Pharmacology Flashcards
What are the clinical uses of antidepressant drugs
Moderate to severe depression
Dysthymia
Generalised anxiety disorder
Panic disorder, OCD, PTSD
Premenstrual dysphoric disorder
Bulimia nervosa
Neuropathic pain
What are the main classes of antidepressant
Monoamine oxidase inhibitors
Monoamine reuptake inhibitors which includes:
- tricyclics
- SSRI
- noradrenaline reuptake inhibitors
Atypicals
What are the monoamine neurotransmitters
Noradrenlaine
5-HT (serotonin)
Dopamine
How do most anti-depressants work
Altering the monoamine neurotransmission in some way
Most enhance their activity at the synapses
How might monoamines be affected in those with depression
There is a deficit in monoamine transmitters which causes depression - particularly serotonin and noradrenaline
Drugs that deplete stores of monoamines can induce low mood
CSF from depressed patients have reduced levels of monoamines or metabolites
Name some MAO inhibitors
Phenelzine - irreversible
Moclobemide - reversible
How do MAO inhibitors work
Irreversible (Phenelzine) or reversible (Moclobemide) inhibitors of monoamine oxidase A and B (enzymes)
MOA A and B are responsible for the metabolism of the monoamine neurotransmitters such as serotonin and noradrenaline
Therefore the inhibitors facilitate their release and storage
What are the side effects of MAO inhibitors
Prevents breakdown of dietary tyramine - cheese
Anticholinergic effects
Hypertensive crisis
Insomnia
Postural hypotension
Peripheral oedema
Name common tricyclic antidepressants
Imipramine
Amitriptyline - used for pain now and more sedating
How do the tricyclic antidepressants work
Block the reuptake of monoamines (mainly noradrenaline and 5-HT) into presynaptic terminals
Named for the 3 rings in their chemical structure
What are the side effects of tricyclic anti-depressants
Anticholinergic - blurred vision, dry mouth, constipation, urinary retention
Sedation
Weight gain
Cardiovascular - Postural hypotension, dizziness tachycardia, arrhythmias
Cardiotoxic in overdose - arrhtymia and arrest
Also seizure and coma
Name common SSRIs
Fluoxetine
Citalopram / Escitalopram
Sertraline
Paroxetine
How do SSRIs work
Selectively inhibit reuptake of serotonin (5-HT) from the synaptic cleft.
List come common side effects of SSRIs
Nausea, V and diarrhoea
Increased risk of GI bleeding
Headache and dizziness
Insomnia
Worsened anxiety/agitation
Transient increase in self-harm / suicidal ideation in <25 years
Sweating / vivid dreams
Sexual dysfunction
Hyponatraemia (in elderly)
Discontinuation effects
How do SNRIs work
Dual monoamine reuptake inhibitors
They block the reuptake of noradrenaline and 5-HT (seratonin) into presynaptic terminals.
Therefore similar side effects to SSRIs
Name common SNRIs
Venlafaxine
Duloxetine
Name common atypical antidepressants
Mirtazapine - blocks alpha 2 adreno- and serotonin receptors
Bupropion - dopamine uptake inhibitor
What are the side effects of mirtazapine
Weight gain
Increased appetite
Sedation - best to take in the evening
Can be good if patient is complaining of lack of appetite and loss of sleep
Also presents with some SSRI side effects like nausea and sexual dysfunction due to serotonin blockage. Though generally less than other SSRIs
Do anti-depressants start working immediately
No
Most have a delayed onset of action of several weeks
Why do you need to be cautious when prescribing anti-depressants to young adults/ teenagers
There can be a transient increase in suicidal ideation, self harm and aggressive ideas in this age group when they take the medications
What is the aim of bipolar treatment
Acutely it is to treat the symptoms = reduce mood in mania and raise mood in depression
Long term it is to stabilise mood - prevent recurrence of mania or depression
How is lithium used
As first-line maintenance in bipolar - mood stabiliser
It reduces both the number and severity of relapses
Offers some protection against antidepressant-induced hypomania if on dual treatment
Can be used in acute mania as well
May be used in recurrent depressive disorder, or schizoaffective disorder
Do you need to monitor lithium doses
YES
Very narrow therapeutic index and can lead to toxicity
Also has a very long half life
Monitor blood levels - 12 hours post-dose
Check weekly when starting or changing dose
Levels are checked every 3-6 months once stable
Also need to check thyroid and renal function every 6 months
What are the common side effects of lithium treatment
Dry mouth / strange taste
Nausea/vomiting and diarrhoea
Polydipsia and polyuria
Tremor - fine
Hypothyroidism - due to thyroid enlargement
Hyperparathyroidism
Long term reduced renal function
Nephrogenic diabetes insipidus
Weight gain
idiopathic intracranial hypertension
leucocytosis
hyperparathyroidism and resultant hypercalcaemia
What are the symptoms of lithium toxicity
Vomiting
Diarrhoea
Ataxia / coarse tremor
Drowsiness / altered conscious level
Convulsions
Coma
Which anti-convulsant drugs can be used as mood stabilisers
Valproic acid/ sodium valproate
Lamotrigine
Carbamazepine
What are the side effects of valproic acid
Drowsiness
Ataxia
CV effects
Induces liver enzymes
Hepatotoxicity
Teratogenicity - causes neural tube defects
Blood dyscrasia: Thrombocytopenia, leucopoenia, red cell hypoplasia.
Weight gain
Nausea, vomiting and diarrhoea.
Loss of hair
Headache, confusion and lethargy.
Pancreatitis
What are the side effects of carbamazepine
Drowsiness
Headache and diplopia
Ataxia
CV effects
Leucopenia
Hepatoxicity, liver failure and cholestatic jaundice.
Induces liver enzymes - interacts with other drugs
Teratogenicity: Spina bifida
Risk of SJS and TEN
What are the side effects of lamotrigine
Small risk of Stevens-Johnson syndrome
Flu-like symptoms
Aseptic meningitis
Ataxia and blurred vision
Which anti-psychotics can be used as mood stabilisers
Quetiapine
Aripiprazole
Olanzapine
Lurasidone
What are the side effects of the anti-psychotics used as mood stabilisers
Sedation
Weight gain
Metabolic syndrome
Extra-pyramidal side-effects (Aripiprazole)
Which herbal/complementary medicine can cause serotonin syndrome
St John’s Wort
Functions similarly to an MAOI
Higher risk if a conventional antidepressant is prescribed alongside it
Which anti-psychotic is most likely to cause extra pyramidal side effects
Chlorpromazine
First generation drugs acting on the D2 receptors will cause these symptoms
Women of child bearing age should not be prescribed sodium valproate - true or false
True
Unless other options are unavailable, AND adequate contraception (ideally depot or IUD) is in place.
Which anti-psychotic is most likely to cause weight gain
Clozapine
Olanzapine
How does acamprosate work to treat alcohol dependence
It acts on the neurotransmitter systems in the brain to reduce the reliance on and craving for alcohol
It helps to normalise the brain chemistry that has been disrupted by alcohol
Good for those who wish to control their drinking, but is not prepared to commit to abstinence from alcohol
List side effects of clozapine
Sialorrhoea - excessive salivation
Constipation - severe
Nausea and vomiting
Seizure
Weight gain
Hypotension - dose related
Neutropenia/agranulocytosis
Myocarditis and cardiomyopathy
How is dopamine involved in the treatment of psychotic disorders
Some evidence that an increase in dopamine level in the mesolimbic system contributes to psychotic disorders like schizophrenia
Many antipsychotics act on dopamine receptors - all act on D2
The more the dopamine receptor binding affinity, the better the therapeutic effect and clinical potency of the antipsychotic agent