Anti-depressants and Anxiolytics Flashcards
How long after you start someone on an anti-depressant before it starts to be effective and symptoms start to improve?
2 - 4 weeks
What are the 5 main classes of anti-depressants?
- Selective Serotonin Reuptake Inhibitors (SSRIs)
- Serotonin/Noradrenaline (dual) Reuptake Inhibitors (SNRIs)
- Tricyclics (TCAs)
- Monoamine Oxidase Inhibitors (MAOIs)
- Novel anti-depressants
Which class of anti-depressants tend to be 1st line in treatment of depression?
Selective Serotonin Reuptake Inhibitors (SSRIs)
What is the common treatment regime/progression of treatment for someone with depression?
- Start them on an SSRI
- If no improvement is seen after a trial of adequate length (at least 2 months) and adequate dose then you tend to switch them to another class of anti-depressant.
- If again there is no improvement, you then add an adjunctive.
Tricyclics:
- Are these well tolerated?
- What are their main side effects?
- These are often very effective but the side effects are usually unacceptable for most people. TCAs are toxic – even a week supply could cause an overdose. CV effects = can cause QT lengthening even at a therapeutic serum.
- They have anti-histaminic and anti-cholinergic effects which cause the following side effects:-
- Anti-histaminic => weight gain, sleepy
- Anti-cholinergic => dry mouth, blurred vision
Names of common TCAs
- Amitriptyline
- Nortriptyline
- Protriptyline
- Imipramine
- Desipramine
- Clomipramine
- Doxepin
How do Tricyclics work?
TCAs work by hitting quite a lot of receptors, as a result they increase serotonin, dopamine and noradrenaline.
Different TCAs hit these receptors in slightly different ways.
What are the 2 subclasses of Tricyclics?
Tertiary TCAs - essentially ‘dirtier drugs’ – lots of amine side chains which are prone to cross reacting with other types of receptors which leads to more side effects. Examples of tertiary TCAs include Imipramine, amitriptyline, doxepin, clomipramine. They also have active metabolites (when they are broken down in the body) including desipramine and nortriptyline.
Secondary TCAs - these are often the active metabolites of the tertiary amines / TCAs. They primarily block noradrenaline. Side effects are the same as tertiary TCAs but are generally less severe. Examples of secondary TCAs include Desipramine, nortriptyline.
How do Monoamine Oxidase Inhibitors (MAOIs) work?
These do the same things as TCAs but in a slightly different way.
MAOIs bind irreversibly to monoamine oxidase which prevents the inactivation of amines such as norepinephrine, dopamine and serotonin (so they are always activated) leading to increased synaptic levels. They are very effective for resistant depression.
What are the side effects associated with MAOIs?
- Orthostatic hypotension
- Weight gain
- Dry mouth
- Sedation
- Sexual dysfunction
- Sleep disturbance
- Cheese reaction – Patients on these may need to alter their diet
- Serotonin syndrome
Describe the ‘cheese reaction’ side effect of MAOIs
This is a reaction caused by eating Tyramine-rich foods whilst on MAOI medication. Tyramine-rich foods include:- aged cheese, beer on tap, red wine, soy sauce, flava beans etc (the tyramine content increases as foods age)
Tyramine affects your blood pressure. It is regulated and broken down by the MAO enzyme and so when on MAOI medication, you cannot break down the tyramine and this can cause a hypertensive crisis or potentially death.
What is Serotonin syndrome?
- Serotonin syndrome is a potentially fatal but rare condition.
- It develops if there are excess serotonin levels – this can happen if you take MAOI with meds that increase serotonin or have sympathomimetic actions.
- Also if you are using a combination of anti-depressants or SSIs at a high dose.
How do SSRIs work?
- SSRIs block pre-synaptic serotonin reuptake so increase the level of serotonin available.
- Used for both depression and anxiety.
- They are relatively safe – very little risk of cardiotoxicity in overdose.
What are the side effects of SSRIs?
They have side effects but they are more tolerable!
- GI upset
- Sexual dysfunction in up to 30% of people
- Anxiety
- Restlessness
- Nervousness
- Insomnia
- Fatigue
- Sedation
- Dizziness
- Activation or discontiunation syndrome can be an issue!
What is activation syndrome and discontinuation syndrome?
- Activation syndrome – caused by an increase in serotonin. Tends to last 2-10 days. Can feel sick, nauseous, increased anxiety, panic and agitation.
- Discontinuation syndrome - happens if you stop SSRIs suddenly. Causes things like agitation, nausea, imbalance (dizziness, vertigo, light headedness) and dysphoria (a state of unease or generalized dissatisfaction with life).