BREXIN ® Piroxicam

BREXIN ® is a drug based on Piroxicam Beta-Cyclodextrin

THERAPEUTIC GROUP: Non-steroidal anti-inflammatory and antirheumatic drugs

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications BREXIN ® Piroxicam

BREXIN ® is indicated for the symptomatic treatment of inflammatory pain associated with rheumatic diseases such as osteoarthritis, rheumatoid arthritis and ankylosing spondylitis, only after careful consideration of the benefit / risk ratio.

Mechanism of action BREXIN ® Piroxicam

Piroxicam, active ingredient of BREXIN ®, is the forefather of a series of non-steroidal anti-inflammatory drugs commonly referred to as Oxicam, characterized by the important therapeutic efficacy useful above all in the course of inflammatory diseases on a rheumatic basis.

By selectively inhibiting inducible Cycloxygenases (COX2), Piroxicam is able to reduce the production of prostaglandins with pro-inflammatory activity, thus causing a lower recall in the inflammatory cells, a reduction in the pain stimulus and a modest antipyretic effect.

The peculiarity of BREXIN ® is the association of the aforementioned active ingredient with Beta-Cyclodextrin, an oligosaccharide derived from starch that can give the compound a series of advantageous pharmacokinetic properties useful for significantly improving the bioavailability of Piroxicam.

More specifically, following the oral intake, the conjugated Piroxicam is rapidly absorbed from the gastro-enteric mucosa, thanks to the increased water solubility, reaching the maximum plasma peak very quickly and consequently guaranteeing activity 2-3 times greater than the non-peak form. conjugated.

These pharmacokinetic properties allowed the active ingredient to perform a significantly more effective therapeutic activity than that of other non-steroidal anti-inflammatory drugs while maintaining the elimination pathway unchanged.

Beta-Cyclodextrin, on the other hand, will finally be metabolized in the colon by the bacterial mylophores in glucose and maltose molecules.

Studies carried out and clinical efficacy

1. THE PIROXICAM IN POST-OPERATIVE PAIN CONTROL (caesarean section)

Acta Med Iran. 2010 May-Jun; 48 (3): 148-53.

Study demonstrating that the intramuscular intake of 20 mg of Piroxicam may be effective in controlling post-operative pain following cesarean delivery, reducing the need for opioids.

2. THE PIROXICAM IN THE TREATMENT OF ACUTE HEMICRAINE

J. Assoc Physicians India. 2011 Aug; 59: 494-7.

Interesting work that demonstrates the efficacy of a new route of administration of Piroxicam, the sublingual one, in the control of pain associated with migraine without aura, also being well tolerated and without clinically relevant side effects.

3. THE ROLE OF PIROXICAM B-CYCLODESTRIN IN ENDOSCOPIC SURGERY

Braz J. Med Biol Res. 2010 Aug; 43 (8): 806-11. Epub 2010 Jul 9.

Interesting Brazilian work that evaluates the effectiveness of Piroxicam Beta-Cyclodextrin in the control of pain associated with endoscopic surgery, when taken in the pre-operative phases. This treatment reduces the amount of opioids used, thus limiting the possible side effects.

Method of use and dosage

BREXIN ®

Piroxicam Beta-Cyclodextrin 191.2 mg tablets equal to 20 mg of Piroxicam;

Effervescent tablets of 191.2 mg of Piroxicam Beta-Cyclodextrin equivalent to 20 mg of Piroxicam;

Granules for oral suspension of 191.2 mg of Piroxicam Beta-Cyclodextrin equivalent to 20 mg of Piroxicam;

Suppositories of 191.2 mg of Piroxicam Beta-Cyclodextrin equivalent to 20 mg of Piroxicam;

Given the numerous side effects of the gastro-enteric mucosa associated with Piroxicam therapy, the prescription regimen for BREXIN ® should be formulated by a specialist in the treatment of rheumatic diseases, after taking into consideration the patient's history, his clinical picture and the cost / benefit ratio that would result from the use of the drug.

In order to minimize possible adverse reactions, it is recommended to take BREXIN ® at the minimum effective dose and for the shortest period possible.

Warnings BREXIN ® Piroxicam

Given the numerous side effects related to BREXIN ® therapy it would be advisable to take the drug under strict medical supervision.

In fact, medical supervision would be useful both in defining the effective dosage and in monitoring the efficacy and safety of the therapy implemented.

For this reason, in order to minimize the incidence and severity of the numerous side effects, it would be advisable to take BREXIN ® at the lowest possible dose and for the shortest possible time.

The use of Piroxicam should be done with particular care in patients suffering from liver, kidney, gastrointestinal and cardiovascular diseases, given the greater susceptibility of these to the side effects of the drug.

It would therefore be advisable to consult your doctor immediately following the onset of unwanted reactions, and possibly incline to suspend therapy in progress.

BREXIN ® granulate for oral suspension contains aspartame and sorbitol, making it therefore contraindicated in patients with phenylketonuria and hereditary problems of fructose intolerance.

BREXIN ® in tablets contains lactose, therefore it is not recommended for use in patients with galactose intolerance, lactase enzyme deficiency or glucose-galactose malabsorption syndrome.

PREGNANCY AND BREASTFEEDING

The use of BREXIN ® during pregnancy and in the subsequent period of breastfeeding is strictly contraindicated, given the importance of prostaglandins in the control of correct embryonic and fetal development.

Malformations affecting the cardiovascular, urinary and respiratory tract of the unborn child as well as unwanted abortions and major complications at the level of delivery are the main consequences related to the uncontrolled use of Piroxicam during the gestational period and especially in the last quarter.

Interactions

Even Piroxicam, like other non-steroidal anti-inflammatory drugs, is susceptible to interaction with other active ingredients, potentially responsible for variations in therapeutic activity and the safety profile.

For this reason it would be appropriate to pay particular attention to the simultaneous assumption of:

Alcohol, oral anticoagulants and selective serotonin reuptake inhibitors due to increased risk of bleeding;
Diuretics, ACE inhibitors, angiotensin II antagonists, methotrexate and ciclosporin, given the ability to increase the renal toxicity of Piroxicam;
Active ingredients capable of altering gastric motility, activated carbon and cimetidine, capable of varying the systemic absorption profile of Piroxicam;
Antibiotics and substrates of cytochromial enzymes, capable of altering the pharmacokinetic profile of Piroxicam, enhancing the potential side effects.
NSAIDs, opioids and corticosteroids given the increased analgesic effect of their interaction;
Lithium, due to the increased concentration of this drug with a significant increase in its toxicity.

Contraindications BREXIN ® Piroxicam

The use of BREXIN ® is contraindicated in case of hypersensitivity to the active ingredient or to one of its excipients, hepatic and renal insufficiency, gastric ulcers and gastrointestinal pathologies, severe heart failure and simultaneous use of anticoagulants or other non-steroidal anti-inflammatory drugs.

Undesirable effects - Side effects

Although the selective inhibition of Piroxicam should have limited the side effects of therapy with non-steroidal anti-inflammatory drugs, different clinical trials and careful post-marketing monitoring have shown that taking this active ingredient can determine quite often the appearance of:

Gastrointestinal reactions such as nausea, vomiting, diarrhea, flatulence, melena, hematemesis, bleeding, enteropathy, gastritis and peptic ulcers;
Fortunately rare metabolic reactions such as hyperkalemia, hypoglycemia and hyperglycemia;
Jaundice, hepatitis and increase in transaminases;
Haematological reactions such as hematocrit reduction, anemia, leukopenia, thrombocytopenia;
Side effects at central level with drowsiness, headache, dizziness, depression, nervousness and insomnia;
Hypertension, angina and associated cardiovascular diseases;
Dermatological hypersensitivity reactions such as eczema, hives, itching, rashes and in the most serious cases but fortunately very rare toxic epidermal necrolysis.

The aforementioned reactions, and in particular the most frequent ones affecting the gastrointestinal mucosa, appear to have incidence and severity proportional to the dose of Piroxicam taken and to the duration of therapy.