antidepressants Flashcards
gepirone (trade name) is….
drug class?
Exxua
serotonin modulators?
escitalopram (trade name) is….
drug class?
Lexapro
SSRI
paroxetine (trade name) is….
drug class?
Paxil
SSRI
esketamine (trade name) is….
drug class?
Spravato
NMDA receptor antagonists
monoamine theory of depression
depression is due to monoamine deficiency
NTs involved in depression
DA, 5HT, NE, E
DA, 5HT, NE, E are all …
monoamines
second messanger systems in depression
types of antidepressants
MAOIs
Reduce enzymatic deactivation of monoamines
tricyclics
imipramine (Tofranil)
desipramine (Norpramin; active metabolite of Imipramine)
trimipramine (Surmontil)
protriptyline (Vivactil)
amitriptyline (Elavil)
nortriptyline (Pamelor, Aventil; active metabolite of amitriptyline)
doxepin (Adapin, Sinequan)
clomipramine (Anafranil)
how do TCAs work?
Block reuptake of 5-HT, NE
Block post-synaptic H, AChM, NE
what does blockage of H do?
Blockade of H = drowsiness, sedation
what does blockage of AChM do?
SE profiles for TCAs
Blockade of H = drowsiness, sedation
– Blockade of AChM = confusion, memory & cognitive impairment (hippocampus), dry mouth, blurred vision, tachycardia, urinary retention (ANS)
– Blockade of NE receptors = orthostatic hypotension (PNS)
- Side effect profiles vary, depending on affinity for H, AChM,
NE
issues with TCAs
Cardiotoxic in large doses
Risk of OD
what drugs are good for pts w depression and chronic pain? why?
TCAs; analgesic properties
TCAs absorption
MAOIs inhibit ______?
MAOa; Most bind irreversibly to MAOA
issues with MAOIs
Consumption of foods containing high levels of tyramine is problematic
Product of fermentation
“Wine and Cheese Effect”
Increases blood pressure
Adherence to a strict diet eliminates danger
Low TI, so OD is possible
Side Effects
MAOI SE profile?
Sedation
Orthostatic hypotension
Dry mouth
Nervousness
Muscle ache
Paresthesia (pricking or tingling sensation)—usually in extremities
may be from the MAOI’s interference with vitamin B6 metabolism
100 mg of vitamin B6 daily may reduce or eliminate these symptoms
Insomnia
Weight gain
Sexual dysfunction
Anorgasmia (inability to achieve orgasm)
Impotency
Urinary difficulty
selegiline is a _____; it is different than others because _____
MAOI; it is transdermally applied so no issues w GI tract
SSRIs
(common ones and their trade names)
Fluoxetine (Prozac)
Sertraline (Zoloft)
Fluvoxamine (Luvox)
Citalopram (Celexa)
Escitalopram (Lexapro)
how do SSRIs work?
Do not bind to 5-HT receptors, rather make 5-HT more available to
bind with receptors
side effects of SSRIs
withdrawal syndrome
sexual dysfunction
serotonin syndrome
what is serotonin syndrome? what causes it ?
High doses, combination of SSRI with another 5-HT agonist
Cognitive disturbances, agitation, ANS dysfunction (like high fevers) motor problems, hallucinations