Aceclofenac

Aceclofenac is a Cyclooxygenase enzyme inhibitor / non-steroidal anti-inflammatory drugs (NSAIDs) belonging to Analgesic, antipyretic, and anti-inflammatory agent class.

Aceclofenac is indicated for the relief of pain and inflammation in osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis.

Aceclofenac is rapidly and completely absorbed from the gastrointestinal tract and circulates mainly as unchanged drug following oral administration. Peak plasma concentration is reached around 1.25 to 3 hours. The volume of distribution is approximately 25 L. It is reported to be highly protein-bound (>99%). 4'-hydroxyaceclofenac is the main metabolite detected in plasma. However other minor metabolites include diclofenac, 5-hydroxyaceclofenac, 5-hydroxydiclofenac, and 4'-hydroxydiclofenac. It is probable that the metabolism of aceclofenac is mediated by CYP2C9. The main route of elimination of acelclofenac is via the urine where the elimination accounts for 70-80% of clearance of the drug. Approximately two thirds of the administered dose is excreted via the urine, mainly as glucuronidated and hydroxylated forms of aceclofenac and About 20% of the dose is excreted into feces.

Aceclofenac shows common side effects like Stomach pain, Diarrhea, Nausea and vomiting, Skin rash, Indigestion, Heartburn, Dizziness, Drowsiness, Visual disturbances.

Aceclofenac is available in the form of Oral tablet and soft gel.

Aceclofenac is available in India, US, Canada, Japan, Singapore, Australia, Russia, China, and Malaysia.

Aceclofenac is an Analgesic, antipyretic, and anti-inflammatory agent belonging to the class Cyclooxygenase enzyme inhibitor / non-steroidal anti-inflammatory drug (NSAIDs).

Aceclofenac potently inhibits the cyclo-oxygenase enzyme (COX) that is involved in the synthesis of prostaglandins, which are inflammatory mediators that cause pain, swelling, inflammation, and fever.

Aceclofenac may remain in your body for approximately 24 hours.

Peak plasma concentration is reached around 1.25 to 3 hours.

Aceclofenac is available in the form of Oral tablet and soft gel.

Aceclofenac tablet is usually taken orally twice daily.

Aceclofenac is a painkiller. It provides relief from pain, stiffness, and swelling due to various conditions related to your bone and joints. It is also used to provide relief from headaches, toothaches, backaches, menstrual pain, sprains, and strains.

Aceclofenac is a Cyclooxygenase enzyme inhibitor / non-steroidal anti-inflammatory drugs (NSAIDs) belonging to Analgesic, antipyretic, and anti-inflammatory agent class.

Aceclofenac works by preventing the release of a chemical substance that causes pain and swelling in your body.

Aceclofenac is approved for use in the following clinical indications

• Ankylosing spondylitis, Osteoarthritis, Rheumatoid arthritis

Aceclofenac is indicated for the relief of pain and inflammation in osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis.

• Ankylosing spondylitis, Osteoarthritis, Rheumatoid arthritis

Adult: As conventional tab or soft gel cap: 100 mg two times a day, in the morning and the evening. As sustained-release tablet: 200 mg once daily.

Aceclofenac is available in various strengths as 100mg and 200mg.

Aceclofenac is available in the form of Oral tablet and soft gel.

• Dosage Adjustment in Kidney Patient

Mild to moderate: As conventional tablet or soft gel: Use the lowest effective dose for the shortest possible duration. Severe: Contraindicated.

• Dosage Adjustment in Hepatic impairment Patient

Mild to moderate: As conventional tablet or soft gel: Initially, 100 mg daily. Severe: Contraindicated.

Aceclofenac is contraindicated in patients with

• Patients with allergy to these drugs or other analogues (diclofenac). Patients with asthma. Like NSAIDS, acetylsalicylic acid and other drugs which inhibit prostagladin-synthesis may precipitate attacks of asthma, acute rhinitis or urticaria.
• Patients with active peptic ulcer.

• Skin rash

Aceclofenac may cause skin allergies (rashes, hives (itchy and painful eruption), or other allergic) in some cases.

• Bleeding disorders

Use Aceclofenac with caution if you have blood-clotting problems as this medicine may prolong the blood clotting time and increase the risk of bleeding.

• Impaired liver function

Use Aceclofenac with caution if you have liver problems as this medicine breaks down in your liver. Hence, it may lead to the accumulation of the medicine and increase the risk of side effects. It may also further cause liver damage.

• Systemic lupus erythematosus

Systemic lupus erythematosus is a condition in which your own immune system attacks your body. This can affect the skin, joints, kidneys, lungs, brain, etc. The symptoms are skin rash, joint pain, and tiredness. Use Aceclofenac with caution if you have systemic lupus erythematosus as it may further worsen your condition.

Avoid the consumption of alcohol while taking Aceclofenac as it will increase the risk of stomach bleeding.

It is not known if Aceclofenac passes into breastmilk. Hence Aceclofenac is not recommended for use while breastfeeding.

Aceclofenac is not recommended for use during pregnancy, especially in the third trimester (last 3 months) as it may harm your foetus. All the risks and benefits should be considered before taking this medicine in the first 6 months of pregnancy.

Common

• CV thrombotic events, including MI and stroke; fluid retention and oedema, new-onset or exacerbation of hypertension, hematologic effects (e.g. decreased platelet adhesion and aggregation, prolonged bleeding time), Hyperkalemia, increased transaminases, renal effects (e.g. deteriorated renal function, precipitated renal failure), drowsiness, dizziness, blurred vision, photosensitivity; hypersensitivity reactions, including anaphylactic or anaphylactoid reactions.
  

There have been no drug interactions reported, but close monitoring of patients on combination with lithium and digoxin, oral antidiabetic agents, anticoagulants, diuretics, and other analgesics.

The common side effects of Aceclofenac include the following

• Common side effects

Stomach pain, Diarrhea, Nausea and vomiting, Skin rash, Indigestion, Heartburn, Dizziness, Drowsiness, Visual disturbances.

• Pregnancy

Pregnancy Category

Aceclofenac is not recommended for use during pregnancy, especially in the third trimester (last 3 months) as it may harm your foetus. All the risks and benefits should be considered before taking this medicine in the first 6 months of pregnancy.

• Nursing Mothers

It is not known if Aceclofenac passes into breastmilk. Hence Aceclofenac is not recommended for use while breastfeeding. If required, it should only be used with caution.

• Pediatric Use

Aceclofenac is not recommended in children under 18 years of age due to lack of safety and efficacy data.

• Symptoms: Headache, vomiting, nausea, epigastric pain, gastrointestinal irritation and bleeding, diarrhea, disorientation, excitation, dizziness, drowsiness, tinnitus, hypotension, fainting, convulsions, respiratory depression, coma, and renal failure or liver damage for significant doses.

• Management: Symptomatic and supportive treatment. Give activated charcoal or perform gastric lavage within 1 hour of ingestion. Administer IV diazepam for frequent or prolonged convulsions. Closely monitors renal and hepatic function.

• Pharmacodynamic

Aceclofenac is a NSAID that inhibits both isoforms of COX enzyme, a key enzyme involved in the inflammatory cascade. COX-1 enzyme is a constitutive enzyme involved in prostacyclin production and protective functions of gastric mucosa whereas COX-2 is an inducible enzyme involved in the production of inflammatory mediators in response to inflammatory stimuli. Aceclofenac displays more selectivity towards COX-2 (IC50 of 0.77uM) than COX-1 (IC50 of >100uM), which promotes its gastric tolerance compared to other NSAIDs. The primary metabolite, 4'-hydroxyaceclofenac, also minimally inhibits COX-2 with IC50 value of 36uM. Although the mode of action of aceclofenac is thought to mainly arise from the inhibition of synthesis of prostaglandins (PGE2), aceclofenac also inhibits the production of inflammatory cytokines, interleukins (IL-1β, IL-6), and tumor necrosis factors (TNF) 1,2. It is also reported that aceclofenac also affects the cell adhesion molecules from neutrophils. Aceclofenac also targets the synthesis of glycosaminoglycan and mediates chrondroprotective effects.

• Pharmacokinetics

Absorption

Aceclofenac is rapidly and completely absorbed from the gastrointestinal tract and circulates mainly as unchanged drug following oral administration. Peak plasma concentrations are reached around 1.25 to 3 hours post-ingestion, and the drug penetrates the synovial fluid where the concentration may reach up to 60% of that in the plasma.

Distribution

The volume of distribution is approximately 25 L. It is reported to be highly protein-bound (>99%)

Metabolism and Excretion

4'-hydroxyaceclofenac is the main metabolite detected in plasma. However other minor metabolites include diclofenac, 5-hydroxyaceclofenac, 5-hydroxydiclofenac, and 4'-hydroxydiclofenac. It is probable that the metabolism of aceclofenac is mediated by CYP2C9. The main route of elimination of acelclofenac is via the urine where the elimination accounts for 70-80% of clearance of the drug. Approximately two thirds of the administered dose is excreted via the urine, mainly as glucuronidated and hydroxylated forms of aceclofenac and About 20% of the dose is excreted into feces.

• https://www.drugs.com/international/aceclofenac.html
• https://www.rxlist.com/clanza-cr-drug.htm#warnings
• https://go.drugbank.com/drugs/DB06736