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IC Part 2 > Anxiety and Sleep > Flashcards

Anxiety and Sleep Flashcards

1
Q

Sedative

A

decreases motor activity, coordination and mental acuity

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2
Q

Hypnotic

A

increases tendency to sleep from which pt easily awakened

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3
Q

Anesthetic

A

induces sleep from which pt is not easily awakened

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4
Q

Most anxiolytic/hypnotics are CNS ____

A

depressants that enhance inhibitory neurotransmission

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5
Q

Barbiturates

A

Bind to the GABAa receptor on the barbiturate binding site

-Inc chloride ion channel flux by increasing channel open time (hyperpolarize cells- decrease neuronal activity)

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6
Q

Complete depressants

A

Produce anesthesia, coma and death with increasing dose

-Include barbiturates, ethanol

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7
Q

Incomplete depressants

A

Typically do not produce anesthesia and will not induce coma or death alone
-non benzodiazepine BZ receptor agonist, benzos

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8
Q

GABAa receptor

A

GABA is primary inhibitor neurotransmitter

Pentameric ion channel coupled receptor

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9
Q

Effects of Barbiturates on organ systems

A
  • CNS- complete CNS depressants with paradoxical excitement and euphoria
  • Resp and CV- at anesthetic doses decreases respiration and bp
  • Liver- induces expression of microsomal enzymes resulting in inc activity–> pharmacokinetic tolerance and dec plasma levels of other drugs
  • Inc porphyrin synthesis which can aggravate porphyria
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10
Q

Toxicity of Barbiturates

A

Overdose or interaction with other CNS depressants- dec in resp and bp, loss of consciousness
- no specific antagonist

Chronic will lead to tolerance (kinetic and dynamic)

  • Addiction, withdrawal (anxiety, tremor, seizures, hyperthermia, cv collapse– can be fatal; cell is working normally with dose of drug, w/o drug will lead to opposite of what the drug was doing)
  • tx: measured reduction over time (tx seizures and anxiety with benzos)
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11
Q

Barbiturates and their uses

A 
Phenobarbital (long acting)
Pentobarbital (med acting)
Secobarbital (med acting)
Methohexital (iv)
Amobarbital (iv)
Thiopental (iv)

-sedative, hypnotics, anticonvulsants, drug induced coma, preanesthetic, anesthetics, WADA test (map language and memory fxns), narcoanalysis (truth serum), euthanasia/lethal injection (vet practice, capital punishment)

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12
Q

Pharmacokinetics of barbs

A
  • readily diffuses across all membranes
  • distributes throughout body depending on lipophilicity
  • crosses placenta (fetal addition)
  • Highly protein bound- drug interactions
  • metabolized in liver
  • excreted in urine
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13
Q

Benzodiazepines MOA

A

Bind to benzodiazepne binding sites (BZ) on GABAa receptor (allosteric activator)

  • inc affinity of GABAa receptors for GABA, which increases likelihood of channel opening
  • Act on smaller subset of GABAa receptors than barbs due to diff expression of subunits that make up pentamer (BZ1, BZ2, BZ3)
  • various receptor subunits can lead to diff binding sites and as well as phamacokinetic differences
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14
Q

Effect of benzos on organ systems

A

-of Diazepam
CNS- incomplete depressant, dec anxiety, skeletal muscle relaxant, anticonvulsant, hypnotic
-paradoxical excitement and euphoria
-Tolerance- sedative, hypnotic, anticonvulsant actions
-No sig effects on respiratory, CV, and GI systems

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15
Q

Side effects and toxicities of benzos

A

(diazepam)

  • Sedation and ataxia
  • Amnesia (esp midazolam)
  • Nightmares, irritability, anxiety, seizures
  • Overdose tx with flumazenil (reverses sedation)
  • Withdrawal with shorter acting drugs (rebound anxiety with alprazolam) –> anxiety, irritability, insomnia, nausea, vomiting, tremor, sweating, anorexia, confusion, psychosis, seizures
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16
Q

Short acting benzos

A

2-4 hrs
Midazolam- rapidly inactivated, iv anesthesia

Triazolam- hypnotic

17
Q

Mod acting benzos

A

10-14 hrs
Alprazolam- anxiolytic/ hypnotic, panic attacks; rapid oral absorption/onset
Chlordiazepoxide- anxiolytic, pre-anesthetic
Lorazepam- anxiolytic/hypnotic, pre-anesthetic

18
Q

Long acting benzos

A

24 hrs

Clonazepam- anticonvulsant

19
Q

Very long acting (active metabolites) benzos

A

Diazepam- anxiolytic, anticonvulsant, muscle relaxant, antispastic, pre-anesthetic (43 hr 1/2 life)

Flurazepam (1/2 life 72 hrs)

20
Q

Other benzos

A

Flunitrazepam- fast acting, “Date rape”, amnestic, no therapeutics

21
Q

Flumazenil

A

reverses overdose and anesthesia from benzos

-short 1/2 life

22
Q

Pharmacokinetics of benzos

A

rapidly absorbed from GI
most administered orally but some from IV or IM (diazepam, lorazepam, midazolam)
highly protein bound, however, few drug interactions
crosses placenta
numerous active metabolites (esp long acting)
metabolized in liver
excreted in urine

23
Q

Non benzo BZ receptor agonists

A

BZ1 agonists- zolpidem, zaleplon
Non selective agonists- eszopiclone

Hypnotic, short 1/2 life, minimal muscle relaxant or anticonvulsant activity, less amnestic than benzos, claimed to produce less tolerance to hypnotic effects than benzos

24
Q

SE of non benzo BZ receptor agonists

A

-Abnormal thinking/behavior (sleepwalking, raiding refrigerator, amnesia, hallucinations)

25
Q

Buspirone

A
  • Nondepressant anxiolytics
  • Partial agonist at 5-HT1a site
  • Slow onset of action 1-2 weeks
  • Dysphoric at high doses
26
Q

SSRIs and other antidepressants

A

non-depressant anxiolytic
inc synaptic availability of 5-HT
-used for generalized anxiety and as prophylaxis for panic disorder

27
Q

Hydroxyzine

A

non-depressant anxiolytic

  • H1 blocker
  • Used pre and post op
  • antipruritic and anti-emetic
28
Q

Melatonin agonist

A

Ramelteon

  • nondepressant drug for insomnia
  • indicated for insomnia with prolongd sleep onset
  • MT1 and MT2 melatonin receptor agonist
29
Q

Orexin antagonist

A

Suvorexant

-indicated for diff with sleep onset and/or sleep maintenance

30
Q

Antihistamines

A

Diphenhydramine
H1 blocker
OTC sedative

31
Q

Trazodone

A

-non depressant drug for insomnia
Blocks 5-HT reuptake, H1 and a1 receptors
antidepressant, but also sedating so it’s used as a hypnotic

IC Part 2 (27 decks)

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