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Pharmacology > Anxiolytics, Hypnotics, Sedatives > Flashcards

Anxiolytics, Hypnotics, Sedatives Flashcards

1
Q

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

A

anxiety

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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 - the most frequently used drugs for anxiety
Azapirones - buspirone
Barbiturates - rarely used today because of severe side effects and a low therapeutic index. These drugs have generally been replaced by the benzodiazepines.

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4
Q

Give some examples of benzodiazepines and their approximate duration of action.

A

Short acting (2 - 8 hour) :

  1. Triazolam (Halcion)
  2. Oxazepam (Serax)
  3. Midazolam (Versed)
  4. Clonazepam (Klonopin)

Intermediate-Acting (10-20 hr):

  1. Temazepam (Restoril)
  2. Lorazepam (Ativan)
  3. Alprazolam (Xanax)

Long-Acting (1-3 days):

  1. Chlordiazepoxide (Librium)
  2. Diazepam (Valium)
  3. Flurazepam (Dalmane)
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5
Q

What is GABA?

A

GABA (gamma-aminobutyric acid) is the major inhibitory neurotransmitter of the CNS

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6
Q

How do benzodiazepines work?

A

When benzodiazepines bind to specific receptors that are separate 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, cel membrane hyper polarization, and decreased hyper polarization, and decreased initiation of action potentials.
Remember that benzodiazepines do not bind to GABA receptors - they bind adjacent to them.

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7
Q

What are the therapeutic indications for benzodiazepines?

A 
These drugs are used clinically as muscle relaxants and in the treatment of the following:
Anxiety disorders
Panic disorders
Status Elipepticus
Sleep disorders
Alcohol withdrawal
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8
Q

DOC of panic disorders

A

alprazolam

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9
Q

DOC of status epilepticus

A

diazepam

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10
Q

DOC of sleep disorders

A

flurazepam or temazepam

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11
Q

DOC alcohol withdrawal

A

diazepam is mot commonly used

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12
Q

Are benzodiazepines effective for controlling pain as well as anxiety?

A

No. they have little analgesic effect.

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13
Q

What is their route of administration?

A

PO, IV, or IM

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14
Q

Where are 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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15
Q

Does dependence occur?

A

Yes. Prolonged use can result in dependence. Abrupt discontinuation can result in withdrawal symptoms, including confusion, anxiety, and agitation.

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16
Q

What is flumazenil (Romazicon) mechanism of action?

A

Flumazenil is a copetitive antagonist of benzodiazepines at the GABAa receptor.

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17
Q

Describe the clinical use of flumazenil (Romazicon) drug.

A

Reversal of benzodiazepine sedation or overdose

18
Q

How is flumazenil (Romazicon) administered?

A

IV use only

19
Q

How long do the effects of flumazenil (Romazicon) last?

A

only 1 hour - repeat doses may be necessary for a heavily sedated patient to remain alert.

20
Q

How does Buspirone (BuSpar) work?

A

acts as a partial agonist at serotonin (5-HT1A) receptors

21
Q

What are the indications for Buspirone (BuSpar)

A

generalized anxiety; however unlike benzodiazepines, its effects may take 1-2 weeks to become apparent

22
Q

What are the pharmacokinetic properties of Buspirone (BuSpar)?

A

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

23
Q

How do the actions of buspirone (BuSpar) differ from those of the benzodiazepines?

A

Buspirone lacks the muscle relaxant and anticonvulsant properties of the benzodiazepines.

24
Q

What advantage does buspirone (BuSpar) have over benzodiazepines?

A

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

25
Q

What toxic effects are associated with Buspirone (BuSpar)?

A

Headache, nausea, dizziness

26
Q

Give 4 examples of barbiturates and their duration of action?

A
  1. Phenobarbital (Luminal) - long acting 1-2 days
  2. Pentobarbital (Nembutal) - short acting/ 2-8 hours.
  3. Amobarbital (Amytal) - short acting
  4. Thiopental (Pentothal) - ultra-short-acting/10-20 minutes.
27
Q

How do Barbiturates work?

A

like benzodiazepines, barbiturates increase the duration of GABA action on Cl-entry into the cell, which results in membrane hyper polarization and a decrease in neuron excitability. Barbiturates do not, however, bind to benzodiazepine receptors.

28
Q

What are the therapeutic indications for barbiturates administration?

A

Induction of anesthesia
Anticonvulsants
Anxiety

29
Q

Induction of anesthesia - which barbiturate?

A

thiopental

30
Q

Anticonvulsants - which barbiturate?

A

phenobarbital

31
Q

Anxiety - which barbiturate?

A

rarely used

32
Q

Why are benzodiazepines favored over barbiturates for the treatment of anxiety?

A

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

33
Q

By what routes can barbiturates be administered?

A

IV, PO, IM

34
Q

What are the pharmacokinetic properties of barbiturates?

A

They are metabolized in the liver and excreted in the urine.

35
Q

What determines the duration of action of thiopental?

A

Redistribution to the other tissues

36
Q

Does barbiturate dependency occur?

A

yes. abrupt cessation can lead to severe withdrawal symptoms (tremor, restlessness, nausea, seizures, and cardiac arrest)

37
Q

For whom are barbiturates contraindicated?

A

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

38
Q

What are the adverse effects of Barbiturate drugs?

A
  1. Drowsiness and decreased motor control
    induction of the P-450 system, which can therefore decrease the effect of other drugs metabolized by these enzymes
  2. addiction
  3. in high doses, respiratory depression and coma
  4. allergic reactions, especially in patients with asthma
39
Q

What is Zolpidem (Ambien) clinical use?

A

treatment of insomnia (sedative)

40
Q

What are the adverse effects of Zolpidem (ambien)?

A

Ataxia, nightmares, headache and confusion

41
Q

What are the clinical uses of Chloral Hydrate - sedation!!?

A

Hypnosis

Sedation (in children)

42
Q

Describe Chloroal Hydrate adverse effects

A

GI distress

Unpleasant taste

Pharmacology (6 decks)

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