sedative/hypnotics DSA Flashcards

1
Q

Benzodiazepines

A
  • Alprazolam
  • Chlordiazepoxide
  • Clonazepam
  • Clorazepate
  • Diazepam
  • Flurazepam
  • Lorazepam
  • Midazolam
  • Oxazepam
  • Triazolam
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2
Q

Benzodiazepine Antagonist

A

-Flumazenil

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3
Q

Barbiturates

A
  • Amobarbital
  • Butabarbital
  • Pentobarbital
  • Phenobarbital
  • Secobarbital
  • Thiopental
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4
Q

Newer sedative-hypnotic drugs

A

-Buspirone
-Eszopiclone
-Meprobamate
-Ramelteon
-Zaleplon
-Zolpidem
(BEMRZZ)

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5
Q

Benzodiazepines- biotransformation

A
  • hepatic metabolism- CYP3A4
  • cumulative toxicity- benzodiazepines w long half-lifes are more likely to cause cumulative effects
  • pts w hepatic insuff- oxazepam and lorazepam
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6
Q

Barbiturates- biotransformation

A

-hepatic metabolism, kidney excretion

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7
Q

Sedative-Hypnotics- sedation effects

A
  • reduction of anxiety

- depressant effects on psychomotor and cognitive fxns

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8
Q

Sedative-Hypnotics- anesthesia

A
  • thiopental and methohexital- lipid-soluble, penetrate brain tissue rapidly after IV admin- induce anesthesia
  • Benzodiazepines used IV for anesthesia in combo w other drugs
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9
Q

Sedative-Hypnotics- anticonvulsant effects

A
  • some benzodiazepines and barbiturates (phenobarbital) are used for seizures
  • zolpidem, zaleplon, eszopiclone lack anticonvulsant activity
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10
Q

Sedative-Hypnotics- m relaxation

A

-zolpidem, zaleplon, eszopiclone do not cause m relaxation

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11
Q

Sedative-Hypnotics- effects on respiration and CV fxn

A
  • depression of medullary resp center- cause of death due to overdose
  • at normal doses, can cause CV depression in pts w dz that impair CV fxn
  • toxic doses- myocardial contractility and vascular tone may be depressed- circulatory collapse
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12
Q

Sedative-Hypnotics- tolerance

A
  • common feature of sedative-hypnotic use- changes in responsiveness of CNS
  • down-reg of GABAa R’s- can cause sedative-hypnotic withdrawal (hyperexcitability of CNS)
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13
Q

Tapering sedative-hypnotics

A
  • abrupt withdrawal of higher doses leads to serious withdrawal signs
  • drugs w short half-lives may lead to signs of withdrawal even between doses
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14
Q

Flumazenil- moa

A
  • binds to benzodiazepine binding site on GABAa Rs- competitive antagonist
  • blocks actions of benzodiazepines, zolpidem, zaleplon, eszopiclone; but does not block the CNS effects of otherrsedative-hypnotics
  • *used for benzodiazepine overdose
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