antidepressants and mood stabilizers Flashcards
Depression
chemical imbalance between 3 neurotransmitters
- norepinephrine
- serotonin
- dopamine
Antidepressants
- orally administered
- 90-95%bound to plasma proteins
- metabolized by the liver with metabolites excreted in urine
- long half lives
- relatively small therapeutic index
Classes of antidepressant drugs
- tricyclics
- Selective Serotoni Reuptake Inhibitors (SSRI’s)
- Sellective Serotonin and Norepinephrine Reuptake Inhibitors (SNRI’s)
- Atypical
- Monoamine Oxidase Inhibitors (MAOI’s)
Tricyclics
Attempt to remedy depression by inactivating the amine pump on the presynaptic nere terminal and limiting the reuptake of both NE and serotonin. May also have effects at muscarinic, histamine , and alpha receptors.
Tertiary Amine Tricyclics
-amitryptyline-can be given IM
Tertiary Amine Tricyclics
-clomipramine - given for OCD, not very selective,
can cause seizures
Doxepin (sinequan)
- tertiary amine tricyclics
- increased sedation
- no CV side effects
Imipramine (Tofranil)
- Tertiary amine tricyclic
- can be given IM
- long actin pamoate formula is available
Trimipramine (Surmontil)
-Tertiary Amine Tricyclic
Secondary Amine Tricyclics
- RX for sleepy depressive
- have affinity for serotonin and added affinity for the NE transporter
- add back the sympathetic component
Amoxapine (Asendin)
-Secondary Amine Tricyclic
_dibenzodiazipe that is a metabolite of the antipsychotic loxapine
-It has a dopaminergic and adrenergic mechanism
Desipramine (norpram)
- Secondary Amine Tricyclics
- metabolite of imipramine
-
maprotiline (ludiomil)
_Secondary Amine Tricyclic
- new
- increased ptotential for seizures
nortryptyline (pamelor)
- Secondary Amine Tricyclic
- metaolite of amitryptyline
- elderly patients
protryptryptyline (vivactil)
- Secondary Amine Tricyclic
- lacks sedative properties
- RX for sleepy depressives
Selective Serotonin Reuptake Inhibitors (SSRI’s)
- often 1st choice for monopolar depression
- most effective in the treatment for premenstrual dysphoric disorder (PMDD)
- safer side effect profile
- work on the serotonin side
citalopram (celexa)
-SSRI
-
escitalopram (lexapro)
- SSRI
- adolescents approved
fluoxetine (prozac)
- SSRI
- 72 hr half life
fluvoxamine (luvox)
-SSRI
Paroxetine (paxil)
- SSRI
- anticholinergic side effects
- social phobia
setraline (zoloft)
-SSRI
36 hr half life
Selective Serotonin and Norepinephrine Reuptake Inhibitors (SNRI’s)
-fewer antimuscarinic and antihistaminic effects than the tricyclics and have more of an adrenergic effect compared to the SSRIs
duloxetine (cymbalta)
- SNRI
- 1:10 affinidy for serotonin (5-HT) and NE transporters
- First approval drug for fibromyalgia
milnacipran (ixel)
- SNRI
- 1:1 affinity for 5 HT and NE transporters
- second approved drug for fibromyalgia
venlafazine (effexor)
- SNRI
- withdrawal and rebound effects
- 1:30 affinity for the 5 HT and NE transporters
desvenlafaxine (pritiq)
- SNRI
- isomer of venlafaxine
Atypical
do not fit in any catagory
bupropion (wellbutrin/zyban)
- Atypical
- no sexual side effects
- no serotonin
- block reuptake of dopamins, NE
- 3 fold increase in risk of seizures
nefazodone (serzone)
-BLACK BOX -liver failure (life threatening)
-serotonergic mechanisms
-
mirtazapine (remeron)
- Atypical
- sedation common adverse effect
- blocks histamine receptors
- block 5 HT2A, alpha 1 and alpha 2 centrall receptors
reboxetine (edronax)
- Atypical
- inhibits NE
trazadone (desyrel)
- Atypical
- sedative hypnotic for those with difficulty sleeping
- drug of choice for sleep
- priapism
vilazodone (viibryd)
- Atypical
- new “dual action”
- blocks sertonin reuptake transporter and acts as a partial agonist at the 5HT1Areceptor
- low incidence of sexual side effects
Monoamine Oxidase Inhibitors (MAOI’s)
- refractory depression
- inactivates the enzyme (MAO) that metabolizes NE and serotonin
MAOI’s
- isocarboxazid (marplan)
- phenelzine (nardil)
- tranylcypromine (Parnate)
antidepressant side effects
- sedation
- CV- orthostatic hypotension, tacycardia,