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NSP Final > Sedatives and Hypnotics > Flashcards

Sedatives and Hypnotics Flashcards

1
Q

what are the two prominent classes of drugs classified as sedative-hypnotics?

A

Benzodiazepine’s
Barbiturates

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2
Q

what is the arousal scale for BARBs and BZDs?

A
  • BARBs extend into the anesthesia-coma-death end (narrow TI)
  • BZDs only extent into the sedation and sleep portion making them safer and more widely used
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3
Q

where do benzodiazepine’s and Barbiturate’s bind?

A

GABA A receptor-ion channel complex found in the brain and allows chloride ions (Cl⁻) to enter the cell, which inhibits nerve activity

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4
Q

what are the three classes of GABA receptors?

A

GABA a, GABA b, GABA c

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5
Q

what two molecules block GABAs actions?

A

bicuculline: interferes with GABA binding
picrotoxin: blocks chloride channel

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6
Q

what are the agonists for benzodiazepine receptor?

A

triazolam
diazepam

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7
Q

what are the antagonists for benzodiazepine receptor?

A

flumazenil
diazepam binding inhibitor (DBI): endogenous peptide

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8
Q

what are the inverse agonists for benzodiazepine receptor?

A

beta-carbolines

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9
Q

what are beta-carbolines?

A

natural product of serotonin breakdown that oppose the calming effects of benzodiazepines and a natural anxiety-promoting substance

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10
Q

what are benzodiazepine’s used to treat?

A

anxiety
epilepsy
sedative-hypnotic needs

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11
Q

where is the most likely site for sedation and hypnotic action in the brain for benzodiazepine’s?

A

in the brainstem; reticular activating system

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12
Q

what is the mechanism of action for the benzodiazepine’s ?

A
  1. bind at different sites
  2. increase the frequency of chloride channel opening
  3. boost GABA effect (IPSP)
  4. enhance GABA action
  5. rely on the presence of GABA (do not mimic)
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13
Q

what are the adverse effects of the benzodiazepine’s?

A
  • have active metabolites
  • produce severe depression when combined with other drugs
  • retrograde amnesia
  • motor incoordination and ataxia
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14
Q

what are the general effects of the benzodiazepines?

A
  • minimal effect on respiration, cardiovascular system and GI system
  • lower abuse potentials than barbs
  • do not accelerate metabolism of other drugs
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15
Q

what is the mechanism of action for the Barbiturate’s ?

A
  1. bind at different sites
  2. increase duration of chloride channel openings
  3. increases duration of GABA effect (IPSP)
  4. release/block the reuptake of GABA
  5. GABA mimetic at high concentrations
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16
Q

what are the adverse effects of the Barbiturates?

A
  • produce anesthesia, coma and death
  • severe CNS depression when used with other depressants (alcohol, antihist, BZD)
  • induce liver microsomal enzymes (CYP P450)
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17
Q

what are the general effects of Barbiturates ?

A
  • do not have active metabolites
  • less selective CNS depression: affects excitatory synapses, cell membranes, GABA receptors
  • minimal cardiovascular effects
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18
Q

what drugs do Barbiturates increase the metabolism of?

A

anticoagulants
contraceptives
phenytoin
vitamin D
vitamin K
corticosteroids

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19
Q

what are the clinical uses for benzodiazepines?

A
  • sedative hypnotics
  • anti-anxiety
  • anti-epileptic
  • anti-depressant
  • anesthetic adjunct
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20
Q

what are the clinical uses for barbiturates ?

A
  • anti-epileptic
  • cerebral edema
  • short acting anesthetic
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21
Q

list the benzodiazepine’s

A

triazolam
oxazepam
chlordiazepoxide
temazepam
lorazepam
nitrazipam
diazepam
flurazepam

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22
Q

list the barbiturates

A

methohexital
thiopental
pentobarbital
secobarbital
amobarbital
phenobarbital

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23
Q

Alcohol is a CNS depressant that shares many pharmacologic properties with

A

the nonbenzodiazepine sedative hypnotics

24
Q

how is alcohol absorbed?

A

rapidly through the stomach, large and small intestines and the colon (30-90 min following ingestion)

25
how is alcohol distributed?
somewhat uniform but both the placenta and BBB are very permeable to alcohol
26
how is alcohol metabolized?
90-98% is oxidized to carbon dioxide and water through alcohol dehydrogenase or aldehyde dehydrogenase pathway
27
what are the three conditions that effect the rate of alcohol metabolism?
- body weight - drinking habits - genetics
28
what is the Microsomal Ethanol Oxidizing System?
alternative pathway for metabolizing ethanol (alcohol) in the liver that uses NADPH, especially important when large amounts of alcohol are consumed or in cases of chronic alcohol use
29
why is alcohol metabolism accelerated when taking barbiturates?
MEOS is induced by barbs
30
what acute CNS effects does alcohol have on the body?
- disruption of mood, thought, memory or function - effects sensory and motor systems - acts as sedative hypnotic - enhances GABA, acetylcholine and serotinergic transmitter systems - inhibits glutamate
31
what cardiovascular effects does alcohol have on the body?
cutaneous vasodilation
32
what GI tract effects does alcohol have on the body?
- gastric acid secretion is increased - direct irritant to gastric mucosa - increased GI bleeding
33
what liver effects does alcohol have on the body?
- fat production increases - protein accumulation - cirrhosis/liver failure
34
what are the drug interactions of alcohol and aspirin?
- anti-platelet action can cause increased GI bleeding - alcohol inhibits platelet aggregation
35
what are the drug interactions for alcohol and oral hypoglycemics ?
alcohol inhibits the metabolism of oral hypoglycemics (tolbutamide) taken by diabetics which causes stronger reduction of blood glucose due to alcohols effect of decreasing blood glucose levels
36
what is the function of Tolbutamide ?
stimulates insulin release
37
what are the characteristics of chronic alcoholism?
- weight loss, nutritional deficiencies, vitamin deficiencies - liver cirrhosis - GI irritant - Wernicke's Encephalopathy - personality changes - Korsakoff's psychosis - delirium treatments - heart failure
38
Disulfiram (Antabuse)
Inhibits Aldehyde Dehydrogenase (ALDH) which leads to accumulation of acetaldehyde when alcohol is consumed — so it's used as a negative reinforcement tool in treating alcohol dependence
39
Naltrexone (ReVia)
opioid receptor antagonist that blocks the brain’s opioid receptors, which are involved in the reward and pleasure pathway triggered by alcohol
40
Acamprosate (Campral)
blocks NMDA (glutamate) receptors, helping to regulate excitatory neurotransmission to restore chemical balance in the brain disrupted by chronic alcohol use
41
what are the types of insomnia?
transient short term long term
42
Transient Insomnia
triggered by minor, temporary stressors like upcoming exams, travel (jet lag), change in schedule or drug-induced (e.g., caffeine, stimulants) but typically resolves on its own once the trigger is gone
43
short term insomnia
Lasts a few weeks, caused by more significant stress or life events like job loss, grief, relationship issues and more persistent than transient
44
long term insomnia
Persists for months or longer, often has no clear or immediate cause but could be related to underlying psychiatric conditions
45
A good anti-insomnia drug should:
Reduce sleep latency Increase total sleep time
46
what are the 5 stages of sleep?
Stage 1: Light sleep — transition from wakefulness Stage 2: Slightly deeper sleep — still light Stage 3: Beginning of deep sleep (slow-wave sleep) Stage 4: Deepest non-REM sleep — important for physical restoration Stage 5: REM (Rapid Eye Movement) sleep — dreaming happens here, also called paradoxical sleep because the brain is active but the body is relaxed
47
what are the time frames of drug prescriptions for insomnia?
transient: small dose for 1-3 nights short term: small dose for 2-3 weeks long term: longer period of time but not exceeding 1 month
48
what are the commonly used hypnotics (BZDs)?
Triazolam (Halcion) Oxazepam (Serax) Temazepam (Restoril) Flurazepam (Dalmane)
49
what are other commonly used hypnotic agents?
Zolpidem (Ambien) Eszopiclone* (Lunesta) Amitriptyline Anti-histaminics (H1) Alcohol (ethanol) Melatonin
50
Triazolam (Halcion)
- short half-life; rapidly absorbed and eliminated (no morning left over sedation) - useful in the elderly (reduced drug metabolism) - more lipid soluble than oxazepam - less of a change in sleep patterns (REM and Stage 4) than flurazepam - recommended for use up to 42 days - rebound daytime anxiety and confusion
51
Oxazepam (Serax)
- short half life; slow onset of action - low lipid solubility/slow penetration into the brain
52
Temazepam (Restoril)
intermediate acting benzodiazepine
53
Flurazepam (Dalmane)
- decreases REM and sleep stage 3 & 4 - long duration of action - short term 14-28 days - morning-after-sedation-hangover effect due to the long half-life of this drug - problematic use in the elderly
54
Zolpidem (Ambien)
- binds to benzodiazepine receptor - is structurally unrelated to the benzodiazepines - has only minor effects on sleep stages - has no anxiolytic, anticonvulsant or muscle relaxant properties - peak activity in 1~2 hrs. (half life = 2.5 hrs) - as effective as a benzodiazepine for inducing sleep
55
Eszopiclone* (Lunesta)
- binds to benzodiazepine receptor - is structurally unrelated to the benzodiazepines - has no anxiolytic properties - peak activity in 1hr (half life = 6 hrs) - as effective as a benzodiazepine for inducing sleep * The only hypnotic FDA approved for a long-term use (more than 42 days)
56
Amitriptyline
a sedative and an antidepressant blocks the reuptake of 2 neurotransmitters (serotonin (5-HT) and norepinephrine)
57
Anti-histaminics (H1)
over-the-counter preparations cold remedies/anti-vertigo (seasickness), anti-allergic medications.

NSP Final (11 decks)

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