antianxiety, relaxants, sedative hypnotics, etOH Flashcards

1
Q

Alprazolam (Xanax)

A

Benzo

intermediate acting

anxiolytic

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2
Q

Chlordiazepoxide (Librium)

A

Benzo

long acting

Anxiolytic, Anticonvulsant, Withdrawal suppressant

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3
Q

Diazepam (Valium)

A

Benzo, Centrally acting musc. relaxant

long acting

Anxiolytic, Anticonvulsant, Anesthesia supplement,
Withdrawal suppressant, Muscle relaxant (for spasms)

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4
Q

Lorazepam (Ativan)

A

Benzo, Centrally acting musc. relaxant

intermediate acting

Hypnotic, Anxiolytic, Anesthesia supplement, Withdrawal suppressant

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5
Q

Midazolam (Versed)

A

Benzo

short-acting

Induction or supplement to anesthesia

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6
Q

Temazepam (Restoril)

A

Benzo

intermediate-acting

hypnotic

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7
Q

Triazolam (Halcion)

A

Benzo

short acting (good to help fall asleep)

hypnotic

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8
Q

Flumazenil (Romazicon)

A

BENZODIAZEPINE ANTAGONIST

antag. at benzo receptor
not v. useful in emergencies: benzos don’t depr. resp that much, won’t reverse barb/opiate/etOH induced resp depr.

  • used in anesthesiology: post-op when given benzo, block effects, come out quicker
  • can trigger seizures in pts dependent on benzos/barbs/etOH
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9
Q

Butalbital (Fiorinal)

A

BARBITURATE

for tension ha, centrally acting relaxant

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10
Q

Pentobarbital (Nembutal)

A

BARBITURATES

intermediate/short acting

sedative-hypnotics

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11
Q

Phenobarbital

A

BARBITURATES

long acting

tx for epilepsy, anticonvulsant

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12
Q

Thiopental (Pentothal)

A

BARBITURATES

ultra-short acting

not currently used
IV induction of sx anesthesia
used for execution, then pancuronium (NM blocker)–>then K to stop heart

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13
Q

Balcofen (Lioresal)

A

CENTRALLY ACTING MUSCLE RELAXANT

analog of GABA, acts as agonist at GABAb

dec. skel. musc tone
tx spasticity (UMN probs)
rehab medicine

adverse: CNS depression, musc. wkness, dependence/abuse potential

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14
Q

Cyclobenzaprine (Flexeril)

A

CENTRALLY ACTING MUSCLE RELAXANT

related to tricyclic antideps.
most widely prescribed muscle relaxant
doesn’t work as well as benzos
don’t operate machinery, drive

highly sedating

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15
Q

Diazepam (Valium)

A

CENTRALLY ACTING MUSCLE RELAXANT

muscle spasms

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16
Q

Metaxalone (Skelaxin)

A

CENTRALLY ACTING MUSCLE RELAXANT

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17
Q

Tizanidine (Zanaflex)

A

CENTRALLY ACTING MUSCLE RELAXANT

alpha2 agonist (like Clonidine) 
CNS effects: dec. skel musc. tone

very sedating (take at night)

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18
Q

Alcohol

A

MISC. ANXIOLYTIC AND SEDATIVE-HYPNOTIC

anxiolytics, sedative, relaxant

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19
Q

Buspirone (Buspar)

A

MISC. ANXIOLYTIC AND SEDATIVE-HYPNOTIC

anti-anxiety, NO musc. relaxation, NOT sedating

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20
Q

Gammahydroxybutyrate (GHB)

A

MISC. ANXIOLYTIC AND SEDATIVE-HYPNOTIC

abused: party/club, date rape

GABA analog, crosses BBB

ergogenic effect: body building

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21
Q

Melatonin

A

MISC. ANXIOLYTIC AND SEDATIVE-HYPNOTIC

nutritional suppl, not prescription, OTC

can normalize sleep patterns- “shift-work disorder”, travel
no effect on REM sleep (good quality sleep!)

don’t work well for most

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22
Q

Ramelteon (Rozerem)

A

MISC. ANXIOLYTIC AND SEDATIVE-HYPNOTIC

melatonin-rec agonist
jet-leg, etc.

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23
Q

Zolpidem (Ambien)

A

MISC. ANXIOLYTIC AND SEDATIVE-HYPNOTIC

longer acting (6-8 hrs)

widely presc. sleep med
newer, even less effect on REM sleep (good!)

non-benzos, but benzo agonist, bind receptors
enhance GABA-stim Cl- influx

less anxiolytic, less musc relaxant

should be prescribed short term

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24
Q

Zaleplon (Sonata)

A

MISC. ANXIOLYTIC AND SEDATIVE-HYPNOTIC

short acting (2-4 hrs)
help getting to sleep initially
or take in middle of night

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25
Q

Oxazepam (Serax)

A

Benzo

intermediate-acting
sleep aid
Hypnotic, Anxiolytic

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26
Q

Disulfiram (Antibuse)

A

etOH tx

inhibits of aldehyde dehydrogenase : blocks conversion of acetaldehyde to acetate
“acetaldehyde sickness”

*induces unpleasant rxn: flushing, ha, nausea, confusion
encourages abstinence

hepatotoxicity
also inhibits p450, drug interactions

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27
Q

Acamprosate (Campral)

A

etOH tx

decrease cravings for alcohol

may involve glutamate and GABA receptors, block NMDA receptors, stimulate GABA-A rec.

less potential for hepatoxicity than others

can use combo with naltrexone

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28
Q

Naltrexone (ReVIA)

A

etOH tx

long-acting opioid antagonist

reduce craving for alcohol in alcoholic

hepatotoxicity can make pain worse

other form: vivitrol: repo injection

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29
Q

Eszopiclone (Lunesta)

A

MISC. ANXIOLYTIC AND SEDATIVE-HYPNOTIC

longer acting (6-8 hrs)

act at benzo receptors (benzo agonist) but NOT benzos

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30
Q

action of these drugs

A

graded dose dep depression of CNS function

see graph

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31
Q

barbituate curve

A

steep curve, more potent than etOH

used to prescribe enough barb sleeping pills to kill someone

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32
Q

etOH curve

A

not v. potent, but steep response curve!

33
Q

benzo curve

A

produce graded effects earlier, but plateau, so less likely to cause death
safer

34
Q

benzo generalities

A

safer than Barbs, less likely to depr. resp. in OD

anticonvulsant for seizures

anxiolytic, acute panic/phobia disorders
GAD more tx by antideps

centrally acting musc. relaxant

35
Q

benzos mech of action

A

(benzo binding enhances GABA) GABA A receptors

influx of Cl—>hyper polarized–>less likely to reach AP

36
Q

barb mech of action

A

barbs also enhance GABA-med opening of Cl- channels
CAN ALSO open Cl- themselves (benzos can’t)
*dangerous

37
Q

what else enhances GABA stim. Cl- influx

A

etOH

(why etOH/benzos/barbs share similar effects and exhibit cross-tolerance) and benzos (ativan) can be used to suppress etOH withdrawal (cross-dependence)

38
Q

higher dose SEs

A

sedation drowsiness, lightheadedness (lower doses)

mental clouding, psychomotor impairment, ataxia
(drunk-like)

memory impairment: anterograde amnesia (new mem.)- good in benzos for unpleasant procedures

disinhibitions
used for date-rape

euphoria, hangover, rebound anxiety, mild resp. depression, tolerance, dependence

*teratogen

39
Q

rohypnol vs valium for date rape

A

rohypnol more soluble in drinks

40
Q

CNS side effects may be especially pronounced in ??

A

elderly patients

or OD

41
Q

if take valium (longer acting benzos) to sleep…

A

have “hangover effect” in morning

42
Q

may experience rebound anxiety

A

especially with short acting drugs such as triazolam (HALCION) or etOH

-perpetrates cycle of dependence

43
Q

one benzo that is more likely to cause respiratory depression?

also ??

A

midazolam (VERSED)
powerful, state of anesthesia

enhanced resp. depression when taken with other resp. depressors (opioids: narco, etc)

44
Q

tolerance develops rapidly to

A

sedative - hypnotic effects
i.e. to help sleep
decreasing effects, use short term for insomnia

45
Q

tolerance does not dev. as rapidly to

A

anxiolytic effect (good!)

get anxiety relief w.out as much sedation

46
Q

benzo dependence?

A

physical and psychological

47
Q

w.drawal symptoms

A

agitation, anxiety, irritability, insomnia, abdominal cramps, sweating, and seizures

48
Q

to avoid benzo withdrawal

A

gradually wean pt off drug by dec. dose by 10% every 2-3 days for 2-3 wks

49
Q

very serious benzo w/drawal symptoms

A

delerium, tremors

grand mal seizures (may be status epilepticus)

life-threatening–>tx!

50
Q

if dependent on short acting drug

if dep. on longer acting drug

A

withdrawal syndrome will tend to be fairly intense, but of a short duration (e.g. 1-5 days)

less intense, but 5-30 days

51
Q

benzos and preggos

A

don’t use! possible teratogenicity

52
Q

benzo effect on sleep

A

decrease sleep latency (time needed to fall asleep)

increase time spent in stage 2 non-REM sleep

dec. time spent in REM sleep (but we need some!)–>so decreases quality of sleep

“REM rebound” when go off benzos: crazy dreams

53
Q

drug suppresses REM sleep the most

A

etOH (poor quality sleep)

then barbs

then benzos

54
Q

diazepam has to undergo

A

Phase 1 oxidative metabolism–>long lived active metabolites
longer acting drugs

then Phase 2: conjugated to glucuronide and excreted

*not easy for alcoholic (liver failure) pts to get rid of–>toxicity

55
Q

some benzo metabolites

A

are active!

may be even harder to get rid of

56
Q

lorazepam and oxazepam are directly

A

conjugated to glucuronide and excreted (no Phase 1: oxidation)
*better for liver failure pts

57
Q

drugs that can inhibit the oxidative metabolism of benzos–>prolong action

A

Cimetidine (Tagamet)
disulfiram (antabuse)
INH

58
Q

benzos can inc. serum levels of

A

digoxin, and possibly phenytoin

59
Q

barbs vs benzos

A

better anesthetic effect
anticonvulsants effects
more euphoric effect
respiration depression

60
Q

barbs are metabolized by

why drug interactions??

A

hepatic microsomal system

induction of microsomal enzymes–>potential for drug interactions

61
Q

barbs adverse effects

A

worse then benzos
GI upset, nausea
allergic reactions, skin

aggravation of acute intermittent porphyria–>induce hepatic enzymes involved in porphyrin synthesis
(vs. benzos: do not induce hepatic drug metabolizing enzymes)

62
Q

?? effects greatly reduced by phenobarbital

A

Warfarin

63
Q

barb abuse

A

?

64
Q

barb poisoning

A

suicide
CNS depression
tx symptomatically, no antidotes

65
Q

Buspirone (Buspar) 2

does not act thru ??

cannot be used for ??

A

newer drug, slower acting, 2-4 weeks!

does not act thru GABA mech, may be partial agonist at serotonin (5-HT)

WILL NOT suppress symps of etOH w.drawal, need to use benzos

better than benzos for long term alcoholic psych care
*don’t use benzos, too similar to etOH, trigger

66
Q

sedative/hypnotic SEs

A

CNS depression

REM rebound

67
Q

antihistamines sometimes used for

A

sedation

*Hydroxyzine (ATARAX, VISTARIL)
*promethazine (PHENERGAN)
diphenhydramine(benadryl)

68
Q

propranolol

A

B-blocker
used for anxiolytic affects
-dec. HR, HTN, etc
-helps “stage fright”

69
Q

etOH metabolism in liver

A

90%

zero order kinetics: constant rate, independent of concentration

metabolized @ 7-10 g/hour

alcohol dehydrogenase pathway
microsomal etOH oxidizing system (MEOS)

70
Q

alcohol dehydrogenase pathway

A

etOH + NAD–>acetaldehyde*

*excess accumulation may be toxic

71
Q

MEOS

A

etOH + NADPH–>acetaldehyde

low doses: most by etOH dehydrogenase pathway

  • this pathway used more @ higher doses and induced w. chronic consumption
  • tolerance and drug interactions
72
Q

aldehyde metabolism

A

acetaldehyde–>acetate–>H2O + CO2

via aldehyde dehydrogenase
*inhibited by disulfiram

some Asians have lower levels aldehyde dehydrogenase

73
Q

etOH probs

A

N/V, e-lyte abnormalities

sleep probe

resp. depression

CV: flushing, warmth, HTN, cardiomyopathies, arrhythmias

74
Q

hangovers from ??

A
acetaldehyde buildup
alcohol analogs present in beverages
metabolic changes and dehydration resulting from acute alcohol
intoxication
pharmacodynamic changes in the brain
75
Q

benefits of drinking

A

mod use (1-2 drinks/day) shown to inc. conc. of HDL, dec. LDL

76
Q

etOH withdrawal: onset, duration

mild?

severe?

A

6-24 hrs after last drink, typ. resolve in 5 days

mild: anxiety, irritability, insomnia, nausea, sweating, tachycardia, palpitations, hypertension.
severe: anxiety, fear, hallucinations (alcohol hallucinosis), delirium, tremors (delirium tremens), grand mal seizures, hypertension, tachycardia, arrhythmias *emergency

77
Q

etOH withdrawal tx

antipsychotics?

A

benzos: diazepam, lorazepam, and oxazepam

phenytoin (dilantin) to control seizures

no anti psychs, make seizures worse

*clonidine for ANS/CV effects

vitamins

78
Q

goal etOH withdrawal tx

A

prevent seizures, delirium, arrythmias

79
Q

general use of benzos

A
anxiety
sedative-hypnotics
acute etOH w.drawal
convulsive seizure, status epilepticus
skel musc spasms
preanesthetic med and supplement
induction of anesthesia