Anxiolytics, Hypnotics, Sedatives Flashcards
an unpleasant emotional state consisting of apprehension, tension, and feelings of danger without a real or logical cause
anxiety
What are some of the physical symptoms seen with anxiety?
Tachycardia, Tachypnea, sweating, trembling, weakness
What are the major classes of drugs used to treat anxiety?
Benzodiazepines - the most frequently used drugs for anxiety
Azapirones - buspirone
Barbiturates - rarely used today because of severe side effects and a low therapeutic index. These drugs have generally been replaced by the benzodiazepines.
Give some examples of benzodiazepines and their approximate duration of action.
Short acting (2 - 8 hour) :
- Triazolam (Halcion)
- Oxazepam (Serax)
- Midazolam (Versed)
- Clonazepam (Klonopin)
Intermediate-Acting (10-20 hr):
- Temazepam (Restoril)
- Lorazepam (Ativan)
- Alprazolam (Xanax)
Long-Acting (1-3 days):
- Chlordiazepoxide (Librium)
- Diazepam (Valium)
- Flurazepam (Dalmane)
What is GABA?
GABA (gamma-aminobutyric acid) is the major inhibitory neurotransmitter of the CNS
How do benzodiazepines work?
When benzodiazepines bind to specific receptors that are separate from but adjacent to the GABAa receptor, they potentiate the binding of GABA to its own receptor. The binding of GABA to its own receptor results in increased chloride ion conductance, cel membrane hyper polarization, and decreased hyper polarization, and decreased initiation of action potentials.
Remember that benzodiazepines do not bind to GABA receptors - they bind adjacent to them.
What are the therapeutic indications for benzodiazepines?
These drugs are used clinically as muscle relaxants and in the treatment of the following: Anxiety disorders Panic disorders Status Elipepticus Sleep disorders Alcohol withdrawal
DOC of panic disorders
alprazolam
DOC of status epilepticus
diazepam
DOC of sleep disorders
flurazepam or temazepam
DOC alcohol withdrawal
diazepam is mot commonly used
Are benzodiazepines effective for controlling pain as well as anxiety?
No. they have little analgesic effect.
What is their route of administration?
PO, IV, or IM
Where are benzodiazepines metabolized?
They are metabolized in the liver and excreted in the urine. Many of the benzodiazepines have active metabolites
Does dependence occur?
Yes. Prolonged use can result in dependence. Abrupt discontinuation can result in withdrawal symptoms, including confusion, anxiety, and agitation.
What is flumazenil (Romazicon) mechanism of action?
Flumazenil is a copetitive antagonist of benzodiazepines at the GABAa receptor.
Describe the clinical use of flumazenil (Romazicon) drug.
Reversal of benzodiazepine sedation or overdose
How is flumazenil (Romazicon) administered?
IV use only
How long do the effects of flumazenil (Romazicon) last?
only 1 hour - repeat doses may be necessary for a heavily sedated patient to remain alert.
How does Buspirone (BuSpar) work?
acts as a partial agonist at serotonin (5-HT1A) receptors
What are the indications for Buspirone (BuSpar)
generalized anxiety; however unlike benzodiazepines, its effects may take 1-2 weeks to become apparent
What are the pharmacokinetic properties of Buspirone (BuSpar)?
This drug is metabolized by the liver and excreted in the urine; its half-life is 2 - 11 hours.
How do the actions of buspirone (BuSpar) differ from those of the benzodiazepines?
Buspirone lacks the muscle relaxant and anticonvulsant properties of the benzodiazepines.
What advantage does buspirone (BuSpar) have over benzodiazepines?
minimal sedation
low abuse potential
no overdose fatalities reported
no withdrawal symptoms
