Tegretol 200 Novartis treatment for epilepsy (5 blisters x 10 tablets)
Dosage form Box of 5 blisters x 10 tablets
Specifications Carbamazepine
Ingredient
| Composition information | Content |
| Carbamazepine | 200mg |
Uses
Indication
Tegretol is indicated in the following cases:
The mechanism of action of carbamazepine - the active ingredient of Tegretol, is only partially explained. Carbamazepine stabilizes the nerve membrane that is too irritated, inhibits the discharge of nerve cells repeated and reduces the spread of excessive impulses through synap. It is thought that the prevention of the repetition of the potential of sodium dependence in nerve cells is reduced through sodium channel blockers depending on the use and on the voltage may be the main mechanism of action of the drug.
While a decrease in glutamate release and stability of nerve cell membrane can be explained mainly for anti -epileptic effects, carbamazepine anti -epilepsy properties may be due to the effect of reducing the rotation of dopamine and noradrenalin.
As an anti-epileptic drug, its activity spectrum includes: Local seizures (simple and complex), with or not developing the whole whole secondary, spastic spastic seizure-shaking seizure, as well as a combination of these types of epilepsy.
In clinical studies, Tegretol is used in the form of single therapy for patients with epilepsy - especially children and teenagers - have been reported mentally -oriented, including positive effects on anxiety and depression symptoms as well as reducing irritability and aggression.
In some studies, the effects are uncertain or have no effect on awareness and mental manifestation, depending on the dose, which has been reported. In other studies, observed the effect of beneficial to attention, perception/memory.
As a mental medicine, Tegretol has a clinical effect in some neurological disorders, such as preventing dramatic pain in spontaneous and secondary nerve pain. In addition, the drug is also used to relieve neurological pain in different conditions, including tabet disease, abnormalities after injury and nerve pain after herpes infection.
In alcoholic syndrome, drugs reduce seizures and improve symptoms caused by alcohol (for example: too agitated, tremor, weak gait). In the central pale diabetes, Tegretol reduces urine volume and reduces thirst.
As a mental medicine, Tegretol has proved clinical effects in emotional disorders, that is, treatment of acute manic attacks as well as treatment of bipolar emotional disorders (emotional-sympathetic), when used in a single therapy or combined with sedatives, antidepressants, or lithiums, in stimulant arthritis and other stimulating drugs and in other stages of acidity, in the form of stimulating drugs Relapse in fast cycle.
Pharmacokinetics
absorption
Carbamazepine tablets are absorbed almost completely but relatively slow. Conventional tablets have an unchanged plasma concentration within 12 hours and 6 hours after taking oral doses according to the corresponding appropriate. About the active ingredient is absorbed, there is no clinical difference between oral dosage forms. After taking a single dose of 400 mg of carbamazepine (tablets), the peak concentration of carbamazepine does not change in plasma about 4.5 micrograms/ml.
Carbamazepine concentration in plasma in a stable state is achieved within 1-2 weeks, depending on the induction of carbamazepine in each individual and inductive in different individuals due to enzyme induction drugs, as well as depending on the condition before treatment, dosage and treatment time.
Carbamazepine concentration in plasma in a stable state is considered a "concentration of treatment" that changes significantly between patients. For most patients, the concentration of 4 - 12 micrograms/ml corresponds to 17 - 50 micromol/liter is reported. Carbamazepine-10, 11-Epoxid concentration (pharmacological metabolites): about 30% of carbamazepine concentration.
Use food does not significantly affect the speed and level of absorption, regardless of Tegretol's preparation.
Distribution
carbamazepine passes through the placenta.
Carbamazepine is connected to serum protein at 70 - 80%. The concentration of the substance does not change in the cerebrospinal fluid and saliva reflects the unite with protein in plasma (20 - 30%). The concentration in breast milk is found to be equivalent to 25-60% of the corresponding concentration in plasma.
Metabolism
Carbamazepine is metabolized in the liver, where Epoxid biological changes are the most important sugar, creating 10.11-transdiol and glucuronide derivatives are the main metabolites. Cytochrom P4503A4 has been identified as the main form of homogeneity responsible for the formation of carbamazepine-10.11 epoxid with pharmacological activity from carbamazepine. 9-Hydroxy-Methyl-10-Cabamoyl Acridan is a small metabolic associated with this line.
After taking a single dose of carbamazepine, about 30% of the drug appears in the urine in the form of the final products via Epoxid. Other important biological changes for carbamazepine leads to various types of monohydroxylation compounds, as well as for carbamazepine n-glucuronids created by UGT2B7.
Elimination
The waste time of carbamazepine is constant on average about 36 hours after taking a single dose. While repeated, on average, only 16 - 24 hours (the induction of the mono -oxygenase system in the liver), depending on the time of drug use. In patients being treated simultaneously with other liver enzyme induction drugs (for example, phenytoin, phenobarbiton), have recorded the average selling time of waste time from 9 -10 hours.
The average selling time of metabolites 10, 11-Epoxid in plasma is about 6 hours after taking oral doses itself.
After taking a single dose of carbamazepine 400 mg, 72% the dose is excreted in urine and 28% in feces. In urine, about 2% of this dose is restored in the form of unchanged drugs and about 1% in the metabolic 10, 11-Epoxid has pharmacological activity.
Before taking Tegretol 200 Novartis treatment for epilepsy (5 blisters x 10 tablets)
How to use
tablets can be taken while eating, after eating or between meals. Should use tablets with some drinks and the rest of the chewing tablet should be swallowed with some drinks.
Dosage
When possible, Tegretol should be prescribed in single therapy. Should start treatment at low doses every day, increase slowly until the optimal effect.
Should adjust the carbamazepine dose according to the needs of each patient to achieve full control of seizures. Determining the plasma concentration can help determine the optimal dose. In the treatment of epilepsy, carbamazepine dose usually requires total carbamazepine levels in plasma about 4 - 12 micrograms/ml (17 - 50 micromol/liter).
When adding Tegretol to the anti -epilepsy treatment, should be done slowly during maintenance, or if necessary, adjust the dose of other anti -epileptic drugs.
Adults
epilepsy
Starting 100 mg to 200 mg, 1 time or 2 times/day. Should increase the dose slowly - generally at 400 mg, 2-3 times/day until the metal response is achieved. In some patients, the dose of 1600 mg or even 2000 mg/day may be appropriate.
Acute and sustainable revival and treatment of bipolar emotional disorders
The dose level: about 400 - 1600 mg/day, the usual dose is 400 - 600 mg/day divided into 2-3 times. During the acute mania, it is advisable to increase the dose quite quickly, while the recommendation of each small dose increases in the treatment of bipolar disorders to ensure optimal tolerance.
Pain of the nerves
The starting dose of 200 - 400 mg should increase slowly every day until the pain is over (usually 200 mg, 3-4 times/day). Then reduce the dose gradually to the lowest maintenance dose possible. The maximum dose recommended is 1200 mg/day. When analgesic is achieved, try to stop treating gradually, until another pain occurs.
kidney failure/liver failure
There is currently no carbamazepine pharmacokinetic data in patients with liver function or renal function.
Children/children and teenagers
epilepsy
For children 4 years of age and less, recommend the starting dose of 20 - 60 mg/day, increasing to every 20 mg to 60 mg, every 2 days. For children over 4 years old, can start treatment with 100 mg/day, increasing to 100 mg each week.
Maintenance dose: 10 - 20 mg/kg body weight/day divided into several times, for example:
Pain of the nerves
Due to the various anti -epileptic drug and pharmacokinetics, need to be cautious when choosing Tegretol dose for elderly patients.
In elderly patients, it is recommended to start the starting dose of 100 mg, 2 times/day. The starting dose of 100 mg, 2 times/day should slowly increase each day until the pain is over (usually 200 mg, 3-4 times/day). After that, the dose should be gradually reduced to the lowest maintenance dose possible. The maximum dose recommended is 1200 mg/day. When analgesic is achieved, try to stop treating gradually, until another pain occurs.
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?
Central nervous system
Central nervous system depression, loss of orientation, level of consciousness, drowsiness, agitation, hallucinations, coma, blurred vision, stuttering, speech, vibration of eyeball, loss of air conditioning, movement disorders, initial reflexes and then reducing reflexes, seizures, mental disorders, muscle vibration, reducing body temperature, omnipriotic relaxation.
Respiratory system
Respiratory failure, pulmonary edema.
cardiovascular system
Tachycardia, hypotension, occasional hypertension, transmission disorders with wide QRS complex, fainting with cardiac arrest.
digestive system
vomiting, slow empty stomach, reducing intestinal motility.
Muscle system
There have been some cases of muscle patterns that have been reported related to carbamazepine poisoning.
Kidney function
Urinary retention, urinary or olower, fluid, water poisoning due to the anti -urinary hormone (ADH) of carbamazepine.
Test results
Hypoglycatrological, can be metabolic, may have hyperglycemia, hypertreatin phosphokinase.
Treatment
No specific antidote.
It is necessary to handle the patient's clinical condition; hospitalized. Measure drug concentration in plasma to confirm carbamazepine poisoning and verify the overdose level.
Gastrointestinal lavage and active carbon. The delay in gastric lavage can delay the absorption, leading to recurrence while recovering from poisoning. Medical care supports at active treatment units, heart monitoring and careful adjustment of electrolyte imbalance.
Special recommendations
Recommended removing toxins from blood by activated carbon. Hemolysis is an effective treatment for carbamazepine overdose.
It is necessary to predict the recurrence and aggravation of symptoms on the 2nd and 3rd day after an overdose due to delayed absorption.
In an emergency, call the 115 emergency center immediately or go to the nearest local health station.
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
Common, ADR> 1/100
Endocrine system: edema, fluid fluid, weight gain, hypoglycemia and blood permeability reduction due to anti -urinary hormone (ADH) leading to attached water poisoning, sleeping, vomiting, headache, confusion, neurological disorders.
Digestive system: Nausea, vomiting, dry mouth, rectal stimulation. Skin and subcutaneous tissue: urticaria, Allergic dermatitis . Uncommon, 1/1000 Rare ADR The immune system: multi -organ sealing disorders with fever, rash, vasculitis, lymphoma, joint pain, enlarged spleen, abnormal liver function tests, bile duct syndrome disappearing; Anaphylactic reaction, angioedema, reducing blood gamma blood. Nervous system: movement disorders, eye movement disorders, pronunciation, dance, peripheral neuropathy, abnormal, mild paralysis, malignant syndrome caused by mental drugs, sterile meningitis with muscle vibration, taste disorders. Cardiovascular: heart disease disorders, arrhythmia, atrioventricular block, slow heart rate, coronary artery disease; Increase or lower blood pressure, circulation, embolism. Digestive system: abdominal pain, pancreatitis, tongitis, stomatitis. Bile liver system: cholestatic hepatitis, jaundice, liver failure, granular liver disease. Skin and subcutaneous tissue: Lupus erythematosus, itching, Stevens-Johnson syndrome, poisoned epidermal necrosis, light sensitivity, skin erythema, pigmentation, acne, hair loss, hip. Muscle system: muscle weakness, bone metabolism disorders, bone puree, joint pain, muscle pain, muscle spasm. Reproduction system: Sexual dysfunction, erectile dysfunction, sperm abnormalities. Testing: increased pressure in the eye, hypercholesterolemia, lipoprotein, hypermagic hormone, prolactin. Not determined frequency Other: Activating herpes 6 virus in humans. 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
contraindicated
Tegretol drug contraindicated in the following cases:
Be cautious when using
should only use Tegretol under medical supervision. Tegretol should only be prescribed after assessing the benefits and risks and under close monitoring of patients with a history of heart, liver or kidney damage, there are side hematological reactions for other drugs, or interrupted Tegretol treatment.
Hematology effects
A blood cell and anemia loss are associated with Tegretol, but due to the low rate of these conditions, it is difficult to estimate the risk of significance to Tegretol. The common risk among untreated patients is generally estimated to be 4.7/1,000,000/year for grain leukemia and 2 people/1,000,000/year for prolifer anemia.
Reduce the number of platelets or temporary or prolonged white blood cells from occasional to frequent relevance to the use of Tegretol. However, in most cases, these effects are transient and not necessarily a sign of anemia onstrumental anemia or grain leukemia. However, it is necessary to count the total amount of blood cells, including platelets before treatment (and maybe both red blood cells and serum iron) at first and periodically.
If the number of white blood cells or platelets is clear or clearly reduced during the treatment period, the patient closely monitor and count the whole blood cell. Tegretol must be stopped if there are any signs of bone marrow failure.
Patients should be notified of early signs and symptoms of hematological problems that may occur, as well as symptoms of skin reactions or liver reactions. If there are reactions such as fever, sore throat, rash, mouth ulcer, easily bruised, hemorrhagic spots or hemorrhage, patients should come to consult the doctor immediately.
Serious skin reaction
Serious skin reactions, including poisoned epidermal necrosis (ten, also known as Lyell syndrome) and Stevens-Johnson syndrome (SJS) have been reported very rare to Tegretol. Patients with serious skin reactions may be hospitalized, as these conditions may be life -threatening and may cause death.
Most cases of Stevens-Johnson syndrome/poisoning epidermal necrosis (SJS/Ten) appear in the first few months of Tegretol treatment. These reactions are estimated to occur at 1 - 6/10,000 new users in countries with the most populated population. If the signs and symptoms suggest serious skin reactions (for example, Stevens-Johnson syndrome, lyell syndrome/poisoned epidermal syndrome), Tegretol should be stopped immediately and should be considered for alternative treatment.
Pharmacogenomics
There is an increasing evidence of the role of various Alleles of white blood cell antigen (HLA) that makes patients more susceptible to adverse immunity reactions.
Related to HLA-B*1502
Determining the people with Allele HLA-B*1502 and avoiding carbamazepine treatment in these people has been shown to reduce the rate of stevens-johnson syndrome/poisoned epidermal necrosis caused by carbamazepine.
Related to HLA-A*3101
Should consider the presence of Allele HLA-A*3101 in patients with ancestors in the population groups at genetics (for example, patients of Japanese population and whites, patients of native American population groups, Spanish and Portuguese population groups, southern Indians and Arabic people before starting with tegretol (viewing information for medical information. Here).
Avoid using Tegretol for patients to detect positive for HLA-A*3101 unless the benefits are significantly higher than the risk. In general, it is not recommended for anyone who is currently using Tegretol because of the risk of Stevens-Johnson syndrome/poisoning epidermal necrosis limited to the first few months of treatment, regardless of HLA-A*3101.
Information for medical staff
If tested for the presence of Allele HLA-B*1502, recommends "determining HLA-B*1502 Genotype" with high resolution. The test is positive if one or two Allele HLA-B*1502 and the test are negative if not discovered Allele HLA-B*1502.
Similarly, if the test is performed on the presence of Allele HLA-A*3101, it is recommended "determining the HLA-A*3101 genotype" with the corresponding high resolution. Testing is positive if one or two Allele HLA- A*3101 and the test is negative if the Allele HLA- A*3101 is not detected.
Other skin reactions
Light skin reactions such as scattered skin rash or burning skin are also possible, most of them are transient and not dangerous. These reactions disappear within a few days or weeks or during continuous treatment or after decreased dose. However, because it may be difficult to distinguish early signs of skin reactions more seriously with mild reactions, patients need to be closely monitored and consider stopping the drug immediately if the reaction is worse when continuing to use the drug.
Allele HLA-A*3101 is found associated with adverse skin reactions less serious by using carbamazepine and may predict the risk of these reactions due to carbamazepine such as hypersensitivity syndrome due to anti-convulsions or non-serious rashes (lumpy rash). However, Allele HLA-B*1502 must not be found for the risk of the above skin reactions.
hypersensitivity
Tegretol can cause hypersensitivity reactions including rashes due to eosin medications and generalized symptoms (dress), dyserty disorders with fever, rash, vascular inflammation, lymph node disease, lymphoma, arthritis, leukopenia, Eosin hyperthermonary hypercasses, enlarged liver, abnormal liver function and loss of bile ducts. out in many different combinations of drugs. Other organs may also be affected (for example, lungs, kidneys, pancreas, heart muscle, colon) (see the unwanted effect).
Allele HLA-A*3101 has been found associated with the appearance of hypersensitivity syndrome, including lumpy rash.
It is necessary to notify patients with hypersensitivity reactions to carbamazepine that about 25-30% of these patients may have hypersensitivity reactions to oxcarbazepine (trileptal).
Cross -hypersensitivity can occur between carbamazepine and anti -epileptic drugs (such as phenytoin, primidone and phenobarbital).
In general, if the signs and symptoms suggest the hypersensitivity reaction, the towerol must be stopped immediately.
epilepsy
Be careful when taking Tegretol for patients with mixed seizures including absent consciousness, typical or not typical. In all this situation, Tegretol can make seizures worse. In case of severe seizures, Tegretol must be stopped.
There may be an increase in the frequency of epilepsy while changing from oral formula to ammunition.
Liver function
Must conduct a liver function evaluation at the beginning of treatment and periodically during Tegretol's treatment, especially in patients with a history of liver disease and in elderly patients. Must stop the drug in the case of more severe liver dysfunction or progressive liver disease.
Kidney function
Recommendation for total urine analysis and blood urea nitrogen test (bun) at the beginning of treatment and periodically.
Hemorrhage reduction
Hemorrhage reduction has been known to carbamazepine. In patients with previous kidney conditions associated with low sodium or patients treated simultaneously with drugs that reduce sodium (for example, diuretics, drugs associated with anti -urinary hormones (ADH) are inappropriate), sodium concentration should be measured before the start of carbamazepine treatment. After that, sodium concentration should be measured after about 2 weeks and then at the distance of each month for the first 3 months of the course or according to clinical needs. In particular, these risk factors can occur for elderly patients. If observations are reduced in sodium blood, water restriction is an important measure if clinically indicated.
thyroid disabilities
Carbamazepine can reduce serum thyroid hormone levels through enzyme induction, which may need to increase the dose of thyroid hormone replacement therapy in patients with thyroid disabilities. Therefore, monitoring the proposed thyroid function to adjust the dose of thyroid hormone replacement therapy.
anti -cholinergic effect
Tegretol shows light anti -anti -cholinergic activity. Therefore, patients with intraocular pressure increased and urinary retention should be closely monitored during treatment.
Mental effects
It should be noted that the ability to activate potential mental disorders and in the elderly patients is confused and agitated.
suicide thoughts and suicide behavior
There have been reports on suicide thoughts and suicide behaviors in patients treated with anti -epileptic drugs in some indications. A comprehensive analysis of random tests that are controlled to the placebo of anti -epileptic drugs has shown a slight increase in the risk of suicide thoughts and suicide behavior. The mechanism of this risk is unknown.
Therefore, it is necessary to monitor patients on signs of suicide thoughts and suicide behavior and should consider appropriate treatment. Advice patients (and patient care) to consult medical advice if suicidal thoughts or suicide behavior.
Pregnant women and women have the ability to reproduce
Carbamazepine may be related to fetal damage when used in pregnant women. Tegretol should only be used during pregnancy if the benefits are higher than possible.
Should fully advise all pregnant women and women who have the ability to reproduce about the risks related to pregnant women because of the risk of teratogenic fetus.
Women have the ability to reproduce should use effective contraception during treatment with carbamazepine and two weeks after the last dose of treatment.
Hormonal effects
Bleeding between cycles has been reported in women using Tegretol while taking hormonal contraceptives. The reliability of hormone contraceptives can be adversely affected by Tegretol. Pregnant women should be recommended to consider using other forms of contraception while using Tegretol.
Monitor plasma concentrations
Although the correlation between the dose and carbamazepine levels in plasma and between plasma concentrations and clinical effects or tolerance are slightly, monitoring of plasma concentrations can be helpful in the following cases: Sudden increase in epilepsy frequency/check the patient's compliance during pregnancy; When treating children or teenagers; suspect absorption disorders; Suspecting poisoning when taking more than one drug.
Effects when reducing the dose and stopping the drug
Sudden stopping Tegretol can start the seizure, so it is necessary to stop the drug gradually for 6 months. If you have to stop Tegretol suddenly in patients with epilepsy, switching to a new anti -epileptic compound should be done with a suitable drug.
Drug interaction
Concentric use CYP3A4 inhibitors or epoxid hydrolase inhibitors with carbamazepine can cause adverse reactions (increasing carbamazepine concentration or carbamazepine-10.11 epoxid in plasma in the corresponding sense). Tegretol dose should be adjusted accordingly and/or track plasma concentrations.
Concentrated use of CYP3A4 induction drugs with carbamazepine may reduce carbamazepine levels in plasma and its treatment effect, while stopping the use of CYP3A4 induction drugs may increase carbamazepine levels in plasma. Tegretol dose may be adjusted.
Carbamazepine is a strong CYP3A4 induction drug and other and II phase II enzyme systems in the liver. Therefore, it may reduce the plasma concentration of medications that are simultaneously metabolized mainly by CYP3A4 by sensing the metabolism of these drugs.
contraceptive
Women have the ability to reproduce should use effective contraception during treatment with Tegretol and two weeks after using the final dose. Due to enzyme induction, Tegretol can lead to loss of treatment effects of oral contraceptives containing estrogen and/or progesterone. Therefore, women should recommend that pregnant women use other contraceptive methods while being treated with Tegretol.
Infertility
There have been reports of very rare cases of fertility impairment in men and/or abnormal sperm.
falls
Tegretol treatment is associated with insomnia, dizziness, drowsiness, hypotension, depression, sedation that can lead to falling and thus causing fractures or other injuries. For patients who are ill, weak health, or using drugs that can worsen these effects, should consider periodically assess the risk of adequate falls for patients with long -term Tegretol treatments
The ability to drive and operate machinery
The patient's reaction ability may be reduced due to the condition leading to seizures and adverse reactions including dizziness, drowsiness, loss of air conditioning, but reduced regulation and blurred vision that has been reported to Tegretol, especially at the beginning of treatment or associated with dosage. Therefore, patients need to be careful when driving or operating machinery.
Pregnancy
Children of mothers with epilepsy have been known to have developing disorders, including deformities. Despite the lack of decisive evidence from controlled studies with carbamazepine treatments, there have been reports on developmental and deformities, including vertebra cracking and other birth defects, such as facial skull defects, cardiovascular defects, low urinary tract defects and defects including different organ systems that have been reported related to the use of Tegretol.
Need to pay attention to the following:
In women who are likely to become pregnant, whenever possible, Tegretol prescription should be prescribed in the form of single therapy, because the rate of birth defects in the children of women who are treated combined with anti -epileptic drugs is higher than in the children of women who are used separately in the form of single therapy. The risk of deformities after using carbamazepine in the form of therapeutic therapy may vary depending on the specific drugs used and may be higher in the form of multi -therapy combination including valproate.
Monitor and Prevention
Folic acid deficiency has been known during pregnancy. There have been reports that anti -epileptic drugs worsen folic acid deficiency. This deficiency can contribute to increasing the rate of birth defects in children of epilepsy women treated. Therefore, it is recommended to supplement folic acid before and during pregnancy.
In newborns
To prevent bleeding disorders in the baby, there is also recommendations to use vitamin K1 for mothers in the last weeks of pregnancy as well as for babies.
There have been several cases of convulsions in infants and/or respiratory failure related to the mother using Tegretol and other anti -epileptic drugs at the same time. A few cases of vomiting, diarrhea and/or reducing breastfeeding in newborns have also been reported related to the mother using Tegretol. These reactions can represent drug suspension syndrome in infants.
breastfeeding period
carbamazepine enters breast milk (about 25-60% of plasma concentrations). It is necessary to consider the benefits of breastfeeding compared to the possibility of having negative adverse effects for children. Mothers who are using Tegretol can be breastfeeding, as long as they are monitored with the adverse reactions that may have (for example, excessive sleep, skin allergic reactions).
There have been a number of reports on cholestatic hepatitis in newborn babies exposed to carbamazepine during before birth and/or during breastfeeding. Therefore, breastfed babies of mothers treated with carbamazepine must be carefully monitored for the disadvantaged effects on the liver.
Medicinal interaction
Cytochrome P450 3A4 (CYP3A4) is the main enzyme that catalyzes the formation of carbamazepine-10,11-Epoxid metabolites. Concentrated with CYP3A4 inhibitors can lead to increased carbamazepine levels in plasma, which can cause adverse reactions. Concentrated with CYP3A4 induction drugs can increase the speed of carbamazepine metabolism, thus leading to the ability to reduce carbamazepine levels in serum and reduce the effectiveness of treatment. Similarly, stop taking CYP3A4 induction drugs may reduce the rate of carbamazepine metabolism leading to increased carbamazepine levels in plasma.
Carbamazepine is a strong CYP3A4 induction drug and other enzyme system I and II in the liver, so it can reduce the concentration of plasma of the drugs used simultaneously metabolized mainly by CYP3A4 due to their metabolism.
Epoxid hydrolase in Microsom Human has been identified as enzyme responsible for the formation of 10.11-transdiol derivative from carbamazepine-10.11 epoxid. Concentrated with Epoxid Hydrolase inhibitors in Microsom Humans can lead to increased carbamazepine-10.11 epoxid levels in plasma.
Interactions lead to contraindications
Contraindicated using Tegretol in combination with monoamine-oidase inhibitors (MA MAI). Before using Tegretol, it is necessary to stop the Mao inhibitors for at least 2 weeks or longer if the clinical condition allows.
Drugs can increase carbamazepine levels in plasma
Because carbamazepine concentration in plasma can lead to adverse reactions (for example: dizziness, drowsiness, loss of air conditioning, but need to adjust the towerol dose accordingly and/or monitor plasma concentrations when used simultaneously with the substances described below:
The drugs may increase the concentration of metabolic metabolites with carbamazepine-10.11-Epoxid in plasma
Because the increase in carbamazepin-10,11-epoxid in plasma can lead to adverse reactions (for example: dizziness, drowsiness, loss of air conditioning, but need to adjust the towerol dose to match and/or monitor plasma concentrations when used simultaneously with the following substances: Loxapine, Quetiapine, Primidone, Progabide, Progabide, Valproic acid, Valnoctam acid and Valnoctam acid Valpromide.
Drugs can reduce carbamazepine levels in plasma
Tegretol dose may have to be adjusted when used simultaneously with the substances described below:
The effect of tegretol on plasma concentrations of medications simultaneously
Carbamazepine may reduce plasma concentrations, or even lose the activity of some drugs. May need to adjust the dose of the following drugs according to clinical requirements:
Anti -inflammatory, anti -inflammatory: buprenorphine, methadone, paracetamol (long -term use of carbamazepine and paracetamol (acetaminophen) may be associated with toxicity to the liver), phenazone (antipipin), tramadol.
Antibiotics: doxycyclin, rifabutin.
Anticoagulants: Oral anticoagulants (for example: Warfarin, Phenprocoumon, Dicoumarol, Acenocoumarol, Rivaroxaban, Dabigatran, Apixaban, Edoxaban).
Antidepressants: Bupropion, Citalopram, Mianserin, Nefazodone, Sertraline, Trazodone, 3 -round antidepressants (e.
anti -vomiting drugs :prepitant.
Anti -epileptic drugs: Clobazam, Clonazepam, Ethosuximide, Felbamate, Lamotrigine, Eslicarbazepine, Oxcarbazepine, Primidone, Tiagabine, Topiramate, Valproic Acid, Zonisamide. To avoid phenytoin poisoning and carbamazepine levels below the treatment level, it is recommended to adjust the phenytoin concentration in plasma and 13 micrograms/ml before using more carbamazepine to the treatment. There have been rare reports on increased mephenytoin levels in plasma.
antifungal drugs: Itraconazole, Voriconazole. Alternative anti -epileptic drugs can be recommended in patients treated with voriconazole or iTraconazole.
Worms: Praziquantel, Albendazole.
Tan Sinh anti -tumor drugs: Imatinib, cyclophosphamid, lapatinib, temsirolimus.
Anti -psychotic drugs: Clozapine, Haloperidol and Bromperidol, olanzapine, Quetiapine, Risperidone, Ziprasidone, Aripiprazole, Paliperidone.
Anti -viral drugs: Protease inhibitors to treat viruses that cause immunodeficiency in humans (HIV) (for example: indinavir, ritonavir, saquinavir).
Anti -anxiety drugs: Alprazolam, Midazolam.
Bronchodilators or asthma treatment: Theophylline.
contraceptive pills: Hormone contraceptives (should be considered for replacement contraceptives).
Cardiovascular treatment: Calcium channel blockers (dihydropyridin), for example: Felodipine, digoxin, simvastatin, Atorvastatin, Lovastatin, Cerivastatin, Ivabradine.
corticosteroid: corticosteroids (for example: prednisolone, dexamethasone).
drugs used in erection dysfunction: Tadalafil.
Immunosuppressive drugs: Ciclosporin, Everolimus, Tacrolimus, Sirolimus.
thyroid drug: levothyroxine.
Other interactions: products containing estrogen and/or progesterone.
The combinations need to consider
There have been simultaneous reports on carbamazepine and levetiracetam increasing caretal toxicity.
There have been simultaneous use of carbamazepine and isoniazid that increases the toxicity of the liver due to isoniazid.
Use a combination of carbamazepine with lithium or metoclopramid, and use a combination of carbamazepine with sedative (haloperidole, thioridazine) that can lead to increased neurological adverse reactions (for the combination of drugs even only "concentrations at the level of treatment in plasma").
Simultaneous use of Tegretol and some diuretics (hydrochlorothiazid, Furosemid) can lead to symptomic sodium loss.
Carbamazepine may oppose the effect of non -reducing muscle relaxants (eg pancuronium). It may be necessary to increase the dose of these drugs and should closely monitor patients to recover from nervous closing faster than expected.
carbamazepine, like other mental activity drugs, can reduce alcohol intolerance. Therefore, it is advisable to advise patients to abstain from alcohol.
Concomplifying the simultaneous use of carbamazepine with direct oral anticoagulants (Rivaroxaban, Dabigatran, Apixaban, and Edoxaban) can lead to reduced plasma concentrations of oral anticoagulants directly acting, causing risk of blood clotting. Therefore, if it is necessary to use the drug simultaneously, it is recommended to monitor the signs and symptoms of blood clotting.
Interpretation of seral tests
Due to the intervention, carbamazepine can lead to false posphenazin concentrations in analysis by high -performance liquid chromatography (HPLC).
Carbamazepine and metabolic 10.11-Epoxid can lead to false 3-round antidepressant concentration in polarized fluorescent immune testing method.
Storage
Store at temperatures not exceeding 30 ° C.
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