Sedatives & Hypnotics Flashcards
Ok, so what’s the difference between a sedative, a hypnotic, and a general anesthetic?
Sedative: Anxiolytic (“inhibit anxiety) – but ideally with minimal effect on motor or mental functions. Hypnotic: Induce sleep (with a much more pronounced CNS depression than sedatives). General Anesthetic: Induce reversible coma – Hypnosis, Amnesia, Analgesia, Muscle relaxation, Attenuation of autonomic reflexes.
Benzodiazepines?
Diazepam, Chordiazepoxide, Lorazepam, Flurazepam, Alprazolam, Midrazolam, Triazolam
Diazepam class?
Benzodiazepine
Chlordiazepoxide class?
Benzodiazepine
Lorazepam class?
Benzodiazepine
Flurazepam class?
Benzodiazepine
Alprazolam class?
Benzodiazepine
Midrazolam class?
Benzodiazepine
Triazolam class?
Benzodiazepine
Benzodiazepine mxn?
GABAa agonist: bind between a1 & y2 subunits.
Diazepam half-life? Active mets for?
43 hrs, 100 hrs
Diazepam for?
Depression, Bipolar, Anticonvulsant, Muscle relaxant
Chlordiazepoxide half life? Active mets for?
10 hrs, 100 hrs
Chlordiazepoxide for?
Depression, Bipolar
Lorazepam half life?
14 hrs
Lorazepam for?
Depression, Bipolar, Sedation, Anticonvulsant, Prevent w/drawal in alcoholics
Flurazepam half life? Active mets for?
74 hrs, 100 hrs
Flurazepam for?
Depression, Bipolar
Alprazolam half life?
12 hrs
Alprazolam for?
Depression, Bipolar Sedation
Midazolam half life?
1.9 hours
Midazolam for?
Anesthesia (calms, anterograde amnesia)
Triazolam half life?
2.9 hours
Triazolam for?
Depression, Bipolar, Sleep
Benzodiazepine side effects?
Daytime sedation, drowsiness, anterograde amnesia, synergistic/additive CNS depression with other drugs (but remember the “ceiling effect”), psychologic & physiologic dependence with chronic use
Use of sedative-hypnotics?
Induce sleep, anxiolysis (GAD, panic disorders, OCD, phobias), muscle relaxation, anticonculsant, pre-anesthetic, recreation
Zolpidem class?
Non-benzodiazepine receptor agonist – BDZ-1 selective agonist
Zolpidem for?
Sedation and hypnosis WITHOUT muscle relaxation or anticonvulsant activity
Zolpidem side effects?
Sleep-walking, next morning impairment (still, generally short half-life, so little hang over)
Flumazenil class?
Benzodiazepine antagonist: Competitive non-selective antagonist
Flumazenil use?
Benzodiazepine overdose
Flumazenil side effect?
Withdrawal (may be life threatening), seizures in mixed overdoses
Barbiturates?
Thiopental & Phenobarbital
Barbiturate mxn?
GABAa agonists
Thiopentinal for?
Induce anasthesia
Phenobarbital for?
Antiepileptic, anticonvulsant
Barbiturate side effects?
Daytime sedation and drowsiness, dose-dependent depression of CNS, psychologic and physiologic dependence (chronic use), significant P450 enzyme induction,
Why cant other barbiturates be used for hypnosis?
Half-lifes are too long: they will accumulate during repetitive administration (hence the preferred use of benzodiazepienes)
Buspirone mxn?
Partial agonist at 5HT1A receptors, NO interaction with GABAa
Buspirone for?
Anxiolytic WITHOUT marked sedation (euphoric, hypnotic, anticonvulsant, muscle relaxant)
Benzos for sedation?
Lorazepam, Alprazolam
Benzos for sleep?
Triazolam, Zolpidem (pseudo-benzo)
Benzos for anesthesia? What else can be used?
Midazolam (+ calming, anterograde amnesia). For induction, thiopental (barbiturate) is used.
Benzos for anticonvulsion? What else can be used?
Lorazepam, Diazepam. Phenobarbital (barbiturate) can also be used.
Benzo for muscle relaxation?
Diazepam
Depression tx?
Antidepressants for long term, Benzos for short term immediacy if needed
Acute anxiety tx?
Benzos
GAD?
SSRIs are first line, then buspirone & benzos
Panic disorder tx?
SSRIs, benzos
OCD tx?
SSRIs
PTSD tx?
Various antidepressants