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4/5/2022 1
Hypnotics &
Sedative
Presented by:- Shalini N. Barad
Lecturer,
Appasaheb Birnale College of Pharmacy
4/5/2022 2
uHYPNOTICS:-
are the drugs which depress CNS and induces sleep
resembling to natural sleep, in NORMAL DOSE.
e.g.:- Barbitone, Butobarbitone, Diazepam,
uSEDATIVES:-
are the drugs which depress CNS and BUT DO NOT induces
sleep, in NORMAL DOSE but clams the nerves.
e.g.:- Barbitone, Butobarbitone, Diazepam,
What do you mean by Hypnotics- Sedative
4/5/2022 3
u Hypnotics:-
F Generally hypnotics used to overcome
INSOMNIA. Which is produced by various
factors like emotional trauma, fear,
apprehension or certain disorders.
u Sedatives:-
F They reduces excitement of nerve and hence
are used in relief of tension, anxiety and
restlessness.
4/5/2022 4
u The difference between hypnotics and
sedative is mainly QUANTITATIVE.
u HYPNOTICS in smaller dose may be
sedative
while SEDATIVE in larger dose produces
hypnotic effect.
u Generally hypnotics and sedatives shown a
characteristic property by depression of
cerebrospinal axis.
4/5/2022 5
Useful:-
u Hypnotics and sedatives are useful to:-
F In potentiating of analgesic drugs.
F To control epileptic seizures.
F As an adjunct to anesthesia.
F To treat hypertension due to stress.
F In narcoanalysis in psychiatry, emotional strain.
4/5/2022 6
Classification:-
u I. BARBITURATES:-
F LONG acting barbiturates (6hrs or more)
e.g. Barbitone, Phenobarbitone*
F Intermediate acting barbiturates(3 to 6hrs)
e.g :- Butobarbitone.
F Short acting barbiturates (less than 3hrs)
e.g :- Cyclobarbitone.
F Ultra short acting barbiturates (1/2 to 1hr)
e.g. Methohexitone sod., Thiopentone sod.
4/5/2022 7
Classification:-
II. BENZODIAZEPINE e.g. Diazepam*,
Nitrazepam, Alprazolam
III Miscellaneous:
a) Amides & imide: Glutethimide*
b) Alcohol & their derivatives: Meprobomate
c) Aldehyde and their derivatives: Paraldehyde
Sleep: The duration and patter of sleep varies
considerably among individuals. The different
phases of sleep and their characteristics are
1. Non Rapid eye movement (NREM) :
I. Stage 0 (awake): From lying down to falling
asleep and occasional nocturnal awakening. Eye
movements are regular or slowly rolling.
II. Stage 1 (dozing): Eye movements are reduced
but there may be bursts of rolling. Neck muscles
relax.
III. Stage 2 (unequivocal sleep): Eye movements are
very little, subjects are easily arousable.
4/5/2022 8
IV. Stage 3 (deep sleep transition): Eye movements
are few, subjects are not easily arousable.
V. Stage 4 (cerebral sleep): Eyes are practically
fixed; subjects are difficult to arouse.
Night terror may occur at this time.
Stages 3 and 4 together are called slow wave
sleep (SWS).
2. Rapid eye movement (REM) sleep (paradoxical
sleep): There are marked, irregular and darting
eye movements; dreams and nightmares occur,
which may be recalled if the subject is aroused.
Muscles are fully relaxed, but irregular body
movements occur occasionally.
4/5/2022 9
4/5/2022 10
1. Diazepam:
Molecular formula : C16H13CIN₂O
Structure:
Chemical Name: 7-Chloro-1,3-dihydro-1-
methyl-5-phenyl-2H-1,4-benzo[f]diazepin-2-
one
4/5/2022 11
Uses
1. Diazepam is used to treat anxiety, alcohol
withdrawal, and seizures.
2. It is also used to relieve muscle spasms and to
provide sedation before procedures.
3. This medication works by calming the brain and
nerves.
4. Diazepam have anti-anxiety, sedative, hypnotics,
anticonvulsant properties.
4/5/2022 12
Storage and stability:
• It should be protecting from exposure to light,
and stores at 15-30°C, freezing should be
avoided.
• Diazepam tablets and extended-release
capsule should be stored in tight, light-
resistant containers at 15-30°C.
• Diazepam oral sol & oral concentrate
solution should be stored at 15 -30°C
Formulations: Tablet, capsule, Injection,
Gel.
Brands: Alzepam, Calmpose, Calmod, Dizac,
Qpam, Valium.
4/5/2022 13
2. Alprazolam:
Molecular Structure: C17H13ClN4
Structure:
Chemical Name: 8-chloro-1-methyl-6-phenyl-
4H [1,2,4] triazolo-1,4-benzo[f]diazepine
14
4/5/2022 15
Uses:
1) It is useful in the short-term management of
insomnia characterized by difficulty in falling
asleep, frequent nocturnal awakenings, and early
morning awakenings.
2) Alprazolam is used to treat anxiety disorders and
panic disorder.
Storage and stability:
• Keep container tightly closed in a dry and well-
ventilated place.
• It should be stored in tight, light-resistant
containers at 15-30°C.
Formulations: Tablet, Capsule, Syrup,
Cream, Gel, Ointment, liquid or injection.
Brands: Aaram, Abizox, Abizox-P, Abizox-
SR, Agcalm, Agcalm-P, Alamflu, Alap.
4/5/2022 16
3. Phenobarbital:
Molecular Formula: C12H12N2O3
Structure:
Chemical Name: 5-ethyl-5-phenylpyrimidine-
2,4,6(1H,3H,5H)-trione
4/5/2022 17
Uses:
1) It is used as long-acting sedative hypnotic
and antiepileptic especially for grandmaal
and petitmal epilepsy.
2) It is useful in nervous and related tension
states.
Storage and stability: It should be
dispensed in well-closed containers. Store at
controlled room temperature 15-30°C.
Formulations: Tab:- IP, Cap:- IP,BP. Elixer-
BP, Inj:- USP.
Brands: Fenobarb, Phenetone, Beetal,
Epitan, Gardenal.
4/5/2022 18
4. Nitrazepam:
Molecular Formula: C15H11N3O3
Uses:
1) It is used to treat the insomnia
2) It's normally used in conjunction with other drugs.
It relaxes the brain and helps in the treatment of
people who have difficulty sleeping.
Storage and stability: Store it at room
temperature. Protect from light and moisture.
Formulations: Tablet, Capsule, Injection.
Brands: Nitravet, Nitraz-5, Nitraz-10, Nitrosun,
Insomin Forte, Gentravit, Hypnotex.
4/5/2022 19
Thank You
4/5/2022 20

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Hypnotics & sedatives

  • 1. 4/5/2022 1 Hypnotics & Sedative Presented by:- Shalini N. Barad Lecturer, Appasaheb Birnale College of Pharmacy
  • 2. 4/5/2022 2 uHYPNOTICS:- are the drugs which depress CNS and induces sleep resembling to natural sleep, in NORMAL DOSE. e.g.:- Barbitone, Butobarbitone, Diazepam, uSEDATIVES:- are the drugs which depress CNS and BUT DO NOT induces sleep, in NORMAL DOSE but clams the nerves. e.g.:- Barbitone, Butobarbitone, Diazepam, What do you mean by Hypnotics- Sedative
  • 3. 4/5/2022 3 u Hypnotics:- F Generally hypnotics used to overcome INSOMNIA. Which is produced by various factors like emotional trauma, fear, apprehension or certain disorders. u Sedatives:- F They reduces excitement of nerve and hence are used in relief of tension, anxiety and restlessness.
  • 4. 4/5/2022 4 u The difference between hypnotics and sedative is mainly QUANTITATIVE. u HYPNOTICS in smaller dose may be sedative while SEDATIVE in larger dose produces hypnotic effect. u Generally hypnotics and sedatives shown a characteristic property by depression of cerebrospinal axis.
  • 5. 4/5/2022 5 Useful:- u Hypnotics and sedatives are useful to:- F In potentiating of analgesic drugs. F To control epileptic seizures. F As an adjunct to anesthesia. F To treat hypertension due to stress. F In narcoanalysis in psychiatry, emotional strain.
  • 6. 4/5/2022 6 Classification:- u I. BARBITURATES:- F LONG acting barbiturates (6hrs or more) e.g. Barbitone, Phenobarbitone* F Intermediate acting barbiturates(3 to 6hrs) e.g :- Butobarbitone. F Short acting barbiturates (less than 3hrs) e.g :- Cyclobarbitone. F Ultra short acting barbiturates (1/2 to 1hr) e.g. Methohexitone sod., Thiopentone sod.
  • 7. 4/5/2022 7 Classification:- II. BENZODIAZEPINE e.g. Diazepam*, Nitrazepam, Alprazolam III Miscellaneous: a) Amides & imide: Glutethimide* b) Alcohol & their derivatives: Meprobomate c) Aldehyde and their derivatives: Paraldehyde
  • 8. Sleep: The duration and patter of sleep varies considerably among individuals. The different phases of sleep and their characteristics are 1. Non Rapid eye movement (NREM) : I. Stage 0 (awake): From lying down to falling asleep and occasional nocturnal awakening. Eye movements are regular or slowly rolling. II. Stage 1 (dozing): Eye movements are reduced but there may be bursts of rolling. Neck muscles relax. III. Stage 2 (unequivocal sleep): Eye movements are very little, subjects are easily arousable. 4/5/2022 8
  • 9. IV. Stage 3 (deep sleep transition): Eye movements are few, subjects are not easily arousable. V. Stage 4 (cerebral sleep): Eyes are practically fixed; subjects are difficult to arouse. Night terror may occur at this time. Stages 3 and 4 together are called slow wave sleep (SWS). 2. Rapid eye movement (REM) sleep (paradoxical sleep): There are marked, irregular and darting eye movements; dreams and nightmares occur, which may be recalled if the subject is aroused. Muscles are fully relaxed, but irregular body movements occur occasionally. 4/5/2022 9
  • 11. 1. Diazepam: Molecular formula : C16H13CIN₂O Structure: Chemical Name: 7-Chloro-1,3-dihydro-1- methyl-5-phenyl-2H-1,4-benzo[f]diazepin-2- one 4/5/2022 11
  • 12. Uses 1. Diazepam is used to treat anxiety, alcohol withdrawal, and seizures. 2. It is also used to relieve muscle spasms and to provide sedation before procedures. 3. This medication works by calming the brain and nerves. 4. Diazepam have anti-anxiety, sedative, hypnotics, anticonvulsant properties. 4/5/2022 12
  • 13. Storage and stability: • It should be protecting from exposure to light, and stores at 15-30°C, freezing should be avoided. • Diazepam tablets and extended-release capsule should be stored in tight, light- resistant containers at 15-30°C. • Diazepam oral sol & oral concentrate solution should be stored at 15 -30°C Formulations: Tablet, capsule, Injection, Gel. Brands: Alzepam, Calmpose, Calmod, Dizac, Qpam, Valium. 4/5/2022 13
  • 14. 2. Alprazolam: Molecular Structure: C17H13ClN4 Structure: Chemical Name: 8-chloro-1-methyl-6-phenyl- 4H [1,2,4] triazolo-1,4-benzo[f]diazepine 14
  • 15. 4/5/2022 15 Uses: 1) It is useful in the short-term management of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and early morning awakenings. 2) Alprazolam is used to treat anxiety disorders and panic disorder. Storage and stability: • Keep container tightly closed in a dry and well- ventilated place. • It should be stored in tight, light-resistant containers at 15-30°C.
  • 16. Formulations: Tablet, Capsule, Syrup, Cream, Gel, Ointment, liquid or injection. Brands: Aaram, Abizox, Abizox-P, Abizox- SR, Agcalm, Agcalm-P, Alamflu, Alap. 4/5/2022 16
  • 17. 3. Phenobarbital: Molecular Formula: C12H12N2O3 Structure: Chemical Name: 5-ethyl-5-phenylpyrimidine- 2,4,6(1H,3H,5H)-trione 4/5/2022 17
  • 18. Uses: 1) It is used as long-acting sedative hypnotic and antiepileptic especially for grandmaal and petitmal epilepsy. 2) It is useful in nervous and related tension states. Storage and stability: It should be dispensed in well-closed containers. Store at controlled room temperature 15-30°C. Formulations: Tab:- IP, Cap:- IP,BP. Elixer- BP, Inj:- USP. Brands: Fenobarb, Phenetone, Beetal, Epitan, Gardenal. 4/5/2022 18
  • 19. 4. Nitrazepam: Molecular Formula: C15H11N3O3 Uses: 1) It is used to treat the insomnia 2) It's normally used in conjunction with other drugs. It relaxes the brain and helps in the treatment of people who have difficulty sleeping. Storage and stability: Store it at room temperature. Protect from light and moisture. Formulations: Tablet, Capsule, Injection. Brands: Nitravet, Nitraz-5, Nitraz-10, Nitrosun, Insomin Forte, Gentravit, Hypnotex. 4/5/2022 19