benzodiazepines as sedative hypnotic
Post on 13-Feb-2017
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Presented by…….
DIPTARCO SINGHA, DURJOY GHOSH &
HRISHAV ROY CHOWDHURY
B.PHARM, 3RD YEAR, 6TH SEMESTER
GURU NANAK INSTITUTE OF PHARMACEUTICAL SCIENCE & TECHNOLOGY
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Benzodiazepines as Sedative - Hypnotic
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Introduction: SEDATIVES CNS depressant drugs , reduce excitement & tension, & produce calmness & relaxation.
HYPNOTICS drugs that produce sleep similar to that of natural arousal sleep.
Both sedative & hypnotic action may reside in the same drug.
A small dose may act as sedative, whereas a large dose of the same drug may act as a hypnotic.
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Classes of Benzodiazepine:
Benzodiazepines
1,4-benzodiazepines
Triazolobenzo-diazepines
Imidazobenzo-diazepine
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Structure:1. 1,4-benzodiazepines
Drug Name
R1 R2 R3 R7 R2’
Diazepam -CH3 =O -H -Cl -H
Prazepam -CH2- =O -H -Cl -H
Oxazepam -H =O -OH -Cl -H
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Structure:2. Triazolobenzodiazepines
Drug Name
R R1
Alprazolam -CH3 -H
Triazolam -CH3 -Cl
Estazolam -H -H
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Structure:3. Imidazobenzodiazepinese.g.
Midazolam Loprazolam
MOA:
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SAR of Benzodiazepine:I. Presence of phenyl ring / pyridyl ring promotes
sedative-hypnotic activity at C5-position.II. If presence of electron withdrawing group like –Cl or
–NO2 (Lorazepam, Clonazepam) at R2’ position, then sedative-hypnotic activity .
III. Presence of electron withdrawing group like –Cl, -F, –NO2 at C7 position, activity.
IV. Substitution at 6,8,9 position of carbon atom, activity.
V. Shifting of double bond present between –N4 & C5 or saturation of double bond activity.
VI. R3 = alkyl group, activity & R3 = -OH or –COOH activity & R1 = -CH3 ,if larger group is present activity.
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Conclusion: Sleep is mainly loss of consciousness. Sleep
is an architectured cyclic process.
These drugs maintains the sleep-wake cycle.
Insomnia is a symptom & its proper treatment depends on finding the cause of sleeplessness. To treat this type of patient, use sedative-hypnotics.
High dose of the drugs may lead to coma or death.
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Marketed Benzodiazepine drugs:
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References:
D. Sriram & P. Yogeeswari, Medicinal Chemistry, 2nd Ed., Pearson, Sedatives, Hypnotics, & Anxiolytic Agents, Benzodiazepines, Page no.: 129-151.
KD Tripathi M.D., Essentials of Medical Pharmacology, 7th Ed., Jaypee Brothers Medical Publishers (P) Ltd., Sedative-Hypnotic, Benzodiazepines, Page no.: 397-410.
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THANK YOU
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