Anti-psychotics

Question 1

the clinical dose for controlling schizophrenia correlates with binding affinity for

Answer 1

D2 receptors

Question 2

Most antipsychotic drugs strongly block postsynaptic

Answer 2

D2 receptors

-Particularly in Mesolimbic-frontal system

Question 3

Drugs that increase dopaminergic activity aggravate

Answer 3

Schizophrenia

Question 4

Dopamine receptor density has been found to be increased in untreated

Answer 4

Schizophrenic patients

Question 5

Clinically useful antipsychotics block

Answer 5

Dopamine receptors

Question 6

Typical or Atypical antipsychotics are differentiated by the presence or absence of side effects observed with conventional, first-generation antipsychotics. What is characteristic of

1. ) Typical antipsychotics
2. ) Atypical antipsychotics

Answer 6

1. ) Substantial risk of EPS

2. ) Reduced risk of EPS

Question 7

Reduce positive, NOT negative symptoms

Answer 7

Typical antipsychotics

Question 8

Reduce positive AND negative symptoms

Answer 8

Atypical antipsychotics

Question 9

Correlate with hyperactivity of Mesolithic D2 receptors

Answer 9

Positive symptoms

Question 10

Correlate with hypoactivity of mesocortical neurons

Answer 10

Negative symptoms

Question 11

Relative blockade of the 5-HT2 receptors may contribute to reduction in

Answer 11

Negative e symptoms

Question 12

What are the typical antipsychotics

Answer 12

Haloperidol and the -azines

Question 13

The atypical antipsychotics are the

Answer 13

-apine’s and idone’s

Question 14

What are three reversible neurological effects (EPS) of antipsychotics?

Answer 14

Parkinson’s-like syndrome, akathisia, and dystonias

Question 15

Occur most frequently with haloperidol and more potent piperazine side-chain phenothiazines

Answer 15

Reversible neurological effects: EPS

Question 16

Antipsychotic toxicity is reversed by decreasing dose and administration of

Answer 16

Antimuscarinic agent

Question 17

Acute dystonic reactions are usually very painful and should be treated immediately. They respond well to treatment with

Answer 17

Diphenhydramine or muscarinic blockers

Question 18

Choreoathetoid movements of the muscles of the lips and buccal cavity

-May be reversible

Answer 18

Tardive dyskinesia

Question 19

To treat tardive dyskinesia, we want to

1. ) Discontinue
2. ) Eliminate
3. ) Add

Answer 19

1. ) Antipsychotic
2. ) All drugs w/ central anticholinergic action
3. ) Diazepam

Question 20

Characterized by muscle rigidity, excessive sweating, hyper Pyrex is, and autonomic instability, which may be life threatening

Answer 20

Neuroleptic malignant syndrome

Question 21

The most severe adverse effect of typical agents

-Fatal in ~10% of cases

Answer 21

Neuroleptic malignant syndrome

Question 22

Treatment for neuroleptic malignant syndrome involves prompt use of

-Can also use dopamine agonists (bromocriptine)

Answer 22

Dantroline

Question 23

A muscle relaxant that acts at the ryanodine receptor to restore calcium levels in muscle cells

Answer 23

Dantrolene

Question 24

Causes hyperprolactinemia, gynecomastia, amenorrhea-galactorrhea syndrome, and infertility

Answer 24

D2 receptor blockade in pituitary

Question 25

There is significant weight gain and hyperglycemia reported for several atypical antipsychotics. But this is less with

Answer 25

Aripiprazole and ziprasidone

Question 26

Some patients on antipsychotics may get hyperlipidemia and may develop

Answer 26

Diabetes Mellitus

Question 27

Major effect that correlates with therapeutic benefit for older (typical) agents

Answer 27

Dopamine Receptor Blockade

Question 28

Parkinson-like syndrome with Brady kinetic, rigidity, and tremor occurs most frequently with

Answer 28

Haloperidol

Question 29

The autonomic effects of antipsychotics are due to the blockade of peripheral

Answer 29

Alpha-adrenergic and/or muscarinic receptors

Question 30

Which antipsychotic has the

1. ) Strongest autonomic effect?
2. ) Weakest?

Answer 30

1. ) Thioridazine

2. ) Haloperidol

Question 31

Alpha-adrenergic receptor blockade also results in

Answer 31

Postural hypotension and failure to ejaculate

Question 32

Atropine-like effects are pronounced with the use of

-Antimuscarinic effects

Answer 32

Thioridazine and aliphatic phenothiazines

Question 33

The antimuscarinic CNS effects of antipsychotics may include a toxic confusional state similar to that produced by

Answer 33

Atropine

Question 34

Have higher 5-HT2 relative to D2 blockade activity as compared to typical agents

Answer 34

Atypical Anti-psychotics

Question 35

Parkinson-like syndrome occurs infrequently with

-Much less common in newer drugs

Answer 35

Clozapine

Question 36

Have intermediate autonomic effects

Answer 36

Atypical

Question 37

Provides a limited D2 block, with a higher affinity for D4 and 5-HT2A

Answer 37

Clozapine

Question 38

Has a unique toxicity: risk for agranulocytosis

Answer 38

Clozapine

Question 39

An effective atypical, but is reserved for treatment-resistant schizophrenia

Answer 39

Clozapine

Question 40

At high dose, inhibits DA response completely

Answer 40

Haloperidol

Question 41

Competitively inhibits DA response until its Emax is reached

Answer 41

Aripiprazole

Question 42

Absorbed readily, though incompletely absorbed when given orally

Answer 42

Anti-psychotics

Question 43

Antipsychotics have a high first-pass transformation, thus bioavailability is

Answer 43

25-35% (65% for haloperidol)

Question 44

Metabolized by oxidative processes (P450s) and by glucuronidation, sulfation, and other conjugation processes

Answer 44

Antipsychotics

Question 45

A metabolite of thioridazine, which is more active than the parent compound

Answer 45

Mesoridazine

Question 46

Biological effects of anti-psychotics usually persist for at least

Answer 46

24 hours