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4Qpharm3-test1 > Benzos & Barbituates > Flashcards

Benzos & Barbituates Flashcards

1
Q

Benzodiezepines MOA

A

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

  • causes a ceiling effect
  • shifts dose response curve, NOT max response
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2
Q

Diazepam indication

A

epilepsy, seizures, muscle relaxation

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3
Q

Benzodiazepines Contraindications, Interactions & SEs

A

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

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4
Q

Benzodiazepines Kinetics

A

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

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5
Q

Benzodiazepines: withdrawal, overdose, kinetics

A

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

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

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6
Q

Diazepam: class and use

A

Long acting benzodiazepine

epilepsy, seizures, muscle relaxation

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7
Q

Chlordiazepoxide: class and use

A

Benzodiazepine

alcohol withdrawal

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8
Q

Flurazepam: class and use

A

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

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9
Q

Temazepam: class and use

A

benzodiazepine
insomnia
(Flurazepam & Temazepam may cause hangover effect)

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10
Q

Midazolam: class and use

A

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

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11
Q

Lorazepam: class and use

A

short-acting benzodiazepine

Epilepsy, seizures, alcohol withdrawal

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12
Q

Oxazepam: class and use

A

short-acting benzodiazepine

use?

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13
Q

Flumazenil: class and use

A

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

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14
Q

Barbiturates: MOA

A
  • acts on GABA receptor
  • stimulates Cl- influx & inhibition INDEPENDENT OF GABA
  • causes marked CNS depression
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15
Q

Barbiturates: Kinetics

A

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

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16
Q

Barbiturates: Contraindications/Interactions

A

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

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17
Q

Barbiturates: Side effects (9)

A 
causes euphoria
CNS depression (drowsiness, mood change, impaired judgment),↓REM sleep, paradoxical excitement, dependence, NVD, vertigo, allergic rxn, vasomotor ↓
18
Q

Barbituates: withdrawal, overdose, comments

A

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

19
Q

Pentobarbital: class and use

A

(aka Nembutal NA)

class: barbiturate
use: ?

20
Q

Phenobarbital: class & use

A

(aka Luminal Na)

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

21
Q

Secobarbital: class & use

A

barbiturate

use: ?

22
Q

Thiopental: class & use

A

barbiturate

ULTRA short-acting, induce anesthesia

23
Q

Zolpidem (Ambien): class & use

A

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

24
Q

Zaleplon (Sonata): class & use

A

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

25
Q

Eszopiclone (Lunesta): class & use

A

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

26
Q

Zoplidem (Ambien): kinetics

A

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

27
Q

Zaleplon (Sonata): kinetics

A

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

28
Q

Eszopiclone (Lunesta): kinetics

A

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

29
Q

Zoplidem (Ambien): contraindications/SEs

A

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

30
Q

Zaleplon (sonata): contraind/SEs

A

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

31
Q

Eszopiclone: contraind/SEs

A

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
Q

Eszopiclone (Lunesta): Withdrawal, OD, comments

A

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

33
Q

How is Eszopliclone different thatn Zoplidem and Zaleplon

A

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

34
Q

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

A

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

35
Q

Ramelteon (Rozarem): kinetics

A

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

36
Q

Ramelteon (Rozarem): SEs

A

ADDITIVE w/EtOH

few SEs: drowsiness, dizziness, nausea

37
Q

Buspirone: class, MOA, indications/use

A

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

38
Q

Buspirone: kinetics

A

takes ~2 weeks tp tale effect
oral absorption
CYP3A4

39
Q

Bupsirone: SEs, withdrawal, OD, comments

A

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
Q

Chloral hydrate (noctec): class, MOA, uses

A

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

41
Q

Chloral hydrate (noctec): kinetics

A

converts to trichloroethanol

high dose=resp & vasomotor ↓

42
Q

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

A

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

4Qpharm3-test1 (9 decks)

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