GABAGAMMA

Active material: Gabapentin
When ATH: N03AX12
CCF: Anticonvulsants
ICD-10 codes (testimony): B02.2, G40, G63.2, R52.2
When CSF: 02.05.10
Manufacturer: WÖRWAG PHARMA GmbH & Co. KG (Germany)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Capsules hard gelatin, №3, white; contents of capsules – white powder.

Excipients: lactose, corn starch, talc, gelatin, Titanium dioxide, iron oxide yellow, iron oxide red.

10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (5) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.

Capsules hard gelatin, №1, yellow color; contents of capsules – white powder.

Excipients: lactose, corn starch, talc, gelatin, Titanium dioxide, iron oxide yellow, iron oxide red.

10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (5) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.

Capsules hard gelatin, №0, orange; contents of capsules – white powder.

Excipients: lactose, corn starch, talc, gelatin, Titanium oxide, iron oxide yellow, iron oxide red.

10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (5) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.

Pharmacological action

The antiepileptic drug. Gabapentin structure is similar to the neurotransmitter gamma-aminobutirovoj acid (GABA), However, its mechanism of action is different from other drugs, interact with GABA-receptor (valproate, barbiturates, benzodiazepines, GABA inhibitors-transaminases, capture GABA inhibitors, GABA agonists and prolekarstvennye forms of GABA). Lacks GABA-ergicheskimi properties and does not affect the capture and the metabolism of GABA.

Preliminary studies have shown, that Gabapentin binds to α₂-δ-subunit voltage-dependent calcium channels and reduces the flow of calcium ions, playing an important role in the occurrence of neuropathic pain. Other mechanisms of action of gabapentin in neuropathic pain are reduced glutamate-dependent neuronal death, increased synthesis of GABA, Suppresses the release of neurotransmitters monoaminovoj group. Gabapentin in clinically relevant concentrations does not bind to receptors or other common neurotransmitters, including GABA receptors_A, GABA_IN, benzodiazepinove, glutamatne and glicinovye NMDA receptors.

Unlike fenitoina and carbamazepine Gabapentin does not interact with sodium channels in vitro. Gabapentin partially relaxing effects of glutamate NMDA receptor agonist in some in vitro tests, but only in a concentration of more than 100 mmol, which is not achieved in vivo. Gabapentin slightly reduces the release of neurotransmitters in vitro monoaminovyh.

Pharmacokinetics

Absorption

After oral administration, C_max Gabapentin in plasma achieved through 2-3 no. Absolute bioavailability of gabapentin capsules is around 60%. Bioavailability of gabapentin is not proportional to dose. So, When increasing doses it decreases. Food, incl. with high content of fat, does not affect the farmakokinetiku.

Distribution and metabolism

Pharmacokinetics does not change when you reapply; equilibrium concentration in the plasma can be predicted on the basis of the results of a single dose of the drug.

Gabapentin is practically not associated with plasma proteins (<3%). V_d is 35.9 l.

Not metabolizmu. The drug does not induce oxidative liver enzymes with mixed function, involved in the metabolism of drugs.

Deduction

Excretion of gabapentin from plasma is best described by using linear model. T_1/2 from the plasma does not depend on the dose and is 5-7 no.

Pharmacokinetics in special clinical situations

Gabapentin is excreted exclusively kidney in an unmodified form.

Gabapentin reduced plasma clearance in the elderly and in patients with impaired renal function. The rate constant for breeding, clearance from plasma and kidney klirens is directly proportional to the QC. Gabapentin is removed from plasma during hemodialysis. In patients with impaired renal function and patients, receiving hemodialysis, recommended dose adjustment.

Testimony

-adults: pain syndrome in diabetic neuropathy, postgerpeticheskaya neuralgia;

-adults and children 12 and older: in the treatment of partial seizures with secondary generalization or without it.

Dosage regimen

The drug is taken orally with or without food. If you want to reduce your dose, Cancel product or replace it with an alternative means to, This should be done gradually over a minimum of one week.

In debilitated patients, as well as patients in grave general condition, with low body weight and after organ transplantation, the dose should be gradually using dosage 100 mg.

When bolevom syndrome in diabetic neuropathy, postherpetic neuralgia adult administered in an initial dose of 900 mg / day 3 receive equal doses. If necessary dose gradually increased to a maximum of- 3600 mg / day. Treatment also can start, gradually increasing the dose during the first three days, according to the following scheme: 1-Day – 300 mg 1 time / day; 2-Day – by 300 mg 2 times / day; 3-Day – by 300 mg 3 times / day.

In the treatment of partial seizures to Adults and children 12 and older effective dose of 900 mg / day to 3600 mg / day. Therapy can start with a dose of 300 mg 3 times/day in the 1-St day or increase gradually to 900 mg according to the scheme, above. In a further dose can be increased to 3600 mg/day divided into 3 reception in equal doses. In order to avoid the resumption convulsing the maximum interval between meals when prescribing medication 3 times / day should not exceed 12 no .

There is no need to monitor the concentration of gabapentin in plasma. Product Gabagamma^® can be used in combination with other protivosudorojnami means excluding changes in its concentration or the concentration of other antiepileptic drugs in plasma.

Patients with renal insufficiency recommended correction doses of gabapentin in accordance with table.

Assign 300 mg a day.

Patients, hemodialysis, who have not previously taken Gabapentin, the drug is recommended in saturating the dose 300-400 mg, and then – by 200-300 mg every 4 h hemodialysis. In debilitated patients, as well as in severe general condition, in patients with low body weight and after organ transplantation increased dosage Gabagamma^® should be gradually using dosage 100 mg.

Side effect

Cardio-vascular system: symptoms of vasodilation, increased blood pressure, heartbeat.

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

From the hematopoietic system: purpura (It is most commonly described as bruising, When physical injury), leukopenia, thrombocytopenia.

On the part of the musculoskeletal system: arthralgia, backache, increased fragility of bones, myalgia.

From the central and peripheral nervous system: dizziness, headache, hyperkinesis, muscular dyskinesia and Dystonia, Choreoathetosis, strengthening, weakening or absence of reflexes, dysarthria, ataxia, nistagmo, paresthesia, convulsions, confusion, fatigue, asthenia, amnesia, depression, aphronia, hostility, emotional lability, insomnia, alarm, drowsiness, hallucinations.

The respiratory system: pneumonia, bronchitis, breathlessness, respiratory infections, cough, pharyngitis, rhinitis.

From the urinary system: urinary infection, urinary incontinence, acute renal failure.

From the senses: blurred vision, amblyopia, diplopia, noise in ears, otitis.

Dermatological reactions: acne, itching, skin rash, erythema multiforme exudative (incl. Stevens-Johnson syndrome).

Other: fever, viral infection, weight gain, peripheral edema, lability in plasma glucose in patients with diabetes mellitus, the pain of various localization, impotence.

Contraindications

- Acute pancreatitis;

-hereditary deficiency of Galactose, lactase deficiency, glucose-galaktoznaya malyabsorbtsiya;

- Hypersensitivity to the drug.

FROM caution should be used in patients with renal insufficiency, in psychotic disorders.

Pregnancy and lactation

Data on the use of drugs Gabagamma^® when pregnancy is missing, Therefore, Gabapentin should assign pregnant only, If the projected benefits to the mother outweighs the potential risk to the fetus and newborn (malformations, slowing of mental and physical development).

Gabapentin is excreted in breast milk, Therefore, at the time of treatment should stop breastfeeding.

Cautions

Although the syndrome with the development of seizures in the treatment of gabapentinom not checked, Nonetheless, a sudden withdrawal of antiepileptic therapy in patients with parcial'nymi tools convulsions can provoke seizures.

Gabapentin is not considered to be an effective treatment for absence.

Patients, requiring joint therapy morphine, You may need to increase the dose of gabapentin. This should ensure a thorough observation of patients for the development of such a sign of oppression CNS, as drowsiness. In this case, the dose of the drug Gabagamma^® or dose of morphine should be adequately reduced.

When adding medication Gabagamma^® other anticonvulsant funds were registered absorption results in determining protein in urine using test strips Ames N-Multistix SG^®. For the determination of protein in the urine it is recommended to use a more specific method of precipitation sulfosalicylic acid.

Effects on ability to drive vehicles and management mechanisms

During treatment, patients should avoid driving a car, as well as the execution of works, requiring quickness of psychomotor reactions.

Overdose

Symptoms: dizziness, diplopia, speech disorder, drowsiness, lethargy, diarrhoea and increased severity of other side effects.

Treatment: gastric lavage, administration of activated charcoal, simptomaticheskaya therapy. Patients with severe renal failure hemodialysis can be shown.

Drug Interactions

When taking morphine for 2 h before taking gabapentin, there has been an increase in the average value of the AUC to Gabapentin 44% compared to gabapentinom alone, that was associated with increased pain threshold (cold pressornyi test). The clinical significance of this effect is not installed, pharmacokinetic characteristics of morphine not changed. Side effects of morphine when coupled with gabapentinom did not differ from those of morphine when administered in conjunction with placebo.

Interaction between gabapentinom and phenobarbital, phenytoin, valproic acid and carbamazepine is not marked. Pharmacokinetics of gabapentin in equilibrium is the same in healthy people and patients, receiving other anti-convulsants.

The simultaneous use of gabapentin with oral contraceptives, containing norethindrone and/or ethinyl estradiol, has not been accompanied by changes in the pharmacokinetics of both components.

The simultaneous use of gabapentin with antacids, containing aluminum and magnesium, accompanied by a decrease in bioavailability Gabapentin approximately 20%. Gabapentin is recommended to take approximately 2 h after administration antacida.

Probenecid has no effect on renal excretion of gabapentin.

A slight decrease in renal excretion of gabapentin while receiving cimetidine, probably, no clinical significance.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 2 year.