This product is a combination of Nimesulide, Paracetamol, cetirizine HCl, phenylephrine HCl & caffeine. Nimesulide and Paracetamol is an anti-inflammatory, analgesic. This combination is used for relief of allergic symptoms of the nose or throat due to upper respiratory tract allergies. Cetirizine HCI and Caffeine in Yanicold Tablets enhances the analgesic activity of Paracetamol.
Indications and Usage
- Relief of nasal and sinus congestion.
- Relief of allergic symptoms of the nose or throat due to upper respiratory tract allergies.
- Relief of sinus pain and headache.
- Adjunct with antibacterials in sinusitis, tonsillitis, and otitis media.
Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) with analgesic antipyretic properties. It selectively inhibits cyclooxygenase-2 (COX-2). It is indicated as second line treatment for acute pain, symptomatic treatment of painful osteoarthritis and primary dysmenorrhoea.
It is classified as a mild analgesic. It is commonly used for the relief of headaches and other minor aches and pains and is a major ingredient in numerous cold and flu remedies. In combination with opioid analgesics, paracetamol can also be used in the management of more severe pain such as post-surgical pain and providing palliative care in advanced cancer patients. Though paracetamol is used to treat inflammatory pain, it is not generally classified as NSAIDs because it exhibit only weak anti-inflammatory activity.
Cetirizine is a second-generation antihistamine used in the treatment of hay fever, allergies, Angioedema, and Urticaria. It is a major metabolite of hydroxyzine and a racemic selective H1 receptor antagonist.
It is a sympathomimetic vasoconstrictor that has been used as a nasal decongestant. Phenylephrine constricts the blood vessels in the nasal mucous membranes and allows the air passages to open up. It is relatively selective alpha-adrenoceptor agonist. The majority of the sympathomimetic action is due to direct stimulation of the adrenoceptors. At therapeutic doses, it does not cause significant stimulation of the central nervous system.
Caffeine is a central nervous system (CNS) stimulant. Caffeine enhances the analgesic activity of Paracetamol.
Nimesulide - after oral administration the peak plasma concentrations of 1.98-9.85 mg/L are achieved within 1 to 3 hrs. Nimesulide undergoes extensive metabolism and is eliminated through urine and feces.
Paracetamol is rapidly and completely absorbed from gastrointestinal tract. Peak plasma is achieved within 0.5 to 2 hrs. The drug is metabolized in the liver. 90% of the drug is excreted through urine.
Absorption: Oral administration, cetirizine HCl is rapidly absorbed, reaching Tmax in approximately 1 hour.
Distribution: Approximately 93% protein bound.
Metabolism: Cetirizine HCl undergoes limited first-pass metabolism. There is minimal metabolism via O-dealkylation resulting in a metabolite with negligible anti-histaminic activity.
Elimination: Cetirizine HCl is excreted in the urine (70%) primarily unchanged and in the feces (10%).Mean elimination half-life is approximately 8.3 hours.
Phenylephrine is absorbed quickly and completely. The biological half-life is 2-3 hrs. It is mainly excreted via the kidneys. The therapeutic plasma concentrations of Phenylephrine are described as 0.04-0.1µg/ml.
Absorption: When ingested, it has near perfect intestinal uptake of around 99-100% up to acute dosages of 10mg/kg bodyweight, the highest studied in humans.This absorption tends to occur almost completely within 45 minutes of ingestion.
Metabolism: caffeine can be metabolizes into dimethylxanthine derivatives (paraxanthine, theobromine, and theophylline) and further metabolized into monoxanthine derivatives and then finally a xanthine molecule. Other metabolic byproducts of caffeine include di and trimethylallanio, mono and dimethyluric acids, and various uracil derivatives.
Distribution: Caffeine is hydrophobic enough to tranverse most barriers in the body and is readily distributed to all organs. A steady state volume of distribution appears to occur at 500-800mL/kg with dosages below 250mg. Doses above 250mg start to increase this amount and habitual users of caffeine are associated with greater distribution.
• Drugs such as alcohol, tricyclic antidepressants barbiturates and other anticonvulsants which induce hepatic microsomal enzymes may increase the hepatotoxicity of paracetamol particularly after over dosage.
• The anti coagulant effect of warfarin may be increased when nepar is administered concomitantly coagulation tests should closely be monitored in such cases.
• Prolonged concutrrent use of paracetamol and a salicylate is not recommended due to increased risk of analgesic nepropathy.
• Nimesulide may be displaced from plasma binding sites by salicylates, fenofibrate, valproic acid and tolbutamide. Nimesulide may increase the plasma concentrations if salicylate methotrexate and frusemide by displacement from plasma proteins.
• Patient with known hypersensitivity to the combination or any of the ingredients of the combination.
• Contradicted in pregnancy and breast feeding
• epigastric pain
• skin rashes
Warning & Precautions
• The combination should be used with caution in patients with renal or hepatic impairment.