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Pharm Test 2 > Antidepressants > Flashcards

Antidepressants Flashcards

(80 cards)

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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
MOAIs Mechanism
NOT 1st line * block MOA - block NE + 5-HT * periphery and brain
26
MAOIs S.E.
``` Postural HypoTN CNS Sexual GI OD - not common ```
27
Seritonin Syndrome
``` Akathisia Altered mental Clonus Tremor Hyperthermia Muscular Hypertonicity ```
28
MAOIs Diet restrictions
Tyramine (cheese, wine, other) - indirect sympathomimetic - Not broken down, up in blood, into nerve, looks like NE, inhibits NE release
29
3rd generation - atypical
Dopamine reuptake *buproprion (WELLBUTRIN) Autoreceptor anatagonist *Mirtazapine (REMERON)
30
3rd gen - atypicals Timeline
Initally = hours-days Delayed mood effect - 1- weeks Used as ADJUNCT w/ other Anti-deps (SSRIs) - no seritonin syndrome
31
Buproprion (WELLBUTRIN) other uses
Smoking cessation (other addictions?)
32
Mirtazapine (REMERON) Other Uses
*sedative properties, appetite stimulant
33
Bupropion (WELLBUTRIN) Mechanism
THERAPEUTIC = Block ***DAT*** + NET Non-therapeutic = block nicotinic receptor (smoking cessation)
34
Bupropion (WELLBUTRIN) S.E.
* CNS * Seizures (dopamine effect) * may cause anxiety (contra-indicated)
35
Buproprion (WELLBUTRIN) Advantages
No seritonin - No sexual effects, ect.
36
Mirtazapine (REMERON) Mechanism
Alpha 2 blocker - up NE release *5-HT enhanced indirectly Non-therapeutic= H1 blocker - sedation - weak antimuscarinic/a1 blocker
37
Mirtazapine (REMERON) S.E.
Sedation - night dosing Weight gain Postural hypoTN
38
Mirtazapine (REMERON) Disadvantage
Antihistimine = up appetie Anticholinergic Cyp inhibition
39
Mirtazapine (REMERON) Advantage
Less side effects
40
Anti-Depr Tolerance
For most effects NOT Sex disfunction (SSRI/SNRI) NOT Cardiac toxicity (TCA
41
Anti-Depr Withdrawal
Discontinuation syndrome | TAPER
42
Bipolar disorder 1
Manic depression w/ major depression
43
Bipolar 2
More depression
44
Bipolar Rxs
* Lithium * Olanzapine (ZYPREXA) * Valproate (divalproate) (DEPACON) * Lamotrigine (LAMICTAL)
45
ACUTE manic emergencies
SEDATION * antipsyc = olanzapine ZYPREXA * Benzo * Anti-convulsants - sodium valproate DEPACON
46
BIPOLAR Maintanence
Mood stabilizers LITHIUM Anti-convuls - valproate DEPACON, lamotrigine LAMICTAL Atypical antipsyc - olanzapine ZYPREXA
47
Bipolar Antidepressant Rxs
* switch from depression to mania * more cycling * lithium + ADD
48
Lithium Mechanism
Unclear/complex * stops Ip3 system - to dopamine receptors * block dopamine release * stop glycogen sythase kinase 3 = Neurotropic/neuroprotective
49
Lithium
Not stopping manic episode
50
Lithium Absorption
Good oral
51
Lithium Excretion
``` Urine *80% reapsorbed *sodium receptors UP Na excretion = DOWN Lithium excretion (toxic) *watch clearance ```
52
Lithium Rx interaction
* sodium depleting Diuretics (reduce lithium 25% dose) * dehydration * NSAIDs * Ace inhibitor
53
Lithium S.E.
*Tremor (add B-blocker) *Renal - polydipsia, polyuria -nephrogenic diabetes insipidus Sedation GI Skin problems
54
Lithium Toxicity
Renal clearance change >2 mEq/L *confusion, ataxia *hypoTN, arrythmia Tx. Supportive, dialysis
55
Bipolar Anticonvulsants
~Valproic acid DEPACON ~Lamotrigine LAMICTAL *treat both poles *prevents depression (not with lithium!!! Perhaps combo?)
56
Bipolar Disorder Mood stablizer Mechs
Unclear
57
Mood stabilizers vs. Lithium
* quicker response * safer * better tolerated
58
SSRIs Metabolism/interactions
Fluoxetine>Sertraline>Escitalopram (newest) PROZAC>ZOLOFT>LEXAPRO (newest) * active metabolites * CYP 2D6
59
Serotonin + NE neurons BOTH contain
Serotonin + NE inhibitors
60
TCAs Mechanism
Block Reputake pumps = 5-HT (SERT) + NE (NET)
61
TCAs 2 + 3 degree amines block
NET + SERT *3 degree metabolized to 2 degree (affect NE + 5HT)
62
TCAs Block receptors for many neurotransmitters
Muscarinic - dryness A1 adrenergic - hypoTN H1 histamine - sleepy
63
TCAs Metab/excretion
* long t1/2 | * kinetics not important for therapy (delayed onset) - but possible toxicity when switching meds
64
TCAs S.E.
MANY - noncompliance * Cardio - tac, block, arrythm * Vascular - a1 block (hypoTN) * Anticholinergic - dryness * CNS- anticholinergic - sedation * Antihistimine - hunger * SERT block - Sexual
65
MAOIs Binding
Irreversible
66
MAOIs Drug interactions
* 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
MAOIs Uses
*atypical depression = respond to MAOIs + SSRIs (NOT TCAs) NO W/ Rxs upping serotonin
68
Anti-depressants in pregnancy
AVOID - Tranylcypromine PARNATE * slight risk fetal malformations - fluoxetine PROZAC, sertraline ZOLOFT * possible limb malformation - amitripyline ELAVIL
69
Anti-depressants Maternal depression
* Untreated maternal depression = delayed fetal development | * stop ADs during pregnancy - 5x risk of relapse
70
What is only anti-depressant for children >8yrs?
Fluoxetine PROZAC
71
What anti-depressant approved for adolescents >12 yrs?
Escitalopram LEXAPRO | Fluoxetine PROZAC
72
Anti-depressants Abuse
No evidence
73
Anti-Depressants Tolerance
``` NONE FOR THERAPEUTIC Most side effects reduced EXCEPT Sexual - SSRI/SNRI Cardio toxicity - TCA TAPER OFF ```
74
Antidepressant What to do if poor response?
5 Ds * Dose? * Duration? Onset * Diagnosis correct? * Drugs adjuncts needed? * Different Tx style (non-pharm)
75
Biplolar Cyclothymia
Mild/moderate depression hypomania
76
Lithium
Maintenance therapy for bipolar *Gradual onset (need adjuncts)
77
Lithium Toxicity
Narrow T.I. - BLOOD LEVEL MONITORING | *use slow release preps
78
Bipolar Tx. Anticonvulsants
Valproic acid DEPACON Lamotrigine LAMICTAL Acute manic episode *lithium adjunct OR 1st line maintenance
79
Bipolar Tx Antipsychotics
Olanzapine ZYPREXA Manic episode S.E. - weight gain, hyperlipidemia, hyperglycemia
80
Bipolar treatment Which lithium alternative good for treating depressive episodes?
Lamotrigine LAMICTAL

Pharm Test 2 (13 decks)

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