ibuproxam

Action and Spectrum

Actions and spectrum: 

• Anti-Inflammatory Action: Ibuproxam, like other NSAIDs, inhibits COX, particularly COX-1 and COX-2 enzymes. By doing so, it interferes with the synthesis of prostaglandins, which are mediators of inflammation. This anti-inflammatory action helps reduce swelling, redness, and pain associated with arthritis. 
• Analgesic (Pain-Relieving) Action: Ibuproxam provides relief from pain by inhibiting prostaglandin synthesis. Prostaglandins sensitize nerve endings to pain, and by reducing their production, ibuproxam diminishes the perception of pain. It is used for the management of various types of pain, including musculoskeletal pain and pain following surgical procedures. 
• Antipyretic Action: Ibuproxam has antipyretic effects, meaning it can reduce fever. Fever is often associated with the release of prostaglandins in the hypothalamus, the part of the brain that regulates body temperature. By inhibiting prostaglandin synthesis, ibuproxam helps lower elevated body temperature. 
• Spectrum of Activity: The ibuproxam encompasses a range of conditions characterized by inflammation, pain, and fever. It is commonly used in the treatment of Osteoarthritis and rheumatoid arthritis, Musculoskeletal pain and injuries, Menstrual pain, Postoperative pain, and Fever associated with various conditions. 

Drug Interaction

Adverse Reaction

Frequency not defined 

hypersensitivity reactions 

GI bleeding 

headache

Black Box Warning

there is no specific black box warning associated with ibuproxam. 

Contraindication / Caution

Contraindication: 

• Asthma and Aspirin Sensitivity: NSAIDs, including ibuproxam, may exacerbate asthma or induce bronchospasm in individuals with a history of aspirin sensitivity or asthma associated with chronic rhinitis, nasal polyps, and other allergic reactions. 
• Severe Renal Impairment or Failure: NSAIDs, including ibuproxam, can impair renal function and are generally contraindicated in individuals with severe renal impairment or renal failure. They should be used with caution in those with pre-existing renal conditions. 
• Severe Hepatic Impairment: Individuals with severe liver impairment may experience difficulties in metabolizing NSAIDs. Ibuproxam is generally contraindicated in severe hepatic impairment. 
• Post-Coronary Artery Bypass Graft (CABG) Surgery: The use of NSAIDs, including ibuproxam, is contraindicated in the perioperative period of CABG surgery due to an increased risk of cardiovascular events. 

Caution: 

• Gastrointestinal Effects: Ibuproxam can cause gastrointestinal (GI) side effects, including ulceration, bleeding, and perforation of the stomach or intestines. Individuals with a history of GI disorders or those taking medications that increase the risk of GI bleeding should use ibuproxam with caution. 
• Renal Impairment: NSAIDs, including ibuproxam, can cause renal toxicity and impair renal function. Caution is advised in individuals with pre-existing renal impairment, and renal function should be monitored during therapy. 
• Hepatic Impairment: Caution is recommended in individuals with liver impairment. Liver function should be monitored, especially in those with pre-existing liver conditions. 
• Fluid Retention and Edema: NSAIDs may cause fluid retention and edema. Individuals with conditions such as heart failure or hypertension should use ibuproxam with caution, and monitoring for signs of fluid retention is important. 
• Hypertension: NSAIDs can potentially increase blood pressure. Individuals those at risk of developing hypertension should use ibuproxam with caution, and blood pressure should be monitored regularly. 

Comorbidities: 

• Cardiovascular Disease: Individuals with cardiovascular disease, including heart failure, coronary artery disease, or those at risk for cardiovascular events, may need careful monitoring when using ibuproxam.  
• Renal Impairment: NSAIDs, including ibuproxam, can cause renal impairment or worsen existing kidney conditions. Caution is advised in individuals with pre-existing renal impairment, and renal function should be monitored during therapy. 
• Liver Disease: Individuals with liver disease or impaired liver function should use ibuproxam cautiously, as NSAIDs can affect liver function. Monitoring of liver enzymes may be necessary. 
• Gastrointestinal Disorders: Ibuproxam is associated with an increased risk of gastrointestinal bleeding, ulceration, and perforation. Individuals with a history of peptic ulcers, GI bleeding, or inflammatory bowel disease should use ibuproxam with caution. 
• Asthma: NSAIDs, including ibuproxam, may exacerbate asthma symptoms in some individuals. Caution is used in patients with asthma, and they should be monitored for respiratory symptoms. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into human milk: 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: 

Ibuproxam is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits pharmacological properties typical of this drug class. Its mechanism of action involves the inhibition of the enzyme cyclooxygenase (COX), specifically COX-1 and COX-2. By inhibiting COX, ibuproxam interferes with the synthesis of prostaglandins, which are signalling molecules involved in inflammation, pain, and fever. The reduction in prostaglandin levels leads to the anti-inflammatory, analgesic (pain-relieving), and antipyretic (fever-reducing) effects of ibuproxam.

The drug gets absorbed after oral administration, and its effects are systemic. Ibuproxam is commonly used to manage conditions such as osteoarthritis, rheumatoid arthritis, musculoskeletal pain, and fever. However, like other NSAIDs, it is associated with potential risks, including gastrointestinal irritation, cardiovascular effects, and renal impairment. The use of ibuproxam should be guided by healthcare professionals, considering individual patient factors and potential contraindications.  

Pharmacodynamics: 

• Anti-Inflammatory Effect: Ibuproxam’s inhibition of COX results in decreased production of prostaglandins, which play a central role in the inflammatory response. By reducing prostaglandin levels, ibuproxam exerts anti-inflammatory effects, helping to alleviate swelling, redness, and other signs of inflammation. 
• Analgesic (Pain-Relieving) Effect: Prostaglandins sensitize nerve endings to pain. By inhibiting their synthesis, ibuproxam reduces pain perception. This analgesic effect makes ibuproxam effective in managing musculoskeletal pain and postoperative pain. 
• Antipyretic Effect: Prostaglandins also contribute to the regulation of body temperature. Ibuproxam’s antipyretic effect is achieved by lowering elevated body temperature, making it useful in the management of fever. 
• Platelet Aggregation: While ibuproxam is not as selective for COX-1 as some other NSAIDs, it can still affect platelet function. COX-1 inhibition may lead to a reduction in thromboxane synthesis, which plays a role in platelet aggregation. This effect is reversible, and platelet function returns to normal shortly after discontinuation of the drug. 
• Renal Effects: Prostaglandins also have a role in maintaining renal blood flow. Inhibition of COX by ibuproxam can lead to alterations in renal function, including sodium and water retention. This is why caution is warranted in individuals with pre-existing renal conditions. 

Pharmacokinetics: 

• Absorption: Ibuproxam is well-absorbed after oral administration. The absorption occurs primarily in the stomach and small intestine. The rate and extent can be influenced by factors such as food intake. 
• Distribution: Ibuproxam is distributed throughout the body via the bloodstream. It has a high plasma protein binding, to albumin. The distribution into tissues, including sites of inflammation, contributes to its therapeutic effects. 
• Metabolism: Ibuproxam undergoes metabolism in the liver. The primary metabolic pathway involves oxidation and hydroxylation. The metabolites formed are generally inactive. Cytochrome P450 enzymes, particularly CYP2C9, play a role in the metabolism of ibuproxam. 
• Excretion: The majority of the metabolites and a small portion of the unchanged drug are excreted in the urine. Renal excretion is an important route of elimination for ibuproxam. The elimination half-life of ibuproxam is in the range of several hours. The elimination half-life of ibuproxam is short, and it is eliminated from the body within a few hours. 

Adminstartion

Administration: 

• Oral Administration: Ibuproxam is commonly available in oral dosage forms, such as tablets or capsules. It is usually taken with a full glass of water. The tablets or capsules should be taken whole and not crushed or chewed unless otherwise directed by the healthcare provider. 
• Food Intake: Ibuproxam can be taken with or without food. However, it can be taken with food or milk may help minimize the risk of gastrointestinal irritation. If stomach upset occurs, taking ibuproxam with food or after meals may be recommended. 
• Frequency of Administration: Ibuproxam is typically taken every 6 to 8 hours as needed for pain relief or as directed by the healthcare provider. The frequency may vary based on the formulation and the specific condition being treated. 
• Duration of Treatment: Ibuproxam is often used for short-term relief of symptoms. The duration of treatment is determined by the healthcare provider based on the specific condition.

Patient Information Leaflet

Patient information leaflet 

Generic Name: ibuproxam 

Pronounced: (eye-byoo-PROX-am) 

Why do we use ibuproxam? 

Ibuproxam is a nonsteroidal anti-inflammatory drug (NSAID) that is commonly used for its anti-inflammatory, analgesic (pain-relieving), and antipyretic (fever-reducing) properties. Ibuproxam is used to alleviate pain associated with various conditions, including musculoskeletal pain, dental pain, menstrual cramps, and postoperative pain. It is prescribed to reduce inflammation in conditions such as osteoarthritis and rheumatoid arthritis. The anti-inflammatory properties of ibuproxam help alleviate swelling and stiffness associated with these conditions. Ibuproxam is effective in reducing fever, making it a common choice for managing febrile conditions such as infections and other illnesses. The drug is often used to manage conditions involving the musculoskeletal system, including sprains, strains, and sports injuries. Ibuproxam can be used to relieve headaches, including tension headaches and migraines.