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.
2
Q
Amitriptyline uses:
A
- Treatment of major depression and chronic pain.
- Watch for drug interactions.
- LONG plasma half-life.
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.
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.
5
Q
Clomipramine uses:
A
- Treatment of major depression and chronic pain.
- *Treatment of OCD.
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.
7
Q
Fluoxetine mechanism of action:
A
SSRI
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).
9
Q
Sertraline mechanism of action:
A
SSRI
10
Q
Sertraline uses:
A
- Antidepressant
- OCD, PTSD, anxiety
11
Q
Bupropion mechanism of action:
A
Weakly blocks NE and DA reuptake.
12
Q
Bupropion uses:
A
- Antidepressant
- Nicotine withdrawal
- SAD
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.
14
Q
Mirtazapine uses:
A
-Antidepressant
15
Q
Mirtazapine side effects:
A
Increases appetite
16
Q
Duloxetine mechanism of action:
A
Blocks both 5HT and NE uptake.
17
Q
Duloxetine uses:
A
Rx more for pain than depression. Also approved for use in fibromyalgia.
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).
19
Q
Phenelzine uses:
A
- Antidepressant.
- Can take about 2 weeks for it to work.
- Not drug of choice (bad side effects).
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.
21
Q
Chlorpromazine mechanism of action:
A
Block DA pathways, particularly D2 receptors.
22
Q
Chlorpromazine uses:
A
Antipsychotic with low to medium potency.
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.
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.
25
Clozapine side effects:
- May cause serious agranulocytosis or other blood dyscrasias.
- Weight gain.
26
Clozapine uses:
Used for schizophrenia, bipolar disorder, personality disorder.
27
Typical antipsychotics potency:
Fluphenazine > Chlorpromazine > Thioridazine
28
Name the typical antipsychotics:
1. Chlorpromazine
2. Thioridazine
3. Fluphenazine
4. Haloperidol
29
Olanzapine mechanism of action and use:
DA and 5HT antagonist - more profound 5HT antagonism than clozapine.
Approved to augment antidepressant action.
30
Olanzapine side effects:
Profound weight gain and diabetes risk.
31
Risperidone misc fact:
Low incidence of extrapyramidal side effects.
32
Quetiapine uses:
Shorter half life than the other atypicals - approved for augmentation against depression.
33
Aripiprazole mechanism of action and use:
D2 partial agonist.
| Approved as an adjunct against depression.
34
Name the atypical antipsychotics:
1. Clozapine
2. Olanzapine
3. Risperidone
4. Quetiapine
5. Aripiprazole
35
Lithium MOA:
Blocks phosphatase converting IP2 to IP1.
36
Lithium uses:
- Used for the treatment of mania and bipolar disease.
| - Increased Na+ excretion causes clinically significant increases in Li levels.
37
Lithium side effects:
- Fatigue
- GI symptoms
- Contraindicated in pregnancy.
38
Valproic acid MOA:
Blocks repetitive neuronal firing, may reduce T-type Ca++ currents, increases GABA concentration.
39
Valproic acid uses:
- Antiseizure drug.
- Bound to plasma protein – competes with phenytoin.
- Inhibits metabolism of phenobarbital, phenytoin, carbamazepine.
40
Valproic acid side effects:
- GI symptoms
- Weight gain
- Teratogenicity: spina bifida.
41
Divalproex MOA:
Blocks repetitive neuronal firing, may reduce T-type Ca++ currents, increases GABA concentration.
42
Divalproex uses:
- Antiseizure drug.
- Bound to plasma protein – competes with phenytoin.
- Inhibits metabolism of phenobarbital, phenytoin, carbamazepine.
43
Divalproex side effects:
- GI symptoms
- Weight gain
- Teratogenicity: spina bifida.
44
Carbamazepine MOA:
Alters ion conductance with use-dependent effect on Na+ channels. Inhibits the generation of repetitive APs.
45
Carbamazepine uses:
- Antiseizure therapy.
- Bipolar I disorder.
- Acute manic episodes.
46
Carbamazepine side effects:
- GI symptoms
- Drowsiness
- Contraindicated in elderly patients.
47
Benzodiazepines MOA:
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
Benzodiazepine misc:
Has potential for drug abuse. Treat abuse with dose reduction.
49
Benzodiazepine side effects:
- Alcohol acts on the same sites – possibility for drug interactions.
- Produce additive CNS depression with other depressive drugs.
- Sedation is biggest adverse effect.
50
Barbiturate vs BDZ:
Barbiturates only act on GABAa receptor.
51
Alprazolam MOA:
GABA enhancement.
52
Alprazolam uses:
- Anxiolytic, *antipanic.
- Short duration, fast onset.
- Forebrain depression, dependence.
53
Buspirone MOA:
Partial agonist at 5-HT1A receptor. Also binds to D2 receptors.
54
Buspirone uses:
- Anxiolytic with delayed onset.
| - Little sedation, no dependence.
55
Chloral hydrate uses:
-Sedative hypnotic.
56
Chloral hydrate SEs:
-Bad taste.
57
Diazepam uses:
- Anxiolytic, sedative, *muscle relaxant.
- Broad CNS depression, dependence.
- Long duration, most rapidly absorbed.
58
Diazepam MOA:
GABA enhancement.
59
Flumazenil MOA:
GABAa receptor antagonist.
60
Flumazenil uses:
Used as an antidote to BDZ side effects.
61
Flurazepam uses:
Primarily used for its hypnotic actions.
62
Lorazepam uses:
Used for hypnotic actions - NO active metabolite.
63
Phenobarbital MOA:
GABA enhancement.
64
Phenobarbital uses:
Most widely used anti-seizure drug.
65
Zolpidem MOA and use:
Binds to omega-1 BDZ receptor.
Use to achieve sleep, less effects on sleep architecture and won't produce daytime drowsiness.
66
Baclofen MOA and use:
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
Tizanidine MOA and use:
Alpha2 agonist that may enhance presynaptic and postsynaptic inhibition.
Treats spasticity, albeit with drowsiness.
68
Typical antipyschotics vs atypicals:
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.
