CNS - Depression & Bipolar - INTRO - SSRIs

44 important questions on CNS - Depression & Bipolar - INTRO - SSRIs

What happens to the response to decreased dose of SSRI in discontinuation syndrome and adverse effects?

  • Discontinuation syndrome: Usually worsens.
  • Adverse effects: Usually worsens.

What are the clinical features of discontinuation syndrome?

  • Dizziness
  • Nausea
  • Anxiety
  • Headache (most common symptoms)

How is depression characterized in response to decreased dose of SSRI?

No acute change or subsequent worsening with relapse or discontinuation syndrome.
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What is the daily oral dose range for Citalopram and its effects?

  • Citalopram: 20-40 mg
  • Insomnia: ++
  • Sexual dysfunction: +++
  • Agitation: +
  • GIT effects: ++
  • Weight gain: 0

Describe the context in which adverse effects occur.

  • Mostly in the first 1-2 weeks of treatment
  • Mostly settle if medication continued
  • Check not a drug interaction +TCA, stop TCA

What is the response to decreased dose of SSRI in serotonin syndrome?

Usually relieved if SSRI ceased & ceasing interacting medicines if possible.

What adverse effects may occur in some patients taking SSRIs?

A more marked stimulation may occur with restlessness and agitation in some patients taking SSRIs.

Describe the adverse effects of Fluoxetine.

  • Fluoxetine: 20-40 mg
  • Insomnia: ++
  • Sexual dysfunction: +++
  • Agitation: ++
  • GIT effects: ++
  • Weight gain: 0

What are the clinical features of serotonin syndrome?

  • Abdominal cramps
  • Agitation
  • Myoclonus
  • Tremulousness
  • Hypo/hypertension
  • Confusion
  • Disorientation
  • Hyperpyrexia
  • Sweating

What should be done if symptoms persist despite intervention in discontinuation syndrome and adverse effects?

  • Discontinuation syndrome: Seek a psychiatric second opinion.
  • Adverse effects: Seek a psychiatric second opinion.

What are some adverse effects of SSRIs?

  • Nausea
  • Nervousness
  • Agitation
  • Diarrhoea
  • Constipation
  • Headache
  • Insomnia

What type of sexual dysfunction may occur with SSRIs?

Sexual dysfunction, including loss of libido, anorgasmia, and ejaculatory disturbance may occur with SSRIs.

How is the response to discontinuation syndrome usually relieved?

  • Usually relieved by increased SSRI dose

What are the adverse effects associated with Fluvoxamine?

  • Fluvoxamine: 100-200 mg
  • Insomnia: +
  • Sexual dysfunction: +++
  • Agitation: +
  • GIT effects: ++
  • Weight gain: 0

What is the recommended action for persistent symptoms in depression and serotonin syndrome?

  • Depression: Seek a psychiatric second opinion.
  • Serotonin syndrome: Urgent referral to an emergency department.

How do SSRIs interact with alcohol and psychomotor functions?

They do not interact with alcohol and have minimal effects on psychomotor functions.

What are the characteristics of Sertraline as a newer SSRI?

  • Undergoes significant first pass metabolism.
  • Its metabolite is only weakly pharmacologically active.
  • Eliminated by liver metabolism.
  • Steady state after 1 week after commencement of treatment.

What is the context for serotonin syndrome?

  • Over dosage
  • Drug interaction, especially SSRI+MAOI/SSRI+TCA
  • Inadequate drug free interval in changing medication

What is a characteristic of Paroxetine regarding metabolism?

Paroxetine undergoes significant first-pass metabolism. It does not have an active metabolite. Its bioavailability is better at higher doses than lower doses-first pass metabolism is saturable.

What are the cardiovascular effects and lethality in overdose of SSRIs?

They have relatively free of cardiovascular adverse effects and have a low lethality in overdose.

What is the daily oral dose range for Sertraline and its effects?

  • Sertraline: 50-100 mg
  • Insomnia: ++
  • Sexual dysfunction: +++
  • Agitation: ++
  • GIT effects: ++
  • Weight gain: 0

What happens in the context of depression regarding treatment?

  • Continuation/worsening of initial illness
  • Patient relapse with continued TXT
  • Some improve with dose increase, some need change of medication

What is the initial dose for major depression in adults and how can it be adjusted?

  • Initial dose: 20 mg once daily.
  • Increase after 3–4 weeks if necessary.
  • Maximum: 60 mg once daily.
  • Elderly usual max: 40 mg once daily, 60 mg can be used.

How is Paroxetine eliminated from the body?

Elimination of Paroxetine is biliary and urinary. Its half-life is approximately 24 hrs, so steady state is reached 1 week after commencement of treatment.

What is the response to depression in terms of treatment change?

  • No acute change except possible adverse events

What type of drug is Fluoxetine and how is it absorbed?

Fluoxetine is a serotonin selective re-uptake blocker. It is well absorbed after oral administration. Maximal blood concentration is achieved after 6 hours.

What is the dosage recommendation for children aged 8-18 with major depression?

  • Initial dose: 10 mg once daily.
  • Increase after 1–2 weeks if necessary.
  • Maximum: 20 mg once daily.

What is the response to serotonin syndrome?

  • Worsens - could be dangerous

What is the recommended fluoxetine dose for adults with bulimia nervosa?

  • Adults over 18 years: 60 mg once daily.

What is the elimination half-life of Citalopram?

Citalopram has an elimination half-life of 30 hours. It is the most 5HT selective agent in this class. Desmethylcitalopram is a major metabolite with weaker serotonin reuptake properties.

How is Fluoxetine metabolized and what is its half-life?

Metabolised in the liver, norfluoxetine is the active metabolite with a half-life of 1 to 2 weeks. Achievement of steady state requires weeks of administration.

How can antidepressants be classified based on tolerability and safety margin?

Antidepressants can be classified into newer and older agents based on tolerability and safety margin. The newer antidepressants are better tolerated, have less lethality in overdose, and are less cardiotoxic than older agents.

What is a characteristic of Fluvoxamine regarding its metabolites?

Fluvoxamine has no known metabolite and has a mean plasma half-life of 20 hours. It is listed as an example of newer SSRIs.

What is the dosage for adults with obsessive-compulsive disorder?

  • Adults over 18 years: 20 mg once daily.

What is a necessary condition for the antidepressant activity of SSRIs, but not sufficient in itself?

Inhibition of 5-HT reuptake may be a necessary condition for the antidepressant activity, but it is not sufficient in itself.

What are the side effects of fluoxetine?

  • Sexual dysfunction
  • Nausea
  • Vomiting

What are some examples of Selective Serotonin Reuptake Inhibitors (SSRIs)?

Examples of SSRIs include citalopram, sertraline, fluoxetine, paroxetine, fluvoxamine, and Bupropion. These medications are used to influence serotonin levels in the brain.

How do SSRIs differ in terms of their pharmacological profiles?

SSRIs differ both in terms of their pharmacological profiles and their pharmacokinetics.

What kind of affinity do SSRIs have for certain receptors?

SSRIs have a slight affinity for histamine, dopamine, serotonin, and muscarinic receptors. This characteristic affects how these drugs interact with various neurotransmitter systems.

What effect does citalopram have that might account for its slightly sedative action?

Citalopram has a modest antihistamine action which might account for its slightly sedative action.

Why was Zimelidine, the first SSRI in Europe, withdrawn?

Zimelidine, the first SSRI in Europe, was withdrawn in the late 1980s due to severe abdominal toxicity. This led to its removal from the market.

What effect does sertraline have that may contribute to its alerting effects?

Sertraline has a slight dopaminomimetic effect which may contribute to its alerting effects.

What is the affinity of SSRIs for the serotonin transporter?

SSRIs have a high affinity for the serotonin transporter both on neuronal and also platelet membranes. This is a key feature of their mechanism of action.

How do SSRIs affect other neurotransmitter systems?

SSRIs affect other neurotransmitter systems which may have some clinical relevance.

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