Huether-25 Davipharm medicine treats epilepsy, convulsions, prevention of migraine (6 blisters x 10 tablets)

Pharmacological group: anti -epileptic drugs, anti -epileptic preparations, other migraine treatment.

Topiramat is a sulfamat derivative of monosaccarid. The exact mechanism of anti -seizures and migraine prevention of Topiramat is still unknown. Research on physiological and biochemistry on cultured nerve cells has identified three properties that can contribute to the anti -epileptic effect of Topiramat.

The repetitive activity is due to the extended reduction of neurons blocked by Topiramat in a time -dependent way, causing sodium channel blockers depending on the state. Topiramat increases the frequency of Y-AminobutyRat (GABA) activating GABAA receptors and increases the possibility of GABA causing the chloride iona line into Neuron, showing that Topiramat increases the activity of neurotransmitters that have this inhibitory effect.

Because of the anti -epileptic properties of Topiramat is noticeably different from benzodiazepin, the drug can moderate the Gabaa receptor group that is not sensitive to benzodiazepine. Topiramat antagonists the effect of kainat causing kainat/ ampa group (A-amino-3-hydroxy-5-methylisoxazol-4propionic acid) of amino acid receptor has a stimulating effect (glutamate), but does not affect the activity of N-Methyl-D-Aspartat (NMDA) in NMDA receptor groups. These effects of Topiramat depend on the concentration of about 1 - 200 μm, with the minimum effect of 1 - 10 μm.

In addition, Topiramat inhibits some isoenzymes of anhydrase carbonic. This pharmacological effect is much weaker than acetazolamid, an anhydrase carbonic inhibitor and is said to not contribute much to the anti -epileptic effect of Topiramat.

pharmacokinetics

Compared to other anti -epileptic drugs, Topiramat's pharmacokinetics has a long time of selling plasma, linear pharmacokinetics, clearly cleared through the kidneys, not significantly linked to protein and lack of active metabolites.

Topiramat does not touch the metabolic enzyme, can be used or without food, and no need to monitor topiramat concentration in plasma regularly. In clinical research, there is no relationship between plasma concentrations and efficiency or unwanted effects.

absorption:

Topiramat is absorbed quickly and strongly. After taking 100 mg Topiramate in healthy people, the peak concentration (cmax) in plasma is 1.5 μg/ ml achieved within 2-3 hours (TMAX).Based on the amount of radioactive isotopes recovered in urine, the percentage of drugs absorbed when taking 100 mg Topiramat marks 14C at least 81%. The effect of food on bioavailability is not significant clinical significance.

Distribution:

In general, 13 - 17% Topiramat is connected to plasma proteins. The ability to bind to low red blood cells and saturated on plasma concentrations 4 μg/ ml. The integral distribution is inversely proportional to the dose. The average indicator distribution is 0.80 - 0.55 l/ kg with a dose of 100 - 1200 mg. The distribution volume is affected by gender, values ​​in women is about 50% in men, due to the higher rate of fat in the female body and does not cause clinical effects.

Metabolism:

Topiramat is not much metabolized (20%) in healthy volunteers. The drug is metabolized up to 50% in patients with anti -epileptic drugs that touch drug metabolic enzymes. There are six metabolites formed by hydroxylation, hydrolysis and glucuronid, which have been isolated, described and qualitated from plasma, urine and manure.

Each metabolic account accounts for

Era:

In humans, the main elimination line of Topiramat is constant and metabolic is through the kidney (at least 81% of the dose). About 66% of Topiramat dose marked 14C eliminated in the form of unchanged urine within 4 days. After using Topiramat 50 mg and 100 mg x 2 times/ day, the renal clearance is about 18 ml/ min and 17 ml/ min. There is evidence of the reabsorption in the renal tubules. Rat research shows a significant increase in the kidney clearance of Topiramat when used with Probenecid. Plasma clearance in humans is about 20 - 30 ml/ minute after drinking.

linear:

Differences in plasma concentrations among objects when using topiramat are low, so it is possible to predict pharmacokinetics. With constant plasma clearance, the pharmacokinetics of the linear topiramat and the area below the concentration curve in plasma increases proportional to the dose in the single dose of 100 - 400 mg oral in healthy people. Patients with normal renal function may need 4-8 days to achieve plasma concentrations in a stable state. CMAX after taking the dose repeated, 100 mg x 2 times/ day in healthy people is 6.76 Ug/ ml. After the dose is repeated 50 mg and 100 mg Topiramat x 2 times/ day, the average duration of the plasma is about 21 hours.

Use with other anti -epileptic drugs:

Use a repeated combination of Topiramat 100 - 400 mg twice a day with phenytoin or carbamazepine increases proportion to the dose of plasma concentrations of Topiramat.

Special subjects:

Patients with renal failure:

Plasma clearance and kidney clearance of Topiramat decreases in patients with medium and severe impaired renal function (CLCR ≤ 70 ml/ minute). Therefore, plasma concentrations in a stable state may be higher when using the drug in patients with renal failure. In addition, patients with renal failure takes more time to achieve the stable state of each dose. In patients with medium and severe renal failure, it is recommended to reduce the starting dose and the maintenance dose. Topiramat is eliminated from hemorrhage effectively by hemolysis. Prolonged hemolysis can reduce Topiramat levels below necessary to maintain anti -seizures. To avoid rapid decrease in plasma concentrations when hemolysis, a Topiramat additional dose may be taken. Actual adjustment dose should be noted:

Topiramat's plasma clearance decreases an average of 26% in patients with severe to severe liver failure. Therefore, be careful when using Topiramat in patients with hepatic failure.

Elderly:

The plasma clearance of Topiramat is constant in the elderly without kidney disease.

Children (pharmacokinetics of children to 12 years):

Topiramat pharmacokinetics in children, like adults using drugs in additional treatment, is linear, with regardless of the dose depends on the dose and plasma concentration stable stability increases proportional to the dose. However, children have higher clearance and shorter selling time. Topiramat plasma concentration results in the same dose of mg/ kg may be lower in children than adults. As in adults, anti -epileptic drugs of liver enzyme reduce plasma concentrations in a stable state.

Very common (can affect more than 1 out of 10 people):

Unwanted effects in children are often the same as on adults. However, the following unwanted effects are more common in children than adults.

Common (can affect 1 to 10 of 100 people):

Be cautious when using

before using this medication, notify your doctor if you are having the following health problems:

If you are not sure if you have one of the above conditions, talk to your doctor or pharmacist before taking Topiramat.

You should not stop the medicine without consulting the doctor.

You should also talk to your doctor before taking any drug contains Topiramat to replace Huether-25/ Huether-50.

You may lose weight when using Topiramat, so your weight will be checked regularly when taking the drug. If you have too much weight loss or children use the drug without adequate weight, you should consult a doctor.

A few patients treated with anti -epileptic drugs such as Topiramat have the thought of self -harming themselves or suicide. If you have these thoughts at any time, contact the doctor immediately.

The drug contains lactose, notify your doctor if you have been told without tolerance to any type of sugar.

Drugs containing Polysorbat 80 can cause allergies and castor oils that can cause vomiting, vomiting, abdominal pain, diarrhea.

use drugs for children

There is no recommendation to use Topiramat in treatment or prevention of migraine in children due to not enough information about safety and effectiveness.

The effect of the drug on driving and operating machinery

dizziness, fatigue and visual problems may occur when using Topiramat. Do not drive or operate machines without consulting the doctor first.

Use drugs for women during pregnancy and lactation

If you are pregnant or nursing, think you may be pregnant or intend to get pregnant, consult your doctor before taking the medication.

Your doctor will discuss contraception used with you, as well as discussing whether Topiramat is suitable for you. Like other anti -epileptic drugs, Topiramat is at risk for the fetus if used during pregnancy. Make sure you understand the risk and benefits of using Topiramat to treat epilepsy during pregnancy.

You should not use Topiramat to prevent migraine if you are pregnant or you are likely to get pregnant and do not use effective contraception.

Women who breastfeed when taking Topiramat must notify the doctor as soon as possible if the child has any abnormal signs.

Medicinal interaction

Notice to your doctor or pharmacist about all medications you are using, including prescription or non -prescribing drugs, vitamins or medicinal herbs. Topiramat and certain drugs can affect each other. Sometimes the dose of Topiramat or other drugs need to be adjusted.

Notify the doctor or pharmacist if you are taking the following drugs:

Notify your doctor if you have a change in bleeding cycle while taking birth control pills and Topiramat.

Keep a list of drugs you are taking and show your doctor or pharmacist before taking a new medicine.

If you are not sure if there are these cases, talk to your doctor or pharmacist before taking the medication.

Use drugs with food and drink:

You can take the same or not with food. Drink plenty of water during the day to prevent kidney stones when using Topiramat. You should avoid drinking when using Topiramat.