Acefinac
Acefinac Uses, Dosage, Side Effects, Food Interaction and all others data.
Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs)
Acefinac 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. Acefinac 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]. Acefinac also targets the synthesis of glycosaminoglycan and mediates chrondroprotective effects .
| Trade Name | Acefinac |
| Generic | Aceclofenac |
| Aceclofenac Other Names | Aceclofenac, Acéclofénac, Aceclofenac betadex, Aceclofenaco, Aceclofenacum |
| Type | Tablet |
| 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 | Ortin Laboratories Ltd |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Acefinac 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.
Acefinac is also used to associated treatment for these conditions: Ankylosing Spondylitis (AS), Osteoarthritis (OA), Rheumatoid Arthritis
How Acefinac 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. Acefinac 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 . Acefinac 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
Acefinac 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.
Acefinac 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
Acefinac 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: Acefinac, like many NSAIDs may increase plasma concentrations of lithium and Digoxin.
Diuretics: Acefinac, like other NSAIDs, may interact the activity of diuretics.
Anticoagulants: Like other NSAIDs, Acefinac may enhance the activity of anticoagulant. Close monitoring of patients on combined anticoagulants and Acefinac 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
Acefinac 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. Acefinac 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
Acefinac 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. Acefinac should not be administered to patients previously sensitive to Acefinac 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 Acefinac
Acefinac contains Aceclofenac see full prescribing information from innovator Acefinac Monograph, Acefinac MSDS, Acefinac FDA label
FAQ
What is Acefinac used for?
Acefinac 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 Acefinac is a painkiller?
Anti-inflammatory painkillers like Acefinac are also called non-steroidal anti-inflammatory drugs (NSAIDs), or sometimes just 'anti-inflammatories'. Acefinac is prescribed for people with painful rheumatic conditions such as osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.
How safe is Acefinac?
Acefinac 100 mg orally twice daily, is a safe, effective, and convenient treatment for active AS.
Is Acefinac 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 Acefinac.
Who should not take Acefinac?
Acefinac is not recommended if you have asthma or a history of asthma in your family. Impaired function of the kidney- Acefinac 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 Acefinac used for teeth pain?
Acefinac has anti-inflammatory properties similar to those of diclofenac and yields good results in the control of dental pain.
Does Acefinac 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 Acefinac as it can cause excessive drowsiness and increase your risk of stomach problems.
Does Acefinac increase blood pressure?
Acefinac may oppose the blood pressure lowering effects of certain medicines to treat high blood pressure, including the following: ACE inhibitors such as captopril.
Is Acefinac a muscle relaxant?
Acefinac 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 Acefinac?
Acefinac 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 Acefinac in children.
Elderly: The pharmacokinetics of Acefinac 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 Acefinac needs to be modified in patients with mild renal impairment.
Hepatic insufficiency: The dose of Acefinac should be reduced in patients with hepatic impairment. An initial daily dose of 100 mg should be administered.
Acefinac SR tablet:
The recommended dose is 200 mg once daily.
What is the Side Effects of Acefinac?
Generally Acefinac 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 Acefinac safe during pregnancy?
There is no information on the use of Acefinac during pregnancy. Acefinac should not be administered during pregnancy, unless there are compelling reasons for doing so. The lowest effective dose should be administered.
Is Acefinac safe during breastfeeding?
There is no information on the secretion of Acefinac in breast milk. The use of Acefinac should therefore be avoided during lactation unless the potential benefits to the mother outweigh the possible risks to the children.
