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pharmacology B > Antidepressants > Flashcards

Antidepressants Flashcards

(39 cards)

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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

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A

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

17
Q

SSRIs

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

SSRIs indications

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

SSRIs side effects

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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

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A

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

21
Q

Sertraline

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A

SSRI.

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

22
Q

Citalopram

23
Q

Paroxetine

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A

SSRI. Duration of action: 1 day

24
Q

Fluvoxamine

25
SSNRIs - selective 5HT and NE reuptake inhibitors
``` inhibit both NET and SERT, but without TCA like side effects Venlafaxine (fax machine) Duloxetine (dual copier/scanner) Reboxetine Bupropione (ball pro) ```
26
Venlafaxine
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
Duloxetin
SSNRI. NET and SERT inhibitor
28
Reboxetine
SNRI - only inhibit NET! | SE: insomnia, weak anticholinergic SEs
29
Bupropione
(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
Tianeptine
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
Agometaline
Is a melatonin receptor AG (MT1 and 2) and 5-HT2c ATG. Has a weak antidepressant effect. I: insomnia (jet-lag) SE: hepatotoxic
32
NE and 5HT receptor ATG antidepressants
``` These drugs not only inhibits reuptake transporters, but also have receptorial effect. Trazadone (trombone) Vilazadone Mirtazapine (mirth and misery) (mianserin) ```
33
Trazadone
is an SRI (inhibits SERT), 5HT2A receptor ATG, and alpha1 R ATG. I: depression, especially with co-pressence of insomnia
34
Vilazadone
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
Mirtazapine | Mianserin
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
Antimania drugs (mood stabilizers)
Lithium If lithium doesn't work: Antiepileptics:Valproid acid, Carbamazepine, Lamotrigine, Gasapentine
37
Acute mania phase therapy
``` 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
Lithium carbonate | Mechanism of action, pharmacokinetics
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
Lithium, Indications and Side effects
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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