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3: Pharmacology > Anti-depressant and bipolar disorder drugs > Flashcards

Anti-depressant and bipolar disorder drugs Flashcards

1
Q

What are the drug interaction of SSRIs- Selective Serotonin Reuptake inhibitors?

A
  • increase 5HT: Serotonin syndrome» with drugs ( MAOs, TCAs and meperidine)
  • most inhibit cytochrome P450 enzymes (partially fluvoxamine and fluoxetine)
  • increase level of benzodiazepines for anxiety disorder
  • Safer drug is Citalopram for interactions
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2
Q

Which is a safer SSRIs antidepressant for interactions?

A

Citalopram

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3
Q

When will you use SSRIs (selective serotonin reuptake inhibitors?

A

To treat major depression, OCD, Bulimia, anxiety disorders and PMDD- premenstral dyspeptic disorder.

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4
Q

Two examples of SSRIs.

A

**Fluoxetine, **Citalopram, **Sertraline, (Escitalopram, Paroxetine, Fluvoxamine, Vilazodone)

(either two)

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5
Q

What is the mechanism for SSRIs?

A

SSRIs: selective blockade of 5HT reuptake

  • cause increase in extra cellular serotonin that initially activate 5HT(1A) autoreceptors, which inhibits serotonin release and reduce extra cellular serotonin to its previous level.
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6
Q

Most of the antidepressants inhibit uptake of ____ and ____.

A

Norepinephrine (NE) and serotonin (5HT)

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7
Q

What are the five main categories of antidepressants?

A

SSRIs- selective serotonin reuptake inhibitors- FIRST LINE DRUG

TCAs- tricyclic antidepressants- SECOND LINE DRUG

SNRIs- Serotonin/ Noradrenaline Receptor Inhibitors

MAOIs- Monoamine Oxidase Inhibitors

MA receptor antagonists

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8
Q

All antidepressants may provoke ____.

A

Seizure ( and no particular drug is safe for depressed epileptic patients)

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9
Q

Antidepressants need at least 2-3 weeks to work because ______.

A

To gradually change the sensitivity of central 5HT and/ or adenoceptors.

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10
Q

A second augmenting drug is normally added with antidepressant. What is it? It is also used in ____ and ____ for mood stabilising action.

A

Lithium (and needs to continue for at least 4-6 months)

Mania and bipolar affective disorders.

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11
Q

Abrupt withdrawal of antidepressant drugs (esp MAOIs) may cause ______.

A

Nausea, vomiting, panic, anxiety and motor restlessness.

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12
Q

What is monoamine theory?

A

Depression resulted from a decrease in activity of central noradrenergic and/or serotonergic systems.

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13
Q

Name three drugs that are used for mood - stabilising properties.

A

Lithium
Carbamazepine
Valproate

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14
Q

Serotonin cleared from synapse by ____, and subsequently breakdown by ____.

A

5-HT re-uptake transporter

intracellular monoamine oxidase A

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15
Q

What are the side effects of taking SSRIs?

A

nausea, agitation, insomnia, drowsiness, sexual dysfunction.

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16
Q

What do you need to be cautious when taking SSRIs?

A

Avoid taking with monoamine oxidase inhibitors (with at least 2 weeks gap). However low overdose risk.

*SSRIs should not be given to patients under 18 years old because this will increase the risk of suicidal behaviour.

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17
Q

What is TCAs (Tricyclic antidepressants)?

A

TCAs (Tricyclic antidepressants) refers to compounds based on dibenzazepine (eg. imipramine) and dibenzo-cycloheptadiene (eg. amitriptyline) ring structure.

It has similar blocking actions at cholinergic muscarinic receptor, alpha- adrenoreceptors and histamine receptors.

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18
Q

Explain the mechanism of TCAs and SNRIs (Serotonin/ Noradrenaline Reuptake Inhibitors).

A

> TCAs: non-specific blockade of 5HT and NE reuptake.

Serotonin and noradrenaline are cleared from synapse by 5HT and NA reuptake transporters, and subsequently breakdown by intracellular monoamine oxidase A (MAO) for both** and catechol-O-methyltransferase (COMT) only for NA**.

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19
Q

SSRIs have (more/less) effective than TCAs, but have worse side effect.

A

more

20
Q

What are the side effects of TCAs?

A

S/E: muscurinic and alpha-blockade,

sedation, seizures, anticholinergic S/E

21
Q

What do you need to be cautious about taking TCAs?

A
  • high risk from overdose (ventricular arrhythmia)
  • interact with other CNS depressants (i.e. alcohol)
  • avoid taking with MAOIs
22
Q

Give two examples of TCAs.

A
  • ** Amitriptyline (most used TCA; for neuropathic pain),
  • Desipramine,
  • Nortriptyline,
  • Clomipramine (Dosulepin, Doxepin, Lofepramine- least dangerous but leads to hepatotoxicity, Trimipramine, Imipramine)
23
Q

Give an example of SNRIs that are not NA-selective inhibitors, and give some details about these drugs.

A

** Venlafaxine- inhibits the reuptake of both 5HT and norepinephrine, is weak and non-selective (may be 5-HT selective), metabolite desvenlafaxine inhibits NA uptake, low risk of overdose.

Duloxetine- use for anxiety disorder. Non-selective and also inhibits DA uptake. Fewer S/E than Venlafaxine, and low risk of overdose.

24
Q

Give some examples of SNRIs that are NA-selective inhibitors, and it’s side effects.

A

** Reboxetine- safe in overdose. [S/E: dizziness, insomnia, anticholinergic effect]

Maprotiline- [S/E: as TCAs]

25
Q

State the major use of TCAs.

A
  • major depression
  • phobic and panic anxiety state
  • OCDs (obsessive-compulsive disorders)
  • neuropathic pain
  • enuresis (involuntary vibration)
26
Q

State the toxicity of TCAs

A

3 ‘C’s: coma, convulsions, and cardiotoxicity

27
Q

State the drug interaction of TCAs

A
  • hypertensive crisis with MAO inhibitors
  • Serotonin syndrome with SSRIs, MAO inhibitors, and meperidine
  • prevent antiHT action of alpha-2 agonists
28
Q

State the types of Monoamine receptors (in depression).

A

1) Adrenergic alpha-2 receptors (Gi- linked GPCR) decrease cAMP
2) 5-HT2 receptors (Gq- linked GPCR) IP3- mediated Ca2+ release
3) 5-HT3 receptors (Ligand gated cation channel)

29
Q

Examples of monoamine receptor antagonists/ blocker (MARA) as anti-depressant.

A

1) ** Mirtazepine:
- Blocks adrenergic a2, 5-HT2C & 5-HT3 receptors, increases 5HT and nor-adrenaline release.
- S/E: Dry mouth, increased appetite & weight gain, drowsiness, insomnia

2) Trazodone
- Blocks 5-HT2A, 5-HT2C, Histamine H1, increases 5HT release.
- S/E: Sedation, hypotension, nausea, cardiac dysrhythmias, dizziness

Others: mianserin

30
Q

What is monoamine receptor antagonists/ blocker (MARA)?

A
  • they are sedative antidepressants, which have little or no activity on amine uptake.
  • they are less cardiotoxic, thus less S/E
31
Q

State the mechanism of MAO inhibitors

A

irreversible inhibition of MAO(A) and MAO(B)

Details:
- Serotonin cleared from synapse by 5-HT & NA re-uptake transporters

  • Subsequent breakdown by intracellular monoamine oxidase A, and catechol-O-methyltransferase (NA only)
  • Some MAOIs nonselective; also inhibit MAO-B
32
Q

Use of MAO inhibitors

A

atypical depression

33
Q

Drug interactions of MAO inhibitors

A

1) serotonin syndrome: SSRIs, TCAs, meperidine

2) Increase Norepinephrine: HT crisis
- Symptoms: increase BP, arrhythmias, excitation, hyperthermia
- Drugs: TCAs, alpha-1 agonists, levodopa, releaser (i.e. tyramine)

34
Q

Examples of MAO inhibitors as anti-depressant.

A

1) Moclobemide:

> Selective MAO-A inhibitor. Short acting, reversible
S/E: Safer than older MAOIs; hypotension, nausea, insomnia, agitation.

2) Phenelzine:

> Non-selective MOA inhibitor.
S/E: “Cheese reaction”. Hypotension, insomnia, weight gain, anticholinergic effects, liver damage

3) Other: Isocarboxazid, tranylcypromine

35
Q

Give an example of selective MAO inhibitor.

A

Moclobemide

36
Q

In bipolar disorder, what drugs are given for treatment?

A
  • Conventional antidepressants controversial
  • usually given with additional anti-mania drug

> Lithium, Antiepileptics, Antipsychotics

37
Q

What is a typical medication use to treat biopolar? and state the mechanism, S/E and notes for this medication.

A

> Lithium

> Mechanism: selectively via certain Na+ channels (e.g. brain, kidneys). It accumulates, and not pumped out by Na+/K+ exchanger.

> S/E: Renal impairment, tremor, cognitive deficits

> Note: More effective against manic episodes than depressive.

38
Q

What is a typical medication more preferred to use over lithium to treat biopolar? and please give two examples.

A

Antiepileptics, as a mood stabaliser

e.g. Carbamezepine, valproate, lamotrigine

Note:
- Valproate and carbamazepine effective against manic phases, less against depression

  • Lamotrigine effective against mania and depression
39
Q

Examples of Antipsychotics for treating bipolar disorder.

A

e.g. Olanzapine, rispereridone, quietapine, aripiprazole

Highly effective against mania, but not depression.

40
Q

Pharmacology of depression is based on increasing _____ and _____ signalling in the brain.

A

serotinergic and noradrenergic signalling

41
Q

What is the first choice of drug types as antidepressant?

A

SSRIs are usually first choice;

then TCAs, SNRIs, Monoamine receptor antagonists.

42
Q

Bipolar disorder is normally treated via ____ or ____.

A

lithium or anticonvulsants.

43
Q

State the mechanism of lithium to treat Bipolar disorder.

A

1) prevent recycling of inositol (decrease PIP2) by blocking inositol monophosphatase
2) decrease cAMP

44
Q

State the S/E of Lithium to treat Bipolar disorder.

A
  • narrow therapeutic index
  • tremor, flu-like symptoms, life-threatening seizures
  • Hypothyroidism with goitre (decrease TSH effects and inhibition of 5’-deiodinase)
  • Nephrogenic Diabetes Insipidus (decrease ADH effect)
45
Q

State the teatogenicity of Lithium to treat Bipolar disorder.

A

Ebstein’s anomaly (malformation of tricuspid valve)

3: Pharmacology (6 decks)

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