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Hypnotics and Sedatives

This document discusses sedatives and hypnotics. It defines sedatives as drugs that calm subjects without inducing sleep, while hypnotics induce and maintain sleep. Both are central nervous system depressants with differing time-action profiles. Sedatives have flatter dose-response curves and are used to calm subjects, while hypnotics have steeper curves and induce sleep. Barbiturates and benzodiazepines are common sedatives and hypnotics. Benzodiazepines enhance the effects of the inhibitory neurotransmitter GABA at GABA-A receptors, indirectly opening chloride channels. They are metabolized in the liver and some have active metabolites that undergo enterohepatic recycling.

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12 views15 pages

Hypnotics and Sedatives

This document discusses sedatives and hypnotics. It defines sedatives as drugs that calm subjects without inducing sleep, while hypnotics induce and maintain sleep. Both are central nervous system depressants with differing time-action profiles. Sedatives have flatter dose-response curves and are used to calm subjects, while hypnotics have steeper curves and induce sleep. Barbiturates and benzodiazepines are common sedatives and hypnotics. Benzodiazepines enhance the effects of the inhibitory neurotransmitter GABA at GABA-A receptors, indirectly opening chloride channels. They are metabolized in the liver and some have active metabolites that undergo enterohepatic recycling.

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cchatruma
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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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