Ch 11 - Anxiolytics, Hypnolytics, and Sedatives - DONE

Question 1

Define anxiety:

Answer 1

An unpleasant emotional state consisting of apprehension, tension, and feelings of danger without a real or logic cause

Question 2

What are some of the physical symptoms seen with anxiety?

Answer 2

• Tachycardia
• Tachypnea
• Sweating
• Trembling
• Weakness

Question 3

What are the major classes of drugs used to treat anxiety?

Answer 3

• Benzodiazepines
• Azapirones
• Barbiturates

Question 4

What si the most frequently used drugs to treat anxiety?

Answer 4

Benzodiazepines

Question 5

Azapirones -

Answer 5

buspirone

Question 6

Barbiturates:

Answer 6

• Rarely used today becaue of severe side effects and a low therapeutic index.
• These drugs have generally been replaced by Benzodiazepines

Question 7

Give examples of short-acting Benzodiazepines:

Time?

Answer 7

2 to 8 hr

• Triazolam
• Oxazepam
• Midazolam
• Clonazepam

Question 8

Give examples of intermediate-acting Benzodiazepines:

Time?

Answer 8

10 to 20hr

• Temazepam
• Lorazepam
• Alprazolam

Question 9

Give examples of long-acting Benzodiazepines:

Time?

Answer 9

1 to 3 days

• Chlordiazepoxide
• Diazepam
• Flurazepam

Question 10

What is GABA?

Answer 10

is the major inhibitory neurotransmitter of the CNS

Question 11

How do Benzodiazepines work?

Answer 11

When Benzodiazepines bind to specific receptors that are separated from but adjacent to the GABAa receptor, they potentiate the binding of GABA to its own receptor.

The binding of GABA to its own receptor results in increased chloride ion conductance, CM hyperpolarization, and decreased initiation of action potentials.

Remember that Benzodiazepines do not bind to GABA receptors: they bind adjacent to them

Question 12

What are the therapeutic indications for Benzodiazepines?

Answer 12

• these drugs are used clinically as muscle relaxants
• and in the treatment of the following (PASSA):
  
  • Panic disorders
  • Anxiety disorders
  • Status epilepticus
  • Sleep disorders
  • Alcohol withdrawal

Question 13

Drugs for Panic disorders:

Answer 13

alprazolam

Question 14

Drugs for Status epilepticus:

Answer 14

diazepam

Question 15

Drugs for Sleep disorders:

Answer 15

flurazepam or temazepam

Question 16

Drugs for Alcohol withdrawal:

Answer 16

diazepam is the most commonly used

Question 17

Are Benzodiazepines effective fro controlling pain as well as anxiety?

Answer 17

No, they have little analgesic effect

Question 18

What is the route of administration for Benzodiazepines?

Answer 18

• PO
• IV
• IM

Question 19

Where are the Benzodiazepines metabolized?

Answer 19

• They are metabolized in the liver and excreted in the urine.
• Many of the Benzodiazepines have active metabolites

Question 20

Does dose dependence occure?

Benzodiazepines

Answer 20

Yes. Prolonged use can result in dependence.

Abrupt discontinuation can result in withdrawal symptoms, including confusion, anxiety, and agitation

Question 21

Benzodiazepines AE:

Answer 21

• Drowsiness and confusion (the most common side effect)
• Ataxia
• Dizziness
• Respiratory depression and death if taken with other CNS depressants such as ethanol

Question 22

Benzodiazepines antagonists:

Answer 22

Flumazenil

Question 23

What is Flumazenil´s mechanism of action?

Answer 23

Flumazenil is a competitive antagonist of Benzodiazepines at the GABAa receptor

Question 24

Describe the clinical use of Flumazenil:

Answer 24

Reversal of Benzodiazepine sedation or overdose

Question 25

What is the route of administration of Flumazenil?

Answer 25

IV use only

Question 26

How long does the effect of Flumazenil last?

Answer 26

Only 1 hour: Repeat doses may be necessary for heavily sedated patients to remain alert

Question 27

Azapirones:

Answer 27

Buspirone

Question 28

How does Buspirone work?

Answer 28

It acts as a partial agonist at serotonin (5-HT_1A) receptors

Question 29

What are the indications for Buspirone?

Answer 29

Buspirone is used for generalized anxiety; however unlike benzodiazepines, its effect may take 1-2 weeks to become apparent.

Question 30

What are the pharmacokinetic properties of Buspirone?

Answer 30

This drug is metabolized by the liver and excreted in the urine; its half-life is 2-11hr

Question 31

How doe the action of Buspirone differ from those of bezodiazepines?

Answer 31

Buspirone lacks the muscle relaxant and anticonvulsant properties of the Benzodiazepines

Question 32

What advantages does Buspirone have over Benzodiazepines?

Answer 32

- minimal sedation - low abuse potential - no overdose fatalities reported - no withdrawal symptoms

Question 33

What toxic effects are associated with Buspirone?

Answer 33

- headache - nausea - dizziness

Question 34

Barbiturates examples:

Answer 34

- Phenobarbital - Pentobarbital - Amobarbital - Thiopental

Question 35

Phenobarbital duration:

Answer 35

long-acting/1-2days

Question 36

Amobarbital duration:

Answer 36

short-acting

Question 37

Thiopental duration:

Answer 37

ultra-short-acting/10-20min

Question 38

Pentobarbital duration:

Answer 38

short-acting/2-8hours

Question 39

How does the Barbiturates work?

Answer 39

- Like benzidiazepines, Barbiturates increase the duration of GABA action on Cl-entry into the cell, which results in membrane hyperpolarization and a decrease in neuron excitability. - Barbiturates do not, however, bind to Benzodiazepines receptors

Question 40

What are the therapeutic indications for Barbiturates administration?

Answer 40

- induction of anesthesia - anticonvultants - anxiety (rarely)

Question 41

Which Barbiturates is used for anticonvultants?

Answer 41

Phenobarbitals

Question 42

Which Barbiturates is used for induction of anesthesia?

Answer 42

thiopental

Question 43

Why are Benzodiazepines favored over Barbiturates for the treatment of anxiety?

Answer 43

Benzodiazepines have much higher therapeutic index, cause less physiological dependence,a dn do not induce hepatic enzymes.

Question 44

What are the pharmacokinetic properties of Barbiturates?

Answer 44

Barbiturates are metabolized in the liver and excreted in the urine

Question 45

What determines the duration action of Thiopental?

Answer 45

redistribution to other tissues

Question 46

Does Barbiturate dependency occur?

Answer 46

Yes. Abrupt cessation can lead to severe withdrawal symptoms (tremors, restlessness, nausea, seizures, and cardiac arrest).

Question 47

For whom are Barbiturate CI?

Answer 47

For patients who have acute intermittent porphyria, because they increase porphyrin synthesis.

Question 48

Barbiturate AE:

Answer 48

- Drowsiness and decreased motor control - Induction of the P-450 system, which can decrease the effect of other drugs metabolized by these enzymes - Addiction - In high doses, respiratory depression and coma - Allergic reactions, especially in patients with asthma

Question 49

What is the clinical use of Zolpidem?

Answer 49

treatment of insomnia

Question 50

Zolpidem AE:

Answer 50

- ataxia - nightmares - headache - confusion

Question 51

What are the clinical uses of Chloral hydrate?

Answer 51

- Hypnosis | - Sedation (in children)

Question 52

Chloral hydrate AE:

Answer 52

- GI distress | - Unpleasant taste