Pentaerythritol tetranitrate

IUPAC nomenclature

2,2-Bis[(nitrooxy)methyl]propane-1,3-diyl dinitrate

Classification

• Organic nitrate antianginal drug

Physiochemical Properties

Mechanism of Action

i. The drug releases NO after denitration reaction.

ii. .Activation of enzyme gunanylate cyclase

iii. Increase in concentration of cGMP within vascular smooth muscles

iv. Vasodilation occurs due to cGMP-dependent protein kinase.

Structure Activity Relationship

General structure activity of organic nitrate antianginal drugs be summarized as:

• The number of nitrate groups determines the potency of organic nitrate for guanylate cyclase activation.
• Increase in nitric group increases the potency.
• Increase in lipophillicity doesn’t have major effect over activation of drug.

Method of synthesis

2,2-bis(hydroxymethyl)-1,3-propandiol is reacted with nitric acid to give pentaerythritol tetranitrate.[1]

Medicinal Uses

Pentaerythritol tetranitrate is used for treatment and prevention of:

• Angina pectoris

Side Effects

Side effects of pentaerythritol tetranitrate are:

• Dizziness
• Headache
• Flushing
• Syncope
• Hypotension
• Tachycardia
• Methemoglobinemia
• Nausea
• Vomiting
• Weakness
• Restlessness
• Uncontrolled urination

MCQs

Q.1 “2,2-Bis[(nitrooxy)methyl]propane-1,3-diyl dinitrate” is the IUPAC nomenclature of which drug?

a) Pentaerythritol tetranitrate

b) Furosemide

c) Amyl Nitrate

d) Bleomycin

Q.2 Melting point of drug pentaerythritol tetranitrate is?

a) 140.5 ^oC

b) 256 ^oC

c) 100 ^oC

d) 342 ^oC

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

 a) i-C, ii-A, iii-D, iv-B

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

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

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

Q.4 Mechanism of action of the drug pentaerythritol tetranitrate includes?

I. The drug releases NO after denitration reaction.

II. ctivation of enzyme gunanylate cyclase

III. Increase in concentration of cGMP within vascular smooth muscles.

a) I, II, III

b) II, III

c) I, III

d) I, II

Q.5   Correct sequence for True and False for the given statements related with the SAR of organic nitrate antianginal drugs can be?

• The number of nitrate groups determines the potency of organic nitrate for guanylate cyclase activation.
• Increase in nitric group increases the potency.
• Increase in lipophillicity doesn’t have major effect over activation of drug.

a) TFF

b) FFT

c) TTT

d) FFF

Q.6 Number of chiral carbons present in the structure of pentaerythritol tetranitrate

a) 0

b) 1

c) 2

d) 3 

Q.7 The drug pentaerythritol tetranitrate is mainly used for?

a) Treatment of angina

b) Treatment of Asthma

c) Treatment of Alzheimer’s disease

d) Treatment of Parkinson disease

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ANSWERS

1-a

2-a

3-c

4-a

5-c

6-a

7-a

REFERENCES