antianxiety, relaxants, sedative hypnotics, etOH Flashcards Preview

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Flashcards in antianxiety, relaxants, sedative hypnotics, etOH Deck (79):
1

Alprazolam (Xanax)

Benzo

intermediate acting

anxiolytic

2

Chlordiazepoxide (Librium)

Benzo

long acting

Anxiolytic, Anticonvulsant, Withdrawal suppressant

3

Diazepam (Valium)

Benzo, Centrally acting musc. relaxant

long acting

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

4

Lorazepam (Ativan)

Benzo, Centrally acting musc. relaxant

intermediate acting

Hypnotic, Anxiolytic, Anesthesia supplement, Withdrawal suppressant

5

Midazolam (Versed)

Benzo

short-acting

Induction or supplement to anesthesia

6

Temazepam (Restoril)

Benzo

intermediate-acting

hypnotic

7

Triazolam (Halcion)

Benzo

short acting (good to help fall asleep)

hypnotic

8

Flumazenil (Romazicon)

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

9

Butalbital (Fiorinal)

BARBITURATE

for tension ha, centrally acting relaxant

10

Pentobarbital (Nembutal)

BARBITURATES

intermediate/short acting

sedative-hypnotics

11

Phenobarbital

BARBITURATES

long acting

tx for epilepsy, anticonvulsant

12

Thiopental (Pentothal)

BARBITURATES

ultra-short acting

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

13

Balcofen (Lioresal)

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

14

Cyclobenzaprine (Flexeril)

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

15

Diazepam (Valium)

CENTRALLY ACTING MUSCLE RELAXANT

muscle spasms

16

Metaxalone (Skelaxin)

CENTRALLY ACTING MUSCLE RELAXANT

17

Tizanidine (Zanaflex)

CENTRALLY ACTING MUSCLE RELAXANT

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

very sedating (take at night)

18

Alcohol

MISC. ANXIOLYTIC AND SEDATIVE-HYPNOTIC

anxiolytics, sedative, relaxant

19

Buspirone (Buspar)

MISC. ANXIOLYTIC AND SEDATIVE-HYPNOTIC

anti-anxiety, NO musc. relaxation, NOT sedating

20

Gammahydroxybutyrate (GHB)

MISC. ANXIOLYTIC AND SEDATIVE-HYPNOTIC

abused: party/club, date rape

GABA analog, crosses BBB

ergogenic effect: body building

21

Melatonin

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

22

Ramelteon (Rozerem)

MISC. ANXIOLYTIC AND SEDATIVE-HYPNOTIC

melatonin-rec agonist
jet-leg, etc.

23

Zolpidem (Ambien)

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

24

Zaleplon (Sonata)

MISC. ANXIOLYTIC AND SEDATIVE-HYPNOTIC

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

25

Oxazepam (Serax)

Benzo

intermediate-acting
sleep aid
Hypnotic, Anxiolytic

26

Disulfiram (Antibuse)

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

27

Acamprosate (Campral)

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

28

Naltrexone (ReVIA)

etOH tx

long-acting opioid antagonist

reduce craving for alcohol in alcoholic

*hepatotoxicity* can make pain worse

other form: vivitrol: repo injection

29

Eszopiclone (Lunesta)

MISC. ANXIOLYTIC AND SEDATIVE-HYPNOTIC

longer acting (6-8 hrs)

act at benzo receptors (benzo agonist) but NOT benzos

30

action of these drugs

graded dose dep depression of CNS function

see graph

31

barbituate curve

steep curve, more potent than etOH
used to prescribe enough barb sleeping pills to kill someone

32

etOH curve

not v. potent, but steep response curve!

33

benzo curve

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

34

benzo generalities

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

benzos mech of action

(benzo binding enhances GABA) GABA A receptors
influx of Cl--->hyper polarized-->less likely to reach AP

36

barb mech of action

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

37

what else enhances GABA stim. Cl- influx

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

higher dose SEs

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

rohypnol vs valium for date rape

rohypnol more soluble in drinks

40

CNS side effects may be especially pronounced in ??

elderly patients
or OD

41

if take valium (longer acting benzos) to sleep...

have "hangover effect" in morning

42

may experience rebound anxiety

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

-perpetrates cycle of dependence

43

one benzo that is more likely to cause respiratory depression?

also ??

midazolam (VERSED)
powerful, state of anesthesia

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

44

tolerance develops rapidly to

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

45

tolerance does not dev. as rapidly to

anxiolytic effect (good!)

get anxiety relief w.out as much sedation

46

benzo dependence?

physical and psychological

47

w.drawal symptoms

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

48

to avoid benzo withdrawal

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

49

very serious benzo w/drawal symptoms

delerium, tremors

grand mal seizures (may be status epilepticus)

life-threatening-->tx!

50

if dependent on short acting drug



if dep. on longer acting drug

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

benzos and preggos

don't use! possible teratogenicity

52

benzo effect on sleep

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

drug suppresses REM sleep the most

etOH (poor quality sleep)

then barbs

then benzos

54

diazepam has to undergo

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

some benzo metabolites

are active!
may be even harder to get rid of

56

lorazepam and oxazepam are directly

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

57

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

Cimetidine (Tagamet)
disulfiram (antabuse)
INH

58

benzos can inc. serum levels of

digoxin, and possibly phenytoin

59

barbs vs benzos

better anesthetic effect
anticonvulsants effects
more euphoric effect
respiration depression

60

barbs are metabolized by


why drug interactions??

hepatic microsomal system

induction of microsomal enzymes-->potential for drug interactions

61

barbs adverse effects

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

?? effects greatly reduced by phenobarbital

Warfarin

63

barb abuse

?

64

barb poisoning

suicide
CNS depression
tx symptomatically, no antidotes

65

Buspirone (Buspar) 2

does not act thru ??




cannot be used for ??

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

sedative/hypnotic SEs

CNS depression

REM rebound

67

antihistamines sometimes used for

sedation

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

68

propranolol

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

69

etOH metabolism in liver

90%

zero order kinetics: constant rate, independent of concentration

metabolized @ 7-10 g/hour

alcohol dehydrogenase pathway
microsomal etOH oxidizing system (MEOS)

70

alcohol dehydrogenase pathway

etOH + NAD-->acetaldehyde*

*excess accumulation may be toxic

71

MEOS

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

aldehyde metabolism

acetaldehyde-->acetate-->H2O + CO2

via aldehyde dehydrogenase
*inhibited by disulfiram

some Asians have lower levels aldehyde dehydrogenase

73

etOH probs

N/V, e-lyte abnormalities

sleep probe

resp. depression

CV: flushing, warmth, HTN, cardiomyopathies, arrhythmias

74

hangovers from ??

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

75

benefits of drinking

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

76

etOH withdrawal: onset, duration



mild?




severe?

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

etOH withdrawal tx






antipsychotics?

benzos: diazepam, lorazepam, and oxazepam

phenytoin (dilantin) to control seizures

no anti psychs, make seizures worse

*clonidine for ANS/CV effects

vitamins

78

goal etOH withdrawal tx

prevent seizures, delirium, arrythmias

79

general use of benzos

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