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Combunox

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Combunox

Combunox

CLINICAL PHARMACOLOGY

Oxycodone HCl component

Oxycodone HCl is a semisynthetic opioid analgesic with multiple actions which involve the central nervous system and smooth muscle. The mechanism of action of oxycodone is not known but is thought to be related to its binding to opiate receptors in the central nervous system. In addition to analgesia, opioids may produce sedation and respiratory depression.

Ibuprofen component

Ibuprofen is a nonsteroidal anti-inflammatory agent that possesses analgesic and antipyretic activities. Its mode of action, similar to other NSAIDs, is not completely understood, but is thought to be related to its inhibition of cyclooxygenase activity and prostaglandin synthesis. Ibuprofen is a peripherally acting analgesic. Ibuprofen does not have any known effects on opiate receptors.

Pharmacokinetics

Absorption

Oxycodone is rapidly absorbed after single dose administration of Combunox (oxycodone hcl and ibuprofen) . Maximum concentrations (Cmax) of oxycodone, ranging from 9.8 ng/mL to 11.7 ng/mL, are obtained within 1.3 hr to 2.1 hr after administration of Combunox (oxycodone hcl and ibuprofen) . Repeated administration of Combunox (oxycodone hcl and ibuprofen) every 6 hours results in approximately 50-65% increase in Cmax. In the presence of food, the bioavailability of oxycodone is slightly (25%) increased.

Ibuprofen is rapidly absorbed after oral administration of Combunox (oxycodone hcl and ibuprofen) . Cmax values range from 18.5 mcg/mL to 34.3 mcg/mL and are reached 1.6 hr to 3.1 hr after oral administration of Combunox (oxycodone hcl and ibuprofen) . Repeated administration of Combunox (oxycodone hcl and ibuprofen) every 6 hours does not result in any accumulation of ibuprofen. The bioavailability of ibuprofen is not altered in the presence of food.

Distribution

Oxycodone binding to protein in serum is approximately 45%.

Ibuprofen is extensively bound to plasma proteins (99%).

Metabolism

Oxycodone is metabolized in the liver by means of N-demethylation and O-demethylation, 6ketoreduction and glucuronidation. The major circulating metabolite is noroxycodone, which possesses weak analgesic activity.

Oxymorphone, the end product of O-demethylation, has analgesic activity but is present in the plasma at low concentrations. Metabolism of oxycodone to oxymorphone occurs via CYP2D6.

Ibuprofen is present as a racemate and following absorption, it undergoes interconversion in the plasma from the R-isomer to the S-isomer.

Both the R- and S- isomers are metabolized to two primary metabolites: (+)-2-4'-(2-hydroxy2-methyl-propyl) phenyl propionic acid and (+)-2-4'-(2-carboxypropyl) phenyl propionic acid, both of which circulate in the plasma at low levels relative to the parent.

Elimination

Oxycodone is eliminated from the systemic circulation with half life (T½) values ranging from 3.1 hr to 3.7 hr after single dose administration of Combunox (oxycodone hcl and ibuprofen) . Urinary excretion of unchanged oxycodone amounts to approximately 4% of the administered oxycodone dose.

Ibuprofen is eliminated from the systemic circulation with half life (T½) values ranging from 1.8 hr to 2.6 hr after single dose administration of Combunox (oxycodone hcl and ibuprofen) . Urinary excretion of unchanged ibuprofen is minimal (less than 0.2% of administered ibuprofen dose).

Special Populations

Gender : There are no gender effects on the pharmacokinetics of oxycodone or ibuprofen after administration of Combunox (oxycodone hcl and ibuprofen) .

Age: The effects of age on the pharmacokinetics of oxycodone and ibuprofen after administration of Combunox (oxycodone hcl and ibuprofen) have not been evaluated.

When either drug was administered alone, the pharmacokinetics of oxycodone and ibuprofen were similar in elderly subjects, compared to young healthy subjects.

Pediatrics: The pharmacokinetics of oxycodone and ibuprofen after administration of Combunox (oxycodone hcl and ibuprofen) have not been evaluated in a pediatric population.

Renal Impairment: The effects of renal impairment on the pharmacokinetics of oxycodone and ibuprofen after administration of Combunox (oxycodone hcl and ibuprofen) have not been evaluated.

Hepatic Impairment: The effects of hepatic impairment on the pharmacokinetics of oxycodone and ibuprofen after administration of Combunox have not been evaluated. (See PRECAUTIONS; Hepatic Effects)

Clinical Studies

Combunox (oxycodone hcl and ibuprofen) was investigated in three clinical studies. Two studies involving a total of 949 patients following dental surgery (removal of ipsilateral molars) and a third study of 456 patients following abdominal/pelvic surgery were conducted. In the three studies patients were administered a single dose of the Combunox (oxycodone hcl and ibuprofen) , ibuprofen alone, oxycodone HCl alone or placebo for acute, moderate to severe pain.

In these single dose studies, Combunox (oxycodone hcl and ibuprofen) produced greater efficacy than placebo and each of Combunox (oxycodone hcl and ibuprofen) 's individual components as measured by the magnitude of pain relief and the reduction in pain intensity through six hours. No multiple dose efficacy studies have been performed with Combunox (oxycodone hcl and ibuprofen) .

Last reviewed on RxList: 9/23/2010
This monograph has been modified to include the generic and brand name in many instances.

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