Antianxiety Agents, Muscle Relaxants, Sedative Hypnotics And Alcohol

Front 1

A drug for treatment of alcoholism. Decreases cravings and helps maintain abstinence in recovering alcoholics. LESS potential for hepatotoxicity!

Back 1

Acamprosate (Campral)

Front 2

in this group of drugs (non-barbiturate and non-benzodiazepine) this one is not a CNS depressant. Low abuse potential! Does not act thru GABA mechanisms

Back 2

Buspirone (BUSPAR)

Front 3

selective in limbic system to relieve anxiety w/out depressing other CNS functions. Enhancing activated GABA receptors effect (which is inhibitory)

Back 3

benzodiazepines (barbiturate and alcohol have similar MOA)

Front 4

short acting benzodiazepine with rebound anxiety effect

Back 4

Triazolam (HALCION) vs longer acting Diazepam (VALIUM) or Flurazepam

Front 5

respiratory depression SE with this short acting benzodiazepine (used to induce or suplement anesthesia)

Back 5

Midazolam (VERSED)

Front 6

avoid benxodiazepines during pregnancy (esp first trimester)

Back 6

trouble falling asleep?->short acting Triazolam (HALCION) trouble staying asleep?->longer acting Diazepam (VALIUM)

Front 7

dreaming stage with Mixed EEG waves and considerable eyeball activity (25% of total sleep time, 2nd longest after NREM(45%))

Back 7

REM

btw: ba bat kst std d mixed(for REM)

Front 8

benzodiazepines and sleep stages

btw: ba bat kst std d mixed(for REM)

Back 8

decrease: sleep latency (falling asleep)
increase: stage 2 non-REM
decrease: duration of stages 3&4
decrease: number of awakenings

Front 9

short acting ?->rebound effect; long acting ? -> hangover effect

Back 9

benzodiazepams are metabolized by hepatic microsomal enzyme system, yet they do not induce drug metabolizing enzymes (unlike barbiturates)

Front 10

impaired liver function? use these benzodiazepines to tackle anxiety/seizures/spasticity/or to induce anestesia:

Back 10

Lorazepam and Oxazepam

Front 11

use of benzodiazepines

Back 11

treatment of anxiety (limbic),
reduce seizures (cortex), spasticity of skeletal m. (brain stem & spinal cord), induction of anesthesia (Midazolam (VERSED))

Front 12

prolong action of benzodiazepines (inhibit oxidative metabolism)

Back 12

Cimetidine (Tagamet) Disulfiram(Antabuse)

Front 13

Hypnotic benzadiazepines from short acting to long acting

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Triazolam, Temazepam, Oxazepam, Lorazepam, Flurazepan

benzodiazepines, (-lam, -pam, Chlordiazepoxide (LIBRIUM)-yes, active metabolite)

Front 14

suffics -tal ?

Back 14

barbiturate

Front 15

which of the benzodiazepines has active metabolites?

Back 15

Chlordiazepoxide

Front 16

long acting barbiturate, thus, it is used mainly as anticonvulsant

Back 16

Phenobarbital

Front 17

Intermediate/short acting barbiturate, thus used as sedative/hypnotic

Back 17

Butalbital, Pentobarbital

Front 18

ultra short acting barbiturates used in surgical anesthesia

Back 18

Thiopental

Front 19

in OD with barbiturates:

Back 19

depression of respiration

Front 20

Pharmacological effects of barbiturates are ANTICONVULSANT, general ANESTHETIC, EUPHORIA)

Back 20

Barbiturates- weak acids that quickly absorbed in GI and very lipid soluble (xBBB)... the more lipid soluble, the faster the onset and shorter duration

Front 21

oral anticoagulant Warfarin effects are...

Back 21

greatly reduced by induction of hepatic enzymes (which barbiturates (-tals) do but not benzodiazepines: Alprazolam (Xanax), Chlordiazepoxide (Librium), Diazepam (Valium), Midazolam (Versed), Ozazepam (Serax), Temazepam (Restoril), Triazolam (Halcion))

Front 22

treatment of hyperbilirubinemia in neonates or induction of coma following head injuries

Back 22

barbiturates: (-tal)

Front 23

SE of barbiturates abuse:

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grand mal seizures
delirium and hallucination
insomnia, tremors, EEG channges
vomiting
anxiety

Front 24

barbiturates OD... what's the antidote?

Back 24

symptomatic treatment (hydration, ventilation) no antidote

Front 25

newer Rx with fewer SE than benzodiazepines. Doesn't act thru GABA mechanisms. Partially agonizes at serotonin (5-HT1A) receptors

Back 25

Buspirone (BUSPAR), a non-benzodiazepine and non-barbiturate

very low abuse potential too!!!!!!!

Front 26

CYP 3A4 and cimetidine increase action of Buspirone (BUSPAR), a non-benzodiazepine and non-barbiturate

Back 26

microsomal inducers (P450 system) decrease bld levels of Buspirone (BUSPAR)

Front 27

newer non barbiturate/non benzodiazepine sedative-hypnotics

Back 27

Zolpidem (Ambien), Zaleplon (shorter acting) (Sonata) and Eszopiclone (Lunesta)

Front 28

Rx used for continuous sedation in ICU. IV administration. Very rapid onset and recovery

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Propofol (non barbiturate/non benzodiazepine )

Front 29

non barbiturate/non benzodiazepine "date rape" drug, also abused by athletes for enhancement of athletic performance

Back 29

Gammahydroxybutyrate (GHB) analog of GABA, x BBB

Hint 29

Easy Lay, Georgia Home Boy, Liquid X, Liquid Ecstasy, Cherry Meth

Front 30

treatment of situational anxiety (beta adrenergic blockers) eg "stage fright"

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Propranolol

Front 31

in OD with benzodiazepines to reverse CNS effects of benzodiazepines

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Flumazenil (ROMAZICON)

Front 32

ANALOG (not the same) of GABA, an agonist, acts in spinal cord to inhibit release of glutamate and aspartate. Treating spasticity in spinal cord injuries, multiple sclerosis, etc

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Baclofen (LIORESAL) Scott Abram;

fact: Diazepam (Valium) enhances presynaptic inhibition to facilitate GABA actions in the spinal cord

Front 33

Used in treating spasm of local origin (strains, pulls, etc). Acts on brainstem level and inhibits alpha and gamma motor systems

Back 33

Cyclobenzaprene (FLEXERIL) (Metaxalone (SKELAXIN) is similar muscle relaxant)

Front 34

skeletal musce relaxant. Can cause hypotension (alpha 2 agonist). very sedating.

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Tizanidine (ZANAFLEX) a centrally acting muscle relaxant

Front 35

what is a fatal level of blood alcohol?

Back 35

.3%-.4%

Front 36

alcohol oxidation: constant amount at constant rate. what is the kinetics order?

Back 36

ZERO

Front 37

what is a toxic product of alcohol dehydrogenase pathway? at lower doses this is the pathway used for alcohol metabolism

Back 37

acetaldehyde (can form abducts with proteins, leading to the inhibition of a variety of enzymes) Alcohol Dehydrogenase pathway

Front 38

this system kicks in with high and chronic alcohol consumption. Accounts for alcohol tolerance and drug interactions

Back 38

Microsomal Ethanol Oxidizing System (MEOS)

Front 39

blocks conversion of acetaldehyde to acetate (inhibits aldehyde dehydrogenase). Thus, increases acetaldehyde levels. Potentially hepatotoxic

Back 39

Disulfiram (ANTABUSE)

Front 40

main goal of reversing alcohol poisoning is?

Back 40

prevention of respiratory depression

Front 41

GABA binds its receptors, Cl- flows into cell, hyperpolarizes it and decreases neuronal firing!

Back 41

Nota bene the mechanism!

Front 42

fetal alcohol syndrome:

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microcephaly, mental retardation, poor coordination, FLATTENED face, joint abnormalities and heart defects

Front 43

for alcohol withdrawal

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benzodiazepines. For bad liver these benzodiazepines: Lorazepam (ATIVAN) and Oxazepam (SERAX)

Front 44

reduces cravings in alcoholics, yet hepatotoxicity is a side effect

Back 44

naltrexone (ReVia);
Clonidine can alleviate autonomic effects (tachycardia, HTN, etc)

Front 45

less hepatotoxic effects yet reduction in cravingsin alcoholics

Back 45

Acamprosate (CAMPRAL);
more effective is a combo of Naltrexone (ReVia) and Acamprosate (CAMPRAL)

Front 46

uses of barbiturates

Back 46

sedative-hypnotic, tension headache
surgical anastesia
induction of coma in head injuries
anticonvulsants (phenobarbital)
hyperbilirubinemia in neonates

Front 47

substitution at C5 (increasing chain length-> more lipid soluble); replacement of oxygen at C2 with sulfur->greater lipid solubility. What happens with duration of action in both cases?

Back 47

decreased duration of action

Front 48

has a "shallow" dose response curve, unlike barbiturates and ethanol

Back 48

Diazepam (VALIUM)

Front 49

increase digoxin serum levels ( and possibly phenytoin)

Back 49

barbiturates (-tal)

Front 50

additive effect with CNS depressants (alcohol, opioids, antihistamines, etc), oral anticoagulant effects reduced (Warfarin blocked), thus, clotting increased with..

Back 50

barbiturates -tals (utra short? Thiopental (PENTOTHAL))