Melosolute

Uses

Melosolute is used for Osteoarthritis, Rheumatoid arthritis, Ankylosing spondylitis

Melosolute is also used to associated treatment for these conditions: Dental Pain, Neuropathic Pain, Osteoarthritis (OA), Pain, Inflammatory, Pauciarticular juvenile rheumatoid arthritis, Polyarticular juvenile rheumatoid arthritis, chronic or unspecified, Postoperative pain, Rheumatoid Arthritis

How Melosolute works

Melosolute inhibits prostaglandin synthetase (cylooxygenase 1 and 2) enzymes leading to a decreased synthesis of prostaglandins, which normally mediate painful inflammatory symptoms. As prostaglandins sensitize neuronal pain receptors, inhibition of their synthesis leads to analgesic and inflammatory effects. Melosolute preferentially inhibits COX-2, but also exerts some activity against COX-1, causing gastrointestinal irritation.

Dosage

Melosolute dosage

For Adults:

• Osteoarthritis: 7.5 mg/day. If necessary, in the absence of improvement, the dose may be increased to 15 mg/day.
• Rheumatoid arthritis: 15 mg/day. In elderly patients the recommended dose for long term treatment is 7.5 mg/day.
• Ankylosing spondylitis: 15 mg/day. In elderly patients the recommended dose is 7.5 mg/day.

Do not exceed the dose of 15 mg/day. The total daily amount should be taken as a single dose. Patients with increased risks for adverse reactions should start treatment with 7.5 mg/day. In dialysis patients with severe renal failure the dose should not exceed 7.5 mg/day

For Children: The pharmacokinetics of Melosolute in paediatric patients under 18 years of age have not been investigated.

Side Effects

Nausea, vomiting, abdominal pain, dyspepsia, constipation or diarrhoea may occur. Ulcers or gastrointestinal bleeding may rarely occur. Skin rash, or urticaria may occur in some individuals. Oedema of the lower limbs may occur during treatment. Onset of an asthma attack has been reported in certain individuals allergic to aspirin or to other NSAIDs. Headache, vertigo or drowsiness may occur.

Toxicity

The oral LD50 in rats is 98 mg/kg. Signs and symptoms of overdose with meloxicam may include shallow breathing, seizure, decreased urine output, gastrointestinal irritation, nausea, vomiting, gastrointestinal bleeding, and black tarry stools. In the case of an overdose, offer supportive treatment and attempt to remove gastrointestinal contents. Cholestyramine has been shown to enhance the elimination of meloxicam.

Precaution

Patient with known CV disease or risk factors for CV disease, fluid retention or heart failure, history of GI bleeding or ulceration. Hepatic and renal impairment. Elderly. Pregnancy and lactation.

Interaction

Other NSAIDs, including high doses of salicylates: Administration of several NSAIDs together may increase the risk of ulcers and of gastrointestinal bleeding, via a synergistic effect.

Oral anticoagulants, heparin and ticlopidine: Increased risk of bleeding via inhibition of platelet function and damage to the gastroduodenal mucosa. Careful monitoring of the effects of anticoagulants is thus essential if it proves impossible to avoid such combined prescription.

Lithium: NSAIDs increase blood lithium levels, which may then reach toxic values.

Methotrexate: NSAIDs may accentuate the haematologic toxicity of methotrexate.

Intrauterine contraceptive devices: NSAIDs appear to decrease the efficacy of intrauterine contraceptive devices.

Food Interaction

• Avoid alcohol. The risk of gastrointestinal bleeding may be increased.
• Take with or without food. The absorption is unaffected by food.

Melosolute Alcohol interaction

[Moderate] GENERALLY AVOID:

The concurrent use of aspirin or nonsteroidal anti-inflammatory drugs (NSAIDs) and ethanol may lead to gastrointestinal (GI) blood loss.

The mechanism may be due to a combined local effect as well as inhibition of prostaglandins leading to decreased integrity of the GI lining.

Patients should be counseled on this potential interaction and advised to refrain from alcohol consumption while taking aspirin or NSAIDs.

Melosolute Hypertension interaction

[Major] Fluid retention and edema have been reported in association with the use of nonsteroidal anti-inflammatory drugs (NSAIDs).

Therapy with NSAIDs should be administered cautiously in patients with preexisting fluid retention, hypertension, or a history of heart failure.

Blood pressure and cardiovascular status should be monitored closely during the initiation of NSAID treatment and throughout the course of therapy.

[Moderate] Nonsteroidal anti-inflammatory drugs (NSAIDs), including topicals, can lead to new onset of hypertension or worsening of preexisting hypertension, either of which can contribute to the increased incidence of cardiovascular events.

NSAIDs should be used with caution in patients with hypertension.

Blood pressure should be monitored closely during the initiation of NSAID therapy and throughout the course of therapy.

Melosolute Drug Interaction

Moderate: aspirin, duloxetine, omega-3 polyunsaturated fatty acids, escitalopram, metoprolol, sertralineUnknown: diphenhydramine, cyclobenzaprine, pregabalin, esomeprazole, acetaminophen / hydrocodone, montelukast, levothyroxine, acetaminophen, cyanocobalamin, ascorbic acid, ergocalciferol, cholecalciferol, alprazolam, cetirizine

Melosolute Disease Interaction

Major: asthma, fluid retention, GI toxicity, rash, renal toxicities, thrombosisModerate: anemia, heart failure, hepatotoxicity, hyperkalemia, hypertension, platelet aggregation inhibition

Volume of Distribution

The volume of distribution of meloxicam is 10-15L. Because of its high binding to albumin, it is likely to be distributed in highly perfused tissues, such as the liver and kidney. Melosolute concentrations in synovial fluid, measured after an oral dose, is estimated at 40% to 50% of the concentrations measured in the plasma. This drug is known to cross the placenta in humans.

Elimination Route

The absolute bioavailability oral capsules after a dose was 89% in one pharmacokinetic study. Cmax was reached 5–6 hours after administration of a single dose given after the first meal of the day. The Cmax doubled when the drug was administered in the fasting state. Despite this, meloxicam can be taken without regard to food, unlike many other NSAIDS.

Melosolute formulated for instillation with bupivacaine produced varied systemic measures following a single dose of varying strength. In patients undergoing bunionectomy, 1.8 mg of meloxicam produced a C_max of 26 ± 14 ng/mL, a median T_max of 18 h, and an AUC_∞ of 2079 ± 1631 ng*h/mL. For a 9 mg dose used in herniorrhaphy, the corresponding values were 225 ± 96 ng/mL, 54 h, and the AUC_∞ was not reported. Lastly, a 12 mg dose used in total knee arthroplasty produced values of 275 ± 134 ng/mL, 36 h, and 25,673 ± 17,666 ng*h/mL.

Half Life

The half-life of meloxicam is approximately 20 hours, which is considerably longer than most other NSAIDS. It can therefore be dosed without the need for slow-release formulations.

Melosolute applied together with bupivacaine for postsurgical analgesia had a median half-life of 33-42 hours, depending on dose and application site.

Clearance

After an oral dose, the total clearance of meloxicam is 0.42–0.48 L/h. The FDA label indicates a plasma clearance from 7 to 9 mL/min. No dose changes are required in mild to moderate renal or hepatic impairment. The use of meloxicam in patients with severe renal or hepatic impairment has not been studied. FDA prescribing information advises against it.

Elimination Route

Melosolute is mainly eliminated through metabolism. Its metabolites are cleared through renal and fecal elimination. Less than 10 About 1.6% of the parent drug is excreted in the feces.

Pregnancy & Breastfeeding use

Pregnancy: It is advisable to avoid the administration of Melosolute during pregnancy.

Lactation: It is unknown whether Melosolute passes into mother’s milk. Melosolute should not be given to nursing mothers.

Contraindication

Melosolute is contraindicated to patients hypersensitive to this drug. Melosolute should not be given to patients who have developed signs of asthma, nasal polyps, angioneurotic oedema or urticaria following the administration of aspirin or NSAIDs. Melosolute is contraindicated to patients with active peptic ulcer during the last six months or a history of recurrent peptic ulcer disease, severe hepatic failure, non-dialysed severe renal failure, gastrointestinal bleeding, cerebrovascular bleeding or other bleeding disorders.

Acute Overdose

Symptoms: Lethargy, drowsiness, nausea, vomiting, epigastric pain, GI bleeding; severe symptoms (e.g. HTN, hepatic dysfunction, resp depression, convulsions, CV collapse, cardiac arrest, coma, acute renal failure).

Management: Supportive and symptomatic treatment. Admin of activated charcoal 1-2 hr after ingestion.

Storage Condition

Store Melosolute tablet in a cool & dry place and away from light. Store Melosolute suppository below 25˚C protected from light and moisture.

Innovators Monograph

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