Premium Members Area
Dr. Derek Tracy: Reviewing Bupropion for Depression
Dr. Tracy is a BRC research fellow and the neuromodulation lead at the Institute of Psychiatry, Psychology, and Neuroscience, King’s College London. Dr. Tracy also sits on the Editorial Board of the British Journal of Psychiatry.
His team published a review paper in Therapeutics Advances in Psychopharmacology titled “Bupropion: a systematic review and meta-analysis of effectiveness as an antidepressant”.
We discuss the following topics:
- The effectiveness of bupropion as monotherapy and combination therapy, and how it compares to other antidepressants
- The limitations of the literature reviewed
- The importance of considering the possibility of insomnia and agitation when prescribing this drug
- Symptom domains for which bupropion may be more effective and symptoms for which it may be less effective
- The use of bupropion to avoid and treat antidepressant-induced sexual dysfunction
- Specific clinical situations in which this drug is a good therapeutic option
Suicide Risk and Antidepressants Use
In 1990, case reports described patients who developed intense suicidal ideation during treatment with fluoxetine. In response to this, the manufacturer performed a meta analysis of 17 randomized trials and found no differences in suicidality with placebo.
In 2003 the FDA issued an advisory about suicidality in pediatric patients, this was in response to reports of suicidality in clinical trials. One year later, in 2004, the FDA reexamines the data and issues a warning on increased suicidality in children and adolescents.
In 2005, they studied young adults and decided to issue an advisory on increased suicidality in young adults. Two years later this was included in the current black box warning.
The Mechanism of Action of SSRIs
This presentation is divided in three sections.
The first section is a brief overview of the monoamine theory of depression and its limitations. The second discusses the effects of 5HT1A receptor downregulation on the mechanism of action of SSRIs. The third section presents recent findings on the role of BDNF in depression.
Fluoxetine: The Oldest SSRI
Paroxetine has activating properties that make it a good option for patients with retarded depression or atypical depression. However, we should avoid activation in patients with insomnia and agitation.
There is something that makes fluoxetine unique: its long half-life, we will discuss the advantages and disadvantages of this in clinical practice. This long half-life allowed the development of a weekly capsule. Fluoxetine is a potent inhibitor of the CYP2D6.
Paroxetine: Sexual Dysfunction and Discontinuation Syndrome
Many clinicians see paroxetine as suitable for anxious depression, this is can be considered an interesting clinical tip that might help you choosing an antidepressant. However, this observation hasn’t been specifically addressed in randomized controlled trials.
Regarding its side effects profile, important features include: higher risk for sexual dysfunction, discontinuation syndrome and weight gain.
Fluvoxamine: Potential for Drug-Drug Interactions
Besides being a SERT inhibitor, fluvoxamine is an agonist at sigma 1 receptors.
The drug is approved in the US for the treatment of OCD but not depression. An interesting point, as this is a widely used antidepressant in other countries.
Fluvoxamine has the potential for drug-drug interactions through inhibition of CYP450 isoenzymes. The dosage range goes from 100 to 300 mg/day.
Sertraline: Less Interactions, Average SSRI
Sertraline is a moderate inhibitor of CYP2D6. In terms of drug-drug interactions this is not as significant as with fluoxetine or paroxetine.
It has a similar side effects profile to other SSRIs.
The dosage range goes from 50 to 200 mg/day.
Citalopram and Escitalopram: Key Similarities and Differences
Citalopram and escitalopram have no significant drug-drug interactions. Citalopram is linked to QT prolongation. This drug was initially approved to be used in a range from 20 to 60 mg/day. In 2011, the FDA recommended against its use in doses higher than 40 mg/day.
Regarding prescribing tips, escitalopram equivalent dose is half that of citalopram
Venlafaxine vs Desvenlafaxine: Similar Efficacy
Venlafaxine is a SNRI that is metabolized to O-desmethylvenlafaxine or desvenlafaxine. In 2008 this active metabolite was approved as antidepressant. In this presentation we will see what the two drugs have in common and their differences. They are similar in terms of efficacy, pharmacodynamics and side effects profile.
There are differences in pharmacokinetic aspects and dosing guidelines for these two SNRIs
Bupropion: Used As Augmenting Option
Bupropion is a norepinephrine dopamine reuptake inhibitor, or NDRI. It is approved as antidepressant as well as for smoking cessation.
Some characteristic aspects of its side effects profile include a lack of sexual side effects, compared to other antidepressants and an increased risk of seizures.
As part of your premium membership you have access to the online course: “Antipsychotics: The Essentials”. The approximate length of this course is 3 hours.
You can download the PPT files and videos for your personal use
1- Introduction to Antipsychotic Medications
Antipsychotics History: the discovery of chlorpromazine and clozapine. First Generation Antipsychotics, Second Generation Antipsychotics: terminology and classification. List of Agents. Differences between FGAs and SGAS.
Approximate length: 21 minutes
2- Mechanism of Action
The four dopamine pathways: an overview. The relationship between dopamine pathways and antipsychotics therapeutic and adverse effects .
The mechanism of action of first and second generation antipsychotics: theories about “atypicality” of second generation antipsychotics.
Approximate length: 23 minutes
3- Indications for Antipsychotic Agents
Overview of common indications for antipsychotics (including off-label uses).
The effects of antipsychotics on schizophrenia symptoms. Classification of phases in schizophrenia treatment. Basic principles guiding antipsychotic selection.
Comparison of the use of antipsychotics in different phases of bipolar disorder.Use of antipsychotics in depression.
Approximate length: 45 minutes
4- Side Effects: Detection and Monitoring
Neurological, metabolic, and other side effects of antipsyhcotic medications. Clinical manifestations of the neuroleptic malignant syndrome.
Approximate length: 45 minutes.
5- A Primer On Selected Antipsychotics
Integration of relevant features of selected antipsychotic medications:
Haloperidol, Chlorpromazine, Fluphenazine, Clozapine, Risperidone, Quetiapine, Aripiprazole, Ziprasidone, Paliperidone, Iloperidone, Asenapine, Lurasidone
Approximate length: 32 minutes.
In this section you will find resources related to CNS receptors.
General classification. Cellular actions of opioid receptors. Anatomical distribution and physiologic effects of mu, delta and kappa receptors
Agonists and antagonists
Approximate length: 14 minutes
The 5HT1A Receptor in Psychopharmacology
The 5-HT1A receptor is a subtype of serotonin receptor located in presynaptic and postsynaptic regions. Activation of this receptor has been involved in
the mechanism of action of anxiolytic, antidepressant and antipsychotic medications.
This article is an illustrated overview of 5HT1A receptor physiology and its role in psychiatric conditions.