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Pharmacology > EXAM #3: SEDATIVES > Flashcards

EXAM #3: SEDATIVES Flashcards

1
Q

What is the definition of CNS depression?

A

Decreased neuronal excitability

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2
Q

What are CNS depressants generally used to treat?

A

1) Anxiety states

2) Sleep disorders

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3
Q

List the categories of selective CNS depressants.

A

Benzodiazepines
Barbiturates
Ethanol

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4
Q

List the categories of non-selective/ general CNS depressants.

A

Antihistamines

Opoid analgesics

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5
Q

What is the effect of sedative anxiolytics?

A

Exertion of a calming effect and relief of anxiety

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6
Q

What is the effect of hyponotics?

A

Production of drowsiness

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7
Q

What are the graded dose-dependent effects of the sedative hypnotics?

A

1) Sedation
2) Sleep
3) Anesthesia
4) Coma
5) Respiratory depression/ death

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8
Q

What is a linear slope sedative-hypnotic? Non-linear? Which is safer?

A

Linear= higher dose leads to increased dose-dependent effects

Non-linear= plateau in dose-dependent effects*

Non-linear are SAFER

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9
Q

What are the indications for sedative-hypnotics (6)?

A

1) Anxiety
2) Insomnia
3) Amnesia
4) Seizures
5) Ethanol withdrawal
6) Muscle relaxation

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10
Q

What suffix is associated with the benzodiazepines?

A
  • “zepam”

- “zolam”

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11
Q

What are the three main pathways of benzodiazepine metabolism?

A

1) Inactive water-soluble glucuronides
2) Weakly active short-lived metabolites
3) Long-lived and active metabolites

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12
Q

What benzodiazepines undergo metabolism to inactive water-soluble glucuronides? What is the half-life/ duration of action?

A

Lorazepam
Oxazepam

Short acting

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13
Q

What benzodiazepines undergo metabolism to weakly active, short-lived metabolites? What is the half-life/ duration of action?

A

Alprazolam
Triazolam

Intermediate-acting

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14
Q

What role does age play in the metabolism of benzodiazepines?

A

Hepatic processing SLOWS in the elderly and INCREASES the half-life

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15
Q

What is the general mechanism of action of the benzodiazepines?

A
  • Bind GABA-A ion channel (Cl-) at specific binding site increasing opening of GABA channels
  • Increased Cl- enters the neuron and is INHIBITORY/ causes HYPERPOLARZIATION
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16
Q

What is Alpha-1 GABA agonism associated with?

A

Sedation
Anti-seizure
Anterograde amnesia

17
Q

What is Alpha 2,3,5 GABA agonism associated with?

A

Anxiolysis

18
Q

What are the adverse effects of the benzodiazepines?

A

1) Respiratory depressant
2) Anterograde amnesia
3) Tolerance
4) Dependence
5) Withdrawal

19
Q

What increases the adverse effects of benzodiazepines?

A

Use with other CNS depressant

20
Q

What drug is strongly associated with anterograde amnesia and is used as a date-rape drug?

A

Flunitrazepam i.e. Rohypnol/ roofies

21
Q

What drugs when combined with benzodiazepines will cause additive CNS depression?

A 
Ethanol 
Opoids 
Anti-consulsants 
Phenothiazine 
Anti-histamines
Tricyclic antidepressants
22
Q

What is the common name for flumazenil? Why is this drug important?

A

Romazicon

Can reverse the adverse effects of benzodiazepine overdose*

23
Q

What is the mechanism of action of Flumazenil?

A

Competitive inhibitor of benzodiazepines

24
Q

What are the “z-drug” benzodiazepine related drugs?

A

Newer sedative agents used to treat insomnia

25
Q

What is the mechanism of action of z-drugs?

A

Agonism of benzodiazepine receptors on GABA-A receptors

26
Q

What are the clinical uses for Barbiturates?

A

1) Anesthesia
2) Sedative/hypnotic
3) Anticonvulsant
4) Medically induced coma

27
Q

What is the important clinical difference between benzodiazepines and barbiturates?

A

Barbiturates follow a linear slope and are much less safe

28
Q

What is the mechanism of action of barbiturates? How does this differ from the benzodiazepines?

A

Barbiturates= increased the duration GABA channel opening

Benzodiazepines increase the frequency of GABA channel opening

29
Q

What is the mechanism of action of Ramelteon?

A

Melatonin receptor agonist

30
Q

What is the clinical use of Ramelteon?

A

Insomnia– especially for people that have difficulty falling asleep

31
Q

What is the mechanism of action of Buspirone?

A

Partial agonist of 5-HT1a receptors (autoreceptors)

  • Decreases 5-HT release
  • Decreases neuronal excitability
32
Q

What is unique about Buspirone?

A

NON-SEDATING anxiolytic (long-term/ maintenance)

  • Less psychomotor impairment
  • Does NOT affect driving skills
33
Q

Where are 5-HT1a receptors located?

A

Located on the pre-synaptic terminal and INHIBIT release of the NT from the pre-synaptic membrane

34
Q

What is classification 5-HT1a receptors?

A

Autoreceptors

35
Q

What Beta-Blocker is used to treat anxiety?

A

Propranolol

36
Q

What facets of anxiety is propranolol treating?

A

Somatic manifestations of anxiety

37
Q

What antihistamines have a mild sedative effect?

A

Hydroxyzine

Diphenhydramine

38
Q

What is the oldest ad most commonly used anxiolytic?

A

Ethanol

Pharmacology (64 decks)

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