Aceclofenaco
Aceclofenaco Uses, Dosage, Side Effects, Food Interaction and all others data.
Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs)
Aceclofenaco 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. Aceclofenaco 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) . It is also reported that aceclofenac also affects the cell adhesion molecules from neutrophils [A19763]. Aceclofenaco also targets the synthesis of glycosaminoglycan and mediates chrondroprotective effects .
| Trade Name | Aceclofenaco |
| Generic | Aceclofenac |
| Aceclofenac Other Names | Aceclofenac, Acéclofénac, Aceclofenac betadex, Aceclofenaco, Aceclofenacum |
| Type | |
| Formula | C16H13Cl2NO4 |
| Weight | Average: 354.18 Monoisotopic: 353.0221633 |
| Protein binding | It is reported to be highly protein-bound (>99%) . |
| Groups | Approved, Investigational |
| Therapeutic Class | Aceclofenac is a non-steroidal agent with antiinflammatory and analgesic properties. Its mode of action is largely based on inhibition of prostaglandin synthesis. Aceclofenac is a potent inhibitor of the enzyme cyclooxygenase, which is involved in the production of prostaglandins. It also stimulates cartilage matrix (glycosaminoglycans) synthesis. |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Aceclofenaco is used for the relief of pain and inflammation in both acute and chronic pain like osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, dental pain, post-traumatic pain, low back pain, gynaecological pain etc.
Aceclofenaco is also used to associated treatment for these conditions: Ankylosing Spondylitis (AS), Osteoarthritis (OA), Rheumatoid Arthritis
How Aceclofenaco works
Through COX-2 inhibition, aceclofenac downregulates the production of various inflammatory mediators including prostaglandin E2 (PGE2), IL-1β, and TNF from the arachidonic acid (AA) pathway. Inhibition of IL-6 is thought to be mediated by diclofenac converted from aceclofenac . Suppressed action of inflammatory cytokines decreases the production of reactive oxygen species. Aceclofenaco is shown to decreased production of nitrous oxide in human articular chondrocytes . In addition, aceclofenac interferes with neutrophil adhesion to endothelium by decreasing the expression of L-selectin (CD62L), which is a cell adhesion molecule expressed on lymphocytes . Aceclofenaco is proposed to stimulate the synthesis of glycosaminoglycan in human osteoarthritic cartilage which may be mediated through its inhibitory action on IL-1 production and activity . The chrondroprotective effects are generated by 4'-hydroxyaceclofenac which suppresses IL-1 mediated production of promatrix metalloproteinase-1 and metalloproteinase-3 and interferes with the release of proteoglycan from chrondrocytes .
Dosage
Aceclofenaco dosage
Adults: The maximum recommended dose is 200 mg daily, taken as two separate 100 mg doses, one tablet in the morning and one in the evening.
Children: There is no clinical data on the use of aceclofenac in children.
Elderly: The pharmacokinetics of aceclofenac are not altered in elderly patients, therefore it is not considered necessary to modify the dose and dose frequency.
Renal insufficiency: There is no evidence that the dosage of aceclofenac needs to be modified in patients with mild renal impairment.
Hepatic insufficiency: The dose of aceclofenac should be reduced in patients with hepatic impairment. An initial daily dose of 100 mg should be administered.
Aceclofenaco SR tablet:
The recommended dose is 200 mg once daily.
Side Effects
Generally aceclofenac is well tolerated. The majority of side effects observed have been reversible and of a minor nature and include gastrointestinal disorders (dyspepsia, abdominal pain, nausea and diarrhoea) and occasional occurance of dizziness. Dermatological side effects including pruritus and rash. Abnormal hepatic enzyme levels and raised serum creatinine have occasionally been reported.
Toxicity
Some common adverse effects include gastro-intestinal disorders (dyspepsia, abdominal pain, nausea), rash, ruber, urticaria, symptoms of enuresis, headache, dizziness, and drowsiness . Oral LD50 value in rats is 130 mg/kg .
Precaution
Aceclofenaco should be administered with caution to patients with symptoms indicative of gastrointestinal disorders, with a history of peptic ulceration, ulcerative colitis, Crohn\'s disease, hepatic porphyria, and coagulation disorders. Patients suffering from severe hepatic impairment must be monitored.
Interaction
Lithium and Digoxin: Aceclofenaco, like many NSAIDs may increase plasma concentrations of lithium and Digoxin.
Diuretics: Aceclofenaco, like other NSAIDs, may interact the activity of diuretics.
Anticoagulants: Like other NSAIDs, Aceclofenaco may enhance the activity of anticoagulant. Close monitoring of patients on combined anticoagulants and Aceclofenaco therapy should be undertaken.
Methotrexate: Caution should be exercised if NSAIDs and Methotrexate are administered within 24 hours of each other, since NSAIDs may increase Methotrexate plasma levels, resulting in increased toxicity.
Food Interaction
- Take with or without food.
Volume of Distribution
The volume of distribution is approximately 25 L .
Elimination Route
Aceclofenaco 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 into the synovial fluid where the concentration may reach up to 60% of that in the plasma . There is no accumulation in regular dosing, with similar maximum plasma concentration (Cmax) and time to reach peak plasma concentration (Tmax) after single and multiple doses .
Half Life
The mean plasma elimination half-life is approximately 4 hours .
Clearance
The mean clearance rate is approximately 5 L/h .
Elimination Route
The main route of elimination 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 . About 20% of the dose is excreted into feces .
Pregnancy & Breastfeeding use
Pregnancy: There is no information on the use of aceclofenac during pregnancy. Aceclofenaco should not be administered during pregnancy, unless there are compelling reasons for doing so. The lowest effective dose should be administered.
Lactation: There is no information on the secretion of aceclofenac in breast milk. The use of aceclofenac should therefore be avoided during lactation unless the potential benefits to the mother outweigh the possible risks to the children.
Contraindication
Aceclofenaco should not be administered to patients with active or suspected peptic ulcer or gastro-intestinal bleeding. It should not be given to patients with moderate to severe renal impairment. Close medical surveillance is also imperative in patients suffering from severe impairment of hepatic function. It should not be prescribed during pregnancy, unless there are compelling reasons for doing so. The lowest effective dosage should be used. Aceclofenaco should not be administered to patients previously sensitive to Aceclofenaco or in whom aspirin or NSAIDs precipitate attacks of asthma, acute rhinitis or urticaria or who are hypersensitive to these drugs.
Acute Overdose
There is no human data available on the consequences of aceclofenac overdosage. After overdosage, following therapeutic measures to be taken: absorption should be prevented as soon as possible by means of gastric lavage and treatment with activated charcoal. Supportive and symptomatic treatment should be given for complications.
Storage Condition
Keep at a cool and dry place, protected from light and moisture.
Innovators Monograph
You find simplified version here Aceclofenaco
Aceclofenaco contains Aceclofenac see full prescribing information from innovator Aceclofenaco Monograph, Aceclofenaco MSDS, Aceclofenaco FDA label
FAQ
What is Aceclofenaco used for?
Aceclofenaco is used for the relief of pain and inflammation in both acute and chronic pain like osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, dental pain, post-traumatic pain, low back pain, gynaecological pain etc.
Is Aceclofenaco is a painkiller?
Anti-inflammatory painkillers like Aceclofenaco are also called non-steroidal anti-inflammatory drugs (NSAIDs), or sometimes just 'anti-inflammatories'. Aceclofenaco is prescribed for people with painful rheumatic conditions such as osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.
How safe is Aceclofenaco?
Aceclofenaco 100 mg orally twice daily, is a safe, effective, and convenient treatment for active AS.
Is Aceclofenaco safe for kidneys?
Patients with mild to moderate renal impairment should be kept under surveillance, since the use of NSAIDs may result in deterioration of renal function. The lowest effective dose should be used and renal function monitored regularly. Effects on renal function are usually reversible on withdrawal of Aceclofenaco.
Who should not take Aceclofenaco?
Aceclofenaco is not recommended if you have asthma or a history of asthma in your family. Impaired function of the kidney- Aceclofenaco is not recommended if you have impaired kidney function. Impaired function of the liver- Use with caution with an initial dose of 100 mg once daily for mild liver failure.
Can Aceclofenaco used for teeth pain?
Aceclofenaco has anti-inflammatory properties similar to those of diclofenac and yields good results in the control of dental pain.
Does Aceclofenaco make me sleepy?
It may cause dizziness, drowsiness or visual disturbances. Use caution while driving or doing anything that requires concentration. Avoid consuming alcohol while taking Aceclofenaco as it can cause excessive drowsiness and increase your risk of stomach problems.
Does Aceclofenaco increase blood pressure?
Aceclofenaco may oppose the blood pressure lowering effects of certain medicines to treat high blood pressure, including the following: ACE inhibitors such as captopril.
Is Aceclofenaco a muscle relaxant?
Aceclofenaco is a non-steroidal anti-inflammatory drug (NSAID) which works by blocking the release of certain chemical messengers that cause pain and inflammation (redness and swelling). Thiocolchicoside is a muscle relaxant.
What is the Dosage of Aceclofenaco?
Aceclofenaco Dosage
Adults: The maximum recommended dose is 200 mg daily, taken as two separate 100 mg doses, one tablet in the morning and one in the evening.
Children: There is no clinical data on the use of Aceclofenaco in children.
Elderly: The pharmacokinetics of Aceclofenaco are not altered in elderly patients, therefore it is not considered necessary to modify the dose and dose frequency.
Renal insufficiency: There is no evidence that the dosage of Aceclofenaco needs to be modified in patients with mild renal impairment.
Hepatic insufficiency: The dose of Aceclofenaco should be reduced in patients with hepatic impairment. An initial daily dose of 100 mg should be administered.
Aceclofenaco SR tablet:
The recommended dose is 200 mg once daily.
What is the Side Effects of Aceclofenaco?
Generally Aceclofenaco is well tolerated. The majority of side effects observed have been reversible and of a minor nature and include gastrointestinal disorders (dyspepsia, abdominal pain, nausea and diarrhoea) and occasional occurance of dizziness. Dermatological side effects including pruritus and rash. Abnormal hepatic enzyme levels and raised serum creatinine have occasionally been reported.
Is Aceclofenaco safe during pregnancy?
There is no information on the use of Aceclofenaco during pregnancy. Aceclofenaco should not be administered during pregnancy, unless there are compelling reasons for doing so. The lowest effective dose should be administered.
Is Aceclofenaco safe during breastfeeding?
There is no information on the secretion of Aceclofenaco in breast milk. The use of Aceclofenaco should therefore be avoided during lactation unless the potential benefits to the mother outweigh the possible risks to the children.
