Meditan

Meditan is a medicine from the category of anticonvulsants.

Indications Meditan

It is used for the treatment of epilepsy - as an additional tool for the treatment of partial seizures (also in the case of complications in the form of generalized secondary type) in children older than 6 years of age and adults. In addition, the drug is used in monotherapy of the above disorders in adolescents from 12 years and adults.

A medication is also prescribed for the treatment of neuropathic pains (peripheral type) - for example, with neuropathy of diabetic origin or post-zoster neuralgia (adults).

[1], [2], [3], [4], [5],

Release form

Release of drugs is carried out in capsules, in an amount of 10 pieces inside the blister pack. Capsules with a volume of 0.1 and 0.4 g are produced by 3 blister packs in a box, and capsules having a volume of 0.3 g are sold on 3 or 6 plates inside the box.

[6], [7], [8], [9]

Pharmacodynamics

There is no precise data on the mechanism of therapeutic influence exerted by gabapentin.

The structure of gabapentin is similar in many respects to the neurotransmitter GABA, but the mechanism of its medicinal effect is different from that of other elements interacting with GABA endings (among them barbiturates, substances slowing the activity of GABA transferase, valproate, inhibiting GABA capture processes, and besides this GABA precursors and agonists of GABA elements).

The therapeutic dose of gabapentin does not lead to synthesis with the endings of other common drugs or with neurotransmitter endings of the brain (among them the end of GABA and GABA, glutamate with benzodiazepines, glycine or NMDA).

The element gabapentin did not interact (with in vitro tests) with Na channels, which distinguishes it from carbamazepine with phenytoin. Separate in vitro test systems showed that gabapentin partially reduced the intensity of the NMDA glutamate agonist effect. To achieve such an effect will be obtained only at drug indices exceeding 100 μmol, and this can not be done in vivo. Also, gabapentin slightly reduces the secretion of monoamine neurotransmitters in vitro.

Gabapentin promotes an increase in GABA metabolism in certain areas of rat brain; this effect is also observed in sodium valproate, but in relation to other cerebral spinal divisions. What significance these effects of gabapentin have on the anticonvulsant effect is not known.

In animals, the active element of the drug passes through the BBB and stops the maximal transient seizures caused by electric shock, and in addition convulsions induced by convulsants of a chemical nature (among them substances slowing the binding of GABA) and triggered by the influence of genetic factors.

[10], [11], [12], [13]

Pharmacokinetics

Absorption.

After oral administration of gabapentin, plasma Cmax values are noted after 2-3 hours. With an increase in the portion of drugs, one can see a tendency to lower the level of bioavailability of the substance (its absorbed part). The absolute bioavailability after taking a capsule with a volume of 0.3 g is about 60%. The consumption of food (also fatty) has no clinical significance for the pharmacokinetic parameters of gabapentin.

The pharmacokinetics of drugs does not affect the repeated use of the drug. While the plasma indices of the drug in clinical tests ranged from 2 to 20 μg / ml, these values do not determine the degree of safety and effectiveness of the drug.

Distribution processes.

The medicinal element is not subjected to protein synthesis within the blood plasma. Indicators of the distribution volume of drugs are 57.7 liters. The level of substance inside the CSF in people with epilepsy is approximately 20% of the minimum equilibrium values within the plasma. Gabapentin is able to pass into the mother's milk.

Excretion.

Gabapentin is excreted unchanged only through the kidneys. The half-life of the element is not tied to the size of the dosage and is on average 5-7 hours.

In adults with disorders in the kidneys, there are lower values of drug clearance within the plasma. The elimination rate constant, as well as the clearance inside the kidneys and plasma are directly proportional to the values of the SC.

The substance is excreted from the plasma during hemodialysis sessions. Therefore, people with disorders of renal activity, who are on hemodialysis, should adjust the size of the portion of Meditan.

[14], [15], [16]

Dosing and administration

Capsules are consumed orally, without binding to eating. Drink the medicine with a lot of liquid (1 cup of plain water).

The mode of use during the initial selection of dosage for adolescents from 12 years and adults: on the first day, take 0.3 g (once) per day; on the second day - a 2-time intake of 0.3 g of drugs; on the 3rd day - a 3-fold use of 0.3 g of the drug.

The process of drug cancellation.

Doctors recommend abolishing drugs gradually, for at least 7 days, regardless of the treatment scheme used.

Epilepsy.

In the case of epilepsy, prolonged treatment is often necessary. A portion of the drug is chosen by the doctor, taking into account the effect of the drug and the patient's tolerance.

Adolescents over 12 years of age and adults with epilepsy are usually prescribed portions in the range of 0.9-3.6 g per day. Therapy starts with titration of a dose of LS or with a dosage of 0.3 g with a triple take for the first day. Further, taking into account the therapeutic effect and tolerability of drugs, each subsequent 2-3 days a portion can be increased by 0.3 g, reaching a maximum of 3.6 g per day.

Some people require less rapid titration of the drug. The shortest period of achieving a portion of 1.8 g per day is 7 days; 2,4 g - 14 days; 3.6 g - 21 days.

With prolonged clinical tests, a serving of 4.8 grams per day was well tolerated. The daily dosage is divided into 3 uses. Intervals between drugs can be no more than 12 hours - this is necessary to avoid interruption of antiepileptic treatment and to prevent the development of seizures.

For children from the age group 6-12 years old, the initial dosage amount per day is 10-15 mg / kg. Effective dosages are achieved by titration for approximately 3 days. Children over 6 years of age should take 25-35 mg / kg per day.

The daily therapeutic dose of 50 mg / kg was found to be well tolerated (tested by prolonged clinical tests). The total dosage per day is divided into 3 equal portions by volume. The interval between uses can be a maximum of 12 hours.

It is not necessary to monitor the indices of drugs inside the blood serum. Also, combined use of Meditan with other anticonvulsants is allowed, because in this case the level of gabapentin inside the plasma or other anticonvulsants inside the blood serum does not change.

Neuropathic pain, having a peripheral nature.

Adults are first titrated with a dose of LS or divide by 3 times the initial daily dose of 0.9 g. After this, taking into account the effect and tolerability, the portion should be increased to the maximum values of 3.6 g per day according to the scheme described above.

Long-term clinical study (more than 5 months) of safety and drug effect of drugs in the treatment of neuropathic pain (diabetic form of pain neuropathy or PGN) was not carried out. If you need longer therapy associated with neuropathic pain, you need the doctor to evaluate the patient's condition before continuing and determine whether additional treatment is necessary.

People with severe general health or some aggravating manifestations (condition after transplantation, low weight) should be given a slower titration, lower the step portion, or prolong the intervals between increases in doses.

Elderly people (age over 65 years).

Older patients should choose portions individually, because they may have a weakened kidney activity. Such patients often have peripheral puffiness and a feeling of weakness or drowsiness.

People with deficiency of renal function.

Persons who have severe forms of impairment, or those who are on hemodialysis, should individually select a therapy regimen. They are recommended to use capsules having a volume of 0.1 g.

Serving size for problems with kidney function:

• values> 80 ml / minute - for a day in general to accept within the limits of 0,9-3,6 g of a medicine;
• the level of QC in the range of 50-79 ml / minute - the use of 0.6-1.8 g of drugs;
• QC values in the range of 30-49 ml / min - intake of 0.3-0.9 g of medication;
• Values of SC within 15-29 ml / minute - application of 0.15 * -0.3 or 0.15 * -0.6 g of substance.

* use in a dose of 0.1 g 3 times a day, with the reception every other day.

People on hemodialysis.

Persons with anuria, who are on hemodialysis and who have never taken Meditane before, should consume a satiating dose of 0.3-0.4 g, then take 0.2-0.3 g after every 4 hours of the session hemodialysis. In those days, when the procedure is not carried out, the drug is not taken.

[20], [21]

Use Meditan during pregnancy

Systemic risks of epilepsy, as well as the use of anticonvulsants.

The probability of developing congenital disease in a child whose mother took anticonvulsants is doubled / tripled. Often there was a "hare" lip, as well as defects in the development of CAS and defects affecting the neural tube. Complex anticonvulsant treatment has an even higher probability of anomalies (in comparison with monotherapy), which is why it is recommended to use monotherapy if it is necessary to use drugs.

Women who are in reproductive age, as well as pregnant women, if there is a need for anticonvulsant treatment, should consult a doctor before commencing it. At the conception planning stage, it is also necessary to revise the need for anticonvulsant therapy. It is forbidden to abruptly and suddenly cancel the use of anticonvulsants, because as a result of this, cramps may appear that will significantly worsen the condition of both women and fetuses.

Delays in the development of children born to mothers with epilepsy are rare. In such cases, it is impossible to differentiate what specifically caused the delay in the development of the child - genetic disorders, mother's epilepsy, social causes, or the use of anticonvulsants during pregnancy.

Risks caused by the use of gabapentin.

There are no relevant relevant data regarding the use of the substance in pregnancy. Animal tests have demonstrated that it has reproductive toxicity, but risks to the human body are unknown. It is forbidden to use Meditana during pregnancy, except when the benefits for women are much more likely than the risks of complications for the fetus.

Gabapentin is excreted with human milk. Because the effect of the medication on infants has not been studied, it is necessary to prescribe it with lactation very carefully. The use of gabapentin in this period is justified only in situations where the benefits for women are more anticipated than the possibility of the appearance of negative consequences for the child.

Contraindications

Contraindicated use in people with intolerance in relation to the active element or other auxiliary components of drugs.

[17], [18]

Side effects Meditan

Taking capsules can lead to some side effects:

• diseases caused by parasites or infections: often there are infections of a viral origin. Often there are infections that affect the urinary or respiratory system, pulmonary inflammation and otitis media;
• disorders affecting lymph and blood-forming processes: often there is leukopenia. Occasionally - thrombocytopenia;
• Immune lesions: occasionally allergy symptoms (such as urticaria) are observed. Perhaps the emergence of DRESS-syndrome or common disorders with different manifestations (among them hepatitis, rashes, fever, eosinophilia, lymphadenopathy, etc.);
• Disorders of nutritional and metabolic processes: Anorexia or an increase in appetite is often noted. Sometimes there is hyperglycemia (mainly in diabetics). Occasionally, hypoglycemia occurs (also usually in diabetics). Possible the development of hyponatremia;
• problems with the psyche: often there is a feeling of anxiety, hostility, confusion, anomalous thinking develops, a state of depression or emotional instability. Occasionally there are hallucinations;
• disturbances in the activity of the National Assembly: often there is a feeling of drowsiness, dizziness or ataxia. Hyperkinesis, headaches, convulsions, tremors, nystagmus are often noted, and besides this, dysarthria, sensitivity disorder (hypesthesia or paresthesia) or coordination, insomnia, amnesia or memory impairment, as well as potentiation of reflexes, their weakening or complete absence. Occasionally there are motor disorders (among those dyskinesia, choreoathetosis or dystonia) or there is a loss of consciousness. Sometimes there may be a disorder of mental function or hypokinesia;
• problems with visual function: often there are visual disturbances (for example, diplopia or amblyopia);
• disorders in the work of the auditory system: often there is a vertigo. Occasionally, there is an ear noise;
• symptoms affecting the work of the heart: occasionally there is an increase in heart rate;
• disturbances of vascular activity: often there is an increase in the values of blood pressure or vasodilation;
• problems associated with respiratory function, sternum and mediastinum: often there is bronchitis, runny nose, dyspnoea, cough or pharyngitis;
• manifestations in the gastrointestinal tract: often there is nausea, diarrhea, gingivitis, vomiting, dental pathology, indigestion, abdominal pain, constipation, dry throat or oral mucosa, and flatulence. Occasionally pancreatitis occurs;
• disorders of the function of the ZHVP and the liver: occasionally jaundice or hepatitis develops;
• lesions affecting the hypodermic layer and epidermis: often there is purpura (usually looks like bruises caused by trauma), itching, facial swelling, rashes and acne. Occasionally, Quincke edema occurs, alopecia, Stevens-Johnson syndrome, erythema polyformiform and drug-induced rash, accompanied by common signs and eosinophilia;
• disorders in connective tissue and skeletal muscle: often there is myalgia, pain in the back, arthralgia and twitching of the muscles. Possible development of rhabdomyolysis or seizures of myoclonic nature;
• problems with the operation of the system of urination or kidneys: urinary incontinence is often observed. Occasionally - failure of renal activity in the acute stage;
• lesions of mammary glands and reproductive organs: often impotence develops. Perhaps the emergence of gynecomastia, mammary gland hypertrophy or sexual dysfunction (this includes anorgasmia, ejaculation disorder and changes in libido);
• systemic signs: most often there is a febrile condition and a feeling of increased fatigue. Also often there is a feeling of weakness or discomfort, pain, swelling of generalized or peripheral nature, gait disorder and flu-like syndrome. Occasionally, there are withdrawal effects (usually hyperhidrosis, a sense of anxiety, nausea, insomnia and pain) and pain in the sternum. There are reports of sudden deaths, but in such cases it was not possible to establish a clear relationship with the use of drugs;
• data from various tests: often there is an increase in weight or a decrease in the number of leukocytes. Sometimes there is an increase in the values of the hepatic function (ALT or AST), as well as bilirubin. There may be an increase in CKK and a fluctuation in the values of sugar in diabetics;
• intoxication or trauma: often there are fractures, injuries or abrasions of a random nature.

There is evidence of the development of acute forms of pancreatitis during the period of therapy with the use of Meditan, but this fact could not be attributed to the use of gabapentin.

In people with a deficiency of renal function in the terminal phase, who are on hemodialysis, myopathy was noted with an increase in the parameters of CK.

Otitis media, infections in the respiratory ducts, bronchitis and convulsions were found only in clinical tests in children. In addition, the children tested often had hyperkinesis and aggressive behavior.

[19],

Overdose

The emergence of life-threatening toxic signs was not noted even with the use of drugs in a dose up to 49 g per day.

Among the manifestations of intoxication: diplopia, dizziness, loss of consciousness, a feeling of lethargy or drowsiness, slurred speech and weak diarrhea. All symptoms disappeared after maintenance therapy. The weakening of absorption of drugs with large portions can limit the absorption of other drugs and reduce the toxic effect in overdose.

While gabapentin can be removed from the body through hemodialysis, it is often not required. Although persons with a deficiency of renal function, this procedure can be shown.

Tests in rats with mice did not allow the detection of a lethal dose of drugs, although in these cases doses up to 8 g / kg were used. Among the signs of acute poisoning in animals, ptosis, ataxia, impaired activity, or vice versa, increased excitability, as well as difficulty in the respiratory process.

Drug intoxication, especially in combination with other CNS suppressing agents, can cause a coma.

Interactions with other drugs

Admission together with antacids (magnesium or aluminum-containing) lowers the bioavailability level of Meditan by a maximum of 24%. You should take the medicine at least 2 hours after using antacids.

Combination with cimetidine results in a slight decrease in renal excretion of gabapentin, but this effect has no clinical significance.

Tests involving volunteers (N = 12) using morphine capsules (60 mg) with a controlled release type 120 minutes before using 0.6 g gabapentin showed that the mean AUC of the latter increased by 44% compared to the regimens in which morphine was not used. Because of this, with such combinations, it is necessary to closely monitor the patients' condition in time to recognize signs of CNS depression (feeling sleepy) and to lower the dosage of Medithan or morphine.

If other medications that interfere with the CNS work, or if the drug is mixed with alcoholic beverages, potentiation of negative signs of gabapentin in the central nervous system (ataxia, drowsiness, etc.) can be observed.

When combined with myelotoxic medicines, the hematotoxic effect increases (leukopenia develops).

[22], [23], [24]

Storage conditions

Meditans should be kept in places that are closed from children's access. The temperature is within 25 ° C.

[25], [26]

Shelf life

Meditan can be used within 24 months of the release of the therapeutic drug.

Application for children

Gabapentin is prescribed in pediatrics for children suffering from epilepsy: as an additional remedy during the treatment of a child over the age of 6 years or as a monotherapy for adolescents from 12 years of age.

[27]

Analogues

Analogues of the medication are medicines Gabamax, Gabagama 800, Gabapentin with Gabaleptom, and in addition Neuralgin with Tebantin, Gabantin 300, Newropentin and Nupintin.

[28], [29]