how sleep is occured

1. SEDATIVE-HYPNOTICS
Presented By :-Sutirtha Patra
B.Pharm,3rd year (6th sem)
Roll No:-18901915119
Reg No:-151890210119 of 2015-16
Guide:-Dr Shyamshree S S Manna
DR. B. C. ROY COLLEGE OF PHARMACY AND ALLIED HEALTH SCIENCE, DURGAPUR

2. INTRODUCTION
 DEFINATION
 SLEEP
 CLASSIFICATION OF SEDATIVE-HYPNOTIC DRUGS
 BARBITURATES
 BENZODIAZEPINES
 NEWER NON-BENZODIAZEPINES HYPOTONICS

3. SEDATIVE-HYPNOTIC
Sedative:- A drug that subdues excitement and calms the
subject with out inducing sleep, though drowsiness may be
produced –refers to decreased responsiveness to any level of
stimulation; is associated with some decrease in motor
activity and ideation -depression of awareness to the
environment and reduction of responsiveness to external
stimulation.
Hypnotic:- A drug that induces and/or maintains sleep,
similar to normal sleep which is can be aroused. Should not
be confused with “Trans like state” - hypnosis, meditation,
magic, flow, and prayer etc. – subjects are passive and
highly suggestible.

4. SLEEP AND TYPES OF SLEEP
The duration and pattern of sleep varies considerably among
individuals. Age has an important effect on quantity and depth of
sleep. It has been recognized that sleep is an architecture cyclic
process.
The different phases of sleep:-
 Stage 0(awake)-Sleep time 1-2%
 Stage 1(dozing)-Sleep time 3-6%
 Stage 2(unequivocal sleep)-Sleep time 40-50%
 Stage 3(deep sleep transition)-Sleep time 5-8%
 Stage 4(cerebral sleep)-Sleep time 10-20%
 REM sleep(paradoxical sleep)-Sleep time20-30%

5. SEDATIVE-HYPNOTIC DRUGS
Types of drugs:-
Barbiturates:
Benzodiazepines:-
Newer nonbenzodiazepine hyponics:-
Hypnotic Antianxiety Anticonvulsant
Diazepam Diazepam Diazepam
Flurazepam Chlordiazepoxide Lorazepam
Long acting Short acting Ultra short acting
Phenobarbitone Pentobarbitone Thiopentone
Zopiclone Zolpidem Zaleplon

6. BARBITURATES
Barbiturates depress the CNS at all level in a dose-dependent
fashion. Now it mainly used in anesthesia and treatment of
epilepsy; use as sedative-hypnotic agents is no longer
recommended.
Mechanism of Action:-
1) Barbiturates share with benzodiazepines the ability to
enhance the action of GABA, but they bind at a different site on
the GABA receptor/chloride channel, and their action seems to
prolong the duration of the opening of GABA-activated chloride
channels.

7. BARBITURATES
(2) At high doses, barbiturates can inhibit the release of the Ca2+ -
dependent neurotransmitter.

8. BARBITURATES
Therapeutic uses :-
• Sedative-hypnotic agents
• Be used in the emergency treatment of convulsions as in status
epilepticus.
• Anesthetic (or be given before anesthetic)
• Combination with antipyretic-analgesic
• Treatment of hyperbilirubinemia and kernicterus in the neonate.
Adverse effects:-
• CNS: Barbiturates cause drowsiness, impaired concentration.
• Drug hangover: Hypnotic doses of barbiturates produce a feeling of
tiredness well after the patient wakes.
• Barbiturates induce the P450 system.
• By inducing aminolevulinic acid (ALA) synthetase, barbiturates
increase porphyrin synthesis, and are contraindicated in patients
with acute intermittent porphyria

9. BENZODIAZEPINES
Hypnotic Antianxiety Anticonvulsant
Diazepam Diazepam Diazepam
Flurazepam Chlordiazepoxide Lorazepam
Mechanism of Action:-

10. BENZODIAZEPINES
Use of Benzodiapines:-
As Hypnotic- Not all are useful as hypnotic agents, although
all have sedative or calming effects
As anxiolytic and for day time sedation
As anticonvulsant – status epilepticus, febrile convulsion,
tetanus
As Muscle relaxant (centrally acting)
Preananesthetic medication, IV anesthesia and conscious
sedation
Alcohol and other sedative-hypnotic withdrawal

11. BENZODIAZEPINES
Adverse effect:-
1. Light-headedness
2. Fatigue
3. Increased reaction time
4. Motor incoordination
5. Impairment of mental and motor functions
6. Confusion
7. Antero-grade amnesia

12. NEWER NON-BENZODIAZEPINES HYPOTONICS
Zopiclone:-
Cyclopyrrolone derivative- active metabolite –
N-desmethylzopiclone
MOA: Binds to α subunit of BZD receptor (Unlike BZD) –
hypnotic action.
No sleep architecture distortion or withdrawal phenomena
Uses: to wean off insomniacs on BZD and short term
therapy for insomnia
Half life: 5 – 6 hours
Adverse effect:-
Taste disturbance vomiting, drowsiness, drymouth, headache

13. NEWER NON-BENZODIAZEPINES HYPOTONICS
Zolpidem:-
MOA: Acts on α1 subunit of BZD receptor (hypnotic)
Lack of effect on sleep stages (REM)
Uses: short term therapy of sleep onset insomnia –
day time sedation less (short half life) – late night(!)
Half life –2 hrs.
Adverse effect:-
For short-term use :-
headache, drowsiness (2%), dizziness (1%), diarrhea (1%)
For long-term use :-
dry mouth (3%),allergy (4%),back pain (3%), chest pain (1%),

14. NEWER NON-BENZODIAZEPINES HYPOTONICS
Zaleplon:-
Does not prolong total sleep time or reduce the number of awakenings
No tolerance or dependence
Uses: Sleep-onset insomnia (1-2 weeks therapy)
Half life - 1 hr.
Adverse effect:-
Muscle cramps
vomiting
sweating
tremors
convulsions

15. REFFERENCE
1. Essentials of Medical Pharmacy by KD Tripathi.
2. SEDATIVE-HYPNOTICS by Dr. D. K. Brahma
3. Sedative-Hypnotic Drugs

16. THANK YOU