zaltoprofen

Action and Spectrum

Actions and Spectrum: 

zaltoprofen works by inhibiting the activity of cyclooxygenase (COX) enzymes, specifically COX-1 and COX-2. These enzymes play a crucial role in producing prostaglandins, which are inflammatory mediators that promote pain, fever, and inflammation. By inhibiting COX enzymes, zaltoprofen reduces the production of prostaglandins, decreasing pain, inflammation, and related symptoms. 

Unlike some other NSAIDs, zaltoprofen exhibits preferential inhibition of COX-2 over COX-1, which means it may have a reduced risk of causing gastrointestinal side effects, such as stomach ulcers and bleeding, which are commonly associated with traditional non-selective NSAIDs. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Nausea 

Dry mouth 

Increased platelet count 

Loss of appetite 

Vomiting 

Drowsiness 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity to NSAIDs: zaltoprofen should not be used in individuals with a known hypersensitivity or allergic reaction to zaltoprofen or other NSAIDs.  
• History of Asthma Attacks, Urticaria, or Allergic Rhinitis: Individuals with a history of asthma attacks, urticaria (hives), or allergic rhinitis (hay fever) triggered by NSAIDs should avoid zaltoprofen.  
• Active or History of Peptic Ulcer Disease: zaltoprofen can irritate the stomach lining and increase the risk of peptic ulcers or gastrointestinal bleeding.  
• Severe Heart Failure: NSAIDs, including zaltoprofen, may exacerbate heart failure or increase the risk of fluid retention in individuals with severe heart failure.  
• Third Trimester of Pregnancy: zaltoprofen is not recommended during the third trimester of pregnancy due to the potential risk of adverse effects on the fetal cardiovascular system and delayed labor. 

Caution: 

• Gastrointestinal Effects: Like other NSAIDs, zaltoprofen can irritate the stomach lining and increase the risk of gastrointestinal ulcers, bleeding, and perforation. 
• Cardiovascular Risks: NSAIDs, including zaltoprofen, may be associated with an increased risk of cardiovascular events such as heart attack or stroke.  
• Renal Function Impairment: zaltoprofen is primarily eliminated through the kidneys. Patients with impaired kidney function may experience reduced drug clearance, leading to increased drug levels.  
• Fluid Retention and Edema: NSAIDs can cause fluid retention and edema (swelling) in some individuals, particularly those with pre-existing heart or kidney problems.  
• Asthma and Aspirin Sensitivity: zaltoprofen should be used with caution in individuals with asthma, nasal polyps, or a history of aspirin sensitivity, as it may trigger bronchospasm or respiratory reactions. 
• Elderly Patients: Elderly patients may be more susceptible to the side effects of zaltoprofen, including gastrointestinal bleeding and impaired renal function. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

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: 

By inhibiting COX-1 and COX-2, zaltoprofen reduces the synthesis of prostaglandins, leading to decreased pain, inflammation, and fever associated with various conditions. 

• Preferential COX-2 Inhibition: zaltoprofen exhibits a degree of preferential COX-2 inhibition, which means it selectively inhibits COX-2 more than COX-1. This selectivity may contribute to a reduced risk of gastrointestinal side effects, such as stomach ulcers and bleeding, often associated with traditional non-selective NSAIDs. 
• Analgesic Effect: The reduction in prostaglandin synthesis by zaltoprofen helps alleviate pain by diminishing the sensitization of pain receptors and reducing inflammation at the site of injury or inflammation. 
• Anti-inflammatory effect: zaltoprofen’s inhibition of prostaglandin production helps to attenuate the inflammatory response, leading to a reduction in inflammation, swelling, and redness in affected tissues. 

Pharmacodynamics:  

zaltoprofen primarily exerts its pharmacological effects by inhibiting cyclooxygenase (COX) enzymes responsible for synthesizing prostaglandins. The key pharmacodynamic aspects of zaltoprofen: 

• Inhibition of COX Enzymes: zaltoprofen inhibits both COX-1 and COX-2 enzymes. COX-1 is constitutively expressed and involved in maintaining normal physiological functions, including protecting the stomach lining and promoting platelet aggregation. COX-2, on the other hand, is mainly induced during inflammation and plays a significant role in generating prostaglandins that mediate pain, inflammation, and fever. 
• Reduction of Prostaglandin Synthesis: By inhibiting COX enzymes, zaltoprofen reduces the production of prostaglandins, lipid mediators involved in various physiological processes, including inflammation, pain, and fever. Reduced prostaglandin synthesis reduces pain sensitivity, decreases inflammation, and lowers fever. 

Pharmacokinetics: 

Absorption 

zaltoprofen is well absorbed after oral administration. It reaches peak plasma concentrations within 1 to 2 hours after ingestion. zaltoprofen has a high plasma protein binding capacity, with approximately 99% of the drug bound to proteins in the bloodstream.  

Distribution 

zaltoprofen is widely distributed throughout the body, allowing it to exert its anti-inflammatory and analgesic effects in various tissues. 

Metabolism 

zaltoprofen undergoes hepatic metabolism primarily by glucuronidation to form inactive metabolites. The liver plays a crucial role in breaking down the drug to prepare it for bodily elimination. 

Elimination and Excretion 

The majority of zaltoprofen and its metabolites are excreted in the urine. A smaller proportion of the drug is eliminated in the feces. The elimination half-life of zaltoprofen is approximately 1.5 to 2 hours. 

Adminstartion

Administration: 

Oral administration 

zaltoprofen is usually taken with or after food to reduce the risk of gastrointestinal irritation. Taking the medication with food can also help improve absorption and reduce the likelihood of stomach upset 

Patient Information Leaflet

Patient information leaflet 

Generic Name: zaltoprofen 

Why do we use zaltoprofen? 

zaltoprofen is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic (pain-relieving) and anti-inflammatory properties. It is used to treat various conditions associated with pain and inflammation. Some common uses of  

• Musculoskeletal Disorders: zaltoprofen is commonly used to relieve pain and inflammation in osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and other musculoskeletal disorders. 
• Postoperative Pain: It may be used for short-term postoperative pain management after surgical procedures. 
• Trauma or Injuries: zaltoprofen can alleviate pain and inflammation from injuries or trauma. 
• Menstrual Pain: It may also be prescribed to relieve menstrual pain (dysmenorrhea). 
• Dental pain: zaltoprofen can reduce pain and inflammation following dental procedures or in cases of dental pain.