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Pharmacology > Sedative-Hypnotics > Flashcards

Sedative-Hypnotics Flashcards

1
Q

What are the sedatives that target GABA-A receptors?

A
  • Benzodiazepines
  • Non-benzodiazepine Agonists
  • Barbiturates
  • Ethanol
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2
Q

GABA-A Receptors

A

Ionotropic receptors that cause Cl- channels to open leading to inhibitory synaptic potentials

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3
Q

GABA-B Receptors

A

Metabotropic G-protein linked receptors that act on presynaptic terminals and regulate the release of GABA or other NTs

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4
Q

What is the most abundant GABA-A configuration?

A

2-alpha
2-beta
1-gamma

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5
Q

What is the binding site on GABA-A for GABA?

A

Alpha/beta interface - normally 2 sites

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6
Q

What is the binding site on GABA-A for benzodiazepines, imidazopyridines and pyrrolopyrazines?

A

Alpha/gamma interface

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7
Q

What are the BZ1 selective class of drugs?

A

Non-benzodiazepines

  • Imidazopyridines
  • Pyrrolopyrazines
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8
Q

Benzodiazepine MOA

A

Binding of the drug acts as a positive allosteric regulator that increases GABA affinity for GABA-A receptor and increases the frequency of Cl- channel opening - more inhibitory signal

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9
Q

Where do the barbiturates bind?

A

Bind to parts of GABA-A separate from BZ sites and lead to increased DURATION of Cl- channel opening rather than frequency

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10
Q

What suffices are indicative of benzodiazepines?

A
  • AM
  • PAM
  • LAM
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11
Q

What are the indications for benzodiazepines?

A
  • Anxiety
  • Sleep disorders
  • Anticonvulsant
  • Treatment for EtOH withdrawal
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12
Q

What are the contraindications of benzodiazepines?

A

Significant pulmonary illness or CNS depression

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13
Q

Benzodiazepines are highly _______.

A

Protein-bound

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14
Q

What happens to the half life of diazepam as the age of patients increases?

A

It will increase due to the decreased hepatic function

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15
Q

What are the benzodiazepines that go directly to phase II metabolism in the liver?

A

LOT
Lorazepam
Oxazepam
Temazepam

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16
Q

What are the benzodiazepines with the shortest half lives?

A

LOT
Lorazepam
Oxazepam
Temazepam

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17
Q

Benzodiazepine SE

A
  • Amnesia
  • Confusion
  • Dizziness
  • Allergic Reaction
  • Tolerance
  • Dependence
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18
Q

What is the tolerance that is developed to benzodiazepines?

A

Tolerance is only developed to the sedative effects, NOT the anti-anxiety effects

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19
Q

What are the imidazopyridines?

A

Zolpidem

Zaleplon

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20
Q

What are the pyrrolpyrazines?

A

Eszopiclone

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21
Q

Non-benzodiazepine MOA

A

Bind selectively to BZ1 and positively modulates GABA-A action

22
Q

Non-benzodiazepine SE

A
  • Similar to benzodiazepines
  • Sleep-driving/eating
  • Anterograde amnesia
23
Q

Which of the non-benzodiazepines has the longest half life?

A

Eszopiclone

24
Q

What are the barbituates?

A

Penobarbital
Methohexital
Thiopental

-AL suffix

25
Q

Barbituate MOA

A

Binds to GABA-A at distinct regions from BZ1/2 and increase duration of Cl- channel opening - at high doses they can directly open Cl- channels

26
Q

What are the short acting barbiturates?

A

Thiopental and Mexihexital

27
Q

What are the long acting barbiturates?

A

Phenobarbital

28
Q

Barbituate SE

A
  • Respiratory Depressant
  • Death from OD
  • Withdrawal
  • Tolerance due to CYP450 induction
29
Q

Ramelteon MOA

A

Melatonin agonist that binds MT1 and 2 receptors with higher affinity that melatonin - no BZ binding

30
Q

Ramelteon SE

A
  • Headache
  • Fatigue
  • Dizziness
31
Q

What is a major advantage of ramelteon?

A

No physical dependence or withdrawal symptoms

32
Q

Do benzodiazepines cure insomnia?

A

No, they will only resolve the symptoms for as long as they are taken.

33
Q

Valeriana officinalis - Herbal MOA

A

Mediate GABA release and inhibit its breakdown - can be used to treat insomnia for up to 4 weeks

34
Q

Chamomile - Herbal MOA

A

Benzodiazepine agonist

35
Q

Passion Flower - Herbal MOA

A

Benzodiazepine partial agonist

36
Q

Buspirone MOA

A

5-HT1A partial agonist

37
Q

Buspirone SE

A
  • Headaches
  • Dizziness
  • Sedation
38
Q

Buspirone Contraindications

A

DO NOT USE alongside a MAO-I

39
Q

Buspirone Indications

A
  • Major depression

- Anxiety disorders

40
Q

What are advantages of buspirone over benzodiazepines?

A
  • NO risk of dependence

- NO sexual dysfunction

41
Q

Sedative (Anxiolytic)

A

Reduces anxiety and exerts a calming effect

42
Q

Hypnotic

A

Produces drowsiness and facilitates the onset and maintenance of sleep

43
Q

Where is GABA synthesized?

A

Nucleus Accumbens

44
Q

Which GABA receptors do all sedatives act on?

A

GABA-A

45
Q

What drug classes does BZ1 bind?

A
  • Benzodiazepines
  • Imidazopyridines
  • Pyrrolopyrazines
46
Q

What drug classes does BZ2 bind?

A
  • Benzodiazepines
47
Q

Flumazenil MOA

A

Competitive antagonist of BZ1 and 2 site and blocks the actions of drugs that act at these sites

48
Q

Benzodiazepine Indications

A

Anxiety, Insomnia, Anesthesia, Alcohol Withdrawal, Seizures

49
Q

What are the benzodiazepines with long half lives?

A
  • Chlordiazepoxide
  • Diazepam
  • Flurazepam
50
Q

What is the metabolism of zaleplon inhibited by?

A

Cimetidine

Pharmacology (74 decks)

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