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DRUGS > 10 - A) ANTIDEPRESSANT DRUGS > Flashcards

10 - A) ANTIDEPRESSANT DRUGS Flashcards

1
Q

TREATMENT OF DEPRESSION

A
  1. Psychotherapy
  2. Medication
    1st choice: SSRIs or TCAs depending on patient’s characteristics
    ↑ Tendency to use new antidepressants
    MIRTAZAPINE
    VENLAFAXINE…
    Controversy
    2, Electroconvulsive therapy
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2
Q

MIRTAZAPINE

A

Treatment of depression; ventlafaxine and mirtazapine have a high conrovery.

Antagonist of alpha-2 adrenergic receptors

MIANSERIN

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3
Q

VENLAFAXINE

A

Treatment of depression; ventlafaxine and mirtazapine have a high conrovery.

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4
Q

CLASSIFICATION OF ANTIDEPRESSANT DRUGS

A

Monoamine reuptake inhibitors
Monoaminoxidase inhibitorrs (MAOIs)
Other

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5
Q

MONOAMINE REUPTAKE INHIBITORS

A

. Monoamine reuptake inhibitors
2.1.1. Non selective inhibitors: Tricyclic Antidepressants: TCAs
IMIPRAMINE, DESIMIPRAMINE, AMITRIPTYLINE, NORTRIPTYLINE, DOXEPIN
2.1.2. Selective Serotonin Reuptake Inhibitors: SSRIs
FLUOXETINE, PAROXETINE, CITALOPRAM, ESCITALOPRAM, SERTRALINE
2.1.3. NA Reuptake Inhibitors: NRIs REBOXETINE
2.1.4. 5-HT/NA Reuptake Inhibitors de: SNRIs
VENLAFAXINE, DULOXETINE
2.1.5. DA & NA Reuptake Inhibitors: BUPROPION

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6
Q

MONOAMINOXIDASE INHIBITORS (MAOIs)

A
  1. 2.1. Irreversible non-selective: TRANYLCYPROMINE

2. 2.2. Reversible MAO-A Inhibitors: MOCLOBEMIDE (RMAIs)

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7
Q

OTHERS

A

Antagonists of α2-adrenergic receptors: MIRTAZAPINE, MIANSERIN
Melatonin receptor agonists, 5HT2 Antagonists?
Phytotherapy: Hypericum (St John’s-wort)

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8
Q

Non selective inhibitors: Tricyclic Antidepressants: TCAs

A 
Antidepressant drugs. Monoamine reuptake drugs (Al igual que los MAOIs and others).
IMIPRAMINE
DESIMIPRAMINE
AMITRIPTYLINE
NORTRIPTYLINE
DOXEPIN

They act by blocking the reuptae of NA and 5-TH, by competing with its transporter. They inhibit DA reuptake too, but in lesser extent.

TCAs block adrenoceptors α1, muscarinic & histaminic receptors; producing ADVERSE REACTIONS.

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9
Q

IMIPRAMINE

A 
Antidepressant drugs. Monoamine reuptake drugs (Al igual que los MAOIs and others).
IMIPRAMINE
DESIMIPRAMINE
AMITRIPTYLINE
NORTRIPTYLINE
DOXEPIN
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10
Q

DESIMIPRAMINE

A 
Antidepressant drugs. Monoamine reuptake drugs (Al igual que los MAOIs and others).
IMIPRAMINE
DESIMIPRAMINE
AMITRIPTYLINE
NORTRIPTYLINE
DOXEPIN
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11
Q

AMITRIPTYLINE

A 
Antidepressant drugs. Monoamine reuptake drugs (Al igual que los MAOIs and others). Its the safest. 
IMIPRAMINE
DESIMIPRAMINE
AMITRIPTYLINE
NORTRIPTYLINE
DOXEPIN
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12
Q

NORTRIPTYLINE

A 
Antidepressant drugs. Monoamine reuptake drugs (Al igual que los MAOIs and others).
IMIPRAMINE
DESIMIPRAMINE
AMITRIPTYLINE
NORTRIPTYLINE
DOXEPIN
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13
Q

DOXEPIN

A 
Antidepressant drugs. Monoamine reuptake drugs (Al igual que los MAOIs and others).
IMIPRAMINE
DESIMIPRAMINE
AMITRIPTYLINE
NORTRIPTYLINE
DOXEPIN
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14
Q

Non selective inhibitors: Tricyclic Antidepressants: TCAs. -> PHARMACOLOGICAL ACTIONS

A

In not depressed people: Sedation, confusion, loss of motor coordination
• In depressed patients: tend to disappear in 10-15 days
- Antidepressant Action (10-15days) Do not produce CNS stimulation
- Anti-anxiety and Sedative Action
- Analgesic Action

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15
Q

ADVERSE REACTIONS DEPENDING ON WHICH TRANSPORTER IS INHIBITED (TCAs)

A

Numerous NORTRIPTYLINE is safer
- By (-) reuptake NA: tachycardia, tremor, anxiety
- By (-) reuptake 5-HT: nausea
- By H1 blockade: Sedation, lack of concentration…
- By muscarinic blockade: Blurred vision, constipation, urinary retention
- By α1 blockade: Orthostatic hypotension
- By K+ channel blockade: CARDIOTOXICITY:Arrhythmias, altered contractility,
altered frequency…
At normal doses, increase the risk of sudden cardiac death

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16
Q

Selective inhibitors: SEROTONIN REUPTAKE INHIBITORS (Drugs)

A

Selective inhibitors: SEROTONIN REUPTAKE INHIBITORS
FLUOXETINE (Prozac) “happiness pill”
PAROXETINE (Serotax) (most potent)
CITALOPRAM (Seropram) (most selective)
ESCITALOPRAM (Cipralex ) ((S)-stereoisomer (Left-enantiomer) of citalopram)
SERTRALINE (also inhibits reuptake of DA)

17
Q

FLUOXETINE

A

Selective inhibitors: SEROTONIN REUPTAKE INHIBITORS

FLUOXETINE (Prozac) “happiness pill”
PAROXETINE (Serotax) (most potent)
CITALOPRAM (Seropram) (most selective)
ESCITALOPRAM (Cipralex ) ((S)-stereoisomer (Left-enantiomer) of citalopram)
SERTRALINE (also inhibits reuptake of DA)

18
Q

PAROXETINE

A

Selective inhibitors: SEROTONIN REUPTAKE INHIBITORS

FLUOXETINE (Prozac) “happiness pill”
PAROXETINE (Serotax) (most potent)
CITALOPRAM (Seropram) (most selective)
ESCITALOPRAM (Cipralex ) ((S)-stereoisomer (Left-enantiomer) of citalopram)
SERTRALINE (also inhibits reuptake of DA)

19
Q

CITALOPRAM

A

Selective inhibitors: SEROTONIN REUPTAKE INHIBITORS

FLUOXETINE (Prozac) “happiness pill”
PAROXETINE (Serotax) (most potent)
CITALOPRAM (Seropram) (most selective)
ESCITALOPRAM (Cipralex ) ((S)-stereoisomer (Left-enantiomer) of citalopram)
SERTRALINE (also inhibits reuptake of DA)

20
Q

ESCITALOPRAM

A

Selective inhibitors: SEROTONIN REUPTAKE INHIBITORS

FLUOXETINE (Prozac) “happiness pill”
PAROXETINE (Serotax) (most potent)
CITALOPRAM (Seropram) (most selective)
ESCITALOPRAM (Cipralex ) ((S)-stereoisomer (Left-enantiomer) of citalopram)
SERTRALINE (also inhibits reuptake of DA)

21
Q

SERTRALINE

A

Selective inhibitors: SEROTONIN REUPTAKE INHIBITORS

FLUOXETINE (Prozac) “happiness pill”
PAROXETINE (Serotax) (most potent)
CITALOPRAM (Seropram) (most selective)
ESCITALOPRAM (Cipralex ) ((S)-stereoisomer (Left-enantiomer) of citalopram)
SERTRALINE (also inhibits reuptake of DA)

22
Q

Selective inhibitors: SEROTONIN REUPTAKE INHIBITORS (Mechanism of action and pharmacological interactions )

A

Selective blockade of 5-HT reuptake transporters.

1 - Antidepressant Action: moderate (2-4 weeks)
Do not produce CNS stimulation
2- Anti-anxiety Action: Effective in panic attack, phobia, bulimia,
obsessive-compulsive disorder…
Depression + Insomnia Treatment

23
Q

Selective inhibitors: SEROTONIN REUPTAKE INHIBITORS (Adverse effects)

A

Adverse Reactions: less than TCAs (< effect on NA)

- Nausea, vomits, anorexia, insomnia, sexual dysfunction, hyponatremia, ↑weight

24
Q

Selective inhibitors: SEROTONIN REUPTAKE INHIBITORS (Interactions)

A

Interactions:
- They are enzymatic inhibitors:  metabolism TCAs (avoid)
- “Serotoninergic Syndrome”: (+ MAOIs, tryptophan or lithium).
Tremor
Hyperthermia
Agitation
- “Withdrawal Syndrome”: malaise, chills, nausea,
unbalance, anxiety, irritability

25
Q

Selective inhibitors:NORADRENALINE REUPTAKE INHIBITORS (NRIs)

A

Roboxetine

26
Q

Selective inhibitors: SEROTONIN AND NORADRENALINE REUPTAKE INHIBITORS (SNRIs)

A

VENLAFAXINE, DULOXETINE

structure different to TCAs

27
Q

Selective inhibitors: DOPAMINE AND NORADRENALINE REUPTAKE INHIBITORS (SNRIs)

A

Buproprion, used for depression and tobacco cessation.

28
Q

MONOAMINE OXIDASE INHIBITORS (MAOIs)

Main enzymes

A

MAO-A: preferent substrates
5-HT, DA, NA …
MAO-B: preferent substrates
phenylethylamine,DA, NA

Antidepressant effect related to
MAO-A inhibition

29
Q 
Monoaminoxidase Inhibitors (MAOIs)
Irreversible non-selective (classic) (Drug)
A

TRANYLCYPROMINE

30
Q

TRANYLCYPROMINE (Mechanism of action, pharmacological actions and adverse reactions)

A 
Monoaminoxidase Inhibitors (MAOIs)
Irreversible non-selective (classic) (Drug)

Mechanism of action:
Non-competitive long lasting binding to MAO-A & MAO-B ; maintained effect until regeneration of new enzyme (≅ 2 weeks)

Pharmacological Actions:
• In not depressed people: euphoria, excitement and increased motor activity
• In depressed patients: Suppression of ideas and feelings of depression

Adverse Reactions:
Excessive central stimulation (tremor, insomnia, excitement):
≅ AMPHETAMINE stimulus

MAO Inhibition; increases endogenous vasopressor amines; hypertensive crisis may appear

Sometimes hypotension due to displacement and emptying of NA from vesicles

31
Q

TRANYLCYPROMINE (Interactions)

A

• HYPERTENSIVE CRISIS:
Increased effects of indirect and mixed sympathomimetic agents
Incresed exogenous amines (some substrate of MAO)
- levodopa, TCAs, cocaine, amphetamines,
nasal decongestants …
- foods rich in tyramine (fermented cheese, cured meat…)
“cheese reaction”
EXACERBATION OF SYMPATHOMIMETIC EFFECTS

• SEROTONINERGIC SYNDROME:
sweating, chills, tremor, ataxia, seizures, disorientation…
MAOIs + TCAs MAOIs + SSRIs

32
Q

Moclobemine

A

Reversible MOA - A- Inhibitors (RMAIs)
Less Adverse Reactions
Less interactions
No cheese reaction

33
Q

Antagonists of α2-adrenergic receptors (presynaptic). Drugs and mechanism of action

A

MIRTAZAPINE, MIANSERIN

α2-adrenergic R activation
inhibits release of NA & 5HT
α2-adrenergic R
blockade increases
release of NA & 5HT

DRUGS (22 decks)

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