Expiration date: 07/2028
Structure and Composition:
The capsules. One capsule contains Gabapentin 100, 300 or 400 mg
Excipients: capsule contents: lactose monohydrate, pregelatinised starch magnesium stearate, talc
hard gelatin capsule: yellow iron oxide red iron oxide, titanium dioxide, gelatin
in blister 10 pcs. 5 in a pack or carton 10 blisters.
Description pharmaceutical form:
Capsules 100 mg. The contents of the capsule: white or almost white crystalline powder. Capsules: Size ?3, Coni-Snap, upper part - pinkish-brown color, the lower part - white.
Capsules 300 mg. The contents of the capsule: white or almost white crystalline powder. Capsules: size ?1, Coni-Snap, upper part - pinkish-brown color, the lower part - a pale yellow color.
Capsules 400 mg. The contents of the capsule: white or almost white crystalline powder. Capsules: size, Coni-Snap, upper part - pinkish-brown color, the lower part - a yellowish-orange color.
Characteristic:
A lipophilic compound having a structural similarity to the neurotransmitter GABA.
Pharmacokinetics:
Bioavailability is not proportional to dose: decreases with increasing dose and is approximately 60% - after repeated (three times per day) for the treatment methods recommended doses of 300-600 mg, and about 30% - at doses 1600 mg. Absorption is fast, Tmax - 3 hours Eating, incl. fat, has no significant effect on bioavailability, while AUC and Cmax increased by approximately 14%. When receiving doses of 300-4800 mg of mean values ??Cmax and AUC increased with increasing dose.
When receiving a single dose of gabapentin plasma concentration of the drug in children 4-12 years is similar to that of adult patients. Repeated receptions equilibrium concentration in blood is reached after 1-2 days and is maintained throughout the course of treatment. In children aged 1 month to 5 years AUC value about 30% lower than in the older age group (dose range: single - 10 mg / kg three times - 10-65 mg / kg per day).
Table 1
The pharmacokinetic performance of gabapentin at steady state after repeated application every 8 hours
| Index | 300 mg | 400 mg |
| Cmax (mcg/ml) | 4,02 | 5,50 |
| Tmax (h) | 2,7 | 2,1 |
| T1/2 (h) | 5,2 | 6,1 |
| AUC (0 — &infin)(mcg·h/ml) | 24,8 | 33,3 |
| Ae* (%) | no data | 63,6 |
* Ae - the amount of gabapentin, urinary excretion
Gabapentin does not bind to blood proteins, volume of distribution - 57.7 liters. It passes through the BBB, enters the breast milk. Concentration in CSF is 20% of the equilibrium concentration in the plasma. Metabolism in human liver gabapentin immaterial, gabapentin does not cause induction of liver enzymes involved in oxidative processes. T1 / 2 -. 7.5 h T1 / 2 and the renal clearance is independent of dose and after repeated administration remain unchanged. Write mainly in the urine (80%) and faeces (20%).
Age-related changes in renal function in elderly patients, as well as kidney disease, manifested in the reduction in creatinine clearance, leads to a decrease in plasma clearance of gabapentin and an increase in T1 / 2. rate of excretion, plasma and renal clearance of gabapentin reduced in proportion to the decrease in creatinine clearance. In patients with reduced renal function or undergoing hemodialysis is recommended to decrease doses of gabapentin in accordance with creatinine clearance.
Description of the pharmacological actions:
At therapeutic concentrations does not bind to GABAB and GABAA receptors, benzodiazepine, glutamate, glycine, N-methyl-D-aspartate. It shows high activity against brain receptors associated with & alpha and structures & delta-voltage-sensitive calcium channels. In vitro identified new peptide receptors in the brain tissue, through which can be mediated anticonvulsant activity of gabapentin and its derivatives (structure and function of receptors gabapentinovyh not fully understood).
Indications:
epilepsy:
- Adults and children over 12 years - as a monotherapy or in combination therapy for the treatment of partial seizures, including proceeding with secondary generalization
- Children from 3 to 12 years - in a combination therapy for the treatment of partial seizures, including proceeding with secondary generalization
- neuropathic pain (neuralgia) in adults.
Contraindications:
- hypersensitivity to the drug
- acute pancreatitis
- Children up to age 3 years.
Application of pregnancy and breastfeeding:
When pregnancy is possible only after a careful assessment of the possible risks and benefits of treatment (due to lack of sufficient clinical experience). When breastfeeding is possible only if the expected therapeutic effect is clearly surpass the degree of danger that the child will be exposed to (gabapentin passes into breast milk, it is impossible to eliminate the risk of serious adverse effects in infants).
Side effect:
CNS: drowsiness (10.6%), dizziness (10.2%), impaired coordination of movements (ataxia), nystagmus, blurred vision (diplopia, amblyopia), headache, tremor, dysarthria, amnesia, abnormal thinking, depression , anxiety, emotional lability, impaired consciousness, irritability, increased nervous irritability, tics, hypo- or areflexia, decreased sensitivity in children younger than 12 years - the hostility and hyperkinesis.
Since the cardiovascular system: an increase or decrease in blood pressure, feeling of rush of blood to the face, extremities warming.
From the digestive system: nausea, vomiting, anorexia, hemorrhagic pancreatitis, constipation, diarrhea, increased appetite, dry throat, gingivitis, loss of tooth enamel or discoloration, flatulence.
From the side of blood: leukopenia.
From the musculoskeletal system: arthralgia, increased fragility of bones, myalgia.
From the respiratory system: cough, pharyngitis, dyspnea, rhinitis.
From the senses: tinnitus.
Allergic reactions: fever, erythema multiforme, Stevens-Johnson syndrome.
For the skin: acne, pruritus.
From the urogenital system: urinary incontinence, impotence.
Laboratory indicators: change in blood glucose levels in clinically relevant range (blood glucose <3.3 or & ge7,8 mmol / l at a rate of 3.5-5.5 mmol / L), elevated liver transaminases.
Other: weight gain, peripheral edema, fatigue, purpura, swelling of the face, abdominal pain, back pain, fever, flu-like symptoms.
Drug Interactions:
When applied with antiepileptic drugs (including phenytoin, carbamazepine, valproic acid, phenobarbital) gabapentin does not change their levels in the blood.
When applied to oral contraceptive preparations, gabapentin has no effect on the action noretidron- and / or etinilestradiolsoderzhaschih contraceptives, but when administered in combination with other antiepileptic drugs, having the ability to reduce the effects of oral contraceptives, it should expect a decrease contraceptive effect.
Antacids containing aluminum or an acid-magnesium, 24% can reduce the bioavailability of gabapentin (gabapentin capsules should be taken no earlier than two hours after ingestion of antacids).
Cimetidine reduces renal elimination of gabapentin.
Alcohol and agents acting on the central nervous system, may increase the side effects of gabapentin on the part of the central nervous system.
Laboratory tests: the analysis of total protein in the urine with litmus paper possible false positive result. In such cases, you should confirm the result using another method of analysis (such as biuret reaction).
Dosage and administration:
Inside, with liquid squeezed the required amount of liquid, regardless of the meal.
Epilepsy
Adults and children over 12 years: usually effective dose of 900-1200 mg / day. Starting dose - 300 mg 3 times a day on the first day. The maximum dose - 3600 mg / day (equal to 3 admission). The maximum interval between doses in the appointment of the drug 3 times per day should not exceed 12 hours, the desired therapeutic blood levels of the drug can be achieved in a few days, using the recommended modes of drug administration.:
A. The first day - 300 mg (1 capsule for 300 mg 1 time per day, or 1 capsule of 100 mg 3 times a day..).
The second day - 600 mg (1 capsule at 300 mg 2 times a day, or 2 capsules of 100 mg 3 times a day..).
Third day - 900 mg (1 capsule at 300 mg three times a day, or three capsules of 100 mg three times a day..).
Fourth day - to increase the dose up to 1,200 mg for 3 doses, ie, 1 caps. 400 mg three times a day.
B. On the first day you can start with the reception 1 caps. 300 mg of 3 times, i.e. 900 mg / day. Then, the daily dose may be increased up to 1200 mg.
Depending on the resulting effect of the dose can be increased to a daily 300-400 mg, and the maximum daily dose, distributed into 3 doses, is 2400 mg, because currently there is not enough data on the effectiveness and safety of higher doses.
Treatment of children aged 3-12 years: The recommended dose for children over 5 years - 25-35 mg / kg / day, for children 3-4 years old - 40 mg / kg / day. The daily dose is divided into 3 doses. Recommended dose calculated per 1 kg of body weight are shown in Tables 2 and 3. The maximum daily dose in this age range is 35-40 mg / kg.
table 2
The initial dose of gabapentin for children 3-12 years
| Body Weight in kg | The daily dose, mg | First day | Seconf day | Third day |
| 17–25 | 600 | 200 mg 1 time a day | 200 mg 2 times a day | 200 mg 3 times a day |
| >26 | 900 | 300 mg 1 time a day | 300 mg 2 times a day | 300 mg 3 times a day |
Table 3
Maintenance doses of gabapentin for children aged 3-12 years
| The total daily dose, mg | |
| 17–25 | 600 | |
| 26–36 | 900 | |
| 37–50 | 1200 | |
| 51–72 | 1800 |
The course of treatment is carried out for a long time (2-3 years), then the dose is gradually reduced.
Treatment of neuropathic pain in adults
Given the resulting effect and tolerability of the drug, the physician establishes by its therapeutic dose titration. Depending on the individual response of the patient the maximum dose can be up to 3600 mg / day.
Recommended modes drug administration:
A. The first day - 300 mg (1 capsule for 300 mg 1 time per day, or 1 capsule of 100 mg 3 times a day..).
The second day - 600 mg (1 capsule at 300 mg 2 times a day, or 2 capsules of 100 mg 3 times a day..).
Third day - 900 mg (1 capsule at 300 mg three times a day, or three capsules of 100 mg three times a day..).
B. With a very intense pain in the first day, you can take 1 caps. 300 mg of 3 times, i.e. 900 mg / day. Then, within 1 week daily dose may be increased up to 1800 mg.
In some cases, a further increase in the dose may be required. The maximum daily dose of 3600 mg divided into 3 doses.
Debilitated patients, with low birth weight or organ transplant dose can be increased strongly at 100 mg per day.
Older patients in accordance with the age-related decrease in creatinine clearance, patients with renal insufficiency (Cl creatinine & le80 ml / min), patients on hemodialysis, the dose should be selected individually as follows (see Table 4..):
Table 4
The recommended dose of gabapentin in reducing kidney function
| Cl creatinine, ml / min | The daily dose for 3 doses in mg / day |
| >80 (norm) | 900–2400 |
| 50–79 | 600–1800 |
| 30–49 | 300–900 |
| 15–29 | 150*–600 |
| <15 | 150*–300 |
* Take a day on 100 mg 3 times a day
Patients on hemodialysis and earlier did not take gabapentin, it is recommended to appoint 300-400 mg loading dose, then every 4 hours of hemodialysis session to appoint 200-300 mg. In the days free from dialysis, can not take gabapentin.
The course of treatment - from 1 week to 1 month, depending on the severity of pain. The duration of treatment depends on the clinical response to therapy.
Overdose:
Symptoms: dizziness, double vision, drowsiness, dysarthria, diarrhea.
Treatment: gastric lavage, activated charcoal, symptomatic therapy. Elimination Gabapentin is excreted by hemodialysis possible.
Precautionary measures:
To apply caution during pregnancy and lactation, renal insufficiency.
In patients with diabetes need to control the level of glucose in the blood, sometimes there is a need to change the dose of antidiabetic drugs.
At the first signs of acute pancreatitis (long abdominal pain, nausea, repeated vomiting) gabapentin treatment should be discontinued. The patient must be carefully examined (clinical and laboratory tests) for early diagnosis of acute pancreatitis.
If lactose intolerance should be noted that 100 mg capsule contains 22.14 mg lactose 300 mg - 66.43 mg, 400 mg - 88.56 mg.
If necessary, reduce the dose or cancel the drug to replace it with an alternative means should gradually over a minimum of 1 week. Abrupt discontinuation of treatment may provoke status epilepticus.
Safety and efficacy of neuralgia therapy in patients aged less than 18 years have not been established. In the event of symptoms in adults somnolence, ataxia, dizziness, fatigue, nausea and / or vomiting, weight gain and drowsiness in children, hyperkinesia and hostility - discontinue treatment and consult a doctor.
During the period of treatment should refrain from driving and transport activities potentially hazardous activities that require high concentration and psychomotor speed reactions.
Special instructions:
When selecting the optimal therapeutic dose is not necessary in the measurement of drug concentrations in plasma.
The drug is ineffective in primary generalized seizures, such as absences.
Storage conditions:
(In original packaging).
