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2 Pharm Unit > 26 Sedative Hypnotics and Anti-anxiety > Flashcards

26 Sedative Hypnotics and Anti-anxiety Flashcards

1
Q

What are of the brain regulates the heartbeat and other visceral functions and processes the emotion fear?

A

Amygdala

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2
Q

What are of the brain is needed for establishment of long-term memory in regions of the cerebral cortex?

A

Hippocampus

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3
Q

Drugs that reduce anxiety, exert calm are _, while drugs that produce drowsiness, encourage sleep are _

A

SedativesHypnotics

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4
Q

How can benzodiezapines be used to avoid producing sedation?

A

Low doses can relieve anxiety without sedation

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5
Q

What are the 2 examples of non-benzodiezapines that interact with benzodiezapine receptors?

A

ZolpidemZaleplon

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6
Q

What are the 4 examples of barbiturates provided?

A

PentobarbitalPhenobarbitalAmobarbitalThiopental

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7
Q

What class of drug is the preferred agent for use as a sedative hypnotic, anxiolytic, muscle relaxant and or anticonvulsant?

A

Benzodiezapines

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8
Q

True or false: Benzodiezapines can be used an anesthetics and analgesics at higher doses.

A

False. These drugs are neither anesthetics or analgesics

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9
Q

What is the receptor target of benzodiezapines? Where are these receptors targets located? What is the effect of receptor activation?

A

GABA-A receptorsLimbic systemGABA mimetic, enhance neuronal inhibition

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10
Q

When barbiturates and benzodiezapines bind GABA-A, what effect does that have on GABA activity?

A

Enhances GABA activity

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11
Q

When GABA binds the GABA-A receptor, what is the effect?

A

Increased chloride conduction, hyperpolarization of neuron

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12
Q

There were 2 examples of GABA antagonists provided. What were they? Which is competitive/non-competitive? What is the effect of their activity on the entire organism?

A

-Bicuculine - competitive-Picrotoxin - Non-competitive-Convulsions

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13
Q

There was a single example of an inverse agonist at the GABA-A receptor provided. -What is it? -Why is it relevant? -What is its mechanism? -Any therapeutic use?

A

-Beta-carbolines-Endogenous beta carbolines cause pathological anxiety-Reduces chloride conductance-No therapeutic use

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14
Q

What is the example of an antagonist that can block agonists at both the benzodiezapine activity at GABA-A receptors?

A

Flumenazil

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15
Q

How, mechanistically, do benzodiezapine enhance GABA conductance at the GABA-A receptor? What is their effect in the absence of GABA?

A

-Increase the FREQUENCY of channel opening in response to agonist-No effect in the absence of agonist

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16
Q

What are the 2 main CYP enzymes responsible for the metabolism of benzodiezapines?

A

CYP3A4CYP2C19

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17
Q

What is the active metabolite of diazepam? Alprazolam? Midazolam?

A

Diazepam - DesmethydiazepamAlprazolam and Midazolam - alpha hydroxy metabolites

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18
Q

Rank the following benzodiezapines in order of increasing half-life. Alprazolam, Diazepam, Lorazepam and Midazolam.

A

MidazolamAlprazolamLorazepamDiazepam

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19
Q

Of the following benzodiezapines, which is used as a preanesthetic medication? Anxiety? Insomnia? Muscle relaxant? Withdrawal?[Alprazolam, Diazepam, Lorazepam and Midazolam]

A

Preanesthetic - MidazolamInsomnia - Alprazolam, LorazepamAnxiety - Lorazepam, DiazepamMuscle relaxant - Diazepam, LorazepamWithdrawal - Diazepam

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20
Q

True or false, benzodiezapines have a high therapeutic index and overdose is not usually life threatening?

A

True, their major advantage over barbiturates

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21
Q

In addition to supporting BP and respiration, gastric lavage, how can you quickly reverse respiratory depression brought about by benzodiezapine overdose? How many treatments and why?

A

Flumenzil IVMultiple doses because flumenazil is short acting

22
Q

True or false, while abuse potential for benzodiezapines is low, physical and psychological dependence may still occur

A

True

23
Q

What are 2 ways by which withdrawal symptoms from benzodiezapines can be precipitated?

A

Stopping benzodiezapine useUse of antagonists

24
Q

True or false: benzodiezapines induce a lot of CYP enzymes therefore can produce several drug interactions

A

False. They don’t induce a lot of CYP enzymes

25
Q

What is the cause of a lot of the deaths associated with benzodiezapines use?

A

Mixing / co-ingesting with other CNS depressants (e.g alcohol)

26
Q

Zolpidem and zaleplon act at what receptor? What is their effect at this receptor? What is the enzyme responsible for their metabolism? What is their main use?

A

-GABA-A receptor-Increase frequency of channel opening (more chloride)-CYP3A4-Induce sleep

27
Q

Usually, zolpidem and zaleplon do not cause respiratory depression or cardiovascular depression. In what scenario is this not the case? (2)

A

IV administrationHeart failure patients (pt. with impaired cardiovascular function)

28
Q

What are 3 major disadvantages of barbiturates over benzodiezapines?

A
  • Respiratory depression- cardiovascular depression- Induction of CYP450 enzymes in liver (drug interactions)
29
Q

What are the 3 main brain areas targeted by barbiturates? What receptor do they bind?

A

Pons, medulla and cortexGABA-A complex (Pons + medulla = reticular formation)

30
Q

What is the mechanism by which barbiturates enhance chloride conductance by GABA-A receptor? What is their action in the absence of GABA?

A

Increase the open time (vs. frequency) of channelAt high doses, can open channel in absence of GABA

31
Q

Arrange the following barbiturates in order of increasing halflife. Pentobarbital, thiopental, phenobarbital and amobarbital. What are they used for?

A

Thiopental - Anesthesia inductionAmobarbital - Preoperative sedationPento - Preoperative sedationPheno - Anticonvulsant

32
Q

Drowsiness, confusion, diminished motor skills and impaired judgment. These are all side effects of _

A

Barbiturates

33
Q

What are the 2 major contraindications of barbiturates?

A

PainPulmonary insufficiency

34
Q

Barbiturates enhance the CNS depressive effects of 3 types of drugs. They are _

A

AntipsychoticsAntihistaminesEthanol

35
Q

True or false, barbiturates have a high therapeutic index and overdose is not usually life threatening?

A

False. Only 10X hypnotic does is enough to cause life threatening respiratory depression, circulatory collapse, renal failure and pulmonary complications

36
Q

How can you treat barbiturate poisoning? (2)

A

Support respiration and BPGastric lavage (activated charcoal, sorbitol)

37
Q

What are 2 types of tolerance that occur with barbiturate use? How long does it take to occur?

A

-Metabolic (increased CYP metabolizing enzymes)-Pharmacodynamic (decreased CNS response)

38
Q

True or false: Physical dependence and cross tolerance develops with continued use of barbiturates

A

True

39
Q

What are 2 other non-benzodiazapine, non-barbiturate antianxiety drugs discussed? What are their target receptors and actions at these receptors?

A

Propranolol - Beta-adrenoreceptor blockerBuspirone - Partial 5HT-1A agonist

40
Q

What enzyme metabolizes buspirone? How does it interact with alcohol? How long does it take to cause its effects? What is the risk of dependence developing?

A

CYP3A4No additive effects with ethanol1-3 weeks before effects are observedNo physical dependence develops

41
Q

Sedation and amnesia for surgery, epilepsy and seizure, control of alcohol withdrawal, muscle relaxation, insomnia. These can all be treated by _ class of drugs.

A

Sedative hypnotics

42
Q

Regardining benzodiazepines, what is the pharmacodynamic mechanism by which tolerance occurs? Does tolerance to benzos result in tolerance to other CNS depressants?

A
  • Tolerance occurs by down regulation of CNS response - Cross tolerance occurs to other benzos and CNS depressants
43
Q

True or false. anxiety, insomnia, irritability, bad dreams, tremors and anorexia are severe symptoms associated with benzodiazepine withdrawal.

A

False. These are considered mild symptoms

44
Q

True or false. agitation, depression, panic, paranoia, muscle twitches and convulsions are considered mild symptoms of benzodiezapine withdrawal

A

False, these are considered severe symptoms

45
Q

Why are barbiturates notorious for causing drug-drug interactions?

A

Barbiturates induce the activity and/or expression ofmany CYPs.

46
Q

How are barbiturates metabolized (2 actions)? How are they excreted?

A

Dealkylated and glucuronidation Renal excretion

47
Q

How are the following drugs related to barbiturates? Beta-blockers, Ca2+ channel blockers, corticosteroids,estrogens, phenothiazines, valproic acid and theophylline

A

Their metabolisms are all enhanced by barbiturates

48
Q

Severe respiratory depression, coma, severe hypotension and hypothermia. These are all signs of _

A

Acute barbiturate toxicity

49
Q

True or false: Anxiety, insomnia, dizziness and nausea are considered mild symptoms of barbiturate withdrawal?

A

True

50
Q

True or False: vomiting, hyperthermia, tremors,delirium, convulsions and death are considered serious symptoms of barbiturate withdrawal

A

True

51
Q

Does buspirone produce CNS depression? Does it produce rebound anxiety or withdrawal signs? What is it used to treat?

A

No NoAnxiety

2 Pharm Unit (17 decks)

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