Antidepressant drugs Flashcards
Antidepressant drugs
- all can be used for prolonged treatment
- all may decrease seizure threshold
- TCAs
- imipramine
- maprotiline
- amoxapine
- clomipramine
- nortriptyline
- amitriptyline
- desipramine
- SSRIs
- fluoxetine
- fluvoxamine
- paroxetine
- citalopram
- sertraline
- SNRIs
- venlafaxine
- desvenlafaxine
- duloxetine
- milnacipran
- MAOIs
- phenelzine
- tranylcypromine
- selegiline
- rasagiline
- Atypical antidepressant durgs
- buproprione
- mirtazapine
- nefazodone
- trazodone
Drugs for bipolar disorders
- Antiepileptics
- carbamazepine
- valproic acid
- lamotrigine
- Atypical antipsychotics
- risperidone
- olanzapine
- ziprasidone
- aripiprazole
- Lithium salts
TCAs
- imipramine
- maprotiline
- amoxapine
- clomipramine
- nortriptyline
- amitriptyline
- desipramine
MOA:
- inhibition NT reuptake (NE, 5-HT) into presynaptic nn terminals
- blocking Rs: 5-HT Rs, a Rs, His and M Rs
- amoxapine also blocks D2 Rs
PK:
- well absorbed orally
- penetrate BBB
- HL aprox 15hs
- variable 1st pass
- metabolized by CYP450
Drug interactions:
- CYP450
- w/ ethanol, anaesthetics and other antidopaminergic
TU:
- mild-moderate depression
- [anic disorders
- neuropathic pain (amitriptyline) and migraine
- improve mood
- increase physical activity
- in 50-70%
- doesn’t help healthy pts
- takes at least 2 weeks for these actins to happen
AE:
- antimuscarinic
- arrhythmias
- orthostatic hypotension (imipramine)
- sedation
- weight gain
- narrow therapeutic index, dangerous in overdose
- CNS -> excitement, delirium
Effectiveness:
- vary inability to inhibit NE and 5-HT
- alternative for pts that don’t responde to SSRIs
SSRIs
- fluoxetine
- fluvoxamine
- paroxetine
- citalopram
- sertraline
MOA: specificaaly inhibit 5-HT reuptake -> increase [ ] in synaptic cleft
PK:
- p.o
- HL = 16-36hs
- metabolism is P450-dependent and glucuronide
- HL = 50h
- sustained release
- metabolite = potent
- and fluoxetine is a potent inhibitor of CYP450 isoenzyme 2D6
TU:
- drugs of choice!!
- for moderate depression
- fluoxetine takes at least 2 weeks to produce effects
AE:
- headache, sweating
- anxiety, agitation
- GI effects
- insomnia
- sexual dysfunction
- increase risk serotonin syndrome when combined w/ drugs enhancing 5-HT transmission
- discontinuation syndrome -> all potential w/ abrupt withdrawal w/ shorter HL = very increased risk
- fluoxetine - lowest risk
Effectiveness: as effective as TCA less likely to cause anticholinergic effects and less dangerous in overdose
SNRIs
- venlafaxine
- desvenlafaxine
- duloxetine
- milnacipran
MOA:
- newer compounds
- relatively non-selective
TU:
- depression
- relieve the physiological symptoms of neuropathic pain
AE:
- little activity at other Rs -> fewer AR; saferin overdose
- duloxetine -> hepatotoxicity, GIT side effects
- venlafaxine -> mild inhibitor of dopamine reuptake (high doses)
Effectiveness: used in pts in whom SSRIs are ineffective
Buproprione
MOA: weak dopamine and NE reuptake inhibitor
TU: decrease craving and attenuates withdrawl symptoms for nicotine
AE: very low incidence of sexual dysfunction, relatively low risk for drug interaction
Mirtazapine
MOA: blocks a2 presynaptic and 5-HT2 Rs
TU: may act more rapidly than other antidopamine
AE: sedating and weight gain
Trazadone
MOA: weak inhibitor of 5-HT reuptake and block postsynaptic 5-HT2A R
AE: w/ chronic use -> may desensitize Rs 50HT1A presynaptic and increase 5-HT release sedating
MAOIs
- phenelzine
- tranylcypromine
- selegiline
- rasagiline
TU:
- pts unresponsive to TCA / allergic
- strong anxiety
- low psychomotor ability
- phobic satates
- atypical depression
AE:
- drug and food interactions
- tyramine -> cheesy reaction
- phentolamine, prazosine -> HT
- hypotension
- atropine-like side effects
- increase appetite, weight gain
- excessive central stimulation
- life-threatening serotonins (MAOI and SSRIs should not be coadministered)
- phenelzine -> very rarely, hepatotoxicity
