3. INTRODUCTION
• Sedatives are a type of drugs that slow down the brain activity. They
reduce anxiety and exert a calming effect.
• Hypnotics are a type of drugs used to induce, extend and improve the
quality of sleep. These produce drowsiness and facilitate the onset
and maintenance of state of sleep.
4. BENZODIAZEPINES
• These are sometimes called benzos. They are class of psychoactive
drugs where core chemical structures the fusion of benzene ring and
a diazepine ring.
• They are depressants; drugs that lower the brain activity prescribed in
conditions such as anxiety, insomnia and seizures.
5. • NB: Benzodiazepines are commonly used in the treatment
of anxiety despite lack of widespread clinical evidence
supporting their use. Clinical guidelines do not recommend
benzodiazepines as first-line treatment of anxiety disorders.
The majority of published clinical data available suggest
similar outcomes and symptom reduction with the
available benzodiazepines when used in the treatment of
the anxiety disorders. Benzodiazepines have similar adverse
events but the rates of these events may differ depending
on individual pharmacokinetic profiles. Overall,
benzodiazepines should be used at the lowest effective
dose for the shortest duration possible with a
comprehensive treatment plan and careful follow-up.
7. Are there differences between benzodiazepines?
Benzodiazepines differ in how quickly they start working, how long
they continue to work, and for what they are most commonly
prescribed.
• Short acting
• intermediate acting
• Long acting
8. Ctdn…
• Diazepam (Valium) and clorazepate (Tranxene) have fast onsets of action
and usually start working within 30 to 60 minutes.
• Oxazepam (Serax) has a slow onset, and lorazepam (Ativan), alprazolam
(Xanax), and clonazepam (Klonopin) have intermediate onsets of action.
• Clorazepate (Tranxene), midazolam (Versed), and triazolam (Halcion) are
short-acting agents with a duration of action of 3 to 8 hours.
• Alprazolam (Xanax), lorazepam (Ativan), estazolam (ProSom), and
temazepam (Restoril) are intermediate-acting agents with a duration of
action of 11 to 20 hours.
• Chlordiazepoxide (Librium), clonazepam (Klonopin), diazepam (Valium),
flurazepam (Dalmane), and quazepam are long-acting agents with a
duration of action of 1 to 3 days.
9. For what conditions are benzodiazepines used?
• anxiety and panic
• seizures (convulsions)
• insomnia or trouble sleeping.
• general anesthesia.
• sedation prior to surgery or diagnostic procedures.
• muscle relaxation.
• alcohol withdrawal and drug-associated agitation.
• nausea and vomiting.
• Depression.
• panic attacks.
10. • Alprazolam (Xanax), chlordiazepoxide (Librium), clorazepate
(Tranxene), diazepam (Valium), lorazepam (Ativan), and midazolam
are used for anxiety disorders.
• Clonazepam (Klonopin), clorazepate (Tranxene), lorazepam (Ativan),
clobazam (Onfi), and diazepam (Valium) are used for seizure
disorders.
• Estazolam (Prosom), flurazepam (Dalmane), quazepam (Doral),
temazepam (Restoril), and triazolam (Halcion) are used for insomnia
or trouble sleeping.
• Midazolam (Versed), lorazepam (Ativan), and diazepam (Valium) are
used in anesthesia.
• Diazepam (Valium) also is used for muscle relaxation.
• Chlordiazepoxide (Librium) is used for alcohol withdrawal.
11. PHARMACOKINETICS
• Most sedative-hypnotic drugs are lipid-soluble and are absorbed
• well from the gastrointestinal tract, with good distribution to the
brain
• All benzodiazepine agents exert similar clinical effects. However,
differences in their pharmacokinetic profiles, such as rate of
absorption, elimination half-life and lipid solubility, contribute to
varying patterns of therapeutic application by influencing onset and
duration of action
12. MECHANISM OF ACTION
•Benzodiazepines work by enhancing a very important
neurotransmitter called GABA at the GABA receptor
•GABA is the chief inhibitory neurotransmitter in the
mammalian CNS. Its role reducing neural excitability
and in humans its responsible muscle tone.
•Benzodiazepine have their effect on the GABAa
receptors.
13. Ctdn.
• Benzodiazepines work by binding on the GABAa receptor and this
type of effect is called allosteric effect which leads to increase in
action at GABA receptor. This leads to opening of ion channels and
allowing the negatively charged chloride ions in to the neurons and
the ions are responsible for pushing the membrane potential further
from zero( hyperpolarization) and the neuron is less likely to fire an
action potential thus producing a calming effect.
14. Ctdn.
• Lorazepam, oxazepam and alprazolam have low hepatic metabolism
and do not have active metabolites
• Diazepam and chlorazepate are rapidly absorbed benzodiazepine
agents and have the most rapid onset of action but also the greatest
abuse/dependence potential.
• Chlordiazepoxide, clonazepam, clorazepate and diazepam are
considered long-acting benzodiazepine agents and are associated
with accumulation which may result in sedation, cognitive
impairment and psychomotor retardation
• Alprazolam and lorazepam are considered short-acting
benzodiazepine agents and have been associated with increased
anxiety, insomnia and rebound effects upon discontinuation
15. Ctdn..
• All benzodiazepine agents result in dependence or tolerance with long-term
use
• Benzodiazepine therapy should be discontinued by a slow taper to avoid
withdrawal effects.
• Transitioning patients from long-acting to short-acting agents may allow for
more flexibility and aid in discontinuing therapy
16. What are the side effects of benzodiazepines?
• The most common side effects associated with benzodiazepines are:
• Sedation.
• Dizziness.
• Weakness.
• Unsteadiness.
• transient drowsiness commonly experienced during the first few days of treatment.
• a feeling of depression.
• loss of orientation.
• Headache.
• sleep disturbance.
• Confusion.
• Irritability.
• Aggression.
• Excitement.
• memory impairment.
17. Ctdn…
• All benzodiazepines can cause physical dependence. Suddenly
stopping therapy after a few months of daily therapy may be
associated with withdrawal symptoms which include a feeling of loss
of self-worth, agitation, and insomnia.
• If benzodiazepines are taken continuously for longer than a few
months, stopping therapy suddenly may produce seizures, tremors,
muscle cramping, vomiting, and sweating. In order to avoid
withdrawal symptoms, the dose of benzodiazepines should be
tapered slowly
18. What are the dangers of benzodiazepine
addiction?
• Two serious concerns of benzodiazepine therapy are
• the potential for abuse (overdose) and
• the development of physical dependence (addiction).
19. BARBITURATES
• Barbiturates are drugs that act as central nervous system depressants, and, by
virtue
• of this, they produce a wide spectrum of effects, from mild sedation to total
anesthesia.
• Barbiturates are therapeutically used as anaesthetics, anticonvulsants,
anxiolytics,
• hypnotics and sedatives. They are usually classified according to the duration
• of their clinical effects into “long-”, “intermediate-”, “short-” and “ultrashort-”
acting
• compounds.
• They are synthetic drugs derived from barbituric acid , which is a
• synthetic condensation product of malonic acid and urea
21. Dosage of barbiturates
• Dosages of Barbiturates:
• The dosages of barbiturates vary depending on the drug and its use.
• Dosage Forms and Strengths
• Amobarbital (Amytal)
• powder for injection: 500mg
• Secobarbital (Seconal)
• capsule: 100mg
• Butabarbital (Butisol)
• tablets: 30mg and 50mg
• oral solution: 30 mg/5 mL
22. Ctdn..
• Dosage Forms and Strengths
• Sedative
• Amobarbital: 30-50 mg intravenously (IV) every 8-12 hours
• Butabarbital: 15 to 30 mg, 3 or 4 times daily
• Hypnotic for short-term treatment of insomnia
• Do not administer for more than 2 weeks
• Amobarbital: 65-200 mg intravenously (IV) at bedtime
• Secobarbital: 100 mg taken orally at bedtime
• Pre-procedure Sedation
• Secobarbital: 200-300 mg orally 1-2 hours before surgery
• Butabarbital: 50 to 100 mg, 60 to 90 minutes before surgery
23. What Are Side Effects Associated with Using
Barbiturates?
• Common side effects of barbiturates include:
• Drowsiness
• Headache
• Low blood pressure (hypotension)
• Nausea
• Sedation
• Skin rash
24. Ctdn..
• Serious side effects of barbiturates include:
• Abnormally slow breathing
• Coma
• Confusion
• Fainting
• Hallucinations
• Temporary breathing cessation
• Rare side effects of barbiturates include:
• Agranulocytosis
• Erythroderma
• Liver injury
• Megaloblastic anemia
• Stevens-Johnson syndrome
25. NB
1. Barbiturates are central nervous system depressants and should not be taken with
alcohol or other drugs that slow the central nervous system, such as
antihistamines, cold and allergy medicines, sleep medications, tranquilizers,
medicine for seizures, narcotics, and muscle relaxants. Combining CNS depressants
can lead to unconsciousness or death.
2. Barbiturates may alter the results of some medical tests
3. Children may be more sensitive to barbiturates and have additional side effects
such as unusual excitement.
4. Older people and those who are very ill may also be more sensitive to barbiturates
and have additional side effects such as confusion, depression, and unusual
excitement.
5. Barbiturates should not be used during pregnancy; they may harm a fetus.
Withdrawal symptoms occur in infants born to mothers who receive barbiturates
in the last trimester of pregnancy.
6. Small amounts of some barbiturates pass into breast milk. Barbiturates are not
recommended for use while breastfeeding to avoid harm to the infant.
