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]]>8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine.
Loxapine is an antipsychotic drug.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 327.8 g/mol |
2 | Physical appearance | Pale yellow crystals from petroleum ether. |
3 | Melting point | 109-111°C |
4 | Solubility | 1.03e-01 g/L |
5 | Octanol/water partition coefficient | 3.6 |
6 | Presence of ring | Piperazine |
7 | Number of chiral centers | Not present |
Loxapine is a dopamine antagonist and serotonin 5-HT2 blocker. Exact mechanism of action is not known. Changes in the level of excitability of subcortical inhibitory areas have been observed, producing calming effects and suppression of aggressive behavior.
Structure activity relationship of phenothiazine like compounds can be described as follows:
i. 2-(4-chlorophenoxy)anyline undergoes acylation using ethylchloroformate to produce N-ethoxycrbonyl-2-(4-chlorophenoxy)aniline.
ii. Treatment of the above formed compound with the mixture of phosphorus oxychloride and phosphorus anhydride yields loxapine.[2]
Loxapine is used for:
Side effects of loxapine are:
Q.1 What are the correct statements related with the physicochemical properties of Loxapine drug?
I. Molecular weight = 300 gm/mol
II. It appears as pale yellow crystals
III. No chiral carbon is present in its structure
IV. Phenothiazine ring is present in the structure
a) I, II, III
b) I, II, IV
c) II, III
d) I. II. III. IV
Q.2 Match the following of the drugs with their correct IUPAC names.
i. Loxapine | A. 7-Chloro-1,3-dihydro-3-hydroxy-1-methyl-5-phenyl-1,4-benzodiazepin-2-one |
ii. Quazepam | B. 8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine |
iii. Temazopam | C. 7-chloro-5-(2-fluorophenyl)-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepine-2-thione |
iv. Clobazam | D. 7-chloro-1-methyl-5-phenyl-1,5-benzodiazepine-2,4-dione |
a) i-B, ii-C, iii-A, iv-D
b) i-C, ii-A, iii-D, iv-B
c) i-A, ii-C, iii-D, iv-B
d) i-D, ii-A, iii-C, iv-B
Q.3 Loxapine is antagonist for which receptors?
I. Dopaminergic receptors
II. Serotonin 5-HT2
III. ß-adrenoceptors
IV. α-adrenoceptors
a) I, III, IV
b) I, II
c) III, IV
d) I, II, IV
Q.4 Correct sequence for True/false for the classification of the drug can be?
a) TFTT
b) TTFF
c) FFTT
d) FFFT
Q.5 Greater potency of phenothiazines with Piperazine side chain substitution is due to?
a) Greater number of favourable Van der Waal’s contacts
b) Bleaching action of chlorine
c) Affinity of fluorine with potassium is higher
d) High molecular weight of fluorine
Q.6 Correct steps for the synthesis of loxapine drug from 2-(4-chlorophenoxy)anyline is?
I. Treatment with Phosphoprus oxychloride
II. Treatment with the mixture of Phosphorus oxychloride and Phosphorus anhydride
III. Acylation with Ethylchloroformate
IV. Alkylation with Ethylchloroformate
a) I – III
b) III – II
c) II – IV
d) III – II
Q.7 Side effect of drug Loxapine are?
a) Depression
b) Muscle spasms
c) Constipation
d) All of the above
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1-c
2-a
3-b
4-a
5-a
6-d
7-d
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