Phensuximide

IUPAC nomenclature

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

Classification

Phensuximide is a succinimide anticonvulsant.

Physiochemical Properties

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.

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