III.

Depressants
Depressants are drugs that inhibit the function of the
central nervous system (CNS)
Drugs that are categorized as depressants include:
• Barbiturates
• Benzodiazepines
• Ethyl alcohol
Why are they abused?
• Individuals abuse depressants to experience euphoria.
• Users take higher doses than therapeutic doses.
What is their effect on the mind?
• Depressant are used To induce sleep, relieve anxiety and
muscle spasms, and prevent seizures.
• They also Cause amnesia, impair mental functioning and
judgment, and cause confusion
• Long-term use of depressants produces psychological
dependence and tolerance .
• Some depressants can relax the muscles.
Unwanted physical effects include:
• Loss of motor coordination
• weakness, headache, blurred vision, dizziness
• Nausea, vomiting
• Slurred speech
• Low blood pressure, and slowed breathing
Prolonged use of depressants can lead to physical
dependence even at doses recommended for
medical treatment.
I. Barbiturates
• Barbiturates are depressants that produce a wide spectrum of
central nervous system depression from mild sedation to coma.
• They also have been used as sedatives, hypnotics, anesthetics,
and anticonvulsants.
Barbiturates are classified as:
• Ultra short-acting barbiturates e.g. Methohexital and
Thiopental
• Short-acting and intermediate-acting barbiturates e.g.
Pentobarbital and Secobarbital
What are its forms?
• Barbiturates come in the form of pills, tablets and
injection.
• Users prefer the short-acting and intermediate
barbiturates
How are they abused?
Barbiturates are abused by swallowing a pill or injecting
a liquid form.
Common side effects of barbiturates are:
• Dizziness, drowsiness, headache, sedation
• Low blood pressure (hypotension),
• Skin rash
• Nausea, vomiting, and abdominal pain.
 Barbiturates Toxicity
• Difficulty thinking, decreased level of consciousness
• Bradycardia or rapid and weak pulse
• Poor coordination, vertigo
• Nausea
• Muscle weakness
• Thirst
• Oliguria
• Decreased temperature
• Dilated pupils.
• Fatal cases are marked by coma, hypotension, and
respiratory depression evidenced by cyanosis and
hypotension.
• Pulmonary edema is another complication
associated with barbiturate toxicity and
contributing to respiratory depression and death.
Treatment / Management
• Treatment of barbiturate toxicity remains supportive as there is no
specific antidote for overdose.
• The first step in treatment, is assessing the patient’s airway, breathing,
and circulation.
• With significant sedation and respiratory depression, intubation and
mechanical ventilation may become necessary.
• Early treatment with activated charcoal may be useful and can be given
via nasogastric tube.
• Other options for managing barbiturate toxicity include forced alkaline
diuresis and hemodialysis for severe cases.
• Bemegride is a central nervous system stimulant that increases
respiration and can be used as a treatment for depressant toxicity. It is,
however, an emetic that raises the concern of emesis and aspiration.
withdrawal symptoms
Chronic abusers can develop severe withdrawal
symptoms within 8 to 15 hours of cessation.
Symptoms include restlessness, tremors,
hyperthermia, sweating, insomnia, anxiety, seizures,
circulatory failure, and potentially death.
• Management of long-term use involves restoring
central nervous system (CNS) inhibitory tone.
Abrupt cessation can lead to severe withdrawal
symptoms
• Discontinuance of barbiturates should be a
gradual reduction
• using medications that demonstrate cross-
tolerance, with the first line being
benzodiazepines.
II. BENZODIAZEPINES
Benzodiazepines are depressants that produce sedation
and hypnosis, relieve anxiety and muscle spasms, and reduce seizures.
Classification of benzodiazepines
There are three types of benzodiazepines: long, intermediate and
short-acting. Short-acting benzodiazepines have stronger withdrawal
or ‘come down’ effects and can be more addictive than long-acting
ones.
Long-acting e.g. diazepam
Intermediate-acting e.g. lorazepam and temazepam
Short-acting e.g. triazolam and alprazolam
Effects of benzodiazepines
Benzodiazepines effects may include:
reduced stress, euphoria, reduced anxiety, calmness,
depression, confusion, impaired thinking and memory
loss, headache, drowsiness, sleepiness, fatigue, dry
mouth, slurred speech, or stuttering double or blurred
vision, impaired coordination, nausea and loss of
appetite diarrhea or constipation.
Injecting benzodiazepines :
Injecting drugs repeatedly and sharing injecting
equipment with other people increases the risk of
experiencing the following effects.
• Vein damage and scarring
• Infection, including hepatitis B, hepatitis C, HIV and AIDS
• Deep vein thrombosis(DVT) and clots which can result in
loss of limbs, damage to organs, stroke and possibly
death.
Overdose
• Benzodiazepines are often present in patients who have
intentionally or accidentally overdosed.
Symptoms include:
• Over-sedation or sleep
• Mood swings and aggression
• Slow, shallow breathing
• Unconsciousness or coma
• Death (more likely when taken with another drug such as
alcohol).
Treatment of benzodiazepine toxicity
Flumazenil, a specific benzodiazepine antagonist, is
useful in reversing the sedation and respiratory
depression
Long-term effects
• impaired thinking or memory loss
• anxiety and depression
• irritability, paranoia and aggression
• personality change
• weakness, lethargy and lack of motivation
• drowsiness, sleepiness and fatigue
• difficulty sleeping or disturbing dream
• skin rashes and weight gain
• addiction
• There is some evidence that long-term, heavy use of benzodiazepines is a risk
factor for epilepsy, stroke and brain tumors.
Withdrawal symptoms
Any patient who has taken a benzodiazepine for longer than 3–4 weeks is likely to
have withdrawal symptoms if the drug is ceased abruptly.
The risk of inducing dependence can be reduced by issuing prescriptions limited to
1–2 weeks supply.
• Headaches
• Aching or twitching muscles
• Dizziness and tremors
• Nausea, vomiting, stomach pains
• Bizarre dreams, difficulty sleeping, fatigue
• Poor concentration
• Anxiety and irritability
• Altered perception, hyperesthesia
• Delusions, hallucinations and paranoia
• Seizures
Treatment of benzodiazepine dependance
1- Gradual withdrawal
2- Substitution:
e.g., short acting by long-acting (Alprazolam with diazepam)
III. Alcohol
• Alcohol is classified as a Central Nervous System Depressant.
• Alcohol does this by enhancing the effects of the
neurotransmitter GABA.
• Alcohol can cause slurred speech, unsteady movement,
disturbed perceptions, and an inability to react quickly.
• Alcohol reduces an individual’s ability to think rationally, lessens
inhibitions, and distorts judgment.
• If an individual consumes too much alcohol too rapidly, they can
depress the CNS to a point of respiratory failure, coma, or death.
Alcohol misuse
• Alcohol misuse is the excessive consumption of
alcohol. It is the inability to control drinking, even
when it negatively affects a person’s life.
• The person consuming alcohol may develop
tolerance and experience withdrawal symptoms
when trying to cut back.
Long term effects of alcohol
Persistent alcohol misuse increases risk of serious health conditions, including:
• Heart disease
• Stroke
• Liver disease
• Liver cancer
• Bowel cancer
• Mouth cancer
• Breast cancer
• Pancreatitis
• Damage to the brain, which can lead to problems with thinking and memory
• With chronic alcohol intake, GABAA receptors are
downregulated and rendered less responsive by
expression of different subtypes , whereas NMDA
receptors are upregulated .
• These compensatory changes produce a
hyperglutamatergic, potentially excitotoxic state
during alcohol withdrawal
Withdrawal symptoms of alcohol
• Hand tremors
• Sweating
• Visual hallucinations
• Depression
• Anxiety
• Insomnia
This often leads to "relief drinking" to avoid withdrawal
symptoms.
Treatment for alcohol misuse
Three medications are FDA-approved for alcohol dependence.
• Naltrexone : This is an injection given by a healthcare
professional once a month. It is used after user’s body is already
detoxified. As an opiate antagonist, it does not treat withdrawal
symptoms but merely suppresses the cravings.
• Acamprosate :Taken orally. It is used along with psychosocial
support and helps to prevent the cravings and urge to drink
alcohol in alcoholism
• It has been found to modulate NMDA receptor transmission and
GABA transmission, to decrease glutamate during alcohol
withdrawal
Disulfiram :
This medication is taken orally.
Mechanism of action
• It interferes with the metabolism of alcohol leading to
accumulation of acetaldehyde
• Alcohol disulfiram reaction usually begins about 10 to 30
minutes after alcohol is ingested.
• Its adverse effects include: Sweating ,Warmth and flushing,
particularly on upper chest and face, Hyperventilation ,dyspnea,
Acetaldehyde breath odor, Blurred vision, Head and neck
throbbing, Thirst, Vertigo, Syncope and Confusion