Generality
Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) able to exert a good analgesic, anti-inflammatory and antipyretic effect.
However, due to its liver toxicity, nimesulide is used as a second-line drug and - for the same reason - in some European countries it has been withdrawn from the market.
Nimesulide - Chemical Structure
In Italy it is still marketed, but its dispensation can only take place upon presentation of a non-repeatable medical prescription. It is available in pharmaceutical formulations suitable for oral, rectal and dermal administration.
Examples of medicinal specialties containing Nimesulide
- Aulin ®
- Aulin Gel ®
- Mesulid ®
- Nimesulide DOC ®
- Sulidamor ®
- Remov ®
Indications
For what it uses
The use of nimesulide is indicated for the treatment of acute pain of various origins and for the treatment of menstrual pain.
Warnings
Due to the hepatotoxicity that nimesulide can cause, if - during treatment with the drug - any symptom indicates a possible liver disorder (loss of appetite, nausea, vomiting, fatigue, dark urine, abdominal pain), the therapy must be stopped immediately and the doctor must be informed immediately.
Nimesulide can cause gastrointestinal ulceration, perforation and / or bleeding. Therefore, before taking the drug it is advisable to inform your doctor if you have already suffered from the above gastrointestinal disorders or if you suffer from ulcerative colitis or Crohn's disease. Patients suffering from cardiac and / or renal disorders should also inform their doctor before taking the drug.
Furthermore, nimesulide can increase the risk of heart attack or stroke, especially when taken at high doses and for long periods.
If nimesulide is to be administered to elderly patients, the doctor may decide to prescribe regular monitoring of cardiac, hepatic, renal and gastrointestinal function.
Nimesulide may adversely affect female fertility, therefore, it should not be taken by women who intend to become pregnant.
Nimesulide can cause side effects that can affect the ability to drive and / or operate machinery. Should these effects occur, these activities should be avoided.
Interactions
Because of the drug interactions that could occur, before starting the nimesulide treatment, you need to tell your doctor if you are already taking any of the following medications:
- Other NSAIDs ;
- Corticosteroids ;
- Anticoagulant drugs, such as, for example, warfarin;
- Antiplatelet agents, such as, for example, acetylsalicylic acid in small doses;
- Antihypertensives ;
- Diuretics ;
- Lithium salts, used for the treatment of bipolar disorder;
- SSRIs (selective serotonin reuptake inhibitors);
- Methotrexate, an anticancer;
- Cyclosporine, an immunosuppressive drug.
However, it is still a good idea to inform your doctor if you are taking - or have recently been - any type of medication, including prescription-free medicines and herbal and homeopathic products.
Side effects
Nimesulide can cause different types of side effects, although not all patients experience them. This depends on the different sensitivity of each individual towards the drug, therefore, it is not said that all the side effects occur with the same intensity in each person.
The following are the main adverse effects that may occur during treatment with nimesulide.
Gastrointestinal disorders
During nimesulide therapy, the following may occur:
- Nausea;
- He retched;
- Diarrhea or constipation;
- Flatulence;
- Gastritis;
- Gastrointestinal ulceration, perforation and / or bleeding;
- Dyspepsia.
Hepatobiliary disorders
Treatment with nimesulide can cause changes in liver function and very severe hepatitis accompanied by jaundice and blockage of the bile flow.
Kidney and urinary tract disorders
Nimesulide therapy can cause:
- Urinary retention;
- Pain during urination;
- hematuria;
- Kidney failure;
- Nephritis.
Skin and subcutaneous tissue disorders
During treatment with nimesulide, the following may occur:
- Skin eruptions;
- Increased sweating;
- Itch;
- Redness and / or inflammation of the skin;
- Erythema multiforme;
- Stevens-Johnson syndrome;
- Toxic epidermal necrolysis.
Blood and lymphatic system disorders
Nimesulide therapy may promote the onset of anemia, leukopenia and eosinophilia.
Cardiovascular disorders
Treatment with nimesulide can cause changes in blood pressure, hot flushes, and tachycardia and may increase the risk of myocardial infarction and stroke.
Psychiatric disorders
Nimesulide therapy can cause anxiety, nervousness and nightmares.
Allergic reactions
Nimesulide can trigger allergic reactions in sensitive individuals. These reactions can occur in the form of:
- Breathing difficulties;
- Asthma;
- Collapse;
- Reduced body temperature;
- Dizziness;
- Headache;
- Insomnia;
- Stomach pains;
- Urticaria;
- Angioedema.
Other side effects
Other side effects that may occur during treatment with nimesulide are:
- Edema;
- hyperkalemia;
- Blurred vision;
- Malaise;
- Fatigue.
Overdose
In case of excessive doses of nimesulide they could be manifested:
- Nausea;
- Stomach pain;
- Drowsiness;
- Gastric ulcer;
- Breathing difficulty.
If nimesulide overdose is suspected, contact your doctor immediately and go to the nearest hospital.
Action mechanism
Nimesulide - as a NSAID - exerts its anti-inflammatory and analgesic action by inhibiting the activity of cyclooxygenase (COX).
Cyclooxygenase is an enzyme of which three different isoforms are known: COX-1, COX-2 and COX-3.
COX-1 is a constitutive isoform, normally present in cells and involved in the mechanisms of cellular homeostasis.
COX-2, on the other hand, is an inducible isoform that is produced by inflammatory cells (inflammatory cytokines) activated.
The task of these enzymes is to convert arachidonic acid into prostaglandins, prostacyclines and thromboxanes.
In particular, prostaglandins - and, more precisely, PGG2 and PGH2 - are involved in inflammatory processes and mediate pain responses.
Nimesulide is able to inhibit COX-2 with a certain selectivity, thus hindering the synthesis of prostaglandins responsible for inflammation and pain.
Mode of Use - Posology
Nimesulide is available for:
- Oral administration in the form of tablets, effervescent tablets, soluble tablets, orosoluble tablets, capsules and granules for oral solution.
- Rectal administration in the form of suppositories.
- Cutaneous administration in the form of gel.
To avoid the occurrence of dangerous adverse effects, during treatment with the drug it is essential to scrupulously follow the indications provided by the doctor, both as regards the amount of nimesulide to be taken, and when it concerns the duration of the same treatment.
In the following, some indications will be given on the doses of nimesulide usually used in therapy.
Oral administration
When administered orally, the dose of nimesulide usually used is 100 mg twice a day, to be taken after meals.
Rectal administration
When administered rectally, the dose of nimesulide usually used is 200 mg twice a day.
Cutaneous administration
The nimesulide-based gel is used for the symptomatic treatment of osteoarticular pain of rheumatic or traumatic nature (osteoarthritis, tendinitis, bursitis, lumbago, sprains and sprains).
In this case, it is recommended to apply the gel 2-3 times a day directly on the affected area, massaging until completely absorbed.
Pregnancy and breastfeeding
Because of the harmful effects it can cause, the use of nimesulide is contraindicated in pregnant women and breast-feeding mothers.
Contraindications
The use of nimesulide is contraindicated in the following cases:
- In patients with known hypersensitivity to the same nimesulide;
- In patients who have experienced allergic reactions after taking other NSAIDs;
- In patients who suffer - or who have suffered in the past - from ulceration, perforation and / or gastrointestinal bleeding;
- In patients with bleeding and / or coagulation disorders;
- In patients who are already taking hepatotoxic drugs;
- In patients with liver failure;
- In patients who abuse drugs and / or alcohol;
- In patients suffering from severe renal and / or cardiac insufficiency;
- In the last trimester of pregnancy;
- During breastfeeding.
