Sedatives/benzo/alcohol & Antipsychotics

Front 1

Benzodiazepines

Back 1

1. Alprazolam (Xanax)
2. Chlordiazepoxide (Librium)
3. Diazepam (Valium)
4. Lorazepam (Ativan)
5. Midazolam (Versed)
6. Ozazepam (Serax)
7. Temazepam (Restoril)
8. Triazolam (Halcion)

Front 2

Benzodiazepine Antagonist

Back 2

Flumazenil (Romazicon)

Front 3

Barbiturates

Back 3

1. Butalbital (Fiorinal)
2. Pentobarbital (Nembutal)
3. Phenobarbital
4. Thiopental (Pentothal)

Front 4

Centrally Acting Muscle Relaxants

Back 4

1. Baclofen (Lioresal)
2. Cyclobenzaprine (Flexeril)
3. Diazepam (Valium)
4. Metaxalone (Skelaxin)
5. Tizanidine (Zanaflex)

Front 5

Miscellaneous Anxiolytics and Sedative Hypnotics

Back 5

1. Alcohol
2. Buspirone (Buspar)
3. Eszopiclone (Lunesta)
4. Gammahydroxybutyrate (GHB)
5. Melatonin
6. Ramelteon (Rozerem)
7. Zolpidem (Ambien)
8. Zaleplon (Sonata)

Front 6

Drugs for Treatment of Alcoholism

Back 6

1. Disulfiram (Antibuse)
2. Acamprosate (Campral)
3. Naltrexone (ReVIA)

Front 7

Therapeutic Effects of Benzodiazepines

Back 7

1. Anxiolytic effect
2. Sedative-hypnotic effect
3. Anticonvulsant effect
4. Muscle relaxation

Front 8

Mechanism of Action of Benzodiazepines and Barbiturates

Back 8

*enhance the effects of the inhibitory neurotransmitter GABA
*interaction of GABA with its receptor causes the chloride channel to open
*influx of chloride which decreases neuronal firing

Front 9

ADRs of Benzodiazepines

Back 9

1. Sedation, drowsiness
2. mental clouding, confusion, slurred speech
3. memory impairment (anterograde amnesia
4. Disinhibition of suppressed behavior
5. possible teratogenicity

Front 10

CNS ADRs of Benzodiazepines

Back 10

1. Euphoria
2. Hangover
3. Rebound anxiety
4. Respiratory depression
5. Toerance
6. Dependence

Front 11

Withdrawal syndrome of benzodiazepines

Back 11

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

Front 12

Effects of Benzodiazepines of Sleep

Back 12

1. Decreased Sleep latency (time needed to fall asleep)
2. Some decrease in duration of REM sleep
3. REM Rebound = increase in REM sleep which leads to increased frequency and intensity of bizarre or frightening dreams

Front 13

Effects of Alcohol and Barbiturates on sleep

Back 13

Very poor quality of sleep = decrease in duration of REM sleep

Front 14

Lorazepam

Back 14

Benzodiazepine not oxidized in the liver and only goes through phase 2 metabolism

Front 15

Diazepam and Chlordiazepoxide

Back 15

Benzodiazepines oxidized in the liver to form active metabolites that tend to have longer durations of action

Front 16

Uses of Benzodiazepines

Back 16

1. treatment of Anxiety
2. sedative-hypnotic agents
3. treatment of acute alcohol withdrawal
4. treatment of convulsive seizures and status epilepticus
5. relief of skeletal muscle spasm and spasticity
6. preanesthetic medication and as an anesthetic supplement
7. induction of anesthesia

Front 17

Major Drug Interactions with Benzodiazepines

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1. Alcohol and CNS depressants
2. Cimetidine
3. Disulfiram
4. Isoniazid
5. Digoxin

Front 18

Short Acting Benzos

Back 18

1. Midazolam
2. Triazolam

Front 19

Intermediate Acting Benzos

Back 19

1. Temazepam
2. Oxazepam
3. Lorazepam
4. Alprazolam

Front 20

Long Acting Benzos

Back 20

1. Chlordiazepoxide
2. Diazepam

Front 21

Long Acting Barbiturates = anticonvulsants

Back 21

1. Phenobarbital

Front 22

Intermediate/Short Acting Barbiturates = sedative/hypnotics

Back 22

1. Pentobarbital
2. Butalbital

Front 23

Ultra Short Acting = induction of anesthesia

Back 23

1. Thiopental

Front 24

Have some ability to cause opening of the Chloride channels without GABA

Back 24

Barbiturates

Front 25

Pharmacokinetics of Barbiturates

Back 25

1. redistribution is important for the termination of action
2. induction of microsomal enzymes = drug interactions

Front 26

ADRs of Barbiturates

Back 26

1. sedation, drowsiness, confusion
2. hangover effect
3. respiratory depression
4. nausea/GI upset
5. aggravation of acute intermittent porphyria

Front 27

Drug Interactions with Barbiturates

Back 27

1. CNS depressants
2. MAO inhibitors
3. Warfarin

Front 28

Uses of Barbiturates

Back 28

1. sedative/hypnotics and anxiolytics
2. induction of surgical anesthesia
3. induction of coma after head injuries
4. anticonvulsants
5. adjuncts for treatment of tension headache

Front 29

Signs of Barbiturate Withdrawal

Back 29

insomnia, anxiety, restlessness, irritability, tremors, EEG changes

Front 30

Barbiturate Poisoning

Back 30

severe CNS depression (coma and depressed respiration) can lead to hypotension, shock, and circulatory collapse

Front 31

Treatment of Barbiturate Poisoning

Back 31

No specific antidotes so it is symptomatic (ventilation and hydration)

Front 32

Buspirone (Buspar)

Back 32

alleviates mild-moderate anxiety with minimal sedative-hypnotic, muscle relaxant, or respiratory depressant effects

Front 33

Drug of choice for treatment of anxiety in patient with a history of alcohol or sedative abuse

Back 33

Buspirone (Buspar)

Front 34

Side effects of Buspirone (Buspar)

Back 34

dizziness, headache, irritability, tachycardia but are relatively safe

Front 35

Mechanism of action of Zolpidem (Ambien), Zaleplon (Sonata), and Eszopiclone (Lunesta)

Back 35

NOT A BENZO, but acts at BENZO receptor
enhance the effects of GABA at the benzodiazepine receptor-chloride channel complex by interacting with a subtype

Front 36

Lowest Tendency of decreasing REM sleep

Back 36

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

Front 37

Duration of action of Zolpidem and Eszopiclone

Back 37

6-8 hours

Front 38

Duration of Action of Zaleplon

Back 38

2-4 hours

Front 39

Side effects of Zolpidem, Zaleplon, Eszopiclone

Back 39

*PERFORMING COMPLEX BEHAVIORS WHILE SLEEPING*
sedation, amnesia, impaired cognitive and motor function

Front 40

Gammahydroxybutyrate (GHB)

Back 40

analog of GABA that can cross the BBB

Front 41

Medication that has been abused by athletes

Back 41

Gammahydroxybutyrate (GHB)

Front 42

Antihistamines used as mild sedatives

Back 42

1. Hydroxyzine (Atarax, Vistaril)
2. Promethazine (Phenergan)

Front 43

Antihistamine used in over the counter sleep aids

Back 43

1. diphenhydramine

Front 44

Melatonin and Ramelteon (Rozerem)

Back 44

used for sleep aid that help regulate circadium rhythm and have little potential for abuse or dependence

Front 45

Beta Blockers used for use of anxiety

Back 45

Propranolol = situational anxiety(stage fright)

Front 46

Flumazenil (Romazicon)

Back 46

Benzodiazepine antagonist used to reverse the CNS depressant effects of Benzos

Front 47

ADRs of Flumazenil (Romazicon)

Back 47

1. can trigger seizures
2. can precipitate symptoms of withdrawal

Front 48

Use of Diazepam (Valium)

Back 48

treating spasticity and muscle spasms

Front 49

Baclofen (Lioresal)

Back 49

analog of GABA that acts as an agonist at certain types of GABA receptors (GABAb)

Front 50

Uses of Baclofen (Lioresal)

Back 50

treat spasticity from multiple sclerosis, spinal cord injuries, etc

Front 51

ADRs of Baclofen (Lioresal)

Back 51

1. CNS depression = sedation, drowsiness, ataxia
2. euphoria
3. hallucinations
4. tremors
5. seizures

Front 52

Cyclobenzaprene (Flexeril) and Metaxalone (Skelaxin)

Back 52

structurally related to the tricyclic antidepressant that inhibits both gamma and alpha motor systems

Front 53

uses of cyclobenzaprene (Flexeril) and Metaxalone (Skelaxin)

Back 53

treat muscle spasms of local origin (strains, pulls)

Front 54

ADRs of cyclobenzaprene (Flexeril) and Metaxalone (Skelaxin)

Back 54

CNS depression (sedation, drowsiness) and anticholinergic effects

Front 55

Absorption of alcohol (ethanol)

Back 55

passive diffusion from the stomach and small intestine

Front 56

where is alcohol distributed to in the body

Back 56

body water

Front 57

2 forms of alcohol metabolism

Back 57

1. Alcohol Dehydrogenase Pathway
2. Microsomal Ethanol Oxidizing System

Front 58

Alcohol oxidation occurs where? Alcohol oxidation follows what kinetics?

Back 58

1. liver
2. zero order kinetics

Front 59

the average adult can metabolize how much alcohol?

Back 59

1 drink per hour

Front 60

Main course of alcohol metabolism at lower doses of alcohol

Back 60

alcohol dehydrogenase pathway

Front 61

at higher doses and with chronic consumption what is the main course of alcohol metabolism

Back 61

Microsomal ethanol oxidizing system

Front 62

Disulfiram (Antabuse)

Back 62

inhibitor of aldehyde dehydrogenase that blocks the conversion of acetaldehyde to acetate

Front 63

Signs that patient on Disulfiram (Antabuse) has consumed alcohol

Back 63

flushing, headache, nausea, and confusion

Front 64

Important side effect with Disulfiram (Antabuse) and Naltrexone (ReVia)

Back 64

hepatotoxicity

Front 65

Effects of alcohol on the CNS

Back 65

1. first - stimulator = confident, social, outgoing
2. impairs intellectual and motor function
3. anterograde amnesia

Front 66

Effects of alcohol on sleep

Back 66

Reduces sleep latency, reduces amount of time spent in REM sleep, and decreases overall quality of sleep

Front 67

Possible alcohol biomarker used to see if alcohol is still in system up to 4-5 days later

Back 67

Alcohol Glucuronide

Front 68

Mechanism of Action of alcohol in the CNS

Back 68

enhanced effects of GABA at the GABA receptor-chloride channel complex

Front 69

Cardiovascular effects of alcohol

Back 69

1. cutaneous vasodilation - warm flushing and feel warm
2. severe intoxication - cardiomyopathy, arrythmias, HTN

Front 70

Other actions of Alcohol

Back 70

1. inhibits secretion of ADH
2. stimulates gastric acid secretion
3. can increase HDL and lower LDL
4. small amounts - suppress appetite

Front 71

Effects of alcohol on the liver

Back 71

1. induces microsomal drug metabolizing system
2. accumulation of fat
3. inflammation, scarring, cirrhosis

Front 72

Characterizations of fetal alcohol syndrome

Back 72

1. microcephaly
2. mental retardation
3. poor coordination
4. flattened face

Front 73

Alcohol Withdrawal Syndrome

Back 73

1. 6-24 hours after alcohol is stopped and resolves within 5 days
2. mild = anxiety, irritability, insomnia, nausea, sweating
3. severe = anxiety, fear, hallucinations, delirium, tremors
*Can be serious, or life threatening

Front 74

Management of Alcohol Withdrawal Syndrome

Back 74

1. prevent seizures, delirium, arrhythmias
2. Benzos suppress symptoms (lorazepam, oxazepam)
3. phenytoin for seizures

Front 75

Use of Clonidine in alcohol withdrawal syndrome

Back 75

alleviate some of the autonomic effects

Front 76

Naltrexone (ReVia)

Back 76

long-acting opioid antagonist that reduces the craving for alcohol

Front 77

Acamprosate (Campral)

Back 77

newer drug approved to decrease craving for alcohol and to help maintain abstinence in recovering alcoholics

Front 78

main side effects of Acamprosate (Campral)

Back 78

diarrhea, anxiety, insomnia, depression
*less potential for hepatotoxicity*

Front 79

Phenothiazines

Back 79

1. Chlorpromazine (Thorazine)
2. Fluphenazine (Prolixin)
3. Prochlorperazine (Compazine)
4. Trifluorperazine (Stelazine, Suprazine)

Front 80

Nonphenothiazines (Butyrophenones)

Back 80

Haloperidol (Haldol)

Front 81

Second Generation or Atypical Antipsychotics

Back 81

1. Clozapine (Clozaril)
2. Olanzapine (Zyprexa)
3. Risperidone (Risperdal)
4. Aripiprazole (Abilify)
5. Quetiapine (Seroquel)
6. Ziprasidone (Geodon)

Front 82

Antipsychotic effects

Back 82

1. alleviate psychotic symptoms
2. effects develop slowly over 2-4 weeks
3. usually no tolerance
4. usually unpleasant

Front 83

Sedation of effects of Antipsychotics

Back 83

1. occurs early in therapy
2. tolerance after a few weeks

Front 84

Pharmacological effects of Antipsychotics

Back 84

1. Antipsychotic
2. Sedation
3. Lower seizure threshold
4. Antiemetic
5. Anticholinergic
6. Cardiovascular
7. Weight gain
8. Inhibit ejactulation, Calcium process

Front 85

greater effect against "positive" symptoms of schizophrenia

Back 85

Chlorpromazine and other "first generations"

Front 86

Antiemetic used to desensitize CTZ and controls nausea and vomiting

Back 86

prochlorperazine (Compazine)

Front 87

Cardiovascular effects of Antipsychotics

Back 87

1. orthostatic hypotension
2. tachycardia
3. EKG changes
4. cardiac arrest and sudden death (older drugs have Black Box Warning)

Front 88

Toxic effects of Antipsychotics

Back 88

1. Idiosyncratic and allergic reactions
2. Neurological Side effects

Front 89

Neurological Side effects with Antipsychotics (EPS)

Back 89

1. Acute dystonia
2. Akathisia
3. Parkinsonism
4. Neuroleptic Malignant Syndrome(NMS)
5. Tardive dyskinesia

Front 90

Acute dystonia

Back 90

1. bizarre muscle spasms, facial grimacing, twitching
2. onset is early
3. Remove drug or add anticholinergic

Front 91

Akathisia

Back 91

1. need to be in motion, fidgeting, packing
2. onset is early
3. remove drug, add anticholinergic or propranolol/benzo

Front 92

Parkinsonism

Back 92

1. tremor and muscular rigidity
2. onset is early
3. remove drug or add anticholinergic

Front 93

Neuroleptic Malignant Syndrome (NMS)

Back 93

1. stupor, severe rigidity, hyperthermia - can be fatal
2. early in therapy and can persist for weeks
3. use Dantrolene or bromocryptine

Front 94

Dantrolene (Dantrium)

Back 94

*Treats Neuroleptic Malignant Syndrome*
inhibits the release of Calcium from the sarcoplasmic reticulum

Front 95

Bromocryptine (Parlodel)

Back 95

*Treats Neuroleptic Malignant Syndrome*
a dopamine agonist

Front 96

Tardive dyskinesia

Back 96

1. involuntary movements - sucking of lips, jaw movements, protrusion of tongue
2. develops after long term therapy
3. more common in females and elderly
4. No treatment

Front 97

Mechanism of Action of antipsychotics

Back 97

1. some are antagonists at D2 receptors
2. some are antagonists at the 5HT receptors
3. some do a little of both

Front 98

Trifluorperazine (Stelazine)

Back 98

*Piperazine Phenothiazine*
1. more potent than chlorpromazine
2. less sedation and anticholinergic
3. more EPS

Front 99

Fluphenazine

Back 99

*Piperazine Phenothiazine*
1. long acting form can be given by depot injection every 3-4 weeks
2. high EPS

Front 100

Prochlorperazine

Back 100

*Piperazine Phenothiazine*
1. antipsychotic used as an antiemetic

Front 101

Haloperidol

Back 101

*Butyrophenone*
1. less anticholinergic activity
2. more EPS
3. less sedation
4. long acting form as injection

Front 102

Clozapine

Back 102

*2nd Generation*
1. block mesolimbic DA receptors and also 5HT2 receptors
2. strong anticholinergic activity and FEW EPS
3. useful in patients who don't respond to other drugs

Front 103

Black Box Warning for Clozapine

Back 103

Potential to cause granulocytopenia and agranulocytosis

Front 104

Common side effects of all 2nd generation antipsychotics

Back 104

1. weight gain
2. hyperglycemia
3. type 2 diabetes

Front 105

Olanzapine

Back 105

*2nd Generation*
1. may cause EPS
2. approved for treatment of schizophrenia and mania

Front 106

Risperidone

Back 106

*2nd Generation*
1. blocks DA and 5HT receptors
2. less EPS than older drugs but more than clozapine and olanzapine
3. most widely used

Front 107

Quetiapine & Ziprasidone

Back 107

*2nd Generation*
1. effective against both positive and negative symptoms
2. very low chance of EPS
3. fairly expensive and less efficacious

Front 108

2nd generation antipsychotic that has fewer metabolic complications

Back 108

Ziprasidone

Front 109

Clinical Uses of Antipsychotics

Back 109

1. Psychosis - schizophrenia
2. Other psychoses (severe acute mania, bipolar)
3. Tic Disorders
4. Antiemetic
5. Intractable hiccup

Front 110

Higher potency drugs (trifluoperazine, fluphenazine, haloperidol)

Back 110

produce fewer cardiovascular and anticholinergic side effects but more EPS

Front 111

Lower Potency drugs

Back 111

produce more cardiovascular and anticholinergic side effects but less EPS