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Questions and Answers
What is the primary function of serotonin receptors in the context of anxiety disorders?
What is the primary function of serotonin receptors in the context of anxiety disorders?
What is the primary mechanism of action of benzodiazepines?
What is the primary mechanism of action of benzodiazepines?
In treating anxiety disorders, what is a significant problem associated with SSRIs?
In treating anxiety disorders, what is a significant problem associated with SSRIs?
Which of the following is a special consideration when prescribing benzodiazepines?
Which of the following is a special consideration when prescribing benzodiazepines?
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Which of the following conditions may switch to another agent or require an additional medication when treating anxiety?
Which of the following conditions may switch to another agent or require an additional medication when treating anxiety?
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What is a common risk associated with the initiation of SSRIs in patients?
What is a common risk associated with the initiation of SSRIs in patients?
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Which condition is most likely to lead to SIADH in the elderly when treated with SSRIs?
Which condition is most likely to lead to SIADH in the elderly when treated with SSRIs?
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What is the therapeutic use of flumazenil?
What is the therapeutic use of flumazenil?
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What is the potential addition to SSRIs that may be considered for treating patients with certain anxiety disorders?
What is the potential addition to SSRIs that may be considered for treating patients with certain anxiety disorders?
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What is NOT a typical indication for the use of benzodiazepines?
What is NOT a typical indication for the use of benzodiazepines?
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Which of the following is a notable characteristic of tricyclic antidepressants compared to SSRIs?
Which of the following is a notable characteristic of tricyclic antidepressants compared to SSRIs?
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What effect does GABA have on neuronal activity?
What effect does GABA have on neuronal activity?
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What aspect of serotonin levels is primarily disrupted in individuals with anxiety disorders?
What aspect of serotonin levels is primarily disrupted in individuals with anxiety disorders?
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What is the potential risk of benzodiazepine withdrawal?
What is the potential risk of benzodiazepine withdrawal?
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Which of the following medications is associated with anxiety and panic disorder?
Which of the following medications is associated with anxiety and panic disorder?
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What is a notable side effect of Buspirone?
What is a notable side effect of Buspirone?
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What distinguishes SSRIs from other anxiolytics?
What distinguishes SSRIs from other anxiolytics?
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Why is Lorazepam considered potentially better for the elderly?
Why is Lorazepam considered potentially better for the elderly?
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What is the mechanism of action of Buspirone?
What is the mechanism of action of Buspirone?
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What makes Buspirone contraindicated for some patients?
What makes Buspirone contraindicated for some patients?
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Which of the following statements is true regarding Clonazepam?
Which of the following statements is true regarding Clonazepam?
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What is a possible risk of abrupt withdrawal from SSRIs?
What is a possible risk of abrupt withdrawal from SSRIs?
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What should be considered regarding patients with renal dysfunction and the use of benzodiazepines?
What should be considered regarding patients with renal dysfunction and the use of benzodiazepines?
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What condition is associated with an increase in appetite, primarily in children?
What condition is associated with an increase in appetite, primarily in children?
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Which of the following conditions is NOT associated with autism in children?
Which of the following conditions is NOT associated with autism in children?
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What condition is primarily treated by Citalopram?
What condition is primarily treated by Citalopram?
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Which of the following SSRIs is not approved for use in children?
Which of the following SSRIs is not approved for use in children?
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What is a significant risk associated with the discontinuation of Paroxetine?
What is a significant risk associated with the discontinuation of Paroxetine?
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How long should one wait after stopping Fluoxetine before starting an MAO inhibitor?
How long should one wait after stopping Fluoxetine before starting an MAO inhibitor?
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Which SSRI is specifically noted for being least likely to interact with CYP450 enzymes?
Which SSRI is specifically noted for being least likely to interact with CYP450 enzymes?
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Which of the following SSRIs is known to cause persistent pulmonary hypertension if used during pregnancy?
Which of the following SSRIs is known to cause persistent pulmonary hypertension if used during pregnancy?
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What significant side effect is most commonly associated with Paroxetine?
What significant side effect is most commonly associated with Paroxetine?
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What secondary condition is treated by Escitalopram?
What secondary condition is treated by Escitalopram?
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Which SSRI has a primary indication to treat Major Depressive Disorder in children as young as 8 years?
Which SSRI has a primary indication to treat Major Depressive Disorder in children as young as 8 years?
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Study Notes
Benzodiazepines
- Increase the frequency of GABA receptor opening, thereby causing the calcium channels to open in the postsynaptic GABA receptor and hyperpolarize (make more negative on the inside) the neuronal membrane which makes it more resistant to receiving an action potential. This slows down nerve conduction, causes CNS depression, and increases the action of GABA, an inhibitory NT, decreasing neuronal excitement.
- Used for a variety of conditions such as short-term management of anxiety (except for Clonazepam), epilepsy, muscle spasms, insomnia, IBS, and for the management of nausea and vomiting associated with chemotherapy.
- Side effects include drowsiness, respiratory depression, hypotension, confusion, blurry vision, and paradoxical anxiety.
- All benzodiazepines are metabolized through the liver, so liver disease increases the half-life of the drug.
- Cannot abruptly stop medication, as individuals can become physically dependent and experience withdrawal symptoms.
- Contraindicated in pregnancy.
- Flumazenil is a competitive antagonist to the GABA receptor and can be used as an antidote.
Intermittent Acting Benzodiazepines
- Last 10-24 hours.
- Due to 3A4 metabolism, highly prone to drug-drug interactions in patients with severe liver failure.
Long Acting Benzodiazepines
- Last longer than 24 hours.
Non-Benzodiazepine Anxiolytics
Buspirone (BuSpar)
- Exact MOA is unknown, but is thought to act as a partial agonist to the 5HT1A receptor.
- Used for generalized anxiety disorder, depression with an overlay of anxiety, situational anxiety.
- Side effects include nausea, headache, nervousness, and lightheadedness.
- Delayed onset of 2-3 weeks, not for acute treatment.
- Can take up to six weeks for maximum effects.
- Pregnancy category B, meaning it can be used.
- Contraindicated in patients with known hypersensitivity to buspirone or in those with severe hepatic or renal disease.
- Frequently used adjunctively with SSRIs in the treatment of treatment-resistant depression.
SSRIs (Selective Serotonin Reuptake Inhibitors)
- Selectively inhibit reuptake of serotonin, desensitizing presynaptic serotonin receptors in a negative feedback loop that normally inhibits serotonin release, which then increases serotonin levels.
- Used for major depressive disorder, panic disorder, obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, premenstrual dysphoric disorder, post traumatic stress disorder, bulimia nervosa, kleptomania, and trichotillomania.
- Side effects include headache, diarrhea, drowsiness or insomnia, agitation and/or anxiety, and sexual dysfunction.
- Abrupt withdrawal can cause withdrawal symptoms and rebound depression.
- Start at lower doses when treating anxiety disorders.
- Not very lethal in overdoses.
- Patients need to be monitored closely for 2-3 weeks of initiation of SSRI therapy, including suicide risk assessment.
Other Psychiatric Drugs
- There are many other classes of psychiatric medications that are essential, but not listed in the text. These include antipsychotics, mood stabilizers, and stimulants.
SSRI's
- SSRI's work by increasing the levels of serotonin in the brain
- It can take 3-4 weeks for the medication to have an effect
- SSRI discontinuation syndrome can be especially problematic when co-administered with tramadol, meperidine, and/or MAO inhibitors
- Discontinuation syndrome includes: effects from missed doses of short acting agents, not an actual withdrawal
- SSRI's can cause serotonin syndrome, especially when administered with other medications
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Citalopram (Celexa)
- Primary receptor: Serotonin
- Secondary: Noriepi and Dopa
- Not approved for children
- Limit the max dose in poor metabolizers of 2C19 or inhibitors of 2C19
- Limit the max dose in patients with hepatic impairment
- The risk of prolonged QT interval increases with co-administration of OCPs in doses of 30mg or more
- Has a lower interaction risk with CYP450 enzymes
-
Escitalopram (Lexapro)
- Primary receptor: Serotonin
- Avoid within 2 weeks of MAOIs
- Caution if CrCl < 30 mL/min
- The S-enantiomer of racemic citalopram (20mg is equal to 40mg of citalopram)
- Has a lower interaction risk with CYP450 enzymes
-
Fluoxetine (Prozac)
- Primary receptor: Serotonin
- Secondary: Norepi
- It is metabolized to norfluoxetine which has a half life of 4-6 days
- Stop MAOIs 14 weeks before or 5 weeks after stopping Fluoxetine
- This is due to the high risk of serotonin syndrome
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Paroxetine (Paxil)
- Primary receptor: Serotonin
- Secondary: Norepi
- May be the most sedating and anticholinergic SSRI
- Can have a high likelihood of discontinuation syndrome
- Pregnancy category C
- Approved in children
- Can cause weight gain, diabetes, HLD, hyperprolactinemia, and rash
- Increase appetite (mainly in children)
- May cause polydipsia associated hyponatremia
Persistent Pulmonary Hypertension
- Exposure during pregnancy, especially after 20 weeks of gestation, may cause persistent pulmonary hypertension
- More common with Paroxetine
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Description
This quiz explores the pharmacology of benzodiazepines, including their action on GABA receptors and their medical applications. You will also learn about the potential side effects, risks of dependence, and important considerations for use and withdrawal. Test your knowledge on this significant class of medications used for various conditions.
