Indications
- monotherapy or as an adjunct 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).
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Add to wishlistInside, swallowing whole, regardless of food intake and drinking plenty of liquid. If it is necessary to reduce the dose, discontinue the drug or replace it with an alternative remedy, this should be done gradually for 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 be started immediately with a dose of 900 mg / day (300 mg 3 times a day) or during the first 3 days, the dose can be increased gradually to 900 mg / day. according to the following scheme:
Day 1: 300 mg once a day;
day 2: 300 mg twice a day;
day 3: 300 mg 3 times a day
Partial seizures
Adults and children over 12 years of age: the effective dose is 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 increase gradually 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 to avoid the resumption of seizures.
Dose selection for renal failure
Patients with renal insufficiency 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*>
* prescribe 300 mg every other day
Recommendations for patients undergoing hemodialysis
Patients on hemodialysis who have not previously taken Gabapentin are recommended to prescribe this drug in a saturating dose of 300-400 mg, and then apply it 200-300 mg every 4 hours of hemodialysis.
With caution:Â kidney failure.
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Use in patients with impaired renal function
Use with caution in patients with renal insufficiency.
In patients with impaired renal function and patients receiving hemodialysis treatment, dose adjustment is recommended.
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Active ingredient:
gabapentin-300 mg;
Auxiliary substances:Â
calcium hydrophosphate dihydrate (Emcompress),
potato starch,
macrogol (polyethylene glycol 6000),
magnesium stearate
Active ingredient:
gabapentin – 300 mg;
Auxiliary substances: Â
calcium hydrophosphate 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 differs from other drugs that interact with GABA receptors (valproic acid, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA uptake inhibitors, GABA agonists and prodrug forms of GABA).
It does not have GABA-ergic properties and does not affect the uptake and metabolism of GABA. Preliminary studies have shown 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 action of Gabapentin in neuropathic pain are a decrease in glutamate-dependent neuronal death, an increase in GABA synthesis, and suppression of the release of monoamine group neurotransmitters. Gabapentin in clinically significant concentrations does not bind to the receptors of other common drugs or neurotransmitters, including GABA, GABA, 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 concentrations greater than 100 mmol, which is not achieved in vivo. Gabapentin slightly reduces the release of monoamine neurotransmitters in vitro.
Pharmacokinetics
The bioavailability of Gabapentin is not proportional to the dose. So, when the dose is increased, it decreases. After oral use, the Cmax of Gabapentin in plasma is reached in 2-3 hours. The absolute bioavailability of Gabapentin in capsules is about 60%. Food, including those with a high fat content, does not affect the pharmacokinetics.
The elimination of Gabapentin from plasma is best described using a linear model. T1 / 2 from plasma does not depend on the dose and averages 5-7 hours. Pharmacokinetics do not change with repeated use; steady-state plasma concentrations can be predicted based on the results of a single dose of the drug.
Gabapentin is almost not bound to plasma proteins (d 57.7 l. It is excreted exclusively by the kidneys in unchanged form, and is not metabolized.
The drug does not induce mixed-function oxidative liver enzymes involved in drug metabolism. The clearance of Gabapentin from plasma decreases in the elderly and patients with impaired renal function. The elimination rate constant, plasma clearance, and renal clearance are directly proportional to creatinine clearance.
Gabapentin is removed from the plasma by hemodialysis. In patients with impaired renal function and patients receiving hemodialysis treatment, dose adjustment is recommended.
There are no data on the use of the drug in pregnant women, so Gabapentin should be used during pregnancy only if the intended benefit to the mother justifies the possible risk to the fetus.
Gabapentin is excreted in breast milk, its effect on the breastfed child is unknown, so during treatment, you should stop breastfeeding.
Use in children
Contraindicated in children under 12 years of age with partial seizures. For the treatment of neuropathic pain, do not prescribe to children and adolescents under 18 years of age.
With caution: Â kidney failure.
Use in patients with impaired renal function
Use with caution in patients with renal insufficiency.
In patients with impaired renal function and patients receiving hemodialysis treatment, dose adjustment is recommended.
In the treatment of neuropathic pain
The body as a whole: Â accidental injuries, asthenia, back pain, flu-like syndrome, headache, infection, pain of various localization, peripheral edema, weight gain;
The digestive tract: Â constipation, diarrhea, dry mouth, dyspepsia, flatulence, nausea, vomiting, abdominal pain;
The nervous system: Â gait disorders, amnesia, ataxia, confusion, dizziness, hypesthesia, drowsiness, impaired thinking, tremor;
Respiratory system: Â shortness of breath, pharyngitis;
Skin and subcutaneous tissues: Â skin rash;
Sensory organs: Â amblyopia.
In the treatment of partial seizures
The body as a whole: Â back pain, fatigue, fever, headache, viral infection, peripheral edema, weight gain, asthenia, – general malaise, facial edema;
Cardiovascular system: Â symptoms of vasodilation or hypertension;
The digestive tract: Â constipation, dental problems, diarrhea, dyspepsia, increased appetite, dry mouth or throat, nausea and / or vomiting, abdominal pain, flatulence, anorexia, gingivitis;
Blood system, lymphatic system: Â leukopenia, purpura (most often described as bruising caused by physical trauma);
Musculoskeletal system: Â fractures, myalgia, and arthralgia.
The nervous system: Â amnesia, ataxia, confusion, impaired coordination, depression, dysarthria, emotional lability, insomnia, nervousness, nystagmus, drowsiness, impaired thinking, tremor, muscle twitching, dizziness, hyperkinesis; increased, weakened or absent reflexes, paresthesia, anxiety, hostility;
Respiratory system: Â cough, pharyngitis, rhinitis, and pneumonia.
Skin and subcutaneous tissues: Â abrasions, wounds, itchy skin, skin rash;
Sensory organs: Â amblyopia, diplopia, visual impairment;
Genitourinary system: Â urinary tract infection, impotence.
Morphine: when taking Gabapentin and morphine together, when morphine was taken 2 hours before use There was a 44% increase in the mean area under the pharmacokinetic AUC of Gabapentin compared to 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, and the pharmacokinetic characteristics of morphine did not change. The side effects of morphine co-administered with Gabapentin did not differ from those of morphine co-administered with placebo.
Interactions between Gabapentin and phenobarbital, phenytoin, valproic acid, and carbamazepine were not observed. The pharmacokinetics of Gabapentin at steady state are similar in healthy individuals and patients receiving other anticonvulsants.
Concomitant use of Gabapentin with oral contraceptives containing norethisterone and / or ethinyl estradiol was not accompanied by changes in the pharmacokinetics of both components.
Concomitant use of Gabapentin with antacids containing aluminum and magnesium is associated with a decrease in the bioavailability of Gabapentin by about 20%. Gabapentin is recommended to be taken approximately 2 hours after taking the antacid.
Probenecid does not affect the renal excretion of Gabapentin.
A slight decrease in the renal excretion of Gabapentin with concomitant use of cimetidine is probably not clinically relevant.
Inside, swallowing whole, regardless of food intake and drinking plenty of liquid. If it is necessary to reduce the dose, discontinue the drug or replace it with an alternative remedy, this should be done gradually for 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 be started immediately with a dose of 900 mg / day (300 mg 3 times a day) or during the first 3 days, the dose can be increased gradually to 900 mg / day. according to the following scheme:
Day 1: 300 mg once a day;
day 2: 300 mg twice a day;
day 3: 300 mg 3 times a day
Partial seizures
Adults and children over 12 years of age: the effective dose is 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 increase gradually 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 to avoid the resumption of seizures.
Dose selection for renal failure
Patients with renal insufficiency 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*>
* prescribe 300 mg every other day
Recommendations for patients undergoing hemodialysis
Patients on hemodialysis who have not previously taken Gabapentin are recommended to prescribe this drug in a saturating dose of 300-400 mg, and then apply it 200-300 mg every 4 hours of hemodialysis.
Symptoms: Â dizziness, double vision, speech disorders, drowsiness, lethargy, diarrhea.
Treatment:Â gastric lavage, taking activated charcoal, symptomatic therapy. Hemodialysis may be indicated for patients with severe renal insufficiency.
Although withdrawal symptoms with seizures have not been reported during Gabapentin treatment, abrupt discontinuation of antiepileptic drug therapy in patients with partial seizures may lead to seizures.
Gabapentin is not considered an effective treatment for absence epilepsy.
Patients who require co-use of morphine may need to increase the dose of Gabapentin. At the same time, it is necessary to ensure careful monitoring of patients for the development of such a sign of central nervous system (CNS) depression as drowsiness. In this case, the dose of Gabapentin or morphine should be adequately reduced.
Laboratory tests
When Gabapentin was added to other anticonvulsants, false positive results were reported when determining protein in the urine using Ames N-Multistix SG®test strips. To determine protein in the urine, it is recommended to use a more specific method of precipitation with sulfosalicylic acid. Patients should avoid driving a car, as well as performing work that requires rapid psychomotor reactions.
Capsules
Store the drug in a dry place protected from light at a temperature not exceeding 25°C. Keep out of reach of children.
life is 2 years. Do not use after the expiration date.
Gabapentin
By prescription
Capsules
Pregnant women as prescribed by a doctor, Adults as prescribed by a doctor, Children as prescribed by a doctor, Children over 12 years of age
Epilepsy
Out of stock
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