Benzos & Barbituates

Question 1

Benzodiezepines MOA

Answer 1

MOA: Binds GABA A recep & ↑affinity for GABA -prolong GABA, depends on GABA

• causes a ceiling effect
• shifts dose response curve, NOT max response

Question 2

Diazepam indication

Answer 2

epilepsy, seizures, muscle relaxation

Question 3

Benzodiazepines Contraindications, Interactions & SEs

Answer 3

Pregnancy cat D, sleep apnea, elderly
Can develop tolerance & physical dependence
CNS depression, paradoxical excitement, super- additive w/ other CNS depressants, sleep related behaviors

Question 4

Benzodiazepines Kinetics

Answer 4

Oral absorption
Duration of action varies based on metabolism -active metabolites extend halflife
Metabolized by CYP3A4
-cimetadine increases t1/2 Kinetics & duration of action are important in DOC

Question 5

Benzodiazepines: withdrawal, overdose, kinetics

Answer 5

abrupt discontinuation can cause rebound insomnia & anxiety- taper dc gradually

OD-generally safe, causes long sleep, fatalities w/alcohol

Question 6

Diazepam: class and use

Answer 6

Long acting benzodiazepine

epilepsy, seizures, muscle relaxation

Question 7

Chlordiazepoxide: class and use

Answer 7

Benzodiazepine

alcohol withdrawal

Question 8

Flurazepam: class and use

Answer 8

long acting benzodiazepine
insomnia
(Flurazepam & Temazepam may cause hangover effect)

Question 9

Temazepam: class and use

Answer 9

benzodiazepine
insomnia
(Flurazepam & Temazepam may cause hangover effect)

Question 10

Midazolam: class and use

Answer 10

short-acting benzodiazepine
Anesthesia prep for surgery
short half-life

Question 11

Lorazepam: class and use

Answer 11

short-acting benzodiazepine

Epilepsy, seizures, alcohol withdrawal

Question 12

Oxazepam: class and use

Answer 12

short-acting benzodiazepine

use?

Question 13

Flumazenil: class and use

Answer 13

BZD antagonist (GABA antagonist), competes with BZDs
reverses CNS effects of BZDs
IV only-slowly, very short acting ~30mins
contra: hx of seizures
SE: triggers withdrawal & seizures if dependent

Question 14

Barbiturates: MOA

Answer 14

• acts on GABA receptor
• stimulates Cl- influx & inhibition INDEPENDENT OF GABA
• causes marked CNS depression

Question 15

Barbiturates: Kinetics

Answer 15

oral, rapid CNS uptake
lipid solubility determines length of action
low margin of safety
liver metabolism via CYP450, long term use can induce CYP450s

Question 16

Barbiturates: Contraindications/Interactions

Answer 16

PORPHYRIA: enhances porphyria production
PULMONARY INSUFFICIENCY: hx of addiction
supra-additive CNS effect esp. when combined w/alcohol

Question 17

Barbiturates: Side effects (9)

Answer 17

causes euphoria
CNS depression (drowsiness, mood change, impaired judgment),↓REM sleep, paradoxical excitement, dependence, NVD, vertigo, allergic rxn, vasomotor ↓

Question 18

Barbituates: withdrawal, overdose, comments

Answer 18

withdrawal can be LIFE THREATENING!!!
OD can cause: coma, resp↓, ↓BP
-DO NOT give stimulants for OD
-forced diuresis & alkalization of urine

Question 19

Pentobarbital: class and use

Answer 19

(aka Nembutal NA)

class: barbiturate
use: ?

Question 20

Phenobarbital: class & use

Answer 20

(aka Luminal Na)

class: barbiturate
use: LONG-ACTING, ANTI-CONVULSANT

Question 21

Secobarbital: class & use

Answer 21

barbiturate

use: ?

Question 22

Thiopental: class & use

Answer 22

barbiturate

ULTRA short-acting, induce anesthesia

Question 23

Zolpidem (Ambien): class & use

Answer 23

“other” sedative: ↑GABA mediated inhibition via BZ1 GABA receptor
STRONG RAPID ACTION
use: insomnia

Question 24

Zaleplon (Sonata): class & use

Answer 24

“other” sedative: ↑GABA mediated inhibition via BZ1 GABA receptor
STRONG RAPID ACTION
use: insomnia

Question 25

Eszopiclone (Lunesta): class & use

Answer 25

"other" sedative: ↑GABA mediated inhibition via BZ1 GABA receptor STRONG RAPID ACTION ***LONG HALF LIFE=long term tx*** use: insomnia

Question 26

Zoplidem (Ambien): kinetics

Answer 26

oral absorption liver metabolism short duration of action high margin of safety

Question 27

Zaleplon (Sonata): kinetics

Answer 27

oral absorption liver metabolism short duration of action high margin of safety

Question 28

Eszopiclone (Lunesta): kinetics

Answer 28

oral absorption liver metabolism short duration of action high margin of safety

Question 29

Zoplidem (Ambien): contraindications/SEs

Answer 29

caution w/Hx of dependence or EtOH abuse GI: NVD CNS: drowsiness sleep behaviors, amnesia, confusion, memory, rebound insomnia

Question 30

Zaleplon (sonata): contraind/SEs

Answer 30

caution w/Hx of dependence or EtOH abuse GI: NVD CNS: drowsiness sleep behaviors, amnesia, confusion, memory, rebound insomnia

Question 31

Eszopiclone: contraind/SEs

Answer 31

caution w/Hx of dependence or EtOH abuse GI: NVD CNS: drowsiness sleep behaviors, amnesia, confusion, memory, rebound insomnia ***withdrawal scs w/abrupt dc after long-term use

Question 32

Eszopiclone (Lunesta): Withdrawal, OD, comments

Answer 32

withdrawal sxs w/abrupt d/c after long term use

Question 33

How is Eszopliclone different thatn Zoplidem and Zaleplon

Answer 33

Eszopliclone has a LONG HALF LIFE, so used in long term treatment & withdrawal sxs w/ abrupt dc after long term use

Question 34

Ramelteon (Rozarem): class, MOA, indications/use

Answer 34

other sedative melatonin analogue (agonist) resets sleep-wake cycle independent of GABA

Question 35

Ramelteon (Rozarem): kinetics

Answer 35

oral absorption, ↑1st pass metabolism CYP1A2 & 2C9 meta= ↑interactions ADDITIVE w/EtOH

Question 36

Ramelteon (Rozarem): SEs

Answer 36

ADDITIVE w/EtOH | few SEs: drowsiness, dizziness, nausea

Question 37

Buspirone: class, MOA, indications/use

Answer 37

other sedative PARTIAL AGONIST of 5-HT receptor (serotonin)-↓serotonin release RELEIVES ANXIETY W/O SEDATION mild anxiety, ADHD, autism, PMS

Question 38

Buspirone: kinetics

Answer 38

takes ~2 weeks tp tale effect oral absorption CYP3A4

Question 39

Bupsirone: SEs, withdrawal, OD, comments

Answer 39

good choice for recovering alcoholics fairly safe at high dose dizziness, HA, NVD, restlessness, nervousness does not potentiate CNS depression w/alcohol or BZDs

Question 40

Chloral hydrate (noctec): class, MOA, uses

Answer 40

other sedative acts on GABA A receptor sedative/hypnotic NO LONGER USED

Question 41

Chloral hydrate (noctec): kinetics

Answer 41

converts to trichloroethanol | high dose=resp & vasomotor ↓

Question 42

Chloral hydrate (noctec): SEs, withdrawal, OD, comments

Answer 42

liver damage, fatal intoxication, NVD, allergic rxn, arrhythmia used globally due to CHEAP cost