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CNS Drugs > L7-8 Antipsychotics > Flashcards

L7-8 Antipsychotics Flashcards

1
Q

What is thought to cause the psychosis and positive symptoms in Schizophrenia?

A

Increased DA in the mesolimbic system

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2
Q

What is thought to cause the negative symptoms and cognitive dysfunction in patients with Schizophrenia?

A

Decreased DA in the hippocampus and prefrontal cortex

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3
Q

How do the classical antipsychotics work vs. the newer atypical antipsychotics?

A

Classic-block D2, treat positive symptoms, no help in negative symptoms

Newer, Atypical-block 5-HT2a, treat negative symptoms better

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4
Q

What are 5 mechanisms that can be theoretically used to treat Schizophrenia?

A

Block D2: classical antipsychotics

Block 5-HT2a: newer antipsychotics. Facilitates DA release in prefrontal cortex to treat negative symptoms

Stimulate NMDA receptors (glutamate): increases DA in mesocortical (combats negative symptoms) and decreases DA in mesolimbic (combats positive symptoms)

Increase GABA: decreased GABA synthesis has been reported in schizophrenia and bipolar perhaps as a result of decreased activity of NMDA receptors. Decrease in GABA leads to overstimulation of cortical neurons

Stimulate M4 receptors (in trial): improve cognitive disorders

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5
Q

What types of receptor blockade do most of the side effects come from with the antipsychotics?

A

muscarininc blockade

alpha-adrenergic blockade

histamine blockade

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6
Q

What are the low potency Phenothiazines?

How do they work?

What types of side effects do they cause?

A

Chlorpromazine and Thioridazine

Block D2, alpha, histamine

Very effective but require high doses

Considerable anti-cholinergic effects, less likely to cause extrapyramidal symptoms

More sedation and hypotension

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7
Q

What are the high potency Phenothiazines?

How do they work?

What types of side effects do they cause?

A

Fluphenazine and trifluoperazine

High potency, more selective for DA receptors

Less anti-cholinergic effects, more likely to cause extrapyramidal symptoms

Less sedation and hypotension

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8
Q

What are the side effects of the classical antipsychotics?

A

Extrapyramidal effects: due to blockage of DA receptors in nigrostriatal system (motor control, Parkinsonian sx), treated with anti-cholinergic drugs

Tardive Dyskinesia: uncontrollable movements of mouth, tongue, face, clozapine and olanzapine less likely to cause

Endocrine effects: weight gain, increarse prolactin release (DA inhibits prolactin), decrease release of sex hormones (decreased libido, infertility, amenorrhea, gynecomastia)

Autonomic effects: due to blockage of muscarininc (dry mouth, blurred vision, constipation, tahycardia), alpha (orthostatic hypotension, difficulty ejaculating), and histamine (sedation)

Seizures: slow frequency of EEG

Neuroleptic Malignant Syndrome: life-threatening-muscle rigidity, catatonia, increase temp, change BP and HR

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9
Q

Which antipsychotics are least likely to cause tardive dyskinesia?

A

clozapine and olanzapine

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10
Q

Which antipsychotics are seizures most likely to occur with?

What patients should not be given antipsychotics?

A

Clozapine, olanzapine, chlorpromazine

Used with caution in untreated epileptics and patients who are withdrawing from CNS depressants

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11
Q

What is neuroleptic malignant syndrome?

How do you treat it?

A

Life-threatening side effect of the classical antipsychotics: muscle rigidity, catatonia, increase in body temp, altered BP and HR

Tx: discontinue antipsychotic immediately, supportive care

Dantrolene, diazapan, and dopamine agonists may also be used

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12
Q

Name the Phenothiazines.

What are they used for?

A

Chlorpromazine, Thioridazine, Fluphenazine, Trifluoperazine, Prochlorperazine

Widely used to treat schizophrenia, used in psychotic episodes, manic episodes, hallucinations

Other uses: nausea, vomitting, pre-anesthetic sedation, premature ejaculation, relieves severe itching

Low potency drugs (chlor and thio): high anti-cholinergic activity-increases autonomic side effects, lower chance of extrapyramidal symptoms

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13
Q

What is important about the phamacokinetics of the phenothiazines?

A

Absorbed erratically when taken orally

Effective IM

24-48 hr half-life, very slow liver elimination

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14
Q

What are the side effects of Phenothiazines?

A

Anticholinergic: blurred vision, constipation, dry mouth, urinary retention, decreased GI motility

Alpha blockade: postural hypotension, inhibition of ejaculation

Negative inotropic action

Mild jaundice in 2nd to 4th week

Decrased seizure threshold (worse with chlorpromazine)

Thioridazine: retinal deposits

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15
Q

Haloperidol

A

Selective blocking of D2 receptors

Similar effects to phenothiazines: sedation, indifference, reduced initiative, decreased anxiety

Well absorbed orally

Often injected in acute situations

Concentration in brain can be much higher than in blood

Slow metabolism and excretion, blood levels stable for 3 days

Most likely of all antipsychotics to cause extrapyramidal symptoms

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16
Q

Pimozide

A

Similar to haloperidol, blocks D2

Can be used for motor and phonic tics in patients with Tourette’s

High extrapyramidal symptoms, moderate sedation, moderate anti-cholinergic

ECG changes, lengthen QT interval

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17
Q

Loxapine

A

Similar to phenothiazines

Used when other drugs have not worked

Lowers seizure threshold more than phenothiazines

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18
Q

Molindone

A

D2 blockade

Moderate sedation, increases motor activity, mild euphoria

Extrapyramidal effects, xerostomia, constipation, hypotension, syncope, tachycardia

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19
Q

Clozapine

A

Atypical antipsychotic, Improves negative symptoms

Binds D4 (mainly in limbic and cerebral cortex and not in striatum) causing lower incidence of extrapyramidal symptoms

Binds 5-HT2a: faciliatates DA release in prefrontal cortex

Inhibits muscarinic, alpha, and histamine receptors

Unlikely to cause tardive dyskinesia

Treat delusions in Parkinson’s disease

Use is reserved for patients who do not respond to conventional drugs

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20
Q

What are the side effects of Clozapine?

A

Sedation

Decreased seizure threshold

Hypotension, tachycardia

Increased salivation, dizziness

Weight gain

Agranulocytosis in 1%-serious!

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21
Q

Olanzapine

A

Similar to clozapine

Blocks D2, D4, 5-HT2a (more effective for negative symptoms)

anticholinergic, extrapyramidal rare

Can improve positive and negative symptoms

Also used to treat bipolar

Does not cause agranulocytosis, less toxicity than clozapine

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22
Q

What are the side effects of Olanzapine?

A

Weight gain-very common

Sedation and dizziness

Orthostatic hypotension

Akathisia (restlessness, anxiety, pacing)

Constipation

Increased incidence of hyperglycemia and type II diabetes

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23
Q

What antipsychotic is most likely to cause weight gain and a high incidence of hyperglycemia and type II diabetes?

A

Olanzapine

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24
Q

Risperidone

A

Atypical antipsychotic

Very effective at relieving positive AND negative symptoms

Used in combo with SSRIs to in treatment resistant depression and in autism

Inhibits D2 and especially 5-HT2a, blocks alpha receptors

Enhances DA in basal ganglia-few extrapyramidal

Low incidence of tardive dyskinesia

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25
Q

What is Paliperidone?

A

The active metabolite of risperidone (atypical antipsychotic)

Supplied as extended release product

26
Q

What is significant about the pharmacokinetics of Risperidone?

A

Well absorbed orally

Highly protein bound

27
Q

What are the side effects of Risperidone?

A

Alpha antagonist: postural hypotension

Agitation, anxiety, insomnia

Headache, nausea, weight gain

extrapyramidal at hihg doses

lengthens QT interval

Increased prolactin release may occur

28
Q

Ziprasidone

A

Similar to risperidone

Blocks D2 and 5-HT2a

Some antidepressant activity

Used in Tourette’s and to treat acute mania

Not as likely to cause weight gain

Orally or IM

29
Q

What are the side effects of Ziprasidone?

A

Prolongs QT interval: avoid in patients with cardiac conduction defects, recent MI, taking TCAs

Sedation and impairs cognitive and motor skills in initial days of tx

May cause hyperprolactinemia

Use in caution with seizure disorders or other drugs that decrease seizure threshold

30
Q

Quetiapine

A

Similar to clozapine, no agranulocytosis

Improves positive and negative symptoms

Few extrapyramidal

Used as adjunct in depression tx

Helps sleep problems in patients with depression

Used as monotherapy in bipolar depression

31
Q

Asenapine

A

Blocks multiple 5-HT receptors (2a and 2c)

Not a strong D2 blocker, but blocks D3

Histamine and alpha1 blocker

Small increase in QT

Less metabolic effects, less likely to cause weight gain

Used off label for tx of nightmares in patients with PTSD

32
Q

Aripiprazole (Abilify)

A

First in a new class called “dopamine system stabilizers”

Activates DA receptors in DA tone is low and blocks DA receptors if tone is high

Partial D2 and 5-HT1a agonist

Antagonist at 5-HT2a

Histamine and alpha1 blocker

No effect on prolactin or QT interval

Unlikely to cause weight gain in adults

Tx of drug-resistant depression and antipsychotic effects

33
Q

What are the side effects of Aripiprazole?

A

Orthostatic hypotension

Elevations in blood glucose: diabetes may develop or worsen

Seizures

Sedation

Decrases motility of esophagus: used in caution in elderly (risk of aspiration pneumonia)

Decreases ability to regulate body temp in hypothalamus

Low incidence of extrapyramidal effects

34
Q

Iloperidone

A

Atypical antipsychotic

Blockade of D2 and 5-HT2a

alpha blockade, no muscarinic effect

35
Q

Lurasidone

A

Atypical antipsychotic

Blocks D2 and 5-HT2a, partial agonist at 5-HT1a

NO antihistamine or antimuscarinic effect

Used in tx of depression associated with bipolar

Some incidence of agranulocytosis and neutropenia-monitor blood counts

36
Q

What two things decrease antipsychotic concentration by inducing liver enzymes and increasing metabolism?

A

Carbamazepine and Smoking

37
Q

What if given with an antipsychotic will cause increased sedation?

What will cause increased side effects such as dry mouth and urinary retention?

A

Sedative-hypnotics

Anti-cholinergics

38
Q

What are the first line drugs for Schizophrenia and why?

When would you give Clozapine?

A

Risperidone, Quetiapine, Olanzapine
due to low incidence of extrapyramidal effects

Clozapine is reserved for paitens who fail to respond to at least two others, or who are disabled by tardive dyskinesia. Clozapine is expensive and needs frequent blood monitoring due to possibility of agranulocytosis

39
Q

Which antipsychotics are most commonly used for Tourette’s syndrome?

A

Haloperidol and Pimozide

40
Q

What is the recommendations for the use of antipsychotics in Alzheimer’s disease?

A

Risperidone has been used but increased mortality.

Use of antipsychotics is not recommended in elderly patients, especially with dementia.

41
Q

What antipsychotic is frequently used as an antiemetic?

A

Prochlorperazine

42
Q

What antipsychotics can be used as adjunct drugs for treatement-resistant depression?

A

Quetiapine, olanzapine, aripiprazole

43
Q

How is Lithium used when treatment is started for bipolar disorder?

A

The onset of action of lithium is slow, so it is common to begin with antipsychotics and/or benzos until mania is controlled, and then maintain on lithium alone.

An antidepressant can be added in the depressive phase.

Maintainance with lithium can prevent both mania and depression and decrease suicide risk.

44
Q

How is lithium excreted?

What is the optimal concentration range?

When is a steady state reached?

A

Excreted by kidney

Optimal concentrations range from 0.6-1.2 mEq/L

Steady-state is generally reached within 5-6 days of treatment

45
Q

What 3 mechanisms can increase lithium concentration?

A
  1. Lithium is reabsorbed by the proximal tubule in the kidney and competes with sodium reabsorption

Decreases in sodium (decrease salt intake, hot weather, exercise) will increase lithium concentration

  1. Thiazide diuretics decrease the clearance of lithium
  2. NSAIDs also decrease lithium clearance
46
Q

What drugs are most commonly used to treat bipolar disorder?

A

Lithium, Valproic acid, Carbamazepine

Lurasidone, Lamotrigine, and Olazapine are also used

47
Q

What are the side effects of Lithium?

A

Tremor: one of the most common side effects

Nausea, diarrhea, anorexia, bloating, ususally transient

Headache, memory impairement, mental confusion

Decreased thyroid function: lithium blocks thyroxine synthesis and release, decreases sensitivity to TSH, possibly causing receptor uncoupling

Edema, weight gain

Can be used during pregnancy

48
Q

What are the renal effects of Lithium?

A

Nephrogenic diabetes insipidus with polyuria and polydypsia, due to loss of ability of the collecting tubule to conserve water under the influence of ADH (Lithium blocks action of ADH)

Resistant to vassopressin, can be treated with amiloride (blocks entry of lithium into collecting duct)

Chronic insterstitial nephritis and nephrotic syndromes may also occur with long-term treatment, but renal failure does not generally result

49
Q

What is considered mild v. severe Lithium toxicity?

How do you treat Lithium overdose?

A

Mild=plasma levels >2.0mEq/L

Severe=plasma levels > 2.5mEq/L

Treat with dialysis and saline

50
Q

What two classes of drugs are generally safe to use in combination with Lithium?

A

Antipsychotics and Benzos

51
Q

What is the significant about the drug interaction between Lithium and antidepressants?

A

Can increase mania in some people

52
Q

What is the significant about the drug interaction between Lithium and Diuretics?

A

Drugs that alter sodium excretion will also affect Lithium, because Lithium and sodium compete for reabsorption.

Thiazide diuretics decrease clearance of Lithium (less lithium is getting excreted, because more sodium is getting excreted)

Amiloride, a K-sparing diuretic has been used to decrease polyuria and has little effect on lithium clearance.

53
Q

What is the significant about the drug interaction between Lithium and NSAIDs?

A

Decrease Lithium clearance and increase plasma concentration

54
Q

What is the significant about the drug interaction between Lithium and sodium?

A

Low sodium intake, sweating, exercise, hot weather–>decrease sodium and may therefore increase plasma lithium concentrations

55
Q

Name the 5 anticonvulsants used in the treatment of bipolar disorder.

A

Valproic acid

Carbamazepine

Lamotrigine

Topiramate

Gabapentin

56
Q

Valproic acid

A

Anticonvulsant that is widely used as a mood stabilizer.

Equal efficacy to Lithium.

Effective in some patients who do not respond to Lithium.

Rapid onset of action.

Few side effects-GI most common.

57
Q

Cabamazepine (Tegretol)

A

Anticonvulsant that can be used in patients who do not respond to lithium or in combination with lithium

Mechanism of action may be related to membrane stabilization

Not recommended during pregnancy and lactation

Stevens Johnson syndrome-worst case side effect

58
Q

What are the side effects of Carbamazepine?

A

GI

CNS toxicity (60%): drowsiness, dizziness, fatigue, clumsines, vertigo, ataxia

Hypersensitivity reactions, rashes

Idiosyncratic hematologic effects-watch for sore throat, fever, bruising

Stevens Johnson Syndrome: genetic testing for presence of HLA B1502 recommended for patients treated with carbamazepine

59
Q

What drugs may increase the toxicity of Carbamazepine when given concurrently?

A

cimetidine, erythromycin, isoniazid, verapamil, diltiazem, propoxyphene, and fluoxetine

these decrease metabolism of carbamazepine

60
Q

Lamotrigine

A

Anticonvulsant, as effective as lithium in tx of bipolar

Common side effects: nausea, ataxia, dizziness, double vision, sleepiness, headache, rash (SJS)

Does not cause weight gain

61
Q

Topiramate (Topamax)

A

Effective as monotherapy in some patients with bipolar

Used as anticonvulsant, tx for alcoholism, to offset weight gain from SSRIs, reduce binge-eating, prevention of migraine

Causes weight loss

62
Q

Gabapentin (Neurotonin)

A

Used as anticonvulsant and for neurologic pain

Not very effect long-term mood stabilizer

GABA analogue, may increase GABA release

Side effects: drowsiness and weight gain common, ataxia, blurred vision, hypertension, back pain

Not recommended in pregnancy

CNS Drugs (6 decks)

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