AGENTS, CONTROLLING THE FUNCTIONS OF THE CENTRAL NERVOUS SYSTEM - Hypnotic drugs Flashcards
Hypnotic drugs are used to treat
Sleep disorders
Hypnotic drugs should
Produce drowsiness, encourage the onset and maintenance of sleep
Which chemical agents are used in the treatment of insomnia?
- Benzodiazepines
- Imidazopyridines
- Barbiturates
Select a hypnotic drug, which is a benzodiazepine derivative
Flurazepam
Tick a hypnotic agent – a barbituric acid derivative
Thyopental
Select a hypnotic drug, which is an imidazopyridine derivative
Zolpidem
Which hypnotic agents is absorbed slowly?
Temazepam
Which barbiturates is an ultra-short-acting drug?
Thiopental
Indicate the barbituric acid derivative, which has 4-5 days elimination half-life
Phenobarbital
Indicate the hypnotic benzodiazepine, which has the shortest elimination half-life
Triazolam
Which hypnotic drugs is more likely to cause cumulative and residual effects?
Phenobarbital
Which hypnotic drugs increases the activity of hepatic drug-metabolizing enzyme systems?
Phenobarbital
Hepatic microsomal drug-metabolizing enzyme induction leads to
Barbiturate tolerance
True or False. Hypnotic benzodiazepines are more powerful enzyme inducers than barbiturates.
FALSE
Indicate the hypnotic drug, which does not change hepatic drug-metabolizing enzyme activity?
- Flurazepam
- Zaleplon
- Triazolam
Barbiturates increase the rate of metabolism of
- Anticoagulants
- Digitalis compounds
- Glucocorticoids
Which agents inhibits hepatic metabolism of hypnotics?
Cimetidin
Which factors can influence the biodisposition of hypnotic agents?
- Alterations in the hepatic function resulting from a disease
- Old age
- Drug-induced increases or decreases in microsomal enzyme activities
Which hypnotics is preferred for elderly patients?
Temazepam
Which hypnotics is preferred in patients with limited hepatic function?
Zolpidem
Indicate the mechanism of barbiturate action (at hypnotic doses)
Increasing the duration of the GABA-gated Cl- channel openings
Imidazopyridines are
Selective agonists of the BZ1 (omega1) subtype of BZ receptors
Which hypnotic agents is a positive allosteric modulator of GABA-A receptor function?
- Zaleplon
- Flurazepam
- Zolpidem
Indicate a hypnotic drug - a selective agonist at the BZ1 receptor subtype
Zolpidem
Which hypnotic agents is able to interact with both BZ1 and BZ2 receptor subtypes?
Flurazepam
Indicate the competitive antagonist of BZ receptors
Flumazenil
Flumazenil blocks the actions of
Zolpidem
Indicate the agent, which interferes with GABA binding
Bicuculline
Which agents blocks the chloride channel directly?
Picrotoxin
Which agents is preferred in the treatment of insomnia?
Hypnotic benzodiazepines
Barbiturates are being replaced by hypnotic benzodiazepines because of
- Low therapeutic index
- Suppression in REM sleep
- High potential of physical dependence and abuse
Which benzodiazepines is used mainly for hypnosis?
Flurazepam
Indicate the main claim for an ideal hypnotic agent
- Rapid onset and sufficient duration of action
- Minor effects on sleep patterns
- Minimal “hangover” effects
Which stage of sleep is responsible for the incidence of dreams?
REM sleep
During slow wave sleep (stage 3 and 4 NREM sleep)
Somnambulism and nightmares occur
All of the hypnotic drugs induce
Decrease the duration of REM sleep
Which hypnotic drugs causes least suppression of REM sleep?
Flurazepam
Although the benzodiazepines continue to be the agents of choice for insomnia, they have
- The possibility of psychological and physiological dependence
- Synergistic depression of CNS with other drugs (especially alcohol)
- Residual drowsiness and daytime sedation
Hypnotic benzodiazepines can cause
A dose-dependent decrease in both REM and slow wave sleep
Which hypnotic benzodiazepines is more likely to cause rebound insomnia?
Triazolam
Which hypnotic benzodiazepines is more likely to cause “hangover” effects such as drowsiness, dysphoria, and mental or motor depression the following day?
Flurazepam
Indicate the hypnotic drug, which binds selectively to the BZ1 receptor subtype, facilitating GABAergic inhibition
Zolpidem
Which statements is correct for zolpidem?
- Causes minor effects on sleep patterns
- The risk of development of tolerance and dependence is less than with the use of hypnotic benzodiazepines
- Has minimal muscle relaxing and anticonvulsant effects
Which agent exerts hypnotic activity with minimal muscle relaxing and anticonvulsant effects?
Zaleplon
True or False. Zolpidem and zaleplon have effectiveness similar to that of hypnotic benzodiazepines in the management of sleep disorders.
TRUE
Which hypnotic drugs is used intravenously as anesthesia?
Thiopental
Indicate the usual cause of death due to overdose of hypnotics
Depression of the medullar respiratory center
Toxic doses of hypnotics may cause a circulatory collapse as a result of
Action on the medullar vasomotor center
