Sedative Hypnotics
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Questions and Answers

Match each term to its definition

sedative (anxiolytic) = reduces anxiety and exerts calming effect, CNS depression should be minimum hypnotics = induce sleep, CNS effects are more pronounced and follow a dose response Sedation/anxiolytic: = reduce nervous excitment, to calm anesthesia = without sensation

Which of the following is a prodrug benzodiazepine that is converted in the stomach by acid hydrolysis to an active drug?

  • Clorazepate (correct)
  • Diazepam
  • Alprazolam
  • Lorazepam

What is clorazepate converted to once activated?

  • oxazepam
  • diazepam
  • desmethyldiazepam (correct)
  • lorazepam

All sedative hypnotics cross the placental barrier and can sedate the baby.

<p>True (A)</p> Signup and view all the answers

Match each drug to its class:

<p>Benzodiazepines = lorazepam, oxazepam, estazolam Barbiturates = Phenobarbital Newer Hypnotics = zolpidem, zaleplon</p> Signup and view all the answers

Match each class of drugs to its description:

<p>Benzodiazepines = (a) biotransformation starts with Phase I especially by CYP 3A4; (b) metabolites then undergo Phase II to form highly water soluble glucuronides; (c) some Phase I metabolites are bioactive and have long half lives (think toxicity from accumulation) Barbiturates = a) metabolic products include Phase II glucuronides</p> Signup and view all the answers

Match each drug to its description

<p>lorazepam, oxazepam, estazolam = drugs that do not produce active metabolites and are safer zolpidem and zaleplon = metabolized to inactive metabolites cimetidine = (OTC drug) inhibits liver enzyme that biotransforms zaleplon, plasma levels rise ketoconazole = inhibits CYP 3A4 which increases plasma levels of eszopiclone</p> Signup and view all the answers

What is the half-life of phenobarbital?

<p>up to 4-5 days (B)</p> Signup and view all the answers

Dose adjustment for reduced kidney function is usually required for sedatives.

<p>False (B)</p> Signup and view all the answers

How is phenobarbital excretion increased?

<p>Making urine alkaline (C)</p> Signup and view all the answers

What percentage of phenobarbital is excreted unchanged in urine?

<p>30% (B)</p> Signup and view all the answers

What can phenobarbital cause?

<p>Liver enzyme induction (A)</p> Signup and view all the answers

Benzodiazepines and the newer hypnotics do not change hepatic enzymes.

<p>True (A)</p> Signup and view all the answers

Which of the following binds to a GABA A receptor site different from the rest?

<p>barbiturates (barbs) (B)</p> Signup and view all the answers

What kind of receptor is the GABA A receptor?

<p>Chloride channel (D)</p> Signup and view all the answers

Match each drug group to its binding site:

<p>Benzodiazepines = Between alpha 1 and gamma 2 (GABA A) Zolpidem, Zaleplon, Eszopiclone = Bind to receptor isoform that contains alpha 1 subunit</p> Signup and view all the answers

What is the mechanism of action (MOA) of benzodiazepines?

<p>Increase the frequency of channel opening (more time for Cl to flow in) (A)</p> Signup and view all the answers

What is the mechanism of action (MOA) of barbiturates?

<p>Increase the duration of the channel opening and at higher doses may substitute for GABA. (B)</p> Signup and view all the answers

What can Benzodiazepines induce? (Select all that apply)

<p>Major CNS depression (B), Surgical anesthesia (C)</p> Signup and view all the answers

Barbiturates are more dangerous than benzodiazepines.

<p>True (A)</p> Signup and view all the answers

What are zolpidem, zaleplon, and eszopiclone used as?

<p>sleep aids (B)</p> Signup and view all the answers

Match each benzodiazepine binding site ligand to its role:

<p>Agonists = Facilitate actions of GABA Antagonists = Treat overdose Inverse Agonist = Produce anxiety and seizures</p> Signup and view all the answers

What is flumazenil used for?

<p>Treat overdose (A)</p> Signup and view all the answers

Why does flumazenil not reverse or block barbiturates, ethanol, or meprobamate?

<p>Flumazenil only affects GABA-A receptors that are activated by benzodiazepines. (A)</p> Signup and view all the answers

Match each drug to its use:

<p>Anesthesia = thiopental, methohexital, diazepam, lorazepam and midazolam Anticonvulsant Effects = clonazepam, nitrazepam, lorazepam and diazepam; phenobarbital and metharbital Muscle Relaxation = benzodiazepines: Diazepam</p> Signup and view all the answers

Match each to its description

<p>benzos (Diazapam) = inhibit polysynaptic reflexes and internuncial transmission and at high doses may also depress transmission at the skeletal muscle junction thiopental and methohexital = short term, rapid acting used to induce stage III anesthesia because of rapid entry into the brain diazepam, lorazepam and midazolam = used to induce anesthesia clonazepam, nitrazepam, lorazapam and diazepam = reverse seizure episodes</p> Signup and view all the answers

What is the usual cause of death due to overdose?

<p>depression of medullary respiration center (B)</p> Signup and view all the answers

Benzodiazepines do not cause physiological dependence.

<p>False (B)</p> Signup and view all the answers

What is the benzodiazepine of choice for treating anxiety?

<p>alprazolam (A)</p> Signup and view all the answers

Which of the following are adverse drug reactions (ADRs) of sedative hypnotics? (Select all that apply)

<p>The most common cause of confusional states in the elderly. (A), Drugs most often involved in deliberate overdose. (B)</p> Signup and view all the answers

Where are orexin A and B found?

<p>The area of the brain that controls wakefulness (D)</p> Signup and view all the answers

Which of the following is an orexin antagonist?

<p>Suvorexant (C)</p> Signup and view all the answers

Which of the following was the world's first benzodiazepine drug?

<p>Chlordiazepoxide (A)</p> Signup and view all the answers

All barbiturates bind to GABA A receptors.

<p>True (A)</p> Signup and view all the answers

Match each drug to its use

<p>hydroxyzine = Induces sleep;an antihistamine (H1 antagonist blocker), older antihistamines cross the BBB ramelteon = melatonin receptor activator (agonist) used to induce sleep buspirone = Used to treat long-term anxiety disorder chloral hydrate = original date rape drug</p> Signup and view all the answers

Which of the following benzodiazepines are considered safer for geriatric patients because their active metabolites are not retained? (Select all that apply)

<p>estazolam (B), Lorazepam (D), oxazepam (A)</p> Signup and view all the answers

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Capital of France (example flashcard)

Paris

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