Anti-depressant Flashcards
Name MAO-A Inhibitor
- moclobemide
- clorgyline
-> selective and reversible
(unlike irreversible MAO-B I selegiline)
Interaction of MAO-A inhibitor
- cheese reaction
- react with many food and drugs which contain large quantities of tyramine
- (beer, yeast, cheese, pickled meat)
- tyramine acts as catecholamine in MAO inhibited patient
-> vasoconstriction and hypertension
*-> less likely to produce cheese reaction in selective and reversible
Advantage of moclobemide
- lacks adverse effects of TCAs
-> alternative option in elderly patients and those with heart disease
Adverse effects of moclobemide
- nausea/ dizziness/ headache/ insomnia
- caution while co-prescribing pethidine, SSRIs and TCAs
Name tricyclic antidepressants
- Amitriptyline (-> Nortriptyline)
- Imipramine (-> Desipramine)
TCA antidepressant MOA
- inhibit NET (norepinephrine transporter) and serotonin transporter (SERT) at neuronal and platelet membrane
Name side effects of TCAs
- anti cholinergic: dry mouth, constipation, urinary retention
- sedation
- increased appetite and wg
TCAs interaction
- potentiate sympathomimetics amines -> avoid adrenaline containing amine
- potentiate CNS depressants
- concurrent MAOI -> hypertensive crisis
Name SSRIs (selective serotonin reuptake inhibitor)
- fluoxetine
- citalopram
- paroxetine
- sertraline
SSRIs general interaction
- serotonin syndrome
-> when concurrent use with serotonergic drugs: MAOI, tramadol, pethidine
Fluoxetine
- longest acting SSRIs
- approved for use in children 7 y/o or older for depression/ OCD
Setraline
juvenile depression efficacy
Name SNRIs (serotonin and noradrenaline reuptake inhibitor) and prominent side effects
- venlafaxine
- nausea/ sweating/ anxiety/ withdrawal syndrome
Name four atypical antidepressants
- trazodone
- mianserin
- mirtazapine
- bupropion
Trazodone
- major drug target: 5HT2A receptor (acts as antagonists) -> directly involve in mood control
- less effective 5HT reuptake blocker, prominent adrenergic bloker -> hypotension
- metabolite strong 5HT2 blocker
- less prone to arrhythmia
- prolonged and painful penile erection
Mianserin
- block presynaptic a2 receptors -> increase release and turnover of NA -> antidepressant effect
- not inhibit uptake of 5HT/ NA
- overdose seizure
- blood dyscrasias
Mirtazapine
- block a2 receptors -> enhance NA and 5 HT release
- NA further increase serotonergic raphe neurons firing via a1 receptors
- selective enhancement of antidepressive 5HT1 receptor -achieved by concurrent blockade of 5HT2 and 3 receptors
Bupropion
- inhibit DA and NA uptake -> excitant effect
- metabolize into amphetamine-like compound -> presynaptic release of DA and NA
- contraindicated in eating disorder and bipolar
- infrequently use - except with atypical features
Treatment for severely depressed
Electroconvulsive therapy
Bipolar disorder drug treatment x3
- anti epileptic drug
- lithium
- atypical antipsychotics (olanzapine, aripriprazole)
=> mood stabilizer
Lithium effect
- calming effect/ mood stabilizer -> treat acute mania
- prophylaxis of recurrent manic and depressive episodes
- anti suicidal effect
Lithium MOA
- dopamine pathway - decrease dopamine transmission
- glutamate pathway
- downregulate NMDA receptor
- modulate associated myoinositol second messenger system -> long term change in neurotransmission and gene transcription
- GABA pathway
- increase level of GABA
- directly activate GABA receptor - Second messenger systems
- cAMP: increase AC, cAMP and CREB (cAMP response element binding protein)
- PI signalling
- suppress GSK-3 (glycogen synthase kinase -3)
-> transcriptional regulation
-> gene expression
-> mood stabilizer
Lithium interactions
- diuretics: cause plasma Li+ level to rise
- NSAID, tetracycline, ACEI: lithium retention
- neurotoxicity with haloperidol, carbamazepine, chlorpromazine
Lithium overdose
- muscle twitching
- coma
- drowsiness