Test 2 Hypnotics and Sedatives Flashcards
How do older sedatives/hypnotics/alcohol differ from Benzos and newer hypnotics?
Benzos and newer hypnotics have a higher margin of safety
What is the indicated use for Alprazolam?
Depression
What is the indicated use for chlordiazepoxide?
Alcohol withdraw syndrome
What is the indicated use for clonazapam?
Convusions, panic disorder, muscle relaxation
What is the indicated use for valium and lorazepam?
Status epilepticus
What is the indicated use for Triazolam?
Early morning insomnia
Which drugs are listed as anxiolytics?
Literally all of them except triazolam and flurazepam
What can make benzos dangerous?
When combined with other CNS depressants, but rarely fatal by themselves, even at high doses
What is the main mechanistical property of benzos?
Sedation and hypnosis, which increase as the dose increases
Decreases time to fall asleep, increases the time of Non rem sleep
Decreases the duration of Rem sleep
What type of amnesia can benzos cause? Differentiate if from the other type.
Anterograde amnesia, given pre operatively and makes them forget what’s about to happen
Retrograde is where their memory is lost of an event that already occurred
What are the three benzos listed as anticonvulsants?
Clonazepam, lorazapam, diazepam
CAD (ativan instead of L)
What does benzos bind to specifically? Causing what action?
GABA A, increases the frequency of channel opening events
What effect do benzos have on neuronal inhibition mediated by GABA?
It potentiates it!
What are the side effects of benzos?
Ataxia, discordination
Abuse/dependence
Withdrawal if using chronically then stopping
Drug to drug interactions with alcohol-increases the absorbtion of benzos
What effect does alcohol have on benzos?
Alcohol increases the absorption rate of BZDs
What are the half life’s of short, intermediate, and long acting benzos?
short- less than 6 hours
Intermediate- 6-24 hours
Long- Over 24 hours
What category is buspirone?
Partial 5-HT 1A agonist at the brain and affinity with D2 receptors
What drug class is zolpidem, zaleplon, and eszopiclone?
Non-benzo
What are the non benzos MOA?
Selectively bind to BZ1 (a1) subtype of GABA A receptor
What are the muscle relaxant and anticonvulsion properties of non benzos?
Minimal of either
When are doe adjustments needed with non benzos?
Hepatic issues, elderly, patients taking cimetidine and rifampin. Inhibitor and inducer, respectively
What is the benzo AND non benzo reversal?
Flumazenil
What drug category is flumazenil?
Competitive BZD antagonist
What are the downsides of barbituates, compared to benzos?
Barbituates are more dangerous overall, higher incidence of toxicity, abuse, and physical dependence
What are the CNS pharmacological properties of barbituates?
Hypnotic- decreases REM time (just like benzos)
Hyperalgesia- INCREASED reaction to painful stimuli
Anesthesia- Thiobarbituates and short acting oxybarbituates for anesthesia induction
Anticonvulsion- Phenobarbital has a selective anticonvulsant action
What are the other pharmacological properties of barbituates?
Dose related respiratory depression
Dose dependent for CV effects, if anesthesia dose, decrease CO and renal perfusion, increased TPR
Psychological- Compulsive misuse
Physical dependence
How do barbituates work?
Increase the duration of GABA gated CL- channel openings
GABA mimetic at high concentrations
Inhibitory excitatory AMPA receptors
What are the drug to drug interactions for barbituates?
Alcohol, antihistamines
What are the situational contraindications to barbituates?
Acute intermittent porphyria-porphin biosynthesis
Pulmonary insufficiency
CV diseases
What is the ideal treatment to barbituate poisening?
Gastric lavage if possible
What are the technical usages for barbituates?
Sedative/hypnotic
Anesthesia-preanesthetic sedation
Anticonvulsant-phenobarbital
Hyperbilirubinemia and kernicterus
