The post PHENYTOIN Synthesis, SAR, MCQ, Structure, Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>5,5-diphenylimidazolidine-2,4-dione.
Phenytoin is a hydantoin derivative anticonvulsant drug.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 252.27 g/mol |
2 | Physical appearance | White crystalline powder |
3 | Melting point | 296.5°C |
4 | Solubility | Insoluble in cold water; soluble in acetic acid |
5 | Octanol/water partition coefficient | 2.47 |
6 | Presence of ring | Imidazolidine, phenyl |
7 | Number of chiral centers | Not present |
Phenytoin targets voltage-gated sodium channel and inhibits the positive feedback loop that results in neuronal propagation of high frequency action potential. In this way, seizures are prevented.
SAR of hydantoins can be described as follows:
Phenytoin can be synthesized by rearrangement on the reaction of urea and benzil.[1]
Phenytoin is used for:
Side Effects
Side effects of phenytoin are:
Headache
Q.1 What are the correct statements related with the physicochemical properties of Phenytoin drug?
I. Molecular weight = 252.27 gm/mol
II. It appears as pale yellow crystals
III. It is very soluble in cold water
IV. Piperidine ring is present in the structure
a) I
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. Phenytoin | A. 5,5-diphenylimidazolidine-2,4-dione |
ii. Butabarbital | B. (RS)-N’-(7-chloroquinolin-4-yl)-N,N-diethyl-pentane-1,4-diamine |
iii. Favipiravir | C. 5-butan-2-yl-5-ethyl-1,3-diazinane-2,4,6-trione |
iv. Chloraquine | D. 6-fluoro-3-hydroxypyrazine-2-carboxamide |
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 Steps for mechanism of action for drug phenytoin?
I. Neuronal propagation is inhibited
II. Inhibition of positive feedback loop of voltage-gated sodium channel
III. Seizures are prevented
IV. Meningitis is prevented
a) I – II – IV
b) I – II – III
c) II – I – III
d) II – I – IV
Q.4 Correct sequence for True/false for the classification of the drug can be?
a) TFTT
b) TTFF
c) FFTT
d) FTFT
Q.5 Type of ring present in the structure of Phenytoin is?
a) Imidazolidine
b) Piperazine
c) Piperidine
d) Pyridine
Q.6 Starting chemicals required for the synthesis of phenytoin are?
I. Urea
II. Phenol
III. Benzil
IV. Sodium amide
a) I , III
b) III , II
c) II , IV
d) III , II
Q.7 Side effect of drug Phenytoin are?
a) Slow heartbeats
b) Loss of coordination
c) Increased growth of hairs
d) All of the above
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1-a
2-c
3-c
4-d
5-a
6-a
7-d
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