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Mediflam 50mg

Mediflam 50mg

Category: Analgesics& Anti-inflammatory
Classification: Tablets
Product English Name: Mediflam 
Product Arabic Name:ميديفلام
Scientific Name English: Diclofenac Potassium
Scientific Name Arabic: ديكلوفيناك
Product Unit: 10Tablets
Product Strength:50mg

Description

Clinical Pharmacology

Pharmacodynamics & Mechanism of Action:

Diclofenac Potassium exhibits analgesic, anti-inflammatory, and antipyretic properties, belonging to a group of medicines called Nonsteroidal anti-inflammatory drugs characterized by inhibition of synthesis of prostaglandins ( the mediators of inflammation ) in peripheral tissues through inhibition of cyclooxygenase enzyme (Nonselective and including COX-1 and COX-2) and this inhibition is responsible for the variety of actions.

Additional information

Pharmacokinetics

Absorption:

Diclofenac is 100% absorbed after oral administration. However, due to first-pass metabolism, only about 50% of the absorbed dose is systemically available. In some fasting volunteers, measurable plasma levels observed within 10 minutes of dosing with diclofenac potassium tablets. Peak plasma levels are achieved approximately in 1 hour with a range of 0.33 to 2 hours.

Distribution:

The apparent volume of distribution (V/F) of diclofenac potassium is 1.3 L/kg. Diclofenac is more than 99% bound to human serum proteins, primarily to albumin. And this binding is constant over the conc. range (0.15 to 105 mcg/mL) achieved with recommended doses.

Diclofenac diffuses into and out of the synovial fluid. Diffusion into the joint occurs when plasma levels are higher than those in the synovial fluid, after which the process reverses and synovial fluid levels are higher than plasma levels.

Metabolism:

The five diclofenac hydroxy metabolites that identified in human plasma and urine, the formation of 4'-hydroxy-diclofenac, the major metabolite, is mediated by CYP2C9. Both Diclofenac & its oxidative metabolites undergo glucuronidation or sulfation followed by biliary excretion. Acyl glucuronidation mediated by UGT2B7 and oxidation mediated by CYP2C8 may also play a role in diclofenac metabolism. CYP3A4 is responsible for the formation of minor metabolites.

Excretion:

Diclofenac is eliminated through metabolism with approximately 65% of the dose is excreted in the urine and approximately 35% in the bile as conjugates of unchanged diclofenac plus metabolites.

Because renal elimination is not a significant pathway of elimination for unchanged diclofenac, dosing adjustment in patients with mild to moderate renal dysfunction is not necessary. The terminal half-life of unchanged diclofenac is approximately 2 hours.

Indications:

For treatment of primary dysmenorrhea.

For relief of mild to moderate pain.

For relief of the signs and symptoms of osteoarthritis.

For relief of the signs and symptoms of rheumatoid arthritis.
Dosage & Administration

For treatment of pain or primary dysmenorrhea the recommended dosage is 50 mg three times a day. With experience, physicians may find that in some patients an initial dose of 100 mg of diclofenac potassium tablets, followed by 50-mg doses, will provide better relief.

For the relief of osteoarthritis, the recommended dosage is 100 to 150 mg/day in divided doses, 50 mg twice a day, or three times a day.

For the relief of rheumatoid arthritis, the recommended dosage is 150 to 200 mg/day in divided doses, 50 mg three times a day or four times a day.
Administration Guides

Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals.

Different formulations of diclofenac are not necessarily bioequivalent even if the milligram strength is the same.

Do not increase the recommended dose by yourself if the goal of treatment not achieved.

Mediflam tablet: The tablets should be swallowed whole with liquid, preferably after meals, and must not be divided or chewed.
Contraindications

Diclofenac potassium is contraindicated in the following patients:

Known hypersensitivity (e.g., anaphylactic reactions and serious skin reactions) to diclofenac or any components of the drug product.

History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Severe, sometimes fatal, anaphylactic reactions to NSAIDs have been reported in such patients.

In the setting of coronary artery bypass graft (CABG) surgery.
Warnings and precautions

Cardiovascular:

NSAIDs may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk.

Diclofenac tablets are contraindicated for treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery.

Gastrointestinal:

NSAIDs cause an increased risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These events can occur at any time during use and without warning symptoms. Elderly patients are at greater risk.

Hepatotoxicity: Inform patients of warning signs and symptoms of hepatotoxicity. Discontinue if abnormal liver tests persist or worsen or if clinical signs and symptoms of liver disease develop.

Hypertension: Patients taking some antihypertensive medications may have impaired response to these therapies when taking NSAIDs. Monitor blood pressure.

Heart Failure and Edema: Avoid use of Diclofenac in patients with severe heart failure unless benefits are expected to outweigh risk of worsening heart failure.

Renal Toxicity: Avoid use of Diclofenac in patients with advanced renal disease unless benefits are expected to outweigh risk of worsening renal function.

– Anaphylactic Reactions: Seek emergency help if an anaphylactic reaction occurs.

– Exacerbation of Asthma Related to Aspirin Sensitivity: Diclofenac is contraindicated in patients with aspirin-sensitive asthma. Monitor patients with preexisting asthma (without aspirin sensitivity).

– Serious Skin Reactions: Discontinue Diclofenac at first appearance of skin rash or other signs of hypersensitivity.

– Drug Rash with Eosinophilia and Systemic Symptoms (DRESS): Discontinue and evaluate clinically.

– Fetal Toxicity: Limit use of NSAIDs, including Diclofenac tablets, between about 20 to 30 weeks in pregnancy due to the risk of oligohydramnios/fetal renal dysfunction. Avoid use of NSAIDs in women at about 30 weeks gestation and later in pregnancy due to the risks of oligohydramnios/fetal renal dysfunction and premature closure of the fetal ductus arteriosus.

– Hematologic Toxicity: Monitor hemoglobin or hematocrit in patients with any signs or symptoms of anemia.
Adverse Reactions

The most frequently reported adverse experiences occurring in approximately 1% to 10% of patients are:
Gastrointestinal experiences including: abdominal pain, constipation, diarrhea, dyspepsia, flatulence, gross bleeding/perforation, heartburn, nausea, GI ulcers (gastric/duodenal) and vomiting.

Others: Abnormal renal function, anemia, dizziness, edema, elevated liver enzymes, headaches, increased bleeding time, pruritus, rashes and tinnitus.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects.
Drug Interactions

A – Drugs That Interfere with Hemostasis:

The concomitant use of diclofenac and anticoagulants have an increased risk of serious bleeding compared to the use of either drug alone.

Concomitant use of drugs that interfere with serotonin reuptake and an NSAID may potentiate the risk of bleeding more than an NSAID alone.

Monitor patients with concomitant use of diclofenac potassium tablets with anticoagulants (e.g., warfarin), antiplatelet agents (e.g., aspirin), selective serotonin reuptake inhibitors (SSRIs), and serotonin norepinephrine reuptake inhibitors (SNRIs) for signs of bleeding the risk of bleeding more than an NSAID alone.

Concomitant use of diclofenac potassium tablets and analgesic doses of aspirin is not generally recommended because of the increased risk of bleeding.

B – Drugs affected when concomitant used with Diclofenac:

Digoxin: serum concentration and prolong the half-life of digoxin has been reported, monitor serum digoxin levels.

Lithium: NSAIDs have produced elevations in plasma lithium levels and reductions in renal lithium clearance, monitor patients for signs of lithium toxicity.

Methotrexate: may increase the risk for methotrexate toxicity (e.g., neutropenia, thrombocytopenia, renal dysfunction), monitor patients for methotrexate toxicity.

Cyclosporine: may increase cyclosporine's nephrotoxicity, monitor patients for signs of worsening renal function.

– ACEls, ARBs, and Beta-Blockers: NSAIDs may diminish thier antihypertensive effect. In patients who are elderly, volume-depleted (including those on diuretic therapy), or have renal impairment, co-administration of an NSAID with ACE inhibitors or ARBs may result in deterioration of renal function, including possible acute renal failure. These effects are usually reversible.

– Diuretics: NSAIDs reduced the natriuretic effect of loop diuretics (e.g., furosemide) and thiazide diuretics in some patients. This effect has been attributed to the NSAID inhibition of renal prostaglandin synthesis, observe patients for signs of worsening renal function, in addition to assuring diuretic efficacy including antihypertensive effects.

C – CYP2C9 Inhibitors or Inducers:

Co-administration of diclofenac with CYP2C9 inhibitors (e.g., voriconazole) may enhance the exposure and toxicity of diclofenac, whereas coadministration with CYP2C9 inducers (e.g, rifampin) may lead to compromised efficacy of diclofenac.
Use in Specific Population

Pregnancy category C: There are no adequate and well-controlled studies in pregnant women, but avoid use of NSAIDs in women at about 30 weeks gestation and later in pregnancy, because NSAIDs, including diclofenac potassium, can cause premature closure of the fetal ductus arteriosus.

Lactation: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from diclofenac, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use: The pharmacokinetics of diclofenac potassium has not been investigated in pediatric patients.

Geriatric Use: As with any NSAIDs, caution should be exercised in treating the elderly (65 years and older).

Renal Impairment: Avoid use of Diclofenac in patients with advanced renal disease unless benefits are expected to outweigh risk of worsening renal function.

Hepatic Impairment: Patients with hepatic disease may require reduced doses of diclofenac potassium.

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