SNRI Side Effects

Hypertension is the most common side effect associated with SNRIs, especially at high doses.
Nausea and vomiting are common gastrointestinal side effects linked to SNRIs.
Combining SNRIs with monoamine oxidase inhibitors (MAOIs) should be avoided due to the increased risk of serotonin syndrome.

Bupropion (Wellbutrin)

Mechanism of action: Norepinephrine and dopamine reuptake inhibitor.
Contraindicated in seizure disorders.
Benefits over SSRIs include a lower risk of sexual side effects.

Dextromethorphan/Bupropion ER (Auvelity)

Dextromethorphan acts as an NMDA receptor antagonist.
Combined with bupropion for enhanced antidepressant effects.
Significant risk when combined with serotonergic medications: Serotonin syndrome.

Trazodone (Desyrel)

Low-dose mechanism of action: Alpha-1 and 5-HT2A receptor antagonist.
Commonly used to treat insomnia.
Rare but serious side effect: Priapism.

Mirtazapine (Remeron)

Antagonizes alpha-2 adrenergic receptor, increasing norepinephrine and serotonin levels.
Common side effect, especially at lower doses: Weight gain.
Less likely to cause sexual dysfunction compared to SSRIs.

NMDA Receptor Antagonists

Ketamine approved for treatment-resistant depression.
Common side effect of esketamine (Spravato): Dissociation.
Effectiveness linked to modulation of the glutamate neurotransmitter system.

Monoamine Oxidase Inhibitors (MAOIs)

Function by inhibiting the enzyme that breaks down norepinephrine, dopamine, and serotonin.
Foods to avoid: Cheese.
Risk of life-threatening condition (serotonin syndrome) when combined with SSRIs.

MAOI Side Effects and Interactions

Common side effect: Orthostatic hypotension.
Should not be combined with SSRIs due to risk of hypertensive crisis.
Serious interaction when combined with sympathomimetics: Hypertensive crisis.

Tricyclic Antidepressants (TCAs)

Block reuptake of serotonin and norepinephrine.
Serious side effect of overdose: QT prolongation and cardiac arrhythmias.
Clomipramine is commonly prescribed for obsessive-compulsive disorder (OCD).

TCA Side Effects

Anticholinergic properties lead to urinary retention.
Common CNS side effect: Sedation.
Fall risk associated with alpha-1 adrenergic receptor blockade.

TCA Overdose

Primary cause of death: Cardiovascular toxicity (arrhythmias).
Electrolyte imbalance commonly associated: Hyponatremia.

SNRI Overview

SNRIs (Serotonin-Norepinephrine Reuptake Inhibitors) primarily inhibit the reuptake of serotonin and norepinephrine.
Duloxetine (Cymbalta) is indicated for both depression and neuropathic pain.

Additional Uses

Venlafaxine is also used for social anxiety disorder alongside its primary use for depression.

Pharmacokinetics of SNRIs

SNRIs are metabolized by the Cytochrome P450 enzyme system.
Dose reduction is required for patients with renal insufficiency.
Hypertension is a common side effect of SNRIs.

SNRI Side Effects

Hypertension is dose-dependent.
Increased sweating is a side effect commonly associated with both SSRIs and SNRIs.
Combining SNRIs with MAOIs poses a risk of serotonin syndrome.

Tricyclic Antidepressants (TCAs) Overview

TCAs also inhibit serotonin and norepinephrine reuptake.
Clomipramine is the TCA commonly used to treat obsessive-compulsive disorder (OCD).
QT prolongation is a notable adverse effect of TCAs.

TCA Pharmacokinetics

TCAs are also metabolized by the Cytochrome P450 system.
They induce sedation, which is why they are typically administered at night.
Elderly patients are particularly at risk due to slow metabolism.

TCA Overdose

Cardiotoxicity (arrhythmias) is the primary cause of death in TCA overdose.
Hyponatremia is a common electrolyte abnormality seen in overdose situations.
Class I antiarrhythmic drugs are contraindicated in treating TCA-induced arrhythmias.

Monoamine Oxidase Inhibitors (MAOIs) Overview

MAOIs work by inhibiting monoamine oxidase, thus preventing neurotransmitter breakdown.
MAO-A primarily degrades serotonin and norepinephrine.
Foods high in tyramine, like cheese, should be avoided due to hypertension risk.

MAOI Drug Interactions

Combining MAOIs with SSRIs can lead to serotonin syndrome.
Pseudoephedrine should be avoided with MAOIs because of the risk of hypertensive crisis.

MAOI Side Effects

Weight gain is one of the common side effects of MAOIs.
Sudden discontinuation can lead to a complicating condition characterized by psychosis and confusion.
High risk of drug and food interactions makes MAOIs less common as first-line therapy for depression.

Bupropion (Wellbutrin) Overview

Bupropion primarily inhibits the reuptake of norepinephrine and dopamine.
It is contraindicated in patients with a seizure disorder.
Patients often prefer bupropion due to its lower risk of sexual side effects compared to SSRIs.

Monoamine Oxidase Inhibitors (MAOIs)

MAOIs function by inhibiting the monoamine oxidase enzyme, preventing the breakdown of neurotransmitters.
Patients on MAOIs must avoid tyramine-rich foods, such as cheese and red wine, to prevent hypertensive crises.
MAO-A isoform is responsible for degrading serotonin, norepinephrine, and dopamine.

MAOI Side Effects

The most commonly associated side effect of MAOIs is orthostatic hypotension.
MAOIs have the highest rate of sexual dysfunction as a side effect.
Discontinuation syndrome may occur with symptoms like psychosis, excitement, and confusion following sudden cessation of MAOIs.

Bupropion (Wellbutrin)

Bupropion acts primarily as a norepinephrine and dopamine reuptake inhibitor.
It should be avoided in patients with a history of seizure disorder due to an increased risk of seizures.
An advantage of bupropion compared to SSRIs is its lower risk of sexual side effects.

Dextromethorphan/Bupropion ER (Auvelity)

Dextromethorphan acts as an NMDA receptor antagonist in Auvelity.
Bupropion is combined with dextromethorphan to enhance antidepressant effects.
Combining dextromethorphan with other serotonergic medications can lead to serotonin syndrome.

Trazodone (Desyrel)

Trazodone is primarily used for insomnia treatment at low doses (25-150 mg).
Its sedative effects are attributed to the blockade of the histamine H1 receptor.
A rare but serious side effect of trazodone is priapism.

Nefazodone

Nefazodone blocks the 5-HT2A receptor, contributing to its antidepressant effects.
It is chemically related to trazodone.
Nefazodone is less commonly prescribed due to risks of hepatotoxicity.

Mirtazapine (Remeron)

Mirtazapine functions as an alpha-2 receptor antagonist.
A common side effect of mirtazapine is weight gain.
Compared to SSRIs, mirtazapine is less likely to cause sexual dysfunction.

Vortioxetine (Trintellix)

Vortioxetine partially agonizes the 5-HT1A receptor.
A common side effect associated with vortioxetine use is headache.
Vortioxetine primarily inhibits the serotonin transporter (SERT) in treating depression.

Bupropion Pharmacokinetics

Primary enzyme for bupropion metabolism is CYP2D6.
Contraindicated in patients with a history of seizure disorder.
Approved for smoking cessation in addition to depression treatment.

Dextromethorphan/Bupropion ER (Auvelity)

Dextromethorphan acts as an NMDA receptor antagonist.
Combining dextromethorphan with serotonergic medications can cause serotonin syndrome.
Symptom improvement can start as early as 1 week after beginning Auvelity for depression.

Trazodone (Desyrel)

Antagonizes the histamine H1 receptor, contributing to its sedative effects.
Commonly used at low doses to treat insomnia.
Rare but serious side effect includes priapism.

Nefazodone

Chemically related to trazodone.
Serious risk of hepatotoxicity limits nefazodone's use.
Inhibits CYP3A4 enzyme, leading to significant drug interactions.

Mirtazapine (Remeron)

Mechanism of action involves alpha-2 adrenergic receptor antagonism.
Common side effect is weight gain.
Less likely to cause sexual dysfunction compared to SSRIs.

Vortioxetine (Trintellix)

Primary mechanism of action is inhibition of the serotonin transporter (SERT).
Partially agonizes the 5-HT1A receptor.
Common side effect includes nausea.

Vilazodone (Viibryd)

Acts as a partial agonist at the 5-HT1A receptor.
Significant adverse effect requiring monitoring is long QT syndrome.
Enhances serotonergic activity by inhibiting the serotonin transporter (SERT).

NMDA Receptor Antagonists

NMDA receptor antagonists, such as ketamine, primarily function by blocking NMDA receptors.
Esketamine (Spravato) is specifically indicated for treatment-resistant depression and acute suicidal ideation.
A significant concern with ketamine treatment is the risk of dissociative symptoms and potential for abuse.

How to Choose an Antidepressant

Bupropion is an antidepressant least likely to cause sexual side effects.
Key considerations for selecting an antidepressant include indication, cost, availability, adverse effects, drug interactions, and patient history of response.
Selective serotonin reuptake inhibitors (SSRIs) are the most commonly prescribed for major depressive disorder (MDD) and anxiety disorders.

Clinical Indications for Antidepressants

The main goal of acute antidepressant treatment is to achieve full remission of depressive symptoms.
A trial of antidepressant therapy should last 8-12 weeks to accurately determine efficacy.
For patients with two or more serious episodes of MDD in the past five years, long-term antidepressant therapy is recommended.

Antidepressant Side Effects and Discontinuation

Tricyclic antidepressants (TCAs) carry the highest risk of fatal overdose among antidepressant classes.
Common symptoms of antidepressant discontinuation syndrome include dizziness and paresthesias.
Short half-life SSRIs, like paroxetine and sertraline, are most likely to cause severe withdrawal symptoms if stopped abruptly.

Antidepressant Drug Interactions

Paroxetine and fluoxetine are potent inhibitors of the CYP2D6 enzyme, impacting drug metabolism.
Citalopram and sertraline are relatively free from significant drug interactions compared to others.
MAOIs are contraindicated with SSRIs due to the risk of serotonin syndrome, a potentially life-threatening condition.

Serotonin Syndrome

Key signs of serotonin syndrome include altered mental status, autonomic instability, and neuromuscular abnormalities.

Antidepressant Selection and Considerations

Selecting an antidepressant involves multiple factors: indication, cost, availability, side effects, drug interactions, and prior response history.
Bupropion, mirtazapine, and nefazodone are associated with the lowest sexual side effects.
Selective serotonin reuptake inhibitors (SSRIs) are the most commonly prescribed for major depressive disorder (MDD) and anxiety disorders.

Clinical Indications for Antidepressants

The primary goal of acute treatment is to achieve full remission of depressive symptoms.
Maximum benefits from antidepressants can typically be observed in 1-2 months.
Patients with multiple severe depressive episodes within 5 years should consider long-term antidepressant therapy.

Antidepressant Drug Interactions

Paroxetine and fluoxetine are potent inhibitors of CYP2D6, contributing to significant drug interactions.
Citalopram and sertraline generally have fewer notable drug interactions.
Concurrent use of SSRIs and monoamine oxidase inhibitors (MAOIs) can lead to serious contraindications due to the risk of serotonin syndrome.

Serotonin Syndrome

Hallmark signs of serotonin syndrome include hyperthermia, autonomic instability, and neuromuscular abnormalities.
Cyproheptadine is commonly used to treat serotonin syndrome by blocking serotonin receptors.
Antidepressants, particularly SSRIs and SNRIs, are the drug class most often linked to causing serotonin syndrome.

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This quiz focuses on the various drugs used in the treatment of mood disorders, specifically targeting their mechanisms and interactions with neurotransmitters. Test your knowledge on the pharmacological agents involved in conditions such as depression and bipolar disorder. Perfect for students and professionals in psychology and psychiatry.