Pharmacology: Antidepressants and Mood Disorders
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Questions and Answers

What are the symptoms of depression?

  • Enthusiasm and rapid thought and speech patterns
  • Intense feelings of sadness, hopelessness, and despair
  • Changes in sleep patterns and appetite, loss of energy, and suicidal thoughts
  • All of the above (correct)

    • What is mania characterized by?

  • Loss of pleasure in usual activities
  • Changes in sleep patterns and appetite, loss of energy
  • Intense feelings of sadness, hopelessness, and despair
  • Enthusiasm, rapid thought and speech patterns (correct)

    • What is the mechanism of action of most clinically useful antidepressant drugs?

  • They decrease the production of norepinephrine in the brain
  • They potentiate the actions of norepinephrine and/or serotonin in the brain (correct)
  • They increase the production of serotonin in the brain
  • They decrease the production of monoamines in the brain

    • Which of the following is NOT a type of antidepressant?

    <p>Antibiotics</p> Signup and view all the answers

    What is the biogenic amine theory?

    <p>A theory that proposes depression is due to a deficiency of monoamines in the brain</p> Signup and view all the answers

    What happens to presynaptic inhibitory receptor densities in the brain with antidepressant drug use?

    <p>They decrease over a 2 to 4 week period</p> Signup and view all the answers

    What is the name of the antidepressant drug that is also known as ZYBAN?

    <p>Bupropion</p> Signup and view all the answers

    What is the name of the antidepressant drug that is also known as CELEXA?

    <p>Citalopram</p> Signup and view all the answers

    What is the potential adverse effect of SSRIs when used in the presence of a MAOI or other highly serotonergic drug?

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

    What is a possible treatment option for men with erectile dysfunction and depression?

    <p>Treatment with sildenafil, vardenafil, or tadalafil</p> Signup and view all the answers

    What is a symptom of SSRI discontinuation syndrome?

    <p>Malaise and flu-like symptoms</p> Signup and view all the answers

    Which of the following SSRIs has the lowest risk of causing a discontinuation syndrome?

    <p>Fluoxetine</p> Signup and view all the answers

    What is a possible adverse effect of SSRIs?

    <p>Gastrointestinal effects</p> Signup and view all the answers

    What is an option for managing SSRI-induced sexual dysfunction?

    <p>Replacing with an antidepressant having fewer sexual side effects</p> Signup and view all the answers

    What is a symptom of serotonin syndrome?

    <p>Hyperthermia</p> Signup and view all the answers

    What type of disorder is bulimia nervosa?

    <p>Eating disorder</p> Signup and view all the answers

    What is the primary mechanism of action of SNRIs in treating depression?

    <p>Inhibiting the reuptake of both serotonin and norepinephrine</p> Signup and view all the answers

    Which of the following is NOT a potential use of SNRIs?

    <p>Treating anxiety disorders</p> Signup and view all the answers

    What is the primary action of bupropion in alleviating depression?

    <p>Inhibiting the reuptake of dopamine</p> Signup and view all the answers

    What is a potential side effect of bupropion?

    <p>All of the above</p> Signup and view all the answers

    Why is bupropion considered to have a relatively low risk for drug-drug interactions?

    <p>It is a weak inhibitor of dopamine and norepinephrine reuptake</p> Signup and view all the answers

    What is a contraindication for the use of bupropion?

    <p>All of the above</p> Signup and view all the answers

    What is the primary advantage of atypical antidepressants over TCAs and SSRIs?

    <p>They have a different side effect profile</p> Signup and view all the answers

    What is a unique feature of bupropion compared to other antidepressants?

    <p>It assists in decreasing nicotine cravings</p> Signup and view all the answers

    What is the primary mechanism by which mirtazapine enhances neurotransmission?

    <p>Blocking of presynaptic α2 receptors and 5-HT2 receptors</p> Signup and view all the answers

    What is a common side effect of mirtazapine?

    <p>Increased appetite and weight gain</p> Signup and view all the answers

    Which of the following is a characteristic of tricyclic antidepressants (TCAs)?

    <p>They block norepinephrine and serotonin reuptake</p> Signup and view all the answers

    What is the therapeutic effect of TCAs on mood?

    <p>Elevated mood</p> Signup and view all the answers

    Which of the following TCAs is a selective inhibitor of norepinephrine reuptake?

    <p>Maprotiline</p> Signup and view all the answers

    What is a common timeframe for the onset of mood elevation with TCAs?

    <p>2 weeks or longer</p> Signup and view all the answers

    Which of the following receptors does amoxapine block?

    <p>5-HT2 and D2 receptors</p> Signup and view all the answers

    What is a characteristic of mirtazapine compared to TCAs?

    <p>It does not cause antimuscarinic side effects</p> Signup and view all the answers

    What is the effect of Monoamine Oxidase Inhibitors (MAOIs) on neurotransmitter molecules?

    <p>They are allowed to escape degradation, accumulating in the presynaptic neuron and leaking into the synaptic space.</p> Signup and view all the answers

    Which MAOI is available in a transdermal delivery system?

    <p>Selegiline</p> Signup and view all the answers

    What is the result of MAOIs forming stable complexes with the enzyme?

    <p>Irreversible inactivation of the enzyme</p> Signup and view all the answers

    What is a consequence of MAOIs inhibiting MAO in the liver and gut?

    <p>Increased risk of drug-drug interactions</p> Signup and view all the answers

    Which patients may benefit from the stimulant properties of MAOIs?

    <p>Those with low psychomotor activity</p> Signup and view all the answers

    What is a therapeutic use of MAOIs?

    <p>All of the above</p> Signup and view all the answers

    What is a characteristic of most MAOIs?

    <p>Irreversible inactivation of the enzyme</p> Signup and view all the answers

    Why is the use of MAOIs now limited?

    <p>Due to the complicated dietary restrictions required of patients</p> Signup and view all the answers

    Study Notes

    Antidepressants: Treatment of Depression and Mania

    • Symptoms of depression: intense feelings of sadness, hopelessness, despair, and inability to experience pleasure in usual activities, changes in sleep patterns and appetite, loss of energy, and suicidal thoughts.
    • Mania is characterized by the opposite behavior: enthusiasm, rapid thought and speech patterns.

    Types of Antidepressants

    • Selective Serotonin Reuptake Inhibitors (SSRIs)
      • Examples: Citalopram, Escitalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline
    • Serotonin/Norepinephrine Reuptake Inhibitors (SNRIs)
      • Examples: Desvenlafaxine, Duloxetine, Venlafaxine
    • Atypical Antidepressants
      • Examples: Bupropion, Mirtazapine, Nefazodone, Trazodone
    • Tricyclic Antidepressants (TCAs)
      • Examples: Amitriptyline, Amoxapine, Clomipramine, Desipramine, Doxepin, Imipramine, Maprotiline, Nortriptyline, Protriptyline, Trimipramine
    • Monoamine Oxidase Inhibitors (MAOIs)
      • Examples: Isocarboxazid, Phenelzine, Selegiline, Tranylcypromine

    Mechanism of Antidepressant Drugs

    • Most clinically useful antidepressant drugs potentiate the actions of norepinephrine and/or serotonin in the brain.
    • The biogenic amine theory proposes that depression is due to a deficiency of monoamines, such as norepinephrine and serotonin, at certain key sites in the brain.
    • Mania is caused by an overproduction of these neurotransmitters.

    Adverse Effects

    • Headache, sweating, anxiety, and agitation
    • Gastrointestinal effects (nausea, vomiting, diarrhea)
    • Weakness and fatigue
    • Sexual dysfunction
    • Changes in weight
    • Sleep disturbances (insomnia and somnolence)
    • Potential for drug-drug interactions

    Sexual Dysfunction

    • Loss of libido, delayed ejaculation, and anorgasmia
    • One option for managing SSRI-induced sexual dysfunction is to replace with an antidepressant having fewer sexual side effects, e.g., bupropion or mirtazapine.

    Discontinuation Syndrome

    • After abrupt withdrawal, agents with shorter half-lives and having inactive metabolites have a higher risk for adverse reaction.
    • Fluoxetine has the lowest risk of causing an SSRI discontinuation syndrome.
    • Signs of discontinuation syndrome include headache, malaise, and flu-like symptoms, agitation, and irritability.

    Serotonin/Norepinephrine Reuptake Inhibitors (SNRIs)

    • Inhibit the reuptake of both serotonin and norepinephrine.
    • May be effective in treating depression in patients in whom SSRIs are ineffective.
    • Depression is often accompanied by chronic painful symptoms, such as backache, muscle aches, postherpetic neuralgia, and fibromyalgia, against which SSRIs are also relatively ineffective.

    Atypical Antidepressants

    • The atypical antidepressants have actions at several different sites.
    • They are not more efficacious than the TCAs or SSRIs, but their side effect profiles are different.

    Bupropion

    • Acts as a weak dopamine and norepinephrine reuptake inhibitor to alleviate the symptoms of depression.
    • Its short half-life may require more than once-a-day dosing or the administration of an extended-release formulation.
    • Also assists in decreasing the craving and attenuating the withdrawal symptoms for nicotine in tobacco users trying to quit smoking.

    Mirtazapine

    • Enhances serotonin and norepinephrine neurotransmission via mechanisms related to its ability to block presynaptic α2 receptors and block 5-HT2 receptors.
    • It is a sedative because of its potent antihistaminic activity.
    • Causes increased appetite and weight gain.
    • It is markedly sedating, which may be an advantage in depressed patients having difficulty sleeping.

    Tricyclic Antidepressants (TCAs)

    • Block norepinephrine and serotonin reuptake into the neuron.
    • Differ in adverse effects relative to the newer class of antidepressants.
    • Include the tertiary amines, such as imipramine, amitriptyline, clomipramine, doxepin, and trimipramine.
    • Include the secondary amines, such as desipramine and nortriptyline.
    • Include the tetracyclics, such as protriptyline, maprotiline, and amoxapine.

    Mechanism of Action of TCAs

    • Inhibit the reuptake of norepinephrine and serotonin into the neuron.
    • Block serotonergic, α-adrenergic, histaminic, and muscarinic receptors leading to adverse effects.

    Monoamine Oxidase Inhibitors (MAOIs)

    • May irreversibly or reversibly inactivate the enzyme, permitting neurotransmitter molecules to escape degradation and accumulate within the presynaptic neuron and leak into the synaptic space.
    • Cause activation of norepinephrine and serotonin receptors, and may be responsible for their indirect antidepressant action.

    Mechanism of Action of MAOIs

    • Inhibit both MAO in the brain and MAO in the liver and gut that catalyze oxidative deamination of drugs and potentially toxic substances.
    • Show a high incidence of drug-drug and drug-food interactions.
    • Selegiline administered as the transdermal patch may produce less inhibition of gut and hepatic MAO at low doses because it avoids first-pass metabolism.

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    Description

    This quiz covers the treatment of depression and mania, including symptoms, characteristics, and antidepressant medications. Topics include affective disorders, mood disorders, and pharmacological interventions.

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