Gabapentin, 300 mg, 50 pcs.

Active substance:

gabapentin - 300 mg; 

Excipients: 

calcium hydrogen phosphate dihydrate (Emcompress),

potato starch,

macrogol (polyethylene glycol 6000),

magnesium stearate

Gabapentin is similar in structure to the neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action is different from other drugs that interact with GABA receptors (valproic acid, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA uptake inhibitors, and agonists GABA).

It does not have GABAergic properties and does not affect the uptake and metabolism of GABA. The results of preliminary studies showed that gabapentin binds to the α2-δ subunit of voltage-dependent calcium channels and reduces the flow of calcium ions, which plays an important role in the occurrence of neuropathic pain.

Other mechanisms of Gabapentin's action in case of neuropathic pain are a decrease in glutamate-dependent death of neurons, an increase in GABA synthesis, suppression, release of neurotransmitters of the monoamine group. Clinically significant concentrations of gabapentin do not bind to receptors of other common drugs or neurotransmitters, including GABAA, GABAA, benzodiazepine, glutamate, glycine or N-methyl-D-aspartate receptors.

Gabapentin, unlike phenytoin and carbamazepine, does not interact with sodium channels in vitro. Gabapentin partially attenuated the effects of the glutamate receptor agonist N-methyl-D-aspartate in some in vitro tests, but only at a concentration of more than 100 μmol, which was not achieved in vivo. Gabapentin slightly reduces the in vitro release of monoamine neurotransmitters.

 Pharmacokinetics

 The bioavailability of gabapentin is not dose proportional. So, with increasing doses, it decreases. After ingestion of Cmax, Gabapentin in plasma is achieved after 2-3 hours. The absolute bioavailability of Gabapentin in capsules is about 60%. Food, including high in fat, does not affect pharmacokinetics.

The elimination of Gabapentin from plasma is best described using a linear model. T1 / 2 from plasma is dose-independent and averages 5-7 hours. The pharmacokinetics do not change with repeated use; equilibrium plasma concentrations can be predicted based on the results of a single dose of the drug.

Gabapentin almost does not bind to plasma proteins (d 57.7 L. It is excreted exclusively by the kidneys unchanged, is not exposed to metabolism.

The drug does not induce oxidative liver enzymes with a mixed function involved in the metabolism of drugs. Gabapentin clearance from plasma is reduced in the elderly and patients with impaired renal function. Excretion rate constant, plasma clearance, and renal clearance are directly proportional to creatinine clearance.

Gabapentin is removed from plasma by hemodialysis. In patients with impaired renal function and patients receiving hemodialysis treatment, a dose adjustment is recommended.

• monotherapy or as an additional tool for the treatment of partial seizures with or without secondary generalization in adults and children from 12 years of age;
• neuropathic pain in adults (18 years and older).

There is no data on the use of the drug in pregnant women, therefore, gabapentin should be used during pregnancy only if the expected benefit to the mother justifies the possible risk to the fetus.

Gabapentin is excreted in breast milk, its effect on the nursing baby is unknown, therefore, during breast-feeding, breast-feeding should be abandoned.

Use in children

Contraindicated under the age of 12 years with partial seizures. For the treatment of neuropathic pain, do not prescribe to children and adolescents under the age of 18 years.

• hypersensitivity to any of the components of the drug,
• age up to 12 years with partial convulsions.

Precautions: renal failure.

Use for impaired renal function

Use with caution in renal failure.

In patients with impaired renal function and patients receiving hemodialysis treatment, a dose adjustment is recommended.

In the treatment of neuropathic pain

The body as a whole: accidental injuries, asthenia, back pain, flu-like syndrome, headache, infection, pain of various localization, peripheral edema, weight gain;

Digestive tract: constipation, diarrhea, dry mouth, dyspepsia, flatulence, nausea, vomiting, abdominal pain;

Nervous system: gait disturbance, amnesia, ataxia, confusion, dizziness, hypesthesia, drowsiness, impaired thinking, tremor;

Respiratory system: shortness of breath, pharyngitis;

Skin and subcutaneous tissue: skin rash;

Sense organs: amblyopia.

In the treatment of partial seizures

The body as a whole: back pain, fatigue, fever, headache, viral infection, peripheral edema, weight gain, asthenia, - general malaise, facial swelling;

Cardiovascular system: symptoms of vasodilation or hypertension;

Digestive tract: constipation, dental disease, diarrhea, dyspepsia, increased appetite, dry mouth or throat, nausea and / or vomiting, abdominal pain, flatulence, anorexia, gingivitis;

Blood system, lymphatic system: leukopenia, purpura (most often it was described as bruising that occurred during physical trauma);

Musculoskeletal system: fractures, myalgia, arthralgia;

Nervous system: amnesia, ataxia, confusion, impaired coordination, depression, dysarthria, emotional lability, insomnia, nervousness, nystagmus, drowsiness, impaired thinking, tremor, muscle twitching, dizziness, hyperkinesia; strengthening, weakening or absence of reflexes, paresthesia, anxiety, hostility;

Respiratory system: cough, pharyngitis, rhinitis, pneumonia;

Skin and subcutaneous tissue: abrasion, window, skin itching, skin rash;

Sensory organs: amblyopia, diplopia, visual impairment;

Genitourinary system: urinary tract infection, impotence.

Morphine: when Gabapentin and morphine were taken together, when morphine was taken 2 hours before taking Gabapentin, there was an increase in the average area under the pharmacokinetic AUC of Gabapentin by 44% compared with Gabapentin monotherapy, which was associated with an increase in the pain threshold (cold pressor test).

The clinical significance of this change has not been established; the pharmacokinetic characteristics of morphine have not changed. Side effects of morphine when coadministered with gabapentin did not differ from those when taking morphine in conjunction with placebo.

No interactions have been observed between gabapentin and phenobarbital, phenytoin, valproic acid, and carbamazepine. The pharmacokinetics of gabapentin in equilibrium is the same in healthy people and patients receiving other anticonvulsants.

The simultaneous use of gabapentin with oral contraceptives containing norethisterone and / or ethinyl estradiol was not accompanied by changes in the pharmacokinetics of both components.

The simultaneous use of Gabapentin with antacids containing aluminum and magnesium is accompanied by a decrease in the bioavailability of Gabapentin by about 20%. Gabapentin is recommended to be taken approximately 2 hours after taking antacid.

Probenecid does not affect Gabapentin renal excretion.

A slight decrease in renal excretion of Gabapentin while taking cimetidine probably does not have clinical significance.

Inside, swallowing whole, regardless of food intake and drinking plenty of fluids. If it is necessary to reduce the dose, cancel the drug or replace it with an alternative agent, this should be done gradually over a period of at least one week.

Neuropathic pain in adults

The initial daily dose is 900 mg, divided into three doses; if necessary, the dose is gradually increased to a maximum of 3600 mg / day. Treatment can begin immediately with a dose of 900 mg / day (300 mg 3 times a day) or during the first 3 days the dose can be gradually increased to 900 mg per day. according to the following scheme:

1st day: 300 mg 1 time per day .;

2nd day: 300 mg 2 times a day .;

3rd day: 300 mg 3 times a day.

Partial cramps

Adults and children from 12 years: effective dose - from 900 to 2400 mg / day. Therapy can be started with a dose of 300 mg 3 times a day. on the first day or gradually increase to 900 mg according to the scheme described above.

Subsequently, the dose can be increased to a maximum of 3600 mg / day (divided into 3 equal doses). The maximum interval between doses when taking the drug three times should not exceed 12 hours in order to avoid the resumption of seizures.

Dose selection for renal failure

Patients with renal failure are recommended to reduce the dose of Gabapentin according to the table:

Creatinine clearance Daily dose (mg / sug)> 80900-240050-79600-120030-49300-60015-29150 * -300150 *

* appoint 300 mg every other day

Recommendations for patients on hemodialysis

Hemodialysis patients who have not previously taken Gabapentin are recommended to prescribe a drug in a saturating dose of 300-400 mg, and then apply it 200-300 mg every 4 hours of hemodialysis.

Symptoms: dizziness, double vision, speech impairment, drowsiness, lethargy, diarrhea.

Treatment: gastric lavage, intake of activated carbon, symptomatic therapy. Patients with severe renal failure may be shown hemodialysis.

Although withdrawal syndrome with the development of seizures was not noted with Gabapentin, nevertheless, a sharp cessation of antiepileptic therapy in patients with partial seizures can provoke the development of seizures.

Gabapentin is not considered an effective treatment for abscess epilepsy.

In patients who require joint therapy with morphine, an increase in the dose of gabapentin may be required. In this case, it is necessary to carefully monitor patients for the development of such a sign of depression of the central nervous system (CNS) as drowsiness. In this case, the dose of gabapentin or morphine should be adequately reduced.

Laboratory research

When Gabapentin was added to other anticonvulsants, false-positive results were recorded when urine protein was detected using Ames N-Multistix SG® test strips. To determine the protein in the urine, it is recommended to use a more specific method of precipitation with sulfosalicylic acid. Patients should avoid driving, as well as performing work requiring the speed of psychomotor reactions.

Capsules