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PMCOL 305 > Sedatives and Hypnotics > Flashcards

Sedatives and Hypnotics Flashcards

1
Q

What do sedatives do?

A

Relieve anxiety, cause relaxation, mild CNS depressants

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2
Q

What do hypnotics do?

A

Cause drowsiness and sleep

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3
Q

What drug class do barbiturates fall under?

A

Schedule IV (USA)

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4
Q

What are some characteristics of sedatives and hypnotics?

A

Orexin antagonists, melatonin agonists, anti-histamines

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5
Q

What drugs treat anxiety?

A

Benzos = ‘aze’-pams

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6
Q

What type of drugs treats seizure disorder?

A

Anti-convulsants
Longer-acting
Phenobarbital

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7
Q

What type of drugs causes anesthesia?

A

Short-acting drugs
Thiopental, midazolam, trazolam

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8
Q

What is the difference between sedatives and hypnotics?

A

Sedatives are for calming
Hypnotics are for sleeping

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9
Q

How are sedatives classified?

A

Lipophilic class = faster onset due to rapid distribution
Longer-acting = anticonvulsants, muscle relaxants, anxiolytics
Shorter-acting = pre-anesthetic sedatives or to treat insomnia

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10
Q

What does the presence of a triazole ring do?

A

Higher potency
Decreased duration of action
Binds GABA better

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11
Q

What are the routes of administration of sedatives?

A

Oral, rectal, injection

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12
Q

How are benzos and barbiturates distributed?

A

Benzos are less lipid soluble than barbituates, absorbed more slowly, slower onset of action
Both are highly bound to plasma proteins
Cross the placenta

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13
Q

What metabolized sedatives?

A

Liver CYP450

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14
Q

What do some sedatives do during metabolism?

A

Some produce active metabolites that prolong the duration of action

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15
Q

What is the half-life of midazolam?

A

2 hours

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16
Q

What is the half-life of diazepam?

A

100 hours

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17
Q

How many half-lives are required for elimination?

A

4-5

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18
Q

What types of people have decreased sedative metabolism?

A

Infants, pregnant women, those with liver disease, the elderly

19
Q

What is floppy infant syndrome?

A

Reduced muscle tone in infants that causes an inability to nurse that can last for months

20
Q

What is the mechanism of GABAa receptor binding of sedatives?

A

GABA binds between alpha and beta subunits
Benzos bind between alpha and gamma subunits in those receptors that contain these subunits

21
Q

What is the mechanism of benzo binding?

A

Bind to a site on the GABAa receptor which increases the frequency of chloride channel openings

22
Q

Where are GABA receptors with benzo binding sites located?

A

Limbic system, reticular activating system, cortex

23
Q

Do GABA receptors that control respiration have benzo sites?

A

Not many

24
Q

What is the mechanism of barbiturate binding?

A

More general effect on GABA receptors
When they bind, the enhance the affinity of the receptor for GABA, which increases the duration of time that they chloride channel is open which leads to neuronal inhibition
Can do this even when GABA isn’t present

25
Q

Benzos are allosteric _?

A

Modulators

26
Q

Barbiturates are allosteric _?

A

Activators

27
Q

What are the acute effects of sedatives?

A

Reduce muscle tone, impair coordination, and increase sedation and sleep
-total sleep time increased, but deep sleep reduced

Reduce anxiety, learning, memory, and can cause bizarre and uninhibited behaviours

28
Q

What are the common side effects of sedatives?

A

Drowsiness, lethargy, dizziness, confusion, reduced libido, diminished concentration, incoordination, and impairment of driving skills
Prevent consolidation of short-term memories, especially alpha subunit-containing receptors
Combined with alcohol to facilitate assault

29
Q

What are the effects of sedatives on a fetus?

A

Rapid entry, increased half-life due to under-developed liver
Potential increased risk of cleft palate, floppy infant syndrome, withdrawal
No risk of major malformations

30
Q

What are the drugs interactions of sedatives?

A

Synergistic with other depressants such as alcohol and opioids
Interact with other drugs metabolized by CYP450 system

31
Q

How is sedative overdose treated?

A

With flumazenil
Relatively rare for benzos by themselves
Barbiturates have a low therapeutic index

32
Q

What rate does tolerance to sedatives happen at?

A

Different rates

Tolerance for sedative effects = days to weeks
Tolerance for anxiolytic effects = 3-4 months
Does not develop for respiratory depression
Users can require 40x the original dose

33
Q

What mechanisms for tolerance develop to barbees?

A

Cellular and metabolic mechanisms

34
Q

What are benzos well-known for?

A

Producing tolerance

35
Q

What are the chronic effects of sedative tolerance?

A

Associated with daytime fatigue, accidents, depression, violence, and increased overall mortality

36
Q

Is withdrawal worse for short-acting or long-acting sedatives?

A

Short-acting
Should be medically supervised due to hyperexcitability

37
Q

What are the symptoms of sedative withdrawal?

A

Insomnia, anxiety, tremor, headache, confusion, difficulty concentrating

38
Q

What is sedative dependence like?

A

Physical and psychological dependence

39
Q

Are benzos or barbiturates more addictive?

A

Barbiturates are more addictive

40
Q

What is the abuse potential in sedatives like?

A

Lower than drugs like cocaine and opioids

41
Q

What does disinhibition of VTA DA-ergic neurons increase?

A

Increases DA release in the NAc

42
Q

What is GHB?

A

Date rape
GABAb receptor agonist = Gi/o linked, inhibits Ca channels, activates GIRK
Precursor of GABA, Glu, and Gly
Dose dependent effects

43
Q

What do low doses of GHB do?

A

Stimulatory effect

44
Q

What do high doses of GHB do?

A

Binds to GABA receptors and can cause sedation

PMCOL 305 (18 decks)

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