Introduction to Sedative-Hypnotics Drugs Sleep, Introduction to Sedatives -hypnotics, Sedative-hypnotic drug classification, Pharmacology of sedative-hypnotic drugs, Overview, New inventions Presented by AGGIM SUMASHREE Department of Pharmacology

1. Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721
A Seminar as a part of curricular requirement for
M . Pharmacy I year I Semester
Presented by
AGGIM SUMASHREE
(20L81S0102)
Pharmacology
Under the guidance of
A .Sudheer Kumar M.Pharm, (Ph.D)
Assistant Professor

2. RIPER
AUTONOMOUS
NAAC &
NBA (UG)
SIRO- DSIR
Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721
Contents :
 Sleep
 Introduction to Sedatives -hypnotics
 Sedative-hypnotic drug classification
 Pharmacology of sedative-hypnotic drugs
 Overview
 New inventions
 References
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3. RIPER
AUTONOMOUS
NAAC &
NBA (UG)
SIRO- DSIR
Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721
Sleep:
 Normal sleep cyclic and repetitive, consists of distinct stages based
on three physiological measures: the electroencephalogram, the
electromyogram and the electronystagmogram.
 Non rapid eye movement (NERM)sleep
70%-75%
stage 1,2
stage 3,4:slow wave sleep,sws
 Rapid eye movement(REM) sleep
3

4. RIPER
AUTONOMOUS
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SIRO- DSIR
Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721
A normal sleep cycle

5. RIPER
AUTONOMOUS
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NBA (UG)
SIRO- DSIR
Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721
• An effective sedative agent should reduce anxiety and exert a calming
effect with little or no effect on motor or mental functions.
• A hypnotic drug produce drowsiness and encourage the onset and
maintenance of a state of sleep that as far as possible resembles the natural
sleep state.
• Hypnotics effects involve more pronounced depression.
• Graded dose-dependent depression of CNS function is a characteristic of
sedative-hypnotics.
Sedatives-hypnotics:

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Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721
Classification :
 Benzodiazepines:
1.Short acting : Triazolam, Temazepam
2.Intermediate acting: Alprazolam, Lorazepam
3.Long acting: Diazepam
 Barbiturtes:
1.long acting: Phenobarbitone
2.Short acting: Butobarbitone, Pentobarbitone
3.Ultra-short acting: Thiopentone, Methohexitone
 Miscellaneous agents: Buspirone, Zaleplon, Zolpidem, cholarhydrate.
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K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 7

8. RIPER
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SIRO- DSIR
Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721
Pharmacology of drugs:
Pharmacology includes
 Mechanism of action
 Pharmacokinetics
 Adverse effects
 Therapeutic uses
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Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721
Mechanism of action:
Sedatives-hypnotics
Bind to GABA receptor at different allosteric sites
Facilitates GABA action
Barbiturates increase duration and benodiazepines increase frequency
of opening of cl channel
Membrane hyperpolarization
CNS depression
9

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Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 10

11. RIPER
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SIRO- DSIR
Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721
Pharmacokinetics:
 Benzodiazipines:
Absorption: orally/I.M/I.V
distribution: pass BBB and Placenta,
secreted into breast milk
Metabolism: in liver by microsomal enzyme
Half-life: long acting-1-3days
short acting-3-8hrs
Intermediate acting-10-20hrs
Excretion: excreted as glucoronide conjugates in urine.
11

12. RIPER
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Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721
 Barbiturates :
Absorption: oral/I.V/I.M
Distribution: to all body
Metabolism: Liver
Excretion: alkalinization of the urine expedites the excretion of
barbiturates.
12

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Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721
Adverse effects :
• Cross placental barrier
• Depression of neonatal vital function
• Detectable in breast milk
• Cvs depression
• Dependence
• Drug-drug interaction
• Pophyria
• Paradoxical excitement in children
13

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Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721
Therapeutic uses
• Epilepsy in emergency
• Short-term use of sedative-hypnotics for treating anxiety
• Premedication prior to surgery
• Panic and Agoraphobia
• Reduces anxiety and aggression
• Sleep disorder, insomnia
• Treatment of muscle plasticity in cerebral plasy and tetanus
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15. RIPER
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Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721
New inventions:
 ROZEREM-Ramelteon
• It appears to be a promising novel hypnotic, provided its
efficacy is established.
• It is a MT1 and MT2 Melatonin receptor agonist introduced in
USA and now approved in India.
 Meloset, Zytonin, Externex are some of the marketed
melatonin receptor agonist drugs.
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16. RIPER
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Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721
Overview :
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K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 17

18. RIPER
AUTONOMOUS
NAAC &
NBA (UG)
SIRO- DSIR
Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 18

19. RIPER
AUTONOMOUS
NAAC &
NBA (UG)
SIRO- DSIR
Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721
References :
• JAMES M. RITTER et,al. “RANG AND DALE’S Textbook of
Pharmacology” 9TH edition 2018 p.577
• KD TRIPATHI “Essentials of Medical Pharmacology Textbook of
pharmacology 7th edition 2013 p.397.
• LUCIA SUKYS-CLAUDINO et al. Braz J Psychiatry Article in
Portuguese 2010 sep- PubMed,gov
19

20. RIPER
AUTONOMOUS
NAAC &
NBA (UG)
SIRO- DSIR
Raghavendra Institute of Pharmaceutical Education and Research - Autonomous
K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 20