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Pharma Recall - Pharmacology > Ch 11 - Anxiolytics, Hypnolytics, and Sedatives - DONE > Flashcards

Ch 11 - Anxiolytics, Hypnolytics, and Sedatives - DONE Flashcards

1
Q

Define anxiety:

A

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

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2
Q

What are some of the physical symptoms seen with anxiety?

A
  • Tachycardia
  • Tachypnea
  • Sweating
  • Trembling
  • Weakness
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3
Q

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

A
  • Benzodiazepines
  • Azapirones
  • Barbiturates
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4
Q

What si the most frequently used drugs to treat anxiety?

A

Benzodiazepines

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5
Q

Azapirones -

A

buspirone

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6
Q

Barbiturates:

A
  • Rarely used today becaue of severe side effects and a low therapeutic index.
  • These drugs have generally been replaced by Benzodiazepines
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7
Q

Give examples of short-acting Benzodiazepines:

Time?

A

2 to 8 hr

  • Triazolam
  • Oxazepam
  • Midazolam
  • Clonazepam
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8
Q

Give examples of intermediate-acting Benzodiazepines:

Time?

A

10 to 20hr

  • Temazepam
  • Lorazepam
  • Alprazolam
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9
Q

Give examples of long-acting Benzodiazepines:

Time?

A

1 to 3 days

  • Chlordiazepoxide
  • Diazepam
  • Flurazepam
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10
Q

What is GABA?

A

is the major inhibitory neurotransmitter of the CNS

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11
Q

How do Benzodiazepines work?

A

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

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12
Q

What are the therapeutic indications for Benzodiazepines?

A
  • 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
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13
Q

Drugs for Panic disorders:

A

alprazolam

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14
Q

Drugs for Status epilepticus:

A

diazepam

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15
Q

Drugs for Sleep disorders:

A

flurazepam or temazepam

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16
Q

Drugs for Alcohol withdrawal:

A

diazepam is the most commonly used

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17
Q

Are Benzodiazepines effective fro controlling pain as well as anxiety?

A

No, they have little analgesic effect

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18
Q

What is the route of administration for Benzodiazepines?

A
  • PO
  • IV
  • IM
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19
Q

Where are the Benzodiazepines metabolized?

A
  • They are metabolized in the liver and excreted in the urine.
  • Many of the Benzodiazepines have active metabolites
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20
Q

Does dose dependence occure?

Benzodiazepines

A

Yes. Prolonged use can result in dependence.

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

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21
Q

Benzodiazepines AE:

A
  • Drowsiness and confusion (the most common side effect)
  • Ataxia
  • Dizziness
  • Respiratory depression and death if taken with other CNS depressants such as ethanol
22
Q

Benzodiazepines antagonists:

A

Flumazenil

23
Q

What is Flumazenil´s mechanism of action?

A

Flumazenil is a competitive antagonist of Benzodiazepines at the GABAa receptor

24
Q

Describe the clinical use of Flumazenil:

A

Reversal of Benzodiazepine sedation or overdose

25
Q

What is the route of administration of Flumazenil?

A

IV use only

26
Q

How long does the effect of Flumazenil last?

A

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

27
Q

Azapirones:

A

Buspirone

28
Q

How does Buspirone work?

A

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

29
Q

What are the indications for Buspirone?

A

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

30
Q

What are the pharmacokinetic properties of Buspirone?

A

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

31
Q

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

A

Buspirone lacks the muscle relaxant and anticonvulsant properties of the Benzodiazepines

32
Q

What advantages does Buspirone have over Benzodiazepines?

A
  • minimal sedation
  • low abuse potential
  • no overdose fatalities reported
  • no withdrawal symptoms
33
Q

What toxic effects are associated with Buspirone?

A
  • headache
  • nausea
  • dizziness
34
Q

Barbiturates examples:

A
  • Phenobarbital
  • Pentobarbital
  • Amobarbital
  • Thiopental
35
Q

Phenobarbital duration:

A

long-acting/1-2days

36
Q

Amobarbital duration:

A

short-acting

37
Q

Thiopental duration:

A

ultra-short-acting/10-20min

38
Q

Pentobarbital duration:

A

short-acting/2-8hours

39
Q

How does the Barbiturates work?

A
  • 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
40
Q

What are the therapeutic indications for Barbiturates administration?

A
  • induction of anesthesia
  • anticonvultants
  • anxiety (rarely)
41
Q

Which Barbiturates is used for anticonvultants?

A

Phenobarbitals

42
Q

Which Barbiturates is used for induction of anesthesia?

A

thiopental

43
Q

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

A

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

44
Q

What are the pharmacokinetic properties of Barbiturates?

A

Barbiturates are metabolized in the liver and excreted in the urine

45
Q

What determines the duration action of Thiopental?

A

redistribution to other tissues

46
Q

Does Barbiturate dependency occur?

A

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

47
Q

For whom are Barbiturate CI?

A

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

48
Q

Barbiturate AE:

A
  • 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
49
Q

What is the clinical use of Zolpidem?

A

treatment of insomnia

50
Q

Zolpidem AE:

A
  • ataxia
  • nightmares
  • headache
  • confusion
51
Q

What are the clinical uses of Chloral hydrate?

A
  • Hypnosis

- Sedation (in children)

52
Q

Chloral hydrate AE:

A
  • GI distress

- Unpleasant taste

Pharma Recall - Pharmacology (14 decks)

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