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Goldberg Chapter 9 
Sedative-Hypnotic Drugs
• Drugs that slow activity in the central nervous system 
• Include prescription drugs 
• To treat anxiety: sedatives 
• To treat insomnia: hypnotics 
• Alcohol is the most widely used depressant 
• Benzodiazepines are the most widely prescribed 
depressants
A. True 
B. False 
True 
48% 
False 
52%
• Chloral hydrate 1832 
• Paraldehyde 1882 
• Bromides 1960s
A. True 
B. False 
True 
52% 
False 
48%
• Veronal was introduced in 1903 
• Barbiturates classifications 
• Short-acting 
• Pentobarbital, secobarbital 
• Intermediate-acting 
• Amobarbital, butabarbital 
• Long-acting 
• Mephbarbital, phenobarbital
A. True 
B. False 
True 
7% 
False 
93%
• Sodium Pentathol 1934 
• Meprobamate 1950s 
• Methaqualone 1965 
• Great risk for physical and 
psychological dependence
A. True 
B. False 
True 
69% 
False 
31%
• 1960 introduced chordiazepoxide (Librium) 
• 1970s introduced diazepam (Valium) 
• Dependence and overdose can occur 
• Rarer than with barbiturates 
• More common in combination with alcohol 
• Rohypnol
A. True 
B. False 
True 
21% 
False 
79%
• Benzodiazepines and 
barbiturates 
• Enhance inhibitory effects of GABA 
• Non-benzodiazepine hypnotics 
• Selectively target the GABA-A receptor 
• Work better as sleep aids rather than anti-anxiety 
medications 
• Zolpidem (Ambien), zaleplon (Sonata), 
eszopiclone (Lunesta)
A. True 
B. False 
True 
15% 
False 
85%
• Anxiolytics 
• Sleeping agents 
• Anticonvulsants 
• Dependence 
• Tolerance & Cross 
Tolerance 
• Withdrawal 
• Toxicity 
• Behavioral 
• Physiological 
• Patterns of abuse
A. True 
B. False 
True 
82% 
False 
18%
• High-dose exposure causes 
intoxication 
• Examples: 
• Volatile solvents 
• Aerosols, propellants, gases 
• Anesthetics 
• Nitrites 
http://www.youtube.com/watch?v=3g99h4qaCio
A. True 
B. False 
True 
67% 
False 
33%
A. True 
B. False 
True 
4% 
False 
96%
• Most abusers are very young 
• Abuse tends to occur as localized fads 
• Dangers: 
• Kidney damage 
• Brain damage 
• Peripheral nerve damage 
• Irritation of respiratory tract 
• Severe headache 
• Death by suffocation
• Naturally occurring chemical found in brain and body 
• Similar to GABA 
• Causes CNS depression 
• Has been used as an anesthetic 
• Considered a date-rape drug 
• Along with Rohypnol and Ketamine 
• GHB is listed on Schedule I 
https://www.youtube.com/watch?v=LPtcU_8yv 
R4

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SOC 204 Goldberg Chapter 9 Sedative-Hypnotic Drugs

  • 1. Goldberg Chapter 9 Sedative-Hypnotic Drugs
  • 2. • Drugs that slow activity in the central nervous system • Include prescription drugs • To treat anxiety: sedatives • To treat insomnia: hypnotics • Alcohol is the most widely used depressant • Benzodiazepines are the most widely prescribed depressants
  • 3. A. True B. False True 48% False 52%
  • 4. • Chloral hydrate 1832 • Paraldehyde 1882 • Bromides 1960s
  • 5. A. True B. False True 52% False 48%
  • 6. • Veronal was introduced in 1903 • Barbiturates classifications • Short-acting • Pentobarbital, secobarbital • Intermediate-acting • Amobarbital, butabarbital • Long-acting • Mephbarbital, phenobarbital
  • 7. A. True B. False True 7% False 93%
  • 8. • Sodium Pentathol 1934 • Meprobamate 1950s • Methaqualone 1965 • Great risk for physical and psychological dependence
  • 9. A. True B. False True 69% False 31%
  • 10. • 1960 introduced chordiazepoxide (Librium) • 1970s introduced diazepam (Valium) • Dependence and overdose can occur • Rarer than with barbiturates • More common in combination with alcohol • Rohypnol
  • 11. A. True B. False True 21% False 79%
  • 12. • Benzodiazepines and barbiturates • Enhance inhibitory effects of GABA • Non-benzodiazepine hypnotics • Selectively target the GABA-A receptor • Work better as sleep aids rather than anti-anxiety medications • Zolpidem (Ambien), zaleplon (Sonata), eszopiclone (Lunesta)
  • 13. A. True B. False True 15% False 85%
  • 14. • Anxiolytics • Sleeping agents • Anticonvulsants • Dependence • Tolerance & Cross Tolerance • Withdrawal • Toxicity • Behavioral • Physiological • Patterns of abuse
  • 15. A. True B. False True 82% False 18%
  • 16. • High-dose exposure causes intoxication • Examples: • Volatile solvents • Aerosols, propellants, gases • Anesthetics • Nitrites http://www.youtube.com/watch?v=3g99h4qaCio
  • 17. A. True B. False True 67% False 33%
  • 18. A. True B. False True 4% False 96%
  • 19. • Most abusers are very young • Abuse tends to occur as localized fads • Dangers: • Kidney damage • Brain damage • Peripheral nerve damage • Irritation of respiratory tract • Severe headache • Death by suffocation
  • 20. • Naturally occurring chemical found in brain and body • Similar to GABA • Causes CNS depression • Has been used as an anesthetic • Considered a date-rape drug • Along with Rohypnol and Ketamine • GHB is listed on Schedule I https://www.youtube.com/watch?v=LPtcU_8yv R4

Editor's Notes

  1. Depressants = drugs that slow activity in the central nervous system Include prescription drugs that treat anxiety (sedatives) and insomnia (hypnotics) As a group, also called sedative-hypnotics Alcohol is the most widely used depressant Benzodiazepines are the most widely prescribed depressants
  2. Chloral hydrate (“knockout drops,” “Mickey Finn”) Synthesized in 1832; used clinically in 1870 Induces sleep in less than an hour Abuse leads to gastric irritation Paraldehyde Synthesized in 1829; used clinically in 1882 Effective with a wide safety margin Noxious taste and odor Bromides Widely used as a sleep agent in patent medicines; appeared in OTC drugs through the 1960s Can accumulate in the body and cause toxic effects
  3. Discovery/introduction 1903: Barbital (Veronal) became the first barbiturate to be used clinically Other popular barbiturates include phenobarbital, amobarbital and secobarbital Grouped on the basis of the time of onset and duration of activity Low-dose, long-acting forms used for daytime relief of anxiety Higher-dose, shorter-acting forms used to induce sleep Short-acting (pentobarbital, secobarbital) Time of onset: 15 minutes Duration of action: 2 to 3 hours Intermediate-acting (amobarbital, butabarbital) Time of onset: 30 minutes Duration of action: 5 to 6 hours Long-acting (mephobarbital, phenobarbital) Time of onset: 1 hour Duration of action: 8 hours or longer
  4. Doubled in the last 15 years
  5. Sodium Pentathol Ultra-short acting barbiturate Administered intravenously Used as an anesthetic for brief surgical procedures Moves very rapidly into the brain Also used to make people relaxed and talkative (truth serum) Thiopental is currently the first of the three drugs administered for the death penalty Meprobamate The first modern antianxiety agent (anxiolytic) Widely prescribed beginning in the 1950s Like barbiturates, can produce psychological and physical dependence Still available as a prescription drug, although largely replaced by benzodiazepines Methaqualone 1965: Despite problems in other countries, methaqualone (Quaalude, Sopor) was introduced in the United States No initial monitoring- Package insert read “Addiction potential not established” Overprescribed; quickly became widely misused and abused 1973: Put on Schedule II 1985: Put on Schedule I
  6. 1960: Introduction of chlordiazepoxide (Librium), the first commercially marketed benzodiazepine Reduces anxiety without inducing sleep Much larger safety margin than barbiturates Physical dependence rare Overdose rare and usually only when combined with other depressants like alcohol 1970s: Diazepam (Valium), a lower-dose benzodiazepine, became for a time the best seller among all prescription drugs Benzodiazepines Dependence and overdose can occur; dosage and time course are critical factors Overdose deaths more likely for drugs sold in higher doses Psychological dependence more likely with drugs that have a rapid onset of effects Physical dependence more likely with drugs that have a short duration of action More differences among the barbiturates and among the benzodiazepines than there are between these two classes of drugs? Rhohypnol A 1990s’ version of a “Mickey Finn” Produces profound intoxication when mixed with alcohol Reports surfaced of the drug being slipped into drinks and used as a “date-rape” drug Changes in laws and in the formulation of the pills should reduce its abuse
  7. 37 for benzo, 34 for other illegal drugs
  8. Benzodiazepines and barbiturates Bond with brain receptors Enhance the normally inhibitory effects of GABA Nonbenzodiazepine hypnotics Selectively target the GABA-A receptor Seem to work better as sleeping pills than as antianxiety drugs Include zolpidem (Ambien), zaleplon (Sonata), and eszopiclone (Lunesta)
  9. Anxiolytics (anxiety-reducers) Sedatives often prescribed to reduce anxiety Four benzodiazepines (Xanax, Ativan, Klonopin, Valium) are among the top 100 most commonly prescribed medications in the United States Concerns about use of sedatives as anxiolytics: Some anxiety disorders respond to anxiolytics while others seem to be treated more effectively by antidepressants or behavior therapy Patients may take the drugs for long period Anxiolytics may be overprescribed Is a person taking the drug to treat a disorder or to feel better in a general way? As sleeping pills Taking a large enough dose of a hypnotic drug helps a person get to sleep more quickly Insomnia is a common complaint, although people sometimes overestimate its severity Today, fewer hypnotics are prescribed than in the past, and they are usually taken for only a few nights at a time Concerns about use as sleeping agents Hypnotics may induce tolerance, dependence, rebound insomnia, and “hangover” effects After 1976, benzodiazepines displaced barbiturates in the sleeping-pill market Safety issues raised that Halcion produces adverse psychiatric reactions in some patients Nonbenzodiazepine hypnotics Zolpidem (Ambien) binds selectively to GABA-A receptors Rapid onset and short duration of action Concern about people driving while still under the influence (from not allowing 8 hours of sleep after taking drug) Eszopiclone (Lunesta) Approved for long-term use Falling asleep w/o pills Have a regular sleep schedule When you go to bed, turn out the lights and relax Exercise regularly but not late in the evening Prepare a comfortable sleep environment in terms of temperature and noise Eat a light snack before bed Avoid tobacco use If you don’t fall asleep within 30 minutes, get up and do something relaxing before trying to fall asleep again Do not nap during the day Avoid chronic use of sleeping pills As anticonvulsants Barbiturates and benzodiazepines, in low doses or combined with other anticonvulsants, may be prescribed for seizure disorders (epilepsies) Potential problems Tolerance can make it difficult to find a dose that is effective but doesn’t cause excessive drowsiness Abrupt withdrawal is likely to cause seizures Dependence Psychological dependence—especially associated with short-acting barbiturates Physical dependence—potentially life-threatening withdrawal syndrome linked to large doses of sedative-hypnotics Barbiturate withdrawal: anxiety, insomnia, tremulousness, weakness, nausea and vomiting, seizures, disorientation, agitation, delusions, and visual and auditory hallucinations Benzodiazepine withdrawal is less severe: anxiety, irritability, or insomnia Cross-dependence occurs among the barbiturates, the benzodiazepines, and alcohol Toxicity Behavioral Alcohol-like intoxication with impaired judgment and coordination Increased risk of injury while driving or engaging in other activities Additive effects if combined with alcohol Physiological Respiratory depression Especially dangerous if combined with alcohol Patterns of abuse Most abuse associated with oral use of legally manufactured products Two types of typical abusers Older adults using prescription drug who develop tolerance and increase their dosage Younger people who obtain drugs to get high; may take high doses and/or mix with alcohol
  10. White, Hispanic, Asian, black
  11. Volatile solvents and other compounds used for intoxicating purposes Have depressant effects similar to sedative-hypnotics High-dose exposure causes intoxication, with effects similar to alcohol Products that can be abused by inhalation include gasoline, glue, paint, lighter fluid, spray cans, nail polish, correction fluid Volatile solvents (petroleum, acetone, toluene) Paint, paint thinner and remover, nail polish remover, correction fluid, glues, cements Overly informative news articles and education programs actually demonstrated how to abuse volatile solvents Abuse tends to occur as localized fads Most abusers are very young—solvents are readily available and inexpensive Aerosols, propellants, gases (butane, propane) Spray paint, hair spray, lighters, whipped cream Anesthetics (nitrous oxide, ether) Current and former medical anesthetics Nitrous oxide (“laughing gas”) was first used in the early 1800s Still used for light anesthesia, especially by dentists Used as a propellant for commercial and home whipping-cream dispensers Nitrites (isoamyl, isobutyl) “Locker room,” “Rush,” “poppers” Relaxes blood vessels which increases blood flow, but also lowers blood pressure. Used as a treatment for cyanide poisoning. With high doses there maybe lightheadedness or faintness Consumer Product Safety Commission has taken steps to remove poppers and other nitrites from the market since 1988
  12. Use has declined in recent years
  13. Kidney damage Brain damage Peripheral nerve damage Irritation of the respiratory tract Severe headache Death by suffocation
  14. Naturally-occurring chemical found in the brain and body Structurally similar to the inhibitory neurotransmitter GABA Causes CNS depression, especially when combined with alcohol Has been used as an anesthetic Behavioral effects similar to alcohol Lack of coordination and slurred speech Considered a date-rape drug Except for a specific formulation used to treat cataplexy, GHB is listed on Schedule I