Anti Depressants Flashcards by Mahdi Akoush

Anti depressants potentiate directly or indirectly —- or —-in the brain
Initial effect of drugs: directly responsible for antidepressant effects?
After 2-4 weeks?

Norepi
Serotonin
Inhibiting reuptake
Presynaptic inhibitory receptors decrease
This leads to the therapeutic response

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SSRIs:
1-
2-
3-
4-
5-
6-

Citalopram cipram
Escitalopram cipralex
Fluvoxamine floxyferal
Paroxetine seroxat
Sertaline zoloft
Fluoxetine prozac

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Action os SSRIs:
Both citalopram and fluoxetine are —— which respective —– are more potent

Specifically inhibit serotonin reuptake
(300-3000 fold greater sleectivity for serotonin as compared to Ne)
Little ability to block dopamine
Little blocking activity at muscarinic alpha adrenergic histamine H1 receptors
Racemic mixture (S more potent yaane escitalopram(s) more potent than citalopram)

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Antidepressants take at least—– to produce improvement on mood and max benefit require——

2 weeks
12 weeks

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Therapeutic indications for SSRI:

Depression
OCD (the only approved is fluvoxamine)
Panic disorder
GAD
Social anxiety disorder
Severe anxiety disorders

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T or F
SSRIs are not well absorbed after oral administration
Well distributed
Plasma half lives between 20-30 hr
Food have little effect on all SSRIs
Peak levels are seen aprox 2 to 8 hrs on av

False
True ((15-30 L/kg))
False 16-36 hrs
False sertaline food increases its absorption
True

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Metabolism of SSRIs
Inhibitors of cyp:

Cyp450 depedent glucuronide or sulfate conjugation
Fluvoxamine inhibits A2 c19 3A3/4
Fluoxetine and fluvoxamine c9
Paroxetine fluoxetine and less actively sertaline 2D6
Dosage adjusted with hepatic inpairment

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Fluoxetine differs from other members by:

Much longer half life (50 hr)
S norfluoxetine is potent
(Half life 10 days)

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Adverse effects of SSRIs

Headache
Sweating
GI
Weakness fatgue diarrhea
Sexual dysfunction
Changes in weight
Sleep disturbances
Suicidal thinking

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Overdoses of SSRIs

Do not usually cause cardiac arrythmias
All the antidepresants may lower the seizures threshold
Serotonin syndrome(hyperthermia, tachycardia muscle rigidity sweating and myoclonus) when used with MAO or highly serotonin drug

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Discontinuation of SSRIs
—— has the lowest risk of causing discontinuation problems

Headache
Agitation irritability
Nervousness
Change in sleep pattern
Floxetine

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SNRIs
1-
2-

Duloxetine
Venlafaxine (effexor ER)

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Actions and inducations

Effective when SSRIs are ineffective
Relief neuropathic pain like TCA

Major depressive state
GAD
Social anxiety disorder

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Venlafaxine
Inhibitor of?
Minimal inhibitor of —-
Substrate of
Side effects
High doses?

Serotonin
At medium to high doses inhibits nor
Mild inhibitor of dopamine
Cyp450
Cyp2D6
Nausea, headache sexual dysfuntion dizzness insomnia constipation
High BP and heart rate

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Duloxetine (cymbalta)
Contraidications
Indications
Side effects

Hepatic insuff
GAD
Diabetic neuropathic pain
Diarrhea sexual dys nausea
Possible ; incr in BP and HR

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Atypical ADs

Bupropion (wellbutrin or zyban la)
Mirtazapine (remeron)
Nefazodone (serzone)
Trazodone (desyrel)

Atypical ADs are more efficient than TCA and SSRIs

False
Different side effects

Bupropion
Mode of action
Actions
Half life
Side effects

Weak dopamine and norepinephrine reuptake inhibitors
Decrease craving and withdrawal sx of nicotine it antagonise nicotinic receptor function
Short
Low incidence of sexual dys and wight gain
Increased risk of epileptic seizures at high doses

Mirtazapin
Mode of action
Side effects

Ser and nor because it block alpha 2 presynaptic and 5HT2 receptors
Sedative because of antihistaminic effect (for patients having sleep difficulties)
Hematological side effects

T or F
Murtazapin cause anti muscarinic side effects of TCA but doent interfere with sexual functioning

False
Don’t do both

TCAs
Mode of action
Choice of drug depends on

Block NE and ser reuptake inhibitos
Tolerance to SE preexisting medical condition duration
If doesnt respond to one TcA may respond to another
Valuable for patients who doesnt respond to SSRIs

T or F
At therapeutic doses they block dopamine transporters
Maprotyline and desipramine are selective inhibitors of NE reuptake

False
True

Which receptors TCA blocks

Alpha adrenergic histaminic and muscarinic (cause of many side effects)
Amoxapine also blocks D2 receptors

Actions of TcA;
Onset:

Elevate mood inprove metnal aletrness increase ohysical activity
2 weeks or longer
Necessitates slow withrawal to minimuze discontinuation syndrome and cholinergic rebound effects

TCA effective in tx of :

Moderate to severe major depression Chronic pain syndrome (neuropathic) Enuresis in children (older than 6h

Which drug us used to control bed wetting by causing contraction of internal sphincter

Imipramine (tofranil) Used cautiosly because of induction of arrythmias

Phamacokinetics

Well absorbed after oral adm Lipophilic Widely distributed Variable 1/2 4-17 hrs for imipramine Metabolized by liver microsomal enz Excreted as in active metabolites in kid

Adverse effects 1- 2 3-

Blockage of muscarinic receptors(blurred vis, xerostomia, urinary retention, constipation and glaucoma) Blockage of alpha adrenergi(orthostatic hypotention dizziness and reflex tschy) Block H1 eeceptors (sedation weight gain sexual dys lower than SSRIs)

Cardiovascular adverse effects

On slide

Precautions of TCA

Like all antidepressants used with caution in known bipolar patients because they may switch to manic episode

T or F TCAs have narrow therapeutic index May exacerbate medical conditions such as epilepsy and arrythmias We can associate with MAO

True (5-6 fold the max may be lethal of imipramine) True False never (risk of hyper)

MAO inhibitors Mode of action Presence Anti depressant action

Form stable complexes with MAO causing itreversible inactivation In brain gut and liver (oxidative deamination of toxic substances like tyramine) Delayed several weeks (altho its fully inhibited after several days)

Therapeutic uses of MAO inhibitors

Depressed patients unresponsive to TCA Low psychomotr activity Phobic states

Names of MaO inhibitors

Phenelzine (Nardil) Tranylcypromine (parnate) Sleegeline (eldepryl or deprenyl)

Pharmacokinetics

Well absorbed after oral Effects require 2-4 weeks Enzyme regeneration varies but requires several weeks after termination

T or F We need minimum 1 week after MAO inhibitors termination to start another med

False Minimum 2 weeks

Adverse effects Drug food interaction Drug drug interaction

Drug food interaction (unable to degrade tyramine which inturn leads to release of large amounts of stored catecholamines from nerves causing head ache tachycardia hypertension cardiac arrythmias nausea) With SSRIs cause serotonin syndrome both drugs require washout periods at least 2 weeks before other type is given Exxxceotionnnnn: fluoxetine should beeee discontineud 6 weeks at least before AO is initiated

Tx of mania Lithium: Mode of action Mode of adm Excretion Toxic Therapeutic index Adverse

Mood stabilizer Unknown (may be decrease norepinephrine release and increase serotonin) Orally Ion Secreted by kidney can be toxic Extreeemly lowwww Headache,dry mouth polydipsia polyuria polyphagia GI (nausea vomittin) ataxia and tremors Give lithium with food

Names of 1-Antiepileptic drugs as mood stabilizers 2-Agents that improve manic sx 3-Management of mania 4-Bipolar depression

1-Carbamazepine, valproic acid and lamotrigine 2-Chlorpromazine and haloperidol 3-Risoeridone olanzapine aripiprazole and quetiapine 4-quetiapine and olanzapine+fluoxetine