This document discusses sedative-hypnotics drugs. It defines sedatives as drugs that reduce excitement and tension, and hypnotics as drugs that induce natural sleep. The document then classifies common sedative-hypnotics such as benzodiazepines and barbiturates. It describes the mechanism of action of benzodiazepines and barbiturates as enhancing the effects of the inhibitory neurotransmitter GABA. The document outlines the pharmacological effects, side effects, and advantages of benzodiazepines relative to barbiturates for use as sedative-hypnotics.

1. SNJB’s SSDJ College of Pharmacy,
Chandwad, Nasik.
SEDATIVE - HYPNOTICS
25-04-2021
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Presented By-
Satpute Manoj Yadavrao
M.Pharmacy 1st Year
Department of Pharmacology
Guided By-
Dr.A.B.Upaganlawar
Associate Professor
Department of Pharmacology

2. CONTENTS :
 DEFINITION
 HISTORY
 CLASSIFICATION
 MECHANISM OF ACTION
 PHARMACOLOGICAL ACTIONS
 SIDE EFFECTS
 ADVANTAGES OF BZD OVER BRT
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3. DEFINITION
 SEDATIVES- Sedatives are CNS depressant agents that
reduce excitement & tension. produce calmness and
relaxation.
 HYPNOTICS-Drugs or chemical that produce sleep
similar to that natural sleep.
 Sleep inducing agents used in Insomnia.
(melatonin hormone responsible for sedation)
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4. HISTORY
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5. INSOMNIA
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6. INSOMNIA TYPES:
 Type1
 Type2
Classification of sleep:
 NREM (Non rapid eye moment sleep)
 REM (Rapid eye moment)
Stages of NREM-
Stage 0- from lying down to falling a sleep.
Stage 1- eye movement .body muscle relax.
(5to10% Total sleep)
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7.  Stage 2- More eye movement. Person may
arousable.(50%Total sleep).
 Stage 3- Deeper sleep with less Eye movement. Person
not easily arousable.
 Stage 4- Deepest level of sleep. Low metabolism rate.
Growth hormone secretion higher. No eye movement.
If awaken –Disorientation.
REM -Dreaming
-HR
-Voluntary muscle relax
-Dream recalled
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8. CLASSIFICATION
 BENZODIAZEPINES-
a) Hypnotics-
e.g. Diazepam, Alprazolam, Flurazepam
b) Anti-anxiety-
e.g. Diazepam, Lorazepam, Oxazepam
C) Anticonvulsant -
e.g. Diazepam, Clonazepam.
 BARBITURATES-
a) Long acting-
e.g. Phenobarbitone, Mephobarbitone
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9. b) Short acting-
e.g. Pentobarbitone, Secobarbitone
c) Ultra short acting-
e.g. Methohexitone, Thiopentone
 NEWER NON-BENZODIZEPINE
e.g. Zolpidem, Zolpiclone, Zaleplon
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10. BENZODIAZEPINES
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 Benzene ring
 Halogen and Nitro group at
7th position confers sedative
hypnotics activity.

11. MECHANISM OF ACTION (BZD)
BZD
Bind in interface of α & γ site at GABAA BZD receptor in CNS
action of GABAA receptor
GABA frequency of Cl- channel opening
Cl- conduction
Neuronal membrane Hyperpolarization
( Sympatic transition)
CNS Depression
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13. PHARMACOGICALACTION
 Reduction of Anxiety.
 Sedation and Hypnotics.
 Muscle Relaxation.
 Anti convalsant.
SIDE EFFECT-
 CNS Depression
BZD ANTAGONIST-
 Flumazenil (BDZ overdosing)
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14. BARBITURATES
 Derivatives of barbituric acid
 Alkyl or Aryl groups at
No 5th position confers sedative-hypnotics activity
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15.  MOA- BRT bind 0n α & β site of GABA
duration of opening of Cl ion channels act as CNS
depression agent
 P’cological Action
Dose dependent action :
 CNS- a) Sedative & Hypnosis
b) Anxiety
c) Produce Euphoria
d) Hyperalgesia
e) Anesthesia (high dose)
f) Anticonvulsant
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16.  Respiratory system-
. a) Respiratory depression (small dose)
b) Respiratory paralysis (high dose)
 Cardiovascular System-
Fall in B.P And H.R
 Kidney-
IV administered urinary output result in G.R
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17.  Adverse Effects-
-Hangover
Mental Confusion
Drowsiness, Constipation
-Prolong administration cause Anemia
-In pregnant women leads to fetal respiratory depression
-Tolerance
 Therapeutic uses-
-sedative hypnotics
-antiepileptic agent
-preanesthetic agent
-general anesthetic agents
-psychiatric disorder like anxiety
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18. BARBITURATE POISONING
o Cause- a) Respiratory paralysis
b) B.P (Hypotension)
o Treatment-
a) Activated charcoal (universal antidote)
b) Gastric cleavage
c) Artificial ventilation
d) Haemodialysis
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19. DOSE-RESPONSE CURVES
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20. ADVANTAGES OF BND OVER BRT
a) Less hangover
b) No respiratory depression
c) No enzyme induction
d) Wide margin of safety
f) Specific antagonist (Flumazenil)
e) Flat/Shallow dose response curve
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Marketed Preparations

22. REFERENCES
 The Pharmacological Basis of Therapeutics, Goodman
and Gillman,12th edition.pg no-457.
 K.D.Thripathi essentials of medical Pharmacology 8th
edition.
 Sedative hypnotics by Dr.D.K.Brahna.
 Lippincott illustrated Reviews-Pharmacology 6th edition
2014.
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