Action and Spectrum

Actions and Spectrum: 

It has a unique mechanism of action that involves the simultaneous release of both aspirin and paracetamol when metabolized in the body. The exact mechanism of action of benorilate is not fully understood, but its active metabolites, aspirin and paracetamol, exert their effects through different pathways: 

aspirin (acetylsalicylic acid): 

• aspirin is a classic NSAID that inhibits the action of cyclooxygenase (COX) enzymes. COX enzymes synthesize prostaglandins, inflammatory mediators promoting pain, fever, and inflammation. 
• By inhibiting COX enzymes, aspirin reduces the production of prostaglandins, leading to anti-inflammatory, analgesic (pain-relieving), and antipyretic (fever-reducing) effects. 
• aspirin is also known for its antiplatelet effects, meaning it can reduce blood clot formation, which is why it is commonly used for preventing cardiovascular events. 

paracetamol (acetaminophen): 

• paracetamol is an analgesic and antipyretic agent, like aspirin, but it does not possess significant anti-inflammatory properties like traditional NSAIDs. 
• The exact mechanism of paracetamol’s action is not fully understood, but it is believed to involve the inhibition of COX enzymes, particularly COX-2, in the central nervous system (CNS). This action reduces pain perception and fever response in the brain. 

Spectrum of Activity: 

benorilate’s spectrum of activity is like that of aspirin and paracetamol. 

• It relieves mild to moderate pain, such as headaches, muscle aches, and joint pain. 
• It can reduce fever caused by various conditions. 
• It has some anti-inflammatory effects but is less potent than other traditional NSAIDs. 

Drug Interaction

Adverse Reaction

Frequency not defined 

GI disturbances 

Hypersensitivity reactions 

Tinnitus 

Heartburn 

Drowsiness 

Dizziness 

Deafness 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Aspirin Sensitivity: benorilate contains aspirin (acetylsalicylic acid), so individuals with known hypersensitivity or allergy to aspirin should not use this medication. Aspirin sensitivity can lead to allergic reactions ranging from mild to severe, including symptoms like hives, difficulty breathing, and anaphylaxis. 
• History of Severe Allergic Reactions: Individuals who have experienced severe allergic reactions (anaphylaxis) to any NSAID, including aspirin or other salicylates, should not use benorilate. 
• Bleeding Disorders: benorilate, like aspirin, has antiplatelet effects that can increase the risk of bleeding. It should be avoided in individuals with bleeding disorders or those taking anticoagulant medications. 
• Peptic Ulcer Disease: aspirin can irritate the stomach lining and increase the risk of peptic ulcer disease. benorilate should be avoided in individuals with active peptic ulcers or a history of gastrointestinal bleeding. 
• Severe Liver or Kidney Impairment: The use of benorilate may be contraindicated in individuals with severe liver or kidney impairment due to potential toxicity and reduced drug clearance. 

Pregnancy / Lactation

Pregnancy consideration: benorilate is not recommended during pregnancy, especially in the last trimester, as it can affect the baby’s circulation and cause other complications. 

Lactation: It should also be avoided during breastfeeding because aspirin and its metabolites can pass into breast milk. 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

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 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: 

• The combination of aspirin and paracetamol in benorilate allows for a broader spectrum of pain relief, as it targets multiple pathways involved in pain and inflammation. 
• The aspirin component provides anti-inflammatory effects, making it practical for conditions where inflammation is prominent, such as arthritis or joint pain. 
• The paracetamol component adds to the analgesic effects, making benorilate suitable for various mild to moderate pain types, including headaches, muscle aches, and dental pain. 

Pharmacodynamics:  

Combining aspirin and paracetamol in benorilate provides a synergistic effect, resulting in a broader spectrum of pain relief than either component alone. 

The anti-inflammatory effects of aspirin complement the analgesic effects of paracetamol, making benorilate effective for conditions with both pain and inflammation, such as arthritis. 

Pharmacokinetics: 

Absorption 

benorilate is administered orally as a tablet or capsule. The absorption of benorilate occurs in the gastrointestinal tract after oral administration. aspirin and paracetamol, the active components of benorilate, are readily absorbed through the intestinal lining and enter the bloodstream. 

Distribution 

Once absorbed into the bloodstream, aspirin, and paracetamol are distributed throughout the body. Both aspirin and paracetamol have relatively high-water solubility, allowing them to distribute into various tissues and organs. 

Metabolism 

In the body, benorilate undergoes metabolic processes that release its active components, aspirin, and paracetamol. aspirin is hydrolyzed to salicylic acid, its active form. Salicylic acid is metabolized in the liver via conjugation to form various metabolites, mainly salicyluric acid and salicyl phenolic glucuronide. paracetamol is metabolized in the liver by conjugation with glucuronic acid and sulfate to form inactive metabolites, which are then excreted in the urine. 

Elimination and Excretion 

The elimination of benorilate and its metabolites occurs mainly via the renal (urinary) route. The metabolites of aspirin (salicyluric acid and salicyl phenolic glucuronide) are eliminated primarily in the urine. The metabolites of paracetamol (glucuronide and sulfate conjugates) are also excreted in the urine. 

Adminstartion

Administration: 

Oral administration 

Take benorilate with food or immediately after meals. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: benorilate 

Why do we use benorilate? 

benorilate is a medication that combines aspirin (acetylsalicylic acid) and paracetamol (acetaminophen). It was primarily used for its analgesic and anti-inflammatory properties. Here are some of the common uses of Benorilate: 

• Pain relief: benorilate alleviates mild to moderate pain, such as headaches, toothaches, menstrual pain, and musculoskeletal pain. 
• Fever reduction: The paracetamol of benorilate helps reduce fever in individuals with febrile conditions. 
• Inflammation: benorilate’s aspirin component helps reduce inflammation in arthritis and other inflammatory disorders. 
• Rheumatic conditions: benorilate may be prescribed to manage symptoms associated with rheumatoid arthritis and osteoarthritis due to its anti-inflammatory effects. 
• General analgesic: It can be a general pain reliever for acute or chronic painful conditions.