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Pharm Final > Sedative Hypnotics > Flashcards

Sedative Hypnotics Flashcards

0
Q

Which type of drug has more pronounced depression of the CNS? Sedative or hypnotic?

A

Hypnotic - can be achieved by increasing dose of sedative as well

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1
Q

Name the 5 major classes of drugs used as hypnotics

A 
Benzodiazepines
Barbiturates
NBBRAs - nonbenzo benzo receptor agonists
5-HT1A partial agonists
MT (melatonin) receptor agonists
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2
Q

Which type of sedative hypnotic drug shows a nonlinear dose-response curve? Why is this important?

A

Benzos

Increasing dose eventually tapers off the sedation effects so they are safer drugs. Older drugs showing linear curve could produce anesthesia or even coma and death with increasing dose

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3
Q

MOA of benzos

A

Bind GABAa receptors at BZ1 or BZ2 which functions as a chloride channel and increase its activity by causing more frequent channel openings. They reduce the EC50 of the GABA induced Cl- influx

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4
Q

Agonists at the benzo receptors produce what two important clinical effects?

A

Anxiolytic (anti-anxiety) and anticonvulsant

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5
Q

-azolam or -azepam is the common ending for what class of drugs?

A

Benzos

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6
Q

What is the method of delivery for benzos? How do they distribute?

A

Oral - highly lipophilic and distribute throughout body

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7
Q

Name the 2 short acting benzos

A

Oxazepam and triazolam

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8
Q

Name the three intermediate acting benzos

A

Alprazolam
Lorazepam
Temazepam

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9
Q

Name the two long acting benzos

A

Diazepam

Flurazepam

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10
Q

What enzyme catalyzes phase I reactions of benzos? After this, how are they excreted?

A

CYP3A4

Conjugated and excreted in urine

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11
Q

Name three benzos that are NOT metabolized by the P450 system

A

Oxazepam
Lorazepam
Temazepam

Skip phase I reactions and are conjugated directly

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12
Q

Which benzo is metabolized in liver to active metabolites that can vary in half lives between 30 and 100 hours?

A

Flurazepam

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13
Q

What is the role of benzos in treating anxiety?

A

They are only given short term, 4-6 weeks, while waiting for the SSRI to take effect

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14
Q

Which benzo is useful in treating muscle spasms and can be used in MS and cerebral palsy?

A

Diazepam

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15
Q

Which benzo is used to treat epileptic seizures?

A

Clonazepam

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16
Q

Name the two benzos used to treat status epilepticus

A

Diazepam and lorazepam

State where brain is constantly having a seizure

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17
Q

Which two benzos can be used in managing alcohol withdrawal?

A

Diazepam and oxazepam

18
Q

Name a benzo for each category used in sleep disorders: long, intermediate, and short acting

A

Long: Flurazepam
Intermed: Temazepam
Short: triazolam

19
Q

Patient taking a sleep aid presets with anxiety, irritability, rage, and hostility. What type of drug was she most likely taking?

A

Benzo - can cause paradoxical effects

Barbiturates also do this

20
Q

Name the only two class of drugs where abrupt withdrawal can kill you

A

Benzos and barbiturates

21
Q

What does flumazenil do? Two adverse effects?

A

It is the only benzo receptor antagonist - used in benzo overdose

Can cause withdrawal in the physiologically dependent
Can lead to seizures if the benzo was being used to treat them

22
Q

-barbital is the common ending for what type of drug? What is the only one of its class without this ending?

A

Barbiturate

Thiopental

23
Q

MOA of barbiturates?

A

Like benzos, act at GABAa receptors (but bind at a different site)
But they also bind less specifically than benzos so they also block glutamate receptors and sodium channels

24
Q

Explain how barbiturates can lead to death by respiratory failure

A

They suppress the hypoxic and chemoreceptor response to CO2. So impulse to breathe is blocked

25
Q

What actions do barbiturates have on CYP enzymes?

A

They are CYP inducers

26
Q

Which barbiturate is still used IV to induce anesthesia?

A

Ultra short acting thiopental

27
Q

Which barbiturate has anticonvulsant properties and is still used to treat tonic-clonic seizures, status epilepticus, and eclampsia?

A

Phenobarbital

28
Q

Which sedative drug can be used to treat hyperbillirubinemia and kernicterus in the neonate?

A

Phenobarbital

29
Q

Which sedative class of drug is contraindicated in patients with porphyria?

A

Barbiturates - increase porphyrin synthesis

30
Q

Which sedative class of drug can cause hangover effects?

A

Barbiturates

31
Q

Which sedative class of drug can cause hyperalgesia?

A

Barbiturates

32
Q

Which class of sedative drug, if given rapidly by IV can lead to cardiovascular collapse?

A

Barbiturates

33
Q

Which class of sedative drugs ONLY acts at the BZ1 subtype receptor? What receptor? What effect is not seen due to the lack of BZ2 binding?

A

NBBRAs - non-benzo benzo receptor agonists

GABAa receptor

BZ2 is responsible for minimizing muscle convulsants, so the NBBRAs aren’t used as muscle relaxants

34
Q

What two sedative drugs are prescribed for patients having trouble with sleep initiation but not maintenance? Which has the shorter duration of action?

A

Zolpidem - NBBRA (1.5-3.5)

Zaleplon - NBBRA - shorter half life (1hr)

35
Q

Name the three NBBRAs

A

Zolpiden
Zaleplon
Eszopiclone

“z” drugs

36
Q

Which sedative drug is approved for improving sleep maintenance?

A

Eszopiclone - NBBRA (6 hour half life)

37
Q

Which class of sedative drug is ONLY an anxiolytic and has no hypnotic, anticonvulsant, or muscle relaxant properties? Name the drug

A

5-HT1A partial agonists

Buspirone

38
Q

Which sedative drug has no interactions with alcohol, no interactions with other sedatives, and has no withdrawal on abrupt discontinuation?

A

5-HT1A partial agonists

Buspirone

39
Q

What drug acts at MT1 and MT2 receptors to treat insomnia with difficulty of sleep onset? What receptor are these?

A

Ramelteon - melatonin receptor agonist

40
Q

What antihistamine with antiemetic properties is also approved for relief of anxiety?

A

Hydroxyzine

42
Q

What drug is commonly used to treat performance anxiety?

A

Propranolol

43
Q

Used for Mild Situational Insomnia

A

Diphenhydramine

Doxylamine

Pharm Final (20 decks)

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