sedative/hypnotics DSA Flashcards
1
Q
Benzodiazepines
A
- Alprazolam
- Chlordiazepoxide
- Clonazepam
- Clorazepate
- Diazepam
- Flurazepam
- Lorazepam
- Midazolam
- Oxazepam
- Triazolam
2
Q
Benzodiazepine Antagonist
A
-Flumazenil
3
Q
Barbiturates
A
- Amobarbital
- Butabarbital
- Pentobarbital
- Phenobarbital
- Secobarbital
- Thiopental
4
Q
Newer sedative-hypnotic drugs
A
-Buspirone
-Eszopiclone
-Meprobamate
-Ramelteon
-Zaleplon
-Zolpidem
(BEMRZZ)
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
6
Q
Barbiturates- biotransformation
A
-hepatic metabolism, kidney excretion
7
Q
Sedative-Hypnotics- sedation effects
A
- reduction of anxiety
- depressant effects on psychomotor and cognitive fxns
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
9
Q
Sedative-Hypnotics- anticonvulsant effects
A
- some benzodiazepines and barbiturates (phenobarbital) are used for seizures
- zolpidem, zaleplon, eszopiclone lack anticonvulsant activity
10
Q
Sedative-Hypnotics- m relaxation
A
-zolpidem, zaleplon, eszopiclone do not cause m relaxation
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
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)
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
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