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]]>8-chloro-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine.
Estazolam is a benzodiazepine sedative-hypnotic.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 294.74 g/mol |
2 | Physical appearance | Solid |
3 | Melting point | 228.5°C |
4 | Octanol/water partition coefficient | 4.7 |
5 | Solubility | Practically insoluble |
6 | Presence of ring | Diazepine, triazole, benzene |
7 | Number of chiral centers | Not present |
i. Estazolam binds nonspecifically with benzodiazepine receptors BNZ1.
ii. It coupled with GABAA receptors and increases the GABA affinity for the GABA receptor.
iii. This results in opening of the chloride channel and thus, causes hyperpolarization of the cell membrane which prevents further excitation of the cell.
Structure Activity Relationship
i. (Z)-7-chloro-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one reacts with phosphorus pentasulfide to give (Z)-7-chloro-5-phenyl-1H-benzo[e][1,4] diazepine-2(3H)-thione .
ii. The compound then undergoes reaction with hydrazine to form 1-((1E,4Z)-7-chloro-5-phenyl-3H-benzo [e][1,4]diazepin-2-yl)hydrazine.
iii. On reaction with trimethoxyerhane, Estazolam is synthesized.
Estazolam is used for:
Side effects of Estazolam are:
MCQs
Q.1 Sedative-hypnotic effect of estazolam is through?
a) Increase the affinity of GABA for GABA receptors
b) Decrease the affinity of GABA for GABA receptors
c) Blocking the calcium channel
d) Alkalization of nuclear material
Q.2 Therapeutic use of drug Estazolam is/are?
a) Treatment of memory loss
b) Sedation during time of Insomnia
c) Treatment of Diabetes
d) Both a) and b)
Q.3 Which amongst the following are the correct statements with respect to the SAR of drug estazolam?
I. Tri-keto form is least stable in aqueous solution.
II. 4,6-dialcoholic tautomeric forms are most stable in aqueous solution.
III. 5,5-disubstituted barbituric acid is the prime requirement for the barbituares to be sedative hypnotics.
a) I, II, III
b) I, II
c) II, III
d) III
Q.4 Number of chiral centers present in the structure of Estazolam?
a) 0
b) 1
c) 2
d) 3
Q.5 Correct sequence for the True/False for the physiochemical properties of the drug Estazolam?
I. Molecular weight = 294.74 gm/mol
II. It is insoluble in water
III. Melting point is 174°C
a) TTF
b) FTF
c) TFT
d) FTT
Q.6 Correct statements for the IUPAC nomenclatures of the drugs are?
I. Estazolam: 5-Ethyl-5-phenyl-1,3-diazinane-2,4,6-trione
II. Oxazepam: 5-oxo-D-prolyl-L-histidyl-Ltryptophyl-L-seryl-Ltyrosyl-3-(1H-indol-2-yl)-L-alanylleucyl-L-arginyl-L-prolylglycinamide.
III. Epinephrine: (R)-3-[-1-hydroxy-2-(methylamino)ethyl]phenol
IV. Zaleplon: (RS)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide.
a) I, II, III
b) I, IV
c) I, III
d) None
Q.7 Match the following drugs with their correct classifications-
i. Oxazepam | A. Benzodiazepine |
ii. Clozapine | B. Nonbenzodiazepine agonist |
iii. Zolpidem | C. Benzapene |
iv. Butabarbital | D. Barbiturate |
a) i-D, ii-B, iii-C, iv-A
b) i-D, ii-C, iii-B, iv-A
c) i-A, ii-C, iii-B, iv-D
d) i-A, ii-C, iii-B, iv-D
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1-a
2-b
3-d
4-a
5-a
6-d
7-c
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