This document discusses different classes of sedative-hypnotic drugs, including benzodiazepines, barbiturates, and other miscellaneous drugs. It describes how benzodiazepines are classified based on their duration of action from short to long-acting. Barbiturates are noted to be replaced by safer benzodiazepines. Both benzodiazepines and barbiturates act on GABA receptors in the brain to produce sedative effects. Side effects, uses, and guidelines for prescribing benzodiazepines are provided.

1. B Y K E F I L W E B A R O B I
M B B S I V
SEDATIVES-HYPNOTIC

2. • Sedative-refers to a substance that moderates
activity and excitement while inducing calming
effect.
• Hypnotic-refers to a substance that causes
drowsiness and facilitates the onset and
maintenance of natural sleep.

3. SEDATIVE-
HYPNOTICS
Benzodiapines
Barbiturates Miscellaneou
s

4. BENZODIAPINES
• All the benzodiapines have the same general
chemical structure
• They are mostly classified into 3 groups:
a) short-acting
b) Intermediate acting
c) Long acting

5. BENZODIAPINE CLASSIFICATION HALF-LIFE
Midazolam Short-acting 2-6
Triazolam Short-acting 2-3
Alprazolam Intermediate-acting 12-15
Estazolam Intermediate-acting 10-24
Lorazepam Intermediate-acting 10-20
Temazepam Intermediate-acting 10-40
Clonazepam Long-acting 18-50
Clorazepate Long-acting 40-50
Diazepam Long-acting 20-80
Flurazepam Long-acting 40-100

6. MOA
• They act on GABA receptors, either increasing or
decreasing the concentrations and activities of the
neurotransmitters, like GABA, serotonin,
noradrenaline, thus inducing sleep.
• Indications
• benzodiazepine can be used in a variety of
treatments. They are used to treat nervousness and
anxiety; therefore they are very effective to treat
insomnia associated with anxiety and mood
instability.

7. • The use of benzodiazepines can lead to abuse, whether
they are taken properly or for the wrong reasons
• Prescribing benzodiapines guidelines
1. Be very cautious about initiating a prescription for
benzodiapines.
2. Prescribe the lowest dose possible.
3. Limit the prescription to 2-3 weeks.
4. Do not have prescriptions available for routine repeat
refills
5. Never re-prescribe if the patient reports losing or
forgetting their tablets
6. Do not prescribe benzodiapines for another doctor’s
patients; tell them to go to their usual prescriber.

8. Short term effects(low doses)
• Euphoria
• “Being in a happy world”
• Fatigue
• Feeling drowsy
• Shallow breathing
• Not being able to take full, deep, normal breaths (2)
• Trouble coordinating your movements
Short term effects(high doses)
• Paranoia
• Aggression
• Easily agitated
• Difficulty remembering
• Irritability
• l

9. Long term effects
• “Rebound effects”
• Over use of these drugs can cause a reversal effect
• Seizures can occur; calm and relaxed feelings dissipate
• Tolerance develops, resulting in dependence
• Must have more and more of the drug to feel an even minor
effects
• Higher risk of overdose
• Withdrawal
• This leads to dependence as well
• No one wants to feel the unpleasant withdrawal effects, so
continues use (2)
COGNITVE EFFECTS
• Memory impairment/Amnesia
• Confusion
• Sleepiness

10. BARBITURATES
• Barbiturates are actually known as CNS depressants
or central nervous system depressants and are in
this class of drug along with benzodiazepines
• Basically, the barbiturates have had their day in
medicine and largely been replaced by much
safer benzodiapines and other CNS drugs.
• The molecular site of action for the barbiturates is
nearly the same as for the benzodiapines

11. • However, there is a significant difference in the effect of
barbiturates at these receptors that is dependent on
dose administered:
I. At lower doses, barbiturates act like benzodiapines
and simply increase the effect of GABA at GABAα
receptor
I. At higher doses ,barbiturates may act as direct agonists
at GABAα receptors in place of GABA ,producing
profound CNS depression.

12. EXAMPLES OF BARBITURATES
Barbiturate Reference Table (list of barbiturates)
Chemical Name Brand Name Half Life
Allobarbital n/a n/a
Alphenal n/a n/a
Amobarbital Amytal Short
Aprobarbital Alurate Short
Brallobarbital Vesparax (mixed) No Reference
Butobarbital Soneryl, Butisol Short
Butalbital Fiorinal, Fioricet Medium
Cyclobarbital Phanodorm Medium
Methylphenobarbital Prominal Long
Mephobarbital Mebaral Long
Methohexital Brevital Very Short
Pentobarbital Nembutal Short
Phenobarbital Luminal Long
Secobarbital Seconal Short
Talbutal Lotusate Medium
Thiamylal Surital Very Short
Thiopental Pentothal Very Short

13. USES
• A barbiturate may be prescribed for a variety of
reasons, the list is extensive, but the most common
use today is as an anesthesia for surgery. This form is
hardly ever abused because they cause almost
immediate unconsciousness. However, other forms
like Phenobarbital are used in treating various
seizure disorders as an anticonvulsant. Other uses of
this form of barbiturate along with mephobarbital
include treating anxiety, insomnia, epilepsy and
delirium tremens

14. SIDE EFFECTS
• The symptoms of barbiturate intoxication resemble
those of alcohol: slurred
speech,incoherence,drowsiness and low mood.
• Tolerance develops to barbiturates, although less
quickly than to opioids.
• Withdrawal -The abrupt withdrawal of barbiturates
from dependent person can be followed by a
withdrawal syndrome resembling that occurring
with alcohol, with a high risk of seizures.

15. OTHER SEDATIVE/MISCELLANEOUS
• Zalopan,Zolpidem and Zoplicone
• All of the bind to the benzodiapine receptor at the
GABAα receptor and increase the effect of GABA.
• However ,none of these drugs produce effects that
are identical to the benzodiapines ,and all of these
drugs have chemical structure that are unrelated to
the benzodiapines.

16. • For the treatment of insomnia, they act
quickly but short duration of action. Hence,
making them more suitable for patients who
have trouble falling asleep and have a
preference for less residual effects the next
day.

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