Antidepressants lecture Flashcards
How long to titrate dose
7 to 10 days
How long is each dose trial
4 to 6, but at least 4 weeks
How long do you keep someone on a dose if its working?
6+ months
Slightly more effective antidepressants?
Paroxetine, escitalopram, venlafaxine, mirtazapine, vortioxetine, amitripyline
1st gen?
MAOI, TCA, TeCAs
2nd gen?
-2nd gen MC
SSRI, SNRI, atypical, serotonin modulators, ketamine
SSRIs
MOA, Dosing, CI, SE, metabolism, why do we use them
we use them because
well tolerated good efficacy. 1st line for MDD
MOA- decreases pump of serotonin reuptake which makes more serotonin in the synapse
Dose- QAM
Metabolized in liver
CI- Allergy or MAOI in last two weeks
SE- GI upset (N/D, anorexia), Sleep change (up or down), Neuro (dizzy, HA), Sexual dusfunction (ED, libido down, anorgasmia), anxiety increases, SI increases
other SE- prolonged QT, wt gain, bleeding, orthostatic hypotension, serotonin syndrome
Name the SSRIs
Sertraline, ciralopram, escitalopram, fluoxetine, paroxetine, fluvoxamine
Longest half life of SSRIs-
Prozac (Fluoxetine) 3 d
If a pt wants to start a MAOI, they have to wait 5 weeks for prozac long half life
When can you expect serotonin syndrome to occur?
within 24 of starting them on a new med. often within 6 hours.
signs of serotonin syndrome? how do you know its serotonin syndrome?
no labs! clinical dx.
Give them benzodiazepines, hydrate
Signs and symptoms: diarrhea, increased bowel sounds, agitation, hyperreflexia, dry mucous membranes, autonomic instabliity, hyperthermia, HTN, tremor, clonus, seizure, death
Sertraline
SE? who gets it?
MC GI upset, diarrhea
likely for insomnia
Less prolonged QT
Most well tolerated
For pregnant
Citalopram/Escitalopram
escitalopram is an isomer of citalopram.
-MC prolonged QT
-easier on liver. least inhibition of hepatic cytochrome enzymes.
-minimal SE profile
FluvoxAMine
shortest half life (15 hrs)
somnolence (drowsy). good for sleep
Most drug interactions (DDI) of 2 cytochromes
**AM meaning you see the morning, sleep through the night
most drug interactions! associate someone about to sleep, and they take all of their pills beforehand
shortest half life because it is the opposite of fluvoxETine
FluoxETine
prozac
longest half life (3 d)
insomnia
anxiety
CI tamoxifen
*ET like the alien with a bra walking around at night
anxiety and insomnia because its opposite of fluoxAMine
Paroxetine
anticholinergic SE
orthostatic hypotension
wt gain
sexual dusfunction
DDI (2 cytochrome systems)
CI tamoxifen
SNRIs - are they used 1st line?
yes, just as much as SSRIs
or 2nd line if can’t tolerate SSRI
SNRI
MOA, dosing, CI, side effects, metabolism
blocks reuptake of 5-HT, and norephinephrine, increases levels in the synapse
qd
kidneys and liver
CI- within 2 weeks of MAOI, allergy, angle closure glaucoma
SE - not as much weight gain as SSRI
GI (N/V/D), dry mouth, constipation, sleep (up or down), HA&dizzy, sexual dysfunction (ED may be less), anxiety, SI, diaphoresis, hypertension, serotonin syndrome
SNRIs name them
**Venlafaxine
Desvenlafaxine
Duloxetine **
Milnacipran
Levomilnacipran
Venlafaxine
SNRI
SE:
Elevated BP
higher N/V
higher SI
think of a vanilla vaccine
you push out some while its upside down (hypertension)
N/V b/c the vanilla doesn’t sit right with the stomach
higher SI because its terrible to only have vanilla
Desvenlafaxine
synthetic metabolite of venlafaxine
SE:
Less HTN & less SE than venlafaxine
“des” = dis as in away or less
vanilla vaccine
Duloxetine
SNRI
Hepatic cytochrome inhibition so more likely to have DDIs
least hypertensive SE
chronic pain indication
Dual - ox - time
Dual because both NE and serotonin
Ox that is standing in the way of drugs (liver cytochrome inhibition)
Imagine stopwatch with two modes. one mode is a slow stream of water and the other mode is ox mode - take on liver metabolism and pain
Milnacipran/Levomilnacipran
SNRI
pseudo-anticholinergic effects (urinary ret, const, dry mou)
used more for pain relief than MDD
** Milk na- sip- ran
When you drink too much milk you get thirsy (drying)
warm Milk is soothing, associate with pain relief
Atypical Anti
2nd line if fail SSRI
1st line in only special cases
Bupropion, Mirtazapine,
Buproprion
MOA
Atypical
MOA- dopamine-NE reuptake inhibitor, antagoniszes nicotinic
for a smoker that can’t take SSRI
SE- dry mouth, insomnia, nausea, seizures more likely
indicated: tobacco cessation, don’t want wt gained from SSRIs, or sexual dysfunct from SSRIs
CI: epilepsy patients, eating disorder (who need to gain weight), or 2 weeks within MAOI
lots of DDI.
- A blue tailed skinny cigarrette plane
- Skinny Dildo plane
Mirtazapine
MOA- Antagonizes alpha 2, 5HT2, 5HT3, which causes incr rel. of serotonin and NE
SE dry mouth, drowsiness, huge weight gain, appetitie incr, sexual dysfunction (less than SSRI), SI.
Less orthostatic hypotension.
indicated for someone with insomnia b/c it causes drowsiness. its good for someone who is too skinny.
fewer DDIs than buproprion
“My Taz Apples”
-Tazmanian devil is a cartoon. he eats tons of apples because he has a big appetite. after eating so many apples he feels full and sleepy. plus all the sugar makes him thirsty.
There’s a small stream in the background indicating less orthostatic hypotension.
Serotonin Modulators
tell me the names and the MOA, the dosing, CI, and SE for all, metabolism
2nd line for who can’t tolerate SSRIs
Nefazodone
Trazodone
Vilazodone
Vortioxetine
QD or BID
Liver
CI within 2 weeks of MAOI
SE- headache, diarrhea, nausea. SI, serotonin syndrome less than SSRI
Nefazodone
like trazodone, it antagonizes 5 HT receptor, incr rel of serotonin
BBW hepatotoxcity (liver disease or elevated liver enzymes)
SE: HA, agitation, dizzy, drowsiness, insomnia, xerostomnia, hypotension
no sexual side effects
less GI upset
less weight gain
- nefarious (for liver toxicity)
- the bad boy who gets laid, is in shape, and isn’t running off to the bathroom
Trazodone
MOA
SE:
sedation, nausea, dry mouth, fatigue, constipation, sexual dysfunction
Rare- Priapism, cardiac arrythmia
Weight NEUTRAL,
no sexual side effects (or less)
“Trail - Zone”
-hook up on the trail (priapism), weight neutral because you can both walk & rest.
the trail is relaxing = sedation
the trail is up a rugged mountain so cardiac arrythmia
Vilazodone
SE: HA, diarrhea, nausea, sexual dysfunction
MOA: partial agonist of 5HT receptors
fast onset
less sexual dysfunction
Picture a luxurious villa zone where you go to relax and unwind. Vilazodone, like staying in a villa, helps elevate your mood quickly.
It’s a foreign spanish villa.
Diarrhea/N from the foreign food.
Vortioxetine
serotonin modulator
dizzy, N/V/D/C
fast onset
less sexual dysfunction
*vortex whirlpool that makes you dizzy and the other symptoms
fast rapids so fast onset
with a banana
Ketamine
general. how long? who is it indicated for? what does it do for the patient?
CI: psychotic symptoms
-Indicated for severe refactory depression w/o psychosis
-who failed ECT
given as IV (ketamine)
given as nasal spray (esketamine)
rapid robust improvement in depression that fades in two weeks
short term therapy only due to neurotoxicity in the long term
-can induce psychotomimetric effects (induce psychosis)
-outpatient clinics w/ restricted distribution system
-if used patients will eventually be switched to antidepressants or antipsychotics for the long term
Ketamine
specific
MOA- opioid AMPA (glutamate agaonist), NMDA antagonist
SE- psychomimetic, HTN, tachycard, anxiety, dizzy, HA
Long term - abuse/addiction, neurotoxicty, bladder toxic, hepatotoxic
CI: anureism, AV malform, ICH, can’t increase BP
DDI- CNS depressants like opiates
MAOI
MOA? drug names?
MAOa breaks down serotonin and NE
MAOb works with MAOa to break down dopamine
Tranylcypromine
Phenelzine
Isocarboxazid
Selegiline
a is the one in charge while b is second in command
MAOI
indications
Extensive side effects, DDIs, and dietary restrictions
Usually only for treatment-resistant or atypical depression
MAOI
CI , DDI, SE
SI- CVD, pheochromocytoma, liver/kidney impair, 2 weeks within other serotonergic drugs. Selegiline is less CI than other MAOIs
DDI numerous
SE- hypotension, GI upset, urinary hesitancy, HA, myoclonic jerks, edema, SI, Hypertensive crisis (180/120) when consuming tyramine
Tyramine- aged cheese, soy sauce, cured measts, tap beer, tofu, sauerkraut (selegiline less so)
TCAs
names, indication, MOA for types
2nd line for depression due to side effects
-treats anxiety, pain
MOA inhibits reuptake of 5-HT and NE
Tertiary amines incr serotonin more
-amitriptyline, doxepin, imipramine, clomipramine, trimipramine
Secondary amines incr NE more
-nortriptyline, desipramine, protriptyline
secondary : mem * Norepi Drive Pack for notrip, desipram, protrip
tertiary mem * mom ADICT (ammi, doxe, imi, clim, tri)
TCAs
dose, CI, SE
low doses!
CI: 2 weeks of MAOI, in acute recovery of an MI
SE: anticholinergic, sexual dysfunction, diaphoresis, tremor, wt gain, incr appetite, SI, cardiotoxicity (prolonged QT), fatal overdose
nortriptyline and desipramine have best tolerability.
think desi pram is a stroller and nortrip is a trip up north. they complement each other well so they both have good side effect profiles
TeCAs
similar to TCAs
have an extra cyclic ring
refractory or atypical depression only
Maprotiline- MOA - block reup NE 5-HT
Amoxapine- MOA - block reup NE. block dopamine receptors.
SE is less anticholinergic SE but more histamine like than TCAs, still have SI
