Cns Pharmacology: Antipsychotic Drugs

Front 1

List the positive symptoms of schizophrenia.

List the negative symptoms of schizophrenia.

Back 1

Positive: hallucinations, delusions, word salad

Negative: poverty of speech, flat affect, anhedonia, apathy

Front 2

Typical antipsychotic drugs are effective at treating (negative or positive) schizophrenic symptoms.

Name the serious side effect associated with typical antipsychotic drugs.

Back 2

Typical antipsychotic drugs are effective at treating positive schizophrenic symptoms.

Typical antipsychotic drugs have extrapyramidal side effects.

Front 3

Compare mechanisms of "typical" and "atypical" antipsychotic drugs.

Back 3

Typical: D2 receptor antagonists

Atypical: lower affinity for D2 receptors & have action on many 5-HT receptor types

Front 4

While atypical antipsychotic drugs are more widely used compared to the "typical" variety, they can induce serious (blank).

Back 4

Atypical antipsychotics can induce serious weight gain and 2ndary diabetes in 30% of patients.

Front 5

Chlorpromazine is a:

a) alpha agonist
b) muscarinic agonist
c) antihistamine

Back 5

Chlorpromazine is a antihistamine and has sedative properties.

Front 6

Rank the following phenothiazines from less potent to more potent:

thioridazine
fluphenazine
chlorpromazine

Which drug has a high incidence of extrapyramidal side effects but lower incidence of anticholinergic & antiadrenergic side effects?

Back 6

Less potent: chlorpromazine

Potent: thioridazine

More potent: fluphenazine = has higher incidence of extrapyramidal SE's & lower incidence of anti-cholinergic & anti-adrenergic SE's compared to less potent chlorpromazine

Front 7

The phenothiazines have different potencies and side effects. What pharmacodynamic property do they have in common?

Back 7

Phenothiazines have roughly the same therapeutic efficacy.

Front 8

List the CNS pharmacological actions of chlorpromazine.

Back 8

(1) sedation
(2) prevents nausea and vomiting
(3) lowers body temperature
(4) causes prolactin release
(5) facilitates seizures by decreasing seizure threshold

Front 9

List the ANS pharmacological actions of chlorpromazine.

Back 9

(1) Muscarinic block: blurred vision, constipation, dry mouth

(2) alpha block: postural hypotension

Front 10

Besides treating schizophrenia and severe mania, chlorpromazine is also used to treat these 2 things:

Back 10

(1) dementia related agitation (Alzheimer's)

(2) prevents nausea and vomiting which may be caused by other drugs

Front 11

What is the mechanism of action for phenothiazine treatment of schizoprenia?

Back 11

Phenothiazines inhibit DA transmission in CNS by blocking postsynaptic receptors.

Front 12

List the 5 extrapyramidal reactions that can occur in a patient taking phenothiazines.

Back 12

(1) Parkinsonian syndrome
(2) akathisia
(3) neuroleptic malignant syndrome
(4) dystonias
(5) tardive dyskinesia

Front 13

Phenothiazines can potentiate these 3 classes of drugs

Back 13

(1) anticholinergics

(2) CNS depressants (sedatives, anesthetics, opiods)

(3) adrenergic antihypertensives

Front 14

Tardive dyskinesia reaction to phenothiazines

-time frame for development
-symptoms
-how to treat it

Back 14

Time frame: develops months - years after starting therapy

Symptoms: abnormal face movements, choreoathetosis

Treatment: avoid the onset altogether with low dose b/c drug withdrawal makes the problem worse

Front 15

Neuroleptic malignant syndrome reaction to phenothiazines

-time frame for development
-symptoms
-how to treat it

Back 15

Time frame: as soon as 30 minutes

Symptoms: muscle rigidity + hyperthermia

Treatment: dantrolene & bromocriptine; supportive treatment

Front 16

This drug is distinct from phenothiazines but it resembles fluphenazine (high potency). This drug can cause extrapyramidal effects.

Back 16

haloperidol

Front 17

Regarding their mechanism of action, why do atypical antipsychotics have a lower propensity to cause extrapyramidal effects?

Back 17

Atypicals (compared to typical antipsychotics) have a greater occupancy at 5-HT receptors relative to DA receptors.

In addition, the atypicals may block DA receptors on mesolimbic neurons rather than nigrostriatal neurons, which may also be an explanation.

Front 18

Clozapine was withdrawn in 1975 after this side effect developed..

Back 18

agranulocytosis

(this was found to be reversible, so clozapine was re-introduced)

Front 19

This drug is similar to clozapine but without the wbc problems. It also blocks ACh, which may explain its lack of extrapyramidal effects. Unlike clozapine, this drug has a higher affinity for D2 receptors compared to 5-HT2 receptors.

Back 19

olanzipine (atypical)

Front 20

This drug is recommended in the treatment of patients expriencing their first schizophrenia episode. It is contraindicated in those who are at risk of ASCVD because it may increase Q-T interval.

Back 20

respiridone (atypical)

Front 21

This drug treats positive and negative symptoms of schizophrenia without extrapyramidal effects. It is a potent 5-HT receptor antagonist with some DA antagonism - just like clozapine - but without the wbc side effects.

Back 21

quetiapine (atypical)

Front 22

This atypical antipschotic is less likely to be associated with weight gain and may cause an increase in the Q-T interval. It is a 2nd line drug.

Back 22

ziprasidone (atypical)

Front 23

This atypical antipsychotic has D2 and 5-HT1 receptor agonist activity, as well as 5-HT2 antagonist activity.

Back 23

aripiprazole (atypical)

Front 24

Describe both the dopamine and glutamine explanations of schizophrenia.

Back 24

Dopamine: is has been shown that there is increased DA receptor density in schizoprenic patients; drugs that increase DA can aggravate psychotic signs/symptoms

Glutamine: "hypofuncitonal NMDA receptor" hypothesis is complementary to the dopamine hypothesis; glycine --which enhances glutamine activity-- improves schizophrenic symptoms

Front 25

What is the evidence in favor of the claim that decreased NMDA receptors is contributory to the symptoms of schizophrenia?

Back 25

(1) pharm: ketamine is a NMDA blocker and can induce both positive & negative symptoms

(2) SNPs are found in brains of schizophrenics -- these reduce binding of glutamate to the receptor

Front 26

Large doses of this amino acid -- when given with clozapine -- can improve negative symptoms.

Back 26

large doses of glycine

Front 27

List the indications of antipsychotic drugs.

Back 27

--schizophrenia
--bipolar disease w/ psychosis
--Tourett's
--disturbed behavior in dementia
--antiemetic (prochlorperazine)
--preop (promethazine)

Front 28

For each of the following buzzword/adverse effect/property/etc, name the anti-psychotic that it describes..

1) anti-emetic and treatment for Alzheimer's agitation
2) causes extrapyramidal effects
3) increases Q-T interval
4) agranulocytosis
5) resembles fluphenazine
6) treats first schizo episode showing many negative symptoms
7) treatment for bipolar mania
8) atypical anti-psychotic that blocks ACh
9) partial DA agonist and 5-HT antagonist
10) typical anti-psychotic that is less likely to cause EP effects and more lkely to to cause anti-cholinergic effects

Back 28

1) anti-emetic and treatment for Alzheimer's agitation = phenothiazines

2) causes extrapyramidal effects = phenothiazines

3) increases Q-T interval = respiridone and ziprasidone

4) agranulocytosis = clozapine

5) resembles fluphenazine = haloperidol

6) treats first schizo episode showing many negative symptoms = respiridone

7) treatment for bipolar mania = quetiapine

8) atypical anti-psychotic that blocks ACh = olanzipine

9) partial DA agonist and 5-HT antagonist = aripiprazole

10) typical anti-psychotic that is less likely to cause EP effects and more likely to to cause anti-cholinergic effects = chlorpromazine

Front 29

Aripiprazole activates D2 receptors when the dopaminergic tone is (low/high). It also inhibits the D2 receptors, but this occurs with when dopaminergic tone is (low/high).

Back 29

Aripiprazole activates D2 receptors when the dopaminergic tone is LOW.

It also inhibits the D2 receptors, but this occurs with when dopaminergic tone is HIGH.