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pharmacology B > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

Tetracyclic Antidepressants (TCAs) general. mechanism of action, indications

A

Mech. of action: inhibit NET and SERT. H1 ATG, alpha1 ATG, M-R ATG.
Indications: Depression, panic disorders, neuropathic pain, migraine prophylaxis.

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2
Q

TCA side effects

A

-Sedation, dizziness, confusion, weight gain (H1 ATGism)
-Dizziness, orthostatic hypotension, relfex tach (alpha 1 blockade)
-Dry mouth, constipation, urinary retention, blurred vision, confusion, impaired cognitive function (M-R blockade)
-Ventricular arrhythmias (blockage of HERG type K+ channels in heart) - only at high dose.
Serotonin syndrome (when given with MAO inhibitors)

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3
Q

Tri and tetracyclic antidepressants (TCAs)

A

Imipramine (imprint)
Amitriptyline (tripping)
Clomipramine
Maprotiline

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4
Q

Imipramine

A

TCA.

inhibits SERT and NET

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5
Q

Amitriptyline

A

TCA. inhibits SERT and NET

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6
Q

clomipramine

A

TCA. inhibit SERT and NET

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7
Q

Maprotiline

A

tetracyclic compound. Inhibits only NET (NET>SERT)

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8
Q

MAO-A inhibitors

A

Clorgylline
Moclobemid =RIMA
Phenelzine (MAO A+B) (funnel)

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9
Q

MAO-B inhibitors

A

Selegiline (sledge hammer)
Rosagiline
Phenelzine

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10
Q

Selegiline, Rosagiline

A

Irreversible MAO-B inhibitors

I: parkinsons disease

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11
Q

Clorgylline

A

Irreversible MAO-A inh.

I: severe cases of depression

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12
Q

Moclobemid

A

also called RIMA = reversible Inhibitor of MAO-A. short acting, commonly used.
I: depression, phobias
SE: excitation, sexual distrubances, sleeping problems, cheese reaction

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13
Q

Cheese reaction/effect

A

MAO-A inhibition leads to decreased tyramine breakdown in GI –> if patient on MAO-A inhibitor eats cheese, wine etc (contains tyramine)–> increased tyramine absorption–> tyramine displaces NE from neuronal vesicles –> hypertensive crisis, blurry vision, diaphoresis.

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14
Q

Serotonin syndrome

A

SSRI + MAO inhibitor –> autonomic instability, aggetation, hyperthermia, HTN, hyper-reflexia, chlonus.

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15
Q

Phenelzine

A

Irreversible inhibitor of both MAO-A and B.
I: severe cases of depression.
SE: cheese effect

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16
Q

Phenelzine

A

Irreversible inhibitor of both MAO-A and B.
I: severe cases of depression.
SE: cheese effect

17
Q

SSRIs

A 
Fluoxetine (fly out)
Paroxetine (parrot air)
Sertraline (desert airline)
Cotalopram (City)
(fluvoxetine)
18
Q

SSRIs indications

A
  • Depression - 1st line
  • Anxiety disorders, OCD
  • Eating disorders - bulimia (not anorexia)
  • PMS
  • Panic attacks (long term), acute: BZDs
19
Q

SSRIs side effects

A
  • GI side effects; nausea, commit, diarrhea (due to 5-HT3 R stimulation)
  • 5-HT2 R stimulation caused SEs: anxiety, insomnia, loss of libido, delayed orgasm
  • headache
  • Serotonin syndrome - if SSRIs are taken in combo with MAO inhibitors.
  • No TCA like side effects (no effects on NET.)
  • hyponatremia, SIADH (increased ADH secretion)
20
Q

Fluoxetine

A

an SSRI. Active metabolite: NorFluoxetine - 7-9days elimination time. Total elimination time: 4-6 days

21
Q

Sertraline

A

SSRI.

Duration of action: 1 day (25-35 hours)

22
Q

Citalopram

A

SSRI

23
Q

Paroxetine

A

SSRI. Duration of action: 1 day

24
Q

Fluvoxamine

A

SSRI

25
Q

SSNRIs - selective 5HT and NE reuptake inhibitors

A 
inhibit both NET and SERT, but without TCA like side effects
Venlafaxine (fax machine)
Duloxetine (dual copier/scanner)
Reboxetine
Bupropione (ball pro)
26
Q

Venlafaxine

A

SSNRI. 1st choice, taken 2x/day.
effect:
-Small dose: only SERT inhibition (act like an SSRI)
-high dose: SERT+NETT inhibition (act like a TCA)
due to dose dependent effect, if low dose is not effective, one can just increase dose and another action is added without having to change drug

27
Q

Duloxetin

A

SSNRI. NET and SERT inhibitor

28
Q

Reboxetine

A

SNRI - only inhibit NET!

SE: insomnia, weak anticholinergic SEs

29
Q

Bupropione

A

(Ball pro).
Inhibits NE and dopamine transporter (NET>DAT). no effect on SERT, and no TCA like SEs (no effect on H1, alpha1, M-Rs). short duration of action (taken 2x/day)
I: Stupor depression, smoking cessation
SE: seizures

30
Q

Tianeptine

A

atypical antidepressant. Increases repute of serotonin (unlike the other antidepressants, that inhibit 5HT reuptake)
effect: uncertain. re-equilibrates NE and 5HT proportion - has an antidepressive effect.
I: alcohol withdrawal syndrome

31
Q

Agometaline

A

Is a melatonin receptor AG (MT1 and 2) and 5-HT2c ATG.
Has a weak antidepressant effect.
I: insomnia (jet-lag)
SE: hepatotoxic

32
Q

NE and 5HT receptor ATG antidepressants

A 
These drugs not only inhibits reuptake transporters, but also have receptorial effect.
Trazadone (trombone)
Vilazadone
Mirtazapine (mirth and misery) 
(mianserin)
33
Q

Trazadone

A

is an SRI (inhibits SERT), 5HT2A receptor ATG, and alpha1 R ATG.
I: depression, especially with co-pressence of insomnia

34
Q

Vilazadone

A

is an SRI (Inhibits SERT), and a partial agonist at 5HT1A receptor.
A strong anxiolytic (stronger than SSRIs etc)
I: depression associated with strong anxiety

35
Q

Mirtazapine

Mianserin

A

alpha2 R ATG, 5HT2 and 5HT3 ATG
alpha 2 blocking effect: increased NE and 5HT release
5HT2,3 blocking effect: diminish SE of SSRIs - given in combination with SSRI to decrease anxiety and insomnia (5HT2 stimulation effect of SSRIs), and decrease GI side effects (5HT3 stimulation effect of SSRIs)
Mianserin - same actions, but not used anymore

36
Q

Antimania drugs (mood stabilizers)

A

Lithium
If lithium doesn’t work:
Antiepileptics:Valproid acid, Carbamazepine, Lamotrigine, Gasapentine

37
Q

Acute mania phase therapy

A 
Lithium and anti epileptics are not effective
Antipsychotics given:
Olazapine
Risperidone
     Acute mania: lithium + olanzapine/risperidone given for       2 weeks until effect of lithium develops. 
Haloperidol
Aripiprazole
BZDs
38
Q

Lithium carbonate

Mechanism of action, pharmacokinetics

A

Action: lithium replace Na+ in excitable tissues, effects of this:
- Couples G potion from the receptor, inhibit adenylate cyclase, inhibit IP3, DAG pathway.
Effect develops after 2-3 weeks.
PK: excreted unchanged via urine - competes with Na+ for reabsorption (patient with hyponatremia - lithium toxicity due to increased reabs.)
low therapeutic index, half-life: 20 hours, can accumulate in neural tissue

39
Q

Lithium, Indications and Side effects

A

I: bipolar disorder - mood stabilizer, unipolar depression
SE: tremor, sedation, nausea, vomit, hypo-thyroidism, interstitial nephritis, nephrogenic diabetes insipidus, edema, decreased cardiac function.
Toxic levels: seizures, hyperactivity, coma.

pharmacology B (6 decks)

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