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