Antidepressants Flashcards
What do monoamines do?q
NOT just refill actually..
synaptic plasticity
dendritic morphology
neurogenesis
first generation antidepressants
TCA, MAO-I
second generation antidep
SSRI, SNRI
5 serotonin SSRIs
citalopram escitalopram fluoxteine paroxteine fluvoxamine
serotonin TCA
clomlpramine
NE SNRI
venlafaxine
desvenlafaxine
duloxetine
NE TCA
nortyptillineimipramine
amitriptylline
desipramine
DA NDRI
bupropion
MAOI
phenelzine
tranylcipramine
citalopram mech of action
blocks 5ht reuptake transporter so 5ht stays in synase
can also block DA and NE reuptake by binding to 5HT R
citalopram also
bidnds to closely related 5HT receptors
histamine, DA, muscarinic (dryness), a and b adrenergic
where are 5HT receptors mostly?
raphe nucleus
side effects citalopram (celexa)
GI, sexual, sleep, sweating, Na_, mania
QT prolongation
venlafaxine side effects
GI, sexual, sleep, sweating, Na_, mania
diastolic blood pressure increase
why were tertiary amines bad?
they block Na+ channels in heart, so if you overdose you can get heart block, but secondary are better (all same but weaker side effects)
different between teritary (imipramine/amitriptyline) and secondary (desipramine/nortriptyline) amines
react more with 5HT than NE
tertiary amines work as
Class 1A anti-arhythmics
nortriptyline side effects
wt gain, sedation, Ach, hypotension, arrhythmia, sexual, sweating
nortriptyline is___in overdose
lethal
chlomipramine is
highly specific to 5HT, so its better for OCD
NDRI
NE-DA reuptake I
wellbutrin/bupropion
side effects wellbutrin
insomnia
tremor
tinnitus
seizures
how do MAOIs work?
suicide inhibitors; complelety kills enzyme; doesnt just block enzyme by occupying space, but gets rid of enzyme
even if you stop an MAOI
2 weeks until body makes new enzyme
Phenelzine (nardil)
developed as TB drug, sedating (MAOI)
tranylcypromine (parnate)
developed as amphetamine- stimulating
serotonin syndrome triad
MS seizures
autonomic instablility
neuromuscular signs
clinically, 5ht syndorme..
hypertensive crisis
seizure
stroke
hypertensive crisis
“cheese syndrome”
low tyramine diet needed (because tyramine is a precursor to D and NE)–>SS
NaSSA
dual reuptake
Mirtazapine (remeron)
do not combine Mirtazpine with
P450 drugs (other MAOIs)
side effects Mirtazpine
sedating, wt gain (histamine)
SARI
serotonin 2A antagonist dual reuptake
Nefazodone
trazodone
*can combine with P450 drugs
GABA drugs
benzodiazepines
what are benzos good for
sedative anziolytic seizure control muscle relaxant anterograde amnesia
benzos should never be
combined witha lcohol
benzos act as
positive allosteric modulator
- -increase R affinity for endogenous GABA
- -increase frequency of opening of CL channel when activated by GABA (and Cl makes resting potential more negative–higher activation energy)
Diazepam is…and binds tooo
nonselective
binds to all alpha R wherever they are in brain
side effects diazepam (valium)
sedation depression amnesa ataxia dependence withdrawal
valium/diazepam is metabolized by the
liver
which benzo is renally cleared?
lorazapam
Zolpidem
alpha 2 selective BZD agonist
zolpidem
zalapion
eszopiclone
zolpidem binds
preferentially to a1 receptors
zolpidem is mostly for
sedation
forget what you did
Buspirone/BuSPar
5HT1A partial agonist
for GAD/Augment MDD
side effects buspirone
dizziness, sedation, nervous/restless
how long for buspirone to work
4 weeks, but no withdrawal after
