Anxiolytic-sedative-hypnotic Drugs (Slattery)

Question 1

Sedative-Hypnotic drug goals?

Answer 1

• Relief of anxiety
• Able to cause sedation
• Able to encourage sleep

Question 2

anxiolytic?

Answer 2

Patient is related; unconcerned with surroundings but fully functional

Question 3

sedative?

Answer 3

dec. activity; calms patient although awake

Question 4

hypnotic?

Answer 4

make drowsy and facilitate the onset and maintenance of sleep; may be easily aroused

Question 5

general anesthesia?

Answer 5

loss of consciousness and the patient can not be aroused

Question 6

What is a linear slope drug?

Answer 6

inc. doses leads to greater effects with linear relationship; “Barbiturates”

Question 7

What is a nonlinear slop drug?

Answer 7

inc. doses does not directly correlate with inc. in drug effects, requires more drug to get proportionate effects
“Benzodiazepines”

Question 8

Common Barbiturates?

Answer 8

Phenobarbital
Pentobarbital
Thiopental

Question 9

Barbiturate mech.

Answer 9

Binds to GABA-A receptor working as a chloride ion channel to hyper polarize cell; Barbiturates inc. the duration of the channel openings;

Question 10

Barbiturate absorption

Answer 10

Absorbed rapidly after oral administration; Highly lipid soluble and reaches peak conc. in 30 seconds; oxidated by hepatic enzymes; long half-life (4-5 days)

Question 11

Why is phenobarbital different?

Answer 11

often secreted unchanged and can be effected by pH (it is a weak acid), inc. pH can lead to more drug excretion

Question 12

Barbiturate interactions?

Answer 12

activity of hepatic drug-metabolizing enzymes may be increased

Question 13

Barbiturates can?

Answer 13

induce sleep with high enough doses

Question 14

Thiopental?

Answer 14

very lipid soluble and favored for induction of anesthesia; short duration of action because of rapid tissue redistribution

Question 15

Can barbiturates lead to drug dependence?

Answer 15

Yes

Question 16

Barbiturates clinical uses?

Answer 16

Hypnosis
Seizure controle
anesthesia induction

Question 17

Common Benzodiazepines?

Answer 17

Diazepam
Lorazepam
Triazolam
Alprazolam

Question 18

benzodiazepine mech.?

Answer 18

Works on GABA-A receptor; binds allosterically to inc. frequency of chloride channels opening

Question 19

Triazolam and Diazepam?

Answer 19

Very rapid effects cause of lipophilicity, Triazolam more so

Question 20

Benzo. differences?

Answer 20

Unlike barbiturates they have little effect on hepatic drug metabolizing enzymes; Exert more anterograde amnesic effects

Question 21

Lorazepam and Diazepam?

Answer 21

often used in anesthesia in combination with other agents

Question 22

Flumazenil?

Answer 22

can reverse benzo. effects because it is a site antagonist; could be used in bento. caused respiratory depression

Question 23

Non-Benzo. Receptor agonist?

Answer 23

Bind to certain GABA-A receptor subtypes; Giving rapid onset, short duration and slow tolerance development “Zolpidem (Ambien)”

Question 24

Buspirone?

Answer 24

Relieves anxiety without sedative or hypnotic effects; Takes a week to kick in so not used for acute anxiety; less motor impairment

Question 25

Ramelteon?

Answer 25

Used to help fall asleep; Agonist for melatonin rec. MT1 and MT2 in suprachiasmatic nuclei “master clock”; low abuse potential