Kruse: intro to drugs of abuse, sedative-hypnotics, alcohol

Question 1

Describe the dose difference on CNS effects of barbituates and Benzodiazepines

Answer 1

• Barbituates have linear effects that can lead to medullary depression and coma
• Benzos level off and don’t become as harmful at higher doses

Question 2

MOA of Benzos

Answer 2

• 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

Question 3

metabolism and excretion of benzos

Answer 3

-CYP3A4 (phase 1) and glucuronidation (phase 2)

Question 4

What benzo has a long half life with active metabolites and very fast onset of action

Answer 4

Diazepam

Question 5

What benzo has the shortest half life

Answer 5

Midazolam

Question 6

what the downfall to using a benzo with long half life like Diazepam

Answer 6

cumulative toxicity

Question 7

what are the 3 intermediate to long acting benzos

Answer 7

Diazepam
Lorazepam
Clonazepam

Question 8

MOA of Barbiturates

Answer 8

-binds to GABAa and increases DURATION of channel opening

Question 9

what is the MOA of newer hypnotics (sleep aids)

Answer 9

-Binds to GABAa receptors that contain the a1-subunit

Question 10

describe the effects of newer hypnotics (sleep aids)

Answer 10

• only approved for treatment of sleep disorders

- no anxiolytic, anesthetic, anticonvulsant, muscle relaxing, respiratory, or cardiovascular effects

Question 11

what are the newer hypnotics (sleep aids)

Answer 11

• eszopiclone
• Zolpidem
• Zaleplon

Question 12

what is the antagonist used in benzo overdose

Answer 12

Flumazenil (fluffy dog in sketchy)

Question 13

MOA of Ramelteon

Answer 13

-agonist at MT1 and MT2 melatonin receptors

Question 14

what is Buspirone approved for treatment of

Answer 14

generalized anxiety disorder

Question 15

what causes hangovers with alcohol use

Answer 15

-Acetaldehyde

Question 16

what blocks alcohol dehydrogenase

Answer 16

Fomepizole

Question 17

What blocks aldehyde dehydrogenase

Answer 17

Disulfiram

Question 18

what are the 2 receptors in the CNS targeted by alcohol

Answer 18

• inhibits ability of glutamate to open NMDA receptor

- enhances effects of GABA on GABAa receptor

Question 19

how would you treat Acute alcohol intoxication

Answer 19

• monitor respiratory depression and aspiration of vomit
• Glucose can treat metabolic alterations such as hypoglycemia and ketosis
• Thiamine to protect against Wernicke-Korsakoff syndrome

Question 20

what is Naltrexone approved for

Answer 20

treatment of alcohol and opiate dependence

Question 21

what is the MOA of Naltrexone

Answer 21

• mu opioid receptor antagonist (long acting)

- short term . . 12 weeks

Question 22

Acamprosate can be used to treat alcohol dependence. What is its MOA

Answer 22

• weak NMDA receptor antagonist and GABAa receptor agonist

- short and long term . . more than 6 months