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neurology FA > opioid analgesics / Benzodiazepines / Barbiturates / Nonbenzodiazepine hypnotics > Flashcards

opioid analgesics / Benzodiazepines / Barbiturates / Nonbenzodiazepine hypnotics Flashcards

1
Q

opioid analgesics - drugs

A
  1. Morphine 2. fentanyl 3. codeine
  2. lorepamide 5. methadone
  3. meperidine 7. dextromethorphan
  4. diphenoxylate 9. pentazocine
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2
Q

opioid receptors

A

μ=morphine, δ=enkephalin, κ=dynorphin

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3
Q

opioid analgesics - mechanism of action

A

act as agonists at opioid receptors to modulate synaptic transmission –> open K+ channels, close Ca2+ channels –> decrease synaptic transmission. Inhibit release of Ach, norepinephrine, 5-HT, glutamate, substance P

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4
Q

opioid analgesics - Inhibit release of

A

Ach, norepinephrine, 5-HT, glutamate, substance P

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5
Q

opioid analgesics - clinical use (and which drugs, if specific)

A
  1. pain controle 2. cough suppressor (dextromethorphan)
  2. diarrhea (loperamide, diphenoxylate)
  3. acute pulmonary edema
  4. maintenance programs for heroin addicts (methadone, buprenorphine + naloxone)
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6
Q

maintenance programs for heroin addicts - drugs

A

methadone, buprenorphine + naloxone

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7
Q

opioid analgesics - toxicity

A
  1. addiction
  2. respiratory depression
  3. constipation (no tolerance)
  4. miosis (pinpoint pupils) (no tolerance) (except meperidine –> mydriasis)
  5. addictive CNS depression with other drugs
  6. opioid withdrawal syndrome
  7. suppressed gag reflex
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8
Q

opioid analgesics - toxicity - tolerance does not develop to

A

miosis and constipation

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9
Q

opioid analgesics toxicity treated with

A

opioid receptor antagonists (naloxone or natrexone)

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10
Q

buprenorphine - mechanism of action

A
  • agonistic effects at μ δ opioid receptors

- antagonist effect at κ opioid receptors

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11
Q

butorphanol - mechanism of action

A
  • κ-opioid receptor agonist

- μ-opioid receptor partial agonist

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12
Q

butorphanol - clinical use

A

severe pain (migraine, labor)

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13
Q

butorphanol vs full opioids agonists according to side effects

A

butorphenol causes less respiratory depression than full opioid agonists

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14
Q

butorphanol - toxicity

A
  • can cause opioid withdrawal symptoms if patient is also taking full opiod agoinsts (competition for opioid receptor)
  • overdose not easily reversed with naloxone
  • less respiratory depression than full opioid agonists
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15
Q

butorphenol - antidote

A

overdose not easily reversed with naloxone

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16
Q

tramadol - mechanism of action

A

very weak opioid agonist

also inhibits 5-HT and norepinephrine reuptake

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17
Q

tramadol - clinical use

A

chronic pain

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18
Q

tramadol toxicity

A
  1. similar to opioid
  2. decreases seizure threshold
  3. serotonin syndrome
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19
Q

dextromethorphan + seretonergic agents –>

A

seretonin syndrome

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20
Q

barbiturates - drugs

A

(-BARBITAL + THIOPENTAL)

  1. phenobarbital
  2. pentobarbital
  3. secobarbital
  4. thiopental
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21
Q

barbiturates - mechanism of action

A

facilitate GABA A by increase DURATION of Cl- channel opening, thus decrease neuron firing

22
Q

barbiturates - contraindicated during

A
  1. porphyria 2. pregnancy
  2. liver disease 4. alcohol
  3. benzodiazepines
  4. CNS depression
23
Q

barbiturates - clinical use

A

sedative for ANXIETY, SEIZURES, INSOMNIA

induction of anesthesia (thiopental)

24
Q

barbiturates - induction of anesthesia - drugs?

A

thiopental

25
Q

barbiturates - toxicity

A
  1. respiratory and cardiovascular depression (can be fatal)
  2. CNS depression (can be exacerbated by alcohol use)
  3. dependence
  4. induces of P-450
  5. withdrawal syndrome
  6. teratogen
26
Q

barbiturates - overdose treatment

A
  1. mechanical respiration
  2. hemodialysis
  3. urine alkalinization
  4. maintain BP
27
Q

benzodiazepines - drugs

A
  1. diazepam 2. lorazepam 3. triazolam 4. oxazepam

5. midazolam 6. chlordiazepoxide 7. alprazolam 8. Temazepam

28
Q

benzodiazepines - mechanism

A

facilitate GABA - A action by increase FREQUENCY of CL- channel opening

29
Q

Most benzodiazepines have … half lives and … metabolites

A

long
active
(NOT THOSE WITH SHORT HALF LIVES)

30
Q

benzodiazepines with short half lives

A
  1. alprazolam
  2. Triazolam
  3. oxazepam
  4. Midazolam
31
Q

benzodiazepines with short half lives - characteristic

A

higher addictive potential

32
Q

substances that bind GABA-A receptor (ligant-gated Cl- channel)

A
  1. benzodiazepines
  2. barbiturates
  3. alcohol
33
Q

benzodiazepines - clinical use

A
  1. anxiety
  2. spasticity
  3. status epilepticus (lorazepam, diazepam)
  4. hypnotic (insmonia)
  5. general anesthetics (amnesia, muscle relaxation)
  6. night terrors
  7. sleepwalking
  8. detoxification (especially alcohol withdrawal - delirium tremens)
  9. ECLAMPSIA
34
Q

benzodiazepines - side effects

A
  1. dependence
  2. addictive CNS depression effects with alcohol
  3. respiratory deppresion less and coma (less risk that barbiturates)
35
Q

benzodiazepines vs barbiturates according side effects

A

benzodiazepines have less respiratory deppresion less and coma risk

36
Q

benzodiazepines - overdose treatment

A

flumazenil (comptetitive antagonist at GABA benzodiazepine receptor)

37
Q

flumazenil - mechanism of action and clinical use / side effects

A
  • comptetitive antagonist at GABA benzodiazepine receptor
  • treat benzodiazepines overdose
  • can precipitate seizures by causing acute benzodiazepine withdrawal
38
Q

Nonbenzodiazepine hypnotics - drugs

A
  1. Zolpidem
  2. Zaleplon
  3. Eszopiclone
39
Q

Nonbenzodiazepine hypnotics - mechanism of action

A

act via the BZ1 subtype of the GABA receptor

40
Q

Nonbenzodiazepine hypnotics - reverse by

A

flumazenil

41
Q

Nonbenzodiazepine hypnotics - clinical use

42
Q

benzodiazepines - useful as general anesthetics because

A
  1. amnesia

2. muscle relaxation

43
Q

Nonbenzodiazepine hypnotics - side effects

A
  1. ataxia 2. headaches 3. confusion
  2. dependency (less risk than benzodiazepines)
  3. modest day-after psychomotor depression and few amnestic effects
  4. short because of rapid metabolism by liver enzyme
44
Q

Nonbenzodiazepine hypnotics vs benzodiazepines according side effects

A
  1. Nonbenzodiazepine hypnotics have less risk than benzodiazepines for dependency
  2. sleep cycle is less affected
45
Q

Nonbenzodiazepine hypnotics - duration (why)

A

short because of rapid metabolism by liver enzyme

46
Q

Nonbenzodiazepine hypnotics vs older sedative hypnotics

A

Nonbenzodiazepine hypnotics cause only modest day-after psychomotor depression and few amnestic effects

47
Q

overdose treatment of 1. opioids 2. benzodiazepines 3. barbiturates

A
  1. opioids –> naloxone, naltrexone
  2. benzodiazepines –> flumazenil
  3. mechanical respiration, hemodialysis, urine alkalinizationm maintain BP
48
Q

Barbiturates vs benzodiazepines according to mechanism of action on GABA - A

A

Barbiturates –> increase the DURATION of Cl- opening

Benzodiazepines –> increase the FREQUENCY of Cl- opening

49
Q

Pentazocine - mechanism

A
  • κ-opioid receptor agonist

- μ-opioid receptor antagonist

50
Q

Pentazocine - clinical use

A

analgesia for moderate pain

51
Q

Pentazocine - adverse effects

A

opioid withdrawal symptoms if patient is also taking full opioid antagonist (competition for opioid receptor)

neurology FA (31 decks)

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