medicalmeds.eu Medicines Antiepileptic means. Mieditang

Mieditang

Producer: JSC Pharmak Ukraine

Code of automatic telephone exchange: N03AX12

Release form: Firm dosage forms. Capsules.

Indications to use: Epilepsy. Diabetic neuropathy. Post-herpetic neuralgia.

General characteristics. Structure:

Active ingredient: gabapentin;

1 capsule contains a gabapentin in terms of 100% anhydrous substance of 100 mg, 300 mg or 400 mg;

excipients: lactose anhydrous, starch corn, talc.

Pharmacological properties:

Pharmacodynamics. Gabapentin is amino acid which on chemical structure is similar to brake mediators of GAMK. However габапентин does not interact with GAMK receptors, does not turn in the course of metabolic reactions neither into GAMK, nor in GAMK agonists, does not inhibit capture or splitting of GAMK.

The mechanism of analgeziruyushchy action of a gabapentin is unknown, however in researches габапентин prevented allodynia at animals (the painful behavior at animals arising in response to irritation which usually should not cause pain) and a hyperalgesia (the strengthened answer to a usual painful irritant).

The mechanism of antiepileptic action of a gabapentin is unknown, but in researches on animals with use of models of a convulsive state габапентин showed the same anticonvulsant activity, as well as other known antikonvulsant.

Pharmacokinetics. At intake габапентин it is quickly absorbed from a digestive tract irrespective of meal. Interaction with foodstuff is absent. The maximum concentration of drug in a blood plasma is reached in 2-3 hours. The dose of drug and its concentration in plasma stay in linear dependence. Repeated administration of drug does not affect parameters of its pharmacokinetics. The indicator of absolute bioavailability makes about 59% and does not change at course reception.

Gabapentin does not contact proteins of plasma. Drug gets through a blood-brain barrier, at patients with epilepsy its concentration in cerebrospinal fluid makes about 20% of the corresponding equivalent concentration of drug in a blood plasma.

Gabapentin is practically not metabolized in a human body, does not cause induction or braking of enzymes of a liver. Drug does not influence metabolism of antiepileptic drugs which are used in the general practice.

Drug is removed only by kidneys in not changed look. The elimination half-life does not depend on a dose and makes 5-7 hours at persons with normal secretory function of kidneys. Gabapentin it is possible to remove from a blood plasma by means of a hemodialysis.

Pharmaceutical characteristics.

Main physical and chemical properties:

capsules on 100 mg: solid gelatin capsules No. 3; case and lid of the capsule of deadwhite color; capsule contents – powdery mix of white or almost white color;

capsules on 300 mg: solid gelatin capsules No. 1; case and lid of the capsule of opaque yellow color; capsule contents – powdery mix of white or almost white color;

capsules on 400 mg: solid gelatin capsules No. 0; case and lid of the capsule of opaque orange color; capsule contents – powdery mix of white or almost white color.

Indications to use:

Treatment of partial epileptic attacks with or without secondary generalization at adults and children is more senior than 6 years in a combination with other antiepileptic drugs.
Treatment of partial epileptic attacks with or without secondary generalization at adults and children is more senior than 12 years as monotherapy.
Treatment of the accompanying neuralgic pain at adults at diabetic neuropathy and post-herpetic neuralgia.

Route of administration and doses:

Accept inside. Meal does not influence Mieditang's action. For decrease in risk of development of side reactions the first dose is recommended to be accepted before going to bed.

Epilepsy

Mieditang is recommended as a component of the combined treatment of patients with epilepsy, since 6 years.

Adults and children are more senior than 12 years. The initial dose makes 300 mg of drug 3 times a day. The effective dose of drug makes 900-3600 mg/days (having divided into 3 receptions).

The maximum break between administrations of drug should not exceed 12 hours.

Children from 6 to 12 years. The initial dose has to make from 10 to 15 mg/kg/days; the effective dose is reached by titration within about three days. The effective dose of a gabapentin at children at the age of 6 years is also more senior makes from 25 to 35 mg/kg/days. Dosages to 50 mg/kg/days are noted by good tolerance in long-term clinical trials. The general daily dose has to be divided into three single doses, the maximum interval of time between receptions should not exceed 12 hours.

In case of the admission of reception of the next dose of drug the passed dose needs to be accepted provided that reception of the dose following according to the schedule will be not earlier than in 4 hours.

Otherwise the passed dose should not be accepted.

Patients of advanced age and patients with a renal failure

To patients with reduced function of kidneys, to patients of advanced age and patients, which

are on a hemodialysis, the dose should be adjusted according to the data provided in the table.

Table

Dosage of a gabapentin at adults taking into account function of kidneys

Clearance of creatinine (ml/min.)                              of Obshchayasutochnaya dozaa (mg/days)
≥                                                                                80 900-3600
                                                                                50-79 600-1800
                                                                                30-49 300-900
15-29                                                                               150b-600
<15c                                                                                 150b-300

the General daily dose should be distributed on three receptions. Decrease in a dosage for patients with renal failures (clearance of creatinine <79 ml/min.).

b Is appointed in a dose of 300 mg every other day.

c At patients with clearance of creatinine <15 ml/min. a daily dose needs to be reduced in proportion to clearance of creatinine (for example, patients with clearance of creatinine of 7,5 ml/min. have to receive a half of that daily dose which is received by patients with clearance of creatinine of 15 ml/min.).

Researches concerning drug use to the children up to 12 years having a renal failure were not conducted.

Use to the patients who are on a hemodialysis

At the patients with an anury who are on a hemodialysis and earlier never receiving габапентин, it is recommended to apply doses of saturation from 300 to 400 mg, then – 200-300 mg of a gabapentin after each 4-hour session of a hemodialysis. In days when dialysis is not carried out, габапентин it is impossible to accept.

At patients with disturbances of functions of kidneys which take place a hemodialysis the maintenance dose of a gabapentin has to be proved by the recommendations concerning a dosage stated in the table. In addition to a maintenance dose reception of 200-300 mg of drug after each 4-hour session of a hemodialysis is recommended.

Neuralgic pain (at diabetic neuropathy and post-herpetic neuralgia)

The adult treatment by Mieditang begin with reception 300 mg of drug in the 1st day, in the 2nd day – 600 mg, having divided into 2 receptions, for the 3rd day – 900 mg, having divided into 3 receptions. If necessary the daily dose to 1800 mg/days can be increased gradually before achievement of analgesic effect (having divided into 3 receptions). In hard cases efficiency of drug was observed at higher doses (from 1800 to 3600 mg/days).

Features of use:

Mieditang's use does not demand carrying out routine monitoring of clinical laboratory parameters. Sharp phase-out of drug as it can lead to increase in frequency of epileptic attacks is not recommended. In need of a dose decline or the termination of administration of drug it needs to be done gradually for at least one week.

Suicide thoughts and behavior were observed at patients who were treated antiepileptic means at some indications. Meta-analysis of randomized platsebokontroliruyemy researches of antiepileptic means also showed the small increased risk of emergence of suicide thoughts and behavior. The origins of this risk are unknown, and the available data do not make impossible the increased risk for a gabapentin.

Therefore it is necessary to control signs of suicide thoughts and behavior and it is necessary to consider the possibility of use of the corresponding treatment. It is necessary to advise patients (and to those who look after them) to ask for medical care at emergence of signs of suicide thoughts and behavior.

As well as in case of reception of other antiepileptic means, attempts of the termination of reception of the accompanying antiepileptic means at treatment of the refraction patients accepting more than one antiepileptic means for achievement of monotherapy by Mieditang have low degree of success.

Gabapentin is not considered effective against primary generalized attacks, such as an absentia epileptica, and it can make heavier attacks at some patients. Therefore габапентин patients should apply with care with the mixed attacks, including an absentia epileptica.

At Mieditang's appointment a sick diabetes mellitus it is necessary to control glucose level in blood and, if necessary, to adjust a dose of hypoglycemic drugs.

At emergence of symptoms of pancreatitis administration of drug needs to be stopped.

There are no data on development of tolerance to a gabapentin.

During treatment it is impossible to accept alcohol because of strengthening of such side reactions as dizziness and drowsiness.

Use to elderly people. Drug use by the patient of advanced age can demand reduction of a dose of a gabapentin (see the section "Route of Administration and Doses").

Use by the patient with renal failures. At patients with renal failures considerable decrease in size of clearance of drug therefore the dose of a gabapentin needs to be modified is noted.

Use at liver diseases. As габапентин does not give in to metabolism in a human body, special researches of pharmacokinetics of drug at patients with an abnormal liver function were not conducted.

Drug use by the patient which are on a hemodialysis.

When studying parameters of pharmacokinetics of a gabapentin at patients with an anury the elimination half-life of drug makes about 132 hours. When carrying out a hemodialysis (3 times a week 4 hours) the elimination half-life of a gabapentin decreased till 51 o'clock. Thus, at such patients the dose of drug is subject to correction (see the section "Route of Administration and Doses").

Laboratory tests

When carrying out semi-quantitative definition of crude protein in urine by means of rapid tests wrong positive results can be received. Therefore it is recommended to check such results of rapid tests by means of the methods based on other analytical principle such as biuretic test, a turbidimetrichesky method or a method of binding of dye, or it is necessary to use these methods right at the beginning.

This drug contains lactose therefore patients cannot apply it with insufficiency of lactose, a galactosemia or a syndrome of disturbance of absorption of a glucose/galactose.

Ability to influence speed of response at control of motor transport or work with other mechanisms.

Patients with uncontrollable epilepsy cannot be allowed to control of motor transport or to work with the raised risk sources. The patients accepting габапентин can be engaged in the activity requiring special attention or speeds of psychomotor reactions only if they are completely sure that administration of drug will not damage to performance of such professional activity owing to possible by-effects.

Side effects:

Infections: viral infections, pneumonia, respiratory infections, infections of an urinary system, otitis of a middle ear.

From system of blood: leukopenia, thrombocytopenia.

From immune system: (pour) allergic reactions.

From metabolic processes: anorexia, increase in appetite, increase in body weight, fluctuation of level of glucose at the patients sick with diabetes.

Mental disturbances: concern, emotional lability, depression, disturbance of thinking, excitement, hallucinations.

From the central nervous system: drowsiness, dizziness, ataxy, spasms, hyperkinesia, dysarthtia, amnesia, tremor, sleeplessness, headache, paresthesias, giposteziya, lack of coordination, nystagmus, strengthening, easing or lack of reflexes, hypokinesia, other motive disturbances (choreoathetosis, dyskinesia, dystonia).

From organs of sight: vision disorder, amblyopia, diplopia.

From acoustic organs: вертиго, a ring in ears.

From cardiovascular system: heart consciousness, arterial hypertension, vasodilation.

From respiratory system: диспноэ, bronchitis, pharyngitis, cough, rhinitis.

From digestive tract: vomiting, nausea, an abdominal pain, an ulitis, diarrhea, a lock, dryness in a mouth, dyspepsia, damage of teeth, swelling, hepatitis, jaundice, increase in hepatic tests (ALT, nuclear heating plant, bilirubin), pancreatitis. In clinical trials communication between developing of pancreatitis and use of a gabapentin was not established.

From skin and hypodermic cellulose: swelled persons, hematomas, rash, an itch, an acne, Stephens-Johnson's syndrome, an angioedema, a multiformny erythema, an allopecia.

From a musculoskeletal system: arthralgia, mialgiya, dorsodynia, muscular twitchings.

From urinogenital system: acute renal failure, urine incontience, increase in mammary glands, impotence.

Others: fatigue, fever, peripheral hypostases, gait disturbance, an adynamy, pain, an indisposition, cold, generalized hypostases, cancellation reaction (concern, sleeplessness, nausea, pain, the increased perspiration), a stethalgia.

At clinical trials respiratory infections, infections of a middle ear, bronchitis, spasms were observed only at children.

Interaction with other medicines:

At simultaneous use with antiacid means absorption of a gabapentin is slowed down and bioavailability of drug decreases by 24% therefore it is recommended to accept Mieditang at least in 2 hours after reception of antiacid means.

At joint reception with Cimetidinum the clearance of a gabapentin decreases by 14% and respectively, concentration of a gabapentin in blood can increase.

Gabapentin can increase concentration of a felbamat in blood. At joint administration of drugs constant observation of the patient for the purpose of early detection of possible collateral symptoms / is necessary for toxicity of a felbamat.

At joint reception with morphine concentration of a gabapentin in blood can increase.

Gabapentin can increase the maximum concentration of norethindrone for 13%.

There are data on what габапентин can increase concentration of Phenytoinum in blood serum.

Gabapentin does not influence concentration of valproic acid, carbamazepine, phenobarbital.

It is necessary to abstain from simultaneous use of a gabapentin with a sundrops (the threshold of convulsive activity decreases).

Not to apply together with a valerian, a St. John's Wort, a kava-kava, Polynesian pepper, Coca which oppress the central nervous system.

Contraindications:

Hypersensitivity to drug components.

Overdose:

Cases of overdose of a gabapentin at one-time use of drug in doses to 49 g are registered.

Symptoms: doubling in eyes, the muffled speech, drowsiness, a lethargy, diarrhea.

Treatment: symptomatic and maintenance therapy. Gabapentin can be brought from an organism by means of a hemodialysis. At overdose it is possible to apply absorbent carbon.

Use during pregnancy or feeding by a breast.

Use of a gabapentin by pregnant women is allowed only when the expected advantage for mother exceeds potential risk for a fruit.

Gabapentin is allocated in breast milk therefore use of drug in the period of a lactation is possible only when the expected advantage for mother exceeds potential risk for the child. In other case during use of drug it is necessary to stop feeding by a breast.

Children.

Up to 6 years it is not recommended to children to use drug.

Mieditang children can appoint more senior than 12 years in a combination with other antiepileptic means for treatment of partial epileptic attacks with or without secondary generalization, and also children are from 6 to 12 years old for treatment of partial epileptic attacks in cases when the standard therapy is insufficiently effective.

Storage conditions:

Period of validity. 2 years. Not to use drug after the termination of the period of validity specified on packaging. To store at a temperature not above 25 °C. To store in the place, unavailable to children.