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Flashcards in Antidepressants Deck (34):
1

What is the hypothesis behind mood

major depressive disorders result from a functional deficiency of NE or 5-HT at synapses in CNS
Neurotropic and endocrine components

2

Neurotropic hypothesis of major depression is

Changes in tropic factors and hormones play a major role
Successful treatment results in changes in:
CREB (cAMP response element binding)
BDNF (brain derived neurotrophic factor

3

What do monoamine NT do and how do antidepressants take advantage

Carry messages between cells
Initiate cascade of events
Reabsorbed back into nerve cells
-Most antidepressants inhibit transporter reuptake molecules so the NT stay in the synapse longer

4

What is the amine hypothesis of major depression and how do antidepressants use this

Depression is associated with changes in serotonin or NE
Many antidepressants cause changes in amine signaling!

5

What neuroendocrine factors are associated with depression

Thyroid dysregulation
Estrogen deficiency
Testosterone deficiency
More severe depression: Abnormal HPA axis, elevated cortisol

6

What are the phases of MDD treatment

Acute: 6-12 weeks. goal is remission (eliminate Sx)
Continuation: 4-9 months after remission. goal is prevent relapse and eliminate residual Sx
Maintenance: 12-36 months. goal is prevent recurrence

7

What meds are associated with inducing depressive Sx

Isotretinoin
Anticonvulsants
Triptans
BB, clonidine, methyldopa, reserpine
Hormone therapy
interferons
varenicline (smoking cessation)

8

What drugs are used as antidepressants

TCA
MAOI
SSRI
SNRI
5HT2
heterocyclic antidepressants

9

What is the PK of antidepressants (general overview)

Rapid oral absorption
Peak plasma in 2-3 hours
Tightly bound to plasma proteins
Hepatic metabolism
Renally cleared

10

Antidepressants can be used to Tx

MDD
panic disorder
GAD
PTSD
OCD
Neuropathic pain, fibromyalgia, PMDD, menopause vasomotor Sx, stress incontinence

11

What are TCA

Block re-uptake transporters of NE and 5-HT
Used in MDD, *chronic pain, *enuresis, and insomnia
-Amitriptyline, Imipramine, Desipramine, Doxepin, Nortriptyline

12

What are ADE of TCA

muscarinic block (anticholinergic)
sedation
weight gain
OD: arrhythmia, seizure

13

What are the most potent TCA's

Most potent 5-HT blockers: Ami, Imi
Most potent NE blocker: Desi, Nor
-highest potency drugs have the most ADE!

14

What are MAO inhibitors

Inhibit monoamine oxidases that normally metabolize NE and serotonin (type A) and dopamine (type B)
Used in unresponsive MDD, anxiety, panic d/o
Selegiline in parkinson's (MAO-B)
-Phenelzine, Tranylcypromine, selegeline

15

MAOI interact with what drugs

Tyramine and sympathomimetics: cause HTN
SSRI: cause serotonin syndrome

16

Toxicities of MAOI are

Hypotension
Insomnia

17

Those on MAOI should avoid these foods (only a few big ones)

dairy
beer
wine
canned aged meat
sardines
liver
yeast
pod beans
chocolate
coffee
licorice
soy sauce

18

What are SSRIs

Selectively inhibit 5-HT transporters w/ modest effects on other NT (fluoxetine and paroxetine mildly block NE)
Used for MDD, GAD, PTSD, OCD, panic d/o, PMDD, bulimia
-Citalopram, Escitalopram, Fluoxetine*, Paroxetnie, Sertraline

19

SSRI interact with

Warfarin*: alprazolam and theophylline increase blood levels
lithium
TCA

20

ADE of SSRI are

anxiety, insomnia, nausea, serotonin syndrome, sexual dysfunction
citalopram: QT prolongation
fluoxetine: anorexia
fluvoxetine: somnolence
paroxetine: anticholinergic ADE (mildly blocks NE)

21

Bolded dosing info on SSRI's

Citalopram: do not dose >40mg/d to avoid QT prolongation risk
Escitalopram: can increase to max dose after 1 week

22

What ADE is common to all antidepressants

Suicidality; Increased risk if <24, Decreased risk if >65
Monitor for behavioral changes and mental status

23

What are SNRI

heterocyclic drugs that block NE and 5HT transporters but LACK alpha blocking, anticholinergic, and antihistaminic actions of TCA
Used for MDD, FAD, neuropathies, fibromyalgia, SUI, and menopause vasomotor Sx
-Venlafaxine*, duloxetine, levomilnacipran

24

ADE of SNRI are

HTN/tachy , insomnia, nausea, serotonin syndrome, sexual dysfunction
dose dependent HTN: venlafaxine
orthostatic hypotension: Duloxetine
HLD: desvenlafaxine
Seizures (venlafaxine, desvenlafaxine)

25

Bolded dosing info on SNRI newer generation

Desvenlafaxine ADE are increased with higher dose, but benefits do not increase with dose
Venlafaxine: reduce dose if sustained HTN occurs

26

What are mixed 5-HT2 antagonists/5-HT1a enhancers

Block 5-HT2 receptors with minor effects on amine transporters
Used for MDD and hypnotics
-Trazodone, Nefazodone, Vilazodone, Vortioxetine

27

ADE of mixed serotonergics are

Nef: hepatic toxicity
Traz: sedation, orthostatic hypotension
Vila: serotonin syndrome, decreased male libido
Vori: GI and sexual dysfunction
Depression and anxiety
Depression with cognitive difficulties

28

What is Buproprion

NE and dopamine reuptake inhibitor
Used in smoking cessation and MDD
May cause seizures (dose related, and increased w/ alcohol withdrawal, head trauma, CNS tumor)

29

What is Miratazepine

Presynaptic a2 blocker w/ some effect on 5-HT
Used for sedation
May cause sedation and weight gain

30

Choose an antidepressant based on

indication
cost
availability
ADE
potential drug interactions
Pt Hx
Pt preference
age and gender
medical status

31

What are non-med options in treating depression

Electorconvulsive therapy
Repetitive Transcranial Magnetic Stimulation

32

What supplements an help Tx depression

Omega 3 fatty acids (EPA +/- DHA): used to augment Tx of MDD
St john's wort: mild-mod MDD. induces hepatic metabolic enzymes
SAMe: under review by task force
Folate: involved in synthesis of new NT, like 5-HT. Reasonable to augment MDD Tx with the 3 compounds

33

What are the 3 folate compounds used in augmenting Tx of MDD

Folic acid
Folinic acid
5-Methyltetrahydrofolate

34

Does exercise play a role in treating depression

Yes! a recent study even confirmed the benefit of exercise on depression
16 kcal/kg/wk exercise associated with greater remission rates in conjunction with an SSRI
Task force says to include exercise in Tx of MDD!