Leracet 500mg J.URIACH medicine for convulsions (6 blisters x 10 tablets)

Dosage form Box of 6 blisters x 10 tablets
Specifications Levetiracetam

Ingredient

Composition information	Content
Levetiracetam	500mg

Uses

indications

Leracet 500 medicine is indicated in the following cases:

Use single therapeutic treatment in the treatment of local starting convulsions with or without mucous chemicals in new patients who are diagnosed with epilepsy aged 16 and older. (Juvenlie Myoclonic Epileepsy). Current anti -epileptic drugs.

Levetiracetam enhances the protection of anti -seizures in many models of local convulsions and the entire first -handedness on animals without the effect of convulsions. Initial metabolites are not active.

In humans, the drug works in both local and whole epilepsy (epilepsy/dramatic force -shaping force for light stimulation) that has affirmed the broad spectrum of the predecessor of the drug.

Mechanism of action

The mechanism of action of levetiracetam has not been fully explained. In vitro and in vivo show that levetiracetam does not change the basic properties of cells and normal neurotransmitters.

In vitro studies show that levetiracetam acts on Ca2+ concentration in nerve cells by inhibiting a part of Ca2+ and reducing Ca2+ release from reserves in nerve cells. Moreover, In vitro studies show that levetiracetam is associated with a specific location in the brain tissue of rodents. This cohesion position is 2A protein in the synap bag, which is thought to be related to the broken bag and the release of neurotransmitters. Researching stimulating sound on epilepsy mice shows that Levetiracetam has a certain affinity with 2A protein in Synap bag, corresponding to the anti -epileptic activity of the drug. This shows that the interaction between levetiracetam and 2A protein in the synap bag can contribute to the anti -epileptic mechanism of the drug.

pharmacokinetics

adults and adolescents

absorption

levetiracetam is quickly absorbed when used orally. Oral bioavailability is absolutely nearly 100%. Peak concentration in plasma (CMAX) reached 1.3 hours after drinking. Stable state is achieved after 2 days with a dose mode 2 times daily. The typical peak concentrations (CMAX) are 31 and 43 μg/ml after a single dose of 1,000 mg and after the dose repeats 1,000 mg twice daily.

distribution

There is no data distribution in human tissue. Both levetiracetam and its initial metabolites are not significantly connected to plasma proteins (

transformation

In Levetiracetam people are almost less metabolized. The main metabolic path (24% of the dose) is to hydrolyze acetamide with yeast. The isomers of cytochrome P450 liver enzymes do not participate in the original metabolism process, UCB L057. Measuring acetamide hydropicity in many tissues including blood cells. UCB L057 metabolites have no pharmacological activity.

People also identify two small metabolites. A substance obtained by hydrogen hydrolidone (1.6% of the dose) and the remaining substance obtained by opening the pyrroolidone ring (0.9% of the dose). Other unknown components account for only 0.6% of the dose.

There is no evidence of Levetiracetam's Invivo transformation and its initial metabolites.

Invitro, Levetiracetam and its initial metabolites are seen as non -inhibition of the main isomers of cytochrome P450 liver enzymes (CYP3A4, 246, 2C9, 2D6, 2E1 and 1A2), Glucuronyl Transferase (UGT1A1 and UGT1A6) and Epoxide hydroxylase processes. In addition, levetiracetam does not affect Valproic acid glucuronylation on Invitro.

In culture liver cells, levetiracetam is small or does not affect the formation of ethinylestradiol or CYP1A1/2. At high concentrations (680 μg/ml) levetiracetam causes mild irritation CYP2B6 and CYP3A4, but at concentrations close to CMAX achieved after the repeated dose of 1,500 mg twice daily, these effects are considered non -biological relevance. So levetiracetam cannot interact with other substances or vice versa.

Elimination

Semi -dumping time in humans is 7 ± 1 hour and does not change according to the dose, sugar or repeated dose. The average body clearance is 0.96 ml/min/kg.

The main elimination line is through the urine, accounting for the average 95% of the dose (about 93% of the dose is eliminated within 48 hours). Only 0.3% of the dosage excreted through feces.

In the first 48 hours, the accumulated excretion of Levetiracetam's urinary tract and its initial metabolites are 66% and 24% of the dose. The renal clearance of levetiracetam and UCB L057 corresponding to 0.6 and 4.2 ml/min/kg shows that levetiracetam excreted glomerular filtration with reabsorption in the renal tubules and shows that the initial metabolites also excreted through the active excretory through the renal tubules along with glomerular filtration. Levetiracetam elimination is correlated with creatinine clearance.

Old people

Selling time increases about 40% (10 to 11 hours) in the elderly due to renal function.

Children (4 to 12 years)

The half -life of Levetiracetam is 6 hours after taking a single dose of 20 mg/kg in children with epilepsy (4 to 12 years old). The peak concentration of plasma is observed after drinking about 0.5 - 1 hour. The peak concentration in plasma and the area below the linear and proportional curve is proportional to the dose. The sale time is about 5 hours.

kidney failure

The whole body clearance of both levetiracetam and its initial metabolites are correlated with creatinine clearance. Therefore, for patients with medium and severe renal failure, levetiracetam's daily maintenance dose is based on creatinine clearance.

In patients with end -stage renal disease, the half -life is destroyed between the separation stages and during the corresponding separation stage is about 25 and 3.1 hours. The rate of levetiracetam is 51% in a 4 -hour separation cycle.

liver failure

There is no change in pharmacokinetics of levetiracetam in patients with mild liver impairment (Child-Pugh a) and average (Child-Pugh B). In patients with severe liver failure (Child-Pugh C), the body clearance of levetiracetam is 50% compared to normal people, mainly due to reduced kidney clearance. No dose adjustment in patients with mild to moderate liver failure. In patients with severe liver failure, creatinine clearance may not fully assess the level of renal failure. Therefore, 50% of the daily maintenance dose should be discounted when the clearance of creatinine

Before taking Leracet 500mg J.URIACH medicine for convulsions (6 blisters x 10 tablets)

How to use

drink levetiracetam with sufficient amount of liquid (such as water).

Dosage

Drugs can be taken with or not with meals, daily dose is divided evenly for two drinks.

Unit of treatment

adults and teenagers aged 16 and over

Normal dose: From 1000 mg (2 tablets) to 3000 mg (6 tablets) per day.

When starting to use levetiracetam, the doctor will set the lower doses for 2 weeks before using the lowest normal dose.

Multi -therapy

adults and adolescents (12 - 17 years old) weighs 50 kg or more

Normal dose: From 1000 mg (2 tablets) to 3000 mg (6 tablets) per day.

infant (6 - 23 months), children (2 - 11 years old), adolescents (12 - 17 years old) weighing less than 50 kg

The doctor will prescribe medication suitable for age, weight and dose.

Oral solution is a form suitable for babies and children under 6 years old.

Common dose: From 20 mg/kg to 60 mg/kg of body weight per day.

babies (1 - 6 months)

Oral solution is a form suitable for babies.

Elderly (from 65 years of age)

Recommendations to adjust the dose in elderly patients with impaired renal function (see the item of patients with renal failure below).

Renal failure

Daily dose should be adjusted based on kidney function.

For adults, refer to the following table and adjust the dose as directed. To use this dose table, it is necessary to estimate creatinine clearance (CLCR) (ml/min) of the patient. It is possible to estimate the CLCR (ml/min) based on the determination of serum creatinine (mg/dl) for adults and adolescents weighing 50 kg or more according to the following formula:

CLCR (ml/min) = {[140 - age (year)] x Weight (kg)}: [72 x Creatinine serum (mg/dl)] x (0.85 for women).

Then, CLCR is adjusted according to the body surface area (BSA) as follows:

CLCR (ml/min/1.73 m2) = Clcr (ml/min): BSA (m2) x 1.73 m2.

Adjusting the dose for adults and adolescents weighing 50 kg or more is impaired kidney function:

Renal failure

Creatinine clearance

(ml/min/1.73 m2)

Dosage and number of times used 500 - 1500 mg x 2 times/day 500 - 1000 mg x 2 times/day 250 - 750 mg x 2 times/day 250 - 500 mg x 2 times/day

500 - 1000 mg x 1 time/day (2)

(2): Additional dose recommends 250 - 500 mg after the appraisal.

In children with renal failure, the dose adjustment must be based on renal function because the levetiracetam clearance is related to kidney function. This recommendation is based on research in adults with renal failure.

CLCR (ml/min/1.73 m2) can be estimated by determining the level of creatinine in serum (mg/dl) for teenagers and children according to the following formula (Schwartz formula):

CLCR (ml/min/1.73 m2) = height (cm) x ks: Creatinine concentration in serum (mg/dl).

Adjusting the dose for babies, children, teenagers weighing less than 50 kg with renal function:

Dosage and number of times used and teenagers under 50 kg 7 - 21 mg/kg x 2 times/day 10 - 30 mg/kg x 2 times/day 7 - 14 mg/kg x 2 times/day 10 - 20 mg/kg x 2 times/day

3.5 - 10.5 mg/kg x 2 times/day

5 - 15 mg/kg x 2 times/day

3.5 - 7 mg/kg x 2 times/day

5 - 10 mg/kg x 2 times/day 7 - 14 mg/kg x 1 time/day (1) (3) 10 - 20 mg/kg x 1 time/day (2) (4)

(2): The recommended attack dose is 15 mg/kg for the first day of treatment with levetiracetam.

(3): Additional dose is 3.5 - 7 mg/kg after the appraisal.

(4): Additional dose recommends 5 - 10 mg/kg after the examination

Hepatic failure

No dose adjustment in patients with mild to medium liver failure. For patients with severe liver failure, creatinine clearance may not fully assess the level of renal failure. Therefore, it is advisable to reduce the daily maintenance daily dose when creatinine clearance below 60 ml/min/1.73 m2.

Treatment time:

levetiracetam is used for a long time as directed by the doctor.

Do not stop treating with levetiracetam without a doctor's instructions because it can increase seizures.

The doctor will reduce the dose slowly if you want to stop treating with levetiracetam.

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?

symptoms

Sleep, agitation, quarrels, consciousness, depression, respiratory failure and coma have been observed in an overdose with levetiracetam.

Overdose

If an exceeding the acute dose, the stomach can be washed or vomiting. There is no specific antidote for levetiracetam. Overdose is mainly treated with symptoms and can be clinical. Separation machine efficiency is 60% for levetiracetam and 74% for the first metabolites.

In case of emergency, call the 115 emergency center immediately or go to the nearest local health station.

What to do when you forget 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double doses to compensate for missed dose.

Side Effects

When using the drug, there are common unwanted effects (ADR) such as:

The most unwanted effects are rhinitis, drowsiness, headache, fatigue and dizziness. The unwanted effects are presented below based on placebo clinical tests in all research indications with a total of 3,416 patients treated with levetiracetam. These data are added with the use of levetiracetam in the corresponding open label expansion studies as well as in experience after circulation. The unwanted effect of levetiracetam is generally similar between age groups (adults and children) and between approved epilepsy indications.

Unwanted effects are reported in clinical studies (in adults, adolescents, children and babies more than 1 month old) and from experience after circulation listed in the table below on each organ system and frequency appears. The unwanted effects are listed in the order of severe reduction and the frequency of appearance is as follows: Very common (≥1/10); Common (≥1/100 to

frequency Thraxis Translation

Hypersensitivity (including angels and anaphylaxis)

Metabolic and nutrition disorders

Anorexia weight loss, weight gain Sodium -reducing sodium blood Likes efforts to commit suicide, suicide intentions, mental disorders, abnormal behaviors, hallucinations, anger, confusion state, panic, emotional unstable/mood change, anxiety perform suicide behavior, personality disorders, abnormal thoughts The beginning convulsions, vestibular disorders, dizziness, coma, run dementia, memory impairment, abnormal coordination/loss of air conditioning, abnormalities, attention disorders

dancing - dancing, movement disorders, hyperactivity

look at a double, blurred view

Often Hepatitis, hepatitis muscle weakness, muscle pain Trauma

In some cases, hair loss can recover after stopping using levetiracetam.

Bone marrow inhibitor is determined in some cases of reduced hemorrhage.

Please inform your doctor any unwanted effects during treatment.

Instructions on how to handle ADR:

Notify the physician with unwanted effects when using the drug.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

contraindicated

Leracet 500 drug contraindicated in the following cases:

Hypersensitivity to levetiracetam, any pyrrolidon derivative, or any ingredient of
.

Be cautious when using

Please see more information about the drug in the instruction sheet of the use of the drug attached.

Caution in children.

According to the current clinical practice, if you have to stop treating with levetiracetam, you must gradually reduce the dose (for example, in adults: decrease 500 mg twice daily for every two or four weeks; in children, do not reduce the dose of more than 100 mg/kg twice daily for every two weeks).

Adjust the dose when using levetiracetam for patients with renal failure. For patients with severe liver failure, kidney function should be assessed before choosing the dose.

There have been reports on suicide, trying to commit suicide and intending to commit suicide in patients treated with levetiracetam. It is necessary to advise patients to immediately notify any symptoms of depression and/or suicide intentions to the treating doctor.

The effect of the drug on the ability to drive and operate machinery

Due to the sensitivity of each individual may vary, some patients may be sleepy or have other symptoms related to the central nervous system at the time of starting or after increased dose. So be cautious when driving or operating machinery.

Use drugs for women during pregnancy and lactation

No even though data on the use of levetiracetam in pregnant women. Animal studies have shown drugs that cause reproductive toxicity. People do not know the potential risk to humans. Levetiracetam should not be used during pregnancy unless necessary.

Like other anti -epileptic drugs, physiological changes during pregnancy can affect levetiracetam concentration. There has been a report on reducing levetiracetam concentration during pregnancy.

levetiracetam is known to go through human milk, so do not breastfeed when using levetiracetam. However, if Levetiracetam is necessary to be used in nursing women, it is necessary to consider the benefits/risks, consider the importance of breastfeeding.

Interactive drug

Please inform your doctor or pharmacist about the medications that you have or are taking recently, including over -the -counter drugs.

levetiracetam can be taken during or outside meals. Do not use alcoholic foods or drinks during treatment with levetiracetam.

Data shows that Levetiracetam does not affect the serum concentration of current anti -epileptic drugs (Phenytoin, Carbamazepine, Valproic, Phenobarbital, Lamotrigine, Gabapentine and Primidone) and these anti -seizures also do not affect the dynamics of levetiracetam.

Levetiracetam's clearance in children using anti -epileptic drugs irritated enamel is 22% higher than they do not use. However, the dose adjustment is not recommended. Levetiracetam does not affect the plasma concentrations of carbamazepine, valproate, topiramate or lamotrigine.

Probenecid (dose of 500 mg four times daily), an excreted inhibitor in the renal tubules, showing the inhibition of the kidney removal mode of the initial metabolic substance but does not inhibit the kidney clearance of levetiracetam. However, the concentration of this metabolite remains low. It is thought that other drugs excreted by active excretion through the renal tubules can also reduce the kidney clearance of metabolites. The impact of levetiracetam on probenecid has not been studied and does not know the effects of levetiracetam on other active excreted drugs, such as non-mineroid anti-inflammatory drugs (NSAIDs), sulfonamide and methotrexate.

Levetiracetam dose 1000 mg daily does not affect the pharmacokinetics of oral contraceptives (Ethinyl estradiol and levonorgestrel) and endocrine parameters (LH and Progesterone) are not changed. Levetiracetam dose of 2000 mg daily does not affect Digoxin's pharmacokinetics, oral contraceptives and warfarin does not affect levetiracetam pharmacokinetics.

There is no data on the effects of antacids on the absorption of levetiracetam not affected by food but the absorption rate is slightly reduced.

There is no data on drug interaction between levetiracetam and alcoholic beverages.

Storage

Store at a temperature not exceeding 30 ° C, avoiding light.

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