Catena caps 300 mg No. 100

Compound

Directions for use and doses

Inside, regardless of food intake. If it is necessary to reduce the dose, discontinue the drug, or replace it with an alternative agent, this should be done gradually over a period of at least 1 week.

Neuropathic pain in adults. The initial dose is 900 mg/day in 3 divided doses; if necessary, depending on the effect, 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:

1st day - 300 mg 1 time per day;

2nd day - 300 mg 2 times a day;

Day 3 - 300 mg 3 times a day.

Partial seizures. Adults and children over 12 years of age: effective dose is from 900 to 3600 mg/day. Therapy can be started with a dose of 300 mg 3 times a day on day 1 or increased gradually to 900 mg according to the regimen described above (see Neuropathic pain in adults). Subsequently, the dose can be increased to a maximum of 3600 mg/day in 3 divided doses in equal doses. The maximum interval between doses when taking the drug 3 times should not exceed 12 hours to avoid resumption of seizures. The drug was well tolerated in doses up to 4800 mg/day.

Children aged 3–12 years: the initial dose of the drug varies from 10 to 15 mg/kg/day, which is prescribed in equal doses 3 times a day and increased to an effective dose over approximately 3 days. The effective dose of gabapentin in children aged 5 years and older is 25–35 mg/kg/day in equal doses in 3 divided doses. The effective dose of gabapentin in children aged 3 to 5 years is 40 mg/kg/day in equal doses in 3 divided doses. The drug was well tolerated in doses up to 50 mg/kg/day with long-term use. The maximum interval between doses of the drug should not exceed 12 hours to avoid resumption of seizures.

There is no need to monitor gabapentin plasma concentrations. Catena® can be used in combination with other anticonvulsants without taking into account changes in its plasma concentration or serum concentrations of other anticonvulsants.

Dose selection for renal failure

In patients with renal failure, a dose reduction of gabapentin is recommended according to the table:

* The daily dose should be administered in 3 divided doses.

** Prescribed 300 mg every other day.

Recommendations for patients undergoing hemodialysis

For patients on hemodialysis who have not previously taken gabapentin, it is recommended to prescribe the drug at a loading dose of 300–400 mg, and then use it at 200–300 mg every 4 hours of hemodialysis.

Catena caps 300 mg No. 100

Compound

Active substance: gabapentin - 300 mg. Excipients: lactose monohydrate, corn starch, talc.

Pharmacokinetics

Gabapentin is absorbed from the gastrointestinal tract.
After oral administration, Cmax of gabapentin in plasma is achieved within 2-3 hours. Absolute bioavailability is about 60%. Taken simultaneously with food (including high-fat food) does not affect the pharmacokinetics of gabapentin. Gabapentin does not bind to plasma proteins and has a Vd of 57.7 l. In patients with epilepsy, gabapentin concentrations in the cerebrospinal fluid are 20% of the corresponding plasma Css at the end of the dosing interval.

Gabapentin is excreted only by the kidneys. T1/2 does not depend on the dose and averages 5-7 hours.

The clearance of gabapentin is reduced in the elderly and in patients with impaired renal function. The elimination rate constant, plasma and renal clearance of gabapentin are directly proportional to creatinine clearance.

Gabapentin is removed from plasma during hemodialysis.

Gabapentin plasma concentrations in children were similar to those in adults.

Indications for use

Treatment of neuropathic pain in adults aged 18 years and older.
Efficacy and safety in patients under 18 years of age have not been established. Monotherapy for partial seizures in epilepsy with and without secondary generalization in adults and children over 12 years of age. The effectiveness and safety of monotherapy in children under 12 years of age have not been established.

As an additional remedy in the treatment of partial seizures in epilepsy with and without secondary generalization in adults and children aged 3 years and older. The safety and effectiveness of adjunctive gabapentin therapy in children less than 3 years of age have not been established.

Contraindications

• Hypersensitivity to gabapentin or auxiliary components of the drug. Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.
• Epilepsy
• Use as monotherapy for partial seizures with and without secondary generalization in children under 12 years of age.
• Use as an additional agent in the treatment of partial seizures with and without secondary generalization in children under 3 years of age.
• Neuropathic pain
• For the treatment of neuropathic pain in children and adolescents under 18 years of age.

With caution: renal failure (see section "Method of administration and dosage").

Directions for use and doses

The drug Catena® is prescribed orally, regardless of food intake. The capsule should be swallowed whole with sufficient liquid. If it is necessary to reduce the dose, discontinue 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 dose is 900 mg per day in three divided doses; if necessary, depending on the effect, the dose is gradually increased to a maximum of 3600 mg/day. It should be taken into account that when using gabapentin at a dose of more than 1800 mg/day, additional effectiveness was not observed.

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:

• Day 1: 300 mg once a day
• Day 2: 300 mg 2 times a day
• Day 3: 300 mg 3 times a day

Partial seizures

Epilepsy usually requires long-term treatment. The dose of the drug is determined by the attending physician depending on individual tolerability and effectiveness of the drug.

Adults and children over 12 years of age: the effective dose is from 900 to 3600 mg per day. Therapy can be started with a dose of 300 mg 3 times a day on the first day or increased gradually to 900 mg according to the regimen described above (see subsection “Neuropathic pain in adults”). Subsequently, the dose can be increased to a maximum of 3600 mg/day in three divided doses in equal doses. The maximum interval between doses when taking the drug three times should not exceed 12 hours to avoid resumption of seizures. The drug was well tolerated in doses up to 4800 mg/day.

Children aged 3-12 years: the initial dose of the drug varies from 10 to 15 mg/kg/day, which is prescribed in equal doses 3 times a day and increased to an effective dose over approximately 3 days. The effective dose of gabapentin in children aged 5 years and older is 25-35 mg/kg/day in equal doses in three doses. The effective dose of gabapentin in children aged 3 to 5 years is 40 mg/kg/day in equal doses in three doses. The drug was well tolerated in doses up to 50 mg/kg/day with long-term use. The maximum interval between doses of the drug should not exceed 12 hours to avoid resumption of seizures.

There is no need to monitor the concentration of gabapentin in the blood plasma. The drug Catena® can be used in combination with other anticonvulsants without taking into account changes in its concentration in the blood plasma or the concentration of other anticonvulsants in the serum.

Patients in serious condition

For the treatment of patients in severe condition, for example, in the case of underweight, after organ transplantation, etc., the dose should be increased more slowly, either using smaller doses or taking longer intervals before increasing the dose.

Elderly patients (over 65 years old)

Due to age-related decline in renal function, elderly patients may require dosage adjustments (see Table 3 for more details). Drowsiness, peripheral edema and asthenia may be more common in elderly patients.

Dose selection for renal failure

In patients with renal failure, a dose reduction of gabapentin is recommended according to Table 1:

* The daily dose should be administered in three doses.

** Prescribed 300 mg every other day.

*** In patients with a creatinine clearance <15 ml/min, the daily dose should be reduced in proportion to the creatinine clearance (for example, a patient with a creatinine clearance of 7.5 ml/min should take half the dose that a patient with a creatinine clearance of 15 ml/min receives).

Recommendations for patients undergoing hemodialysis

For patients on hemodialysis who have not previously taken gabapentin, it is recommended to prescribe the drug at a loading dose of 300-400 mg, and then use it at 200-300 mg every 4 hours of hemodialysis.

For patients with reduced renal function undergoing dialysis, the maintenance dose of gabapentin should be adjusted according to the recommendations presented in Table 3. In addition to maintenance therapy, 200-300 mg of gabapentin is recommended after each 4-hour dialysis session.

Storage conditions

Store out of the reach of children at a temperature not exceeding 25°C.

Best before date

3 years. Do not use after the expiration date.

special instructions

Suicidal thoughts and behavior
Antiepileptic drugs, including gabapentin, may increase the risk of suicidal thoughts or behavior. A meta-analysis of randomized placebo-controlled trials of antiepileptic drugs demonstrated a small increase in the risk of suicidal ideation and behavior. The mechanism for increasing this risk is unknown, but for gabapentin it cannot be excluded. Therefore, patients receiving these drugs should be closely monitored for new or worsening depression, the emergence of suicidal thoughts or behavior, and any changes in behavior. Patients or their caregivers should seek medical attention if signs of suicidal thoughts or behavior occur.

Acute pancreatitis

If acute pancreatitis occurs during the use of gabapentin, it is necessary to evaluate the possibility of discontinuing the drug.

Convulsions (syndrome “Interaction with other drugs”).

Respiratory depression

The use of gabapentin may be associated with severe respiratory depression. Patients most at risk are those with impaired respiratory function, respiratory or neurological disease, renal failure, concomitant use of CNS depressants, and elderly patients. Dose adjustment may be required for these patients.

Description

Anticonvulsant drug.

Dosage form

Yellow capsules, size No. 1; the contents of the capsules are white crystalline powder.

Use in children

The effectiveness and safety of treatment for neuropathic pain in patients under 18 years of age have not been established.
The effectiveness and safety of gabapentin monotherapy in the treatment of partial seizures in children under 12 years of age and adjunctive gabapentin therapy in the treatment of partial seizures in children under 3 years of age have not been established.

Pharmacodynamics

Antiepileptic drug.
Its chemical structure is similar to GABA, which functions as an inhibitory transmitter in the central nervous system. The mechanism of action of gabapentin is believed to be different from other anticonvulsants acting through the GABA synapse (including valproate, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA uptake inhibitors, GABA agonists and GABA prodrugs). In vitro studies have shown that gabapentin is characterized by the presence of a novel peptide binding site in rat brain tissue, including the hippocampus and cerebral cortex, which may be related to the anticonvulsant activity of gabapentin and its derivatives. Gabapentin in clinically significant concentrations does not bind to other conventional drugs and neurotransmitter receptors in the brain, incl. with GABAA-, GABAB-, benzodiazepine receptors, with NMDA receptors. The mechanism of action of gabapentin has not been definitively established.

Side effects

From the nervous system: amnesia, ataxia, confusion, impaired coordination of movements, depression, dizziness, dysarthria, increased nervous excitability, nystagmus, drowsiness, impaired thinking, tremor, convulsions, amblyopia, diplopia, hyperkinesia, increased, weakened or absent reflexes, paresthesia, anxiety, hostility, gait disturbance.
From the digestive system: changes in tooth staining, diarrhea, increased appetite, dry mouth, nausea, vomiting, flatulence, anorexia, gingivitis, abdominal pain, pancreatitis, changes in liver function tests.

From the hematopoietic system: leukopenia, decreased number of leukocytes, thrombocytopenic purpura.

From the respiratory system: rhinitis, pharyngitis, cough, pneumonia.

From the musculoskeletal system: myalgia, arthralgia, bone fractures.

From the cardiovascular system: arterial hypertension, manifestations of vasodilation.

From the urinary system: urinary tract infections, urinary incontinence.

Allergic reactions: erythema multiforme, Stevens-Johnson syndrome.

Dermatological reactions: skin maceration, acne, itching, rash.

Other: back pain, fatigue, peripheral edema, impotence, asthenia, malaise, facial swelling, weight gain, accidental injury, asthenia, flu-like syndrome, fluctuations in blood glucose, in children - viral infection, otitis media.

Use during pregnancy and breastfeeding

General risk associated with epilepsy and antiepileptic drugs
The risk of having children with congenital anomalies in mothers who are treated with anticonvulsants increases by 2-3 times. Most often, cleft lip and palate, malformations of the cardiovascular system and neural tube defects are observed. However, the simultaneous use of several anticonvulsants may be associated with a greater risk of developmental defects than in the case of monotherapy. Therefore, if possible, only one of the anticonvulsants should be used.

Women of childbearing age, and all women who may become pregnant, should seek advice from a qualified healthcare professional. If a woman is planning a pregnancy, the need for anticonvulsant therapy should be re-evaluated. However, anticonvulsant drugs should not be discontinued abruptly, as this can lead to resumption of seizures with serious consequences for the mother and child.

In rare cases, developmental delays have been observed in children whose mothers have epilepsy. It is not possible to determine whether the child's developmental delay is due to genetic or social factors, maternal illness, or anticonvulsant therapy.

Risk associated with gabapentin

There are no data on the use of gabapentin in pregnant women. The results of tests conducted on animals showed the toxicity of the drug to the fetus. People have no data regarding the possible risk. Therefore, gabapentin should be used during pregnancy only if the expected benefit to the mother significantly outweighs the possible risk to the fetus.

In the cases that have been reported, it is impossible to give a definitive conclusion about whether or not the use of gabapentin during pregnancy is accompanied by an increased risk of malformations, firstly, due to the presence of epilepsy itself, and secondly, due to the use of other anticonvulsants .

Breast-feeding

Gabapentin is excreted in breast milk, its effect on the nursing baby is unknown, therefore, during breastfeeding, the drug should be prescribed only if the benefit to the mother significantly outweighs the risk to the infant.

Fertility

Animal studies have not shown an effect of gabapentin on fertility.

Interaction

Spontaneous cases have been reported, and the literature suggests that respiratory depression and/or symptoms of sedation may be associated with gabapentin and opioid analgesics.
In some of these cases, the authors attributed these symptoms to the concomitant use of gabapentin and opioids, especially in elderly patients. When gabapentin 600 mg was administered 2 hours after administration of morphine 60 mg extended-release capsules, there was a 44% increase in the mean area under the gabapentin concentration-time curve (AUC) compared with gabapentin monotherapy, which was associated with an increase in pain threshold (cold pressor test). The clinical significance of this change has not been established; the pharmacokinetic characteristics of morphine did not change. The side effects of morphine when taken together with gabapentin did not differ from those when morphine was taken together with placebo. The extent to which these drugs interact at other doses is unknown.

No interactions were observed between gabapentin and phenobarbital, phenytoin, valproic acid and carbamazepine. The pharmacokinetics of gabapentin at steady state are similar in healthy subjects 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.

The simultaneous use of gabapentin with antacids containing aluminum and magnesium is accompanied by a decrease in the bioavailability of gabapentin by approximately 24%. It is recommended to take gabapentin approximately 2 hours after taking the antacid.

Probenecid does not affect the renal excretion of gabapentin.

The small decrease (14%) in renal excretion of gabapentin with concomitant use of cimetidine is probably not clinically significant.

With simultaneous use of naproxen (250 mg) and gabapentin (125 mg), an increase in gabapentin absorption from 12% to 15% was observed. Gabapentin has no effect on the pharmacokinetic parameters of naproxen. The indicated doses of drugs are less than the minimum therapeutic ones. The simultaneous use of these drugs in large doses has not been studied.

Overdose

With a single dose of 49 g of gabapentin, the following symptoms were observed: dizziness, double vision, speech impairment, drowsiness, loss of consciousness, lethargy and mild diarrhea, which completely disappeared with symptomatic therapy.
It should be taken into account that after taking high doses of gabapentin, its absorption in the intestine decreases.

An overdose of gabapentin may result in coma, especially with the simultaneous use of other drugs that depress the central nervous system (CNS).

Although gabapentin can be eliminated by hemodialysis, current experience shows that this is not usually necessary. Hemodialysis may be indicated in patients with severe renal failure.

In experiments on mice and rats, to which the drug was administered in doses of up to 8000 mg/kg, it was not possible to establish the lethal dose of gabapentin when administered orally. Signs of acute toxicity in animals included ataxia, difficulty breathing, ptosis, hypoactivity or agitation.

Impact on the ability to drive vehicles and operate machinery

While taking the drug, patients are not recommended to drive vehicles or engage in potentially hazardous activities that require increased concentration and speed of psychomotor reactions, until it is confirmed that there is no negative effect of the drug on the performance of these functions. Gabapentin affects the central nervous system and may cause dizziness, drowsiness, confusion, loss of consciousness, or other central nervous system symptoms. Even if mild or moderate, these undesirable effects can be potentially dangerous for patients driving vehicles or operating machinery. This likelihood is especially high at the beginning of treatment or after increasing the dose of the drug.