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Pharm Exam 4 > Module 8 - Psychotherapeutics > Flashcards

Module 8 - Psychotherapeutics Flashcards

1
Q

What type of drug is Aripiprazole (Abilify) and what is its MOA?

A
  • Type: Antipsychotic
  • MOA: It is a partial agonist at 5HT1A and D2 and antagonist at 5HT3 receptors. Thus it enhances effects if dopamine levels are low but decreases effects if dopamine levels are high. As a partial agonist, it occupies all D2 receptors in the brain for a prolonged period of time but, because of its agonist effect, does not cause Parkinsonian side effects.
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2
Q

What are the indications for using Aripiprazole (Abilify)?

A

indicated for the treatment of schizophrenia, major depressive disorders and bipolar disorders (used to treat depression in adults as an add-on treatment to an antidepressant when an antidepressant alone is not enough)

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3
Q

What are some benefits to using Aripiprazole (Abilify) compare to other typical agents?

A

This drug causes no weight gain, hypotension, or prolactin release, no anticholinergic or dysrhythmic effects

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4
Q

What are some drug interactions associated with Aripiprazole (Abilify)?

A
  • CYP 3A4 inhibitors (e.g., ketoconazole) and 2D6 inhibitors (e.g. quinidine, fluoxetine) increase aripiprazole serum levels and the dose should be reduced to at least one-half the normal dose.
  • In contrast, 3A4 inducers (e.g., carbamazepine) may require a doubling of the aripiprazole dose.
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5
Q

What are the s/x associated with Aripiprazole (Abilify)?

A
  • Common side effects (>10%) include nausea, vomiting, constipation, headache, dizziness, akathisia (restlessness), anxiety & insomnia.
  • There are warnings of neuroleptic malignant syndrome (high fever, rigid muscles, shaking, confusion, sweating, increased heart rate & blood pressure) and tardive dyskinesia.
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6
Q

What are some blackbox warnings for with Aripiprazole (Abilify)?

A

increased mortality in elderly subjects when used off-label in elderly patients with dementia-related psychosis and increased risk of suicide in teenagers and young adults (approved only adults 18 and over with depression).

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7
Q

What type of drug is Rivastigmine (Exelon) and what are the indications for using it?

A
  • Type: Cholinesterase inhibitor
  • Indications: It is indicated for Alzheimer’s dementia as well as dementia associated with Parkinson’s disease.​
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8
Q

What are some advantages of using rivastigmine?

A

A potential advantage of rivastigmine is that it is metabolized by hydrolysis and thus is not susceptible to drug interactions associated with the P450 enzyme system.

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9
Q

What type of drug is Donepezil [Aricept] and what is its MOA?

A
  • Type: Acetylcholinesterase inhibitor
  • MOA: increase intracerebral levels of acetylcholine by inhibiting the breakdown of acetylcholine
    • They briefly improve cognition (memory, thought, recognition, awareness, behavior, & judgment).
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10
Q

What is the indication for using Donepezil [Aricept]?

A

indicated for the treatment of mild to severe dementia of the Alzheimer’s type.

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11
Q

What are the s/x associated with Donepezil [Aricept]?

A

Side effects are due to elevated acetylcholine, including nausea, vomiting, dyspepsia, diarrhea, dizziness, headache, and bronchoconstriction.

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12
Q

What time of the day should Donepezil [Aricept] be taken?

A

It is administered 5 or 10 mg once a day (although 10 mg provided no benefit over the 5 mg dose) in the evening just before sleeping

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13
Q

What type of drug is Buspirone (Buspar) and what is its MOA?

A
  • Type: Anxiolytic, sedative & hypnotic
  • MOA: Buspirone is not chemically related to any of the anxiolytic/sedative/hypnotic drugs. Its mechanism of action is unknown but it differs from the benzodiazepines in that it does not exert anticonvulsant or muscle relaxant effects, does not cause sedation, has no abuse potential, and does not intensify the effects of CNS depressants (benzodiazepines, alcohol, etc). It appears to have a high affinity for serotonin (5-HT1A) receptors but has no significant affinity for benzodiazepine receptors nor does it affect GABA binding.
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14
Q

What are the indications for using Buspirone (Buspar)?

A

Buspirone is indicated (5 mg tid) for management of anxiety disorders or for the short-term relief of symptoms of anxiety but may require 1-4 weeks before beneficial effects are seen

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15
Q

What are the s/x associated with Buspirone (Buspar)?

A
  • Buspirone’s use is not associated with prominent sedative effects nor does it have abuse potential.
  • Buspirone-treated patients show no rebound anxiety or withdrawal signs on abrupt discontinuance.
  • Most common side effects are dizziness, nausea, headache, nervousness, lightheadedness, and excitement. It does not affect driving skills nor potentiate the effect of CNS depressants.
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16
Q

What type of drug is Fluoxetine [Prozac] and what is its MOA?

A
  • Type: SSRI
  • MOA: Selectively blocks the neuronal reuptake of serotonin [5-HT], a monoamine neurotransmitter. As a result of the reuptake blockade, the concentration of serotonin in the synapse increases, causing increased activation of postsynaptic receptors.

This is the prototype drug

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17
Q

What are the indications for using Fluoxetine [Prozac]?

A

It is indicated for the treatment of depression, bulimia, panic disorder, and obsessive-compulsive disorder.

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18
Q

What are some drug interactions associated with Fluoxetine [Prozac]?

A
  • Fluoxetine appears to compete for elimination of TCA, hence producing high and prolonged blood levels of TCAs.
  • Deaths have been reported when used with MAOIs.
  • Fluoxetine inhibits CYP 2D6.
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19
Q

What are the s/x associated with Fluoxetine [Prozac]?

A
  • Headache, insomnia, drowsiness, nausea, diarrhea, weight loss, nervousness were side effects reported in >10% of patients.
  • Cardiac side effects were rare.
  • Discontinuation syndrome is reported when antidepressants are stopped abruptly. This is prevented by slowly decreasing the dose of the drug.
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20
Q

What are the advantages of using an SSRI for depression therapy?

A
  • The SSRIs are equally effective as the TCAs in the treatment of depression and pharmacodynamically they are very similar to each other.
  • The SSRIs are not faster acting or more effective than the TCAs but have a different side effect profile.
  • Absent with the SSRIs are sedation, weight gain, anticholinergic effect, and cardiovascular compromise see with the TCAs
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21
Q

What are some considerations to take when discontinuing an SSRI?

A
  • Withdrawal symptoms or “discontinuation syndrome” have been reported with all SSRIs, more with paroxetine, few with fluoxetine (because of long half-life of its active metabolite).
  • The most common symptoms include anxiety, paresthesia, confusion, tremor, sweating, irritability, memory problems, and anorexia.
  • Drugs should be withdrawn slowly.
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22
Q

What are the s/x associated with SSRI’s?

A
  • Side effects reported in more than 10% of patients include nausea, insomnia, sedation, headache, dizziness, agitation, fatigue, and dry mouth.
  • Movement disorders have been reported with the SSRIs.
  • The SSRIs have epileptogenic potential so must be used with caution in patients with a history of seizures.
  • Sexual dysfunction is common and often leads to non-compliance.
  • increased risk of GI bleeds in patients who take SSRIs
  • Risk of serotonin syndrome. This occurs most commonly when two drugs that enhance serotonin are used together.
  • Use with MAO inhibitors in contraindicated.
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23
Q

What are the signs and symptoms of serotonin syndrome?

A

Agitation, confusion, anxiety, incoordination, hyperreflexia, excessive sweating, tremor and fever.

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24
Q

What type of drug is Bupropion (Wellbutrin) and what is its MOA?

A
  • Type: Anti-depressant (SNRI, or serotonin-norepinephrine reuptake inhibitor). IT IS NOT AN SSRI OR TCA, related but not the same.
  • MOA: It is a weak blocker of reuptake of serotonin and norepinephrine and also inhibits reuptake of dopamine
25
Q

What are the indications for taking Bupropion (Wellbutrin)?

A
  • Depression - is often used as an alternative to other antidepressants because it does not cause sexual dysfunction, sedation, or weight gain.
26
Q

What are the s/x associated with Bupropion (Wellbutrin)?

A

Insomnia, agitation, anxiety, headache and dry mouth. Rarely, it causes dose-related seizures and is contraindicated in patients thought to have an increased risk of seizures.

27
Q

What are some drug interactions associated with Bupropion (Wellbutrin)?

A
  • Sympathomimetics: By blocking reuptake of NE, tricyclics can increase the pressor response to both indirect-acting sympathomimetics as well as epinephrine (as in local anesthetics). In patients receiving TCAs, if a pressor response is needed, use phenylephrine in reduced doses.
  • Anticholinergics: Be cautious of the use of centrally active anticholinergic drugs for preoperative medication because of increased likelihood of postoperative delirium and confusion.
  • Antihypertensives: TCAs may block the effect of centrally mediated antihypertensive action of methyldopa and clonidine.
  • Opioids: TCAs augment the analgesic, ventilatory depressant, and CNS depressant effects of opioids.
  • MAOI: Concomitant administration of MAO inhibitors and TCA may result in sudden and intense CNS and atropine-like effects. Deaths have been reported Contraindicated
  • SSRIs increase TCA blood level & toxicity.
28
Q

What is the drug of choice for Bipolar disorders?

A

Medical Letter Drug of Choice on “drugs for mania” states: Lithium is considered by many to be the drug of choice for long-term maintenance to prevent both manic and depressive episodes in patients with bipolar disorder

29
Q

What are the indications for using Lithium?

A
  • Lithium is indicated in the treatment or prevention of mania in manic-depressive patients. It is a “mood stabilizer”, preventing mood swings in patients with bipolar affective disorder.
  • It is the only mood stabilizer that has been demonstrated to lower the suicide rate in patients with bipolar disorder.
30
Q

What is the MOA of Lithium and how when should the drug be taken?

A
  • MOA: Lithium has a complicated set of actions on cells, but the relative importance of each is in doubt. Lithium must enter the cell to. act, so its onset is slow (takes 1-2 weeks to reach therapeutic effect). The mechanism is not clear
  • the therapeutic index is very small and the drug must be administered in divided daily doses. Take immediately after meals or with food to avoid stomach upset. Drink 8 to 12 glasses of water or liquid every day while taking this drug.
31
Q

What are the s/x associated with Lithium?

A

Before treatment is started one should obtain a CBC, urinalysis, common biochemical tests, and an ECG to serve as a baseline in assessing possible complications of treatment.

  • Edema, fine hand tremor, polydipsia and polyuria (30-50% of patients), and mild thirst may occur in patients at therapeutic levels.
    • Elderly patients may become confused even at therapeutic levels
  • Lithium may cause sedation
  • May also prolong the neuromuscular blocking effect of both depolarizing and nondepolarizing drugs.
  • Mild lithium toxicity is reflected by sedation, nausea, skeletal muscle weakness, and widening of the QRS complex.
  • Toxic lithium levels may cause renal damage, encephalopathy and coma.
    • Diuretics & NSAIDS quickly cause lithium toxicity.
  • Teratogen, Pregnancy Cat. D
32
Q

What type of drug is Valproic Acid [Depakote] and what is its MOA?

A
  • Type: Anticonvulsant
  • MOA: Its mechanism of action is not known. The correlation between blood levels and clinical effect is poor.​
33
Q

What are the indications for using Valproic Acid [Depakote]?

A
  • Useful in the prophylaxis of recurrence of manic attacks
  • Preferred drug for all manic episodes except euphoric mania.
  • Valproate is highly effective; it works faster and has a higher therapeutic index and a more desirable side effect profile than lithium.
34
Q

What are the s/x of Valproic Acid [Depakote]?

A
  • nausea, vomiting, dizziness, and somnolence.
  • In spite of these GI effects valproate may cause weight gain.
  • Depakote is enteric coated and may cause less GI distress than valproic acid
    *
35
Q

What type of drug is Methylphenidate [Ritalin] and what is its MOA?

A
  • Type: Drug for ADHD & narcolepsy
  • MOA: Methylphenidate is a mild CNS stimulant. The exact mechanism of action is not fully understood. One suggestion of the action of the drugs in ADHD is that low doses selectively stimulate inhibitory neurons. They may also stimulate the ascending reticuloarousal system (ARAS) to respond more appropriately to external stimuli, increasing tolerance to frustration and prolonging attention span.
36
Q

What are the indications for using Methylphenidate [Ritalin]?

A
  • indicated for the treatment of attention deficit disorders and narcolepsy (an overpowering desire for sleep).
  • The American Academy of Pediatrics suggests that children as young a 4 years of age may be treated for ADD or ADHD.
  • Methylphenidate (This is the DOC) has proved more effective than tricyclic antidepressants, caffeine, and other psychostimulants (e.g. pemoline and deanol) and has fewer side effects than does dextroamphetamine
37
Q

What are the s/x associated with Methylphenidate [Ritalin]?

A
  • Common side effects are motor or vocal tics, sleep disturbances (insomnia), depression, headache, stomach ache, suppression of appetite, elevated blood pressure, and, with large continuous doses, a reduction of growth.
  • Methylphenidate may lower seizure threshold.
  • Dexmethylphenidate has a black box warning of drug dependence.
38
Q

What are the drug interactions associated with Methylphenidate [Ritalin]?

A
  • The pharmacological effects of methylphenidate may be enhanced by MAO inhibitors.
  • Tolerance as well as euphoria and misuse are rare.
39
Q

What type of drug is Isocarboxazid [Marplan] and what is its MOA?

A
  • Type: MAOI
  • MOA: Irreversibly blocks MAO, A & B leading to increased intraneuronal concentrations of amine neurotransmitters such as dopamine, norepinephrine, epinephrine, and serotonin​
40
Q

What are some s/x associated with MAO inhibitors?

A
  • By forming the false transmitter, octopamine, the MAO inhibitors may produce hypotension.
  • However, the big concern is hypertensive crisis in patients who are given indirect-acting sympathomimetic amines (e.g. ephedrine, amphetamine) or foods rich in tyramine (certain processed cheeses, fermented sausages [e.g. salami] or pickled herring, and yeast extracts).
  • Direction CNS stimulation leads to the adverse effects of: Anxiety, Insomnia, Agitation, Hypomania, and even mania
41
Q

What are the indications for using MAO inhibitors?

A
  • MAO inhibitors areequal to SSRIs and TCAs for relieving depression. They are used only for patients with atypical depression or refractory to other antidepressants.
  • DOC for patients with atypical depression
42
Q

What are the signs & symptoms associated with a hypertensive crisis caused by MAO inhibitors?

A
  • headache, tachycardia, palpitations, N/V, sweating.
  • If these symptoms develop have the pt. seek medical attention immediately
43
Q

What are some drug interactions associated with MAO inhibitors?

A
  • Sympathomimetics can cause a hypertensive crisis
  • TCAs can cause a hypertensive crisis
  • SSRIs taken with MAO inhibitors can cause serotonin syndrome
  • Antihypertensive drugs taken with MAO inhibitors can further lower BP
44
Q

What type of drug is Phenelzine [Nardil]?

A

It is a MAO inhibitor

45
Q

What type of drug is Tranylcypromine?

A

It is a MAO inhibitor

46
Q

What type of drug is Lorazepam [Ativan] and what is its MOA?

A
  • Type: Benzodiazepine
  • MOA: By enhancing the effect of GABA in the limbic system, the benzodiazepines reduce anxiety. They promote sleep through effects on the cortical areas. They induce muscle relaxation through effects on supraspinal motor areas. They produce confusion and anterograde amnesia through action on the hippocampus and cerebral cortex. ​
47
Q

What are the indications for using Lorazepam (Ativan)?

A
  • DOC in elderly or subjects with liver cirrhosis
  • PO for treatment of anxiety
  • IV it is indicated for the treatment of status epilepticus or as a pre-anesthetic.
  • Indicated for chemotherapy-induced nausea & vomiting, acute alcohol withdrawal syndrome, and psychogenic catatonia
48
Q

What is the prototype drug for Benzodiazepines?

A

Diazepam [Valium]

49
Q

What are the s/x associated with benzodiazepines?

A
  • Sedation, ataxia, and psychomotor slowing. The benzodiazepines depress the CNS, cardiovascular, and respiratory systems but much less than the barbiturates.
  • Prolonged use can lead to dependence
  • Pregnancy Cat D. - They cause fetal deformities
  • Can increase the risk of falls in the elderly (use Lorazepam)
50
Q

What are the drug interactions associated with benzodiazepines?

A
  • These drugs undergo very few important interactions with other drugs.
  • They do not induce hepatic drug-metabolizing enzymes (they don’t accelerate the metabolism of other drugs)
51
Q

What type of drug is Olanzapine [Zyprexa] and what is its MOA?

A
  • Type: 2nd generation Atypical Anti-psychotics
  • MOA: Blocks receptors for serotonin, dopamine, histamine acetylcholine, and norepinephrine. Therapeutic effects are believed to results from blocking 5-HT2 and D2 receptors. Adverse effects result in part from blocking receptors for histamine, acetylcholine, and norepinephrine.
52
Q

What are the indications for using Olanzapine [Zyprexa]?

A
  • It is approved for treatment of schizophrenia and acute mania, and both manic and depressive episodes of bipolar disorder.
  • Olanzapine is equally effective and as safe as risperidone but olanzapine has a better response of negative symptoms, is longer lasting, and causes less EPS.
  • The medical letter suggests olanzapine may be the most effective of the antipsychotics but it also is most likely to cause metabolic adverse effects.
53
Q

What are the adverse effects of Olanzapine [Zyprexa]?

A
  • Adverse effects occurring more frequently than placebo included dizziness and somnolence, an increase in prolactin and weight gain.
  • Non-diabetic patients may develop diabetes and diabetes may be made worse in diabetic patients.
    • ​​Olanzapine caused ketoacidosis in a diabetic patient and caused elevation of triglycerides​
    • BG levels could not be controlled during olanzapine therapy
  • Other side effects were postural hypotension and constipation.
  • Anticholinergic effects, somnolence & orthostatic hypotension result from antagonism of H1 and α1 receptors.
  • However, the package brochure warns of neuroleptic malignant syndrome and tardive dyskinesia
54
Q

What type of drug is Haloperidol [Haldol] and what is its MOA?

A
  • Type: butyrophenones & antipsychotic
  • MOA: It blocks receptors for dopamine, acetylcholine, histamine, and norepinephrine. There is little question that blockade at these receptors is responsible for the major adverse effects of this drug. The current theory is that this drug suppresses symptoms of psychosis by blocking the dopamine receptors in the brain.
55
Q

What are the indications for using Haloperidol [Haldol]?

A
  • Haloperidol is used as the initial drug for treating psychotic disorders, in the treatment of Tourette’s syndrome and in controlling hyperactivity, particularly in children.
  • It is also used for some conditions in which other antipsychotic drugs are not used, including mental retardation, and Huntington’s disease.
  • Because it is available as an injection, it is often used to control acute mania in bipolar disorder.
56
Q

What are the s/x of using Haloperidol [Haldol]?

A
  • EPS reactions occur frequently (Acute dystonia, parkinsonism, akathisia)
  • Sedation, hypotension, and anticholinergic effects are uncommon
57
Q

What is the first-line drug for Borderline Personality Disorder?

A

Because valproic acid works faster, has a higher therapeutic index, and more desirable side effect profile than lithium, valproic acid has become a first-line treatment for BPD (Borderline Personality Disorder)

58
Q

What are some blackbox warnings for Valproic Acid?

A

There is a black box warning of pancreatitis and rarely may cause thrombocytopenia and liver failure.

Pharm Exam 4 (3 decks)

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