Pharm22 Sedative-Hypnotics

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Common side effect of hypnotic agents

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Sedation

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Occurs when sedative hypnotics are used chronically or at high doses

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tolerance

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The most common type of drug interaction of sedative hypnotics with out depressant medications

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Additive CNS Depression

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Benzodiazepines used to promote sleep

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Temazepam
Trizolam
Flurazepam

kaplan - oxazepam

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Benzodiazepine used for anxiety

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Alprazolam

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Nonbenzodiazepine used as an anxiolytic

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buspirone

GAD

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nonbenzodiazepine used for sleep

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Zolpidem

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Major effect of benzos on sleep @ high doses

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REM is decreased

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Neurologic SE of Benzos

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Anterograde amnesia

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Reason benzos are used cautiously in pregnancy

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Ability to cross placenta

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Main route of metabolism for benzodiazepines

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Hepatic

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Benzo's that undergo extrahepatic conjugation (useful in elderly or hepatically impaired)

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Lorazepam
Oxazepam
Temazepam

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MOA Benzos

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↑frequency of GABA mediated chloride channel opening

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Antidote to Benzo overdose

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Flumenazil

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Benzo with useful relaxant effects in SkM spasticity of central origin

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Diazepam

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Benzo that has high efficacy in absence seizures and in anxiety states, such as agoraphobia

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Clonazepam

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Benzos that are most effective in the treatment of panic disorder

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Alprazolam and Clonazepam

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Benzo that is used for anesthesia

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Midazolam

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DOC Status Epilepticus

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Diazepam

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Longer acting benzos used in the mgmt of withdrawal states of alcohol and barbiturates

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Chlordiazepoxide
Diazepam

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Agents (benzos) having active metabolites, long half lives, and high incidence of adverse effects

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Diazepam
Flurazepam
Chlordiazepoxide
Clorazepate

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Barbiturates may ppt this hematologic condition

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Acute Intermittent Porphyria

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Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property

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Liver enzyme INDUCTION

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Barbiturate MOA

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↑duration of GABA mediated Cl channel opening

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Barbiturate used for induction of anesthesia

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Thiopental

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Site of action of Zaleplon and Zolpidem

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Partial agonists @BZ1

*Not BZ2, therefore no anxiety effects

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Good hynoptic activity with less CNS SE than most benzos

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Zolpidem
Zaleplon

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Agent that is a partial agonist for the 5-HT1a receptor

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Buspirone

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DOC GAD

not effective in acute anxiety

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Buspirone

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Mechanism of Thiopental effect termination

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redistribution

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With the exception of _____, barbiturates are extensively metabolized

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phenobarbital

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Antidote to Benzo poisoning

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Flumenazil

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BZ1 agonists which bind to α1 GABAa subunit

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Zaleplon
Zolpidem
Eszopiclone

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Antidote for BZ1 agonists

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Flumenazil

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REM decreases are more rare in the newer hypnotics _____ and _____

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Zaleplon
Zolpidem

also less tolerance effects

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______ is effective in Cerebral palsy

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Diazepam

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Result of physiologic dependence to sedative-hypnotics

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abstinence syndrome upon withdrawal (seizures, anxiety, tremors, hyperreflexia)

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Benzos for long term treatment of panic and phobic disorders

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Alprazolam
Clonazepam

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Consideration in dosage in elderly for insomnia

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decrease dosage

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Use of Zolpidem, Zaleplon, Eszopiclone

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Insomnia

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Bipolar disorder

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Clonazepam

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Muscle spasticity

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Diazepam

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Management of withdrawal states

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Chlordiazepoxide
Diazepam

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Drugs which produce additive depression

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Alcohol/Benzo/Barbiturates
Antihistamines
B-blockers
Anticholinergics
Opioids
TCAs

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drug used in GAD which binds 5-HT1 and does not affect driving skills

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Buspirone

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activates melatonin receptors in the suprachiasmatic nuclei of the CNS, decreasing the latency of sleep

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Ramelteon

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Side effects of Ramelteon

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↓testosterone
↑prolactin

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_____ of urine helps in the elimination of barbiturates

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alkalinization

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short acting benzos

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Triazolam
Oxazepam
Midazolam

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explanation for the increased sensitivty of elderly patients after administration of a single dose of a benzodiazepine

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changes in brain function that accompany the aging process