PHENSUXIMIDE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses

Phensuximide

IUPAC nomenclature

1-methyl-3-phenyl-pyrrolidine-2,5-dione

Classification

Phensuximide is a succinimide anticonvulsant.

 

Physiochemical Properties

S. NO. PHYSICAL AND CHEMICAL PROPERTIES
1 Molecular weight 189.21 g/mol
2 Physical appearance Present in solid form
3 Melting point 72°C
4 Solubility 7020 mg/L
5 Octanol/water partition coefficient 0.7
6 Presence of ring Pyrrolidine, phenyl
7 Number of chiral centers 1

 

 

Mechanism of Action

  • It inhibits neuronal systems that are important for generation of three per second rhythm.
  • It inhibits depolarization-induced accumulation of cyclic adenosine monophosphate and GMP in brain tissues.

Structure Activity Relationship

SAR of succinimides can be discussed as follows:

  • Phenyl substitution makes them active against electrically induced convulsion.
  • N-methylation decreases activity against electroshock seizures.
  • N-methylation also increases the activity against chemically induced convulsions.

 

Method of synthesis

Phensuximide can be synthesized by the reaction of phenylsuccinic acid or its anhydride with methylamine. [1]

 

Therapeutic Uses

Phensuximide is used for:

  • The treatment of epilepsy

 

Side Effects

Side effects of Phensuximide are: 

  • Dizziness
  • Drowsiness

 

MCQs 

Q.1 “1-methyl-3-phenyl-pyrrolidine-2,5-dione” is the IUPAC nomenclature of which drug?

a) Phensuximide

b) Halothane

c) Dutasteride

d) Fulvestrant

Q.2 Correct melting point of the drug Phensuximide is?

a) 72°C

b) 172°C

c) 272°C

d) 372°C

Q.3 Match the following with correct classifications of the drugs.

i. Phensuximide A. Inhalational anesthetics
ii. Oxazepam B. ß-blockers
iii. Halothane C. Sedative hypnotic
iv. Esmolol D. Anticonvulsant drug

a) i-A, ii-C, iii-D, iv-B

b) i-C, ii-A, iii-B, iv-D

c) i-D, ii-C, iii-A, iv-B

d) i-A, ii-D, iii-C, iv-B

Q.4 Mechanism of action of drug phensuximide includes?

I. Inhibition of neuronal systems that is important for generation of three per second rhythm.

II. Inhibition of depolarization-induced accumulation of cyclic adenosine monophosphate and GMP in brain tissues.

III. Inhibits releases of Acetylcholine from the presynaptic nerves.

IV. Antagonizes the muscarinic receptors.

a) I, IV

b) II, III

c) I, III, IV

d) I, II

Q.5   Correct sequence for True and False for the given statements related with the SAR of succinimide drugs?

  • Phenyl substitution makes them active against electrically induced convulsion.
  • N-methylation increases activity against electroshock seizures.
  • N-methylation also increases the activity against chemically induced convulsions.

a) FFT

b) TFT

c) TFF

d) FFF

Q.6 Which drug is formed on reaction of phenylsuccinic acid with methylamine?

a) Halothane

b) Oxazepam

c) Phensuximide

d) Piperacetazine

 Q.7 The drug Phensuximide is mainly used for?

a) Treatment of epilepsy

b) Treatment of pain due to gout

c) As an antiviral drug

d) All of the above

 

 

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ANSWERS

1-a

2-a

3-c

4-d

5-b

6-c

7-a

 

REFERENCES

[1] Vardanyan R, Hruby V. Synthesis of essential drugs. Elsevier; 2006 Mar 10.

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