Sign Out
Alaxan FR contains the synergistic combination of ibuprofen and paracetamol in a capsule. The inflammatory activity of ibuprofen and paracetamol combination is greater compared to the individual ingredients. Because pain is usually accompanied by inflammation, pain relief is more evident when inflammation is controlled by ibuprofen. This capsule format allows complete dissolution of the drugs in at least 10 min, which leads to faster absorption. Faster absorption usually leads to earlier onset of pain relief.
Pharmacology: Paracetamol is an analgesic-antipyretic agent which acts centrally, specifically on the hypothalamus by elevating the pain threshold. It has a weak anti-inflammatory activity.
Ibuprofen is an analgesic/anti-inflammatory/antipyretic agent which acts mainly on the peripheral nerve endings inhibiting prostaglandin release in the injured tissue.
The unique value of ibuprofen-paracetamol combination in Alaxan FR is a 2-way synergism. Paracetamol potentiates the anti-inflammatory activity of ibuprofen and ibuprofen potentiates the analgesic effect of paracetamol through alleviation of inflammatory symptoms.
Pharmacokinetics: There are no significant changes in the pharmacokinetic properties (ie, volume of distribution, clearance rate) of ibuprofen and paracetamol when taken together.
Peak plasma concentration of ibuprofen and paracetamol in the ibuprofen-paracetamol fixed-dose combination occurs 45 min after oral administration and is about 23.3 mcg·hr/mL and 8.28 mcg·hr/mL, respectively.
Paracetamol is rapidly and completely absorbed after oral administration. Peak plasma concentrations occur between 15 min to 2 hrs after ingestion. The absolute oral bioavailability of paracetamol is about 80% and is independent of dose in the range of 5-20 mg/kg.
Paracetamol is not bound to plasma proteins to any extent. The concentrations of paracetamol in saliva are similar to those in plasma. Concentrations in whole blood are up to 20% higher and in breast milk about 20% lower than the plasma concentration. Paracetamol crosses the placenta.
Paracetamol is extensively metabolized in the liver and the total body clearance is about 5 mL/kg/min. The clearance of paracetamol is reduced and the half-life increased following a hepatotoxic overdose. 2-5% of a therapeutic dose of paracetamol is excreted unchanged in the urine. Its renal clearance is about 10 mL/min and is weakly dependent on the urine flow rate but not on pH.
Ibuprofen is rapidly and almost completely absorbed following oral administration. Peak serum levels are achieved between 1-2 hrs after dosing.
The absorption and elimination of ibuprofen are not affected by the dosage regimen. Peak serum levels are reduced and delayed when the drug is taken after food.
Ibuprofen is rapidly eliminated from the plasma with half-life of about 2 hrs.
Ibuprofen is about 99% protein-bound. The high plasma protein-binding of ibuprofen results in relatively low volume of distribution (0.1 L/kg).
Ibuprofen is excreted in the breast milk in very small amounts not sufficient to have any effect in the infant. It is not known whether the drug crosses the placenta.
Ibuprofen is extensively metabolized in the liver. 90% of the dose is excreted in the urine and the remainder presumably in the feces. Less than 10% of the dose is excreted unchanged. Excretion is essentially complete within 24 hrs.
