Pharm - Sedatives & Alcohol Flashcards
What are examples of the Benzodiazepines?
MIDAZOLAM
ALPRAZOLAM (Xanax ®)
TRIAZOLAM (Halcion®)
DIAZEPAM (Valium®)
FLURAZEPAM
NITRAZEPAM
LORAZEPAM
FLUNITRAZEPAM (Rohypnol® Date rape drug)
OXAZEPAM
CHLORDIAZEPOXIDE
What is the Mechanism of Action for Benzodiazepines ?
Bind to a receptor site on the GABA channel; different from the GABA binding site. This increases the binding of GABA resulting in increased frequency of channel opening.
What are examples of Non - Benzodiazepine ?
ZOLPIDEM
ZALEPLON
What are the clinical applications of Benzodiazepines ?
- Acute Anxiolytic
- Hypnotic
- Muscle Relaxation
- Anticonvolustants
- Alcohol Withdrawal
Which Benzodiazepines are excreted by Glucorodination?
Lorazepam
Temazepam
By what process are all other Benzodiazepines eliminated ?
Oxidation by CYP450/ CYP3A4/2C19
True or False? Phase I metabolites are usually active.
TRUE!!
What is an examples of a Long acting BZD?
Diazepam
What is an example of a short acting BZD?
Midazolam, Triazolam
What is an example of an Intermediate acting BZD?
Alprazolam
What type of BZD is preferred as a sedative?
Short- acting preferred
What type of BZD is preferred as a Hypnotic?
Long-acting preferred for maintaining sleep,
short-acting for inducing sleep
Which BZD’s are Only useful for Hypnosis?
Zolpidem & Zaleplon
What is the Antagonist used for Benzodiazepines?
FLUMAZENIL
Which drug is a competitive antagonist of Orexin (OX)) 1& 2 receptors - shutting down the release of Histamine ?
Suvorexant