Anti-Anxiety Drugs; Antipsychotic Drugs

Front 1

Chlordiazepoxide is what type of drug?

Back 1

A benzo (Librium)

Front 2

T/F There is a great deal of pharmacological difference among currently marketed benzos

Back 2

F!

Front 3

What are the active metabolites of diazepam?

Back 3

desmethyldiazepam and oxazepam

Front 4

What are the main differences in benzos due to?

Back 4

Their disposition/how fast they're metabolized

Front 5

desmethyldiazepam disappears (faster, more slowly) than the parent diazepam

Back 5

more slowly

Front 6

What are the active metabolites of chlordiazepoxide?

Back 6

desmethyldiazepam and desmethyldiazepoxide

Front 7

Why do oxazempam and lorazepam have shorter duraiton of action than other benzos?

Back 7

They are conjugated to form glucuronides, which are excreted directly.

Front 8

How are benzos differentiated from other CNS depressants?

Back 8

by slope of dose-effect curve.

They're active over a wide range of doses, with a very large dose required for death.

Front 9

T/F It is easier with benzos than other drugs to produce anti-anxiety but non-sedative effect

Back 9

T

Front 10

What is the cellular MOA of benzos?

Back 10

There are specific benzo receptors in central synapses. Binding affinity is correlated with potency.

They increase the affinity of the GABA-A receptor for its ligand GABA.

Front 11

Competitive antagonist acting at benzo receptors

Back 11

flumazenil

Front 12

drugs that bind tot he benzo receptor but produce opposite effects of benzos (anxiety, convulsions) are called _______

Back 12

inverse agonists

Front 13

What is the most common reason benzos are abused?

Back 13

Patients who desire to continue meds longer than their physician seems advisable to self-medicate anxiety or nervousness.

Front 14

Mild physical dependence symtpoms of benzos

Back 14

Anxiety, dysphoria, insomnia, loss of appetite

Front 15

Severe physical dependence symtpoms of benzos

Back 15

Usually only associated with long-term administration of high doses as commonly occurs in cases of abuse. Serious and may include convulsions

Front 16

What is meprobamate?

Back 16

anti-anxiety drug ranking between benzos and barbiturates in toxicity.

Higher incidence of drowsiness and ataxia.

Usage replaced by benzos

Front 17

Buspirone: MOA and use

Back 17

Modulation of serotonergic transmission; does NOT interact at benzo-GABA receptor complex, therefore little to no sedative side effects.

Front 18

Hydroxyzine: MOA and use

Back 18

antihistamine with sedative effects. Most often used for derm conditions with psych component. Has little to no abuse potential, but can result in drug interactions with other depressants. Typical anticholinergic effects.

Front 19

Propranolol: MOA and use

Back 19

beta-adrenergic blocker that attenuates the sympathetic nervous system arousal that accompanies fear and anxiety.

Front 20

first line treatment for panic

Back 20

SSRIs

Front 21

how many subgroups of phenothiazines?

Back 21

3

Front 22

neuroleptics are aka

Back 22

antipsychotics

Front 23

Reserpine: MOA and what's special

Back 23

nonspecific depletion of tissue stores of monoamines (especially catecholamines).

Front 24

4 main chemical classes of antipsychotics

Back 24

1) Phenothiazines

2) Thioxanthenes

3) Butyrophenones

4) Miscellaneous structures/atypicals

Front 25

What are the 3 structural subgroups of phenothiazines?

Back 25

Aliphatic - High dose
Piperidine - High dose
Piperazine - Low dose

Front 26

Aliphatic subgroup of phenothiazines: what drug

Back 26

chlorpromazine (Thorazine)

Front 27

Piperidine subgroup of phenothiazines: what drug

Back 27

thioridazine

Front 28

Piperazine subgroup of phenothiazines: what drug

Back 28

trifluoperazine

Front 29

The "typical" antipsychotics, except haloperidol, end in what?

Back 29

-azine

Front 30

ALl typical antipsychotics block ____ receptors

Back 30

D2

Front 31

What is the prototype of the butyrophenones?

Back 31

haloperidol

Front 32

What's special about the butyrophenones?

Back 32

no anticholinergic properdies and hence has a high incidence of extrapyramidal symptoms

Front 33

Clozapine is an (atypical, typical) antipsychotic

Back 33

atypical

Front 34

What side effect is clozapine associated with?

Back 34

unusually high incidence of agranulocytosis

Front 35

What is the good thing about clozapine compared to typical antipsychotics?

Back 35

Low incidece of neurological side effects (extrapyramidal and tardive dyskinesia)

Front 36

Extrapyramidal side effects in antipsychotics are due to what?

Back 36

blockade of DA receptors in the dopaminergic nigrostriatal tract

Front 37

There is an important balance between dopaminergic and __________ systems in regulation extrapyramidal motor system.

Back 37

cholinergic

Front 38

Extrapyramidal effects of antipsychotics are generally treated with which class of drug?

Back 38

Anticholinergics (benztropine)

Front 39

Incidence of extrapyramidal side effects is inversely proportional to what?

Back 39

the amount of anticholinergic activity of the drug

Front 40

Which classes of antipsychotics have the highest incidence of extrapyramidal side effects?

Back 40

Haloperidol (butyrophenones)

and

Piperazine phenothiazines

Front 41

Which classes of antipsychotics have the LOWEST incidence of extrapyramidal side effects?

Back 41

Aliphatic phenothiazines

Piperidine phenothiazines

Front 42

In general, the (highest, lowest) potency drugs have the highest neurologic side effects

Back 42

Highest

Front 43

What toxicity does chlorpromazine (aliphatic phenothiazine) have?

Back 43

Corneal deposits - Chlorpromazine

Front 44

What toxicity does thioridazine (piperidine phenothiazine) have?

Back 44

reTinal deposits - thioridazine

Front 45

main anticholinergic used to treat extrapyramidal effects of antipsychotics

Back 45

benztropine

Front 46

In what groups is tardive dyskinesia the biggest risk?

Back 46

More common in elderly and in females

Front 47

Clozapine: MOA

Back 47

5HT2 (strong) and D2-D4 receptor blockers (weak)

Front 48

What are the serotonin-dopamine antagonists (SDAs?)

Back 48

atypical antipsychotics

Front 49

Aripiprazole: MOA

Back 49

Instead of a DA receptor antagonist, appears to work as a D2 partial agonist.

Also acts at 5HT receptors

Front 50

Side effects of atypical antipsychotics

Back 50

Agranulocytosis (1-2 %) - clozapine
Weight gain
Hyperglycemia, type II diabetes (persons at risk, with weight gain), hyperlipidemia
Expensive, but may decrease total cost of treatment

Front 51

Clinical uses of antipsychotics

Back 51

Schizophrenia
Psychomotor stimulant overdoses
Nausea and vomiting
Intractable hiccough
Gilles de la Tourette syndrome
Acute mania and bipolar disorder

Front 52

What is used to counteract psychomotor stimulant (amphetamine, cocaine) OD?

Back 52

Chlorpromazine

Front 53

What is used to counteract hallucinogen with anticholinergic properties OD?

Back 53

physostigmine

Front 54

Used for control of intractable hiccough

Back 54

haloperidol

Front 55

What is neuroleptic malignant syndrome?

Back 55

very severe form of acute pseudoparkinsonism.

FEVER

Fever
Encephalopathy
Vitals unstable
Elevated enzymes
Rigidity of muscles

Front 56

What cardiovascular side effects are seen in antipsychotic drug use?

Back 56

Increased risk of acute cardiac death due to prolonged QT intervals

Front 57

n acute condition involving a severe and dangerous leukopenia (lowered white blood cell count), most commonly of neutrophils causing a neutropenia in the circulating blood.

Back 57

agranulocytosis

Front 58

What is the cause of the weight gain seen in patients treated with (especially atypical) antipsychotics?

Back 58

blockade of central histamine H1 receptors.

Associated with hyperglycemia, which can contribute to the development of diabetes and hyperlipidemia.