Benzos & Barbituates Flashcards Preview

4Qpharm3-test1 > Benzos & Barbituates > Flashcards

Flashcards in Benzos & Barbituates Deck (42):
1

Benzodiezepines MOA

MOA: Binds GABA A recep & ↑affinity for GABA -prolong GABA, depends on GABA
-causes a ceiling effect
-shifts dose response curve, NOT max response

2

Diazepam indication

epilepsy, seizures, muscle relaxation

3

Benzodiazepines Contraindications, Interactions & SEs

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

4

Benzodiazepines Kinetics

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

5

Benzodiazepines: withdrawal, overdose, kinetics

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

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

6

Diazepam: class and use

Long acting benzodiazepine
epilepsy, seizures, muscle relaxation

7

Chlordiazepoxide: class and use

Benzodiazepine
alcohol withdrawal

8

Flurazepam: class and use

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

9

Temazepam: class and use

benzodiazepine
insomnia
(Flurazepam & Temazepam may cause hangover effect)

10

Midazolam: class and use

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

11

Lorazepam: class and use

short-acting benzodiazepine
Epilepsy, seizures, alcohol withdrawal

12

Oxazepam: class and use

short-acting benzodiazepine
use?

13

Flumazenil: class and use

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

14

Barbiturates: MOA

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

15

Barbiturates: Kinetics

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

16

Barbiturates: Contraindications/Interactions

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

17

Barbiturates: Side effects (9)

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

18

Barbituates: withdrawal, overdose, comments

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

19

Pentobarbital: class and use

(aka Nembutal NA)
class: barbiturate
use: ?

20

Phenobarbital: class & use

(aka Luminal Na)
class: barbiturate
use: LONG-ACTING, ANTI-CONVULSANT

21

Secobarbital: class & use

barbiturate
use: ?

22

Thiopental: class & use

barbiturate
ULTRA short-acting, induce anesthesia

23

Zolpidem (Ambien): class & use

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

24

Zaleplon (Sonata): class & use

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

25

Eszopiclone (Lunesta): class & use

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

26

Zoplidem (Ambien): kinetics

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

27

Zaleplon (Sonata): kinetics

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

28

Eszopiclone (Lunesta): kinetics

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

29

Zoplidem (Ambien): contraindications/SEs

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

30

Zaleplon (sonata): contraind/SEs

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

31

Eszopiclone: contraind/SEs

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

32

Eszopiclone (Lunesta): Withdrawal, OD, comments

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

33

How is Eszopliclone different thatn Zoplidem and Zaleplon

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

34

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

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

35

Ramelteon (Rozarem): kinetics

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

36

Ramelteon (Rozarem): SEs

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

37

Buspirone: class, MOA, indications/use

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

38

Buspirone: kinetics

takes ~2 weeks tp tale effect
oral absorption
CYP3A4

39

Bupsirone: SEs, withdrawal, OD, comments

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

40

Chloral hydrate (noctec): class, MOA, uses

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

41

Chloral hydrate (noctec): kinetics

converts to trichloroethanol
high dose=resp & vasomotor ↓

42

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

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