Tavalin: Antidepressants Flashcards by Robert Ellis

TCA’s

Amitriptyline
Nortriptyline
Doxepin
Protritptyline
trimipramine
desipramine
comipramine

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SSRI’s

fluoxetine-prozac
Citalopram
Escitalopram-lexapro
Paroxetine-paxil
sertraline-zoloft

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atypical antidepressants 2nd and 3rd gen

venlafaxine-effexor
duloxetine-cymbalta
buprprion-wellbutrin
Mirtazapine-remeron
trazadone
OLEPTRO -ER trazadone

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MAOIs

trancylopromine
Isocarboxazid
Phenelzine

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mood stabilizers

lithium
valproate
carbemazepine

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biogenic amine hypothesis

functional deficit of monoamines-NE and Serotonin- involved in the pathophys of depression

*therefore antidepressants act to increase levels of monoamines

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three types fo depression

secondary/reactive-60%
endogenoud-unipolar-25%-more common in women, pre-post partem-20-40
bipolar-manic depression-15% can be misdiagnosed as endogenous is mania is missed

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NRI’s and SNRI’s belong to which class

atypical antipsychotics 2nd and 3d generation

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NE made presynaptically from

l tyrosine

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SER made presynaptically from

L tryptophan

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Ne and Ser cross modulating

auto and heteroreceptors are on the presynaptic membrane

serotonergic receptors contain NE receptors and vice versa

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Works in the presynaptic terminal to degrade both SER and NE

MAO

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inhibits NE reptake to the presynaptic terminal by NET

TCAs and SNRIs

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inhibits SER reuptake to the presynaptic terminal by SERT

SSRIs, TCAs, SNRIs

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works presynaptically to increase the amount of SER and NE for release

MAOi they inhibit the breakdown

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black box warning on all antidepressants

suicidal thoughts double that in the control population

all children and all adults up to 24 years of age-should be closely monitored especially during the initial weeks -elitic signs of worsening depression
8benefits do outweigh the risk

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st johns wort

interferes with HIV meds, heart disease emds, cancer, orga transplat rejection

cyp induction

mild -moderate depression

no better than placeo and worse than SSRI

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antidepressants are substrates for

ABCB1-(MDR1;pgp) present at the BBB-limiting the ability for given drug to accumulate in the brain where its intended sight of action is

SNP (t vs C) determine whether or not a dictated therapy would cause depression remission

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drugs that are substrates for MDR1

citalopram, venlafaxine,paroxetine, amitriptyline

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Not substrates for MDR1

Fluoxetine

mertazepine

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which allele indicates overall higher rate of MDRI transport activity

C allele

CC and CT are bad for treatmen remission

if pt has these alleles there will be less accumulation in the brain

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Newer drugs since the first gen TCAs show

fewer side effects, but not a reduced number of treatment resistant patients–> SSRI’s used as primary comparator

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indications for TCAs

pain and anxiety, major depressive disroder, phobia, panic disorders, OCD, ADHD, nocturnal enuresis, depression associated with shizophrenia

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MOA for TCA’s

inhibit reuptake of SER and NE into presynaptic terminals, potential and prologn their action, subsequent receptor and transporter regulaiton with repeated tx,

also block muscarinic cholinergic, H1 and alpha ARs–these lead to side effects

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side effects of TCA's

acutely-2-6 weeks-drowsiness, dysphoria, anxiety, impaired thinking, symptoms improve but EUPHORIgenic orthostatic hypoertension blurred visions, worsened ANGLE claucoma, urinary retention, tachcardia M2 antagonism sedation H1 antagonism and Alpah AR weight gain, sexual disturbances

overdose on TCA's

low Ther-index, CV effects=arryhtmias, myocardial depressioin, worsening of CHF, acidosis, delerium seizures

PK's for TCA's

lipid-brain and fat long half life, protein bound-high volume of distribution-limites excretion and polong half life suffer from 1st pass metab.-incompletely absorbed

tertiary amines metabolixed to secondary by demethylation

imipramine--> desipramine amitrip--< nortrip

tricyclin ring subject to

oxidation cyp 2d6 and conjugation

indications for SSRIS

first line for MDD COD aDHD, eating, social anxiety disorder panic,

better compliance of SSRIS due to

negligble efect on H1, mACH, alpha 1--less undesireable side effectsd

MOA of SSRIs

SELECTIVE inhibition of SERT-prolong action of 5ht

escilatolpram is the active isomer of

citalopram-racemix mixture

therapuetic index of SSRIs

higher than TCA's therfore less risk of overdose

side effects of SSRI's

fewer than other decreaed libido, anxiety agitation, -2-6 most gone nausea, low incidence of CV and anticholinergic defects

increased risk of birth defects with which SSRI

paroxetine-paxil

PK for SSRI's

moderate bioavailability-better than TCAs high protein binding, long half life,

SSRI with half life if 7-9 days

norfluoxetine-metabolite of fluoxetine thus fluoxetine can be formulated for once weekly dosing

cyps inhibited y SSRIS

2d6 and 2c19

absolutely contraindicated within 2 weeks of taking and SSRI

MAOi wil cause serotonin syndrome

indication for atypical antidepressants

major depresive disorder but have diff mechs of action

PK for atypical antidepressants

similar to TCAS but with shroter half life

SNRIs-

venlafaxine | duloxetine

SNRI void of antiACH, antiH1, and antiAlphaAr protperties

venlafaxine

MOA for venlafaxine

inhibit serotonin and nroepinephrine reuptake no TCA like side effects

side effects of Venlafaxine

small sustained HTN, sweating diszziness, nausea and anxity

most potent SNRI available

duloxetine-cymbalta

100x more potent than venlafaxine

duloxetine half life of 12 hours cyp 2d6 and 1a2 metabolism

analog of antipsychotic loxapine

amoxamine

extrapyramidal motor side effects

amoxamine-Dopa receptor antagonism

useful for depression in a psychotic patient

amoxamine

moa for amoxamine

mixed inhibition of NET>SERT=DAT

weak blocker of DAT, SERT, NET

buproprion | -active metabolite is a NEreuptake blocker

also can be used in smoking cessation

buproprion

should be administered as divided doses or extended release formulaiton

wellbutrin

selective inhibitor of NA with increased risk of seizures

maprotiline-NRI

increased risk of seizure

Buproprion | Maprotiline-NRI

enhances release of Ser and NE bu antagonizing presynaptic alpha 2ARs

mirtazepine also antagonizes 5ht2 receptors-vasoconstriction??

side effect of mirteazepine

potent antihistaminergic-sedation

tetracyclin antidepressant

mirtazepine

SARI's-serotonin antagonist and reuptake inhibitors

Trazodone Nefazedone

MOA for trazadone

moderate inhibition of serotonin reuptake but primarily acts and a 5ht2 agonist and 5HT1 agonists

depression characterized by anxiety and sleep disturbances

trazadone

SMS-serotonin Modulator stimulators

Vilazodone-potent 5HT1 agonist and SSRI Vortioxetine-blocker f SERT agonist og %ht1a, agonist of 5HT1b, antagonist at 5HT1d, 3A and 7 also beta bloker

Used for patients who are unresposnive to treatment and who ECT is not a option panic disorder and agoraphobia

MAOi's

irreversible inhibition of MAOa and B in nerve terminals

MAOI

MAO-Ametabolizes

norepi and serotonin and tyroimine

MAO-b metaboliszed

dopamine selective

acute side eeffects of MAOis that abate within a couple weeks

cna stimulation, agitation, euphoria,

daily dosing required inspite of irreversible inibition of the target enzyme

MAOi's

MAOI taking pateitns should avoid what foods

those containing high amounts of tyramine

MAOI's shouldnt be taken with OTC shit

sympathomimetic drugs-cold remedies, diet aids, stimulants, a causes acute HTN reaction

MAOI shouldnt be taken with what prescriptions

SSRIS-serotonin syndome Meperidine, DXM, --Hypepyrexia, delerium, convulsions, coma, death

different between antimanic drugs and mood stabilizers

mood stabilizers do not take away the mania but prevent cycline between manic and severe depressive

mood stabilizers youse as maintainence therapy for bipolar disorders

lithium valproate carbemazepine

MOA for lithium

inihbit Inositol phosphate activity also inhbits neurotransmitter stimulatesd ACyclase actiivty only works in fuycking 60% of ppl

PK for lithium

total body water distribution som in bone half life 20 hours no metabolism out the urine

therapeutic window for lithium

very narrow target 0.5-1.0 toxic at 1.5 brady-tachycardia, acne, psoriasis, tremor ataxia, hypotheydoid, nephrogenic DI

drug interactions with lithium

sensitive to diuretics and antiinflamatory NSAIDS

valproic dosing

should be decreased bc it inhibits its own metabolism over time monitor liver funciton too

drug that should be increased with repeated treatment

carbemazepine induces its own metabolism

Tavalin: Antidepressants Flashcards

(81 cards)