aceclofenac/paracetamol

Action and Spectrum

Actions and Spectrum: 

Action: 

aceclofenac is a nonsteroidal anti-inflammatory drug (NSAID). It works generally by inhibiting the enzyme cyclooxygenase (COX), specifically COX-2, which is involved in synthesizing prostaglandins. Prostaglandins are chemicals in the body that mediate pain, inflammation, and fever.

By inhibiting COX-2, aceclofenac reduces the production of prostaglandins, decreasing pain and inflammation. The action of paracetamol is believed to work primarily in the central nervous system. It is thought to inhibit the synthesis of prostaglandins in the brain and also spinal cord, which are involved in pain and fever regulation. 

Spectrum: 

Pain Relief: aceclofenac relieves pain, including mild to moderate pain associated with osteoarthritis, rheumatoid arthritis, and musculoskeletal disorders. 

Anti-Inflammatory: It has anti-inflammatory properties, making it helpful in reducing inflammation and swelling in conditions like arthritis. 

Antipyretic: aceclofenac can also help lower fever. 

Pain Relief: paracetamol is commonly used for pain relief, especially for mild to moderate pain, such as headaches, toothaches, and musculoskeletal pain. 

Antipyretic: It is also an effective fever reducer and is often used to lower elevated body temperature associated with fever. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Nausea 

Vomiting 

Loss of appetite  

Stomach pain 

Heartburn 

Diarrhea 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Hypersensitivity or Allergy: Individuals with a known hypersensitivity or allergy to aceclofenac, paracetamol, or any other ingredients in the medication should avoid using it. 
• Severe Liver Disease: aceclofenac is metabolized by the liver, and paracetamol can also affect the liver. Therefore, it is generally not recommended for individuals with severe liver disease or impairment. 
• Severe Kidney Disease: If you have any severe kidney disease or kidney impairment, a healthcare professional should avoid or carefully monitor this combination of medications, as it can affect kidney function. 
• Active Peptic Ulcer Disease: aceclofenac is an NSAID, and NSAIDs can enhance the risk of gastrointestinal bleeding and exacerbate peptic ulcers. Therefore, this medication is contraindicated in individuals with active peptic ulcer disease. 
• History of Gastrointestinal Bleeding or Perforation: If you have a history of gastrointestinal bleeding or perforation associated with NSAID use, it is best to avoid aceclofenac/paracetamol. 
• Asthma and Nasal Polyps: NSAIDs, including aceclofenac, can trigger or exacerbate asthma symptoms and nasal polyps in some individuals. It is contraindicated in individuals with a history of these conditions related to NSAID use. 
• Pregnancy and Breastfeeding: The safety of aceclofenac/paracetamol during pregnancy and breastfeeding may vary depending on local guidelines and individual circumstances.  
• Children: This combination medication in children and infants may be contraindicated or require special consideration, as dosing and safety can differ by age.  
• Alcohol Abuse: Combining alcohol with aceclofenac/paracetamol can increase the risk of liver damage. Therefore, it is generally advised to avoid alcohol while taking this medication. 
• Certain Medical Conditions: People with certain medical conditions, such as heart disease, high blood pressure, blood disorders, or a history of stroke, may need special monitoring or dosage adjustments when taking this medication. 

Caution 

• Gastrointestinal Issues: NSAIDs like aceclofenac can increase the risk of gastrointestinal side effects, including stomach ulcers, bleeding, and perforation. Suppose you have a history of gastrointestinal problems, such as gastritis, ulcers, or gastrointestinal bleeding, or are at high risk. In that case, your healthcare provider may recommend alternative treatments or closely monitor your condition while using this medication. 
• Renal Function: aceclofenac can affect kidney function, and paracetamol may also have an impact. If you have reduced kidney function or a history of kidney disease, your healthcare provider may need to adjust the dose or choose alternative pain relief options. 
• Cardiovascular Conditions: NSAIDs, including aceclofenac, can increase the risk of heart-related issues like heart attack or stroke, mainly when used for an extended period. If you have a history of heart disease, hypertension (high blood pressure), or other cardiovascular conditions, discuss the use of this medication with your healthcare provider. 
• Asthma: NSAIDs, including aceclofenac, may worsen asthma symptoms in some individuals. If you have asthma or a history of bronchospasm or other respiratory conditions, inform your healthcare provider.  
• Fluid Retention and Edema: Some individuals may experience fluid retention or edema using NSAIDs like aceclofenac. This may be of concern if you have conditions such as heart failure or high blood pressure. Inform your healthcare provider if you notice swelling or sudden weight gain. 
• Blood Disorders: If you have a prior history of blood disorders or are taking anticoagulants (blood-thinning medications), using aceclofenac/paracetamol may require close monitoring due to the potential for enhanced bleeding risk. 
• Elderly Population: Elderly individuals are generally at a higher risk of experiencing side effects from medications, including NSAIDs. Caution should be exercised when using aceclofenac/paracetamol in older people, with careful monitoring for side effects, mainly gastrointestinal and renal function. 
• Alcohol Consumption: Combining alcohol with aceclofenac/paracetamol can increase the risk of liver damage.  
• Drug Interactions: aceclofenac/paracetamol may interact with other medications you are taking.

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned. 

Lactation:   

Excreted into human milk: Not known. 

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: 

aceclofenac/paracetamol is a combination medication with dual pharmacological actions. aceclofenac, a nonsteroidal anti-inflammatory drug (NSAID), exerts its effects by inhibiting the enzyme cyclooxygenase (COX-2), which diminishes the synthesis of prostaglandins responsible for pain and inflammation. This results in pain relief and anti-inflammatory effects, making it useful in conditions like arthritis.

paracetamol (acetaminophen) primarily works within the central nervous system, inhibiting prostaglandin synthesis, and influencing the hypothalamic heat-regulating center to lower fever and provide analgesia. These components offer a broad spectrum of action, providing pain relief, reducing inflammation, and lowering fever, often used in managing musculoskeletal pain, arthritis, and fever-associated conditions.  

Pharmacodynamics: 

Mechanism of action: aceclofenac/paracetamol is a combination drug that contains two active ingredients, aceclofenac and paracetamol (acetaminophen). Each of these components has its mechanism of action, and their combination provides a broader spectrum of pain relief and fever reduction. 

aceclofenac works primarily by inhibiting the cyclooxygenase (COX), particularly COX-2, which is responsible for converting arachidonic acid into prostaglandins. Prostaglandins are chemical messengers in the body that play a crucial role in inflammation, pain, and fever. By inhibiting COX-2, aceclofenac reduces the synthesis of prostaglandins, decreasing pain, inflammation, and fever. 

The action is believed to exert its effects mainly within the central nervous system (brain and spinal cord). paracetamol is thought to reduce the production of prostaglandins specifically in the brain, particularly in the hypothalamus, which regulates body temperature. paracetamol helps lower elevated body temperature (fever) and provides analgesic (pain-relieving) effects by reducing prostaglandin production in the brain.

It may also have a weak anti-inflammatory effect, but it is less pronounced than NSAIDs like aceclofenac. The combination of aceclofenac and paracetamol in a single medication allows for a dual mechanism of action, providing both anti-inflammatory and analgesic effects (through aceclofenac) and antipyretic effects (through paracetamol). 

Pharmacokinetics: 

Absorption 

aceclofenac is well absorbed from the GIT (gastrointestinal tract) after oral administration. It is usually taken orally in the form of tablets or capsules. The absorption is relatively rapid, with peak plasma concentrations reached within 1 to 3 hours after ingestion. paracetamol is also well absorbed from the gastrointestinal tract after oral administration.  

Distribution 

aceclofenac is highly protein-bound, primarily to albumin in the blood. It has a relatively small volume of the distribution, indicating that it remains mainly within the bloodstream. 

paracetamol has a relatively large volume of distribution, indicating that it is distributed throughout the body’s tissues. It is known to cross the blood-brain barrier to exert its analgesic and antipyretic effects on the central nervous system. 

Metabolism 

aceclofenac undergoes extensive metabolism in the liver. It is metabolized into its active metabolite, diclofenac, among other inactive metabolites. Diclofenac is responsible for the majority of the drug’s pharmacological effects. 

paracetamol undergoes metabolism primarily in the liver. The major metabolic pathway involves conjugation with sulfate and glucuronic acid, forming water-soluble metabolites.

The cytochrome P450 system metabolizes a smaller portion into a highly toxic metabolite, typically detoxified through glutathione conjugation. However, in cases of overdose, this detoxification pathway can become overwhelmed, leading to potential liver toxicity. 

Elimination and Excretion 

The metabolites of aceclofenac, including diclofenac, are primarily excreted through the urine, with a smaller portion excreted in the feces. The elimination half-life of aceclofenac is relatively short, typically around 4 to 4.3 hours. 

The majority of paracetamol and its metabolites are generally excreted through the urine. A small portion is excreted in the feces. The elimination half-life of paracetamol is relatively short, typically around 2 to 3 hours in adults. 

Adminstartion

Administration: 

aceclofenac/paracetamol combination medication is typically available as oral tablets or capsules. The administration of aceclofenac/paracetamol should be done according to your healthcare provider’s instructions, the product label, or the specific recommendations provided by the manufacturer.  

Dosage: The appropriate dosage of aceclofenac/paracetamol will depend on your age, weight, medical condition, and the specific formulation of the medication. Follow your healthcare provider’s prescribed dosage instructions carefully. 

Frequency: aceclofenac/paracetamol is usually taken orally with or without food. The dosing frequency may vary, but it is often taken one to two times daily. Follow the prescribed dosing schedule provided by your healthcare provider. 

Duration: Use aceclofenac/paracetamol for the shortest duration necessary to relieve your symptoms. It is not typically intended for long-term use unless specifically directed by your healthcare provider. 

Swallow Whole: Swallow the tablet or capsule whole with a glass of water.  

Avoid Alcohol: It is generally recommended to avoid alcohol consumption while taking aceclofenac/paracetamol, as alcohol can increase the risk of liver damage. 

Storage: Store the medication at the recommended temperature and away from moisture and direct sunlight. Follow the storage instructions provided on the medication packaging. 

Monitoring: During treatment with aceclofenac/paracetamol, your healthcare provider may recommend periodic check-ups and monitoring to assess its effectiveness and detect any potential side effects or adverse reactions. 

Patient Information Leaflet: Read the PIL which is provided with the medication, as it contains essential information about the drug, its potential side effects, and any specific precautions or warnings. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: aceclofenac/paracetamol 

Why do we use aceclofenac/paracetamol? 

aceclofenac/paracetamol is a combination medication that contains two active ingredients: aceclofenac and paracetamol (also known as acetaminophen in some regions). This combination is typically prescribed for its analgesic (pain-relieving), anti-inflammatory, and antipyretic (fever-reducing) properties.  

Pain Relief: This combination medication is used to alleviate pain, exceptionally mild to moderate pain associated with various conditions, including but not limited to: 

• Musculoskeletal pain, like back pain, neck pain, and joint pain. 
• Dental pain: For pain relief after dental procedures or due to dental conditions. 
• Menstrual pain: To alleviate the discomfort associated with menstrual cramps. 

Inflammatory Conditions: aceclofenac, one of the active ingredients, is an NSAID (nonsteroidal anti-inflammatory drug). It helps reduce inflammation, making it effective in managing conditions like: 

Osteoarthritis: To alleviate pain and inflammation associated with this degenerative joint disease. 

Rheumatoid arthritis: To diminish joint pain and inflammation in patients with this autoimmune disorder. 

Ankylosing spondylitis: To relieve pain and stiffness in the spine and joints. 

Fever Reduction: paracetamol, the other active ingredient, has antipyretic properties and is used to reduce fever associated with various illnesses, such as the common cold, flu, or other infections. 

Postoperative Pain: aceclofenac/paracetamol may be prescribed after surgical procedures to manage postoperative pain and inflammation. 

Trauma and Injuries: It can manage pain and inflammation from injuries, such as strains, sprains, or minor trauma. 

Headaches and Migraines: To relieve pain, including tension-type headaches and migraines. 

Dental Procedures: Dentists may prescribe this combination of medications to manage pain and inflammation following dental surgeries or procedures. 

Other Painful Conditions: It may be used for other painful conditions as deemed appropriate by a healthcare provider.