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Lec. 2: Sedative-Hypnotic Drugs Flashcards

1
Q

What are the three main categories of sedative hypnotic drugs?

A
  1. Benzodiazepines
  2. Barbiturates
  3. Miscellaneous Drugs
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2
Q

What drug further depresses the CNS as dose is increased? (Lethal and therapeutic range are close together)

A

Barbiturates

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3
Q

What drug has a greater range between therapeutic and lethal doses?

A

Benzodiazepines

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4
Q

What is a sedative?

A

A drug that reduces anxiety (anxiolytic) and produces a sense of calm in an individual.

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5
Q

What is a hypnotic?

A

A drug that induces drowsiness and promotes sleep.

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6
Q

Name five general uses of sedative-hypnotic drugs.

A
  1. Anxiolytic (anxiety)
  2. Anticonvulsant
  3. Sedative Hynotics
  4. Central Muscle Relaxant
  5. Potentiation of CNS Depression
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7
Q

What sedative-hypnotic drug is used to treat anxiety?

A

Benzodiazepines

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8
Q

What sedative-hynotic drug is used to treat epilepsy?

A

Barbiturates and Benzodiazepines

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9
Q

What sedative-hypnotic drug is used to treat alcohol detoxification?

A

Benzodiazepines

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10
Q

What sedative-hypnotic drug is used to treat insomnia?

A

Benzodiazepines and non-benzodiazepines

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11
Q

What sedative-hypnotic drug is used to treat spasticity (central muscle relaxant)?

A

Benzodiazepines

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12
Q

What sedative-hypnotic drug is used as an anesthetic (potentiation of CNS depression)?

A

Barbiturates and benzodiazepines

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13
Q

What determines how onset and duration of action of a drug?

A

Lipid solubility

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14
Q

Describe the hangover effect of highly lipid soluble drugs.

A

Drug hangs around in the body and will re-enter the CNS

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15
Q

Name two barbiturates that have a long (8-12 hrs) duration of action.

A
  1. Phenobarbital

2. Mephobarbital

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16
Q

Name the barbiturate that has a ultra-short (15-20 min) duration of action.

A

Thiopental

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17
Q

What is the clinical use of Thiopental?

A

Anesthesia

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18
Q

What is the clinical use of Phenobarbital?

A

Hypnotic and Anticonvulsant

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19
Q

What is the clinical use of Mephobarbital?

A

Anticonvulsant

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20
Q

Name three barbiturates that have an intermediate (2-4 hrs) duration of action.

A
  1. Pentobarbital
  2. Secobarbital
  3. Amobarbital
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21
Q

Barbiturates bind to ? receptors and increase or decrease the duration of opening of ? ion channels, thus leading to ?-polarization of the neuron.

A
  1. GABA
  2. Increase
  3. Cl-
  4. Hyper-polarization
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22
Q

Where are barbiturates metabolized and where are they excreted?

A

Metabolized in the liver and excreted by the kidneys.

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23
Q

What are the effects of barbiturates on the CNS?

A

Cause CNS depression from sedation to coma and death.

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24
Q

What are the effects of barbiturates on the respiratory system?

A

Causes inhibition of ganglionic transmission, decrease in BP, and decreased sympathetic tone

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25
Q

What are the effects of barbiturates on the GI tract?

A

Decreased tone and contractions of GI and urinary smooth muscle.

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26
Q

***What are the effects of barbiturates on the liver?

A

Causes induction of cytochrome P-450 enzymes in the liver.

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27
Q

What are six major problems with barbiturates?

A
  1. Narrow therapeutic index
  2. Lethal in overdose
  3. Rapid development of tolerance that may lead to physical dependence (addiction)
  4. Cross placental barrier
  5. Exacerbate Porphyrin synthesis
  6. Drug interactions result from cytochrome P-450.
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28
Q

Barbiturates cause induction of cytochrome P-450. Why can this be a problem when taking other drugs?

A

This can lower the therapeutic effectiveness of many drugs.

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29
Q

Name six drug interactions that are created from the induction of cytochrome P-450 enzymes from barbiturates.

A
  1. TCA’s
  2. Anticoagulants
  3. Quinidine
  4. Digoxin
  5. Estrogen
  6. Antibiotics
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30
Q

Name the three components of the benzodiazepines structure.

A
  1. Benzene ring
  2. Benzene ring
  3. 7-membered ring (diazepine)
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31
Q

What three electronegative substitutions can be made on Benzodiazepine to increase anxiolytic activity?

A

Cl > Br > NO2

32
Q

Name two short acting (2.5 hr) BZDs.

A
  1. Midazolam

2. Triazolam

33
Q

Name the six intermediate acting (12-15 hrs) BZDs.

A
  1. Alprozolam
  2. Halazepam
  3. Lorazepam
  4. Oxazepam
  5. Temazepan
  6. Estazolam
34
Q

Name the five long acting (20-60 hrs) BZDs.

A
  1. Chlordiazepoxide
  2. Chlonazepam
  3. Diazepam
  4. Flurazepam
  5. Chlorazepate
35
Q

What is the name of the BZD antagonist?

A

Flumazenil

36
Q

What is the only BZD that transforms directly to a 3-Hydroxy derivative and is it short, intermediate, or long acting?

A
  1. Estazolam

2. Intermediate Acting

37
Q

How many biotransformations do short acting BZDs AND Alprazolam undergo and what derivative do they become?

A
  1. One

2. Alpha-Hydroxy derivative

38
Q

What is the final form that BZDs take before being excreted and where are they excreted?

A
  1. Glucuronide Conjugates

2. Kidney

39
Q

What is the only BZD that transforms directly to a 3-hydroxy derivative and is it long, intermediate, or short acting?

A
  1. Estazolam

2. Intermediate acting

40
Q

How many transformations does Quazepam undergo and is it a long, intermediate, or short acting drug?

A
  1. Two

2. Intermediate

41
Q

What two BZD have the most biotransformations (longest half-life) and how many do they have?

A
  1. Chlordiazepoxide and Flurazepam
  2. Chlordiazepoxide: 4
    Flurazepam: 3
42
Q

What is the name of the intermediate acting BZD that acts as a 3-hydroxy compound and that most long acting BZDs will transform into?

43
Q

What is the name of the two intermediate acting BZD that transform directly into glucuronide conjugates?

A
  1. Lorazepam

2. Temazepam

44
Q

BZD bind to the ? receptor and cause the increase of ? ion channel opening.

A
  1. GABA(A)

2. Cl- ion

45
Q

T or F. Ethanol can also bind to GABA(A) receptors and can therefore summate with BZDs.

46
Q

What receptor do barbiturates and BZDs act on?

47
Q

BZD bind to GABA(A) and change the ? the channel opens, but barbiturates bind to GABA(A) and change the ? the channel opens.

A
  1. Frequency

2. Amount of time

48
Q

BZD binding to GABA(A) cause the opening of ? channels and influx of ? ions, which leads to the ?-polarization of the neuron.

A
  1. Cl-
  2. Cl-
  3. Hyper-polarization
49
Q

What is the action of Midazolam?

A

It is a full BZD agonist

50
Q

T or F. Midazolam can be used for conscious sedation and as a pre-medication for dental or minor surgery?

51
Q

Diazepam is a long acting BZD and midazolam is short acting. Which drug is more water soluble and has a faster onset and shorter duration of action?

52
Q

What drug can be used to block the effects of Buspirone?

A

Flumazenil

53
Q

Buspirone does not act directly with the GABAergic system, but is a partial agonist with ? receptors.

54
Q

Where does Flumazenil perform its action?

A

At the BZD binding site on the GABA receptor

55
Q

What is the clinical use to Flumazenil?

A

Reversal of BZD induced sedation

56
Q

Flumazenil can only be administered via ? and has a very ? duration of action.

A
  1. IV

2. Short

57
Q

BZD with inducers of cytochrome P-450 cause what?

A

Increased rate of metabolism, which reduces bioavailability of BZDs.

58
Q

BZD with inhibitors of cytochrome P-450 cause what?

A

Decreased rate of metabolism, which increases the bioavailability of BZD and prolongs their effects.

59
Q

T or F. If BZD can be withdrawn quickly.

A

False. They should be withdrawn gradually; there is a real risk of eliciting withdrawal or abstinence syndrome.

60
Q

What type of dependence is likely to develop after prolonged used of BZD?

A

Physical dependence

61
Q

What are BZD used for in dentistry?

A

Pre-operative sedation and balanced anesthesia

62
Q

What type of drug could be used to treat general anxiety disorder?

63
Q

BZDs and most hypnotics suppress what stages of sleep?

A

Stages 3, 4, and 5

64
Q

What drug can be used to restore the sleep pattern to normal and induces sleep when the patient is awake?

65
Q

What is the effect of BZD on stages 1 and 2?

A

Increases length of stages

66
Q

What is the effect of BZD on stages 3, 4, and 5?

A

Decreases length of stages

67
Q

Do short acting BZD increase or decrease latency of sleep onset?

68
Q

Which BZD have the highest abuse potential with alcohol?

A

Long acting BZD hypnotics

69
Q

In what stage is there rapid eye movement?

70
Q

T or F. The REM sleep is called paradoxical sleep since the EEG pattern of REM resembles wakefulness.

71
Q

Which is better for normal sleep, BZD or zolpidem?

A

Zolpidem because it induces sleep and then causes little change.

72
Q

What non-BZD is best for patients that awaken in the middle of the night and can’t go back to sleep?

73
Q

Do antihistamines cause drowsiness?

74
Q

Does alcohol help or hinder sleep?

75
Q

What is an effective short term hypnotic drug and will cause drug dependency insomnia within two weeks?

A

Chloral Hydrate

76
Q

Are short or long acting BZD preferred for elderly patients?

A

Short acting BZD

Pharmacology (9 decks)

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