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Pharmacology Block 3 > Neuropsychopharmacology > Flashcards

Neuropsychopharmacology Flashcards

1
Q

Amitriptyline mechanism of action:

A
  • Blocks 5HT and NE reuptake.
  • Produces elevation of mood in depressed patients after about 2-3 weeks.
  • Restores a normal balance in monoaminergic transmission.
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2
Q

Amitriptyline uses:

A
  • Treatment of major depression and chronic pain.
  • Watch for drug interactions.
  • LONG plasma half-life.
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3
Q

Amitriptyline side effects:

A
  • Sedation, cardiac abnormalities (*use with caution in patients with recent myocardial infarctions).
  • *Overdose: acute toxicity. Hyperpyrexia, HTN or hypotension, seizures, coma and cardiac conduction defects.
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4
Q

Clomipramine mechanism of action:

A
  • Blocks 5HT and NE reuptake.
  • Produces elevation of mood in depressed patients after about 2-3 weeks.
  • Restores a normal balance in monoaminergic transmission.
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5
Q

Clomipramine uses:

A
  • Treatment of major depression and chronic pain.

- *Treatment of OCD.

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6
Q

Clomipramine side effects:

A
  • Sedation, cardiac abnormalities (*use with caution in patients with recent myocardial infarctions).
  • *Overdose: acute toxicity. Hyperpyrexia, HTN or hypotension, seizures, coma and cardiac conduction defects.
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7
Q

Fluoxetine mechanism of action:

A

SSRI

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8
Q

Fluoxetine uses:

A
  • Antidepressant
  • PMDD
  • Won’t produce SSR discontinuation disorder (self-tapering), and less side effects than TCAs (no headache, tremors, visual disturbances).
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9
Q

Sertraline mechanism of action:

A

SSRI

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10
Q

Sertraline uses:

A
  • Antidepressant

- OCD, PTSD, anxiety

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11
Q

Bupropion mechanism of action:

A

Weakly blocks NE and DA reuptake.

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12
Q

Bupropion uses:

A
  • Antidepressant
  • Nicotine withdrawal
  • SAD
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13
Q

Mirtazapine mechanism of action:

A
  • Blocks presynaptic alpha2 receptors in brain, causing a stimulation of NE release.
  • Also blocks alpha2 heteroreceptors, causing 5HT release.
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14
Q

Mirtazapine uses:

A

-Antidepressant

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15
Q

Mirtazapine side effects:

A

Increases appetite

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16
Q

Duloxetine mechanism of action:

A

Blocks both 5HT and NE uptake.

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17
Q

Duloxetine uses:

A

Rx more for pain than depression. Also approved for use in fibromyalgia.

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18
Q

Phenelzine mechanism of action:

A

Irreversible inhibitor of MAO (blocks the oxidative deamination of naturally occurring biogenic amines such as NE, DA, 5HT).

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19
Q

Phenelzine uses:

A
  • Antidepressant.
  • Can take about 2 weeks for it to work.
  • Not drug of choice (bad side effects).
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20
Q

Phenelzine side effects:

A
  • Acute toxicity can produce agitation, hallucinations, hyperpyrexia, convulsions and changes in BP.
  • *Food interaction – tyramine (which releases NE) can produce a hypertensive crisis.
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21
Q

Chlorpromazine mechanism of action:

A

Block DA pathways, particularly D2 receptors.

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22
Q

Chlorpromazine uses:

A

Antipsychotic with low to medium potency.

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23
Q

Typical antipsychotics possible side effects:

A
  • Pronounced anticholinergic actions.
  • Dystonias, parkinsonism, akathisia as a result of the DA receptor blockade.
  • Orthostatic hypotension.
  • Neuroleptic malignant syndrome: fever, mutism, EPS, possible death.
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24
Q

Atypical antipsychotics mechanism of action:

A
  • Blocks DA AND 5HT receptors.
  • Muscarinic antagonist.
  • Improves positive symptoms and negative symptoms.
  • Lowers seizure thresholds more than other antipsychotics.
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25
Q

Clozapine side effects:

A
  • May cause serious agranulocytosis or other blood dyscrasias.
  • Weight gain.
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26
Q

Clozapine uses:

A

Used for schizophrenia, bipolar disorder, personality disorder.

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27
Q

Typical antipsychotics potency:

A

Fluphenazine > Chlorpromazine > Thioridazine

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28
Q

Name the typical antipsychotics:

A
  1. Chlorpromazine
  2. Thioridazine
  3. Fluphenazine
  4. Haloperidol
29
Q

Olanzapine mechanism of action and use:

A

DA and 5HT antagonist - more profound 5HT antagonism than clozapine.
Approved to augment antidepressant action.

30
Q

Olanzapine side effects:

A

Profound weight gain and diabetes risk.

31
Q

Risperidone misc fact:

A

Low incidence of extrapyramidal side effects.

32
Q

Quetiapine uses:

A

Shorter half life than the other atypicals - approved for augmentation against depression.

33
Q

Aripiprazole mechanism of action and use:

A

D2 partial agonist.

Approved as an adjunct against depression.

34
Q

Name the atypical antipsychotics:

A
  1. Clozapine
  2. Olanzapine
  3. Risperidone
  4. Quetiapine
  5. Aripiprazole
35
Q

Lithium MOA:

A

Blocks phosphatase converting IP2 to IP1.

36
Q

Lithium uses:

A
  • Used for the treatment of mania and bipolar disease.

- Increased Na+ excretion causes clinically significant increases in Li levels.

37
Q

Lithium side effects:

A
  • Fatigue
  • GI symptoms
  • Contraindicated in pregnancy.
38
Q

Valproic acid MOA:

A

Blocks repetitive neuronal firing, may reduce T-type Ca++ currents, increases GABA concentration.

39
Q

Valproic acid uses:

A
  • Antiseizure drug.
  • Bound to plasma protein – competes with phenytoin.
  • Inhibits metabolism of phenobarbital, phenytoin, carbamazepine.
40
Q

Valproic acid side effects:

A
  • GI symptoms
  • Weight gain
  • Teratogenicity: spina bifida.
41
Q

Divalproex MOA:

A

Blocks repetitive neuronal firing, may reduce T-type Ca++ currents, increases GABA concentration.

42
Q

Divalproex uses:

A
  • Antiseizure drug.
  • Bound to plasma protein – competes with phenytoin.
  • Inhibits metabolism of phenobarbital, phenytoin, carbamazepine.
43
Q

Divalproex side effects:

A
  • GI symptoms
  • Weight gain
  • Teratogenicity: spina bifida.
44
Q

Carbamazepine MOA:

A

Alters ion conductance with use-dependent effect on Na+ channels. Inhibits the generation of repetitive APs.

45
Q

Carbamazepine uses:

A
  • Antiseizure therapy.
  • Bipolar I disorder.
  • Acute manic episodes.
46
Q

Carbamazepine side effects:

A
  • GI symptoms
  • Drowsiness
  • Contraindicated in elderly patients.
47
Q

Benzodiazepines MOA:

A

Act at sites on the GABA receptor-chloride ion channel complex. Binding at BDZ & GABAA receptor increases chloride conductance, hyperpolarizes the membrane (less likely to fire an AP).

48
Q

Benzodiazepine misc:

A

Has potential for drug abuse. Treat abuse with dose reduction.

49
Q

Benzodiazepine side effects:

A
  • Alcohol acts on the same sites – possibility for drug interactions.
  • Produce additive CNS depression with other depressive drugs.
  • Sedation is biggest adverse effect.
50
Q

Barbiturate vs BDZ:

A

Barbiturates only act on GABAa receptor.

51
Q

Alprazolam MOA:

A

GABA enhancement.

52
Q

Alprazolam uses:

A
  • Anxiolytic, *antipanic.
  • Short duration, fast onset.
  • Forebrain depression, dependence.
53
Q

Buspirone MOA:

A

Partial agonist at 5-HT1A receptor. Also binds to D2 receptors.

54
Q

Buspirone uses:

A
  • Anxiolytic with delayed onset.

- Little sedation, no dependence.

55
Q

Chloral hydrate uses:

A

-Sedative hypnotic.

56
Q

Chloral hydrate SEs:

A

-Bad taste.

57
Q

Diazepam uses:

A
  • Anxiolytic, sedative, *muscle relaxant.
  • Broad CNS depression, dependence.
  • Long duration, most rapidly absorbed.
58
Q

Diazepam MOA:

A

GABA enhancement.

59
Q

Flumazenil MOA:

A

GABAa receptor antagonist.

60
Q

Flumazenil uses:

A

Used as an antidote to BDZ side effects.

61
Q

Flurazepam uses:

A

Primarily used for its hypnotic actions.

62
Q

Lorazepam uses:

A

Used for hypnotic actions - NO active metabolite.

63
Q

Phenobarbital MOA:

A

GABA enhancement.

64
Q

Phenobarbital uses:

A

Most widely used anti-seizure drug.

65
Q

Zolpidem MOA and use:

A

Binds to omega-1 BDZ receptor.

Use to achieve sleep, less effects on sleep architecture and won’t produce daytime drowsiness.

66
Q

Baclofen MOA and use:

A

GABA mimetic agent that works at GABAb receptors. Results in hyperpolarization, causing presynaptic inhibition. Results in decreased release of excitatory transmitters such as glutamate.

Use to treat muscle spasticity.

67
Q

Tizanidine MOA and use:

A

Alpha2 agonist that may enhance presynaptic and postsynaptic inhibition.

Treats spasticity, albeit with drowsiness.

68
Q

Typical antipyschotics vs atypicals:

A

Typicals block DA reuptake, while atypicals block DA as well as 5HT reuptake.

Typicals help with positive symptoms, while atypicals help with positive symptoms and more negative symptoms.

Pharmacology Block 3 (11 decks)

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