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521-Pharmacology > Antidepressants > Flashcards

Antidepressants Flashcards

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
Q

Desipramine

A

TCA
-more NET inhibition
-more selective

25
Q

two 5-HT receptor modulators(antagonists)

A

-Trazodone
-Vortioxetine

26
Q

Bupropion

A

-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
Q

Mirtazapine

A

-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
Q

Amoxapine and Maprotiline

A

-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
Q

Vilazodone

A

-potentially binds to serotonin transporter, but minamally to dopamine and norepi transporters
-partial agonist of the 5-HT1A receptor

30
Q

MAOIs

A

-used for unresponsive depression
-some MAOIs resemple amphetamines and selegiline has amphetamine like metabolites

31
Q

Phenelzime

A

MAOI

32
Q

Isocarboxazid

A

MAOI

33
Q

Tranylcypromine

A

MAOI

34
Q

Selegiline

A

MAOI
-transdermal and sublingual forms bypass liver and gut

35
Q

Atypical antipsychotics

A

-used to treat schizophrenia, bipolar, depression with psychotic features, and MDD without psychotic features

36
Q

Aripiprazole or quetiapine

A

-atypical antipsychotic with SSRI and SNRI

37
Q

Olanzapine with fluoxetine

A

-treatment resistant major depression
-following inadequate response to at least two antidepressants

38
Q

Quetiapine

A

-atypical antipsychotics
-may have antidepressant activity alone

39
Q

Brexiprazole

A

-atypical antipsychotic
-FDA approved for major depression

40
Q

OTC antidepressants

A

-ST John;s wort: Seratonin syndrome
-S-adenosylmethionine (SAMe)
-Omega-3 fatty acids: mania in BP
-5-hydroxytryptophan (5-HTP)
-Dehydroepiandrosterone (DHEA): mania

41
Q

Delay in onset of antidepressants

A

-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
Q

Serotonin syndrome

A

-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
Q

SSRI effect on SERT

A

-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
Q

SNRIs target

A

-inhibit serotonin and norepi transporters
-tend to have greater affinity for SERT than NET

45
Q

Pharmacodynamics of TCAs

A

-activity is related to inhibition of serotonin and norepi reuptake
-common adverse effects
-tend to be potent histamine H1 receptor antagonists

46
Q

Trazodone

A

-inhibits 5-HT2A
-agonists of this receptor are hallucinogenics and anxigenic
-weak, but selective, inhibitor of SERT
-moderate H1 antagonist

47
Q

Vortioxetine

A

-multimodal effects on many 5-HT receptors
-allosteric inhibitor of SERT

48
Q

Why do 5-HT 2 receptor antagonists have
antidepressant effects?

A

-depressed patients have more 5-HT2A receptors
-over density of receptors suggests involvement of depression
-SSRI downregulate receptors

49
Q

Pharmacodynamics of MAOIs

A

-mitigating the actions of MAO in the neuron and increasing
monoamine content
-two types

49
Q

MAO-A

A

-present in both DA and NE neurons
-primary substrates are NE and 5-HT

50
Q

MAO-B

A

-found primarily in serotonergic and histaminergic neurons
-primary acts on DA

51
Q

Phenelzine and tranylcypromine

A

-irreversible
-non selective MAOIs

52
Q

Selegiline

A

-irreversible MAO-B specific drug at low doses(Parkinson’s)
- nonselective MAOI at high doses

53
Q

Shared features of antidepressants

A

-rapid oral absorption
peak plasma within 2-3 hours
-tightly bound to plasma protein
-undergo hepatic metabolism
-renally cleared

54
Q

Fluoxetine

A

-SSRI
-metabolized into active product: norfluoxetine
-longest half life of all SSRIs
-Need to discontinue for 4 weeks before starting MAOI: serotonin sndrome

55
Q

Selective SNRIs

A

-Venlafaxine -> desvenlafaxine
-duloxetine

56
Q

pharmacokinetics of duloxetine

A

-metabolized by 2D6 and 1A2
hepatic impairment significantly alters levels

57
Q

pharmacokinetis of TCS

A

-dose at night: sedating
-substrates of 2D6 systems
-TCA serum levels influenced by concurrent fluoxetine

58
Q

pharmacokinetics of MAOIs

A

-extensive first-pass effects that may substantially
decrease bioavailability

521-Pharmacology (11 decks)

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