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Pharm > antianxiety, relaxants, sedative hypnotics, etOH > Flashcards

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
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 ```

Pharm (45 decks)

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