Action and Spectrum

Actions and Spectrum:

diflunisal is a non-steroidal anti-inflammatory drug (NSAID) used to relieve pain, reduce inflammation, and lower fever. It works by inhibiting the production of certain chemicals in the body that cause inflammation and pain. diflunisal is typically used to treat conditions such as osteoarthritis, rheumatoid arthritis, and menstrual pain. It is available in tablet form and is usually taken twice a day with or without food.

diflunisal is a non-selective COX inhibitor, which means it blocks both COX-1 and COX-2 enzymes. COX-1 is responsible for the production of prostaglandins that play a role in protecting the stomach lining and maintaining normal blood flow to the kidneys. COX-2 is responsible for the production of prostaglandins that play a role in inflammation and pain.

By blocking both COX-1 and COX-2, diflunisal can help relieve pain and inflammation but also increase the risk of stomach bleeding and kidney problems. diflunisal is considered to be a second-line therapy for pain and inflammation management, and it is not as widely used as other NSAIDs such as ibuprofen and naproxen.

Drug Interaction

Adverse Reaction

Frequency Defined

1-10%

Rash

Body fluid retention

Abdominal pain

Diarrhea

Constipation

Flatulence

Nausea

Indigestion

Dizziness

Insomnia

Headache

>10%

Increased liver function test

Black Box Warning

Black Box Warning

diflunisal carries a Black Box Warning, which is the most serious type of warning issued by the US Food and Drug Administration (FDA), due to the potential for serious gastrointestinal (GI) bleeding.

Contraindication / Caution

Contraindication/Caution:

Contraindications:

Hypersensitivity to diflunisal or any of its components

Active gastrointestinal bleeding

History of peptic ulcer disease

Cautions:

Use with caution in patients with a history of gastrointestinal bleeding or peptic ulcer disease

Use with caution in patients with bleeding disorders or taking blood thinning medications

May cause drowsiness or dizziness, use caution when operating heavy machinery or performing tasks that require alertness

May increase the risk of gastrointestinal bleeding, monitor for signs of bleeding and report any unusual symptoms to a healthcare provider

May cause an allergic reaction in some individuals, monitor for signs of an allergic reaction and seek medical attention if necessary.

Pregnancy / Lactation

Pregnancy warnings:   

US FDA pregnancy category: C

Lactation:  

Excreted into human milk is known

Pregnancy Categories:        

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology: 

diflunisal is a non-steroidal anti-inflammatory drug (NSAID) that is used to reduce pain and inflammation. It works by inhibiting the production of prostaglandins, which are molecules that contribute to inflammation and pain.

Pharmacodynamics: 

diflunisal is thought to have a similar mechanism of action as other NSAIDs, such as aspirin and ibuprofen, but it is less likely to cause gastric irritation or bleeding. It is also less likely to cause kidney and liver damage compared to other NSAIDs.

Pharmacokinetics: 

Absorption

diflunisal is well absorbed after oral administration, with peak plasma concentrations reached within 2-4 hours.

Distribution 

It is widely distributed throughout the body, with a large volume of distribution of approximately 70-100 L. It is highly bound to plasma proteins (over 99%).

Metabolism 

diflunisal is metabolized in the liver by oxidation and conjugation. The primary metabolite is the glucuronide conjugate.

Eimination and Excretion 

diflunisal and its metabolites are primarily excreted in the urine, with less than 2% excreted in the feces. The elimination half-life of diflunisal is approximately 12 hours.

Adminstartion

Administration: 

orally administration:

diflunisal is typically administered orally, usually twice daily, with or without food. The dosage and duration of treatment will depend on the specific condition being treated and the patient’s response to the medication.

It is important to follow the dosage and administration instructions provided by a healthcare provider and to not exceed the recommended dosage. Patients should also inform their healthcare provider of any other medications they are currently taking as diflunisal may interact with certain drugs.

Patient Information Leaflet

Patient information leaflet

Generic Name: diflunisal

Why do we use diflunisal?

diflunisal is a non-steroidal anti-inflammatory drug (NSAID) that is used to reduce pain, inflammation, and fever. It is commonly used to treat conditions such as osteoarthritis, rheumatoid arthritis, and other types of inflammatory conditions. diflunisal is also used to relieve pain and discomfort associated with menstrual periods.

Additionally, it may be used to relieve pain from other types of muscle and joint aches, toothaches, and other types of pain. It works by blocking the production of certain chemicals in the body that cause inflammation and pain.