Hypnotics and Sedatives

Sedatives & Hypnotics
Dr. Kumari Anjana

Assistant Professor
Deptt. of Veterinary Pharmacology & Toxicology
Bihar Veterinary College, Bihar Animal Sciences University, Patna
Sedatives
 A drug that subdues excitement and calms the
subject without inducing sleep, though
drowsiness may be produced.
 Sedation refers to decreased responsiveness
to any level of stimulation; is associated with
some decrease in motor activity and ideation.
Hypnotics
 A drug that induces and/or maintains
sleep, similar to normal arousable sleep.
 Hypnosis is derived from ‘Hypnos’, the
Greek god of sleep.
Salient features of Sedatives and Hypnotics
 The Sedatives and Hypnotics are more or less

general CNS depressants with some what differing
time-action and dose action relationships.
 Those with quicker onset, shorter duration and
steeper dose-response curves are preferred as
hypnotics while more slowly acting drugs with
flatter dose-response curves are employed as
sedatives.
 However, there is considerable overlap; a hypnotic
at lower dose may act as sedatives.
Salient features of Sedatives & Hypnotics contd…
 Thus, sedation-hypnosis-general anesthesia may be

regarded as increasing grades of CNS depression.
 Both Sedatives and Hypnotics do not possess analgesic
property, but dull the perception of pain sensation.
 Hypnotics given in high doses can produce general
anesthesia.
 Hypnotics in higher doses cause deep sleep (narcosis)
and hence are also called as narcotics.
 Treatment of insomnia is the most important use of
this class of drugs.
Salient features of Sedatives & Hypnotics contd…
 The difference between sedatives and tranquillizers is also

indistinct except that the tranquillizers produce a state of
calmness with less drowsiness.
 Tranquillized animals are usually easy to handle, but they
may be aroused by and respond to stimuli in a normal way
(biting, scratching and kicking).
 Sedatives are used in veterinary medicine generally for
producing restrain, to facilitate handling and transport, and
to modify behavior of animals.
 Sedatives are commonly included in pre- anesthetic
medication and are also used to facilitate minor surgery or
diagnostic procedures.
Barbiturates: Barbitone,
Phenobarbione
Amobarbitone,
Secobarbitone
Benzodiazepines:
Hypnotics Diazepam, Flurazepam,
Nitrazipam, Flunitrazepam
Anxiolytics Diazepam,
Chlordiazepoxide,
Oxazepam, Lorazepam.
Benzodiazepines
 Benzodiazepines are commonly used as sedatives
or hypnotics in man and dog.
 These compounds have several advantages over
barbiturates as hypnotic and sedatives. ---
o Benzodiazepines have high therapeutic index.
Ingestion of even 20 hypnotic doses does not
usually endanger life—there is no loss of
consciousness.
o Hypnotic doses do not affect respiration or
cardiovascular function.
Benzodiazepines contd…
o BZDs have practically no action on other body
systems. Only on i.v. injection the BP falls
and cardiac contractibility decreases.
o BZDs do not alter disposition of other drugs

by microsomal enzyme induction.
o Their toxicity (due to higher dosage) can be

overcome by giving specific benzodiazepine
receptor antagonist flumazenil.
Mechanism of Action of Benzodiazepines
Mechanism of Action
 Benzodiazepines preferentially act on mid brain
ascending reticular formation (maintains sleep-
wakefulness cycle) and on limbic system (thought and
mental functions).
 Their mechanism of action is through enhancing
presynaptic or postsynaptic inhibition of specific
benzodiazepine receptor which is an integral part of
GABAA receptor-Cl- channel complex.
 The subunit of this complex form a pentameric
transmembrane anion channel gated by the primary ligand
(GABA), and modulated by secondary ligands BZDs.
 Only the α and β subunits are required for GABA action, and
most likely the binding site for GABA is located on the β
subunits, while the α /γ subunit interface carries the BZDs
binding site.
 The modulatory BZD receptor increases the frequency of CI-
channel opening induced by submaximal concentrations of
GABA. The BZDs also enhance binding of GABA to GABAA
receptor.
 It is noteworthy that, the BZDs do not themselves increase
CI- conductance, these exert only GABA facilitation, but not
GABA mimetic action.
 GABA modulates activation of Cl-channels within the neuronal
membrane of excitable neurons.
Drugs affecting GABAA receptor – Cl- Channel complex
 GABA:Endogenous agonist at GABAA receptor promote Cl- influx

 Mucimol: Agonist at GABAA site
 Bicuculline: Competitive antagonist at GABA A receptor
 Picrotoxin: Blocks Cl- channel noncompetitively; acts on picrotoxin
sensitive site
 Barbiturates: Agonist at an allosteric site; prolong GABA action; open
Cl- Channel
 Alcohol, Inhalational anaesthetics, Propofol: open Cl- Channel directly.
 Benzodiazepines: Agonist at an allosteric BZD site-facilitate GABA
action.
 Β-carboline: inverse agonist at BZD site- impede GABA action
 Flumazenil: competitive antagonist at BZD site
Pharmacokinetics
 Oral absorption of benzodiazepines differs due to their
variation in lipid solubility.
 These drugs due to lipid solubility gain access into CNS.
 Benzodiazepines are metabolized in liver through Most of the
benzodiazepine drugs have active metabolites (glucuronide
conjugates) are excreted through urine.
 Most of the benzodiazepine drugs have active metabolites
(chlordiazepoxide, desmethyldiazepam, diazepam, flurazepam
etc.) which undergo enterohepatic recycling (have long half-
lives).
 Chlorazepine is metabolically activated to desmethyldiazepine,
which is further metabolically activated to oxazepam.
Thank You

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Sedatives & Hypnotics

Dr. Kumari Anjana

 The Sedatives and Hypnotics are more or less

 Thus, sedation-hypnosis-general anesthesia may be

 The difference between sedatives and tranquillizers is also

o BZDs do not alter disposition of other drugs

o Their toxicity (due to higher dosage) can be

 GABA:Endogenous agonist at GABAA receptor promote Cl- influx

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