Pharmacology Flashcards
Name the SSRIs.
Fluoxetine Setraline Citalopram Escitalopram Paroxetine
What is the mechanism of action of the SSRIs?
Specifically inhibit serotonin reuptake at the pre-synaptic membrane, increasing the serotonin concentration in the synaptic cleft.
What are some advantages of using an SSRI over other types of anti-depressants?
Less sedating
Fewer anti-muscarinic effects
Lower risk of cardiotoxicity
Safer in overdose
What are some ADRs of SSRIs?
GI disturbances (nausea, vomiting, dyspepsia, diarrhoea, constipation, abdominal pain)
Altered appetite
Drowsiness OR insomnia
Sexual dysfunction
Name the TCAs.
Amitryptilline
Imipramine
Lofepramine
Nortryptilline
What is the mechanism of action of the TCAs?
Inhibit reuptake of serotonin and NA at the pre-synaptic membrane, increasing their concentrations in the synaptic cleft.
Also block serotonergic, alpha-adrenergicm histaminic and muscarinic receptors.
What are some ADRs of TCAs?
Sedation, weight gain, dry mouth, constipation, urinary retention, blurred vision, tachycardia, arrythmias, nausea, drowsiness.
What are the PK of TCAs? (absorption/metabolism)
Absorbed by the gut
Lipid soluble
Metabolised by the liver
What are the PK of SSRIs? (absorption/metabolism)
Almost completely absorbed from gut and metabolised by liver
Give an example of a NaSSA.
Mirtazapine
What is the mechanism of action of mirtazapine?
Enhances serotonin and NA neurotranmission.
Also classed as a TCA as well as a NaSSA
What are the indications for mirtazapine?
Severe depression, PTSD
What are some contra-indications for mirtazapine?
Renal impairment
Pregnancy
Hepatic impairment
Jaundice
What are the ADRs of mirtazapine?
Weight gain Sedation Hallucinations Confusion Mania Postural hypotension
Name the SNRIs.
Venlafaxine
Duloxetine
What is the mechanism of action of SNRIs?
Inhibit the re-uptake of serotonin and noradrenaline at the pre-synaptic membrane, increasing their concentration at the synaptic cleft.
What are the ADRs of SNRIs?
Same as SSRIs (GI disturbances, appetite changes, sleep disturbances)
PLUS increased BP, dry mouth, hyponatraemia
Name the MAOIs.
Isocarboxacid
Phenelzine
What is the mechanism of action of the MAOIs?
Inhibit the enzyme monoamine oxidase.
Prevents inactivation of monoamines (serotonin, NA, dopamine) within the neurone, causing excess neurotransmitter to diffuse into the synaptic cleft.
Why are MAOIs not often used?
Drug-food interactions -
MAOIs also inhibit the breakdown of tyramine, a chemical found in cheese. In excess, tyramine causes the release of large amounts of catecholamines, resulting in a hypertensive crisis.
What are the signs/symptoms of a hypertensive crisis?
HYPERTENSION Occipital headache Stiff neck Tachycardia Nausea Cardiac arrythmias Seizures Stroke
Name the typical antipsychotics.
Haloperidol
Chlorpromazine
Name the atypical antipsychotics.
Olanzapine Risperidone Clozapine Quetiapine Aripiprazole Paliperidone
What is the mechanism of action of antipsychotics?
Inhibition of the dopamine D2 receptors in the CNS (some have actions at other receptors as well)
What is the difference between the atypical and typical antipsychotics?
Atypical antipsychotics produce fewer EP signs and are more effective at treating the negative symptoms of schizophrenia.
What are the indications for clozapine?
Treatment resistant schizophrenia
- Failure of 2 antipsychotics
- One of which should be an atypical antipsychotic
- Over 6-8 weeks each
What are the side effects of clozapine?
AGRANULOCYTOSIS
(Requires regular haemotological monitoring)
Myocarditis