Composition, form of production and packaging
Capsules of yellow color, size 1; the contents of the capsules are a white crystalline powder.
1 caps.
gabapentin 300 mg
Excipients: lactose monohydrate, corn starch, talc.
The composition of the shell of the capsule: titanium dioxide (E171), iron oxide, yellow oxide (E172), gelatin.
10 pieces. - blisters (5) - packs of cardboard.
Capsules of orange color, size в„–0; the contents of the capsules are a white crystalline powder.
1 caps.
gabapentin 400 mg
Excipients: lactose monohydrate, corn starch, talc.
The composition of the capsule shell: titanium dioxide (E171), iron oxide pigment yellow (E172), iron oxide red (E172), gelatin.
10 pieces. - blisters (5) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
Anticonvulsant drug. Gabapentin is similar in structure to the neurotransmitter GABA (GABA), but its mechanism of action differs from that of some other drugs interacting with GABA receptors, including valproate, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA capture inhibitors, GABA agonists and prodrugs 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? 2 -? - 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, inhibition of the release of neurotransmitters of the monoamine group.
Gabapentin does not bind to receptors of other common drugs or neurotransmitters, including GABA A receptors, GABA B , benzodiazepine, glutamate, glycine or N-methyl-D-aspartate at clinically significant concentrations.
Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels.
PHARMACOKINETICS
Suction
The bioavailability of gabapentin is not proportional to the dose, as the dose is increased, it decreases. After ingestion C max gabapentin in plasma is achieved after 2-3 hours. Absolute bioavailability of gabapentin in capsules is about 60%. Food, incl. 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. C ss in plasma can be determined based on the results of a single dose of the drug. Gabapentin practically does not bind to plasma proteins (<3%). V d - 57.7 l.
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
T 1/2 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.
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). Efficacy and safety in patients under the age of 18 years are not established;
- monotherapy of partial seizures in 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 tool 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.
DOSING MODE
The preparation of Katen В® is prescribed inside, regardless of the meal. 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 daily dose is 900 mg (in 3 divided doses); if necessary, depending on the effect, the dose is gradually increased to a maximum of 3.6 g / day. Treatment can begin immediately with a dose of 900 mg / day (300 mg 3 times / day) or within the first 3 days the dose can be increased gradually to 900 mg per day according to the following scheme:
- 1st day: 300 mg once a day;
- 2nd day: 300 mg 2 times / day;
- Day 3: 300 mg 3 times / day.
Partial cramps
Adults and children over the age of 12 years
The effective dose is from 900 mg to 3.6 g per day. Therapy can be started with a dose of 300 mg 3 times / day on the first day or increased gradually to 900 mg according to the scheme described above (see Neuropathic Pain in Adults). Subsequently, the dose can be increased to a maximum of 3.6 g / day in 3 divided 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 4.8 g / 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 / day and increased 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 inchildren aged 3 to 5 years is 40 mg / kg / day in equal doses in 3 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 В® 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 3 divided doses.
** Assign 300 mg every other day.
Patients who are on hemodialysis who have not previously taken gabapentin, it is recommended to prescribe the drug at a saturating dose of 300-400 mg, and then apply it at 200-300 mg every 4 hours of hemodialysis.
SIDE EFFECT
From the cardiovascular system: symptoms of vasodilation, hypertension.
From the digestive system: indigestion, flatulence, nausea, vomiting, abdominal pain, constipation, diarrhea, dry mouth or throat, anorexia, gingivitis, dental diseases, increased appetite, increased activity of hepatic transaminases.
From the musculoskeletal system: myalgia, arthralgia, back pain, increased brittle bone.
From the nervous system: drowsiness, dizziness, ataxia, amnesia, confusion, impaired coordination, fatigue, impaired thinking, tremor, hypoesthesia, depression, dysarthria, insomnia, nervousness, nystagmus, strengthening, weakening or lack of reflexes, asthenia, anxiety, hostility, hyperkinesia, emotional lability.
On the part of the respiratory system: pharyngitis, rhinitis, shortness of breath, cough, pneumonia, bronchitis, respiratory infections.
From the genitourinary system: urinary tract infections, impotence.
From the sense organs: visual impairment, amblyopia, diplopia.
On the part of the organs of hematopoiesis: leukopenia, purpura (most often it is described as bruising that occurs during physical trauma).
Allergic reactions: skin rash, itching, acne.
Other: fever, viral infection, weight gain, pain of different localization, 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 blood glucose concentration in patients with diabetes mellitus, chest pain, an increase in the volume of mammary glands, gynecomastia, an increase in liver function parameters, multiform erythema exudative (including Stevens-Johnson syndrome), hallucinations, motor disorders such as choreoathetosis , dyskinesia and dystonia, palpitation, pancreatitis, tinnitus, thrombocytopenia, incontinence, myoclonus.
CONTRAINDICATIONS
- children's age till 3 years;
- hypersensitivity to gabapentin or auxiliary components of the drug.
With caution should prescribe the drug for kidney failure.
PREGNANCY AND LACTATION
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.
Gabapentin is excreted in breast milk, so during treatment should abandon breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution should prescribe the drug for kidney failure.
Patients who are on hemodialysis who have not previously taken gabapentin, it is recommended to prescribe the drug at a saturating dose of 300-400 mg, and then apply it at 200-300 mg every 4 hours of hemodialysis.
APPLICATION FOR CHILDREN
Contraindicated in childhood up to 3 years.
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 CNS depression, like drowsiness. In this case, the dose of gabapentin or morphine should be adequately reduced.
With the joint use of gabapentin and other anticonvulsants, false positive results were detected in the determination of protein in the urine using Ames N-Multistix SGВ® test strips. To determine the protein in the urine it is recommended to use a more specific method of precipitation with sulfosalicylic acid.
Impact on the ability to drive vehicles and manage mechanisms
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.
OVERDOSE
Symptoms: dizziness, double vision, speech impairment, drowsiness, lethargy and diarrhea.
Treatment: gastric lavage, reception of activated charcoal, symptomatic therapy. Patients with severe renal insufficiency can be shown hemodialysis.
DRUG INTERACTION
With the simultaneous use of gabapentin and morphine, when morphine was taken 2 hours prior to gabapentin administration, the mean value of gabapentin AUC increased 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 remain unchanged. The side effects of morphine when taken together with gabapentin did not differ from those when taking morphine together with placebo.
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 ethinylestradiol 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%. It is recommended to take gabapentin approximately 2 hours after taking the 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.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 3 years. Do not use after the expiration date.
