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33 Cards in this Set
- Front
- Back
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Sedative-hypnotics
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Sedative - reduces excitatory responsiveness to external stimuli, calming effect
Hypnotic - causes drowsiness and sleep Are anxiolytic |
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GABAa receptor drugs
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GABA, barbiturates, benzodiazepines, alcohol
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GABAa binding sites
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BDZ1
BDZ2 gamma subunit required for benzos to exert effects |
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GABAa channel opening
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Benzos - channel opens more frequently
Barbiturates and anesthetics - channel opens for longer durations |
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Penicillin at GABA
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high doses (esp with renal impairment) block the open channel activated by GABA = UNCOMPETITIVE INHIBITION... requires activation of receptors or enzymes before they can inhibit
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Benzodiazepines
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ZOLAM or ZEPAM
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Anxiety or aggression
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_ZEPAM
site of action - GABA receptors in the limbic system (hippo, amygdala) |
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Severe anxiety with strong autonomic overactivity - Panic attacks
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Alprazolam or Clonazepam for immediate relief + other drugs for prevention (SSRIs)
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Insomnia
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Flurazepam, Temazepam
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Anticonvulsants
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Diazepam, lrazepam, Clonazepam for seizures, ex. status epilepticus
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Muscle spasms
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Diazepam - inhibits synaptic pathways in spinal cord
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Benzo unwanted effects
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Anterograde amnesia (all)
Breakthrough panic attacks (w short-acting agents) Tolerance - several months, withdrawal symptoms |
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Metabolism of Benzos
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Phase 1 - can give active metabolites
Phase 2 - glucuronide conjugation, INACTIVE Excreted in urine |
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Benzos for elderly
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Give those without active metabolites:
Lorazepam Oxazepam Temazepam (LorOxTEm) |
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Flumazenil (Romazicon)
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Benzodiazepine antagonist - be cautious of precipitating seizures
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Alprazolam (Xanax)
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Treat panic disorders
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Midazolam (versed)
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Parenteral med for sedation prior to anesthesia. Large incidence of anterograde amnesia
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Triazolam (Halcion)
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Can produce severe anterograde amnesia, paradoxical agitation and aggression
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Flunitrazepam
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Street drug
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Omega-1/BDZ1 Agonists
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Zaleplon (Sonata)
Zolpidem (Ambien) Escopliclone (Lunesta) "ZAZOLES" |
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Ethanol
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interactions with benzos - synergistic, can cause severe life threatening respiratory depression of medullary respiratory center
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Benzos for Ethanol Withdrawal
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Use long-acting benzo to taper (Diazepam)
Short acting drugs like lorazepam and oxazepam are useful with liver disease |
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Barbituate effects
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Sedative-hypnotics with potential for anesthesia, coma, death
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Phenobarbital
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Treat seizures in children
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Thiopental
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IV induction of anesthesia
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Metabolism of Barbituates
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Induce CYPs - can increase their own metabolism as well as that of other drugs
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Benzos selective for SLEEP
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GABAa receptors with alpha1 (and gamma) subunits - ventrolateral preoptic nucleus (VLPO) sends projections to inhibit arousal pathways
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non-selective benzos
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1) induce sleep
2) decrease number of awakenings 3) increase duration of stages 1 and 2 BUT 4) DECREASE Stages 3, 4, and REM sleep |
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Scopolamine and sleep
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Anti-muscarinic
decrease sleep latency, decrease # of awakenings, increase slow wave sleep, decrease REM sleep |
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Diphenhydramine, promethazine, other sedating anti-histamines effects on sleep
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decrease sleep latency, decrease # of awakenings, increase slow wave sleep, decrease REM sleep
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Ethanol effects on sleep
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Complicated, similar to scopolamine,
2/3 - ethanol is helpful hypnotic Normalization of sleep occurs in insomniacs Suppression of REM, increase in slow waave sleep, variable effects on latency and # of awakenings |
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Ramelteon
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Agonist on MT1 and MT2 melatonin receptors
17x more potent than melatonin Metabolism by CYP1A2 Adverse effects - dizziness, fatigue, endocrine disorders |
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MT1
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sleep onset, general sleepiness
inhibitory signal transduction motifs 17x more potent than melatonin |
