Gabapentin

Gabapentin is an anticonvulsant drug that is used to treat epilepsy and neuropathic pain. It is most known under brand name Neurontin. The drug is also used off-label to treat depression and anxiety disorder. The exact mechanism of action of Gabapentin is yet not fully understood, though it is suggested that the drug works by increasing GABA content in the brain.

Brand Canonpharma

In stock 1652 Items

Available since: 2019-09-19

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Clinical Pharmacology

pharmachologic effect

- monotherapy or as an additional agent for the treatment of partial seizures with secondary generalization or without it in adults and children from 12;

- neuropathic pain in adults (18 years and older).

Pharmacokinetics

- monotherapy or as an additional agent for the treatment of partial seizures with secondary generalization or without it in adults and children from 12;

- neuropathic pain in adults (18 years and older).

Indications

- monotherapy or as an additional agent for the treatment of partial seizures with secondary generalization or without it in adults and children from 12;

- neuropathic pain in adults (18 years and older).

Composition

1 caps
gabapentin	300 mg

Excipients: calcium stearate - 4.2 mg, sodium carboxymethyl starch (type A) - 4.2 mg, microcrystalline cellulose - 111.6 mg.

Gabapentin is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Gabapentin	Canonpharma	Russia	capsules
Gabagamma	Artezan Pharma	Germany	capsules
Gabapentin	Piq-Pharma	Russia	capsules
Katena	Belupo	Croatia	capsules
Convalis	Lecco	Russia	capsules
Tebantine	Gedeon Richter	Hungary	capsules
Neurontin	Pfizer	USA	pills
Neurontin	Pfizer	USA	capsules

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Dosage and Administration

Orally, 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 be started immediately with a dose of 900 mg / day (300 mg 3 times per day) or during the first 3 days the dose can be increased gradually to 900 mg per day. as follows:

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. on the first day or increase gradually 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

Patients with renal insufficiency are recommended to reduce the dose of Gabapentin according to the table:

Creatinine clearance	Daily dose (mg / sug)
>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

Patients on hemodialysis who have not previously taken gabapentin are advised to prescribe a drug in a saturating dose of 300-400 mg, and then use it on 200-300 mg every 4 hours of hemodialysis.

Adverse reactions

In the treatment of neuropathic pain

The body as a whole: accidental injuries, asthenia, back pain, flu-like syndrome, headache, infection, pain of different localization, peripheral edema, weight gain;

Digestive tract: constipation, diarrhea, dry mouth, dyspepsia, flatulence, nausea, vomiting, abdominal pain;

Nervous system: gait disturbance, amnesia, ataxia, confusion, dizziness, hypoesthesia, drowsiness, impaired thinking, tremor;

Respiratory system: shortness of breath, pharyngitis;

Skin and Subcutaneous Tissue: skin rash;

Sense organs: amblyopia.

In the treatment of partial seizures

The body as a whole: back pain, fatigue, fever, headache, viral infection, peripheral edema, weight gain, asthenia, - general malaise, swelling of the face;

Cardiovascular system: symptoms of vasodilation or hypertension;

Digestive tract: constipation, dental disease, diarrhea, dyspepsia, increased appetite, dry mouth or throat, 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);

Osteoporosis: fractures, myalgia, arthralgia;

Nervous system: amnesia, ataxia, confusion, incoordination, depression, dysarthria, emotional lability, insomnia, nervousness, nystagmus, drowsiness, impaired thinking, tremor, muscle twitching, dizziness, hyperkinesis; strengthening, weakening or lack of reflexes, paresthesia, anxiety, hostility;

Respiratory system: cough, pharyngitis, rhinitis, pneumonia;

Skin and subcutaneous tissue: abrasions, window, itchy skin, skin rash;

Sense organs: amblyopia, diplopia, visual disturbances;

Urogenital system: urinary tract infection, impotence.

Contraindications

- hypersensitivity to any of the components of the drug,

- age up to 12 years with partial convulsions.

With care: renal failure.

Drug interactions

Morphine: when Gabapentin and morphine were taken together, when morphine was administered 2 hours before Gabapentin, there was an increase in the average pharmacokinetic AUC area of Gabapentin by 44% compared with monotherapy with Gabapentin, which was associated with an increase in pain threshold (cold pressure 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 taken together with gabapentin did not differ from those of taking morphine 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 renal excretion of Gabapentin while taking cimetidine at the same time probably has no clinical significance.

Pregnancy and Lactation

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.

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

Special instructions

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

With renal failure

Use with caution in renal failure.

In patients with impaired renal function and patients receiving treatment with hemodialysis, dose adjustment is recommended.

For children: Contraindicated in the age of 12 years with partial convulsions. For the treatment of neuropathic pain, do not prescribe to children and adolescents under 18 years of age.

Overdosage

Symptoms: dizziness, double vision, speech disorder, drowsiness, lethargy, diarrhea.

Treatment: gastric lavage, reception of Activated charcoal, symptomatic therapy. Hemodialysis may be indicated in patients with severe renal insufficiency.

Brand name: Gabapentin
Active ingredient: Gabapentin
Dosage form: Hard gelatin capsules, size No. 0, white; the contents of the capsules are white or white with a yellowish tinge powder.
Manufacturer: Canonpharma
Country of Origin: Russia