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HOME >> API >> API List 3 >> Oxcarbazepine >> Interaction

INTERACTION
Oxcarbazepine CAS number 28721-07-5

Oxcarbazepine was evaluated in human liver microsomes to determine its capacity to inhibit the major cytochrome P450 enzymes responsible for the metabolism of other drugs. Results demonstrate that oxcarbazepine and its pharmacologically active 10-monohydroxy metabolite (MHD) have little or no capacity to function as inhibitors for most of the human cytochrome P450 enzymes evaluated (CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP2E1, CYP4A9 and CYP4A11) with the exception of CYP2C19 and CYP3A4/5. Although inhibition of CYP3A4/5 by oxcarbazepine and MHD did occur at high concentrations, it is not likely to be of clinical significance. The inhibition of CYP2C19 by oxcarbazepine and MHD, however, is clinically relevantIn vitro, the UDP-glucuronyl transferase level was increased, indicating induction of this enzyme. Increases of 22% with MHD and 47% with oxcarbazepine were observed. As MHD, the predominant plasma substrate, is only a weak inducer of UDP-glucuronyl transferase, it is unlikely to have an effect on drugs that are mainly eliminated by conjugation through UDP-glucuronyl transferasen addition, oxcarbazepine and MHD induce a subgroup of the cytochrome P450 3A family (CYP3A4 and CYP3A5) responsible for the metabolism of dihydropyridine calcium antagonists, oral contraceptives and cyclosporine resulting in a lower plasma concentration of these drugs.As binding of MHD to plasma proteins is low (40%), clinically significant interactions with other drugs through competition for protein binding sites are unlikely.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription medication you may use, especially: calcium channel blockers , other seizure control medication (e.g., carbamazepine, phenytoin, phenobarbital, valproic acid). This medication may decrease the effectiveness of combination-type birth control pills. You may need to use an additional form of reliable birth control while using this medication. Consult your doctor or pharmacist. Tell your doctor if you take any drugs that make you drowsy, such as: medicine for sleep, sedatives, tranquilizers, anti-anxiety drugs (e.g., diazepam), narcotic pain relievers (e.g., hydrocodone, codeine), psychiatric medicines (e.g., phenothiazines such as chlorpromazine, or tricyclics such as amitriptyline), muscle relaxants, antihistamines that cause drowsiness (e.g., diphenhydramine). Check the labels on all your medicines (e.g., cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about the safe use of those products. Do not start or stop any medicine without doctor or pharmacist approval.

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