Anti-Cox II Tablets: Rapid Pain Relief for Osteoarthritis and Rheumatoid Arthritis

Composition:

Each tablet contains: Meloxicam 15mg.

Properties:

Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) that demonstrates anti-inflammatory, analgesic, and antipyretic effects in animal models. The mechanism of action of meloxicam, like other NSAIDs, may be associated with prostaglandin synthetase (cyclo-oxygenase) inhibition.

Absorption

The absolute bioavailability of meloxicam capsules was 89% following a single oral dose of 30 mg compared with 30 mg IV bolus injection. Dose-proportional pharmacokinetics were observed after single intravenous doses in the range of 5 mg to 60 mg. After multiple oral doses, the pharmacokinetics of meloxicam capsules were dose-proportional over the range of 7.5 mg to 15 mg. Mean Cmax was achieved within four to five hours after a 7.5 mg meloxicam tablet was taken under fasted conditions, indicating prolonged drug absorption.

Distribution

The mean volume of distribution (Vss) of meloxicam is approximately 10 L. Meloxicam is approximately 99.4% bound to human plasma proteins (primarily albumin) within the therapeutic dose range. The fraction of protein binding is independent of drug concentration, over the clinically relevant concentration range, but decreases to approximately 99% in patients with renal disease.

Metabolism

Meloxicam is almost completely metabolized to four pharmacologically inactive metabolites. The major metabolite, 5-carboxy meloxicam (60% of the dose), from P-450 mediated metabolism was formed by oxidation of an intermediate metabolite 5-hydroxymethyl meloxicam which is also excreted to a lesser extent (9% of the dose). In vitro studies indicate that cytochrome P-450 2C9 plays an important role in this metabolic pathway with a minor contribution of the CYP 3A4 isozyme. Peroxidase activity is probably responsible for the other two metabolites which account for 16% and 4% of the administered dose, respectively.

Excretion

Meloxicam excretion is predominantly in the form of metabolites, and occurs to equal extents in the urine and feces. Only traces of the unchanged parent compound are excreted in the urine (0.2%) and feces (1.6%). The mean elimination half-life (t½) ranges from 15 hours to 20 hours. The elimination half-life is constant across dose levels indicating linear metabolism within the therapeutic dose range. Plasma clearance ranges from 7 to 9 mL/min.

Hepatic Insufficiency

Following a single 15 mg dose of meloxicam, there was no marked difference in plasma concentrations in subjects with mild and moderate hepatic impairment compared to healthy volunteers.

Renal Insufficiency

Meloxicam pharmacokinetics have been investigated in subjects with different degrees of renal insufficiency. Total drug plasma concentrations decreased with the degree of renal impairment while free AUC values were similar. There is no need for dose adjustment in patients with mild to moderate renal failure (CrCL > 15 mL/min). Patients with severe renal insufficiency have not been adequately studied. The use of Anticox II in subjects with severe renal impairment is not recommended.

Indications:

• Relief of the signs and symptoms of osteoarthritis and rheumatoid arthritis.
• Relief of the signs and symptoms of polyarticular course Juvenile Rheumatoid Arthritis in children who can swallow capsules.

Dosage Administration:

• For the relief of the signs and symptoms of osteoarthritis, the recommended starting and maintenance oral dose of Anticox II is 7.5 mg once daily. Some patients may receive additional benefit by increasing the dose to 15 mg once daily. • For the relief of the signs and symptoms of rheumatoid arthritis, the recommended starting and maintenance oral dose of Anticox II is 7.5 mg once daily. Some patients may receive additional benefit by increasing the dose to 15 mg once daily. • The maximum recommended daily oral dose of Anticox II is 15 mg regardless of formulation.

Contraindications:

Anticox II is contraindicated in patients with known hypersensitivity to meloxicam. Anticox II should not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Anticox II is contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery.

Precautions and Warnings:

Cardiovascular Thrombotic Event:

To minimize the potential risk for an adverse CV event in patients treated with an NSAID, the lowest effective dose should be used for the shortest duration possible. NSAIDs, (meloxicam) tablets, can lead to the onset of new hypertension or worsening of pre-existing hypertension.

Hypertension:

NSAIDs, (meloxicam) can lead to the onset of new hypertension or worsening of pre-existing hypertension. Blood pressure (BP) should be monitored closely during the initiation of NSAID treatment and throughout the course of therapy.

Congestive Heart Failure and Edema:

Fluid retention and edema have been observed in some patients taking NSAIDs. AnticoxII should be used with caution in patients with fluid retention, hypertension, or heart failure.

Gastrointestinal (GI) Effects - Risk of GI Ulceration, Bleeding, and Perforation:

NSAIDs, including Anticox II, can cause serious gastrointestinal (GI) adverse events including inflammation, bleeding, ulceration, and perforation of the stomach, small intestine, or large intestine. To minimize the potential risk for an adverse GI event in patients treated with an NSAID, the lowest effective dose should be used for the shortest possible duration.

Renal Effects:

Long-term administration of NSAIDs, including (meloxicam), can result in renal papillary necrosis, renal insufficiency, acute renal failure, and other renal injury. Patients at the greatest risk of this reaction are those with impaired renal function, heart failure, liver dysfunction, those taking diuretics, ACE inhibitors, and angiotensin II receptor antagonists, and the elderly. Discontinuation of NSAID therapy is usually followed by recovery to the pretreatment state.

Advanced Renal Disease:

No information is available from controlled clinical studies regarding the use of AnticoxII in patients with advanced renal disease. Therefore, treatment with AnticoxII is not recommended in these patients with advanced renal disease.

Side Effects:

Gastrointestinal (GI) adverse events were the most frequently reported adverse events in all treatment groups across meloxicam trials. The following is a list of adverse drug reactions occurring in < 2% of patients.

• Body as a Whole: allergic reaction, anaphylactoid reactions including shock, face edema, fatigue, fever, hot flushes, malaise, syncope, weight decrease, weight increase
• Gastrointestinal: colitis, dry mouth, du

odenal ulcer, gastric ulcer, gastritis,

• Heart Rate and Rhythm: arrhythmia, palpitation, tachycardia
• Respiratory: asthma, bronchospasm, dyspnea

Packing:

Pack of 1, 2, or 3 strips each of 10 tablets (15 mg).

Notes:

Pregnancy & Lactation:

Pregnancy Category B In late pregnancy, as with other NSAIDs, Anticox II should be avoided because it may cause premature closure of the ductus arteriosus. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants, 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 safety and effectiveness of meloxicam in pediatric JRA patients from 2 to 17 years of age have been evaluated in three clinical trials.

Geriatric Use:

As with any NSAID, caution should be exercised in treating the elderly (65 years and older).

Anti-Cox II Tablets is a product manufactured by Adwia Pharmaceuticals Industries. Adwia is a leading Egyptian company founded in 1984 with a mission to bring the latest technologies and the highest available know-how to the market. They are committed to innovation and care and have a proven track record of success. For more information about Adwia Pharmaceuticals Industries, please visit their website or contact them directly.