Gabapentin capsules 300mg №50

Composition

1 capsule contains:

• Active substance
  • Gabapentin
    • In terms of 100% substance) 300.0 mg.

• Excipients

  Calcium stearate 4.2 mg, sodium carboxymethyl starch Type A 4.2 mg, microcrystalline cellulose 111.6 mg.

• The composition of the shell of the capsule

  Titanium dioxide 2%, gelatin to 100%.

In a blister pack of 10 capsules. The package contains 5 blister packs.

Indications for use

• Monotherapy or as an additional agent for the treatment of partial seizures with secondary generalization or without it in adults and children from 12 years.
• Neuropathic pain in adults (18 years and older).

Pharmacokinetics

• Suction and distribution

  The bioavailability of Gabapentin is not proportional to the dose. So, with increasing doses, it decreases. After ingestion maximum concentration (C _max ) Plasma gabapentin is reached in 2–3 h. The absolute bioavailability of gabapentin in capsules is about 60%. Food, including those with a high fat content, does not affect the pharmacokinetics.

• Metabolism and excretion

  Removal of gabapentin from plasma is best described using a linear model. Period of stay (T _1/2 a) plasma does not depend on the dose and averages 5-7 hours. Pharmacokinetics do not change with repeated uses; equilibrium plasma concentrations can be predicted based on the results of a single dose of the drug. Gabapentin is practically not bound to plasma proteins (<3%) and has a distribution volume of 57.7 liters.Excreted exclusively by the kidneys in unchanged form, is not exposed to metabolism. The drug does not induce mixed-function oxidative liver enzymes involved in drug metabolism.

• Pharmacokinetics in special clinical situations
  • In the elderly and patients with impaired renal function

    The clearance of Gabapentin from plasma is reduced in the elderly and in patients with impaired renal function. The elimination 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 treatment with hemodialysis, dose adjustment is recommended.

Clinical Pharmacology

Gabapentin is similar in structure to the neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action differs from other drugs that interact with GABA receptors (valproskaya acid, barbiturates, benzodiazepines, GABA inhibitors, GAMA inhibitors, agonists, agonists, agonists, agonists, agonists, GABA, agonists, agonists, GABA, agonists, agonists, GABA, and agonists GABA). It does not possess GABA-ergic properties and does not affect the seizure and metabolism of GABA. Preliminary studies have shown that gabapentin binds to α ₂ -δ-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 in neuropathic pain are the reduction of glutamate-dependent neuronal death, an increase in GABA synthesis, and the suppression of the release of neurotransmitters of the monoamine group.At clinically relevant concentrations, gabapentin does not bind to receptors for other common drugs or neurotransmitters, including the GABAA, GABAH, 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 N-methyl-B-aspartate glutamate receptor agonist in some in vitro tests, but only at a concentration of more than 100 μmol, which is not achieved in vivo. Gabapentin somewhat reduces the release of monoamine neurotransmitters in vitro.

Use during pregnancy and lactation

• Pregnancy

  There are no data on the use of the drug in pregnant women, so Gabapentin should be used during pregnancy only if the intended benefit to the mother justifies the possible risk to the fetus.

• Lactation

  Gabapentin is excreted in breast milk, its effect on the infant being fed is unknown, so during treatment breastfeeding should be abandoned.

Contraindications

• Hypersensitivity to any of the components of the drug.
• Age up to 12 years with partial convulsions.

• Renal failure.

Side effect

• In the treatment of neuropathic pain
  • Body as a whole

    Accidental injuries, asthenia, back pain, flu-like syndrome, headache, infection, pain of various locations, peripheral edema, weight gain.

  • Digestive tract

    Constipation, diarrhea, dry mouth, dyspepsia, flatulence, nausea, vomiting, abdominal pain.

  • Nervous system

    Violation of gait, amnesia, ataxia, confusion, dizziness, hypesthesia, drowsiness, impaired thinking, tremor.

  • Respiratory system

    Dyspnea, pharyngitis.

  • Leather and subcutaneous tissue

    Skin rash.

  • Sense organs

    Amblyopia.

• In the treatment of partial seizures
  • Body as a whole

    Back pain, fatigue, fever, headache, viral infection, peripheral edema, weight gain, asthenia, general malaise, swelling of the face.

  • The cardiovascular system

    Symptoms of vasodilation or hypertension.

  • Digestive tract

    Constipation, dental disease, diarrhea, dyspepsia, increased appetite, dry mouth or pharynx, nausea and / or vomiting, abdominal pain, flatulence, anorexia, gingivitis.

  • Blood system, lymphatic system

    Leukopenia, purpura (most often it was described as bruising that occurred during physical injury).

  • Musculoskeletal system

    Fractures, myalgia, arthralgia.

  • Nervous system

    Amnesia, ataxia, confusion, lack of coordination, depression, dysarthria / Emotional lability, insomnia, nervousness, nystagmus, drowsiness, disturbed thinking, tremor, muscle twitching, dizziness, hyperkinesis; strengthening, weakening or lack of reflexes, paresthesia, anxiety, hostility.

  • Respiratory system

    Cough, pharyngitis, rhinitis, pneumonia.

  • Leather and subcutaneous tissue

    Abrasions, acne, itchy skin, skin rash.

  • Sense organs

    Amblyopia, diplopia, blurred vision.

  • Genitourinary system

    Urinary tract infection, impotence.

Interaction

Morphine - when Gabapentin and morphine were taken together, when morphine was taken 2 hours before Gabapentin, there was an increase in the mean area under the concentration-time pharmacokinetic curve (AUC) of Gabapentin by 44% compared with monotherapy with Gabapentin, which was associated with an increase in pain threshold (cold pressor test). The clinical significance of this change has not been established, and the pharmacokinetic characteristics of morphine did not change. The side effects of morphine when administered together with Gabapentin did not differ from those of morphine taken together with placebo.

The interaction between Gabapentin and phenobarbital, phenytoin, valproic acid and carbamazepine was not observed. The pharmacokinetics of Gabapentin in equilibrium are 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 the bioavailability of Gabapentin by about 20%. Gabapentin is recommended to be taken approximately 2 hours after taking the antacid.

Probenecid does not affect the renal excretion of Gabapentin.

A slight decrease in the renal excretion of Gabapentin while taking cimetidine at the same time probably has no clinical significance.

Overdose

• Symptoms: dizziness, double vision, speech disorder, drowsiness, lethargy, diarrhea.
• Treatment: gastric lavage, reception of Activated carbon, symptomatic therapy. Hemodialysis may be indicated in patients with severe renal insufficiency.

Dosage and administration

Inside, swallowing whole, regardless of the meal and drink plenty of liquids. If it is necessary to reduce the dose, discontinue the drug or replace it with an alternative means, this should be done gradually over at least one week.

• Neuropathic pain in adults

  The initial daily dose is 900 mg, divided into three doses; if necessary, gradually increase the dose to a maximum of 3600 mg / day.

  Treatment can begin immediately with a dose of 900 mg / day (300 mg 3 times a day) or during the first 3 days the dose can be increased gradually to 900 mg per day according to the following scheme:

  • 1st day: 300 mg 1 time per day.
  • 2nd day: 300 mg 2 times a day.
  • 3rd day: 300 mg 3 times a day.

• Partial seizures
  • Adults and children from 12 years: effective dose - from 900 to 2400 mg / day.

  Therapy can be started with a dose of 300 mg 3 times a day at the first laziness or gradually increased to 900 mg according to the scheme described above. Subsequently, the dose can be increased to a maximum of 3,600 mg / day (divided into 3 equal doses). The maximum interval between doses with a triple dose of the drug should not exceed 12 hours in order to avoid renewed seizures.

• Selection of doses for renal failure
  Tab. Patients with renal insufficiency are recommended to reduce the dose of Gabapentin according to the table.
  
  

  Creatinine clearance	Daily dose, mg / day
  > 80	900-2400
  50-79	600-1200
  30-49	300-600
  15-29	150*-300
  < 15	150*

  * designate 300 mg every other day.

• Recommendations for patients on hemodialysis

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

Precautionary measures

Although the withdrawal syndrome with the development of convulsions during treatment with Gabapentin is not marked, nevertheless, an abrupt cessation of therapy with antiepileptic drugs in patients with partial seizures may provoke the development of convulsions.

Gabapentin is not considered an effective treatment for absans epilepsy.

In patients who require co-therapy with morphine, an increase in the dose of Gabapentin may be required. It is necessary to ensure careful monitoring of patients for the development of such a symptom of depression of the central nervous system (CNS), as drowsiness. In this case, the dose of Gabapentin or morphine should be adequately reduced.

• Laboratory research

  When Gabapentin was added to other anticonvulsants, false-positive results were detected in the determination of urine protein using Ames N-Multistix SG test strips. To determine the protein in the urine, it is recommended to use a more specific method for the precipitation of sulfosalicylic acid.

• Influence on ability to drive motor transport and control mechanisms

  Patients should avoid driving, as well as performing work that requires quick psychomotor reactions.

Storage conditions

• Store in a dry place protected from light at a temperature not exceeding 25 ° C.