2. Sedative-Hypnotic Drugs (depressants)
• Drugs that slow activity in the central nervous system
• Include prescription drugs
o To treat anxiety: sedatives
o To treat insomnia: hypnotics
• Alcohol is the most widely used depressant
• Benzodiazepines are the most widely prescribed
depressants
3. The nonmedical use of
controlled medications by
adolescents is increasing.
A. True
B. False
True
False
4%
96%
4. Sedative-Hypnotic Drugs
• Sedative-hypnotic drugs are central nervous
system depressants that produce relaxing to
sleep-inducing effects
• Three main types of
sedative-hypnotic
drugs:
o Barbiturates
o Nonbarbiturate sedatives
o Minor tranquilizers
5. Classification
• Classified based on potency and the length of time they
act:
o Ultra-short-acting
o Short-acting (less than 4 hours)
o Intermediate-acting (4 to 6 hours)
o Long-acting (more than 6 hours)
• Drugs that take effect rapidly
have a higher abuse potential
than slow-acting drugs
6. Sedative-Hypnotic Drugs
A. Increase energy
B. Depress the CNS
C. Are very quick-acting
D. Have little potential for
abuse
IncreaseenergyDepressthe
CNS
Are
very
quick-acting
Havelittle
potentialfor...
8% 4%
16%
72%
7. Effects
• Produce a depressed, mood-altering action on the
central nervous system – act on GABA
• Slow activity of the cardiovascular, muscular and
respiratory systems
• Can cause confusion, inadequate emotional control,
slurred speech, poor judgment, and intoxication
8. Medical Uses
• Used primarily to treat
o Anxiety
o Insomnia
o Convulsive disorders
• Short-acting barbiturates
continue to be used for
anesthetic purposes
9. Mechanisms of Action
• Benzodiazepines and
barbiturates
o Enhance inhibitory effects of GABA
• Non-benzodiazepine hypnotics
o Selectively target the GABA-A receptor
o Work better as sleep aids rather than anti-anxiety
medications
o Zolpidem (Ambien), zaleplon (Sonata),
eszopiclone (Lunesta)
10. Medical uses for barbiturates
do NOT include:
A. Treating
depression
B. Reducing anxiety
C. Controlling
seizures
D. Inducing sleep Treatingdepression
Reducing
anxietyControllingseizures
Inducingsleep
54%
38%
8%
0%
11. Non-barbiturate Sedatives
• Older drugs with similar actions to barbiturates
• With the advent of safer drugs, rarely used now
• Chloral hydrate 1832
• Paraldehyde 1882
• Bromides 1960s
12. Adolescent boys are more likely to
give medications to their friends than
adolescent girls.
A. True
B. False
True
False
0%0%
13. Barbiturates
• Veronal was introduced in 1903
• Barbiturates classifications
o Short-acting
• Pentobarbital, secobarbital
o Intermediate-acting
• Amobarbital, butabarbital
o Long-acting
• Mephbarbital, phenobarbital
14. Barbiturates, continued
• Sodium Pentathol 1934
• Meprobamate 1950s
• Methaqualone 1965
• Great risk for physical and
psychological dependence
• Produce a depressed, mood-altering
action on the central nervous system
– act on GABA
• Slow activity of the cardiovascular,
muscular and respiratory systems
• Can cause confusion, inadequate
emotional control, slurred speech,
poor judgment, and intoxication
16. Benzodiazepines
• 1960 introduced chordiazepoxide (Librium)
• 1970s introduced diazepam (Valium)
• Dependence and overdose can occur
o Tolerance
o Withdrawal
o Rarer than with barbiturates
o More common in combination with alcohol
• Wider margin of safety and fewer side effects than
barbiturates
• Used to treat anxiety
18. Doctors are more likely to
prescribe barbiturates for
sleep now than they were
20 years ago.
A. True
B. False
True
False
0%0%
19. In comparison to barbiturates,
benzodiazepines
A. Have more severe
side effects
B. Are not addictive
C. Do not cause
withdrawal
symptoms
D. Have a wider safety
margin
Havem
oresevere
sideef...Are
notaddictive
Do
notcause
w
ithdraw
al...
Havea
w
idersafety
m
argin
8%
73%
19%
0%
20. Do you know someone who has had their
drink spiked with GHB or roofies?
A. I think so
B. I don’t think so
Ithinkso
Idon’tthinkso
65%
35%
21. Do you know someone who has drugged
someone else by spiking their drink?
A. I think so
B. I don’t think so
Ithinkso
Idon’tthinkso
64%
36%
22. Gamma Hydroxybutyric
Acid
• 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
o Along with Rohypnol and Ketamine
• GHB is listed on Schedule I
https://www.youtube.com/watch?v=LPtcU_8yvR4
https://www.youtube.com/watch?v=YwtBEkFXBjQ
https://www.youtube.com/watch?v=2udrpuNxcmM
23. When it is used in
conjunction with alcohol,
the effects of Rohypnol
can be fatal.
A. True
B. False
True
False
6%
94%
24. Inhalants
• Most frequently used class of
illegal drugs among
adolescents aged 12 and 13
• Sudden Sniffing Death
Syndrome
25. Inhalants
• High-dose exposure causes
intoxication
• Examples:
o Volatile solvents
o Aerosols, propellants, gases
o Anesthetics
o Nitrites
http://www.youtube.com/watch?v=3g99h4qaCio
26. Inhalants
• Most abusers are very young
• Abuse tends to occur as localized fads
• Dangers:
o Kidney damage
o Brain damage
o Peripheral nerve damage
o Irritation of respiratory tract
o Severe headache
o Death by suffocation
27. The highest rate of
inhalant use by
youths occurs
among Asians.
A. True
B. False
True
False
42%
58%
28. More people die from
inhaling air fresheners than
from inhaling gasoline.
A. True
B. False
True
False
0%0%
29. Nitrous oxide has
been used as an
anesthetic by dentists.
A. True
B. False
True
False
0%
100%
30. Benefits Risks
• Anxiolytics
• Sleeping agents
• Anticonvulsants
• Dependence
o Tolerance & Cross Tolerance
o Withdrawal
• Toxicity
o Behavioral
o Physiological
• Can be fatal with alcohol
• Patterns of abuse
Editor's Notes
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
Barbiturates
Barbiturates are used to treat anxiety, insomnia, and seizure disorders. They are not, however, prescribed as often due to the availability of benzodiazepines and non-benzodiazepines. Barbiturates can be addictive and have strong withdrawal symptoms and rebound (exaggerated) effects on rapid eye movement (REM) sleep when they are abruptly stopped and can interfere with sleep. It is advisable, therefore, to stop barbiturates by slowly lowering their dose over a period of more than five or six days. It also is important to use the correct dose of barbiturates since a relatively small overdose may lead to coma or death.
The main differences among barbiturates are their half-lives (duration of their effects). Drugs such as secobarbital sodium and pentobarbital sodium are short-acting, while others such as amobarbital sodium and butabarbital sodium are intermediate-acting, and phenobarbital and mephobarbital are long-acting.
Examples of barbiturates:
Nembutal (phenobarbital)
Mebaral (mephobarbital)
Amytal Sodium (amobarbital sodium)
Butisol (butabarbital sodium)
Seconal Sodium Pulvules (secobarbital sodium)
Doubled in the last 15 years
Barbiturates
Barbiturates are used to treat anxiety, insomnia, and seizure disorders. They are not, however, prescribed as often due to the availability of benzodiazepines and non-benzodiazepines. Barbiturates can be addictive and have strong withdrawal symptoms and rebound (exaggerated) effects on rapid eye movement (REM) sleep when they are abruptly stopped and can interfere with sleep. It is advisable, therefore, to stop barbiturates by slowly lowering their dose over a period of more than five or six days. It also is important to use the correct dose of barbiturates since a relatively small overdose may lead to coma or death.
The main differences among barbiturates are their half-lives (duration of their effects). Drugs such as secobarbital sodium and pentobarbital sodium are short-acting, while others such as amobarbital sodium and butabarbital sodium are intermediate-acting, and phenobarbital and mephobarbital are long-acting.
Examples of barbiturates:
Nembutal (phenobarbital)
Mebaral (mephobarbital)
Amytal Sodium (amobarbital sodium)
Butisol (butabarbital sodium)
Seconal Sodium Pulvules (secobarbital sodium)
In 2011, 4.3% of high school seniors had used a sedative for nonmedical purposes within the previous 12 months
Girls are more likely to intentionally abuse prescription drugs than boys
One misconception among adolescents is that these drugs provide a medically safe high
37 for benzo, 34 for other illegal drugs
Can cause confusion, short attention span, impaired cognitive functioning, inadequate emotional control, slurred speech, poor judgment, hangovers, and intoxication
Barbital
Sedative-hypnotic drug used to treat anxiety and nervousness; the original barbiturate
Veronal
Brand name for barbital
Phenobarbital
Second barbiturate developed
Produces relaxation and relieves anxiety
HAZARDS
Reduced attention span
Impaired cognitive functioning
Diminished hand-eye coordination
Inadequate emotional control
Nausea
Vomiting
Birth defects
Confusion
Poor judgment
Slurred speech
Vertigo
Diarrhea
Respiratory failure
Violent behavior
Combination of alcohol and barbiturates can lead to accidental or intentional death
Withdrawal is life-threatening without medical supervision: marked by profuse sweating, insomnia, muscular twitching, paranoia, vomiting, aches and pains, cramps, quick temper, nightmares, hallucinations, and seizures
The effectiveness of barbiturates as sleep agents is questionable, because they interfere with rapid eye movement (REM), and may result in rebound insomnia
Anticonvulsants
These drugs may be used to treat conditions that contribute towards sleep disruption such as restless legs syndrome, nocturnal eating syndrome, periodic limb movement disorder, and insomnia related tobipolar disorder.
Examples of anticonvulsants:
Tegretol (carbamazepine)
Carbatrol (carbamazepine extended-release)
Depakene (valproic acid)
Depakote (divalproex sodium)
Neurontin (gabapentin)
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)
Chloral hydrate (“knockout drops” or Mickey Finns)
Induces sleep
Works rapidly
Margin between effective dose (ED) and lethal dose (LD) is slight
Risk of hepatoxicity
Produces gastric distress, vomiting, and flatulence
Paraldehyde
Effective and safe central nervous system depressant
Used with severely disturbed mental patients
Produces a terrible smell and taste
Bromides
Used to treat epileptic convulsions
Build up in the body, cause depression, and can be highly toxic
Meprobamate (Miltown and Equanil)
Minor tranquilizer used for psychosomatic conditions
Severe withdrawal and low margin of safety
Minor tranquilizer
Drug used primarily to relieve anxiety
Anxiolytic
Anxiety-reducing drugs
Methaqualone (Quaalude)
Relieves tension and anxiety without barbiturate-like aftereffects
Withdrawal symptoms can be extremely severe, including mania, seizures, vomiting, convulsions, and death
Induces dreamlike moods at low dosage levels
Memory is affected
Especially lethal in combination with alcohol
In 2011, 4.3% of high school seniors had used a sedative for nonmedical purposes within the previous 12 months
Girls are more likely to intentionally abuse prescription drugs than boys
One misconception among adolescents is that these drugs provide a medically safe high
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
Barbiturates
Barbiturates are used to treat anxiety, insomnia, and seizure disorders. They are not, however, prescribed as often due to the availability of benzodiazepines and non-benzodiazepines. Barbiturates can be addictive and have strong withdrawal symptoms and rebound (exaggerated) effects on rapid eye movement (REM) sleep when they are abruptly stopped and can interfere with sleep. It is advisable, therefore, to stop barbiturates by slowly lowering their dose over a period of more than five or six days. It also is important to use the correct dose of barbiturates since a relatively small overdose may lead to coma or death.
The main differences among barbiturates are their half-lives (duration of their effects). Drugs such as secobarbital sodium and pentobarbital sodium are short-acting, while others such as amobarbital sodium and butabarbital sodium are intermediate-acting, and phenobarbital and mephobarbital are long-acting.
Examples of barbiturates:
Nembutal (phenobarbital)
Mebaral (mephobarbital)
Amytal Sodium (amobarbital sodium)
Butisol (butabarbital sodium)
Seconal Sodium Pulvules (secobarbital sodium)
Classified based on potency and the length of time they act:
Ultra-short-acting
Short-acting (less than 4 hours)
Intermediate-acting (4 to 6 hours)
Long-acting (more than 6 hours)
Drugs that take effect rapidly have a higher abuse potential than slow-acting drugs
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
Can cause confusion, short attention span, impaired cognitive functioning, inadequate emotional control, slurred speech, poor judgment, hangovers, and intoxication
Barbital
Sedative-hypnotic drug used to treat anxiety and nervousness; the original barbiturate
Veronal
Brand name for barbital
Phenobarbital
Second barbiturate developed
Produces relaxation and relieves anxiety
HAZARDS
Reduced attention span
Impaired cognitive functioning
Diminished hand-eye coordination
Inadequate emotional control
Nausea
Vomiting
Birth defects
Confusion
Poor judgment
Slurred speech
Vertigo
Diarrhea
Respiratory failure
Violent behavior
Combination of alcohol and barbiturates can lead to accidental or intentional death
Withdrawal is life-threatening without medical supervision: marked by profuse sweating, insomnia, muscular twitching, paranoia, vomiting, aches and pains, cramps, quick temper, nightmares, hallucinations, and seizures
HAZARDS
Reduced attention span
Impaired cognitive functioning
Diminished hand-eye coordination
Inadequate emotional control
Nausea
Vomiting
Birth defects
Confusion
Poor judgment
Slurred speech
Vertigo
Diarrhea
Respiratory failure
Violent behavior
Combination of alcohol and barbiturates can lead to accidental or intentional death
Withdrawal is life-threatening without medical supervision: marked by profuse sweating, insomnia, muscular twitching, paranoia, vomiting, aches and pains, cramps, quick temper, nightmares, hallucinations, and seizures
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
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
Inhalants serve as gateway drugs
Twice as many 8th-grade students use inhalants as 12th-grade students
Strong relationship between inhalant use and other problem behaviors and sensation-seeking
Sudden Sniffing Death Syndrome
http://www.drugfreeworld.org/drugfacts/inhalants/international-statistics.html
22% first time users
Long-term effects: nosebleeds, liver and kidney damage, sores, weight loss, depression, irritability, disorientation, paranoia, hostility, and bone marrow abnormalities
Inhalants serve as gateway drugs
Twice as many 8th-grade students use inhalants as 12th-grade students
Strong relationship between inhalant use and other problem behaviors and sensation-seeking
Sudden Sniffing Death Syndrome
http://www.drugfreeworld.org/drugfacts/inhalants/international-statistics.html
22% first time users
Long-term effects: nosebleeds, liver and kidney damage, sores, weight loss, depression, irritability, disorientation, paranoia, hostility, and bone marrow abnormalities
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
Glue (volatile hydrocarbon solvents)
Psychoactive agent is toluene
Possible immediate cardiorespiratory arrest
Brain damage and memory loss
Anesthetic inhalants
Ether used as industrial solvent and anesthetic
Nitrous oxide (laughing gas)
Can cause irreparable brain damage or death due to decreased oxygen (hypoxia)
Nitrite inhalants
Inhaled for sexual purposes
Amyl nitrite: used to treat angina pectoris and congestive heart failure
Butyl nitrite: found in perfume and antifreeze
Isobutyl: used to treat angina pain; causes vasodilation, flushing, and warmth
Suppresses the immune system
Inhalants serve as gateway drugs
Twice as many 8th-grade students use inhalants as 12th-grade students
Strong relationship between inhalant use and other problem behaviors and sensation-seeking
Sudden Sniffing Death Syndrome
http://www.drugfreeworld.org/drugfacts/inhalants/international-statistics.html
22% first time users
Long-term effects: nosebleeds, liver and kidney damage, sores, weight loss, depression, irritability, disorientation, paranoia, hostility, and bone marrow abnormalities
Kidney damage
Brain damage
Peripheral nerve damage
Irritation of the respiratory tract
Severe headache
Death by suffocation
White, Hispanic, Asian, black
Use has declined in recent years
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
HAZARDS
Reduced attention span
Impaired cognitive functioning
Diminished hand-eye coordination
Inadequate emotional control
Nausea
Vomiting
Birth defects
Confusion
Poor judgment
Slurred speech
Vertigo
Diarrhea
Respiratory failure
Violent behavior
Combination of alcohol and barbiturates can lead to accidental or intentional death
Withdrawal is life-threatening without medical supervision: marked by profuse sweating, insomnia, muscular twitching, paranoia, vomiting, aches and pains, cramps, quick temper, nightmares, hallucinations, and seizures