Active substanceGabapentinGabapentin
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  • Dosage form: & nbspcapsules
    Composition:

    One capsule contains:

    Capsules 100 mg: active substance: gabapentin - 100 mg; Excipients: lactose monohydrate, corn starch, talc; capsule shell: titanium dioxide (E 171), gelatin.

    Capsules 300 mg: active substance: gabapentin 300 mg; Excipients: lactose monohydrate, corn starch, talc; capsule shell: titanium dioxide (E 171), iron dye oxide yellow (E 172), gelatin.

    Capsules 400 mg: active substance: gabapentin 400 mg; Excipients: lactose monohydrate, corn starch, talc; capsule shell: titanium dioxide (E 171), iron oxide yellow dye (E 172), iron oxide red dye (E 172), gelatin.

    Description:

    Capsules 100 mg: white crystalline powder in a capsule shell of white color, size 3.

    Capsules 300 mg: white crystalline powder in a capsule shell of yellow color, size 1.

    Capsules 400 mg: white crystalline powder in capsule shell of orange color, size 0.

    Pharmacotherapeutic group:Antiepileptic remedy
    ATX: & nbsp

    N.03.A.X.12   Gabapentin

    Pharmacodynamics:Gabapentin structurally similar to the neurotransmitter (GABA) gamma-aminobutyric acid, 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 and pro dosage forms of GABA: it does not possess GABA-ergic properties and does not affect the capture and metabolism of GABA. Preliminary studies have shown that gabapentin binds to α2-δ-subunit of voltage-dependent calcium channels and suppresses the flow of calcium ions, which plays an important role in the occurrence of neuropathic pain. Other mechanisms involved in the action of gabapentin in neuropathic pain are: reduction of glutamate-dependent neuronal death, an increase in GABA synthesis, suppression of the release of neurotransmitters of the monoamine group. Gabapentin in clinically significant concentrations does not bind to receptors of other common drugs or neurotransmitters, including GABA receptorsA, GABAAT, 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 the dose; so, with an increase in the dose, it decreases. After oral administration, the maximum concentration (Cmax) gabapentin in plasma is achieved after 2-3 hours. 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.

    Distribution

    Pharmacokinetics does not change with repeated application; equilibrium concentrations in plasma can be predicted based on the results of a single dose of the drug. Gabapentin practically does not bind to plasma proteins (<3%) and has a volume distribution of 57.7 liters.

    Metabolism

    There are no signs of metabolism in humans. The drug does not induce oxidative liver enzymes with a mixed function involved in the metabolism of drugs.

    Excretion

    Half-life (T1/2) from the plasma does not depend on the dose and averages 5-7 hours. It is excreted exclusively by the kidneys in unchanged form.

    Pharmacokinetics in special clinical cases

    The clearance of gabapentin from plasma decreases in elderly people and in patients with impaired renal function. The rate of elimination constant, clearance from plasma and renal clearance are directly proportional to the creatinine clearance. Gabapentin is removed from the plasma during hemodialysis. In patients with impaired renal function and patients receiving hemodialysis treatment, dose adjustment is recommended (see Dosage and Administration).It has been established that concentrations of gabapentin in plasma in children aged 4 to 12 years are generally similar to those in adults.

    Indications:

    - Treatment of neuropathic pain in adults (18 years and older). Efficiency and. Safety in patients under the age of 18 years is not established.

    - Monotherapy of partial seizures with epilepsy with secondary generalization and without it in adults and children over the age of 12 years. The efficacy and safety of monotherapy in children under the age of 12 years are not established.

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

    Contraindications:Increased sensitivity to gabapentin or ancillary components of the drug. Children under 3 years.
    Carefully:Renal failure (see "Method of administration and dose").
    Pregnancy and lactation:

    Pregnancy

    Data on the safety and efficacy of the drug during pregnancy are not available, so the use of gabapentin in pregnancy is possible only if the intended benefit for the mother justifies the possible risk to the fetus.

    Lactation

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

    Dosing and Administration:

    The drug Catena® is prescribed internally, regardless of food intake. If it is necessary to reduce the dose, cancel 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 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. Treatment may start with a dose of 900 mg / day (300 mg 3 times a day) or within the first 3 days the dose may be increased gradually to 900 mg a day according to the following scheme:

    1st day: 300 mg once a day

    2nd day: 300 mg twice daily

    3rd day: 300 mg 3 times daily

    Partial cramps

    Adults and children over the age of 12: The effective dose is from 900 to 3600 mg per day. Therapy can begin 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 (see the section "Neuropathic pain in adults"). Subsequently, the dose can be increased to a maximum of 3600 mg / day in three doses in equal doses.The maximum interval between doses with a three-time intake of the drug should not exceed 12 hours in order to avoid the resumption of seizures. A good tolerability of the drug in doses up to 4800 mg / day was noted.

    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 raised to an effective rate for about 3 days. 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 three divided doses. A good tolerability of the drug in doses up to 50 mg / kg / day with long-term use was noted. The maximum interval between taking doses of the drug should not exceed 12 hours in order to avoid the resumption of seizures.

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

    Selection of a dose for renal failure

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

    Creatinine clearance (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 given in three divided doses.

    ** Assign 300 mg every other day.

    Recommendations for patients on hemodialysis

    Patients who are on hemodialysis who have not previously taken gabapentin, the drug is recommended to be prescribed in a saturating dose of 300-400 mg, and then apply it at 200-300 mg every 4 hours of hemodialysis.

    Side effects:

    From the cardiovascular system: symptoms of vasodilation, hypertension.

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

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

    From the nervous system: drowsiness, dizziness, ataxia, amnesia, confusion, impaired coordination, increased fatigue, impaired thinking, tremor, hypoesthesia, depression, dysarthria, insomnia,nervousness, nystagmus, strengthening, weakening or lack of reflexes, asthenia, anxiety, hostility, hyperkinesia, emotional lability.

    From the respiratory system: pharyngitis, rhinitis, dyspnea, cough, pneumonia, bronchitis, respiratory infections.

    From the genitourinary system: urinary tract infection, impotence.

    From the sense organs: impaired vision, amblyopia, diplopia.

    From the hematopoiesis: leukopenia, purpura (most often it is described as bruising that occurs with physical trauma).

    Allergic reactions: skin rash, itching, acne.

    Other: fever, viral infection, weight gain, pain of various locations, peripheral edema, edema of the face, headache.

    Post-registration application experience

    Cases of sudden unexplained death have been reported, whose association with treatment with gabapentin has not been established. Other adverse events: acute renal failure, allergic reactions, including hives, alopecia, angioedema, generalized edema; fluctuations in the concentration of glucose in the blood in patients with diabetes mellitus, chest pain, an increase in the volume of the mammary glands, gynecomastia,increased liver function, multiforme exudative erythema (including Stevens-Johnson syndrome), hallucinations, motor disorders such as choreoathetosis, dyskinesia and dystonia, palpitations, pancreatitis, tinnitus, thrombocytopenia, urinary incontinence, myoclonus.

    Overdose:

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

    Treatment: gastric lavage, reception of activated charcoal, symptomatic therapy. Patients with severe renal insufficiency can be shown hemodialysis.

    Interaction:

    With the simultaneous use of gabapentin and morphine, when morphine was taken 2 hours before taking gabapentin, an increase in the mean area under the pharmacokinetic concentration-time curve (AUC) of gabapentin by 44% was observed compared to gabapentin ionotherapy, 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 remain unchanged. The side effects of morphine when taken together with gabapentin did not differ from those when taking morphine together withplacebo.

    Interactions between gabapentin and phenobarbital, phenytoin, valproic acid and carbamazepine have not been observed. The pharmacokinetics of gabapentin in the equilibrium state 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 bioavailability of gabapentin by approximately 20%. Gabapentin it is recommended to take about 2 hours after taking an antacid. Probenecid does not affect renal excretion of gabapentin.

    A small decrease in renal excretion of gabapentin with simultaneous administration of cimetidine is probably of no clinical significance.

    Special instructions:

    When co-administered with morphine in patients, the concentration of gabapentin may increase. In this case, it is necessary to ensure close 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 (see "Interaction with other drugs").

    Laboratory research

    With the combined use of gabapentin and other anticonvulsants, false positive results were detected in the determination of protein in the urine 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.

    Effect on the ability to drive transp. cf. and fur:During the period of treatment it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:Capsules 100 mg, 300 mg, 400 mg.
    Packaging:

    Capsules 100 mg: For 10 capsules in PVC / Al blister. Two blisters are placed together with instructions for use in a cardboard box.

    Capsules 300 mg and 400 mg: For 10 capsules in PVC / Al blister. Five blisters are placed together with instructions for use in a cardboard box.

    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children!

    Shelf life:

    3 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-002168/10
    Date of registration:17.03.2010 / 07.06.2010
    Expiration Date:Unlimited
    The owner of the registration certificate:Beluga, medicines and cosmetics.Beluga, medicines and cosmetics. Croatia
    Manufacturer: & nbsp
    Representation: & nbspBeluga, medicines and cosmetics. Beluga, medicines and cosmetics. Croatia
    Information update date: & nbsp26.12.2017
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