Pharmacology Flashcards
What is the mechanism of action of the monoamine oxidase inhibitors?
Inhibit monoamine oxidase
Monoamine oxidase breaks down serotonin and noradrenaline in the brain - so inhibiting the enzyme inhibits breakdown
What are some of the side effects of the monoamine oxidase inhibitors?
Cheese reaction
Insomnia
Postural hypotension
Peripheral oedema
What is the “cheese reaction”
A side effect of monoamine oxidase inhibitors
Hypertensive crisis caused by inhibition of MAO-A in the gut which prevents the breakdown of dietary tyramine
(tyramine exists in wine and cheese)
Patients need to avoid these foods
With which drug class are patients required to have a restricted diet?
Monoamine oxidase inhibitors
Give some examples of tricyclic antidepressants
Imipramine
Dosulepin
Amitriptyline
Lofepramine
What is the mechanism of action of tricyclic antidepressants?
Block the reuptake of monoamines (noradrenaline and 5-HT) into presynaptic terminals
What are some of the side effects of tricyclic antidepressants?
Anticholinergic effects (blurred vision, dry mouth, constipation, urinary retention)
Antihistaminergic effects
(sedation and weight gain)
Cardiac effects
(postural hypotension, tachycardia)
Fatal arrhythmias with overdose
Give some examples of selective serotonin re-uptake inhibitors (SSRIs)
Fluoxetine
Citalopram
Sertraline
Paroxetine
What is the mechanism of action of the SSRIs?
Selective inhibition of the re-uptake of serotonin (5-HT)
What are some of the side effects of SSRIs?
Nausea Headache Sweating Vivid dreams Worsening of anxiety Sexual dysfunction Hyponatraemia
*relatively safe in overdose compared to the others
With which drug class is there a transient increase in the risk of self-harm in patients <25 years old?
Selective serotonin reuptake inhibitors
*This drug class should be avoided in adolescence
Give some examples of dual reuptake inhibitors (SNRIs)
Venlafaxine
Duloxetine
What is the mechanism of action of the SNRIs?
Block the reuptake of monoamines (noradrenaline and 5-HT) into presynaptic terminals
Which drug class lack major receptor-blocking actions and therefore have fewer side effects than tricyclics?
Dual reuptake inhibitors
Give some examples of atypical antidepressants
Mirtazapine
Bupropion
Give some examples of antidepressants which are noradrenaline selective?
Reboxetine
Desipramine
Protriptyline
Give some examples of antidepressants which are 5-HT selective
Fluoxetine
Citalopram
Sertraline
Paroxetine
What is the gold standard medication for bipolar disorder?
Lithium
What is the mechanism of action of lithium?
Blocks phosphatidylinositol pathway
or
inhibits Glycogen Synthase Kinase 3β
What are some of the side effects of lithium?
Dry mouth/ strange taste Weight gain Sedation Polydipsia/ polyuria Tremor GI upset Ankle swelling
Hypothyroidism
Reduced renal function
What medication should not be taken in combination with lithium?
NSAIDs
Diuretics
ACE. I/ ARBs
Give some examples of anticonvulsants which are used long term as mood stabilisers for bipolar disorder
Valproate, lamotrigine, carbamazepine
Which drug which can be used as a mood stabiliser in bipolar disorder should not be given to women of child bearing age?
Valproate
- teratogenic
Give some examples of antipsychotics which are used long term as mood stabilisers for bipolar disorder
Quetiapine
Aripiprazole
Olanzapine
Lurasidone
What are some side effects of antipsychotics used for bipolar disorder?
Sedation
Weight gain
What is the monoamine hypothesis?
Depression results from a functional deficit of monoamine transmitters - particularly serotonin and noradrenaline
How long should you trial an antidepressant before deciding it isn’t working?
About 2-3 months
What factors may contribute to a patient not responding to medications?
May not be compliant
Dosage too low
Social factors
Might not be the right drug for them
Why do some antidepressants work for some people and not for others?
Everyone has different genetics - one patient may have more of a serotonin problem and the other more a noradrenaline issue
How long should a patient be continued on antidepressants for?
At least 6 months from the resolution of symptoms
NB - what makes you well keeps you well
What are some of the side effects of anticonvulsants which can be used in the management of bipolar disorder?
Sodium valproate is teratogenic
Lamotrigine takes a long time to work and can cause Steven Johnson’s syndrome
Carbamazepine can be quite sedative
What investigations need to be routinely done for patients taking lithium?
Bloods
Lithium levels 12 hours after dose
Thyroid function, parathyroid function and renal function every 6 months
Which antidepressants are the worst in overdose?
Tricyclics are fatal in overdose
SSRIs are not so bad in overdose
Why should tricyclics be avoided in patients with prostatism?
They cause urinary retention (anticholinergic effects)
Which class of antidepressants are useful in patients who are struggling to sleep?
Tricyclic antidepressants - these are sedative
Which drugs are most associated with weight gain?
Mirtazapine, tricyclics, lithium and antipsychotics
Why does lithium require monitoring?
It has a narrow therapeutic index
What drugs are used to treat anxiety disorders?
SSRIs (first line), other antidepressants
Pregabalin (as mono therapy or to augment antidepressants)
B-blockers and benzodiazepines for symptomatic relief
What drugs are used to treat OCD?
SSRIs/ clomipramine - tricyclic
Antipsychotics
What is the mechanism of action of benzodiazepine?
What are the pharmacological effects of this drug class?
Enhance the effect of GABA by allosteric modulation
Relaxation
Anticonvulsant effects
Sedation
What are some of the side effects of benzodiazepines?
Sedation
Psychomotor retardation / impaired coordination
Dependency
Alcohol interaction
Aggression
Anterograde amnesia
Give some examples of benzodiazepines
Diazepam (valium)
Lorazepam
Chlordiazepoxide
Which benzodiazepine is suitable for use in the community?
Diazepam (valium) this is because it has a longer half life than the others
What are some of the clinical uses of benzodiazepines?
Acute treatment of extreme anxiety
Alcohol withdrawal
Mania
Delirium
Status epilepticus
Rapid tranquilisation
What is the mechanism of action of pregabalin, a drug which can be used in the management of anxiety?
Calcium channel blocker and GABA enhancer
*NB only considered if the patient doesn’t respond to other treatments
What specific symptoms are b-blockers useful for?
Physical symptoms such as palpitations and tremors
Give some examples of typical antipsychotics
Chlorpromazine, thioridazine, haloperidol
Give some examples of atypical antipsychotics
Olanzapine, quetiapine, aripiprazole, clozapine
Amisulpramide
What is the mechanism of action of the antipsychotics?
Block dopamine D2 receptors, blocking dopaminergic transmission in the mesolimbic pathways
Which type of antipsychotic are more associated with extra-pyramidal side effects?
Typical antipsychotics