Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Which antipsychotics are least likely to cause tardive dyskinesia?

A

clozapine and olanzapine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Loxapine

A

Similar to phenothiazines

Used when other drugs have not worked

Lowers seizure threshold more than phenothiazines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Molindone

A

D2 blockade

Moderate sedation, increases motor activity, mild euphoria

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

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

A

Olanzapine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
What is Paliperidone?
The active metabolite of risperidone (atypical antipsychotic) Supplied as extended release product
26
What is significant about the pharmacokinetics of Risperidone?
Well absorbed orally Highly protein bound
27
What are the side effects of Risperidone?
Alpha antagonist: postural hypotension Agitation, anxiety, insomnia Headache, nausea, weight gain extrapyramidal at hihg doses lengthens QT interval Increased prolactin release may occur
28
Ziprasidone
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
What are the side effects of Ziprasidone?
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
Quetiapine
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
Asenapine
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
Aripiprazole (Abilify)
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
What are the side effects of Aripiprazole?
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
Iloperidone
Atypical antipsychotic Blockade of D2 and 5-HT2a alpha blockade, no muscarinic effect
35
Lurasidone
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
What two things decrease antipsychotic concentration by inducing liver enzymes and increasing metabolism?
Carbamazepine and Smoking
37
What if given with an antipsychotic will cause increased sedation? What will cause increased side effects such as dry mouth and urinary retention?
Sedative-hypnotics Anti-cholinergics
38
What are the first line drugs for Schizophrenia and why? When would you give Clozapine?
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
Which antipsychotics are most commonly used for Tourette's syndrome?
Haloperidol and Pimozide
40
What is the recommendations for the use of antipsychotics in Alzheimer's disease?
Risperidone has been used but increased mortality. Use of antipsychotics is not recommended in elderly patients, especially with dementia.
41
What antipsychotic is frequently used as an antiemetic?
Prochlorperazine
42
What antipsychotics can be used as adjunct drugs for treatement-resistant depression?
Quetiapine, olanzapine, aripiprazole
43
How is Lithium used when treatment is started for bipolar disorder?
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
How is lithium excreted? What is the optimal concentration range? When is a steady state reached?
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
What 3 mechanisms can increase lithium concentration?
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 2. Thiazide diuretics decrease the clearance of lithium 3. NSAIDs also decrease lithium clearance
46
What drugs are most commonly used to treat bipolar disorder?
**Lithium, Valproic acid, Carbamazepine** Lurasidone, Lamotrigine, and Olazapine are also used
47
What are the side effects of Lithium?
**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
What are the renal effects of Lithium?
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
What is considered mild v. severe Lithium toxicity? How do you treat Lithium overdose?
Mild=plasma levels \>2.0mEq/L Severe=plasma levels \> 2.5mEq/L Treat with dialysis and saline
50
What two classes of drugs are generally safe to use in combination with Lithium?
Antipsychotics and Benzos
51
What is the significant about the drug interaction between Lithium and antidepressants?
Can increase mania in some people
52
What is the significant about the drug interaction between Lithium and Diuretics?
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
What is the significant about the drug interaction between Lithium and NSAIDs?
Decrease Lithium clearance and increase plasma concentration
54
What is the significant about the drug interaction between Lithium and sodium?
Low sodium intake, sweating, exercise, hot weather--\>decrease sodium and may therefore increase plasma lithium concentrations
55
Name the 5 anticonvulsants used in the treatment of bipolar disorder.
Valproic acid Carbamazepine Lamotrigine Topiramate Gabapentin
56
Valproic acid
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
Cabamazepine (Tegretol)
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
What are the side effects of Carbamazepine?
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
What drugs may increase the toxicity of Carbamazepine when given concurrently?
cimetidine, erythromycin, isoniazid, verapamil, diltiazem, propoxyphene, and fluoxetine these decrease metabolism of carbamazepine
60
Lamotrigine
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
Topiramate (Topamax)
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
Gabapentin (Neurotonin)
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)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions