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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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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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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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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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