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]]>8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine
Midazolam is a benzodiazepine sedative-hypnotic.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 325.8 g/mol |
2 | Physical appearance | White to light yellow crystalline solid |
3 | Melting point | 159°C |
4 | Octanol/water partition coefficient | Log Kow=4.33 |
5 | Solubility | 1.34X10-1 mg/L in water |
6 | Presence of ring | Present |
7 | Number of chiral centers | Not present |
The sedation effect, relaxing of skeletal muscles, inducing of sleep, anesthesia and amnesia properties of drug is due to the increase in activity of GABA by the drug. Midazolam binds with GABAA receptors and potentiates the effects of GABA by increasing the frequency of chloride channel opening and hyperpolarization.
(2-amino-5-chlorophenyl)(2-fluorophenyl)methanone and N-(3-amino-2-oxopropyl)acetamide undergoes a ring forming reaction in the presence of a catalyst to give midazolam. [2]
Midazolam is used for:
Side effects of Midazolam are:
Q.1 Match the following with correct SAR of the drug Midazolam-
i. An electronegative group at 7-position of the ring A | A. Increases the functional anxiolytic activity |
ii. Substitutions at 6, 8 or 9 position with electronegative group on ring A | B. Decreases the functional anxiolytic activity |
C. Decrease the functional anxiolytic activity | |
D. Increase the functional anxiolytic activity |
a) i-A, ii-D
b) i-A, ii-C
c) i-B, ii-C
d) i-B, ii-D
Q.2 Correct sequence for the True/False for correct IUPAC names of the drug can be?
a) TFTF
b) TTFF
c) FFTT
d) TTFT
Q.3 Number of chiral carbons present in the structure of Midazolam?
a) 0
b) 1
c) 2
d) 3
Q.4 Midazolam drug shows its action through??
a) Agonizing the acetylcholine receptors
b) Antagonizing the muscarinic receptors
c) Binding with GABAA receptors
d) ß-inhibition
Q.5 Which amongst the following is a therapeutic use of drug Midazolam?
a) Inducing drowsiness in children
b) Treatment of Alzhiemer’s disease
c) Treatment of Overactive bladder
d) Treatment of Asthma
Q.6 Which of the following drug and their classification are correct?
I. Benztropin: acetylcholine antagonist
II. Fesoterodine: Nitrogen mustard
III. Flurazepam: benzodiazepine sedative hypnotic
IV. Midazolam: Acetylcholine Nicotinic receptor antagonist
a) I, III
b) I, III, IV
c) II, IV
d) I, II, III, IV
Q.7 (2-amino-5-chlorophenyl)(2-fluorophenyl)methanone and N-(3-amino-2-oxopropyl)acetamide undergoes a ring forming reaction in the presence of a catalyst to give which drug?
a) Fesoterodine
b) Midazolam
c) Fludarabine
d) Methotrexate
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1-a
2-b
3-a
4-c
5-a
6-a
7-b
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