Flexyx

Flexyx drugs: Trileptal

Trileptal - General Information:

Trileptal is structurally a derivative of carbamazepine, adding an extra oxygen atom to the benzylcarboxamide group. This difference helps reduce the impact on the liver of metabolizing the drug, and also prevents the serious forms of anemia occasionally associated with carbamazepine. Aside from this reduction in side effects, it is thought to have the same mechanism as carbamazepine - sodium channel inhibition - and is generally used to treat partial seizures in epileptic children and adults.




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Generic Trileptal (Oxcarbazepine) - 150mg 60 pills for $52.92 Trileptal (Oxcarbazepine) helps reduce the frequency of partial epileptic seizures, a form of epilepsy in which neural disturbances are limited to a specific region of the brain and the victim remains conscious throughout the attack. Trileptal may be prescribed by itself to treat the problem in adults. It can also be used in combination with other seizure medications in adults and in children as young as four years old. Oxcarbazepine can cause drowsiness, dizziness, and loss of coordination, which could impair your ability to drive a vehicle or operate dangerous machinery. Do not attempt hazardous activities until you know how the drug affects you.

Pharmacology:

Trileptal is structurally a derivative of carbamazepine, adding an extra oxygen atom to the benzylcarboxamide group. This difference helps reduce the impact on the liver of metabolizing the drug, and also prevents the serious forms of anemia occasionally associated with carbamazepine. Aside from this reduction in side effects, it is thought to have the same mechanism as carbamazepine - sodium channel inhibition - and is generally used to treat the same conditions.

Trileptal for patients

Patients who have exhibited hypersensitivity reactions to carbamazepine should be informed that approximately 25-30% of these patients may experience hypersensitivity reactions with Trileptal^TM(oxcarbazepine).

Female patients of childbearing age should be warned that the concurrent use of Trileptal with hormonal contraceptives may render this method of contraception less effective. Additional non-hormonal forms of contraception are recommended when using Trileptal.

Caution should be exercised if alcohol is taken in combination with Trileptal therapy, due to a possible additive sedative effect.

Patients should be advised that Trileptal may cause dizziness and somnolence. Accordingly, patients should be advised not to drive or operate machinery until they have gained sufficient experience on Trileptal to gauge whether it adversely affects their ability to drive or operate machinery.

Trileptal Interactions

Oxcarbazepine can inhibit CYP2C19 and induce CYP3A4/5 with potentially important effects on plasma concentrations of other drugs. In addition, several AED’s that are cytochrome P450 inducers can decrease plasma concentrations of oxcarbazepine and MHD.

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 CYP 3A4/5 by OXC and MHD did occur at high concentrations, it is not likely to be of clinical significance. The inhibition of CYP-2C19 by OXC and MHD, however, is clinically relevant.

In 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 transferase (e.g., valproic acid, lamotrigine).

In addition, oxcarbazepine and MHD induce a subgroup of the cytochrome P450 3A family (CYP3A4 and CYP3A5) responsible for the metabolism of dihydropyridine calcium antagonists and oral contraceptives, 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.

Antiepileptic drugs

Potential interactions between Trileptal and other AEDs were assessed in clinical studies. The effect of these interactions on mean AUCs and C_min are summarized in Table 2:

Table 2: Summary of AED interactions with Trileptal

AED Co-administered	Dose of AED (mg/day)	Trileptal dose (mg/day)	Influence of Trileptal on AED Concentration (Mean change, 90% Confidence Interval)	Influence of AED On MHD Concentration (Mean change, 90% Confidence Interval)
Carbamazepine	400-2000	900	nc1	40% decrease [CI: 17% decrease, 57% decrease]
Phenobarbital	100-150	600-1800	14% increase [CI: 2% increase, 24% increase]	25% decrease [CI: 12% decrease, 51% decrease]
Phenytoin	250-500	600-1800	nc1,2	30% decrease [CI: 3% decrease, 48 % decrease]
		>1200-2400	up to 40% increase3 [CI: 12% increase, 60 % increase]
Valproic acid	400-2800	600-1800	nc1	18% decrease [CI: 13% decrease, 40 % decrease]

¹- nc denotes a mean change of less than 10%
²- Pediatrics
³- Mean increase in adults at high Trileptal doses

In vivo, the plasma levels of phenytoin increased by up to 40%, when Trileptal was given at doses above 1200 mg/day. Therefore, when using doses of Trileptal greater than 1200 mg/day during adjunctive therapy, a decrease in the dose of phenytoin may be required. The increase of phenobarbital level, however, is small (15%) when given with Trileptal.

Strong inducers of cytochrome P450 enzymes (i.e. carbamazepine, phenytoin and phenobarbital) have been shown to decrease the plasma levels of MHD (29-40%).

No autoinduction has been observed with Trileptal.

Hormonal contraceptives

Co-administration of Trileptal with an oral contraceptive has been shown to influence the plasma concentrations of the two hormonal components, ethinylestradiol (EE) and levonorgestrel (LNG). The mean AUC values of EE were decreased by 48% [90% CI: 22-65] in one study and 52% [90% CI: 38-52] in another study [1,2]. The mean AUC values of LNG were decreased by 32% [90% CI: 20-45] in one study and 52% [90% CI: 42-52] in another study. Therefore, concurrent use of Trileptal with hormonal contraceptives may render these contraceptives less effective. Studies with other oral or implant contraceptives have not been conducted.

Calcium Antagonists

After repeated co-administration of Trileptal, the AUC of felodipine was lowered by 28% [90% CI: 20-33].

Verapamil produced a decrease of 20% [90% CI: 18-27] of the plasma levels of MHD.

Other drug interactions

Cimetidine, erythromycin and dextropropoxyphene had no effect on the pharmacokinetics of MHD. Results with warfarin wshow no evidence of interaction with either single or repeated doses of Trileptal.

Trileptal Contraindications

Oxcarbazepine should not be used in patients with a known hypersensitivity to oxcarbazepine or to any of its components.

Additional information about Trileptal

Trileptal Indication: For use as monotherapy or adjunctive therapy in the treatment of partial seizures in adults with epilepsy and as adjunctive therapy in the treatment of partial seizures in children ages 4-16 with epilepsy.
Mechanism Of Action: The exact mechanism by which oxcarbazepine exerts its anticonvulsant effect is unknown. It is known that the pharmacological activity of oxcarbazepine occurs primarily through its 10-monohydroxy metabolite (MHD). In vitro studies indicate an MHD-induced blockade of voltage-sensitive sodium channels, resulting in stabilization of hyperexcited neuronal membranes, inhibition of repetitive neuronal discharges, and diminution of propagation of synaptic impulses.
Drug Interactions: Cyclosporine Trileptal decreases the effect of cyclosporine
Felodipine Trileptal decreases the levels of felodipine
Mestranol Trileptal decreases the effect of the contraceptive
Ethinyl Estradiol Trileptal decreases the effect of the contraceptive
Ethotoin Trileptal increases the effect of hydantoin
Fosphenytoin Trileptal increases the effect of hydantoin
Mephenytoin Trileptal increases the effect of hydantoin
Phenytoin Trileptal increases the effect of hydantoin
Food Interactions: Not Available
Generic Name: Oxcarbazepine
Synonyms: Oxcarbamazepine
Drug Category: Anticonvulsants
Drug Type: Small Molecule; Approved
Other Brand Names containing Oxcarbazepine: Trileptal;
Absorption: Completely absorbed following oral administration. Food has no effect on the rate and extent of absorption of oxcarbazepine.
Toxicity (Overdose): Isolated cases of overdose with oxcarbazepine have been reported. The maximum dose taken was approximately 24,000 mg. All patients recovered with symptomatic treatment.
Protein Binding: Approximately 40% of the active 10-monohydroxy metabolite (MHD) is bound to serum proteins, predominantly to albumin. Neither oxcarbazepine nor its MHD binds with alpha-1–acid blycoprotein.
Biotransformation: Oxcarbazepine is completely absorbed and extensively metabolized to its pharmacologically active 10-monohydroxy metabolite (MHD). MHD is metabolized further by conjugation with glucuronic acid.
Half Life: The half-life of the parent is about 2 hours, while the half-life of MHD is about 9 hours, so that MHD is responsible for most anti-epileptic activity.
Dosage Forms of Trileptal: Tablet Oral
Suspension Oral
Chemical IUPAC Name: 5-oxo-6H-benzo[b][1]benzazepine-11-carboxamide
Chemical Formula: C15H12N2O2
Oxcarbazepine on Wikipedia: http://en.wikipedia.org/wiki/Oxcarbazepine
Organisms Affected: Humans and other mammals