PCOL M2.3 Flashcards
- Oxazepam
BENZODIAZEPINES
I. Short-acting (2-8 hours)
- Midazolam
BENZODIAZEPINES
I. Short-acting (2-8 hours)
- Triazolam
BENZODIAZEPINES
I. Short-acting (2-8 hours)
- Chlordiazepoxide
BENZODIAZEPINES
III. Long-acting (1-3 days)
- Diazepam
BENZODIAZEPINES
III. Long-acting (1-3 days)
- Chlorazepate
BENZODIAZEPINES
III. Long-acting (1-3 days)
- Flurazepam
BENZODIAZEPINES
III. Long-acting (1-3 days)
- Quazepam
BENZODIAZEPINES
III. Long-acting (1-3 days)
- Nordazepam
BENZODIAZEPINES
III. Long-acting (1-3 days)
- Lorazepam
BENZODIAZEPINES
II. Intermediate-acting (10-20 hours)
- Alprazolam
BENZODIAZEPINES
II. Intermediate-acting (10-20 hours)
- Temazepam
BENZODIAZEPINES
II. Intermediate-acting (10-20 hours)
- Estazolam
BENZODIAZEPINES
II. Intermediate-acting (10-20 hours)
BENZODIAZEPINES
I. Short-acting (2-8 hours)
- Oxazepam
- Midazolam
- Triazolam
BENZODIAZEPINES
II. Intermediate-acting (10-20 hours)
- Temazepam
- Lorazepam
- Alprazolam
- Estazolam
BENZODIAZEPINES
III. Long-acting (1-3 days)
- Chlordiazepoxide
- Diazepam
- Flurazepam
- Chlorazepate
- Quazepam
- Nordazepam – active metabolite of Diazepam, Chlordiazepoxide, and chlorazepate
BARBITURATES
Long-acting ( > 6 hours)
- Phenobarbital
- Barbital
BARBITURATES
Intermediate-acting (3-5 hours)
- Amobarbital
- Butabarbital
BARBITURATES
Short-acting (2 hrs.)
- Pentobarbital
- Hexobarbital
- Secobarbital
Ultra-short-acting (30 minutes)
- Thiopental
New sedative hypnotics in MISCELLANEOUS AGENTS
*Zaleplon and Eszopiclone *Ramelteon and Tasimelteon *Almorexant and Suvorexant
Absorption and Distribution = extremely rapid
triazolam & diazepam
A prodrug, is converted to its active form,
desmethyldiazepam (nordiazepam), by acid
hydrolysis in the stomach.
Clorazepate
barbiturates absorbed rapidly into the blood following oral
administration.
eszopiclone, zaleplon,
zolpidem
lipophilic character
placental barrier during
pregnancy
detectable in breast milk and may
exert depressant effects in the nursing infant
All sedative-hypnotics
Metabolized by microsomal drug-metabolizing enzyme
systems of the liver.
Biotransformation of BZDs
Elimination half-life of more than 40 hours
Desmethyldiazepam
Active metabolite of chlordiazepoxide, diazepam,
prazepam, and clorazepate.
Desmethyldiazepam
undergo alpha-hydroxylation
Alprazolam and Triazolam
The resulting metabolites appear to exert short-lived
pharmacologic effects because they are rapidly
conjugated to form inactive glucuronides.
Alprazolam and Triazolam
The short elimination half-life of ———(2–3 hours)
favors its use as a hypnotic rather than as a sedative drug.
triazolam
With relatively short half-lives metabolized directly to inactive glucoronides
less likely to cause residual effects.
Estazolam, Oxazepam, Lorazepam
They are affected by inhibitors and inducers of hepatic
P450 isozymes
Diazepam, Midazolam, Triazolam