INTRODUCTION CLASSIFICATION: SEDATIVE AND HYPNOTICS BARBITURATES BENZODIAZEPINES SITE OF ACTION MECHANISM OF ACTION NEWER NONBENZODIAZEPINES HYPNOTICS PHARMACOKINETICS SIDE EFFECTS Mechanism of action Benzodiazepines Increase frequency of opening of cl- channels induced by GABA. Increase binding of GABA to GABA® receptor. Reduction of anxiety. Reduce anxiety by selectively enhancing GABAergic transmission in neurons having the α-2 subunit in their GABA® receptor. The hypnotic effect are mediated by α1-GABA® receptor Anticonvulsant effect is partially although not completely, mediated by α1-GABA® receptors.

1. SEDATIVES AND HYPNOTICS
A
SEMINAR
OF
MASTER OF PHARMACY
IN
PHARMACOLOGY
BY
PRAKHAR VARSHNEY
M.PHARM (PHARMACOLOGY) 1ST SEM 1STYEAR
SUBJECT CODE - MPL102T
SUBJECT NAME- ADVANCED PHARMACOLOGY – I
DEPARTMENT OF PHARMACOLOGY
TEERTHANKER MAHAVEER COLLEGE OF PHARMACY
TEERTHANKER MAHAVEER UNIVERSITY
MORADABAD INDIA
SESSION: 2022-2023 1

2. CONTENTS
1. INTRODUCTION
2. CLASSIFICATION: SEDATIVE AND HYPNOTICS
3. BARBITURATES
4. BENZODIAZEPINES
5. SITE OF ACTION
6. MECHANISM OF ACTION
7. NEWER NONBENZODIAZEPINES HYPNOTICS
8. PHARMACOKINETICS
9. SIDE EFFECTS
10. REFERENCES
2

3. INTRODUCTION
Sedatives and hypnotics used to treat Insomnia (poor sleeping).
SEDATIVES:- A drug that reduces excitement, calms the subject without
inducing sleep.
Ex:-Phenobarbitone, Thiopentone, Alperazolam , Oxazepam
HYPNOTICS:- A drug which produces sleep resembling natural sleep.
Hypnotics are used to maintain the sleep.
Ex:-diazepam, clonazepam, clobazam
3

4. TRANSIENT INSOMNIA
1-3 DAYS
SHORT ACTING INSOMNIA
3-21 DAYS
CHRONIC INSOMNIA
>3 DAYS
I
N
S
O
M
I
N
A
INSOMNIA are related
to poor sleeping habits,
depression, anxiety, lack of
exercise, chronic illness

5. SEDATIVES
AND
HYPNOTICS
BARBITURATES
BENZODIAZEPINES
NEWER NONBENZODIAZEPINE
HYPNOTICS
5

6.  BENZODIAZEPINES ARE A CLASS OF DRUGS THAT
CAN TREAT RANGE OF CONDITIONS. DOCTORS
OFTEN TO PRESCRIBE THEM TO TREAT ANXIETY,
SEIZURES, AND INSOMNIA.
 THE SHORT TERM USE OF THESE MEDICATION IS
USUALLY SAFE AND EFFECTIVE BUT LONG TERM
USE CAN LEAD TO TOLERANCE, DEPENDENCE,
AND OTHER ADVERSE EFFECT.

7. 7

8. 8

9. 9

10. 10

11. 11
REFERENCE;- https://www.slideshare.net/drashutoshtiwari/sedative-hypnotic-45187755

12. SITE OF ACTION
• Midbrain- Wakefulness
• Limbic system- Thought & mental functions
• Medulla – Muscle Relaxation
• Cerebellum – Ataxia
 Effect : Limbic system > midbrain RAS
Therapeutic dose Anxiolytic > Sedative
Higher dose Depress RAS Sedative effect and hypnotic effect
12

13. 13
Sedation
(Sedatives)
Sleep
(hypnotics)
Anesthesia
Anesthetic
Coma Death
Dose Dependent Action

14. 14

15. 15
REFERENCE;- https://www.slideshare.net/drashutoshtiwari/sedative-hypnotic-45187755

16. 16
Mechanism of action
Benzodiazepines
I. Increase frequency of opening of cl- channels induced by GABA.
II. Increase binding of GABA to GABA® receptor.
III. Reduction of anxiety. Reduce anxiety by selectively enhancing
GABAergic transmission in neurons having the α-2 subunit in their
GABA® receptor.
IV.The hypnotic effect are mediated by α1-GABA® receptor
V. Anticonvulsant effect is partially although not completely, mediated by
α1-GABA® receptors.

17. Pharmacokinetics
1. Slow elimination of parent drug & active metabolite.
2. Relatively slow elimination but marked
redistribution.
3. Relatively slow elimination but marked
redistribution.
4. Ultrarapid elimination
5. Lipophilic
17

18. SIDE EFFECTS OF SEDATIVES AND HYPNOTICS
1. Somnolence (drowsiness)
2. Headache
3. Asthenia (weakness)
4. Ataxia (impaired coordination, balance and speech)
5. Neuromuscular and skeletal weakness.
6. Hallucination
7. Dry mouth
8. Short- term forgetfulness

19. THANK YOU