Neyralgin

Neuralgin is a drug from a subcategory of anticonvulsants.

Indications Neuralgin

It is used in adults to eliminate having a high intensity of pain (also neuropathic).

In addition, it is used in combination with other anticonvulsants to eliminate seizures of a partial nature of epilepsy (accompanied by a secondary stage of generalization or not) - adults and adolescents from 12 years of age. At the same time, it is prescribed for partial seizures - children of 6-12 years old.

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

Release form

The release of the component is realized in capsules, 100 pieces inside the bottle or 10 pieces inside the cell plate; in a pack - 3 such records.

[5], [6]

Pharmacodynamics

Accurately determine the principle of gabapentin exposure at the moment failed. The element is structurally related to the neurotransmitter GABA, but by the type of its influence it differs from other active components interacting with GABA synapses (among them barbiturates with valproates, benzodiazepines and substances that slow down the activity of GABA transaminase, and slow down the processes of GABA capture, and besides this prodrug GABA and GABA agonists).

In vitro tests using gabapentin labeled with a radioactive isotope, a description of a new peptide binding region inside the rat brain, which included the hippocampus with the neocortex, which may be associated with the anesthetic and anticonvulsant effects of gabapentin, as well as its structural derivatives, was produced. The gabapentin synthesis zone is defined under the guise of the α2-δ subunit of the voltage-sensitive Ca channels.

Gabapentin, which is at the level of clinical indicators, is not synthesized with other common neurotransmitter or therapeutic cerebral endings, including GABA-A and GABA-B, and in addition glutamate, benzodiazepine, glycine or N-methyl-d-aspartate endings.

During in vitro procedures, gabapentin does not interact with Na channels, which distinguishes it from carbamazepine with phenytoin. The substance partially weakens the response to the activity of an NMDA glutamate agonist with separate in vitro testing, but only at values above 100 μm, which cannot be obtained in vivo.

The drug slightly reduces the amount of monoamine neurotransmitters released in vitro. Its use in rats causes an increase in GABA turnover in certain cerebral areas (an effect similar to the effect of sodium valproate, albeit in other areas of the brain). What significance such activity of gabapentin has for anti-convulsive activity still needs to be clarified.

In animals, the substance penetrates the brain without complications, preventing seizures caused by maximum electroshock or chemical convulsants (among them, elements that slow down GABA binding), and also genetic models of seizures.

[7]

Pharmacokinetics

After oral administration, gabapentin is absorbed at high speed inside the gastrointestinal tract, without reference to the use of food; in general, no interaction with food is observed. Plasma Cmax values are recorded after 2-3 hours. Portion size and plasma drug parameters are linearly dependent. Repeated administration of the drug does not change the pharmacokinetic characteristics. The values of absolute bioavailability are approximately 59%, not changing in the case of course use.

Synthesis with intraplasma blood protein in gabapentin is absent. The substance passes through the hepatoencephalic barrier; in epileptics, its values inside the cerebrospinal fluid are approximately 20% of the level of the corresponding equilibrium plasma parameters of drugs.

The drug is almost not subjected to metabolic processes within the human body, does not lead to a slowdown or induction of hepatic enzymes. The drug prevents the metabolism of the most commonly used anticonvulsants.

Excretion in an unchanged state is carried out only through the kidneys. Half-life is not tied to the size of the portion, on average equal to 5-7 hours in people with healthy secretory activity of the kidneys. From the blood plasma, the substance can be eliminated through hemodialysis.

Dosing and administration

It is possible to use a capsule without binding to food. To reduce the likelihood of negative symptoms, the first portion is recommended before bedtime.

In the case of pain of neuropathic genesis, for the first day you need to apply 0.3 g of the drug 1-fold, for the 2nd day - 2-fold 0.3 g, and for the 3rd day - 3-fold 0.3 g If necessary, the daily dosage is gradually increased until an analgesic effect is obtained (maximum 1.8 g, which are divided into 3 uses). In severe stages of the disease, higher portions are used - 1.8-3.6 g per day.

In the case of epilepsy, complex therapy is performed. Persons over the age of 12 should first use 0.3 g of the drug 3 times a day. The most effective are the portions in the range of 0.9-1.8 g per day (it is required to divide them into 3 uses). Use the substance with a maximum of 12-hour intervals.

Children from the age group of 6-12 years old should use 25-35 mg / kg per day (the dosage is divided into 3 uses).

Use Neuralgin during pregnancy

Prescribing medication to pregnant women is allowed only in situations where the benefits of its introduction to a woman are considered more likely than the risk of developing negative effects on the fetus.

The active element (gabapentin) is excreted with the mother's milk, which is why you cannot breastfeed when using it.

Contraindications

It is contraindicated to use in case of strong intolerance associated with medicinal substances.

[8]

Side effects Neuralgin

Among the side effects are:

• infectious infections: viruses, lesions of the urinary tract, pneumonia, and otitis media;
• lesions affecting the blood system: leuko- or thrombocytopenia;
• immune disorders: allergies;
• metabolic disorders: changes in blood sugar values, anorexia, increased appetite and increase or decrease in weight;
• mental disorders: depression, hallucinations, anxiety or excitement, thought disorder and emotional lability;
• lesions affecting the work of NA: ataxia, amnesia, drowsiness, dysarthria and convulsions, and in addition hyperkinesia, headaches, insomnia, dizziness and tremor. In addition, coordination disorder, nystagmus, hypokinesia with paresthesias and hypoesthesia, as well as potentiation / decrease / disappearance of reflexes and other motor disorders (dystonia, athetosis or dyskinesia);
• problems with visual function: diplopia or amblyopia, as well as the weakening of visual acuity;
• hearing impairment disorders: vertigo or ear ringing;
• lesions of the cardio-vascular apparatus: heartbeat, dilation of blood vessels and increased pressure;
• impaired respiratory function: pharyngitis, rhinitis, cough, dyspnea, and bronchitis;
• digestive disorders: diarrhea, vomiting, constipation, gingivitis, abdominal pain, dental disease, dry oral mucosa and flatulence, and besides hepatitis, jaundice, pancreatitis, and an increase in liver samples;
• epidermal lesions: pruritus, acne, SJS, angioedema, bruises and rashes, and in addition facial puffiness, polyformal erythema and alopecia;
• ODA damage: arthralgia, pain in the back, muscle twitching and myalgia;
• disorders of urogenital activity: urinary incontinence, kidney failure, gynecomastia and impotence;
• other signs: severe fatigue, asthenia, edema (sometimes peripheral), gait disorder, and at the same time, pain, fever, cold and discomfort, sternum pain and withdrawal syndrome (including nausea, hyperhidrosis, insomnia and anxiety).

[9], [10], [11], [12]

Overdose

Signs of intoxication: drowsiness, frequent and loose stools, double vision, lethargy and slurred speech.

In such cases sorbents are assigned to the victim. The drug can be excreted using hemodialysis sessions.

[13]

Interactions with other drugs

The drug is allowed to combine with other anticonvulsants (carbamazepine, phenobarbital, and besides this valproic acid and phenytoin), oral contraception (containing ethinyl estradiol or norethindrone) and means that block the secretion of the tubules and reduce renal excretion of gabapentin.

Antacids that contain Al3 + as well as Mg2 + in their composition lower the bioavailability level of the drug by about 20%, which is why it is recommended to use it after 2 hours after the administration of antacids.

With combined use with myelotoxic drugs, hematotoxicity is potentiated (development of leukopenia).

When using morphine capsules having a controlled release at a dosage of 60 mg in 2 hours, together with gabapentin in a 0.6 g serving, the average AUC of the latter increased by 44% in comparison with the AUC values of gabapentin used without morphine. Because of this, it is necessary to carefully monitor the condition of people, noting such a symptom of suppression of the function of the central nervous system as a feeling of drowsiness. With such a violation, it is necessary to lower the portion of morphine or gabapentin accordingly.

[14], [15]

Storage conditions

Neuralgin is required to be maintained at temperature values in the range of 15-30 ° C.

[16]

Shelf life

Neuralgin can be used for 5 years from the time a therapeutic substance is released.

[17], [18]

Application for children

Neuralgin is used in adjuvant treatment with secondary generalization (or not) of partial seizures in children over 6 years of age.

The drug may be prescribed for monotherapy for the above disorders for children over 12 years of age.

[19]

Analogs

Analogues of the drug are drugs Gababamma, Gabantin with Gabastadin, Nupintin with Gabaleptom, Tebantin with Gatonin, and besides Gabamax and Meditan with Gabapentin. In addition to Gabat, Convalis with Grimodin and Epigan with Newropent.