Psychopharmacology Flashcards

1
Q

What are the four major categories of antidepressants?

A
  • Tricyclic antidepressants (TCAs)
  • Monoamine oxidase inhibitors (MAOIs)
  • Selective serotonin reuptake inhibitors (SSRIs)
  • Atypical antidepressants
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2
Q
  • What are the two most common agents to treat major depression?
A

SSRIs and atypical antidepressants

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3
Q

The choice of a particular medication used for a given patient should be made based on…

A
  • Patient’s symptoms
  • Previous treatment responses by the patient or a family member to a particular drug
  • Medication side effect profile
  • Comorbid conditions
  • Risk of suicide
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4
Q

What is the MOA of TCAs?

A

Inhibit the reuptake of NE and serotonin, increasing availability in the synapse

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5
Q

Why are TCAs rarely used as first-line agents?

A

Higher incidence of side effects, require greater monitoring of dosing, and can be lethal in overdose

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6
Q

What are some common TCAs?

A
  • Imipramine
  • Amitryptiline
  • Trimipramine
  • Nortriptyline
  • Despiramine
  • Clomipramine
  • Doxepin
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7
Q

What is the treatment for TCA overdose?

A

Sodium bicarbonate

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8
Q

What are the side effects of TCAs?

A

(Anti-HAM)

  • AntiHistaminic properties: sedation
  • AntiAdrenergic properties (CV SE): orthostatic hypotension, tachycardia, arrhythmias
  • AntiMuscarinic efects: dry mouth, constipation, urinary retention
  • Weight gain
  • Lethal in overdose (assess suicide risk)
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9
Q

What are the major complications of TCAs?

A

3Cs

  • Convulsions
  • Coma
  • Cardiotoxicity
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10
Q

What is the mechanism of action of MAOIs?

A

Prevent the inactivation of biogenic amines such as NE, serotonin, dopamine, and tyramine by irreversibly inhibiting the enzymes MAO-A and -B

Increase the amount of these transmitters in synapses

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11
Q

When are MAOIs considered very effective?

A

For certain types of refractory depression and in refractory panic disorder

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12
Q

What are some examples of MAOIs?

A
  • Phenelzine (Nardil)
  • Tranylcypromine (Parnate)
  • Isocarboxazid (Marplan)
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13
Q

What are the common SE of MAOIs?

A
  • Orthostatic hypotension
  • Drowsiness
  • Weight gain
  • Sexual dysfunction
  • Dry mouth
  • Sleep dysfunction
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14
Q

What is serotonin syndrome? What antidepressants can cause it?

A

Occurs when SSRIs and MAOIs are taken together

Characterized by lethargy, restlessness, confusion, flushing, diaphoresis, tremor, and myoclonic jerks

May progress to hyperthermia, hypertonicity, rhabdomyolysis, renal failure, convulsions, coma, and death

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15
Q

How can MAOis lead to hypertensive crisis?

A

When MAOIs are taken with tyramine-rich foods or sympathomimetics - causes a buildup of stored catecholamines

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16
Q

What is the MOA of SSRIs?

A

Inhibit presynaptic serotonin pumps, leading to increased availability of serotonin in synaptic clefts

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17
Q

What advantages do SSRIs have over other antidepressants?

A
  • Low incidence of side effects
  • No food restrictions
  • Much safer in overdose
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18
Q

What are some examples of SSRIs?

A
  • Fluoxetine (Prozac)
  • Sertraline (Zoloft)
  • Paroxetine (Paxil)
  • Fluvoxamine (Luvox)
  • Citalopram (Celexa)
  • Escitalopram (Lexapro)
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19
Q

Which SSRI has the longest half life?

A

Fluoxetine

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20
Q

Which SSRI is the most activating (stimulating) and most serotonin specific?

A

Paroxetine

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21
Q

Which SSRI has the highest risk for GI disturbances?

A

Sertraline

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22
Q

What are the side effects of SSRIs?

A
  • Sexual dysfunction (25-30%)
  • GI disturbance
  • Insomnia
  • Headache
  • Anorexia, weight loss
  • Serotonin syndrome when used with MAOIs
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23
Q

What are the types of atypical antidepressants?

A
  • Serotonin/NE reuptake inhibitors (SNRIs)
  • NE/Dopamine reuptake inhibitors (NDRIs)
  • Serotonin antagonist and reuptake inhibitors (SARIs)
  • NE and serotonin antagonists (NASAs)
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24
Q

What type of atypical antidepressant is Venlafaxine (Effexor)? When is it especially useful? When should it not be used?

A
  • SNRI
  • Especially useful in treating refractory depression and CAP
  • Can increase BP; do not use in patients with untreated or labile BP
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25
What type of atypical antidepressant is Bupropion (Wellbutrin)? When is Bupropion commonly used? What is its most significant advantage over SSRIs?
* NDRI * Commonly used to aid in smoking cessation, and also useful in the treatment of SAD and adult ADHD * Most significant advantage over SSRIs is relative lack of sexual side effects
26
What SE are seen with Bupropion at high doses? When is Bupropion contraindicated?
* Side Effects * Similar to SSRIs * Increased sweating and increased risk of seizures and psychosis at high doses * Not optimal for patients with significant anxiety * Contraindicated in patients with seizure or active eating disorders and those currently on MAOI
27
What type of atypical antidepressant are Nefazodone and Trazodone? When are they especially useful?
* SARIs * Especially useful in treatment of refractory major depression, major depression with anxiety and insomnia
28
What are some side effects of SARIs?
Nausea, dizziness, orthostatic hypotension, cardiac arrhythmias, **sedation,** and **priapism** (Trazadone)
29
What type of atypical antidepressant is Mirtazapine? When is it useful?
* NASA * Useful in treatment of refractory major depression, especially in patients who need to gain weight
30
What are some side effects of the NASAs?
* Sedation * Weight gain * Dizziness * Somnolence * Tremor * Agranulocytosis
31
At what dose do you reach the maximal sedative effect of Mirtazapine? What happens at higher doses?
Maximum sedative effect at doses 15 mg and less; at higher doses, it increases NE uptake and is therefore less sedating
32
What are the differences in MOA of traditional and atypical antipsychotics?
* Traditional: Work by blocking dopamine receptors * Atypical: Block both dopamine and serotonin receptors (effect on dopamine is weaker)
33
What is meant by "potency" when describing antipsychotics?
Potency refers to the action on dopamine receptors, not the level of efficacy
34
What are the low potency traditional antipsychotics? What are their characteristics?
* Chlorpromazine (Thorazine) and Thioridazine (Mellaril) * These antipsychotics have a higher incidence of anticholinergic and antihistaminic side effects than high-potency traditional antipsychotics * Lower incidence of extrapyramidal side effects (EPSEs) and neuroleptic malignant syndrome
35
What are the High Potency traditional antipsychotics? What are their characteristics?
* Haloperidol (Haldol), Fluphenazine (Prolixin), Trifluoperazine (Stelazine), Perphenazine (Trilafon), Pimozide (Orap) * These antipsychotics have higher incidence of EPSEs and neuroleptic malignant syndrome * They have lower incidence of anticholinergic and antihistaminic side effects
36
Which high potency antipsychotics are also available in long-acting forms?
Haloperidol and fluphenazine (IM injections)
37
Both traditional and atypical neuroleptics have similar efficacies in treating _______ psychotic symptoms Atypical antipsychotics have been shown to be more effective in treating _______ psychotic symptoms
Positive Negative
38
What are the side effects of traditional antipsychotics? (8)
1. Antidopaminergic effects (EPSEs) 2. Anti-HAM effects 3. Weight gain 4. Elevated liver enzymes, jaundice 5. Opthalmologic problems 6. Dermatologic problems 7. Seizures 8. Tardive dyskinesia
39
What are the Extrapyramidal side effects (EPSEs) associated with traditional antipsychotics?
* **Parkinsonism**: masklike face, cogwheel rigidity, pill rolling tremor * **Akathisia**: subjective anxiety and restlessness, objective fidgetiness * **Dystonia**: Sustained contraction of muscles of the neck, tongue, eyes (painful) * **Hyperprolactinemia**: Decreased libido, galactorrhea, gynecomastia, impotence, amenorrhea, osteoporosis
40
How are EPSEs treated?
* Reducing dose of antipsychotic * Administering antiparkinsonian, anticholinergic, or antihistaminic medications * Amantadine (Symmetrel) * Benadryl * Benztropine (Congentin)
41
What opthalmologic problems are associated with antipsychotic use?
Irreversible retinal pigmentation with high doses of Mellaril (Thioridazine), deposits in lens and cornea with Chlorpromazine
42
What causes tardive dyskinesia?
Hypothesized to be caused by increase in number of dopamine receptors, causing lower levels of acetylcholine
43
What are the characteristics of tardive dyskinesia?
* Choreoathetoid (writhing) movements of the mouth and tongue (patients who have used neuroleptics for more than 6 months) * Most often occurs in older women * 50% of cases will spontaneously remit, but untreated cases may be permanent
44
What is neuroleptic malignant syndrome?
A rare syndrome that occurs most often in males early in treatment with neuroleptics **Medical emergency** (20% mortality rate if untreated)
45
What are the symptoms of neuroleptic malignant syndrome?
FALTER * **F**ever * **A**utonomic instability (tachy, labile htn, diaphoresis) * **L**eukocytosis * **T**remor * **E**levated creatine phosphokinase (CPK) * **R**igidity (lead pipe rigidity considered universal)
46
What is the treatment for Neuroleptic Malignant syndrome?
* Discontinuation of current medications * Administration of supportive medical care (hydration, cooling) * Sodium dantrolene, bromocriptine, and amantadine are also useful * Patient can restart same neuroleptic at a later time
47
Which type of drug is first-line in the treatment of Schizophrenia?
Atypical antipsychotics
48
What are some examples of atypical antipsychotics?
* Clozapine (Clozaril) * Risperidone (Risperdal) * Quetiapine (Seroquel) * Olanzapine (Zyprexa) * Ziprasidone (Geodon)
49
What are the general side effects of atypical antipsychotics?
* Some anti-HAM effects * 1% incidence of agranulocytosis
50
What specific side effects are associated with clozapine?
* Agranulocytosis * 2-5% incidence of seizures
51
What specific side effects are associated with Olanzapine? What precautions are taken?
Can cause hyperlipidemia, glucose intolerance, weight gain, and liver toxicity Monitor liver function tests (LFTs)
52
What specific side effects are associated with Quetiapine? What are recommended precautions?
Less propensity for weight gain but has been shown to cause cataracts in beagle dogs Periodic (q6months) slit lamp examinations are recommended
53
What monitoring must accompany clozapine administration?
Patients on clozapine must have weekly blood draws to check white blood cell counts because it can cause agranulocytosis
54
What are the mood stabilizers?
Lithium, Carbamazepine, and Valproic acid
55
Aside from treating acute mania, what are other uses for mood stabilizers?
* Potentiation of antidepressants in patients with major depression refractory to monotherapy * Potentiation of antipsychotics in patients with schizophrenia * Enhancement of abstinence in treatment of alcoholism * Treatment of aggression and impulsivity
56
What is the first-line choice in treatment of acute mania and prophylaxis for both manic and depressive episodes in bipolar disorder?
Lithium
57
How is lithium secreted? How long is its onset of action? What is the major drawback of lithium use?
* Secreted by the kidney * Onset of action takes 5-7 days * High incidence of side effects and very narrow therapeutic index
58
What are the therapeutic, toxic, and lethal ranges of lithium blood levels?
* Therapeutic: 0.7 - 1.2 * Toxic: \> 1.5 * Lethal: \> 2.0
59
What factors affect lithium levels?
* NSAIDs (increase lithium levels) * Aspirin * Dehydration (increases lithium levels) * Salt deprivation (increases) * Impaired renal function (increases) * Diuretics
60
What are the main side effects of lithium?
* fine tremor, sedation, ataxia, thirst, metallic taste, polyuria, edema, weight gain, GI problems * **Hypothyroidism** * **Nephrogenic diabetes insipidus**
61
What can be caused by toxic lithium levels?
Altered mental status, coarse tremors, convulsions, and death
62
What is the best use of carbamazepine?
Especially useful in treating *mixed**-***episodes, and *rapid-cycling* bipolar disorder Also useful in managing trigeminal neuralgia
63
What is the MOA of Carbamazepine? What is its onset of action?
Anticonvulsant that works by blocking sodium channels and inhibiting action potentials Onset of action is 5-7 days
64
What are the main side effects of Carbamazepine (Tegetol)? What must be monitored when using this drug?
* Rash, drowsiness, ataxia, slurred speech, **leukopenia, hyponatremia, aplastic anemia**, and **agranulocytosis** * Elevates liver enzymes * Teratogenic effects when used during pregnancy * Neural tube defects * Pretreatment CBC and LFTs must be obtained and monitored regularly
65
Which anticonvulstant is especially useful in treating mixed manic episodes and rapid cycling bipolar disorder and is shown to increase CNS levels of GABA?
Valproic acid
66
What are the SE of Valproic acid? What monitoring is necessary?
* Side effects include sedation, weight gain, alopecia, hemorrhagic pancreatitis, **hepatotoxicity, and thrombocytopenia** * Teratogenic effects during pregnancy (neural tube) * Monitoring of LFTs and CBCs is necessary
67
What are the common indications for anxiolytics/hypnotics?
* Anxiety disorders * Muscle spasm * Seizures * Sleep disorders * Alcohol withdrawal * Anesthesia induction
68
What is the MOA of benzodiazepines?
Work by potentiating the effects of GABA
69
What substance should never be used when a patient is taking benzodiazepines (BDZs)?
Alcohol (BDZs can be lethal when mixed with alcohol)
70
What are the long acting BDZs (1-3 days)? (3) Which ones are rapid onset?
* Chlordiazepoxide used in alcohol detoxification * Diazepam: rapid onset * Flurazepam: rapid onset
71
What are the intermediate acting BDZs (10-20 hours)? (4) Which ones treat panic attacks? Which one treats insomnia?
* Alprazolam - treatment of panic attacks * Clonazepam - treatment of panic attacks * Lorazepam - treatment of panic attacks * Temazepam - treatment of insomnia
72
What are the short acting BDZs (3-8 hours)?
* Oxazepam * Triazolam
73
What are the side effects of BDZs? What is seen in BDZ intoxication?
* SE: Drowsiness, impairment of intellectual function, reduced motor coordination * Toxicity: Respiratory depression in overdose, especially when combined with alcohol
74
Which types of drugs are considered anxiolytics?
* Benzodiazepines * Barbiturates * Buspirone
75
What drugs are chemically not BDZs but have the same effect and are useful in short-term treatment of insomnia?
Zolpidem (Ambien) Zaleplon (Sonata)
76
What is the MOA of Buspirone? When is it used?
MOA: Anxiolytic reaction due to partial agonist action at 5HT-1A receptor Alternative to BDZ or venlafaxine for treating generalized anxiety disorder
77
Which beta blocker is useful in treating the autonomic effects of panic attacks or performance anxiety?
Propanalol
78
Which drugs have HAM side effects?
TCAs and low potency antipsychotics