Kruse: intro to drugs of abuse, sedative-hypnotics, alcohol Flashcards
Describe the dose difference on CNS effects of barbituates and Benzodiazepines
- Barbituates have linear effects that can lead to medullary depression and coma
- Benzos level off and don’t become as harmful at higher doses
MOA of Benzos
- Act on GABAa receptors
- they lower the threshold for GABA so u still need to have GABA on board to work
- increase Chloride influx, hyperpolarizations, lower number of actions potentials
metabolism and excretion of benzos
-CYP3A4 (phase 1) and glucuronidation (phase 2)
What benzo has a long half life with active metabolites and very fast onset of action
Diazepam
What benzo has the shortest half life
Midazolam
what the downfall to using a benzo with long half life like Diazepam
cumulative toxicity
what are the 3 intermediate to long acting benzos
Diazepam
Lorazepam
Clonazepam
MOA of Barbiturates
-binds to GABAa and increases DURATION of channel opening
what is the MOA of newer hypnotics (sleep aids)
-Binds to GABAa receptors that contain the a1-subunit
describe the effects of newer hypnotics (sleep aids)
- only approved for treatment of sleep disorders
- no anxiolytic, anesthetic, anticonvulsant, muscle relaxing, respiratory, or cardiovascular effects
what are the newer hypnotics (sleep aids)
- eszopiclone
- Zolpidem
- Zaleplon
what is the antagonist used in benzo overdose
Flumazenil (fluffy dog in sketchy)
MOA of Ramelteon
-agonist at MT1 and MT2 melatonin receptors
what is Buspirone approved for treatment of
generalized anxiety disorder
what causes hangovers with alcohol use
-Acetaldehyde
what blocks alcohol dehydrogenase
Fomepizole
What blocks aldehyde dehydrogenase
Disulfiram
what are the 2 receptors in the CNS targeted by alcohol
- inhibits ability of glutamate to open NMDA receptor
- enhances effects of GABA on GABAa receptor
how would you treat Acute alcohol intoxication
- monitor respiratory depression and aspiration of vomit
- Glucose can treat metabolic alterations such as hypoglycemia and ketosis
- Thiamine to protect against Wernicke-Korsakoff syndrome
what is Naltrexone approved for
treatment of alcohol and opiate dependence
what is the MOA of Naltrexone
- mu opioid receptor antagonist (long acting)
- short term . . 12 weeks
Acamprosate can be used to treat alcohol dependence. What is its MOA
- weak NMDA receptor antagonist and GABAa receptor agonist
- short and long term . . more than 6 months
