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Pharmacology > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

What is the monoamine hypothesis of depression?

A

Proposes that depression is due to a functional deficit of monoamine neurotransmitters like norepinephrine and serotonin at certain sites in the brain

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2
Q

Name the major classes of antidepressant drugs.

A

Tricyclic antidepressants (TCA) SSRIs SNRIs NRIs NDRIs MAO inhibitors Atypical antidepressants

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3
Q

What are SSRIs used for?

A

First-line treatment for depression and anxiety disorders

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4
Q

Name some common SSRIs.

A

Fluoxetine Fluvoxamine Paroxetine Sertraline Citalopram Escitalopram

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5
Q

What is the therapeutic lag for antidepressants?

A

2-4 weeks before a measurable therapeutic response is evident

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6
Q

Describe the neurotrophic hypothesis of depression.

A

Depression results from decreased neurotrophic support leading to neuronal atrophy decreased hippocampal neurogenesis and loss of glia

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7
Q

What is the role of BDNF in depression?

A

Brain-Derived Neurotrophic Factor (BDNF) is decreased in depression contributing to neuronal atrophy and reduced neurogenesis

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8
Q

List adverse effects common to SSRIs.

A

GI symptoms headache insomnia anxiety sexual dysfunction increased risk of GI bleeding serotonin syndrome discontinuation syndrome

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9
Q

What is serotonin syndrome?

A

A potentially life-threatening condition due to excessive serotonin causing symptoms like agitation confusion rapid heart rate and high blood pressure

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10
Q

What is the role of MAO inhibitors in treating depression?

A

Inhibit monoamine oxidase preventing the breakdown of monoamine neurotransmitters thus increasing their availability

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11
Q

Name some adverse effects of tricyclic antidepressants (TCAs).

A

Sedation weight gain dry mouth constipation urinary retention blurred vision tachycardia orthostatic hypotension

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12
Q

What is the role of norepinephrine reuptake inhibitors (NRIs)?

A

Increase norepinephrine levels by inhibiting its reuptake thus enhancing mood

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13
Q

What is the mechanism of action of SNRIs?

A

Inhibit the reuptake of both serotonin and norepinephrine

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14
Q

What is an important pharmacokinetic consideration for fluoxetine?

A

Fluoxetine has the longest half-life among SSRIs and must be discontinued 4 weeks before starting an MAOI

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15
Q

What is the role of neuroendocrine interactions in depression?

A

Dysfunction of the hypothalamic-pituitary-adrenal (HPA) axis and the role of stress response can contribute to depression

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16
Q

Name some drugs classified as atypical antidepressants.

A

Bupropion trazodone nefazodone mirtazapine mianserin agomelatine vortioxetine

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17
Q

What is the significance of active metabolites in antidepressants?

A

Active metabolites can affect the duration of drug action and influence switching from one medication to another

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18
Q

What is the role of glutamate in depression?

A

The glutamate hypothesis suggests that rapid actions of drugs like ketamine may be due to their effects on glutamate neurotransmission

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19
Q

Name the primary cellular targets for tricyclic antidepressants (TCAs).

A

Inhibit the reuptake of norepinephrine and serotonin

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20
Q

What is the main mechanism of action for SSRIs?

A

Selective inhibition of serotonin reuptake

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21
Q

Describe the pharmacokinetics of most SSRIs.

A

Good absorption significant liver metabolism (CYP450) and variable half-lives

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22
Q

What is a common adverse effect specific to paroxetine?

A

Increased risk of teratogenic effects (cardiac) in the first trimester of pregnancy

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23
Q

What are the therapeutic uses of SNRIs beyond depression?

A

Used for generalized anxiety disorder (GAD) panic disorder (PD) social anxiety disorder and chronic pain conditions

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24
Q

Describe the “switch” phenomenon in bipolar disorder treatment with antidepressants.

A

Antidepressants can induce a switch from a depressed episode to a manic or hypomanic episode in bipolar patients

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25
Q

What is the relationship between dietary sodium and lithium pharmacokinetics?

A

Alterations in dietary sodium can affect lithium levels as sodium depletion increases lithium reabsorption

26
Q

How does exercise affect lithium levels?

A

Exercise can alter sodium levels impacting lithium reabsorption and potentially causing toxicity or subtherapeutic levels

27
Q

What are the signs of lithium toxicity?

A

Nausea vomiting diarrhea tremor confusion seizures and potentially coma

28
Q

Why is lithium contraindicated in patients with renal impairment?

A

Reduced renal function can lead to lithium accumulation and toxicity

29
Q

What is the role of bupropion in depression treatment?

A

Acts as a norepinephrine-dopamine reuptake inhibitor (NDRI) and is also used for smoking cessation

30
Q

What is the importance of CYP450 interactions in antidepressant pharmacology?

A

Many antidepressants are metabolized by CYP450 enzymes and drug interactions can affect their levels and efficacy

31
Q

What is the mechanism of action of monoamine oxidase inhibitors (MAOIs)?

A

Inhibit the enzyme monoamine oxidase increasing levels of neurotransmitters like serotonin and norepinephrine

32
Q

What is the role of serotonin in the neurobiology of depression?

A

Serotonin deficits are associated with mood disorders and enhancing its levels can improve depressive symptoms

33
Q

What is the importance of neurogenesis in treating depression?

A

Increased neurogenesis particularly in the hippocampus is thought to correlate with the therapeutic effects of antidepressants

34
Q

How does fluvoxamine differ from other SSRIs in terms of enzyme inhibition?

A

Fluvoxamine is a potent inhibitor of CYP3A4

35
Q

What is the role of psychotropic medication in treating severe depression with suicidal risk?

A

Medications like ECT are used when rapid response is needed and delay in antidepressant effects is hazardous

36
Q

Describe the discontinuation syndrome associated with antidepressants.

A

Symptoms can include flu-like symptoms insomnia nausea imbalance sensory disturbances and hyperarousal

37
Q

What is the primary use of mirtazapine in depression treatment?

A

An atypical antidepressant with noradrenergic and specific serotonergic activity

38
Q

How do MAOIs interact with dietary tyramine?

A

MAOIs can cause hypertensive crisis when taken with tyramine-rich foods due to increased levels of tyramine

39
Q

What are the most common adverse effects of lithium?

A

Tremor hypothyroidism weight gain renal dysfunction and polyuria

40
Q

What is the clinical use of agomelatine?

A

Atypical antidepressant that acts as a melatonin receptor agonist and 5-HT2C antagonist

41
Q

What is the main therapeutic action of tricyclic antidepressants?

A

Inhibit the reuptake of norepinephrine and serotonin enhancing mood

42
Q

What is the pharmacological action of vortioxetine?

A

Atypical antidepressant that modulates serotonin receptor activity and inhibits serotonin reuptake

43
Q

How does nefazodone differ from trazodone?

A

Both are atypical antidepressants but nefazodone has a higher risk of hepatotoxicity

44
Q

What are the effects of antidepressants on anxiety during early treatment?

A

May increase anxiety agitation and suicidal ideation during the first few weeks

45
Q

What is the clinical significance of escitalopram?

A

S-enantiomer of citalopram with improved efficacy and fewer side effects

46
Q

Describe the cytokine hypothesis of depression.

A

Proposes that increased levels of pro-inflammatory cytokines contribute to depressive symptoms

47
Q

How do SNRIs differ from SSRIs in terms of neurotransmitter targets?

A

SNRIs inhibit the reuptake of both serotonin and norepinephrine while SSRIs are selective for serotonin

48
Q

What is the role of electroconvulsive therapy (ECT) in depression?

A

Used for severe depression especially when rapid treatment response is needed or other treatments have failed

49
Q

What are the most common side effects of tricyclic antidepressants?

A

Sedation anticholinergic effects orthostatic hypotension and cardiotoxicity

50
Q

What is the role of St. John’s wort in treating depression?

A

Herbal antidepressant that may interact with various drugs and has a risk of inducing serotonin syndrome

51
Q

How is bipolar disorder treated with anticonvulsants?

A

Anticonvulsants like valproate and lamotrigine are used for mood stabilization and to prevent manic episodes

52
Q

What are the potential interactions between SSRIs and NSAIDs?

A

Increased risk of gastrointestinal bleeding

53
Q

How does serotonin receptor antagonism contribute to antidepressant effects?

A

Blocking certain serotonin receptors can help alleviate depressive symptoms and improve mood

54
Q

What is the role of atypical antipsychotics in treating bipolar disorder?

A

Used for mood stabilization and treatment of acute manic episodes

55
Q

What are the implications of CYP450 polymorphism in antidepressant therapy?

A

Genetic variations can lead to differences in drug metabolism and response among individuals

56
Q

How does ketamine work as a rapid-acting antidepressant?

A

Acts on the glutamate system particularly NMDA receptors to produce quick antidepressant effects

57
Q

What is the clinical use of tricyclic antidepressants in neuropathic pain?

A

TCAs are effective in treating chronic neuropathic pain due to their analgesic properties

58
Q

What is the significance of serotonin-norepinephrine reuptake inhibition?

A

Provides a dual mechanism of action enhancing both serotonin and norepinephrine neurotransmission for improved efficacy in depression

59
Q

How does the inhibition of MAO contribute to the antidepressant effect?

A

Prevents the breakdown of monoamine neurotransmitters increasing their availability in the brain

60
Q

What are the therapeutic effects of bupropion?

A

Antidepressant and smoking cessation aid with a favorable side effect profile including minimal sexual dysfunction

Pharmacology (8 decks)

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