The post CLOBAZAM Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>7-chloro-1-methyl-5-phenyl-1,5-benzodiazepine-2,4-dione.
Clobazam is a benzodiazepine sedative-hypnotic.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 300.74 g/mol |
2 | Physical appearance | White to almost white crystalline powder |
3 | Melting point | 166-168°C |
4 | Octanol/water partition coefficient | 2.12 |
5 | Solubility | 188 mg/L in water |
6 | Presence of ring | Diazepine, benzene |
7 | Number of chiral centers | Not present |
i. Clobazam binds at distinct binding sites associated with the chloride ionopore present at the post synaptic GABA receptor.
ii. Clobazam increases the opening duration of the chloride ionopore.
iii. This results in increase in the inhibitory effect of GABA through hyperpolarization and stabilization of membrane. [1]
i. 5-chloro-2-nitro-Nphenylaniline is reacted with mono alkyl malonate to produce corresponding alkyl 3-((5-chloro2-nitrophenyl) (phenyl)amino)-3-oxopropanoate.
ii. This on reduction produces diamine compound.
iii. Cyclization of alkyl 3-((2-amino-5- chlorophenyl) (phenyl) amino)-3-oxopropanoate in acid medium produces 8-chloro- 1-phenyllH-benzo[b][l,4]diazepine-2,4(3H,5H)-dione.
iv. Reaction of the above formed compound with methylhalide produces clobazam.
Clobazam is used for:
Side Effects
Side effects of clobazam are:
MCQ
Q.1 ‘7-chloro-1-methyl-5-phenyl-1,5-benzodiazepine-2,4-dione’ is the IUPAC nomenclature of which drug?
a) Clobazam
b) Diazepam
c) Triazolam
d) Mephobarbital
Q.2 Molecular weight of Clobazam?
a) 281.27 gm/mol
b) 300.74 gm/mol
c) 553.78 gm/mol
d) 109.33 gm/mol
Q.3 Match the following with correct classifications of the drugs?
i. Clobazam | A. Benzodiazepine |
ii. Clozapine | B. Butyrophenone class |
iii. Zolpidem | C. Benzapene |
iv. Pimozide | D. Nonbenzodiazepine agonist |
a) i-A, ii-C, iii-D, iv-B
b) i-C, ii-A, iii-D, iv-B
c) i-D, ii-A, iii-B, iv-C
d) i-B, ii-D, iii-A, iv-C
Q.4 Correct steps for the mechanism of action of the drug Clobazam
I. Hyperpolarization and stabilization of membrane
II. Increase in duration of chloride ionopore opening
III. Binding with GABA receptors
a) I – III – II
b) I – II – III
c) III – II – I
d) II – I – III
Q.5 Correct sequence for True and False for the given statements related with the SAR of drug clobazam?
a) TFTF
b) FFTT
c)FTFF
d) FFTF
Q.6 Number of chiral centers present in Clobazam is?
a) 1
b) 2
c) 3
d) 0
Q.7 The drug clobazam is mainly used for?
a) Treatment of Seizures
b) Treatment of dizziness
c) Treatment of drooling
d) All of the above
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1-a
2-b
3-a
4-c
5-b
6-d
7-a
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