L1 Antidepressants Flashcards
5-HT is broken down mainly by
MAO-A
Noradrenaline is broken down mainly by
MAO-A and MAO-B
Dopamine is broken down mainly by
MAO-A and MAO-b
What is the type of MAOi used in Parkinson’s disease?
MAO-B
Phenelzine is: (2)
- non-selective for MAO-A vs MAO-B
- and irreversible MAOi
ADR of MAOis
- postural hypotension - dopamine as inhibitory neurotransmitter, cervical block
- restlessness or insomnia - CNS stimulation
- should not be combined with other drugs with seretoninergic function eg. pethidine - myoclonus, hyperexcitability, loss of consciousness, increased muscular tone
Significant drug-food interaction related to the use of MAOIs (also its major limitation)
the ‘cheese’ reaction
- cheeses and concentrated yeast products eg. marmites
Tyramine has a high affinity for
NA transporters
TCAs were initially produced as
potential antipsychotic drugs in 1949, but found to be ineffective in schizophrenia
Examples of non-selective TCAs
imipramine, amitriptyline, nortriptyline
Example of NET-selective TCA
desipramine
Which one of the non-selective TCAs has the mildest side effect profile?
nortriptyline
ADR of TCAs (4)
- sedation - H1 antagonism, tolerance can be developed in 1-2weeks
- postural hypotension - a-adrenoceptor sympathetic block
- dry mouth, blurred vision, constipation - muscarinic receptor antagonism
- ddi - rely on hepatic metabolism
Which is the first drug class to be developed for the purpose of antidepressant treatment?
SSRIs
What is the mostly widely prescribed antidepressant currently?
Fluoxetine
3 key advantages of SSRIs
- low affinity for alpha-adrenoceptors
- low affinity for muscarinic cholinergic receptors
- lack of effect at histamine receptors