2. Sedative and Hypnotic Drugs Flashcards

1
Q

Sedative-Hypnotic drugs have three categories including Benzodiazepines, barbiturates and miscellaneous agents. Benzodiazepines have short acting (triazolam), long acting (flurazepam) and intermediate acting such as?

A

Alprazolam

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2
Q

Barbiturates have an ultra-short action such as thiopental, short acting such a secobarbital, and what is the long acting barbiturate? (Note: misc drugs are busprione, eszopiclone, zaleplon, and zolpidem)

A

Phenobarbital (he likes dis one)

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3
Q

Sedative drugs are CNS depressants, moderates and calms the patient, fast acting, is anxiolytic and causes sedation. Hypnotic drugs produce drowsiness and facilitates the onset and maintenance of sleep, they involve more pronounced depression of?

A

CNS (which can be acheived by many drugs by increasing dosage)

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4
Q

barbiturates and benzodiazepines have the same effect as lower doses, but as doses increase the effects do as well. At the max dosage, benzos can only cause anesthesia, what can barbiturates cause?

A

Increasing dosage of barbiturates can lead to medullary depression, coma and at even higher doses- DEATH

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5
Q

Clinically, sedative hypontic drugs are used for relief of anxiety, insomnia, sedation before procedures, epilepsy, seizures, control ETOH and other withdrawal states, muscle relaxation, and as diagnostic aids or for tx in?

A

Psychiatry (my strange addiction type shit)

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6
Q

What acts on GABAa receptors to cause sedation, hypnotic effects, muscle relaxation, anxiolytic and anticonvulsant effects?

A

Benzodiazepines

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7
Q

What acts on GABAa receptors to cause a wide spectrum of effects, such as mild sedation to anesthesia?

A

Barbiturates

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8
Q

Benzos are widely used and distributed through the body including CNS, placenta and breast milk, they are metabolized by CYP3A4 and elimination ranges from 2-100 hours, there is a risk of dependence and tolerance and the MOA is what?

A

Bind to GABAa receptor and enhances GABAs effects leading to increase chloride influx, hyperpolarization, decreasing number of action potentials = CNS depression

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9
Q

Benzos are used to treat anxiety, including alprazolam, diazepam, clonazepam, lorazepam. Advantages include that there is a high therapeutic index (flumazenil is used for overdose), low risk of drug drug interaction and minimal effect on?

A

Cardiovascular or autonomic function

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10
Q

Disadvantages of benzos used for anxiety states include a risk of dependence, depression of CNS when combined with other drugs, especially ETOH… Newer antidepressants are sometimes preferred such as?

A

SSRIs

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11
Q

What drug has a 1/2 life of >100, active metabolites, and has a very fast rate of onset after administration?

A

Diazepam

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12
Q

What drug has a 1/2 life of 5-14, no active metabolites, and has a slow rate of onset after administration?

A

Oxazepam

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13
Q

What drug has a 1/2 life of 10-20hrs, no active metabolites, and has an intermediate rate of onset after administration?

A

Lorazepam

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14
Q

What drug has a 1/2 life of 12-15, no active metabolites, and has a fast rate of onset after administration?

A

Alprazolam

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15
Q

What drug has a 1/2 life of 20-50hrs, no active metabolites, and has an intermediate of onset after administration?

A

Clonazepam

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16
Q
The following drugs are considered what type?
alprazolam
oxazepam
temazepam
midazolam
triazolam
A

Short to intermediate acting benzodiazepines

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17
Q

The following drugs are considered what type?
diazepam
lorazepam
clonazepam

A

Intermediate to long acting benzodiazepines

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18
Q

What can occur with benzodiazepines due to long half lives which leaves them more likely to cause cumulative effects with multiple doses?

A

Cumulative toxicity

19
Q

What drug is indicated for anxiety, bound 80% to human serum protein, extensively* metabolized by CYP3A4, also indicated for panic disorder, open angle glaucoma (not narrow angle), contra with keto/itraconazole, and causes dependence and withdrawal reactions (taper)?

A

Alprazolam

20
Q

What benzo drug is given IM or IV for preoperative sedation/anxiolysis/amnesia, prior to or during diagnostic therapeutic and endoscopic procedures, IV for induction of general anesthesia, BBW: resp depression and arrest?

A

Midazolam

21
Q

What benzo exerts anxiolytic, sedative, muscle relaxant, anticonvulsant and amnestic effects, with active metabolite N-desmethyldiazepam having a 1/2 life of up to 100 hours, 1/2 increase 2-5 fold in mild/mod cirrhosis to 500hours?

A

Diazepam

22
Q

Diazepam (aka Valium) is indicated for anxiety disorders or short term relief of anxiety, can be used with alcohol withdrawal to relieve acute agitation, tremor, delerium and hallucinosis, contra in people w HS to the drug and children under the age of 6, contraindicated in patients with myasthenia gravis, severe resp insufficiency, and?

A

severe hepatic insufficiency

23
Q

Diazepam may be used in patients with open angle glaucoma but contraindicated in narrow angle, it is NOT recommended in tx of psychotic patients and patients should not consume what?

A

ALCOHOL due to CNS depression

24
Q

What benzo is used in the treatment of anxiety, anxiety with depression and/or acute alcohol withdrawal?

A

Oxazapam

25
Q

What benzo is indicated for short term treatment of insomnia (7-10days max), with a BBW stating concomitant use with opiods may result in profound sedation, respiratory depression, coma and death?

A

Triazolam

26
Q

What is a long acting hypnotic agent useful for treatment of insomnia (cant fall asleep, awake at night, or early am), failure of insomnia to remit after 7-10 days requires further work up for other illnesses (NOT long term use)?

A

Flurazepam

27
Q

What is used in the treatment of seizure disorders such as epilepsy, and is also used before surgery and medical procedures to relieve anxiety?

A

Lorazepam

28
Q

What is a benzo receptor antagonist which competitively inhibits the activity at the benzo recognition site on the GABA receptor complex, used for complete/partial reversal* of sedative benzo effects and for benzo overdose**?

A

Flumazenil

29
Q

Flumazenil, which is used as an antidote for benzodiazepine overdose, and is associated with what, which are most frequent in patients who have been on benzos for long term sedation or in overdose cases?

A

*Seizures

30
Q

barbiturates are used in the treatment of anxiety, epilepsy, to induce sleep and classic anesthetics, however today use is limited to extreme insomnia, unresponsive seizures, induction of anesthesia, combo w acetaminophen and caffeine for tension headaches and counteract stimulant effects of drugs such as?2

A

cocaine and meth

31
Q

Barbiturates are widely distributed in CNS, placenta, and breast milk, can induce* CYP450 enzymes (especially phenobarbital), MOA: bind to GABAa receptor increasing GABA release = CNS depression, there is a risk of?

A

Dependence and tolerance

32
Q
Match drug with its indication
Ultrashort acting Thiopental
Short acting secobarbital
Long acting phenobarbital
Insomnia
Seizures
Anesthesia
A

Ultrashort acting Thiopental = Anesthesia
Short acting secobarbital = Insomnia
Long acting phenobarbital = Seizures

33
Q

What barbiturate is aka as pentothal and admin via IV only, mainly used for sole anesthetic agent for breif 15 minute procedures, with adverse reactions including resp depression, myocardial depression and caridac arrhythmias?

A

Thiopental (anesthesia only)

34
Q

What drug is used as a hypnotic for short term tx of insomnia since it loses its effectiveness in 2 weeks and a preanesthetic, contra in HS pts, and pts w hx of mainfest or latent porphyria, marked impairment of liver function, and resp disease? (failure of insomnia to remit after 7-10 day = presence of primary psychiatric illness)

A

Secobarbital

35
Q

What barbiturate is used as a sedative or hypnotic, contra in pt w HS, and w hx of manifest or latent porphyria, failure of insomnia to remit after 7-10 day = presence of primary psychiatric illness, admin w caution if at all to mentall depressed, suicidal tendencies or hx of drug abuse, drug show to induce liver microsomal enzymes?

A

Phenobarbital

36
Q

Tx for insomnia vaires, benzos are used but can cause daytime sedation and may develop anterograde amnesia and tolerance. Zolpidem, Zaleplon and eszopiclone (new drugs) are highly effective, rapid onset with minimal hangover effects, zolpidem has biphasic release for susatinaed sleep and what has the longest half life?

A

Eszopiclone

37
Q

What is a new drug that has a MOA of agonist at MT1 and MT2 melatonin receptors, used for insomnia, metabolized by CYP1A2, and SE include dizziness, somnolence, fatigue and endocrine changes?

A

Ramelteon

38
Q

Newer hypnotics (sleep aids) ex: eszopiclone, zolpidem, zaleplon, are metabolized by CYP3A4, with short half lifes (6hrs), MOA: bind GABAa1 subunit, which is ONLY approved for treatment of?

A

Sleep disorders (not for anxiolytic, anesthetic, anticonvulsant, or anything)

39
Q

What drug is used for the treatment of generalized anxiety disorder, which take more than one week to become established, does not cause sedation, hypnotic, euphoric, or anticonvulsant effects, metabolized via CYP3A4 and MOA is UNKNOWN?

A

Buspirone

40
Q

What drug is a nonbenzodiazepine hypnotic which interacts with gamma-aminobutyric acid benzodiazepine (GABA-BZ) receptor complex, indicated only for short term tx of insomnia, *note sleep distrubances can be presenting sign of physical and or psychiatric disorder- be careful prescribing and only for 7-10 days?

A

Zaleplon

41
Q

What is a nonbenzodiazepine hypnotic indicated for short term tx of insomnia chracterized by difficulty with sleep initiation, only prescribe for 7-10 days, dont take if allergic to drug, can caues worsening of depression or suicidal thinking may occur?

A

Zolpidem (drug interactions with other CNS depressant or alcohol)

42
Q

What nonbenzodiazepine hypnotic is used for tx of insomnia characterized by difficulty with sleep onset, melatonin MT1/2 receptor agonit >MT3, demonstrates full agonist activity, which is believed to contribute to its sleep promoting properties, metabolized via CYP1A2 ?

A

Ramelteon

43
Q

What nonbenzodiazepine hypnotic is used for tx of insomnia, decreasing sleep latency and improve maintence, there are CNS depressant effects, when used w alcohol can cause additive psychomotor impairment, pts w hepatic impairment, impaired resp function, impaired drug metabolism should not use it?

A

Eszopiclone

44
Q

Meprobamate is used to tx anxiety disorders which works by slowing activity in the brain to allow for relaxation. What is used for short term as a sedative or sleep medicine, alcohol withdrawal symptoms?

A

Chloral Hydrate