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521-Pharmacology > Antidepressants > Flashcards

Antidepressants Flashcards

(60 cards)

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1
Q

Major depressive disorder (MDD)

A

-depressed mood most of the time in the last 2 weeks
-AKA major depression or unipolar depression

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2
Q

monoamine hypothesis

A

-idea thar a deficit in function or amount of monoamines is central to the biology of depression

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3
Q

Neurotrophic hypothesis

A

-evidence that neurotrophic factors play a major role in depression
–nerve growth factors such as brain-derived neurotrophic factor (BDNF)
–BDNF activates tyrosine kinase receptor B in neurons and glia

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4
Q

Neuroendocrine factors

A

-association with the number of hormonal abnormalities

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5
Q

Evidence to support the monoamine hypothesis

A

-Reserpine treatment: depression in a subset of patients
-Depressed patients respond to Fluoxetine suffer relapse when given tryptophan free diets
-patients on desipramine less likely to relapse on tryptophan free diets

-all classes of antidepressants enhance availability of 5-HT, NE, DA

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6
Q

Inconsistencies with monoamine hypothesis

A

-many studies found no alteration in function or levels of monoamines in depressed patients
-Glutamate appears to be important
-antidepressants impact glutamate transmission
-Ketamine shows rapid antidepressant effects

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7
Q

Evidence supporting neurotrophic hypothesis

A

-decrease in CSF level of BDNF in patients with depression
-major depression decrease size of hippocampus
-All known classes of antidepressants are associated with an increase in BDNF levels in animal models and humans
(chronic, but not acute, administration)

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8
Q

Inconsistencies with the neurotrophic hypothesis

A

-BDNF knockout mice do not show consistent depressive behavior
-Genetic polymorphisms for BDNF may yield very
different effects
– Mutations in BDNF associated with altered anxiety and
depressive behavior in both animal and human studies

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9
Q

Pathophysiology of depression

A

-abnormalities in HPA axis
-Thyroid dysregulation
-sex steroid are implicated: post pregnancy, testosterone, hormone replacement therapy

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10
Q

Integration of hypotheses regarding the
pathophysiology of depression

A

-monoamine, neurotrophic, and neuroendocrine systems are interrellated
–HPA and steroid abnormalities may suppress transcription of BDNF gene
–chronic stress–>cortisol–>decrease BDNF synthesis
-chronic activation of monoamine receptors by antidepressants increases BDNF expression

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11
Q

SSRIs

A

-inhibit serotonin transporter (SERT)
-indications in GAD, PTSD, OCD, panic disorder, PMDD, and bulimia
-highly lipophilic

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12
Q

mild Serotonin syndrome

A

fever
-sweating
-agitation
tachycardia
-diarrhea
-tremors
-poor coordination

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12
Q

Moderate serotonin syndrome

A

-hyperthermia
-hypomania
-hypertension
-hyperflexia
-clonus
-myoclonus

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13
Q

severe serotonin syndrome

A

-hyperthermia
-seizure
-coma
-death
-rigidity

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14
Q

drugs that block both serotonin and norepinephrine transporters

A

-SNRIs: newer
-TCAs: older

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15
Q

SNRIs

A

-serotonin-norepinephrine reuptake inhibitor
-bind serotonin (SERT) and norepinephrine (NET) transporters

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16
Q

Venlafaxine

A

SNRI
-inhibitor of SERT
-weak inhibitor of NET

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17
Q

desvenlafaxine

A

SNRI
-Inhibit both SERT and NET

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18
Q

Duloxetine

A

SNRI
–Inhibit both SERT and NET

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19
Q

Levomilnacipran

A

SNRI
-more potent inhibitor of NET than SERT

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20
Q

TCAs

A

-used in depression that is unresponsive to more commonly used SSRIs and SNRIs
-share similar structure

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21
Q

Imipramine

A

TCA
-more serotonin effects initially but then metabolite had nor NET inhibition

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22
Q

-tryptyline

A

TCAs

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23
Q

Doxepin

A

TCA

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24
Desipramine
TCA -more NET inhibition -more selective
25
two 5-HT receptor modulators(antagonists)
-Trazodone -Vortioxetine
26
Bupropion
-unicyclic -resembles amphetamine and has CNS activating properties -Not commonly associated with sexual side effecs -modest inhibitors of NET and dopamine reuptake -no effect on serotonin system
27
Mirtazapine
-tetracyclic -not commonly associated with sexual side effects -antagonist of the presynaptic a2 autoreceptor: enhances release of both NE and 5-HT -potent H1 antagonist
28
Amoxapine and Maprotiline
-tetracyclic -comparable to TCAs -not commonly perscribed -potent NET inhibitors and less potent SERT inhibitors -Amoxapine (unlike TCAs) also moderate inhibitor of postsynaptic D2 receptor – antipsychotic properties
29
Vilazodone
-potentially binds to serotonin transporter, but minamally to dopamine and norepi transporters -partial agonist of the 5-HT1A receptor
30
MAOIs
-used for unresponsive depression -some MAOIs resemple amphetamines and selegiline has amphetamine like metabolites
31
Phenelzime
MAOI
32
Isocarboxazid
MAOI
33
Tranylcypromine
MAOI
34
Selegiline
MAOI -transdermal and sublingual forms bypass liver and gut
35
Atypical antipsychotics
-used to treat schizophrenia, bipolar, depression with psychotic features, and MDD without psychotic features
36
Aripiprazole or quetiapine
-atypical antipsychotic with SSRI and SNRI
37
Olanzapine with fluoxetine
-treatment resistant major depression -following inadequate response to at least two antidepressants
38
Quetiapine
-atypical antipsychotics -may have antidepressant activity alone
39
Brexiprazole
-atypical antipsychotic -FDA approved for major depression
40
OTC antidepressants
-ST John;s wort: Seratonin syndrome -S-adenosylmethionine (SAMe) -Omega-3 fatty acids: mania in BP -5-hydroxytryptophan (5-HTP) -Dehydroepiandrosterone (DHEA): mania
41
Delay in onset of antidepressants
-NTs released at low levels and exert autoinhibitory feedback -Short term use of antidepressants result in increased release of NT: increased simulation of inhibitory autoreceptors -chronic used of antidepressants results in downregulation of presynaptic autoreceptors
42
Serotonin syndrome
-glycoprotein with 12 transmembrane regions -located in axon terminal and cell body -Extracellular serotonin binds to transporter, conformational change(serotonin, Na, and Cl moved into cell) -Binding of intracellular K releases serotonin inside of cell
43
SSRI effect on SERT
-allosterically inhibit SERT -not at serotonin site -80% inhibition at therapeutic doses -SERT polymorphisms determine activity of transporters -SSRI habe little effect on other neurotransmitters
44
SNRIs target
-inhibit serotonin and norepi transporters -tend to have greater affinity for SERT than NET
45
Pharmacodynamics of TCAs
-activity is related to inhibition of serotonin and norepi reuptake -common adverse effects -tend to be potent histamine H1 receptor antagonists
46
Trazodone
-inhibits 5-HT2A -agonists of this receptor are hallucinogenics and anxigenic -weak, but selective, inhibitor of SERT -moderate H1 antagonist
47
Vortioxetine
-multimodal effects on many 5-HT receptors -allosteric inhibitor of SERT
48
Why do 5-HT 2 receptor antagonists have antidepressant effects?
-depressed patients have more 5-HT2A receptors -over density of receptors suggests involvement of depression -SSRI downregulate receptors
49
Pharmacodynamics of MAOIs
-mitigating the actions of MAO in the neuron and increasing monoamine content -two types
49
MAO-A
-present in both DA and NE neurons -primary substrates are NE and 5-HT
50
MAO-B
-found primarily in serotonergic and histaminergic neurons -primary acts on DA
51
Phenelzine and tranylcypromine
-irreversible -non selective MAOIs
52
Selegiline
-irreversible MAO-B specific drug at low doses(Parkinson's) - nonselective MAOI at high doses
53
Shared features of antidepressants
-rapid oral absorption peak plasma within 2-3 hours -tightly bound to plasma protein -undergo hepatic metabolism -renally cleared
54
Fluoxetine
-SSRI -metabolized into active product: norfluoxetine -longest half life of all SSRIs -Need to discontinue for 4 weeks before starting MAOI: serotonin sndrome
55
Selective SNRIs
-Venlafaxine -> desvenlafaxine -duloxetine
56
pharmacokinetics of duloxetine
-metabolized by 2D6 and 1A2 hepatic impairment significantly alters levels
57
pharmacokinetis of TCS
-dose at night: sedating -substrates of 2D6 systems -TCA serum levels influenced by concurrent fluoxetine
58
pharmacokinetics of MAOIs
-extensive first-pass effects that may substantially decrease bioavailability

521-Pharmacology (11 decks)

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