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