Description
Latin name
Gabagamma
packaging 20 pcs
Pharmacological action
Antiepileptic drug. Gabapentin is similar in structure to the neurotransmitter gamma-aminobutyric acid (GABA), however, its mechanism of action is different from other drugs that interact with GABA receptors (valproate, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA uptake inhibitors, GABA agonists and prodrug forms of GABA). It does not have GABAergic properties and does not affect the uptake and metabolism of GABA. Preliminary studies have shown that gabapentin binds to the 2 – subunit of voltage-dependent calcium channels and reduces the flow of calcium ions, which plays an important role in the occurrence of neuropathic pain.
Other mechanisms of action of gabapentin for neuropathic pain are a decrease in glutamate-dependent death of neurons, an increase in GABA synthesis, and suppression of the release of neurotransmitters of the monoamine group.
Gabapentin at clinically significant concentrations does not bind to receptors of other common drugs or neurotransmitters, including GABAA, GABAA, benzodiazepine, glutamate, glycine or N-methyl-D-aspartate receptors. Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels in vitro. Gabapentin partially attenuated the effects of the glutamate receptor agonist N-methyl-D-asparagus in some in vitro tests, but only at a concentration of more than 100 μmol, which was not achieved in vivo. Gabapentin slightly reduces the in vitro release of monoamine neurotransmitters.
Pharmacokinetics
Absorption and distribution
The bioavailability of gabapentin is not proportional to the dose. So, with an increase in dose, it decreases. After ingestion of Cmax gabapentin in plasma is achieved after 2-3 hours. The absolute bioavailability of gabapentin in capsules is about 60%. Food, including high in fat, does not affect pharmacokinetics.
Plasma Gabapentin excretion is best described using a linear model. T1 / 2 from plasma is dose-independent and averages 5 7 hours.
Pharmacokinetics do not change with repeated use equilibrium plasma concentrations can be predicted based on the results of a single dose.
Gabapentin practically does not bind to plasma proteins (d – 57.7 l.
Metabolism and excretion
Excreted exclusively by the kidneys unchanged, is not metabolized. The drug does not induce oxidative liver enzymes with a mixed function involved in drug metabolism.
Pharmacokinetics in special clinical cases
Plasma gabapentin clearance is reduced in the elderly and patients with impaired renal function. Excretion rate constant, plasma clearance, and renal clearance are directly proportional to creatinine clearance. Gabapentin is removed from plasma by hemodialysis. In patients with impaired renal function and patients receiving hemodialysis treatment, dose adjustment is recommended.
Indications
In the complex therapy of partial seizures with or without secondary generalization in adults and children over 12 years of age, pain syndrome in diabetic neuropathy, postherpetic neuralgia in adults
Contraindications
acute pancreatitis
hereditary galactase deficiency
lactase deficiency
glucose-galactose malabsorption syndrome
hypersensitivity to any component of the drug.
Precautions: renal failure, psychotic illness.
Pregnancy and lactation
Risk associated with epilepsy and antiepileptic drugs in general
In mothers receiving antiepileptic drugs, 2-3 times increased risk of having children with birth defects. The most frequently reported cases are the birth of children with cleft lip, malformations of the cardiovascular system and neural tube defects. Combined therapy with several antiepileptic drugs increases the risk of congenital malformations to a greater extent than monotherapy. Therefore, when possible, monotherapy is preferred. Women in childbearing age who need anticonvulsant
therapy should consult a specialist. The need for continued anticonvulsant treatment should be reviewed if pregnancy is planned. Do not abruptly cancel
antiepileptic drugs, as this can lead to the resumption of convulsive seizures, which can have serious consequences for maternal and child health. Development delay in children born to women with epilepsy is rare. It is not possible to differentiate what causes the developmental delay: genetic, social factors, maternal epilepsy, or the use of antiepileptic drugs.
Risk associated with the use of gabapentin
There are no data on the use of gabapentin in pregnant women.
Reproductive toxicity has been shown in animal studies. The potential risk to humans is not known. Gabapentin should not be used during pregnancy unless the potential benefit to the mother outweighs the potential risk to the fetus.
Certain findings regarding whether there is an increased risk of congenital malformations, if gabapentin was used during pregnancy, can not be done because in every report on the use of gabapentin in pregnancy, there was epilepsy as such and concomitant therapy with antiepileptic drugs.
Gabapentin is distributed into mother ² ¢s milk. Since the effect of gabapentin on children with breastfeeding is not known, caution should be exercised when prescribing gabapentin to a nursing mother. Gabapentin should be used in nursing mothers only if the potential benefit to the mother outweighs the potential risk to the fetus.
Composition
1 capsule contains:
Active ingredient: bifidobacteria, sorbed on activated carbon
Excipient: lactose monohydrate – up to 0.2 g lactose, corn starch, talc, gelatin, titanium oxide, iron oxide yellow, iron oxide red.
Side effects
The frequency of adverse reactions observed during clinical trials in patients with epilepsy (in combination therapy and with gabapentin monotherapy) and in patients with neuropathic pain is distributed in the following order: very often (more than 10% cases), often (1% -10% of cases), infrequently (0.1% -1% of cases), rarely (0.01% -0.1% of cases), very rarely (less than 0.01% of cases, including reports of single side effects). Where a different frequency of side effects was noted, The highest frequency is indicated. The frequency of adverse reactions noted in post-marketing observations cannot be estimated based on available data. In the data below, their frequency is indicated as unknown. In each group, unwanted effects are presented in decreasing order of severity.
Infections and parasitic diseases: very often – viral diseases often – pneumonia, respiratory diseases, urinary tract infections, infectious diseases, otitis media.
From the hemopoietic system: often – leukopenia is unknown – thrombocytopenia.
On the part of the immune system: rarely – allergic reactions (including urticaria rash) unknown – drug rash with eosinophilia and systemic symptoms (DRESS syndrome).
From the side of metabolism and nutrition: often – anorexia, increased appetite.
From the psyche: often – hostility, confusion and emotional lability, depression, anxiety, increased nervous irritability, impaired thinking is unknown – hallucinations.
From the nervous system: very often – drowsiness, dizziness, ataxia often – convulsions, hyperkinesis, dysarthria, amnesia, tremors, impaired sensations, such as paresthesia, decreased sensitivity, impaired coordination of movements, nystagmus, increased, decreased or absent reflexes rarely – hypokinesia is unknown – other disorders of motor functions (including dyskinesia, dystonia).
From the side of the organ of vision: often – visual impairment, such as decreased visual acuity, double vision.
On the part of the organ of hearing and labyrinth disorders: often – dizziness is unknown – ringing in the ears.
From the cardiovascular system: often – arterial hypertension, rarely vasodilation – palpitations.
From the respiratory system: often – dyspnea, bronchitis, pharyngitis, cough, rhinitis.
From the digestive system: often – vomiting, nausea, dental abnormalities, gingivitis, diarrhea, abdominal pain, dipepsy, constipation, dry mouth and throat, flatulence unknown – pancreatitis, hepatitis, jaundice.
From the skin and subcutaneous tissues: often – facial swelling, a hemorrhagic rash most often described as bruising as a result of physical trauma, rash, itching, acne unknown – Stevens-Johnson syndrome, angioedema, erythema multiforme, alopecia.
From the musculoskeletal system and connective tissue: often – joint pain, muscle pain, back pain, convulsive twitching unknown – myoclonus.
From the kidneys and urinary tract: unknown – acute renal failure, urinary incontinence.
From the genitals and mammary gland: often – impotence is unknown – chest hypertrophy, gynecomastia.
General disorders and disorders at the injection site: very often – fatigue, fever often – peripheral edema, gait disturbances, asthenia, pain, malaise, flu-like syndrome rarely – generalized edema is unknown – withdrawal syndrome (mainly anxiety, insomnia, nausea, pain sweating), chest pain. Cases of sudden unexpected death have been reported when a causal relationship with gabapetpine treatment has not been established.
From laboratory and instrumental studies: often – leukopenia, rarely, weight gain increased levels of liver enzymes (ACT, ALT) and bilirubin are unknown fluctuations in blood glucose levels in patients with diabetes.
Injuries, intoxications and complications of manipulations: often – accidental injury, fracture, abrasions.
In the treatment of gabapentin, there are reports of cases of acute pancreatitis. A causal relationship with gabapentin has not been established.
Cases of myopathy have been reported with increased levels of creatine kinase in patients with end-stage renal failure undergoing hemodialysis.
Infections of the respiratory tract, otitis media, bronchitis, and seizures in children have been reported only in clinical studies. In addition, in clinical trials in children, in most cases, aggressive behavior and hyperkinesis were noted.
Drug Interaction
A study involving healthy volunteers (n = 12) showed that co-administration of morphine in 20 mg / capsule controlled release capsules. 2 hours before gabapentin administration, there was a 44% increase in the mean AUC of gabapentin compared to this index without morphine intake. Patients, co-hosts of morphine and gabapentin should be closely monitored for the risk of developing CNS depression (drowsiness). If such symptoms occur, the dose of gabapentin or morphine should be reduced.
No interaction was observed between gabapentin and phenobarbital, phenytoin, valproic acid or carbamazepine. The equilibrium status of gabapentin pharmacokinetics is the same for healthy subjects and patients with epilepsy receiving other anticonvulsants.
Concomitant administration of gabapentin and oral contraceptives containing norethindrone and / or ethinyl estradiol does not affect the pharmacokinetics of any component.
With the use of gabapentin with antacids containing aluminum and magnesium, the bioavailability of gabapentin is reduced by 24%. It is recommended to take gabapentin approximately 2 hours after taking antacid drugs.
Renal excretion of gabapentin does not change when taking probenecid.
When co-administered with cimetidine, there is a slight decrease in renal excretion of gabapentin, which is not clinically relevant.
Overdose
Symptoms: dizziness, diplopia, impaired speech, drowsiness, lethargy, diarrhea and increased severity of other side effects.
Treatment: gastric lavage, activated carbon intake, symptomatic therapy. Hemodialysis may be indicated in patients with severe renal insufficiency.
Storage conditions
The drug should be stored out of the reach of children at a temperature not exceeding 25 ° C.
Shelf suitability
3 Year
pharmacy terms for
pharmacy sdflfp90 p17dfro41 p17dfro41 p17dfro41 p17dfrod140 and sfc
Prescription
Dosage form
Dosage form
cap uly
