SEDATIVES &

HYPNOTIC'S
▪ Paraldehyde
▪ Glutethimide
▪ Chloral hydrate
PRESENTED BY:

❑ AYESHA KABIR
❑ MAROOSHA FAISAL
❑ BUSHRA AZAM
❑ AMMARA BATOOL
❑ SAMRA BATOOL

PRESENTED TO: MAM SHAMAILA MUZZAFAR

PRESENTATION CONTENT:
▪ INTRODUCTION
▪ MECHANISM OF ACTION
▪ THERAPEUTIC INDICATIONS
 CLASSIFICATION OF SEDATIVE HYPNOTICS
4
Benzodiazepines Barbiturates Miscellaneous
Short acting(2-5h) Long acting Melatonin receptor agonist
Triazolam Phenobarbitone Ramelteon
Oxazepam Methobabitone Melatonin
Intermediate acting(10-24h) Intermediate Carbamate derivatives
Alprazolam Amobarbitone Meprobamate
Estazolam Butobarbitone Non carbamate derivatives
Lorazepam Short acting Gultethimide
Nitrazepam Pentabarbitone Other Antidepressants
Long acting(20-50h) Secobabitone Dpxepin
Diazepam Flurazepam Ultra short acting Mirtazapine
Clonazepam Thiopentone Trazodone
Chlordiazepam Methohexitone Antihistaminics
Non benzodiazepines(Z drugs) Non barbiturates Hydroxyzine
Zolpidem Chloral hydrate Cyprohepatadin
Zopiclone Paraldehyde
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NON-BARBITURATES

❖ Paraldehyde.
❖ Chloral hydrate
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Paraldehyde[Non barbiturate]:
Paraldehyde is the cyclic trimer of acetaldehyde molecules.
Formally, it is a derivative of 1,3,5-trioxane, with a methyl group
substituted for a hydrogen atom at each carbon. The
corresponding tetramer is metaldehyde. A colorless liquid, it is
sparingly soluble in water and highly soluble in ethanol.
Formula: C6H12O3
Molar mass: 132.16 g/mol
Boiling point: 124 °C
Density: 0.996 g/cm3
paraldehyde ; Belongs to the class of aldehydes and derivatives.
Used as hypnotics and sedatives.
 Mechanism of action 7

Increase inhibitory effect of GABA neurotransmission(similar to chloral

hydrate) .Primarily metabolized by liver converted to metabolite acetaldehyde.

Leading to increase chloride ion influx which lead to neuronal

hyperpolarization.

Paraldehyde may also interact with other neuronal system dopamine in brain
which lead to its sedative effects.

Primarily this drug was used as management of

severe agitation or delirium.Don,t used in practice
due to side effects and its safest alternative are
available .
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THERAPEUTIC INDICATIONS:
Paraldehyde is used to treat :
• certain convulsive disorders.
• Withdrawal symptoms of alcoholism
• treatment of nervous and mental conditions to calm
or relax patients who are nervous or tense and to
produce sleep.
• It is employed in delirium tremens
• status epileptics.
• Anxiety
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CHLORALHYDRATE:
Chloral hydrate is a geminal diol with the formula
C₂H₃Cl₃O₂. It is a colorless solid. It has limited use as a
sedative and hypnotic pharmaceutical drug. It is also a
useful laboratory chemical reagent and precursor. It is
derived from chloral by the addition of one equivalent of
water.
Formula: C2H3Cl3O2
Molar mass: 165.4 g/mol
IUPAC ID: 2,2,2-trichloroethane-1,1-diol
 Mechanism of action
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Primarily CNS depressant

Prodrug metabolized in liver and convert to Trichloroethanol .

Trichloroethanol enhances activity of GABA(inhibitory

neurotransmitter) in brain leading increase chloride ion influx and
hyperpolarization of membrane

In this way reduces excitability and produces sedative and

hypnotic effects and also anticonvulsive effects

Due to side effects and high range of ADR’s

(Respiratory depression and Cardiovascular
effects) so no longer commonly used due to
availability of safer and more effective alternative.
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THERAPUTIC INDICATIONS:
Chloral hydrate Oral Solution is indicated for short-term treatment
(maximum 2 weeks) of severe insomnia in children and adolescents
with suspected or definite neurodevelopmental disorder, when the
insomnia is interfering with normal daily life and other therapies
(behavioural and pharmacologic) have failed.it is also employed in
alcohol withdrawal symptoms, anxiety and agitation.
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MICELLANIOUS
❖Glutithimide
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GLUTETHIMIDE:
Glutethimide is a hypnotic sedative that was introduced by Ciba in 1954
as a safe alternative to barbiturates to treat insomnia. Before long,
however, it had become clear that glutethimide was just as likely to cause
addiction and caused similar withdrawal symptoms. Doriden was the
brand-name version.

Molar mass: 217.264 g/mol

Density:1.1±0.1 g/cm3
Boiling Point: 393.5±31.0 °C at 760 mmHg
 Mechanism of action 14

Glutethimide is a sedative hypnotic drug,

Glutethimide exhibit weak anticholinergic properties ,block

action of acetyl choline ,a neurotransmitter involved in various
process including regulation of wakefulness and sleep, and lead
to sedative and hypnotic property

Glutethimide also enhances the inhibitory effect of GABA, leading to

sedative, hypnotic and anxiolytic effects.

Glutethimide have high potential of abuse

and dependance, safer alternatives are
available ,so it is no longer used in
treatment of insomnia.
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THERAPUTIC INDICATIONS:
Glutethimide is a hypnotic and sedative agent intended
to treat :
• insomnia without causing depression of
respiration..
• The hypnotic effect is roughly analogous to that of
pentobarbital.
• It is given to patients who cannot tolerate
barbiturates. However, it does not have any
advantage over benzodiazepines, and therefore it is
rarely used.
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