Kruse- Intro to Drugs of Abuse Sedative-Hypnotics Alcohol Flashcards
Sedatives do what?
-decrease CNS activity, moderate excitement, and calms the recipient
Hypnotics do what?
-produces drowsiness and facilitates the onset and maintenance of sleep and from which the recipient can be aroused easily
Where/How do Benzodiazpines work?
- Act on ligand gated ion channels aka GABAa receptors
- cause sedation, hypnotic effects, muscle relaxation, anxiolytic and anticonvulsant effects
- makes receptor more active in lower concentrations of GABA
- so you need BOTH a BENZO and GABA receptor presents
Where/How do Barbiturates work?
- Act on GABAa receptors
- cause a wide spectrum of effects: mild sedation to anesthesia
- Keep receptor open for longer period of time
Where do Benzodiazepines distribute?
-CNS, Placenta, and Breast-milk
How are Benzodiazepines processed?
- CYP34A phase 1
- Glucuridation phase 2
Do Benzodiazepines have a risk of dependence and tolerance?
-yes
Benzodiazepines examples?
- Diazepam (Valium)
- alprazolam (Xanax)
- lorazepam (Ativan)
Half life and onset of Chlordiazepoxide? active metabolites?
- greater than 100 hours
- intermediate onset
- yes
Half life and onset of Diazepam? Active metabolites?
- greater than 100 hours
- very fast
- yes
Half life and onset of Oxazepam? Active metabolites?
- 5-14 hours
- Slow
- none
Half life and onset Lorazepam? Active metabolites?
- 10-20 hours
- intermediate
- none
Use of Midazolam?
- rapid on and rapid off
- dentists use this to induce anesthesia or in other quick surgery settings
Intermediate to lond acting Benzodiazepines are?
- Diazepam
- Lorazepam
- Clonozepam
Short acting benzodiazepines are?
- Midazolam
- Oxazepam
- Alprazolam
- Temazepam
- Triazolam
How do Barbiturates work?
What are examples?
risk of dependence and tolerance?
- binding to GABA a receptor and increase duration of time the channel is actually open
- —“arbitals”
- yes, risk of both but not all people have risk or dependence. all people build tolerance
How do Benzodiazepines work?
-Causes GABA receptors to be activated at lower concentrations
Barbiturates are mostly used for what? examples?
-sleep aids
-Eszopiclone
-Zolpidem
-Zaleplon
“Sleep Ezzy with barbiurates”
Sedative-hypnotics are used to treat what?
-anxiety, insomnia, epilepsy, siezures, control withdrawals
Benzo Drugs to treat anxiety?
How high is the theraputic index? What is the antagonist (antidote) to overdose?
What are the disadvantages?
- Clonazepam
- Lorazepam
- Alprazolam
- Diazepam
- high
- Flumazenil treats OD
-disadvantages are dependence risk, CNS depression, SSRIs are preferred for these reasons
Benzo drugs used for insomnia? side effect?
-Eszopiclone (long half life)
-Zolpidem (2 sustain sleep)
-Zaleplon (both Zol and Zal act rapidly)
EZZy Sleep
-sleep shopping and sleep driving
Ramelteon is used to treat what?
MOA?
bioavailability?
Metabolized by?
- insomnia
- agonist at MT1 and MT 2 melatonin receptors
- low bioavailability
- CYP1A2