Anxiety and Sleep

Question 1

decreases motor activity, coordination, and mental acuity

Answer 1

sedative

Question 2

increases tendency to sleep from which the patient is easily awakened

Answer 2

hypnotic

Question 3

induces sleep from which the patient is not easily awakened

Answer 3

anesthetic

Question 4

• produce anesthesia, coma and and death
• barbiturates
• ethanol

Answer 4

complete CNS depressants

Question 5

• typically don’t produce anesthesia and will not induce coma or death alone
• benzodiazepenes
• non benzodiazepine, BZ receptor agonists

Answer 5

incomplete CNS depressants

Question 6

Barbiturates bind that barbiturate binding site on the _______ receptor, increasing ______ ion channel flux by increasing channel open time

Answer 6

GABAa

chloride

Question 7

effect of barbiturates on CNS? respiratory and cardiovascular?

Answer 7

• complete CNS depressant

- no effect on cardiovascular up to anesthetic dose

Question 8

barbiturates induce what type of tolerance?

Answer 8

pharmacokinetic (induce CYP450, decrease plasma levels of other drugs)

Question 9

• tolerance to this class of drugs develops over time (kinetic and dynamic)
• addiction common
• withdrawal - anxiety, tremor, n/v, weight loss, psychosis, seizures, hyperthermia, cardiovascular collapse can be fatal
• treatment: measured reduction over time (2-3 wks)

Answer 9

barbiturates

Question 10

long acting barbiturate?

Answer 10

phenobarbital

Question 11

pentobarbital and secobarbital are _______ acting barbiturates

Answer 11

medium

Question 12

methohexital and amobarbital are ______ acting barbiturates

Answer 12

short, given IV

Question 13

ultra short acting barbiturate given IV?

Answer 13

thiopental

Question 14

used as sedatives, hypnotics (not 1st line), anticonvulsants, drug induced coma, preanesthetic, anesthetic, WADA test, truth serum, euthanasia

Answer 14

barbiturate uses

Question 15

• readily diffuse across all membranes
• redistribution accounts for differences in duration of action
• cross placenta
• high bound to plasma proteins (drug interactions)
• metabolized in liver
• excreted in urine

Answer 15

pharmacokinetics of barbiturates

Question 16

Benzodiazepines bind to BZ sites on GABAa receptor, increase _______ of GABAa receptor for GABA increasing likelihood of channel opening

Answer 16

affinity

Question 17

what underlies the differences in effects of various benzodiazepine compounds?

Answer 17

heterogeneity of receptor subunits, different affinities for BZ binding sites

Question 18

• incomplete CNS depressant
• decreased anxiety
• skeletal muscle relaxant
• anticonvulsant
• hypnotic
• tolerance develops to sedative, hypnotic, anticonvulsant actions
• paradoxical excitement
• no CV, resp, GI effects

Answer 18

effects of diazepam (benzodiazepines)

Question 19

• sedation and ataxia
• amnesia
• nightmares, irritability, anxiety, seizures
• treat acute overdose with flumazenil
• withdrawal: rebound anxiety irritability, insomnia, tremor, sweating, anorexia, seizures, psychosis
• low risk of fatal OD if used alone

Answer 19

side effects of benzos (diazepam)

Question 20

midazolam and triazolam are _______ benzodiazepines

Answer 20

short acting

Question 21

most rapidly inactivated benzo used for anesthesia IV?

Answer 21

midazolam

Question 22

anxiolytic/hypnotic used for panic attacks, rapid oral absorption/onset

Answer 22

alprazolam

Question 23

chlordiazepoxide, lorazepam are _____ benzos used as anziolytics/preanesthetic

Answer 23

moderate acting

Question 24

long acting benzo used as anticonvulsant?

Answer 24

clonazepam

Question 25

very long acting benzo with active metabolites used as anxiolytic, anticonvulsant, muscle relaxant, antispastic, pre-anesthetic?

Answer 25

diazepam

Question 26

flurazpeam is a _____ benzo

Answer 26

very long acting

Question 27

fast acting, amnestic, date rape drug, no therapeutic use

Answer 27

flunitrazepam

Question 28

used to reverse overdose of benzos and anesthesia?

Answer 28

flumazenil

Question 29

- rapidly absorbed from GI - admin orally, highly protein bound but few drug interactions - cross placenta - numerous active metabolites - metabolized in liver, excreted in urine

Answer 29

benzodiazepines

Question 30

- BZ1 agonists and non selective - hypnotic, short half life, less amnestic than benzos - produce less tolerance - hallucinations, sleepwalking, amnesia

Answer 30

zolpidem, zaleplon, eszopiclone

Question 31

partial agonist at 5-HT1a site, slow onset of action 1-2 wks, dysphoric at high doses

Answer 31

buspirone

Question 32

increase synaptic availability of 5-HT, used for GAD and prophylaxis for panic attack

Answer 32

SSRIs

Question 33

H1 blocker, pre and post op, antipruritic and antiemetic

Answer 33

hydroxyzine

Question 34

MT1/2 melatonin receptor antagonist, indicated for insomnia with prolonged sleep onset

Answer 34

ramelteon

Question 35

indicated for difficulties with sleep onset or maintenance, orexin antagonist

Answer 35

suvorexant

Question 36

H1 blocker, common OTC sedative

Answer 36

diphenhydramine

Question 37

blocks 5HT reuptake, antidepressant but also used as hypnotic

Answer 37

trazodone