AULIN ® Nimesulide

AULIN ® is a drug based on Nimesulide

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

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

Indications AULIN ® Nimesulide

AULIN ® is indicated in the short-term symptomatic treatment of acute inflammatory or gynecological pain, such as that present in the case of dysmenorrhoea.

Mechanism of action AULIN ® Nimesulide

Nimesulide, the active ingredient of AULIN ®, is a non-steroidal anti-inflammatory drug which, due to its particular chemical properties, and in particular the sulfoanilidic functional group, represents the forefather of the subclass of sulfonamides.

This non-acid active ingredient, taken by mouth, reaches the gastric environment where it is converted into the protonated form, it becomes more liposoluble, crossing cell membranes very easily and thus maintaining a bioavailability greater than 50% of the total dose taken.

Once reached the plasma peak after about 2 hours and bound to the plasma proteins, the nimesulide is distributed among the various organs and apparatuses where it exercises its therapeutic action

In fact, different studies have shown that this active principle can mainly exert an inhibiting effect on COX2, guaranteeing:

Inhibition of prostaglandin synthesis such as PGE2, with a pro-inflammatory, algogenic and pyrogenic action;
A sensitive antioxidant action, hindering the release of oxidizing agents by neutrophils and detoxifying the organism from the pathogenic action of the superoxide anion;
A protection of cartilaginous tissues and the extracellular matrix by inhibiting some enzymes with proteolytic activity and known as metalloproteases.

All the aforementioned molecular mechanisms of action allow nimesulide to act as an anti-inflammatory and analgesic, while preserving the protective action of some prostaglandins on the health of the gastric mucosa.

After its activity, after about 3-5 hours, it is metabolized to the hepatic level by the cytochromial system CYP2C9 and subsequently eliminated in the form of an inactive metabolite mainly through the urine.

Studies carried out and clinical efficacy

1. THE NIMESULIDE AS AN ANTICANCER AGENT

Eur J Med Chem. 2012 Jan; 47 (1): 432-44. Epub 2011 Nov 15.

Experimental study that evaluates the efficacy of COX2 inhibitors such as nimesulide in the treatment of neoplastic diseases. More precisely, this active ingredient has been shown to reduce the growth of breast cancer cells, resulting in a safe and tolerable pharmacokinetic point of view.

2. THE NIMESULIDE IN THE PROTECTION OF NEURONAL DAMAGE

J Neurotrauma. 2012 May 1; 29 (7): 1518-29. Epub 2012 Mar 29.

Very interesting experimental study that demonstrates how the simultaneous intake of nimesulide and magnesium sulfate can reduce neuronal damage induced by transient ischemic events.

3.SANGUINATE ASSOCIATED WITH THE USE OF NIMESULIDE

Case report reporting an important side effect associated with nimesulide treatment in a 50-year-old patient with ankylosing spondylitis. In this case the retroperitoneal hemorrhage risked seriously compromising renal function.

Method of use and dosage

AULIN ®

Nimesulide 100 mg tablets;

Granules for oral suspension of 50 or 100 mg of nimesulide;

Suppository for rectal use from 200 mg of nimesulide.

For the treatment of acute pain, in adults it is generally recommended to take a tablet or a sachet of 100 mg of nimesulide, twice a day, preferably after meals, or a suppository of 200 mg always twice a day .

The dosage could be reviewed by your doctor based on the severity of the disease, therapeutic efficacy and above all the simultaneous presence of diseases affecting the liver and kidney.

Warnings AULIN ® Nimesulide

AULIN ® therapy should be understood as short-term symptomatic therapy, useful for overcoming acute pain states.

For this reason, and given that the incidence of side effects is proportional to the duration of therapy, it would be appropriate to limit the intake of nimesulide as soon as possible.

Particular caution should be exercised by patients suffering from hepatic, renal or gastrointestinal pathologies, who should consult their physician before taking AULIN and agreeing to periodically monitor the efficacy and safety of the therapy.

Should any side effects appear, the patient should immediately contact his doctor, taking into consideration the possibility of immediately suspending the therapy in progress.

AULIN ® tablets contain lactose, therefore its use is not recommended in patients with lactose intolerance, lactase enzyme deficiency and glucose-galactose malabsorption syndrome.

AULIN ® granulate for oral suspension instead contains sucrose, making it so little indicated in patients suffering from hereditary syndromes of fructose intolerance, glucose / galactose malabsorption and sucrose-isomaltase deficiency.

PREGNANCY AND BREASTFEEDING

Given the ability of nimesulide to significantly reduce the production of prostaglandins, molecules useful for ensuring correct fetal and embryonic development, the use of AULIN ® is contraindicated throughout the pregnancy.

In fact, different studies show that the administration of NSAIDs in gestation can significantly increase the risk of malformations in the respiratory and cardiovascular system of the unborn child, increasing at the same time the risk of bleeding and complications at the time of delivery.

Interactions

Like other non-steroidal anti-inflammatory drugs, nimesulide could also interact with different active ingredients capable of varying both its pharmacokinetic and pharmacodynamic characteristics and its safety profile.

For this reason the patient should pay particular attention to the simultaneous assumption of:

Diuretics, ACE inhibitors, angiotensin II antagonists, methotrexate and ciclosporin, capable of increasing renal toxicity of nimesulide;
Valproic acid, fenofibrates, salicylates, tolbutamide able to compete with nimesulide for binding to the active site, thus reducing its therapeutic efficacy;
Active ingredients capable of altering gastric motility, thus causing significant variations in drug absorption;
Antibiotics and substrates of cytochromial enzymes, for alterations affecting pharmacokinetic and pharmacodynamic properties;
NSAIDs and opioids, given the increased analgesic effect of their interaction;
Anticoagulants, given the increased risk of bleeding associated with the simultaneous use of NSAIDs.

Contraindications AULIN ® Nimesulide

The use of AULIN ® 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 and severe heart failure.

Undesirable effects - Side effects

Despite the fact that nimesulide presents a direct inhibitory activity mainly towards COX2, reducing the risk of adverse reactions of the gastrointestinal tract, it is useful to remember how therapy with AULIN ® can determine the appearance of:

Dermatological reactions on an allergic basis such as skin rash, pruritus, urticaria and edema;
Haematological reactions such as anemia, neutrophilia, thrombocytopenia, granule cytopenia;
Central reactions such as drowsiness, headache, insomnia and dizziness;
Cardiovascular reactions such as tachycardia and hypertension;
Gastrointestinal reactions such as epigastric pain, nausea, vomiting, diarrhea and gastralgia;
Metabolic reactions such as hyperkalemia;
Respiratory reactions on an allergic basis such as asthma, dyspnea and bronchospasm;
Urogenital disorders such as dysuria, oliguria and isolated hematuria;
Changes in liver function.

In most cases, however, these side effects have affected patients predisposed or subjected to inadequate and prolonged treatment.