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NMSP > Sedative and Hypnotic Drugs > Flashcards

Sedative and Hypnotic Drugs Flashcards

1
Q

Amphetamine, Methylphenidate, and methamphetamine are stimulants that are what schedule drug class? What does that mean?

A

Schedule 2

  • medical use
  • high potential for abuse/dependanve
  • require written presecription
  • no refills allowed
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2
Q

Phentobarbital and secobarbital are what schedule drug schedule? What does that mean?

A

Schedule 2

  • medical use
  • high potential for abuse/dependanve
  • require written presecription
  • no refills allowed
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3
Q

Alprazolam, Clonazepam, midazolam, Diazepam, and Lorazepam are what drug scedule? What does that mean>

A

Schedule 4

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4
Q

What is the most prescribed benzodiazepine?

A

alprazolam (xanax)

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5
Q

Clonazepam(long half life), Alprazolam, Lorazepam, and triazolam are high or low potent Benzos?

A

Higher

CALT –> It is highly potent and dangerous to join cult

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6
Q

Chorldiazepoxide, diazepam, temazepam(short half life) are high or low potent Benzos?

A

Low

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7
Q

Flunitrazepam is also known as what?

A

date rape drug, not prescribed sold on the streets

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8
Q

What drug class facilitates GABA interaction with the GABAa receptors to increase the frequency of the Cl- channel opening in response to GABA but does not have GABA-mimetic effects?

A

Benzodiazepines - causes local hyperpolarization, meaning cell is less likely to fire

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9
Q

What anti anxiety med is useful to only treat sx of acute, transient stress?

A

Benzodiazepines

75% show improvement, 35% show marked improvement; 25% have no response
• best used in combination with psychotherapy

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10
Q

What IV benzo can cause respiratory depression and apnea?

A

midazolam

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11
Q

– >in healthy adults, little effect on either cardiac output or
blood pressure with therapeutic doses
–> large doses cause clinically insignificant decreases in blood pressure and cardiac output

Are the cardiovascular effects of what drug?

A

Benzodiazepines

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12
Q

phase I reactions (CYP3A4) and then glucuronidation (phase II) are the metabolism for most drugs in what class?

A

Benzodiazepines

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13
Q

Elderly are particularly susceptible to side effects while alcoholics and barbiturate drug abusers are resistant to what drug?

A

Benzodiazepines

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14
Q

Paradoxic reactions, such as excitement leading to nightmares, hyperactivity, insomnia, irritability, agitation, and/or rage/hostility, occur occasionally in the elderly and young occur with what drug?

A

Benzodiazepines

• benzodiazepines change normal sleep patterns… gain stage II sleep at the expense of stages I, III, IV and REM sleep

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15
Q

What is MOA of Diazepam, alprazolam, temazepam, midazolam?

A

-binds to specific GABA-A receptor subunits at central nervous system (CNS) neuronal synapses facilitating GABA- mediated chloride ion channel opening frequency

• enhances membrane hyperpolarization

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16
Q 
Dose- dependent depressant effects on the CNS including:
• sedation
• relief of
anxiety
• amnesia
• hypnosis
• anesthesia
• coma
can be caused by what drug?
A
  1. Diazepam (valium)
  2. Alprazolam (xanax)
  3. Temazepam (restoril)
  4. Midazolam (Versed)- also causes respiratory depression
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17
Q

Opioids + Benzos can cause what?

A

sedation, respiratory depression, coma, and death

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18
Q
  • alcohol withdrawal syndrome:
  • anxiety, acute/severe:
  • management of anxiety disorders
  • muscle spasm, spasticity, and/or rigidity:
  • spasticity caused by upper motor neuron disorders:
  • seizures, acute, active: adjunct intermittent if seizures are refractory, atypical for patient, etc.
  • status epilepticus:

Are indications for what drug?

A

Diazepam

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19
Q

How is diazepam administered?

A
  • Oral or injectable
  • metabolized by CYP3A4
  • half like of 60-72 hours
  • caution with kidney or liver problems
20
Q

What is temazepam used for?

A

Insomnia

21
Q

What is triazolam (halcyon) used for?

A

Insomnia, also can cause amnesia (used as a murder defense)

22
Q

Zolpidiem, Eszopiclone, and zaleplon are what?

A

non-benzodiazepine agonists

-eszopiclone was the first approved for long term use because no tolerance or dependance

23
Q

What drug binds selectively to BZ1 receptors, a subgroup of GABA-A receptors, acting like benzodiazepines to enhance membrane hyperpolarization?

A

Zolpidem (Ambien)

24
Q

What drug has rapid onset of hypnosis with few amnestic effects or day-after psychomotor depression or somnolence

-BUT NO anxiolytic, anesthetic, anticonvulsant, muscle relaxing, respiratory, or cardiovascular effects?

A

zolpidem (Ambien)

25
Q

What is the use of zolpidem (Ambien)?

A

Insomnia

26
Q

Can zolpidem (ambien) be used in pregnancy?

A

yes

27
Q

What drug is an antagonist at benzodiazepine-binding sites on the GABA-
A receptor?

A

Flumazenil

28
Q

What drug is used for management of benzodiazepine overdose and reversal of benzodiazepine- induced sedation during surgical procedures

A

Flumazenil –> reverses Benzes in 1-2 minutes

29
Q

What drug blocks actions of benzodiazepines and zolpidem

A

Flumazenil

• does not block other sedative- hypnotic drugs like barbiturates, alcohol, ramelteon, suvorexant

30
Q

What is a long-acting barbiturate (t1/2 = 10 hr) used to control tonic-clonic seizures?

A

Phenobarbital

31
Q

What barbiturate is used for headache pain and has a half life of 35 hours?

A

butablbital

32
Q

What is MOA of barbiturates?

A

– binds to the GABAA receptor, increases the DURATION of GABA-gated channel openings

–↑ chloride influx, ↑ hyperpolarization, ↓ number of action potentials (= CNS depression)

DIFFERENCES FROM BENZOS
– at higher doses, barbiturates also lead directly to Cl- channel opening in absence of GABA
– also inhibit a subset of excitatory glutamate receptors
• these latter 2 actions are not shared by benzodiazepines and may help explain why
barbiturates have a much lower margin of safety

33
Q

What drugs can easily cross the placenta and cause respiratory depression in the fetus?

A

Barbiturates

34
Q

Barbiturates are classic inducers of what?

A

CYP3A4

  • undergo hepatic metabolism and excretion via kidney
35
Q

-high risks for dependence and development of drug tolerance

– cause respiratory depression, do not use if compromised
respiration

– cause sneezing, cough, laryngospasm, hiccough

– confusion, somnolence, impaired psychomotor performance

– unusual behavioral reactions can occur, but rarely:
• attitudinal depression
• manic behavior, anxiety, hostility, rage…

– possible severe consequences if combined with other CNS depressants (e.g., alcohol)

are adverse side effects of what?

A

Barbiturates

36
Q

What is MOA of Buspirone?

A

A nonbenzodiazepine anxiolytic

• mechanism uncertain: partial agonist at 5- HT receptors, but interactions with other receptor

37
Q

What nonbenzodiazepine anxiolytic is used in generalized anxiety states

  • useful to augment partial response to antidepressant
  • lacks tolerance, dependence, and withdrawal
A

Buspirone

38
Q
  • insomnia
  • agitation
  • nausea
  • alsoriskof
  • tachycardia
  • paresthesias
  • gastrointestinal distress
  • Interactions: CYP3A 4 inducers and inhibitors

Are side effects for what drug?

A

Buspirone

has interactions with CYP3A 4 inducers and inhibitors

  • does not cause sedation, hypnotic, euphoric, anticonvulsant, or muscle relaxant effects of benzodiazepines
  • does not augment sedation of alcohol or other CNS depressants
  • little effect on cognitive or psychomotor function
39
Q

What drug activates MT1 and

MT2 receptors in suprachiasmatic nuclei in the CNS?

A

Ramelteon

40
Q

What are the effects of Ramelteon?

A

-rapid onset of sleep
with minimal rebound insomnia or withdrawal symptoms

  • used from sleep disorders, esp falling asleep
  • no abuse, withdrawal, or dependency risk but doesn’t work well
41
Q

What enzyme does ramelteon activate?

A

CYP1A2

42
Q

What drug blocks binding of orexins, neuropeptides that promote wakefulness?

A

Suvorexant

43
Q

What are the clinical applications of suvorexant?

A

sleep disorders, especially those characterize d by difficulty in falling asleep

44
Q

What drug antagonizes H1 receptors and inhibits reuptake of NE and 5-HT?

A

Doxepin

45
Q

What are the applications of doxepin?

A

• insomnia, sleep
maintenance only

• treatment- resistant
major unipolar depressive disorder (requires ~ 2wks of treatment)

  • causes sefation
46
Q

Black box warning of all antidepressants related to increased suicidal ideation
possible anticholinergic effects (opposite of SLUDGE) and CNS depression impairing ability to operate machinery, etc are toxicities of what?

A

Doxepin

47
Q

What drug class causes sedation but does not relieve anxiety?

A

antihistamines

NMSP (14 decks)

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