SSRI Pharmacology Quiz

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Questions and Answers

Which of the following SSRIs has the longest half-life?

Paroxetine

Sertraline

Escitalopram

Fluoxetine (correct)

Which of the following statements is FALSE regarding SSRI absorption?

They are poorly absorbed after oral administration (correct)

They are generally well absorbed after oral administration

Food may slightly enhance absorption

Peak effects range from 3 to 8 hours after administration

Which SSRI has the highest potential for slowing or blocking the metabolism of other drugs?

Paroxetine

Fluoxetine

Sertraline

Fluvoxamine (correct)

What is the primary mechanism of action through which SSRIs exert their therapeutic effect?

Serotonin reuptake inhibition Signup and view all the answers

According to the content, which of the following is a potential risk associated with paroxetine use during the first trimester of pregnancy?

Major congenital malformations, particularly heart defects Signup and view all the answers

Which of the following is NOT a common side effect associated with SSRI use?

Weight loss Signup and view all the answers

Which SSRI is most associated with weight gain?

Paroxetine Signup and view all the answers

What is a potential cardiovascular effect associated with all SSRIs?

Lengthened QT interval Signup and view all the answers

According to the content, what is the maximum recommended daily dose of citalopram for an elderly patient?

20 mg Signup and view all the answers

Which SSRI is most likely to cause headaches as a side effect?

Fluoxetine Signup and view all the answers

What is the primary effect of SSRIs on sleep patterns?

Improved sleep quality as a result of treating depression and anxiety Signup and view all the answers

What hematologic adverse effect is associated with SSRI use?

Functional impairment of platelet aggregation Signup and view all the answers

What is a key symptom of Serotonin Syndrome?

Myoclonus Signup and view all the answers

Which of the following best describes the relationship between SSRI dosage and antidepressant efficacy?

Antidepressant efficacy does not differ with higher dosages, but risk of adverse effects may increase Signup and view all the answers

What is the primary reason SSRIs are often preferred over MAOIs and benzodiazepines for treating social anxiety disorder?

They are generally safer to use Signup and view all the answers

Which of the following is NOT a symptom of serotonin syndrome?

Hyporeflexia Signup and view all the answers

Which SSRI is least likely to be associated with withdrawal syndrome?

Fluoxetine Signup and view all the answers

Which SSRI is metabolized by CYP3A4 and should be avoided with ketoconazole?

Fluvoxamine Signup and view all the answers

Which of the following laboratory test interferences is associated with bupropion?

False-positive result on urinary amphetamine screens Signup and view all the answers

What is a common clinical strategy to minimize the GI side effects associated with sertraline?

Start at 25 mg/day and increase to 50 mg/day after 3 weeks Signup and view all the answers

Which antidepressant is contraindicated with MAOIs due to the risk of hypertensive crisis?

Bupropion Signup and view all the answers

Which of these medications, when combined with paroxetine, has an increased risk of precipitating serotonin syndrome in the elderly?

Tramadol Signup and view all the answers

Which of the following best describes the mechanism of action of mirtazapine?

Blocks presynaptic alpha-2 adrenergic receptors and postsynaptic serotonin receptors Signup and view all the answers

For which condition is the extended-release formulation of venlafaxine approved?

Generalized anxiety disoder Signup and view all the answers

Which medication's dose should be reduced to 20 mg when given with potent CYP3A4 inhibitors?

Vilazodone Signup and view all the answers

What is a potential remedy for loss of efficacy of SSRIs while on full dose of medication?

Tapering drug use and rechallenging with the same medication Signup and view all the answers

Which of the following best summarizes the interaction between SSRIs and warfarin?

SSRIs may increase the anticoagulant effect of warfarin or increase the prothrombin time. Signup and view all the answers

Which of the following is approved for use in fibromyalgia?

Milnacipran Signup and view all the answers

Which of the following statements best describes the use of bupropion in bipolar disorder?

Bupropion is less likely to induce mania in persons with bipolar 1 disorder compared with TCAs. Signup and view all the answers

What is the recommended starting dose of vortioxetine for patients who are known to be poor metabolizers of CYP2D6?

10mg/day Signup and view all the answers

Which tricyclic antidepressant (TCA) is associated with the lowest risk of causing orthostatic hypotension?

Nortriptyline Signup and view all the answers

A patient taking a TCA is scheduled for elective surgery. When should the TCA be discontinued to minimize the risk of hypertensive episodes during the procedure?

Several days before surgery Signup and view all the answers

Which of the following is NOT considered a common autonomic side effect of tricyclic antidepressants?

Hypertensive crisis Signup and view all the answers

Which of the following TCAs has a higher risk of causing parkinsonian symptoms due to its dopaminergic blocking activity?

Amoxapine Signup and view all the answers

Which of the following is a rare but potentially life-threatening hepatic side effect associated with tricyclic antidepressants?

Fulminant acute hepatitis Signup and view all the answers

What is a common symptom of neonatal withdrawal syndrome that may occur in infants whose mothers used tricyclic antidepressants during pregnancy?

Tachypnea Signup and view all the answers

What is the typical initial dosage range for Liothyronine when added to antidepressants?

25–50 µg/day Signup and view all the answers

Which of the following is a primary mechanism of action of Monoamine oxidase inhibitors (MAOIs)?

Inhibiting the degradation of neurotransmitters Signup and view all the answers

Which of the following adverse effects is considered common at the prescribed dosage of Liothyronine?

Diarrhea Signup and view all the answers

A patient on an MAOI presents with a severe headache, stiff neck, and diaphoresis after consuming aged cheese. What is the most likely cause?

Tyramine-induced hypertensive crisis Signup and view all the answers

Which patient condition is a contraindication for the use of Liothyronine?

Cardiac disease Signup and view all the answers

Which of the following is the most appropriate daily starting dose for phenelzine?

15mg Signup and view all the answers

What is the expected response when a patient undergoes a TRH Stimulation Test for subclinical hypothyroidism?

TSH increase of 5–25 mIU/mL Signup and view all the answers

Why should MAOIs be used with caution in patients taking SSRIs, lithium, or tryptophan?

Due to the risk of serotonin syndrome Signup and view all the answers

Which of the following statements is true regarding the interaction of SSRIs and Liothyronine?

SSRIs mildly alter thyroid function Signup and view all the answers

What is a common early sign of MAOI overdose?

Agitation Signup and view all the answers

Transdermal selegiline at low doses selectively inhibits which enzyme?

MAOB Signup and view all the answers

Which of the following best describes the mechanism of action of T3 in the brain?

Binding to intracellular receptors to influence gene transcription Signup and view all the answers

Thyroid hormones are used primarily as augmentation therapy for?

Patients who have not responded to other antidepressants Signup and view all the answers

What is the primary mechanism by which T4 influences brain function?

Is converted into T3 inside neurons Signup and view all the answers

Which of the following is a known active metabolite of nefazodone?

mCPP Signup and view all the answers

What is a primary mechanism through which Trazodone works?

Potent antagonism of 5-HT2A/5-HT2C receptors Signup and view all the answers

Which of the following is a therapeutic advantage of nefazodone over SSRIs?

Improved REM sleep and sleep continuity Signup and view all the answers

What is a significant risk associated with Trazodone, particularly concerning male patients?

Priapism Signup and view all the answers

Which of the following is NOT a common side effect associated with Tricyclic Antidepressants (TCAs)?

Weight gain Signup and view all the answers

What is a specific clinical application of Clomipramine among the Tricyclic Antidepressants (TCAs)?

Treatment of Obsessive-Compulsive Disorder (OCD) Signup and view all the answers

Which of the following is a cardiovascular precaution specifically related to nefazodone?

Risk of postural hypotension Signup and view all the answers

If a patient needs to switch from SSRIs to nefazodone, what should clinicians be cautious about?

Exacerbation of withdrawal symptoms Signup and view all the answers

Which of the following is a common effect of Trazodone that makes it a first-line treatment for insomnia?

Sedative effect Signup and view all the answers

Which condition is specifically mentioned as NOT effectively treated by nefazodone?

Obsessive-Compulsive Disorder (OCD) Signup and view all the answers

What class of drugs are known for potentially causing cardiac issues including tachycardia, flattened T waves, and prolonged QT intervals?

TCAs Signup and view all the answers

What effect does food have on the risk of orthostatic hypotension, when associated with Trazodone?

Food increases the risk of orthostatic hypotension Signup and view all the answers

Which of the following best describes how Tricyclic Antidepressants (TCAs) work?

By blocking the reabsorption of serotonin and norepinephrine, making more available to the brain Signup and view all the answers

What is a significant consideration for using TCAs in elderly patients?

Elderly patients may require lower doses due to slower metabolism, particularly women Signup and view all the answers

Which of the following drug classes when combined with Trazodone, increases risk of hypotension?

Antihypertensives Signup and view all the answers

Study Notes

Pharmacokinetics of Selective Serotonin Reuptake Inhibitors (SSRIs)

Half-lives vary significantly among SSRIs.
- Fluoxetine (Prozac): 4-6 days (active metabolite 7-9 days)
- Sertraline (Zoloft): 26 hours (less active metabolite 3-5 days)
- Citalopram (Celexa): 35 hours
- Escitalopram (Lexapro): 27-32 hours
- Paroxetine (Paxil): 21 hours
- Fluvoxamine (Luvox): 15 hours
Food may slightly enhance absorption.
SSRIs are generally well absorbed orally.
Peak effects usually occur within 3-8 hours.
Different binding to plasma proteins, with sertraline, fluoxetine, and paroxetine having the highest binding, and escitalopram the lowest.
Wide therapeutic index.
May potentially slow or block the metabolism of other drugs; fluvoxamine has the most significant potential for interactions.

Pharmacodynamics of SSRIs

Therapeutic effect is mediated by serotonin reuptake inhibition.
Higher doses do not increase antidepressant efficacy but may increase side effects.
Concurrent use with triptans or tramadol can cause serotonin syndrome.

Therapeutic Uses of SSRIs

Depression: All except fluvoxamine are FDA-approved; trial other SSRIs before switching to non-SSRIs.
Suicide risk: Black box warning; risk may decrease over time for adults and elderly but not consistently shown for adolescents. Some studies show SSRIs can protect against suicide by improving depressive symptoms.
Pregnancy/Postpartum: Relapse rates are high, continuing medication is common. No increased risk for major congenital malformations (except paroxetine, which has possible risk in first trimester). Paroxetine may cause infant discontinuation syndrome, and/or increased risk of congenital disabilities, particularly heart defects. Small risk to babies from mothers taking SSRIs late in pregnancy, specifically regarding pulmonary hypertension. Minimal amounts in breast milk, no known harm.
Elderly/Medically Ill: Safe and generally well-tolerated; paroxetine has anticholinergic activity, which can cause issues. Potential for cognitive deficits, prolonged bleeding time, and hyponatremia.
Children: Fluoxetine has shown consistent effectiveness; sertraline effective in social anxiety.
Anxiety Disorders: Generalized anxiety disorder, obsessive-compulsive disorder, indicated for OCD, social anxiety disorders, and panic disorder. Higher doses often needed compared to typical depression doses.

Other Indications

Panic disorder: Paroxetine, fluoxetine, and sertraline. Fluoxetine can initially heighten anxiety. Start with low doses and increase gradually.
Social anxiety disorder: SSRIs safer than MAOIs or benzodiazepines for this.
Post-traumatic stress disorder (PTSD): SSRIs have broad effects on symptom clusters.
Bulimia nervosa: Fluoxetine (60mg/day).
Anorexia nervosa: SSRIs are part of a larger therapeutic approach.
Premenstrual dysphoric disorder: Sertraline, paroxetine, fluoxetine, and fluvoxamine show symptom reduction.
Premature ejaculation: Fluoxetine and sertraline.
Paraphilias: SSRIs can reduce frequency of unconventional sexual activities, urges, or fantasies.
Autism: Sertraline, fluvoxamine, fluoxetine, and clomipramine may be considered.

Precautions and Adverse Reactions

Sexual dysfunction: Common to all SSRIs.
Gastrointestinal (GI) effects: Nausea, diarrhea, anorexia, vomiting, flatulence, and dyspepsia are frequent. Sertraline and fluvoxamine produce the most intense GI symptoms. Delayed-release paroxetine has less intense GI side effects.
Weight gain: Estimated one-third of users gain weight, possibly due to metabolic mechanisms and/or increased appetite, resistant to diet and exercise. Paroxetine associated with most rapid and pronounced gain.
Cardiovascular effects: Can prolong the QT interval, increased risk when combined with antipsychotics. FDA guidelines for citalopram in specific patient populations (hepatic impairment, age 60+, CYP2D6 poor metabolizers, concomitant cimetidine use). Maximum dose restrictions for citalopram and precautions for patients with congenital QT syndrome. Electrolyte and blood concentration monitoring.
Headaches: Fluoxetine more likely to cause headaches.
Central nervous system effects: Anxiety, insomnia, sedation (potential for vivid/nightmarish dreams, emotional blunting—leading to discontinuation—yawning increase. Seizures possible, more so with maximal doses). Extrapyramidal symptoms are rare. Anticholinergic effects (dry mouth, constipation, sedation): Paroxetine has mild but dose-dependent impact.
Hematologic effects: Potential for impaired platelet aggregation (bruising/bleeding issues). NSAID use with SSRIs raises gastric bleeding risk. Proton pump inhibitors may minimize this risk.
Electrolyte and glucose disturbances: Acute decreases in glucose are common. Possible long-term increase in glucose levels.
Endocrine and allergic reactions: Prolactin elevation, and possibly mammoplasia and galactorrhea; reversible upon discontinuation.

Serotonin Syndrome

Symptoms arise from combination with MAOIs, l-tryptophan, or lithium. Symptoms progress from diarrhea and restlessness to extreme agitation, hyperreflexia, autonomic instability, myoclonus, seizures, hyperthermia, rigidity, delirium, coma, status epilepticus, and death.
Immediate withdrawal of the causative drugs and supportive care are needed.

Overdose

Generally, not life-threatening on its own, but potentially problematic when combined with similar medications.

Withdrawal

Possible but generally resolves over a few weeks. Fluoxetine is associated with a lower risk.

Drug Interactions

Many specific interactions; fluvoxamine has significant risk. Other drug interactions exist.

Dosage Guidelines

Detailed dosage guidelines exist for each SSRI, taking into consideration various factors. Specific guidelines for initiating, titrating, and maintaining dosages.

Selective Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs)

Include venlafaxine, desvenlafaxine, duloxetine, levomilnacipran, and milnacipran.
Various indications, including depression, generalized anxiety disorder, social anxiety disorder, neuropathic pain, and others.
Specific adverse reactions, including nausea, sexual side effects, and potential discontinuation syndrome.
Interactions with other medications occur with CYP2D6 isoenzyme.
Detailed dosing information for each medication.

Bupropion

Mechanism: Norepinephrine and dopamine reuptake inhibition.
Low risk of sexual dysfunction/sedation; possible modest weight loss. No withdrawal syndrome.
Administration form options: immediate, sustained, and extended release.
Therapeutic indications: Depression, smoking cessation, bipolar disorders, ADHD, and others.
Specific adverse reactions, including headaches, insomnia, dry mouth, and tremor.
Drug interactions: Avoid with MAOIs.
Detailed dosage guidelines and maximum doses.

Mirtazapine

Mechanism: Antagonism of presynaptic α2-adrenergic receptors and blockade of postsynaptic serotonin receptors; unique mechanism compared to other agents.
Potential to reduce nausea/diarrhea; increased appetite and sedation are reported side effects.
Therapeutic indications: Depression, insomnia, nausea associated with chemotherapy or other medical treatments.
Specific adverse reactions, including somnolence, possible breast milk excretion, and risk of agranulocytosis.
Interactions with CNS depressants and MAOIs.
Dosage guidelines and maximum doses.

Nefazodone

Mechanism: Inhibits serotonin and norepinephrine uptake.
Potential liver function issues warrant frequent monitoring.
Therapeutic indications: Depression, panic disorder, generalized anxiety disorder, but not OCD.
Common side effects: Sedation, nausea, dizziness, vision problems.
Precautions: Risk of postural hypotension and potentially severe hepatic failure. Switching from SSRIs could exacerbate withdrawal.

Trazodone

Mechanism: Weak serotonin reuptake inhibition, potent 5-HT2A/2C antagonism.
Therapeutic indications: Depressive disorders, insomnia, but also erectile dysfunction and agitation.
Common side effects: Sedation, dizziness, orthostatic hypotension.
Precautions: Potential problems with priapism. Interactions with other CNS depressants.

TCAs (Tricyclic Antidepressants)

Mechanism: Increase serotonin and norepinephrine but also affect other receptors, potentially leading to multiple side effects; this also enables use in several indications beyond depression.
Side effects: Anticholinergic effects (dry mouth, constipation, sedation), orthostatic hypotension, sedation, lightheadedness.
Uses: Major Depression Disorder, Panic Disorder, Generalized Anxiety Disorder, Obsessive-Compulsive Disorder, Chronic Pain and Migraines and others,
Specific drug-related considerations and precautions.

Monoamine Oxidase Inhibitors (MAOIs)

Mechanism: Inhibit monoamine oxidase enzymes, increasing neurotransmitters like norepinephrine, serotonin, dopamine, and tyramine.
Crucial concern: Tyramine-rich foods can cause hypertensive crisis.
Uses: Depression (especially atypical depression).
Specific drug-interactions and precautions to avoid problems.

Thyroid Hormones (as Adjuvant therapy)

Mechanism: Influences neurotransmitter receptor genes through binding to intracellular receptors.
Primarily for augmenting antidepressants (liiothyronine.)
Dosage parameters and risks.
Drug interactions, notably with warfarin and other medications.

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Description

Test your knowledge on the pharmacological aspects of SSRIs, including their metabolism, side effects, and dosage recommendations. This quiz covers key concepts related to Selective Serotonin Reuptake Inhibitors used in treating depression and anxiety. Assess your understanding of the therapeutic effects and risks associated with these medications.