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Pharm Test 2 > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

Depression Tx options

A
  • Psychotherapy
  • ECT
  • Light Therapy
  • Vagal nerve Stimulation
  • Transcranial Magnetic Stimulation
  • Pharmacotherapy (ADDs)
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2
Q

SSRIs

Rxs

A
  • fluoxetine (PROZAC)
  • escitalopram (LEXAPRO)
  • sertraline (ZOLOFT)
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3
Q

SNRIs

Rxs

A

Duloxetine (CYMBALTA)

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4
Q

TCAs

Rxs

A
  • amiriptyline (ELAVIL)

* despiramine (NORPRAMIN)

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5
Q

MAOIs

Rxs

A

Tranylcypromine (PARNATE)

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6
Q

Other

Rxs

A

Buproprion (WELLBUTRIN)

Mirtazapine (REMERON)

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7
Q

Therapeutic effects of Anti-Depressants on mood appear after…

A

2-6 weeks

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8
Q

Seritonin sythesis and metabolism

A

From tryptophan to melatonin

SYNTH = ECL cells, Brain-stem (raphie nuclei)

Effect on platelets

*METAB= MAO

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9
Q

How many seritonin receptor types?

A

7

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10
Q

SSRI

Neurochemical effects

A
  • Block SERT, Inhibit serotonin re-uptake (5-HT)
  • 2ndary= down reg autoreceptor for inhibition
  • SELECTIVE (no hitting NE receptor)
  • need tryptophan to make more serotonin
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11
Q

SSRI

Consequences

A

Over time , receptors downregulated

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12
Q

SSRI

Absorption

A

Good, mostly protein bound

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13
Q

SSRIs

Interactions

A

CYP (2D6)
*warfarin, Tricycl anti-depressants, etc.

Fluoxetine>Sertraline>Escitalopram
PROZAC>ZOLOFT>LEXAPRO

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14
Q

SSRIs

Adverse Effects

A

*CNS - insomnia, agitation
*GI
*Seritonin syndrome
*Sexual dysfunction - all seritonin enhancers
*ESCITALOPRAM (Lexapro) - prolong QT
START W/ LOWER DOSE TO MEDIATE S.E. (no help with sexual)

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15
Q

SSRIs

timeline

A
  • Initially : adverse effects (hours-days)

* Therapeutic response (1-6 weeks) GRADUAL (no euphoria)

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16
Q

SSRIs

Other uses

A

ADD
Anxiety
Eating disorders

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17
Q

SNRIs

Mechanism

A
  • block SERT

* Block NET (norepi reuptake)

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18
Q

SNRIs

S.E

A
  • Discontinuation syndrome = short t/12
  • Hepatic Cyp metab + inhibition
  • UP BP at high dose = alpha 1 receptor on vessels
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19
Q

SNRIs

Other uses

A
  • neuropathic pain

* also = anxiety, fibromyalgia,

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20
Q

SSRIs SNRIs

Overdose

A

W/ MAOIs, other seritonin enhancers, St.John’s Wort

  • Seritonin syndrome = hyperthermia, muscle rigidity, akathesia, myoclonus, (MAYBE LETHAL?)
  • SNRIs = HTN
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21
Q

SSRIs vs SNRIs

Efficacy

A
  • No evidence for superiority (individual differences)

* If no tryptophan in diet = SNRI better

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22
Q

TCAs

Tertiary
Secondary

A 
Tertiary = amitriptylin (ELAVIL)
Secondary = deipramine (NORPRAMIN)
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23
Q

TCA

S.E.

A

*heart
-NET block= tach, palp
-anticholinergic = conduction
Arrythmia
*a1 block = ortho hypo
*anthi-cholinergic= dry mouth, constipation
*CNS - antichol/anthi histimine

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24
Q

TCA

OD toxic

A
  • cario arrythmia - low T.E., no receptor, no time diminishing
    • Tx = lidocaine
  • lethal = suicide
  • 2ary amines - better S.E.s than 3rd
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25
Q

MOAIs

Mechanism

A

NOT 1st line

  • block MOA - block NE + 5-HT
  • periphery and brain
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26
Q

MAOIs

S.E.

A 
Postural HypoTN
CNS
Sexual
GI
OD - not common
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27
Q

Seritonin Syndrome

A 
Akathisia
Altered mental
Clonus
Tremor
Hyperthermia
Muscular Hypertonicity
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28
Q

MAOIs

Diet restrictions

A

Tyramine (cheese, wine, other)

  • indirect sympathomimetic
  • Not broken down, up in blood, into nerve, looks like NE, inhibits NE release
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29
Q

3rd generation - atypical

A

Dopamine reuptake
*buproprion (WELLBUTRIN)

Autoreceptor anatagonist
*Mirtazapine (REMERON)

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30
Q

3rd gen - atypicals

Timeline

A

Initally = hours-days

Delayed mood effect - 1- weeks

Used as ADJUNCT w/ other Anti-deps (SSRIs) - no seritonin syndrome

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31
Q

Buproprion (WELLBUTRIN)

other uses

A

Smoking cessation (other addictions?)

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32
Q

Mirtazapine (REMERON)

Other Uses

A

*sedative properties, appetite stimulant

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33
Q

Bupropion (WELLBUTRIN)

Mechanism

A

THERAPEUTIC = Block DAT + NET

Non-therapeutic = block nicotinic receptor (smoking cessation)

34
Q

Bupropion (WELLBUTRIN)

S.E.

A
  • CNS
  • Seizures (dopamine effect)
  • may cause anxiety (contra-indicated)
35
Q

Buproprion (WELLBUTRIN)

Advantages

A

No seritonin - No sexual effects, ect.

36
Q

Mirtazapine (REMERON)

Mechanism

A

Alpha 2 blocker - up NE release
*5-HT enhanced indirectly

Non-therapeutic= H1 blocker - sedation
- weak antimuscarinic/a1 blocker

37
Q

Mirtazapine (REMERON)

S.E.

A

Sedation - night dosing
Weight gain
Postural hypoTN

38
Q

Mirtazapine (REMERON)

Disadvantage

A

Antihistimine = up appetie
Anticholinergic
Cyp inhibition

39
Q

Mirtazapine (REMERON)

Advantage

A

Less side effects

40
Q

Anti-Depr

Tolerance

A

For most effects
NOT Sex disfunction (SSRI/SNRI)
NOT Cardiac toxicity (TCA

41
Q

Anti-Depr

Withdrawal

A

Discontinuation syndrome

TAPER

42
Q

Bipolar disorder 1

A

Manic depression w/ major depression

43
Q

Bipolar 2

A

More depression

44
Q

Bipolar

Rxs

A
  • Lithium
  • Olanzapine (ZYPREXA)
  • Valproate (divalproate) (DEPACON)
  • Lamotrigine (LAMICTAL)
45
Q

ACUTE manic emergencies

A

SEDATION

  • antipsyc = olanzapine ZYPREXA
  • Benzo
  • Anti-convulsants - sodium valproate DEPACON
46
Q

BIPOLAR Maintanence

A

Mood stabilizers
LITHIUM
Anti-convuls - valproate DEPACON, lamotrigine LAMICTAL
Atypical antipsyc - olanzapine ZYPREXA

47
Q

Bipolar

Antidepressant Rxs

A
  • switch from depression to mania
  • more cycling
  • lithium + ADD
48
Q

Lithium

Mechanism

A

Unclear/complex

  • stops Ip3 system - to dopamine receptors
  • block dopamine release
  • stop glycogen sythase kinase 3 = Neurotropic/neuroprotective
49
Q

Lithium

A

Not stopping manic episode

50
Q

Lithium

Absorption

51
Q

Lithium

Excretion

A 
Urine
*80% reapsorbed
*sodium receptors 
UP Na excretion = DOWN Lithium excretion (toxic)
*watch clearance
52
Q

Lithium

Rx interaction

A
  • sodium depleting Diuretics (reduce lithium 25% dose)
  • dehydration
  • NSAIDs
  • Ace inhibitor
53
Q

Lithium

S.E.

A

*Tremor (add B-blocker)
*Renal - polydipsia, polyuria
-nephrogenic diabetes insipidus
Sedation
GI
Skin problems

54
Q

Lithium

Toxicity

A

Renal clearance change
>2 mEq/L
*confusion, ataxia

*hypoTN, arrythmia

Tx. Supportive, dialysis

55
Q

Bipolar

Anticonvulsants

A

~Valproic acid DEPACON
~Lamotrigine LAMICTAL
*treat both poles
*prevents depression (not with lithium!!! Perhaps combo?)

56
Q

Bipolar Disorder

Mood stablizer Mechs

57
Q

Mood stabilizers vs. Lithium

A
  • quicker response
  • safer
  • better tolerated
58
Q

SSRIs

Metabolism/interactions

A

Fluoxetine>Sertraline>Escitalopram (newest)
PROZAC>ZOLOFT>LEXAPRO (newest)

  • active metabolites
  • CYP 2D6
59
Q

Serotonin + NE neurons BOTH contain

A

Serotonin + NE inhibitors

60
Q

TCAs

Mechanism

A

Block Reputake pumps = 5-HT (SERT) + NE (NET)

61
Q

TCAs

2 + 3 degree amines block

A

NET + SERT

*3 degree metabolized to 2 degree (affect NE + 5HT)

62
Q

TCAs

Block receptors for many neurotransmitters

A

Muscarinic - dryness
A1 adrenergic - hypoTN
H1 histamine - sleepy

63
Q

TCAs

Metab/excretion

A
  • long t1/2

* kinetics not important for therapy (delayed onset) - but possible toxicity when switching meds

64
Q

TCAs

S.E.

A

MANY - noncompliance

  • Cardio - tac, block, arrythm
  • Vascular - a1 block (hypoTN)
  • Anticholinergic - dryness
  • CNS- anticholinergic - sedation
  • Antihistimine - hunger
  • SERT block - Sexual
65
Q

MAOIs

Binding

A

Irreversible

66
Q

MAOIs

Drug interactions

A
  • sympathomimetics
  • Meperidine DEMEROL/Dextromethorphan, ADDs - serotonin syndrome

2-5 WEEKS WAIT AFTER MAOI TO START NEW RX
2 WEEKS WAIT B/F STARTING MAOIs

67
Q

MAOIs

Uses

A

*atypical depression = respond to MAOIs + SSRIs (NOT TCAs)

NO W/ Rxs upping serotonin

68
Q

Anti-depressants in pregnancy

A

AVOID - Tranylcypromine PARNATE

  • slight risk fetal malformations - fluoxetine PROZAC, sertraline ZOLOFT
  • possible limb malformation - amitripyline ELAVIL
69
Q

Anti-depressants

Maternal depression

A
  • Untreated maternal depression = delayed fetal development

* stop ADs during pregnancy - 5x risk of relapse

70
Q

What is only anti-depressant for children >8yrs?

A

Fluoxetine PROZAC

71
Q

What anti-depressant approved for adolescents >12 yrs?

A

Escitalopram LEXAPRO

Fluoxetine PROZAC

72
Q

Anti-depressants

Abuse

A

No evidence

73
Q

Anti-Depressants

Tolerance

A 
NONE FOR THERAPEUTIC
Most side effects reduced
EXCEPT
Sexual - SSRI/SNRI
Cardio toxicity - TCA
TAPER OFF
74
Q

Antidepressant

What to do if poor response?

A

5 Ds

  • Dose?
  • Duration? Onset
  • Diagnosis correct?
  • Drugs adjuncts needed?
  • Different Tx style (non-pharm)
75
Q

Biplolar

Cyclothymia

A

Mild/moderate depression hypomania

76
Q

Lithium

A

Maintenance therapy for bipolar

*Gradual onset (need adjuncts)

77
Q

Lithium

Toxicity

A

Narrow T.I. - BLOOD LEVEL MONITORING

*use slow release preps

78
Q

Bipolar Tx.

Anticonvulsants

A

Valproic acid DEPACON
Lamotrigine LAMICTAL

Acute manic episode
*lithium adjunct OR 1st line maintenance

79
Q

Bipolar Tx

Antipsychotics

A

Olanzapine ZYPREXA

Manic episode
S.E. - weight gain, hyperlipidemia, hyperglycemia

80
Q

Bipolar treatment

Which lithium alternative good for treating depressive episodes?

A

Lamotrigine LAMICTAL

Pharm Test 2 (13 decks)

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