Paracetamol is commonly used for its analgesic and antipyretic effects. It is used for the temporary relief from fever, minor aches and pain.
Indications:
●Lower back pain
●Fever
●Osteoarthiritis
●Dysmennorhea
Rationale of Combination:
Product Description:
The therapeutic effects of Nimesulide are the result of its complete mode of action which targets a number of key mediators of the inflammatory process such as: COX-2 mediated prostaglandins, free radicals, proteolytic enzymes and histamine. Whereas, Paracetamol is major ingredient in numerous cold and flu medications and many prescription analgesics. At therapeutic doses Paracetamol does not irritate the lining of the stomach nor affect blood coagulation, kidney function, or the fetal ductus arteriosus but lacks anti inflammatory action which is substituted with the addition of Nimesulide in combination. The fixed dose combination of Nimesulide and Paracetamol demonstrate a quicker onset and longer duration of antipyretic and analgesic action.
Pharmacology:
Nimesulide:
Nimesulide is rapidly absorbed following oral administration. Food, gender and advanced age have negligible effects on Nimesulide pharmacokinetics. The protein binding of Nimesulide is >97.5%. Nimesulide posses a shorter half life (1.8-4.7) and is hepatically metabolized. 50% of the drug is renally eliminated.
Paracetamol:
Paracetamol is a widely used analgesic and antipyretic agent. Paracetamol is well absorbed in gastro intestinal tract. Oral bioavailability is dose dependant since the half life of Paracetamol is 1-3hrs. Paracetamol is distributed throughout the body fluids in a homogeneous way. Paracetamol given at therapeutic doses binds to plasma proteins at less than 20%Metabolites are excreted through the kidneys in the urine.
Adverse Effects:
Paracetamol causes nausea, allergic reactions, skin rashes, acute renal tubular necrosis. Nimesulide induces certain side effects which include diarrhea, vomiting, skin rash, heart burn, headache and itching whereas it has been clinically characterized with hepatic-toxicity.
Contraindications:
Patients suffering from certain conditions, such as liver disease, bleeding disorders, and kidney disease and pregnant women should not take this medication.
Drug Interactions:
Nimesulide had no significant effect on fasting blood and glucose tolerance in patients treated with antidiabetic agents. Nimesulide may cause enzymatic induction of Theophylline when administered concomitantly with it. Nimesulide does not appear to interact with Warfarin, in clinical practice, although interaction with oral anticoagulants or other highly protein bound drugs cannot be ruled out. Paracetamol reduces the absorption of cholestyramine within 1 hour of administration whereas it accelerates the absorption with metoclopramide.
Potentially Fatal:
Nimesulide is banned for its usage in children below 12 years since it induces liver toxicity.