Expiration date: 04/2027

Composition

Capsules 300 mg. One capsule contains active substance: Gabapentin 300 mg

Excipients: lactose monohydrate; corn starch; talc

shell: titanium dioxide (E171); dye iron oxide yellow (E172); gelatin

Capsules 400 mg. One capsule contains active substance: Gabapentin 400 mg

Excipients: lactose monohydrate; corn starch; talc

shell: titanium dioxide (E171); dye iron oxide yellow (E172); dye iron oxide red (E172); gelatin

The drug forms

300 mg capsules: white crystalline powder in the capsule shell yellow, size 1.

400 mg capsules: white crystalline powder in the capsule shell orange size 0.

pharmachologic effect

Mode of action - antiepileptic.

pharmacodynamics

Gabapentin is structurally similar to the neurotransmitter GABA but its mechanism of action differs from that of some other drugs that interact with GABA receptors, including valproate, barbiturates, benzodiazepines, inhibitors of GABA-transaminase reuptake inhibitors GABA agonists, GABA prodrugs of GABA: it does not GABAergic properties and has no effect on capture and GABA metabolism. Preliminary studies showed that gabapentin binds to ?2-?-subunit voltazhzavisimyh calcium channels and inhibits the flow of calcium ions, which plays an important role in the onset of neuropathic pain. Other mechanisms involved in the action of gabapentin for neuropathic pain are glutamatzavisimoy reduction in neuronal death, increasing the synthesis of GABA, inhibition of monoamine neurotransmitter release group. Gabapentin at clinically relevant concentrations, does not bind to receptors or other drugs common neurotransmitters, including GABA receptors, GABAB, benzodiazepine, glutamate, glycine, or N-methyl-D-aspartate. Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels.

Pharmacokinetics

Suction

The bioavailability of gabapentin is not proportional to dose; Thus, with increasing dose is reduced. After oral administration, Cmax of gabapentin in plasma achieved in 2-3 hours. The absolute bioavailability of gabapentin capsules is approximately 60%. Foods including with a high content of fat, it has no effect on pharmacokinetics. Excretion of gabapentin plasma is best described by a linear model.

Distribution

Pharmacokinetics does not change with repeated use; Css plasma can be predicted on the basis of the results of a single dose. Gabapentin is almost bound to plasma proteins (<3%) and Vd is 57.7 liters.

Metabolism

Signs in human metabolism were found. The drug does not induce liver oxidative enzymes mixed function involved in the metabolism of drugs.

breeding

T1 / 2 of plasma is independent of dose and averages 5-7 hours. Displayed only kidneys unchanged.

Pharmacokinetics in special clinical situations

Clearance from plasma gabapentin reduced in the elderly and patients with impaired renal function. The constant rate of excretion, clearance from the plasma and renal clearance are directly proportional to creatinine Cl. Gabapentin is removed from plasma by hemodialysis. In patients with impaired renal function and patients receiving hemodialysis, dose adjustment is recommended (see. "Dosage and administration"). It is found that the plasma concentration of gabapentin in children between the ages of 4 and 12 are generally similar to those in adults.

Indications Katena® drug

• Treatment of neuropathic pain in adults 18 years and older (efficacy and safety in patients below the age of 18 years have not been established);
  
• monotherapy of partial seizures in epilepsy with secondary generalization and without adults and children over the age of 12 years (effectiveness and safety of monotherapy in children have not been established in the age of 12);
  
• as an additional tool in the treatment of partial seizures in epilepsy with secondary generalization and without adults and children aged 3 years and older (safety and efficacy of gabapentin adjunctive therapy in children aged less than 3 years have not been established).
  

Contraindications

• Hypersensitivity to gabapentin or auxiliary components of the drug;
  
• Children up to age 3 years.
  

Precautions: renal impairment (see "Dosage and Administration".).

Pregnancy and breast-feeding

Data on the safety and efficacy of the drug in pregnancy, so the use of gabapentin during pregnancy is possible only if the expected benefit to the mother justifies the potential risk to the fetus.

Gabapentin is excreted in breast milk, so during treatment should abandon breastfeeding.

Side effects

From the CCC: vasodilation symptoms of hypertension.

From the digestive system: dyspepsia, flatulence, nausea, vomiting, abdominal pain, constipation, diarrhea, dry mouth or throat, anorexia, gingivitis, dental disease, increase in appetite, increase in liver transaminases.

From the musculoskeletal system: myalgia, arthralgia, back pain, increased fragility of bones.

CNS: drowsiness, dizziness, ataxia, amnesia, confusion, loss of coordination, fatigue, abnormal thinking, tremor, hypoesthesia, depression, dysarthria, insomnia, nervousness, nystagmus, strengthening, weakening or absence of reflexes, fatigue, anxiety, hostility , hyperkinesia, emotional lability.

The respiratory system: pharyngitis, rhinitis, dyspnea, cough, pneumonia, bronchitis, respiratory infection.

With the genitourinary system: urinary tract infection, impotence.

From the senses: blurred vision, amblyopia, diplopia.

From the side of hematopoiesis: leukopenia, purpura (often it is described as bruising, occurred when a physical injury).

Allergic reactions: skin rash, itching, acne.

Other: fever, viral infection, weight gain, pain of various localization, peripheral edema, facial edema, headache.

Post-registration experience

Cases of sudden unexplained death, whose connection with the treatment with gabapentin has not been established. Other adverse events: Acute renal failure, allergic reactions, including urticaria, alopecia, angioedema, generalized edema; fluctuations in blood glucose levels in diabetic patients, chest pain, an increase in the volume of the breast, gynecomastia, increased liver function tests, erythema multiforme exudative (including Stevens-Dzhoneona syndrome), hallucinations, movement disorders such as choreoathetosis , dyskinesia and dystonia, palpitations, pancreatitis, tinnitus, anemia, urinary incontinence, myoclonus.

Interaction

With simultaneous use of gabapentin and morphine when morphine was taken 2 hours prior to gabapentin, the increase observed average AUC of gabapentin by 44% compared to a monotherapy gabapentin that was associated with an increase in pain threshold (cold pressor test). The clinical significance of this change is not established, the pharmacokinetic characteristics of morphine is not changed. Side effects of morphine during coadministration with gabapentin did not differ from that of morphine when taking in conjunction with the placebo.

The interaction between gabapentin and phenobarbital, phenytoin, carbamazepine and valproic acid were observed. The pharmacokinetics of gabapentin in the equilibrium state is the same 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 the two components.

The simultaneous use of gabapentin with antacids that contain aluminum and magnesium, followed by reduction of gabapentin bioavailability by approximately 20%. Gabapentin is recommended to take approximately 2 hours after antacids.

Probenecid does not affect the renal excretion of gabapentin.

A slight decrease in renal excretion of gabapentin while taking cimetidine probably have no clinical significance.

Dosing and Administration

Inside, regardless of meals. If you need to reduce the dose, stop the drug or replace it with an alternative means, it should be done gradually over a minimum of 1 week.

Neuropathic pain in adults. The initial dose is 900 mg / day in 3 divided doses equal doses; if necessary, depending on the effect of gradually increasing the dose until a maximum - 3600 mg / day. Treatment can be started immediately with a dose of 900 mg / day (300 mg 3 times daily) or within the first 3 days, the dose can be increased gradually to 900 mg / day as follows:

1st day - 300 mg 1 time per day;

Day 2 - 300 mg 2 times a day;

3rd day - 300 mg 3 times a day.

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

Children aged 3-12 years: initial dose varies from 10 to 15 mg / kg / day, which is administered in equal doses three times a day and to increase effective for about 3 days. The effective dose of gabapentin in children aged 5 years and older is 25-35 mg / kg / day in 3 equal doses reception. The effective dose of gabapentin in children aged 3 to 5 years is 40 mg / kg / day in 3 equal doses reception. It was well tolerated in doses up to 50 mg / kg / day for prolonged use. The maximum interval between doses of the drug dose should not exceed 12 hours in order to avoid the resumption of seizures.

There is no need to control the concentration of gabapentin in plasma. Katena® drug may be used in combination with other anticonvulsants excluding changes in its concentration in plasma or other anticonvulsants concentration in serum.

Selection of doses in renal failure

Patients with renal impairment is recommended to decrease the dose of gabapentin according to the table:

Cl creatinine, ml / min	Daily dose, mg / day *
>80	900–3600
50–79	600–1800
30–49	300–900
15–29	150**–600
<15	150**–300

* The daily dose should be administered in 3 doses.

** Assign to 300 mg every other day.

The recommendations for patients on hemodialysis

Patients on hemodialysis who had not previously received gabapentin, a drug is recommended to be administered in a saturating dose of 300-400 mg, and then apply it to 200-300 mg every 4 hours of hemodialysis.

Overdose

Symptoms: dizziness, double vision, impaired speech, drowsiness, lethargy and diarrhea.

Treatment: gastric lavage, activated charcoal, symptomatic therapy. Patients with severe renal insufficiency, hemodialysis may be indicated.

special instructions

When co-therapy in patients morphine may occur increasing the concentration of gabapentin. It is necessary to ensure thorough monitoring of patients for the development of such a feature of CNS depression, drowsiness. In this case, the dose of gabapentin or morphine should be reduced appropriately (see. "Interaction").

Laboratory research

When combined gabapentin and other anticonvulsants were reported false positive results in the determination of protein in urine using test strips Ames N-Multistix SG®. For the determination of protein in urine it is recommended to use more specific sulfosalicylic acid precipitation method.

Effects on ability to drive or to perform work requiring higher rate of physical and mental reactions. In the period of treatment should refrain from driving motor vehicles and activities potentially hazardous activities that require high concentration and psychomotor speed reactions.

release Form

Capsules, 300 mg and 400 mg. On 10 caps. PVC / aluminum blister. 5 blisters placed into cardboard boxes.

Manufacturer

Belupo, medications and cosmetics dd, Croatia. 48000, Koprivnica, ul. Danica, 5.

Representation Belupo, medications and cosmetics dd, the Republic of Croatia in Russia: 119330, Moscow Lomonosov Ave, 38, Apt. 71-72.

Phone: +7 (495) 933-72-13 Fax: +7 (495) 933-72-15

e-mail: [email protected]

Conditions of supply of pharmacies

On prescription.

Storage conditions Katena® drug

The temperature is not above 25 ° C.

Keep out of the reach of children.

The shelf life of the drug Katena®

3 years.

Do not use beyond the expiration date printed on the package.