Trileptal 300 Novartis medicine for local epilepsy (5 blisters x 10 tablets)
Dosage form Box of 5 blisters x 10 tablets
Specifications Oxcarbazepine
Ingredient
| Composition information | Content |
| Oxcarbazepine | 300mg |
Uses
Indications
trileptal drugs are indicated in the following cases:
Pharmacy
Mechanism of action
The pharmacological activity of trileptal (or oxcarbazepine) is mainly promoted through the metabolic product (MHD) of oxcarbazepine. The mechanism of action of oxcarbazepine and MHD is said to be mainly based on the blockage of voltage sensitive channels, thus stabilizing nerve membranes to be excited, inhibiting repetitive stimulation in nerve cells and reducing the spread of pulses through neurological synap. In addition, the increased potassium conductivity and the modulation of high voltage calcium channels can also contribute to the anti -seizure effects of the drug. There is no important drug interaction with the receptor of nervous regulation or neurotransmitters.
Pharmacological properties
Oxcarbazepine and its active metabolic products (MHD) are both resistant to convulsions and efficiency on animals. They protect rodents that are anti -spasms - total convulsions, at a lower extent, shaking seizures, and loss or reduction of the frequency of chronic local seizures on Rhesus monkeys are implanted with aluminum pieces. No tolerance (for example, anti -convulsive activity) for spastic - convulsions are observed on mice and mice treated daily for 5 days or for 4 weeks with oxcarbazepine or MHD.
pharmacokinetic
absorption
After taking Trileptal tablets, Oxcarbazepine is completely absorbed and metabolized mostly into a pharmacological metabolic product (10- monohydroxy, MHD).
After using a single dose of 600mg of Trileptal tablets on men who volunteered healthy fasting, the average CMAX value of MHD is 34mmol/l, with an average average TMAX value of 4.5 hours.
The tablet form and oxcarbazepine oral chaos are biological equivalent because the average concentration curve at the single dose and stable state, CMAX and AUC in the range of 0.85 to 1.86 (90% of reliable intervals).
In a human weight balancing study, only 2% of the total number of radioactive in plasma is due to the constant oxcarbazepine, about 70% due to MHD and the rest is due to the quickly eliminated secondary metabolic products.
Food does not affect the ratio and ability to absorb oxcarbazepine. Therefore Trileptal can be used or not accompanied by food.
Distribution
The apps of MHD's apparent distribution is 49L. About 40% MHD is associated with serum protein, mainly with albumin. This cohesion is in the scope of treatment. Oxcarbazepine and MHD are not attached to Alpha-1-acid Glycoprotein.
Biological/metabolic transformation
Oxcarbazepine is quickly converted by cytosolic enzymes in the liver into MHD, which is mainly responsible for the pharmacological effects of trileptal. MHD continues to be metabolized by a combination with glucuronic acid. A small amount (4% of the dose) is oxidized into non-active metabolic products (derivatives 10.11-dihydroxy, DHD).
Elimination
Oxcarbazepine is eliminated from the body, largely in the form of metabolic products and is excreted mainly through the kidneys. More than 95% of the dosage is discharged into urine, of which less than 1% of oxcarbazepine form is constant. The amount of excretion through the part accounts for less than 4% of the dose.
About 80% of the dose is excreted in the urine in the form of or MHD combining glucuronide (49%) or a constant MHD (27%), while the amount of DHD is not active, accounting for about 3% and the combination substances of Oxcarbazepine accounts for 13% of the dose. Oxcarbazepine is quickly excluded from the plasma with the half -life of about 1.3 - 2.3 hours. In contrast, the semi -cancellation time in the plasma of MHD is 9.3 ± 1.8 hours.
linear/non -linear
MHD concentration in plasma in a sustainable state is achieved after 2-3 days in patients when Trileptal is used to be divided into two times a day. In a sustainable state, MHD's pharmacokinetics are linearly and shows the balance of the dose balance at 300 - 2400mg/day.
Special subjects
Hepatic failure
pharmacokinetics and metabolism of oxcarbazepine and MHD have been assessed on healthy volunteers and subjects with liver failure after taking only 900mg. Mild and moderate liver failure does not affect the pharmacokinetics of oxcarbazepine and MHD. Trileptal has not been studied in patients with severe liver failure.
kidney failure
There is a linear relationship between creatinine clearance and the renal clearance of MHD. When Trileptal is given a single dose of 300mg in patients with renal impairment (Creatinine clearance ratio
Children
The purification of MHD is adjusted to the weight will decrease when age and weight increase to the age and weight of adults. Therefore, the average purification of MHD has been adjusted to children in children (from 1 month of age to 4 years old) will account for 93% higher than the purification in adults. Therefore, the exposure of MHD in the body of these children is only about half of the exposure of MHD in adults, when the same dose is also adjusted in weight.
The average purification of MHD has been adjusted to children in children (from 4 to 12 years old) will be 43% higher than the average purification in adults. Therefore, the exposure of MHD in the body of these children is only two -thirds of the exposure in adults, when the same dosage is adjusted to the body. Once there is a weight gain, for patients ≥ 13 years old, the purification of MHD is adjusted according to the weight, which is considered to achieve MHD purification in adults.
Pregnant women
Due to physiological changes during pregnancy, plasma MHD concentration may decrease during pregnancy.
Older people
After using a single dose (300mg) and many times (600mg/day) Trileptal on the elderly volunteers (60 - 82 years old), maximum plasma concentrations and AUC values of MHD are 30-60% higher than younger volunteers (18 - 32 years old). Comparing the clearance coefficient between young people and the elderly shows that this difference is due to the decline in age related to the creatinine clearance coefficient. There is no need for any special recommendations for the dose because the treatment is adjusted by individuals.
Gender
There is no difference in pharmacokinetics related to gender seen in children, adults or the elderly.
Before taking Trileptal 300 Novartis medicine for local epilepsy (5 blisters x 10 tablets)
How to use
Oral drugs.
The tablets are slashed, so it can be broken into two half of the tablet, making it easier for patients to swallow pills. For young children or patients who cannot swallow pills or doses that do not allow the use of tablets, can use Triileptal in the form of existing in the market.
Trileptal oral fluid and trileptal film tablets are biological equivalent and can be converted at equal doses.
trileptal can be used or not accompanied by food.
Dosage
Coordinate treatment in adults
Start using Trileptal at a dose of 600mg/day, divided into twice a day. If clinically indicated, the dose may be increased by a maximum amount of 600mg/day with the distance between the times approximately 1 week, the maximum daily dose recommended is 1200mg/day. The daily dose is over 1200mg/day, which shows higher efficiency in the control test, but most patients are not able to tolerate the dose of 2400mg/day, mainly due to the effects on the central nervous system. It is recommended to closely monitor patients and plasma concentrations of anti -epileptic drugs when used simultaneously in the period of trileptal dose, as these concentrations may be changed, especially in the doses of trileptal greater than 1200mg/day.
Convert to monomers in adults
Patients who use simultaneous anti -epileptic drugs can be transferred to single therapy by starting Trileptal treatment at a dose of 600mg/day (the dose is divided into 2 times a day) while at the same time starting to reduce the anti -epileptic dose attached. Anti -epileptic drugs should be used at the same time within 3 to 6 weeks, while the maximum dose of Trileptal should be achieved after about 2 to 4 weeks.
The dosage of trileptal can be increased according to clinical indicators with a maximum increase of 600mg/day with the distance between the times is approximately 1 week to achieve the maximum daily recommendation of 2400mg/day. The daily dose of 1200mg/day has been shown in a study that is effective in patients who use monomers to start with Trileptal. Patients should be closely monitored during this transition.
Starting monomers in adults
Patients who are not treated with anti -epileptic drugs may be started to be mono -therapy with Trileptal. In these patients, start using Trileptal at a dose of 600mg/day (divided into twice a day), the dose should be increased by 300mg/day after every 3 days to 1200mg/day. The control tests in these patients have tested the effect of the dose of 1200mg/day, the dose of 2400mg/day has been shown to be effective on patients transferring from other anti -epileptic drugs to monomers with trileptal (see above).
Coordinate treatment for children (from 2 to 16 years old)
In children from 4 to 16 years old, starting trileptal with daily dose from 8 - 10mg/kg usually does not exceed 600mg/day, divided into twice a day. The destination dose of trileptal should be achieved for 2 weeks and depends on the patient's weight, according to the following chart:
In children from 2 to under 4 years old, starting to use trileptal at daily dose from 8 to 10mg/kg usually does not exceed 600mg/day, divided into twice a day. For patients under 20kg, the dose can be considered from 16 to 20mg/kg. The maximum maintenance dose of Trileptal should be achieved within 2-4 weeks and must not exceed 60mg/kg/day with the dosage mode twice a day.
In children's clinical trials (2-4 years old), which intends to achieve the target dose of 60mg/kg/day, 50% of patients who achieve the final dose are at least 55mg/kg/day. In coordination treatment (with or without anti -epileptic sensor enzyme), when normalized according to weight, the elite clearance (l/hour/kg) decreases while the age increases, so children from 2 to
Conversion to single therapy for children (from 4 to 16 years old)
Patients with combination of anti -epileptic drugs can be transferred to single therapy by starting Trileptal treatment with a dose of 8 - 10mg/kg/day divided into two times, while at the same time starting to reduce the anti -epileptic dose attached. The combination of epilepsy medications can be completely stopped within 3-6 weeks while the trileeptal dose may increase according to clinical indicators with a maximum dose increase of 10mg/kg/day with a dose gap is approximately a week to achieve the recommended daily dosage. Patients should be closely monitored during this transition period.
Total daily dose recommended by trileptal is shown in Table 1 below.
Starting single therapy for children's patients (from 4 to 16 years old)
Patients are not treated with anti -epileptic drugs that can be used for monomers starting with trileptal. In these patients, start using Trileptal at a dose of 8 - 10mg/kg/day divided twice a day. The dose should be increased by 5 mg/kg/day after every 3 days according to the recommended daily dosage as in the table below.
Table 1: Triileptal's maintenance dose range for children according to weight in single therapy.
weight in kg
60
For patients with renal function (creatinine clearance below 30ml/minute), starting trileptal with a dose equal to half the starting dose is often used (300mg/day, divided twice a day) and increasing the dose to achieve the desired clinical response.
Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.
What to do when overdose? The maximum dose has been used is about 48,000mg.
Signs and symptoms
Testing: Reduce respiratory frequency, extend QT. Central nervous system disorders: drowsiness and drowsiness, dizziness, vibration of the eyeball, loss of air conditioning, tremor, coordination disorders (unusual coordination), convulsions, headaches, coma, consciousness, movement disorders. Mental disorders: aggression, excitement, confusion. Management There is no specific antidote. Symptomatic treatment and support should be conducted appropriately. The removal of gastrointestinal or inactive carbon should be considered. What to do when you forget a dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Note that it should not be used double the prescribed dose.
Side Effects
When using trileptal drugs , you may experience unwanted effects (ADR).
Safety data summary
The most commonly common reactions include drowsiness, headache, dizziness, double look, nausea, vomiting, fatigue, in> 10% of patients.
In clinical trials, adverse events (AE) are usually at mild to medium levels, more airy and more common at the beginning of treatment.
Analysis of unwanted effect charts according to the organ system is based on harmful phenomena from clinical trials assessed to be related to Trileptal. In addition, the clinical reports of harmful experience from programs with patients are identified and experienced when bringing the drug to the market are also taken into account.
Very common
Gastrointestinal disorders : vomiting, nausea.
Common
Mental disorders: agitation (for example: nervous tension), unstable emotions, confusion, depression, insensitivity. Nervous system disorders: loss of air conditioning, tremor, vibration of the eyeball, disorder of attention, dementia. Gastrointestinal disorders: diarrhea, abdominal pain, constipation. Skin and subcutaneous tissue disorders: rash, hair loss, acne. Less Hyper enzyme increased, alkaline phosphatase in the blood. Very rare Immune system disorders: Anaphylactic reaction, hypersensitivity (including hypersensitivity to many organs) are characterized by manifestations such as rash, fever. Other organs or systems may be affected such as blood and lymphatic system (e.g. leukemia loves EOSIN, thrombocytopenia, leukopenia, lymph nodes, enlarged spleen), liver (for example, hepatitis, abnormal tests of liver function), muscle and joint (for example, swelling of joints, muscle pain, joint pain), nervous system (eg liver - liver), pulmonary pulmonary impairment (for example, kidney impairment). Bronchospasm, interstitial lung disease, shortness of breath), angioedema. Endocrine disorders: Hypothyroidism. Disorders of metabolic and nutrition: Hypotrusal hypoglycet* Having signs and symptoms such as convulsions, brain disease, consciousness, confusion, hypothyroidism, visual disorders (for example, blurred vision), vomiting, nausea, folic acid deficiency. digestive disorders: pancreatitis or increase lipase and increase amylase. Hepatitis: Hepatitis. Skin and subcutaneous tissue disorders: Stevens-Johnson syndrome, poisoned epidermal necrosis (lyell syndrome), angioedema, polymorphic erythematosus. * While using Trileptal, it is very rare to lower sodium-clinical significance (sodium In clinical trials in children from 1 month of age to 4 years of age, the most harmful reaction is drowsiness, in about 11% of patients. The reactions are harmful with frequency> 1% and Unwanted effects recorded from spontaneous reports and cases in literature (unknown frequency) The following unwanted effects have been recorded from Trilental's after -sales experience through spontaneous reports and reports in literature. Because these unwanted effects are voluntarily reported from unknown sample -sized disease sources, it is impossible to accurately estimate the frequency, so this item will be classified as unknown frequency. The effects do not want to be listed below according to the media system classification. In each organ system, ADRS is recorded in the order of gradual decline in severity. Nervous system disorders: Language disorders (including speech disorder), more common when increasing trileptal dose. Instructions on how to handle ADR When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.
Warnings
Before using the drug you need to read the instructions carefully and refer to the information below.
Contraindicated
Triileptal drug contraindicated in the following cases:
Precautions when using
Hypersensitivity
The hypersensitivity reaction type I (instantly) includes rash, itching, urticaria, angioedema and anaphylactic reports recorded in the after -sales stage. There have been reports on evaluation and angioed cases including larynx, bar, lips and eyelids in patients after taking the first doses of trileptal or the next dose. If the patient has these reactions after trileptal treatment, stop taking the drug and start treatment with another drug.
Patients who have had a hypersensitivity reaction to carbamazepine should be informed that about 25-30% of these patients may be sensitive to Trileptal.
Hypersensitivity reactions, including hypersensitivity in many organs can also occur in patients without a history of hypersensitivity to carbamazepine. These reactions may affect the skin, liver, blood, lymphatic system or other organs, occur individually or combine together in the disease of the whole body reaction. In general, if there are signs and symptoms suggesting the hypersensitivity reaction, TriLeptal must be stopped immediately.
Effects on skin
When using Trileptal, it is very rare for serious skin-skin reactions, including Stevens-Johnson syndrome, poisoned epidermal necrosis (Lyell syndrome) and a variety of erythema. Patients with serious skin reactions may have to be hospitalized, because these conditions may be life -threatening and death (although very rare). The above reactions are used by trileptal both in children and adults. The average time to start the reaction is 19 days. There are also some cases of serious skin reactions when using Trileptal. When the patient has a skin reaction to Trileptal, it is necessary to consider stopping trileptal and replacing with other anti -epileptic drugs.
Pharmacological genes
There is more and more evidence that different isotopic genes (allele) of white blood cell antigen (HLA) plays a role in related to side effects on skin in patients susceptible.
Regarding HLA-B*1502
Rescue studies in Chinese and Thai-Chinese patients showed a strong correlation between SJS/Ten-Ten skin reactions caused by Carbamazepine and patients with HLA-B*1502 white blood cell antigen.
Because the chemical structure of oxcarbazepine is similar to the structure of carbamazepine, it is likely that patients with HLA-B*1502 isotope genes also increase the risk of SJS/Ten's skin reaction with Oxcarbazepine.
The frequency of HLA -B*1502 isotope gene is 2 - 12% of the Chinese population, about 8% of Thai people, more than 15% in the Philippines and some Malaysians. This isotope gene frequency is up to 2% in Korea and 6% in India, respectively. The frequency of HLA-B*1502 is not significant in Europeans, some races in Africa, native Americans, Spanish origin and in Japan (
Checking the presence of HLA-B*1502 isotope gene should be considered in patients with ancestors in the genetic risk group, before the beginning of Trileptal treatment (see information for medical experts below). Trileptal should be avoided for patients whose test results show positive for HLA-B*1502 unless the benefits are out of risk. HLA-B*1502 can be a risk factor for the development of SJS/Ten in Chinese population using other anti-epileptic drugs (AED) involving SJS/Ten.
Therefore, it is necessary to consider avoiding drugs related to SJS/Ten in HLA-B*1502 positive patients, when other alternative treatments are accepted. The screening is not recommended for patients with HLA-B*1502 frequency or patients who are using Trileptal, because the risk of SJS/Ten is limited to the first few months of treatment regardless of HLA-B*1502.
Regarding HLA-A*3101
Human leukemia (HLA) -A*3101 can be a risk factor for side effects in the skin such as SJS, Ten, Dress, Agep and lumpy rash. The frequency of HLA-A*3101 isotope gene changes diverse among peoples and its frequency is about 2 to 5% in European population and about 10% in Japanese people. The frequency of this isotope gene is estimated to be less than 5% in most people in Australia, Asia, Africa and North America with a few exceptions of 5-12%. The frequency of more than 15% is estimated in some ethnic groups such as South America (Argentina and Brazil), North America (Navajo, Sioux and Mexico Sonora Seri) and South India (Tamil Nadu) and between 10-15% in indigenous peoples in the same region.
The frequency of isotopic gene is listed here that represents the percentage of chromosomes in special population that has this isotope gene, meaning that the percentage that the patient carries a copy of this isotope gene on at least one of their two chromosomes (the "carrier frequency") is nearly double the frequency of the isotope gene. Therefore, the percentage of patients is at risk of twice the frequency of isotope gene.
There are figures that HLA-A*3101 is related to an increase in the risk of side effects on the skin due to carbamazepine including sjs, ten,, rashes by drugs combined with acidic hyperthemics due to allergies, or acute acne rash (AGEP) and an inlaid base. Inadequate data consolidated for the recommendation of testing the presence of HLA-A*3101 isotopes in patients before the beginning of treatment with oxcarbazepine. Genetic tests do not recommend for patients who are using Trileptal, because the risk of SJS, Ten, Dress and lumpy rash limits the range in the first few months of treatment, regardless of HLA-A*3101.
The limit of genetic screening
The results of genetic screening never replace appropriate clinical alert and patient management. Many Asian patients are positive for HLA-B*1502 and Trileptal treatment is not sjs/ten and negative patients with HLA-B*1502 any race can still be sjs/ten.
Similarly to HLA A*3101 positive patients and using Trileptal is not sjs, ten, dress, Agep or lumpy rash and negative patients with HLA-A*any race can still suffer from severe side effects on the skin. The role of other potential factors in the development and diseases from these skin reactions such as AED dose, compliance, simultaneous use with other drugs, other accompanying diseases and the level of skin monitoring has not been studied.
Information for medical experts
If checking the presence of HLA-B*1502 isotopes is made, HLA-B*1502 genotype is recommended. Positive testing if either HLA-B*1502 isotopes are detected and negative if no isotope gene is detected. Similarly, if checking the presence of HLA-B*3101 isotopes is made, "high-resolution HLA-B*3101 gene" is recommended. Positive testing if either HLA-B*3101 isotopes are detected and negative if no isotope gene is detected.
The risk of aggravation of epilepsy
The risk of aggravation is reported when using trileptal, this risk is considered special in children, but can also occur in adults. In case of aggravation, it is recommended to stop using Trileptal.
Hypothensi
There are 2.7% of patients using Trileptal with sodium concentrations in serum below 125mmol/liter, often asymptomatic and no requirements for treatment. Experience from clinical trials shows that the concentration of sodium-bars will return to normal after the dose decrease or stop trileptal or when the patient is treated cautiously (for example, limiting imported fluid).
For patients who have had kidney disease in advance, accompanied by a lack of sodium content (such as inappropriate ADH secretion syndrome) or with patients using sodium waste (e.g. diuretic, adh excretory drugs adh), the amount of sodium-level concentration must be quantified before starting to use trileptal. After that, the sodium-level concentration is also required after about 2 weeks and then the monthly test for the first 3 months of treatment, or depending on the clinical requirements. These risk factors are particularly needed for elderly patients.
For patients using Trileptal and starting to use drugs to lower sodium, they also monitor sodium evaluation as mentioned above. In general, when encountering clinical symptoms about sodium-lowering when using trileptal, it can be considered to measure the content of sodium-bar. Other patients may have a sodium-concentration that is assessed as part of the routine studies in the labo.
Every patient with a heart failure or secondary heart disease needs to be tested regularly to determine if there is an epidemic accumulation? If the accumulation of fluid or the heart worsens, it is necessary to assess the concentration of sodium-bar. When sodium-lowered, it is important to limit the use of water. Because oxcarbazepine in a very rare case can weaken cardiac transmission, careful monitoring of patients who have had a heart transmission disorder (for example, atrial block, arrhythmia).
Hypothyroidism
Hypothyroidism is a very rare adverse reaction of oxcarbazepine. Because of the importance of thyroid hormones with the development of children after birth, the thyroid function should be assessed before starting treatment with Trileptal in a group of children's patients, especially in children from 2 years of age. Recommended monitoring of thyroid function when treating with trileptal in groups of children.
Liver function
Very rare hepatitis, most of the cases are easily over. If suspected of having hepatitis, it is recommended to stop using trileptal. Precautions when treating with patients with severe liver failure.
Kidney function
Precautions when using trileptal for patients with impaired renal function (creatinine clearance is less than 30ml/min), especially when the starting dose and when increasing the dose.
Hematology effects
There have been reports in very rare cases of granulocytosis, anemia and reduced hemorrhage in patients treated with trileptal in after -sales research. However, due to the new incidence of these conditions is very low and the noise factors (such as the main disease, the drug used simultaneously), cannot identify the cause and effect. It is necessary to consider stopping the drug if there is any significant symptoms of bone marrow failure.
intentions and suicide behavior
There have been reports on behavior and suicide intentions in patients treating anti -epileptic drugs in some indications. A comprehensive study of random clinical trials, controlled to the placebo of anti -epileptic drugs shows a slight increase in the risk of behavior and suicide intentions. The mechanism of this risk is not known. Therefore, patients should be monitored with signs of behavior and suicide intentions and need to consider appropriate treatments, patients (and patient care) should ask the doctor when they see signs of intentions or suicide behavior.
Drug interaction
Hormone contraceptives
Patients with reproductive age should be warned that when coordinating trileptal with contraceptive hormones can cause loss of effect. When using Trileptal, it is recommended to use non -hormone contraceptive measures.
alcohol
Be careful when using alcohol with trileptal because it can increase the effect of drowsiness.
Effects when stopping drugs
As with all anti -epileptic drugs, Trileptal should be stopped gradually in each level, to minimize the risk of increasing convulsions.
The ability to drive and operate machinery
Agricultural reactions such as dizziness, drowsiness, loss of air conditioning, double view, blurred vision, visual disorders, sodium reduction and consciousness have been reported to trileptal, especially at the beginning of treatment, or the conversion phase when the dose adjustments (more commonly in the stage of increasing dose). Therefore, it is necessary to warn patients when driving and operating machinery.
Pregnancy
Summary of risks
Children of epilepsy mothers are susceptible to development disorders, including malformations. Using oxcarbazepine during pregnancy shows that this drug can cause serious malformations at birth, although data on quantity is limited. The most common birth defects are observed when treated with oxcarbazepine is the left ventricular septum defect, atrial atrial septum defect, cleft palate with cleft lips, down syndrome, hip dysplasia (one and two sides), scleroderma and congenital deformities.
Based on data in a list of pregnancy registration in North America, the rate of serious birth defects, is defined as structural abnormalities that need surgery, medication or cosmetic, diagnosed within 12 weeks after birth in mothers using oxcarbazepine in the first three months of pregnancy is 2% (95% trusted interval: 0.6 to 5.1%). When compared to pregnant women who do not use any anti -epileptic drugs, the relative risk (RR) has a birth defect for pregnant women using oxcarbazepine is 1.6 (95% of reliable interval: 0.46 to 5.7).
Clinical consideration
Consider the following cases:
Should use minimum doses that tend to treat.
Monitor and Prevention
Anti -epileptic drugs can cause folic acid deficiency, which is a cause of abnormalities for the fetus. Before and during pregnancy, it is recommended to supplement folic acid for pregnant women.
Due to physiological changes during pregnancy, plasma concentrations of metabolites have the activity of oxcarbazepine, 10-Monohydroxy derivatives (MHD) can gradually decrease during pregnancy. It is recommended that clinical response should be carefully monitored in women treated with trileptal during pregnancy and determining the change of plasma MHD concentration should be considered to ensure that the control of seizures adequately maintained during pregnancy. The concentration of plasma MHD after birth may also be considered for special monitoring in case the use of drugs increases during pregnancy.
In newborn children
There have been reports on bleeding disorders in newborns because mothers use anti -epileptic drugs. To be cautious, preventive measures should be taken by using mothers to use vitamin K1 in the last few weeks of pregnancy and for babies.
oxcarbazepine and active metabolites (MHD) through the placenta fence. MHD concentration in the babies and mother's plasma is equivalent in a case.
Breastfeeding period
Summary of risks
Oxacarbazepine and its active metabolites (MHD) are excreted into breast milk. The concentration of drugs in breast milk is 50% of plasma concentrations found for both substances. It is unclear the effects of children exposed to Trileptal in this path. Therefore, do not use trileptal during breastfeeding.
Drug interaction
Enzyme inhibitors
Oxcarbazepine is evaluated in human liver microsoms to determine the ability to inhibit cytochrome p450 enzymes that are responsible for the metabolism of other drugs. The results showed that oxcarbazepine and metabolic products have pharmacological activity of the drug (monohydroxy derivatives, MHD) inhibit CYP2C19. Therefore, there may be interactions when combined with high doses of trileptal with drugs metabolized by CYP2C19 (eg phenobarbital, phenytoin, see below). In some patients treated with trileptal and drugs metabolized through CYP2C19 may need to reduce the dose of combined drugs. In human liver microsom, oxcarbazepine and MHD have little or unable to work as inhibitors for the following enzymes: CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP2E1, CYP4A9 and CYP4A11.
Enzyme induction
In vitro and in vivo oxcarbazepine and MHD causing Cytochrome CYP3A4 and CYP3A5 induction are responsible for the metabolism of dihydropyridine calcium antagonists and oral contraceptives, and anti -epileptic drugs (for example, carbamazepine), resulting in reduced plasma concentration of these drugs (see below). The reduction in plasma concentration is also observed in other drugs metabolized mainly by CYP3A4 and CYP3A5, for example immunosuppressive drugs (such as ciclosporin).
in vitro, oxcarbazepine and MHD are weak induction substances UDP glucuronyl transferase and so in vivo is not sure these substances affect the effects of drugs excreted mainly by the catalytic path of UDP-Glucuronyl Transferase (for example, Valproic acid, Lamotrigine). But even if Oxcarbazepine and MHD are only UDP-glucuronyl-transferase weak induction, they still need higher doses of drugs in combination with trileptal and are metabolized through CYP3A4 or through conjugate (UDP-Glucurony-Transferase). When stopping using trileptal, it is necessary to reduce the dose of the combined drug.
Studies on enzyme induction on human liver cells have identified as oxcarbazepine and MHD are the induction substances of the isenzyme of the CYP2B and CYP3A4 feces. It is unclear the induction effect of oxcarbazepine/MHD on other ISOENZYM CYP.
Anti -epileptic drugs and enzyme induction drugs
The likely interactions between Trileptal and other anti -epileptic drugs (AED) have been assessed through clinical studies.
In Vivo, phenytoin plasma concentration increases by 40% when Trileptal is used at a dose of 1200mg/day. Therefore, when using Trileptal dose is higher than 1200mg/day during complementary treatment, phenytoin dose should be reduced. However, the increase in the level of phenobarbital is low (15%) when used with Trileptal.
Strong induction substances of cytochrome P450 enzymes or UDP glucuronyl -gansferase enzymes (e.g. rifampicin, carbamazepine, phenytoin and phenobarbital) have been seen as reducing the plasma concentration of MHD (29 - 49%). Not observed the induction of Trileptal.
Hormone contraceptives
Triileptal is seen as effective for two components, ethinylestradiol (EE) and levonorgestrel (LNG), in an oral oral contraceptive. The average AUC values of EE decreased by 48 - 52% and of LNG decreased by 32 - 52%. Studies with oral or other implant contraceptives have not been conducted. Therefore, simultaneous use of trileptal with hormone contraceptives can reduce these contraceptives.
Calcium antagonists
After simultaneous use with trileptal, the AUC values of Felodipine are reduced by 28%. However, plasma concentrations remain recommended for treatment. On the other hand, Verapamil reduces MHD's 20% plasma concentration. The decrease in this plasma concentration of MHD is not considered clinically related.
Other drug interactions
cimetidine, erythromycine and dextropropoxyphene does not affect MHD's pharmacokinetics, and viloxazine only causes minor changes to the plasma concentration of MHD (about 10% higher than simultaneously). The results with Warfarin showed no evidence of drug interactions when used once or more times with trileptal.
Cavalry
Due to the absence of studies on the cavalry of the drug, this drug should not be mixed with other drugs.
Storage
Storage below 30 ° C. Storage drugs in the packaging is intact.
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