Overview

Depressants slow down (or “depress”) the normal

activity that goes on in the brain.

Doctors often prescribe central nervous system (CNS)

depressants to patients who are anxious or can’t sleep.

When used as directed, CNS depressants are safe and

helpful for people who need them.

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 1) CNS depressants are usually not obtained
illicitly and self-administered but rather are
prescribed under the direction of a physician.

 2) CNS depressants if not monitored correctly

could be potentially dangerous and harmful;
most problems stem from inadequate
professional supervision and chronic use.

 3) Several drug groups have the ability to cause

CNS depression and the major reason of death
and drug overdose
CNS depressants are a diverse group of drugs that share
an ability to reduce CNS activity and diminishes the
brain’s levels of awareness.
Depressant drugs include:
 Antihistamines: drugs that often cause CNS
depression, used to treat allergies, and are often
found over-the-counter drugs.
 Sedatives- to relieve anxiety, fear, and apprehension.
 Anxiolytic- drugs that relieves anxiety.
 Hypnotics- used to induce drowsiness and encourage
sleep.
 Amnesic- causing the loss of memory.
 Anesthesia- a state characterized by loss of sensation
or consciousness
 Depressantsare usually classified according
to the degree of their medical effects on the
body. For example:
 Sedatives cause mild depression
and relaxation
 Anxiolytic—drugs that relieve
anxiety
 Hypnotics induce drowsiness and
encourage sleep
 Amnesiac effects can cause the
loss of memory
 Thesame drug can cause different effects
depending on dose.
 Low dose (sedatives—relieve
anxiety and promote relaxation)
 Higher doses (hypnotics—can cause
drowsiness and promote sleep)
 Even higher doses (anesthetics can
cause anesthesia and are used for
patient management during
surgery)
Sedation Hypnosis Anesthesia Coma Death
To treat To treat For Surgery Inadvertent Fatal
Anxiety Insomnia Overdose Overdose
Low Dose High
 Sedative – hypnotics

 Tranquillizers

 Anesthetics
 ↓ vitality

 ↓ excitability

↓ HR & RR .
 Sedatives:
Drugs which decrease the activity, calm the
recipient,
cause sedation and in large dose they induce
sleep.
Hypnotics:
Drugs which induce sleep that resembles the
natural sleep.
e.g. Barbiturates
 Bind non-selectively to benzodiazepine receptors
(GABAA-dependent).
 GABA A receptors → increase Cl influx → hyperpolarization

 GABA B receptors → Gi protein → ↓cAMP →relaxation

 Affect neurons that have receptors for the

neurotransmitter GABA
 GABA: most common inhibitory transmitter in brain regions

 Limbic system (alter mood)

 RAS (cause drowsiness)
 Motor cortex (relax muscles)
Reported side effects include
 drowsiness,
 lightheadedness,
 lethargy,
 impairment of mental
 physical activities,
 skin rashes,
 nausea,
 diminished libido,
 irregularities in menstrual cycle,
 blood cell abnormalities, and increased
sensitivity to alcohol and other CNS depressants.
 MOA:

They have GABA like action → ↑ opening time

of chloride channels → ↑conductance of
chloride ions → hyperpolarization.
 Barbiturates can become uncontrollable
because of their addictive agents to one’s
body. It has been known to be replaced by
Benzodiazepine’s which is safer to use and
less abuse liability.

 Uncontrolled use of Barbiturates can cause a

state of acute or chronic intoxication.
Moreover, people that use Barbiturates can
have some loss of inhibition, euphoria, and
behavioral stimulation.
 Low doses relieve tension and anxiety,
effects that give several Barbiturates
substantial abuse potential.
 Drawbacks of Barbiturates are extensive and
severe, for example;
1) They lack selectivity and safety
2) They have substantial tendency to
create tolerance, dependence,
withdrawal, and abuse
3) They cause problems with drug
interaction
 Definition:
Tranquillizers are drugs which relief mental
anxiety
and stress without affecting the consciousness.
e.g. Chlorpromazine (CPZ)
 CPZ mechanism of action:
• It is D2 , 5 HT , H1 and alpha 1 antagonist .
 Specific signs for CPZ:
1- No loss of righting reflex.
2- Creeping gait.
3- State of catalepsy (loss of muscles control) →
onset
time.
4- ↓ Touch & pain reflexes.
 Drugs with barbiturate-like properties:
 Chloralhydrate
 Glutethimide
 Methyprylon
 Methaqualone
 Antihistamines
 Propofol(abused general anesthetic)
 GHB (gamma hydroxybutyrate)
Most obsolete, not used or prescribed
 1965: Despite problems in other
countries, methaqualone (Quaalude, Sopor)
was introduced in the United States
 No initial monitoring—no perceived abuse potential
 Overprescribed; quickly became widely misused
and abused
 Methaqualone users can develop
psychological and physical dependence as
easily as users of barbiturates

 Meprobamate (Equanil, Miltown) – 1950’s

1st non-barbiturate “tranquilizer”
Less respiratory suppression

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Chloral Hydrate (Noctec) – since 1880’s
Metabolized like alcohol
Tolerance like barbiturates
Bedtime sedative for elderly
“Mickey Finn” (w/alcohol) – 1st date rape
drug

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Paraldehyde – precedes barbiturates
By-product of ethyl alcohol metabolism
Used to treat DT’s
Dependence – toxicity for stomach, liver,
kidneys

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Potent CNS depressants
General anesthesia = most severe state of
intentional drug-induced CNS depression
= opioid narcotic + volatile anesthetic
(no pain +unconsciousness)
Depression of all CNS functions
- sedation, sleep, depressed reflexes,
amnesia, unconsciousness

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Inhalation – gases or volatile liquids
Nitrous oxide – dentistry
Abuse with canned whipped cream sniffing
= hypoxia (Oxygen deprivation)
= brain damage
Injection – Thiopental (Pentothal) barbiturate
Propofol and others resemble GABA

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Gamma-hydroxybutyrate
Naturally occurring 4-carbon molecule
in mammal brains
Structure like, synthesized from GABA
Anesthetic in other countries
Use in sleep disorders, alcohol and opioid
dependence

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Euphoriant – makes you feel good!
Common “date rape” drug
Doesn’t enhance body building or sex!
Effects – disinhibition, excitement,
drunkenness, amnesia
Dangerous overdose – stupor, delirium,
unconsciousness, coma
NO ANTIDOTE – only life support

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 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, 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
 TheAmerican Psychiatric Association
considers dependence on CNS depressants a
psychiatric disorder.
 People most likely to abuse CNS depressants
include individuals who:
 Use drugs to relieve continual stress
 Paradoxically feel euphoria and
stimulation from depressants
 Use depressants to counteract the
unpleasant effects of other drugs of
abuse
 Combine depressants with alcohol
and heroin to potentiate the effects
 Detoxification: The elimination of a toxic
substance, such as a drug, and its effects
 With CNS depressants, this is
achieved by substituting a longer-
acting barbiturate for the offending
CNS depressant and gradually
reducing the dose to avoid unpleasant
withdrawal effects. Withdrawal from
CNS depressants, if not managed
properly, can be very dangerous, or
even fatal.
 Withdrawal from any drug or alcohol is by far a
very hard and difficult situation to obdure. Many
signs and symptoms are different in many people
because of the distribution of the drug and it’s
components.
 Withdrawal symptoms may include anxiety,
tremors, nightmares, insomnia, anorexia,
vomiting, seizures, delirium, and maniacal
activity As a counselor, we face many people
with many difficulties.
 We trigger the problems by helping clients confront
their problems and find solutions that are concrete
for them to live healthy lives.
 In either case, patients addicted to barbiturates and
benzodiazaphines should not stop taking them on
their own because of the high-risk withdrawal state.

 Client’s rather should be seen by a professional,

whether it’s a family doctor, psychologist,
psychiatrist or any counselor that is experienced with
drug and alcohol addictions.

 In most cases addmitted to a rehab facility that can

monitor the dependence and give the help needed
for recovery.
 It is important to remember the elimination of
physical dependence is not a cure. If an
individual is abusing a CNS depressant because of
emotional instability, personal problems, or a
very stressful environment, eliminating physical
dependence alone will not solve the problem and
drug dependence is likely to reoccur.

 Without psychological support at this stage, the

detoxification will only be temporary and
therapy will fail
1)Textbook- Hansen, Venturelli, Fleckenstein, 2012.

2)H.P. Rang, M.M. Dale, M.J Ritter, R.J. Flower (2007).

Anxiolytic and hypnotic drugs. Rang and Dale’s
Pharmacology, 6th edition, Elsevier health sciences,
London.

3) Websites on Anxiety Disorders Association of

America, The Anxiety Network International and "Freedom
from Fear"