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

(-BARBITAL + THIOPENTAL) 1. phenobarbital 2. pentobarbital 3. secobarbital 4. thiopental

opioid analgesics / Benzodiazepines / Barbiturates / Nonbenzodiazepine hypnotics Flashcards by Anthos Christofides

opioid analgesics - drugs

Morphine 2. fentanyl 3. codeine
lorepamide 5. methadone
meperidine 7. dextromethorphan
diphenoxylate 9. pentazocine

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opioid receptors

μ=morphine, δ=enkephalin, κ=dynorphin

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opioid analgesics - mechanism of action

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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opioid analgesics - Inhibit release of

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

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

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

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maintenance programs for heroin addicts - drugs

methadone, buprenorphine + naloxone

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opioid analgesics - toxicity

addiction
respiratory depression
constipation (no tolerance)
miosis (pinpoint pupils) (no tolerance) (except meperidine –> mydriasis)
addictive CNS depression with other drugs
opioid withdrawal syndrome
suppressed gag reflex

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opioid analgesics - toxicity - tolerance does not develop to

miosis and constipation

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opioid analgesics toxicity treated with

opioid receptor antagonists (naloxone or natrexone)

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buprenorphine - mechanism of action

agonistic effects at μ δ opioid receptors

- antagonist effect at κ opioid receptors

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butorphanol - mechanism of action

κ-opioid receptor agonist

- μ-opioid receptor partial agonist

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butorphanol - clinical use

severe pain (migraine, labor)

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butorphanol vs full opioids agonists according to side effects

butorphenol causes less respiratory depression than full opioid agonists

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butorphanol - toxicity

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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butorphenol - antidote

overdose not easily reversed with naloxone

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tramadol - mechanism of action

very weak opioid agonist

also inhibits 5-HT and norepinephrine reuptake

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tramadol - clinical use

chronic pain

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tramadol toxicity

similar to opioid
decreases seizure threshold
serotonin syndrome

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dextromethorphan + seretonergic agents –>

seretonin syndrome

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barbiturates - drugs

(-BARBITAL + THIOPENTAL)

phenobarbital
pentobarbital
secobarbital
thiopental

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barbiturates - mechanism of action

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

barbiturates - contraindicated during

porphyria 2. pregnancy
liver disease 4. alcohol
benzodiazepines
CNS depression

barbiturates - clinical use

sedative for ANXIETY, SEIZURES, INSOMNIA

induction of anesthesia (thiopental)

barbiturates - induction of anesthesia - drugs?

thiopental

barbiturates - toxicity

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

barbiturates - overdose treatment

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

benzodiazepines - drugs

1. diazepam 2. lorazepam 3. triazolam 4. oxazepam | 5. midazolam 6. chlordiazepoxide 7. alprazolam 8. Temazepam

benzodiazepines - mechanism

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

Most benzodiazepines have ... half lives and ... metabolites

long active (NOT THOSE WITH SHORT HALF LIVES)

benzodiazepines with short half lives

1. alprazolam 2. Triazolam 3. oxazepam 4. Midazolam

benzodiazepines with short half lives - characteristic

higher addictive potential

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

1. benzodiazepines 2. barbiturates 3. alcohol

benzodiazepines - clinical use

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

benzodiazepines - side effects

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

benzodiazepines vs barbiturates according side effects

benzodiazepines have less respiratory deppresion less and coma risk

benzodiazepines - overdose treatment

flumazenil (comptetitive antagonist at GABA benzodiazepine receptor)

flumazenil - mechanism of action and clinical use / side effects

- comptetitive antagonist at GABA benzodiazepine receptor - treat benzodiazepines overdose - can precipitate seizures by causing acute benzodiazepine withdrawal

Nonbenzodiazepine hypnotics - drugs

1. Zolpidem 2. Zaleplon 3. Eszopiclone

Nonbenzodiazepine hypnotics - mechanism of action

act via the BZ1 subtype of the GABA receptor

Nonbenzodiazepine hypnotics - reverse by

flumazenil

Nonbenzodiazepine hypnotics - clinical use

insomnia

benzodiazepines - useful as general anesthetics because

1. amnesia | 2. muscle relaxation

Nonbenzodiazepine hypnotics - side effects

1. ataxia 2. headaches 3. confusion 4. dependency (less risk than benzodiazepines) 5. modest day-after psychomotor depression and few amnestic effects 6. short because of rapid metabolism by liver enzyme

Nonbenzodiazepine hypnotics vs benzodiazepines according side effects

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

Nonbenzodiazepine hypnotics - duration (why)

short because of rapid metabolism by liver enzyme

Nonbenzodiazepine hypnotics vs older sedative hypnotics

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

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

1. opioids --> naloxone, naltrexone 2. benzodiazepines --> flumazenil 3. mechanical respiration, hemodialysis, urine alkalinizationm maintain BP

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

Barbiturates --> increase the DURATION of Cl- opening | Benzodiazepines --> increase the FREQUENCY of Cl- opening

Pentazocine - mechanism

- κ-opioid receptor agonist | - μ-opioid receptor antagonist

Pentazocine - clinical use

analgesia for moderate pain

Pentazocine - adverse effects

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