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Questions and Answers
A patient with major depressive disorder (MDD) is prescribed fluoxetine. What is the primary mechanism of action of this medication?
A patient with major depressive disorder (MDD) is prescribed fluoxetine. What is the primary mechanism of action of this medication?
- Increase of dopamine release in the synaptic cleft.
- Inhibition of serotonin reuptake in the presynaptic cleft. (correct)
- Inhibition of dopamine reuptake in the synaptic cleft.
- Inhibition of norepinephrine reuptake in the presynaptic cleft.
Which of the following SSRIs is most likely to cause a discontinuation syndrome if abruptly stopped, and why?
Which of the following SSRIs is most likely to cause a discontinuation syndrome if abruptly stopped, and why?
- Paroxetine, due to its short half-life. (correct)
- Sertraline, due to its active metabolite with a long half-life.
- Citalopram, due to its interactions with other medications.
- Fluoxetine, due to its long half-life.
A patient taking venlafaxine for depression reports a recent increase in blood pressure. How is venlafaxine related to this side-effect?
A patient taking venlafaxine for depression reports a recent increase in blood pressure. How is venlafaxine related to this side-effect?
- Venlafaxine's anticholinergic properties lead to decreased heart rate and increased blood pressure.
- Venlafaxine’s effect on serotonin reuptake at low doses causes blood pressure elevation.
- Venlafaxine primarily affects dopamine reuptake, leading to increased blood pressure.
- Venlafaxine inhibits both serotonin and norepinephrine reuptake, with norepinephrine inhibition contributing to blood pressure increase, particularly at higher doses. (correct)
A physician is considering prescribing an antidepressant for a patient with both depression and diabetic neuropathy. Which of the following medications would be most appropriate?
A physician is considering prescribing an antidepressant for a patient with both depression and diabetic neuropathy. Which of the following medications would be most appropriate?
Which of the following is a key difference between SSRIs and SNRIs in terms of their mechanism of action?
Which of the following is a key difference between SSRIs and SNRIs in terms of their mechanism of action?
A patient with a history of liver disease requires antidepressant therapy. Which agent requires close monitoring of liver function due to the risk of hepatotoxicity?
A patient with a history of liver disease requires antidepressant therapy. Which agent requires close monitoring of liver function due to the risk of hepatotoxicity?
A patient with a known CYP2D6 polymorphism is prescribed paroxetine. What is the most important consideration regarding this patient's treatment?
A patient with a known CYP2D6 polymorphism is prescribed paroxetine. What is the most important consideration regarding this patient's treatment?
A patient reports experiencing nausea and diarrhea shortly after starting antidepressant treatment. Which of the following medications is most likely to be the cause?
A patient reports experiencing nausea and diarrhea shortly after starting antidepressant treatment. Which of the following medications is most likely to be the cause?
Flashcards
SSRIs
SSRIs
Selective Serotonin Reuptake Inhibitors used for treating depression and anxiety.
Fluoxetine (Prozac®)
Fluoxetine (Prozac®)
An SSRI effective for MDD, OCD, and bulimia with a long half-life.
Sertraline (Zoloft®)
Sertraline (Zoloft®)
An SSRI used for MDD, PTSD, and anxiety disorders with a half-life of 60–80 hours.
Paroxetine (Paxil®)
Paroxetine (Paxil®)
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SNRIs
SNRIs
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Venlafaxine (Effexor®)
Venlafaxine (Effexor®)
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Duloxetine (Cymbalta®)
Duloxetine (Cymbalta®)
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CYP2D6
CYP2D6
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Study Notes
Selective Serotonin Reuptake Inhibitors (SSRIs)
- Fluoxetine (Prozac®): Used for MDD, anxiety, OCD, and bulimia. Inhibits serotonin reuptake, increasing serotonin levels. Metabolized by CYP2D6 to norfluoxetine (active metabolite). Long half-life (~7-9 days).
- Sertraline (Zoloft®): Treats MDD, PTSD, panic disorder, and social anxiety. Blocks serotonin transporter (SERT). Active metabolite has a half-life of 60-80 hours. Can cause GI distress.
- Paroxetine (Paxil®): Used for depression, GAD, and panic disorder. Selectively inhibits serotonin reuptake. Metabolized by CYP2D6, short half-life (~24 hours). High risk of discontinuation syndrome. More anticholinergic effects.
Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs)
- Venlafaxine (Effexor®): Used for depression, GAD, panic disorder, and neuropathic pain. Inhibits serotonin and norepinephrine reuptake. Metabolized by CYP2D6 to desvenlafaxine (active metabolite). Dose-dependent increase in blood pressure.
- Duloxetine (Cymbalta®): Dose-dependent blood pressure increase.
Atypical Antidepressants
- Bupropion (Wellbutrin®): Used for depression and smoking cessation. Blocks norepinephrine and dopamine reuptake. Short half-life (12 hours). Avoid in patients with seizures or eating disorders.
- Mirtazapine (Remeron®): Used for depression, appetite stimulation, and insomnia. A2 antagonist. Increases norepinephrine and serotonin release. Can cause weight gain and sedation.
- Trazodone (Desyrel®): Used for depression (higher doses) and insomnia (lower doses). Weak serotonin reuptake inhibitor, blocks several other receptors. Highly sedating; used as a sleep aid. Risk of priapism.
Tricyclic Antidepressants (TCAs)
- Amitriptyline: Used for depression, chronic pain, and migraine prevention. Blocks norepinephrine and serotonin reuptake.
Monoamine Oxidase Inhibitors (MAOIs)
- Phenelzine (Nardil®): Used for treatment-resistant depression. Irreversibly inhibits MAO-A and MAO-B, increasing serotonin, norepinephrine, and dopamine levels. Requires a low-tyramine diet.
Antipsychotics
- Haloperidol (Haldol®): Used for schizophrenia, acute agitation, and delirium. Blocks D2 receptors. Long half-life (~20 hours). High risk of extrapyramidal symptoms (EPS), including tardive dyskinesia.
- Risperidone (Risperdal®): Used for schizophrenia and bipolar disorder. D2 and 5-HT2A receptor antagonist. Hepatic metabolism via CYP2D6. Causes prolactin elevation; moderate metabolic side effects.
- Quetiapine (Seroquel®): D2 and 5-HT2A receptor antagonist; strong antihistamine effects. Low risk of EPS but high metabolic effects (weight gain, diabetes).
Mood Stabilizers
- Lithium: Used for bipolar disorder (mania and depression). Alters sodium transport in nerve cells. Renally excreted; narrow therapeutic index (0.6–1.2 mEq/L). Monitor kidney function, thyroid function, and lithium levels to avoid toxicity.
Additional Notes
- Some drugs require monitoring liver function.
- Avoid certain drugs in patients with specific conditions (e.g., seizures, eating disorders).
- Some drugs have significant side effects.
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Description
Explore the pharmacology of SSRIs and SNRIs, including their mechanisms of action, uses, and key characteristics. Learn about specific drugs like fluoxetine, sertraline, paroxetine, and venlafaxine. Understand their metabolism, half-lives, and clinical applications in treating depression and anxiety disorders.
