Sedative Hypnotics Flashcards
Classification of sedatives and hypnotics.
- Benzodiazepines - diazepam, alprazolam, lorazepam, nitrazepam, clobazam
- Barbiturates - phenobarbitone, secobarbitone, thiopentone, meohobarbitone
- Non-benzodiazepines - Zolpidem, zipiclone, zaleplon, eszopiclone.
- Melatonin receptor agonists-ramelteon
- Miscellaneous - chloro hydrate, promethazine, opioids, neuroleptics, etc.
Name the clinical uses of sedatives and hypnotics?
- Anxiety
- Sleep disorders
- Bipolar disorders
- Seizure management
- Muscle spasticity
- Management of withdrawal states
Which drugs when added with sedative hypnotics causes additive CNS depression?
- Alcoholic beverages
- Anti-histamines
- Anti-psychotic drugs
- Opioid analgesics
- Tricyclic antidepressants
What are the toxicities of sedatives and hypnotics?
- Psychomotor dysfunction
- Overdose
- Additive CNS depression (cardiac and respiratory depression)
- increase anticoagulant effect
- acute porphyria
- formation of liver microsomal enzymes that metabolize drugs
What peptide is found in the hypothalamus and involved in wakefulness?
What’s it’s antagonist?
Orexin
Suvorexant
Flumanzenil is used for the overdose of which drugs?
Benzodiazepines, eszopiclone, zaleplon
Clinical applications of benzodiazepines?
- Anxiety states and anxiety disorder
- Panic attacks
- Insomnia
- Skeletal muscle relaxation
- Seizure control
Mechanism of action of benzodiazepines
Bind GABA(A) receptors to facilitate chloride channel opening and increase frequency.
Mechanism of action of barbiturates
Bind to GABA(A) receptor sites (different from benzodiazepines) and facilitate chloride channel opening and increase duration.
Clinical applications of barbiturates
- Anesthesia
- Insomnia and sedation
- Seizure disorders
Which hypnotic drug causes endocrine changes?
Ramelteon (melatonin receptor agonist)
Name 5-HT agonist for anxiety state?
Buspirone
Name newer hypnotics used for sleep disorders.
- Eszopiclone
- Zaleplon
- Zolpidem