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Side effects gabapentin 100mg capsules: Gabapentin: Uses, Dosage, Side Effects, Warnings

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Gabapentin Dosage Guide + Max Dose, Adjustments

Medically reviewed by Drugs.com. Last updated on Jan 16, 2023.

Applies to the following strengths: 800 mg; 600 mg; 100 mg; 300 mg; 400 mg; 250 mg/5 mL; enacarbil 600 mg; 300 mg/24 hours; 600 mg/24 hours; 300 mg/24 hours-600 mg/24 hours; 450 mg/24 hours; 750 mg/24 hours; 900 mg/24 hours; enacarbil 300 mg

Usual Adult Dose for:

  • Epilepsy
  • Postherpetic Neuralgia
  • Restless Legs Syndrome

Usual Pediatric Dose for:

  • Epilepsy
Additional dosage information:
  • Renal Dose Adjustments
  • Liver Dose Adjustments
  • Dose Adjustments
  • Precautions
  • Dialysis
  • Other Comments

Usual Adult Dose for Epilepsy

Initial dose: 300 mg orally 3 times a day
Maintenance dose: 300 to 600 mg orally 3 times a day
Maximum dose: 2400 to 3600 mg/day

Comments:

  • Doses up to 2400 mg/day have been well tolerated in long-term studies; doses of 3600 mg/day have be used in a small number of patients for a relatively short duration and have been well tolerated.
  • The maximum time between doses should not exceed 12 hours.
  • The safety and effectiveness of gabapentin available under the trade name Gralise or Horizant have not been studied in patients with epilepsy.

Use: Adjunctive therapy in the treatment of partial onset seizures, with and without secondary generalization

Usual Adult Dose for Postherpetic Neuralgia

Immediate-release:
Initial dose:
Day 1: 300 mg orally once
Day 2: 300 mg orally 2 times day
Day 3: 300 mg orally 3 times a day

  • Titrate dose as needed for pain relief

Maintenance dose: 900 to 1800 mg/day orally in 3 divided doses
Maximum dose: 1800 mg per day

Extended-release: Gralise (gabapentin) 24-hour extended-release tablets:
Initial dose:
Day 1: 300 mg orally with the evening meal
Day 2: 600 mg orally with the evening meal
Days 3 through 6: 900 mg orally with the evening meal
Days 7 through 10: 1200 mg orally with the evening meal
Days 11 through 14: 1500 mg orally with the evening meal
Maintenance dose (Day 15 and onward): 1800 mg orally with the evening meal

Extended-release: Horizant (gabapentin enacarbil) extended release tablets:
Initial dose:
Day 1 to Day 3: 600 mg orally once a day
Maintenance dose (Day 4 and onward): 600 mg orally twice a day
Maximum dose: 1200 mg/day

Comments:

  • The extended-release products Gralise and Horizant are not interchangeable with each other or other gabapentin products due to differing pharmacokinetic profiles.
  • In clinical trials, exceeding maximum doses have not shown additional benefits, but higher doses have resulted in increase in adverse reactions.

Use: For the management of postherpetic neuralgia.

Usual Adult Dose for Restless Legs Syndrome

600 mg orally once daily with food at about 5 PM
Maximum dose: 600 mg

Comment:

  • Gabapentin enacarbil available under the trade name Horizant is the only gabapentin product approved for treatment of Restless Legs Syndrome (RLS).
  • A daily dose of 1200 mg provided no additional benefit compared with the 600 mg dose, but caused an increase in adverse reactions.
  • This drug is not recommended for patients who are required to sleep during the daytime and remain awake at night.

Use: For the treatment of moderate-to-severe primary RLS in adults.

Usual Pediatric Dose for Epilepsy

Age: 3 to 11 years:
Initial dose: 10 to 15 mg/kg/day orally in 3 divided doses
Maintenance dose:
Age: 3 to 4 years: 40 mg/kg/day orally and in 3 divided doses (3 times a day)
Age: 5 to 11 years: 25 to 35 mg/kg/day in 3 divided doses (3 times a day)
Maximum dose: Doses up to 50 mg/kg/day have been well tolerated in a long term clinical study

Age: 12 years or older:
Initial dose: 300 mg orally 3 times a day
Maintenance dose: 300 to 600 mg orally 3 times a day
Maximum dose: 2400 to 3600 mg/day; doses up to 2400 mg/day have been well tolerated in long-term studies; doses of 3600 mg/day have be used in a small number of patients for a relatively short duration and have been well tolerated.

Comments:

  • Initial doses should be titrated over 3 days to the recommended maintenance doses.
  • The maximum time between doses should not exceed 12 hours.
  • The safety and effectiveness of gabapentin available under the trade name Gralise or Horizant have not been studied in pediatric patients and patients with epilepsy.

Use: Adjunctive therapy in the treatment of partial onset seizures, with and without secondary generalization in patients 3 years of age and older.

Renal Dose Adjustments

Immediate release:
12 years or older: Doses should be divided and administered 3 times a day

  • CrCl 60 mL/min or greater: 900 to 3600 mg/day
  • CrCl 30 to 59 mL/min: 400 to 1400 mg/day
  • CrCl 15 to 29 mL/min: 200 to 700 mg/day
  • CrCl 15 mL/min: 100 to 300 mg/day (reduce daily dose in proportion to CrCl)

Less than 12 years: Data not available

Extended release: Gralise (24-hour extended-release tablets):

  • CrCl greater than or equal to 60 mL/min: No adjustment recommended
  • CrCl 30 to 60 mL/min: 600 to 1800 mg orally with the evening meal
  • CrCl less than 30 mL/min: Not recommended

Extended-release: Horizant (gabapentin enacarbil extended-release tablets):
RESTLESS LEGS SYNDROME:

  • CrCl greater than or equal to 60 mL/min: No adjustment recommended
  • CrCl 30 to 59 mL/min: Initial dose: 300 mg orally once a day and increase to 600 mg as needed
  • CrCl 15 to 29 mL/min: 300 mg orally once a day
  • CrCl less than 15 mL/min: 300 mg orally every other day

POSTHERPETIC NEURALGIA:

  • CrCl 60 mL/min or greater: No adjustment recommended
  • CrCl 30 to 59 mL/min: Initial dose: 300 mg orally once a day for 3 days, then 300 mg orally 2 times a day; increase to 600 mg orally 2 times a day as needed
  • CrCl 15 to 29 mL/min: Initial dose: 300 mg orally in the morning on day 1 and day 3; then 300 mg once a day in the morning; may increase to 300 mg orally 2 times a day if needed
  • CrCl less than 15 mL/min: 300 mg orally every other day; increase to 300 mg orally once daily if needed

Liver Dose Adjustments

Data not available

Dose Adjustments

Geriatric Patients: Because elderly patients are more likely to have decreased renal function, the dose of this drug should be adjusted based on CrCl values.

Drug Withdrawal:

  • The drug should be gradually withdrawn
  • If immediate-release dose is reduced, discontinued, or substituted with an alternative medication, this should be done gradually over a minimum of 1 week (a longer period may be needed at the discretion of the prescriber)
  • If Gralise is discontinued, this should be discontinued over a minimum of 1 week or longer
  • If Horizant is discontinued in patient receiving 600 mg/day or less, discontinuation may be done without tapering
  • If Horizant is discontinued in patients receiving this drug twice a day, reduce to once daily for 1 week prior to discontinuation

Precautions

CONTRAINDICATIONS:

  • Hypersensitivity to active substance or any product excipients

Safety and efficacy have not been established in patients younger than 18 years in the management of postherpetic neuralgia or Restless Leg Syndrome.
Safety and efficacy have not been established in patients younger than 3 years in the adjunctive treatment of partial seizures.
Safety and efficacy have not been established in patients younger than 18 years for gabapentin available under the trade names Gralise or Horizant.

Consult WARNINGS section for additional precautions.

Dialysis

Immediate-release: 12 years or older:

  • Adjust dose based on CrCl and provide post-hemodialysis supplemental dose after each 4 hours of hemodialysis: See manufacturer product labeling for post-hemodialysis supplemental dose

Extended-release:

  • Gralise: Hemodialysis: Not recommended
  • Horizant (gabapentin enacarbil):

RESTLESS LEGS SYNDROME:

  • CrCl less than 15 mL/min on hemodialysis: Not recommended

POSTHERPETIC NEURALGIA:

  • CrCl less than 15 mL/min on hemodialysis: 300 mg orally following every dialysis; increase to 600 mg orally following every dialysis if needed

Other Comments

Administration advice:
Immediate-release:

  • Take orally with or without food
  • Swallow capsules whole with water
  • If 600 mg or 800 mg tablets are scored to administer half-tablet, the unused half-tablet should be used as next dose; if half-tablet is not used within 28 days of dividing, the scored tablet should be discarded

Extended-release:

  • Horizant (gabapentin enacarbil): Take orally once a day about 5 PM for Restless Leg Syndrome or twice a day in the morning and evening for Postherpetic Neuralgia; swallow tablets whole with food; do not cut, crush, or chew tablets
  • Gralise extended-release tablets should be taken once daily with the evening meal; do not cut, crush, or chew tablets
  • Horizant and Gralise are not interchangeable with each other or other gabapentin products

MISSED DOSES:
Horizant: If a dose is missed, skip the missed dose and take the next dose at the scheduled time
Gralise: If a dose is missed, take with food as soon as they remember; if it is almost time for the next dose, skip the missed dose and take the next dose at the regular time; do not take two doses at the same time

Storage:

  • Oral Solution: Store in the refrigerator (2C to 8C [36F to 46F])

General:

  • If gabapentin is discontinued and/or an alternate anticonvulsant medication is added to the therapy, this should be done gradually over a minimum of 1 week.

Monitoring:

  • Monitor for respiratory depression in at-risk patients (patients with respiratory impairment and/or on concomitant CNS depression medications)
  • Monitor for the emergence of worsening depression, suicidal thoughts, or behavior, and/or any unusual changes in mood or behavior

Patient Advice:

  • Patients should be instructed to read the US FDA-approved patient labeling (Medication Guide).
  • Patients, families, and caregivers should understand that this drug may increase the risk of suicidal thoughts and behavior and they should be instructed to report any unusual change in mood or behavior, worsening of depression, or suicidal thoughts or behaviors to their healthcare provider immediately.
  • Patients, families, and caregivers should be instructed to report a rash or other signs or symptoms of hypersensitivity, such as fever or lymphadenopathy as this may signal a more serious event; patients should be instructed to stop therapy and seek medical care if they develop signs or symptoms of anaphylaxis or angioedema.
  • Patients should be counseled on concomitant alcohol use; patients on taking Horizant should be instructed to avoid alcohol as alcohol may cause the drug to be released faster from its extended-release tablet.
  • Patients, families, and caregivers should understand that this drug may cause respiratory depression, especially in patients with underlying respiratory impairment and/or concomitant use of CNS depressants.
  • Women of childbearing potential should speak with their healthcare provider if they become or intend to become pregnant, and if they intend or are breastfeeding.
  • Patients should be instructed not to drive a car or perform hazardous tasks until they gain sufficient experience with this drug to understand how it affects their mental and/or motor performance.

More about

Patient resources

  • Drug Information
  • Gabapentin (Advanced Reading)
  • Gabapentin Tablets (PHN)
  • Gabapentin Tablets 600 mg and 800 mg
  • Gabapentin Capsules
  • Gabapentin Oral Solution
Other brands

Neurontin, Gralise, Gabarone

Professional resources

  • Prescribing Information

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer

Gabapentin Interactions Checker – Drugs.com

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There are 266 drugs known to interact with
gabapentin, along with
4 disease interactions, and 1 alcohol/food interaction.

Of the total drug interactions,
27 are major, 229 are moderate, and 10 are minor.

Does gabapentin interact with my other drugs?

Enter other medications to view a detailed report.

  • View all 266 medications that may interact with gabapentin
  • View gabapentin alcohol/food interactions (1)
  • View gabapentin disease interactions (4)

Most frequently checked interactions

View interaction reports for gabapentin and the medicines listed below.

  • Major
  • Moderate
  • Minor
  • Unknown
  • Adderall (amphetamine / dextroamphetamine)
  • Ambien (zolpidem)
  • Aspir 81 (aspirin)
  • Aspirin Low Strength (aspirin)
  • Benadryl (diphenhydramine)
  • Cymbalta (duloxetine)
  • Eliquis (apixaban)
  • Fish Oil (omega-3 polyunsaturated fatty acids)
  • Flexeril (cyclobenzaprine)
  • Flonase (fluticasone nasal)
  • Lasix (furosemide)
  • Lexapro (escitalopram)
  • Lipitor (atorvastatin)
  • Lyrica (pregabalin)
  • Metoprolol Succinate ER (metoprolol)
  • Metoprolol Tartrate (metoprolol)
  • Nexium (esomeprazole)
  • Norco (acetaminophen / hydrocodone)
  • ProAir HFA (albuterol)
  • Seroquel (quetiapine)
  • Singulair (montelukast)
  • Synthroid (levothyroxine)
  • Tylenol (acetaminophen)
  • Vitamin B12 (cyanocobalamin)
  • Vitamin C (ascorbic acid)
  • Vitamin D2 (ergocalciferol)
  • Vitamin D3 (cholecalciferol)
  • Xanax (alprazolam)
  • Zoloft (sertraline)
  • Zyrtec (cetirizine)

Gabapentin alcohol/food interactions

There is 1 alcohol/food interaction with gabapentin.

Gabapentin disease interactions

There are 4 disease interactions with gabapentin which include:

  • drug dependence
  • renal dysfunction
  • suicidal tendency
  • hemodialysis

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Drug Interaction Classification
These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
MajorHighly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
ModerateModerately clinically significant. Usually avoid combinations; use it only under special circumstances.
MinorMinimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
UnknownNo interaction information available.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer

Gabapentin instructions for use: indications, contraindications, side effects – description of Gabapentin caps. 100 mg: 30 or 100 pcs. (40912)

šŸ’Š Ingredients of Gabapentin

āœ… Use of Gabapentin

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Interaction

Description of the active ingredients of the preparation

Gabapentin
(Gabapentin)

The scientific information provided is general and cannot be used to make decisions.
decisions about the use of a particular drug.

Update date: 2022. 06.09

Marketing authorization holder:

AUROBINDO PHARMA Ltd.
(India)

ATX code:

N03AX12

(Gabapentin)

Active substance:
gabapentin
(gabapentin)

Rec.INN

WHO registered

Dosage form

Gabapentin

Caps. 100 mg: 30 or 100 pcs.

reg. No.: LP-002191
dated 21.08.13
– Active

Release form, packaging and composition
drug Gabapentin

Capsules hard gelatin, No. 3, white capsule body, white capsule cap, printed in black ink: “02” on the capsule body; on the cap of the capsule – “D”. The contents of the capsule are white or almost white crystalline powder.

Excipients : corn starch 24 mg, talc 10 mg.

Capsule composition: titanium dioxide 2.1119%, sodium lauryl sulfate 0.08%, gelatin up to 100%.
Ink composition: shellac 24-27%, anhydrous alcohol 23-26%, isopropanol 1-3%, butanol 1-3%, propylene glycol 3-7%, iron dye black oxide 24-28%, potassium hydroxide 0.05- 0.1%, concentrated ammonia solution 1-2%, purified water 15.1-21.8%.

10 pcs. – Al/Al blisters (3) – cardboard packs.
10 pcs. – Al/Al blisters (10) – cardboard packs.

Clinical and pharmacological group:

Anticonvulsant drug

Pharmacotherapeutic group:

Anticonvulsant

Pharmacological action

Antiepileptic. According to the chemical structure, it is similar to GABA, which acts as an inhibitory neurotransmitter in the central nervous system. The mechanism of action of gabapentin is believed to be different from other anticonvulsants that act through GABA synapses (including valproate, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA uptake inhibitors, GABA agonists, and GABA prodrugs). In vitro studies have shown that gabapentin is characterized by the presence of a novel peptide binding site in rat brain tissues, including the hippocampus and cerebral cortex, which may be related to the anticonvulsant activity of gabapentin and its derivatives. Gabapentin in clinically significant concentrations does not bind to other conventional drugs and neurotransmitter receptors in the brain, incl. with GABA A -, GABA B -, benzodiazepine receptors, with NMDA receptors.

The mechanism of action of gabapentin has not been definitively established.

Pharmacokinetics

Gabapentin is absorbed from the gastrointestinal tract. After oral administration, C max of gabapentin in plasma is reached after 2-3 hours. Absolute bioavailability is about 60%. Reception simultaneously with food (including those with a high fat content) does not affect the pharmacokinetics of gabapentin.

Gabapentin does not bind to plasma proteins and has a V d 57.7 l. In patients with epilepsy, the concentration of gabapentin in the cerebrospinal fluid is 20% of the corresponding C ss in plasma at the end of the dosing interval.

Gabapentin is excreted by the kidneys only. T 1/2 does not depend on the dose and averages 5-7 hours.

The clearance of gabapentin is reduced in the elderly and in patients with impaired renal function. The elimination rate constant, plasma and renal clearance of gabapentin are directly proportional to creatinine clearance.

Gabapentin is removed from plasma by hemodialysis.

Plasma concentrations of gabapentin in children were similar to those in adults.

Indications of the active substances of the drug

Gabapentin

Treatment of neuropathic pain in adults over 18 years of age; monotherapy of partial seizures with and without secondary generalization in adults and children over 12 years of age; as an adjunct in the treatment of partial seizures with and without secondary generalization in adults and children aged 3 years and older.

Open list of ICD-10 codes

G40 Epilepsy
G62.9 Polyneuropathy, unspecified
R52.2 Other persistent pain (chronic)

Dosage regimen

The method of administration and dosing regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. Compliance of the dosage form of a particular drug with indications for use and dosing regimen should be strictly observed.

Individual, depending on indications and treatment regimen.

Side effects

From the side of the nervous system: amnesia, ataxia, confusion, impaired coordination of movements, depression, dizziness, dysarthria, increased nervous excitability, nystagmus, drowsiness, impaired thinking, tremor, convulsions, amblyopia, diplopia, hyperkinesia , strengthening, weakening or absence of reflexes, paresthesia, anxiety, hostility, gait disturbance.

From the digestive system: discoloration of teeth, diarrhea, increased appetite, dry mouth, nausea, vomiting, flatulence, anorexia, gingivitis, abdominal pain, pancreatitis, changes in liver function tests.

From the side of the hematopoietic system: leukopenia, decrease in the number of leukocytes, thrombocytopenic purpura.

From the respiratory system: rhinitis, pharyngitis, cough, pneumonia.

From the musculoskeletal system: myalgia, arthralgia, bone fractures.

From the side of the cardiovascular system: arterial hypertension, manifestations of vasodilation.

From the urinary system: urinary tract infections, urinary incontinence.

Allergic reactions: erythema multiforme, Stevens-Johnson syndrome.

Dermatological reactions: skin maceration, acne, itching, rash.

Other: back pain, fatigue, peripheral edema, impotence, asthenia, malaise, facial swelling, weight gain, accidental injury, asthenia, influenza-like syndrome, blood glucose fluctuations, in children – viral infection, otitis media .

Contraindications for use

Hypersensitivity to gabapentin.

Use in pregnancy and lactation

Adequate and well-controlled studies on the safety of the use of gabapentin during pregnancy and lactation in humans have not been conducted. If necessary, use during pregnancy and lactation should carefully weigh the expected benefit of therapy for the mother and the potential risk to the fetus or infant.

Gabapentin is excreted in breast milk. When used during lactation, the nature of the action of gabapentin on an infant has not been established.

Use for impaired renal function

Patients with impaired renal function, as well as patients on hemodialysis, require adjustment of the dosing regimen.

Pediatric Use

The efficacy and safety of neuropathic pain therapy in patients under 18 years of age have not been established.

Efficacy and safety of gabapentin monotherapy in the treatment of partial seizures in children under 12 years of age and additional therapy with gabapentin in the treatment of partial seizures in children under 3 years of age have not been established

Use in elderly patients

Elderly patients may require dosage adjustment gabapentin due to the fact that in this category of patients, a decrease in renal clearance is possible.

Special instructions

Abrupt discontinuation of anticonvulsant therapy in patients with partial seizures may provoke status convulsions. If necessary, dose reduction, discontinuation of gabapentin or replacement with an alternative agent should be gradual over a period of at least 1 week.

Gabapentin is not an effective treatment for absence seizures.

False-positive urine protein test results have been reported when co-administered with other anticonvulsants. To determine the protein in the urine, it is recommended to use a more specific method of precipitation of sulfosalicylic acid.

Patients with impaired renal function, as well as patients on hemodialysis, require adjustment of the dosing regimen.

Elderly patients may require correction of the dosing regimen of gabapentin due to the fact that in this category of patients a decrease in renal clearance is possible.

The efficacy and safety of neuropathic pain therapy in patients under 18 years of age have not been established.

The efficacy and safety of gabapentin monotherapy in the treatment of partial seizures in children under 12 years of age and additional therapy with gabapentin in the treatment of partial seizures in children under 3 years of age have not been established.

Avoid drinking alcohol during treatment.

Influence on the ability to drive vehicles and mechanisms

Before determining the individual response to treatment, the patient should refrain from potentially hazardous activities associated with the need for concentration and increased speed of psychomotor reactions.

Drug interactions

Simultaneous use with antacids reduces the absorption of gabapentin from the gastrointestinal tract.

When used simultaneously with felbamate, an increase in T 1/2 felbamate is possible.

With simultaneous use, a case of an increase in the concentration of phenytoin in the blood plasma is described.

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Gabapentin . Description of the drug in the reference book Vidal.

Tebantine capsules 300mg ā„–50

Composition

1 capsule contains:

capsule content:

active ingredient: gabapentin 100 mg, 300 mg or 400 mg;

excipients: magnesium stearate, talc, pregelatinized starch, lactose monohydrate;

hard gelatin capsule composition:

cap: iron dye red oxide E172, iron dye yellow oxide E172, titanium dioxide E171, gelatin;

case: iron dye red oxide E172 (for a dose of 300 mg and 400 mg), iron dye yellow oxide E172 (for a dose of 300 mg and 400 mg), titanium dioxide E171, gelatin.

Dosage form

Capsules.

Description

Capsule content:

White or almost white crystalline powder.

Capsules 100 mg

Coni-SnapĀ® capsules, size #3, cap: pinkish brown, body: white.

Capsules 300 mg

Size #1 Coni-SnapĀ® capsules, cap: pinkish brown, body: light yellow.

Capsules 400 mg

Coni-SnapĀ® capsules, size #0, cap: pinkish brown, body: yellowish orange.

Action

Antiepileptic drug. Gabapentin is structurally similar to the neurotransmitter gamma-aminobutyric acid (GABA). It is a lipophilic substance. However, its mechanism of action differs from that of some other drugs that interact with GABA receptors, including valproic acid drugs, barbiturates, benzodiazepines, GABA transferase inhibitors, GABA reuptake inhibitors, GABA agonists, and GABA prodrugs: it does not have GABAergic properties and does not affect GABA uptake and metabolism. Preliminary studies suggest that gabapentin binds to ?2-? a subunit of voltage-gated calcium channels and suppresses the flow of calcium ions, which plays an important role in the occurrence of neuropathic pain. Other mechanisms involved in the action of gabapentin in neuropathic pain are: a decrease in glutamate-dependent neuronal death, an increase in GABA synthesis, and suppression of the release of monoamine neurotransmitters. Gabapentin does not bind to receptors for other common drugs or transmitters at clinically relevant concentrations, including the GABAA and GABAB, benzodiazepine, glutamate, glycine, or NMDA receptors.
Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels in vitro. Gabapentin partially attenuated the effects of the NMDA glutamate receptor agonist in some in vitro tests, but only at concentrations above 100 Āµmol, which is not achieved in vivo. Gabapentin slightly reduces the release of monoamine neurotransmitters and modifies the activity of the enzymes GABA synthetase and glutamate synthetase in vitro. The use of gabapentin in rats led to an increase in GABA metabolism in some areas of the brain; this effect was similar to that of valproic acid, although it was observed in other parts of the brain. The significance of these effects of gabapentin for its anticonvulsant activity has not been established. In animals, gabapentin easily penetrates the brain tissue and prevents seizures caused by maximal electric shock, chemicals, including inhibitors of GABA synthesis, and also caused by genetic factors.

Pharmacokinetics

Absorption – fast. After oral administration, the maximum plasma concentration (Cmax) is reached after 3 hours. With repeated administration, the maximum concentration of Cmax is reached approximately 1 hour faster (tmax) than with a single dose. The bioavailability of gabapentin is not proportional to the dose: it decreases with increasing dose. The absolute bioavailability of gabapentin capsules is about 60%. Food, including those with a high fat content, does not significantly affect the pharmacokinetics, in such cases there is a ~ 14% increase in AUC and Cmax. When taking the drug at a dose of 300 to 4800 mg, the average Cmax and AUC increased as the dose increased. The deviation from linearity in the case of both indicators is very small at doses not exceeding 600 mg; at high doses, the increase is not so significant.

After single oral administration of gabapentin, plasma concentrations of the drug in children aged 4 to 12 years are similar to those in adults. With repeated doses, the equilibrium state was reached after 1-2 days and persisted throughout the course of treatment.

Metabolism: Gabapentin is practically not metabolized in the human body and does not induce mixed-function liver oxidative enzymes involved in drug metabolism.

Distribution: Gabapentin practically does not bind to plasma proteins (less than 3%), the volume of distribution is 57.7 liters. The concentration of gabapentin in the CSF is 20% of the plasma concentration at equilibrium. Passes through the blood-brain barrier, penetrates into breast milk.

Elimination: The elimination of gabapentin from plasma is linear. The half-life (T1 / 2) is 5-7 hours, does not depend on the dose. The elimination rate constant, plasma clearance, and renal clearance of gabapentin are directly proportional to creatinine clearance. Gabapentin is excreted by the kidneys unchanged. Removed from plasma during hemodialysis.

Special groups of patients

Plasma clearance of gabapentin is reduced in elderly patients and patients with impaired renal function, T1 / 2 with creatinine clearance less than 30 ml / min. is about 52 hours. In patients with impaired renal function and patients on hemodialysis, dose adjustment is recommended.

Indications for use

– Partial seizures with or without secondary generalization in adults and children over 12 years of age as monotherapy or adjunctive therapy.

– Partial convulsions with or without secondary generalization in children 3 to 12 years of age as adjunctive therapy.

– Neuropathic pain in patients over 18 years of age. Efficacy and safety in patients under 18 years of age have not been established.

Contraindications

– Hypersensitivity to any of the components of the drug;

– acute pancreatitis;

– monotherapy in children aged 3 to 12 years;

– children under 3 years of age;

– lactation period;

– lactase deficiency, lactose intolerance, glucose-galactose malabsorption (the dosage form of the drug contains lactose).

Use in 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 expected benefit to the mother justifies the possible risk to the fetus.

Gabapentin is excreted in breast milk, its effect on breastfed infants is unknown, therefore TebantinĀ® should be used during breastfeeding only if the benefit to the mother clearly outweighs the risk to the infant.

Use in children

Contraindicated in children under 3 years of age.
The use of TebantinĀ® as monotherapy is contraindicated in children aged 3 to 12 years.
The safety and efficacy of neuropathic pain therapy in patients under 18 years of age have not been established.

Side effects

In the treatment of partial seizures

General: back pain, chest pain, fever, fatigue, flu-like syndrome, asthenia, malaise.

From the side of the nervous system: drowsiness, dizziness, headache, amnesia, ataxia, depression, emotional lability, increased nervous excitability, nystagmus (dose-dependent), tremor, muscle twitching, hyperkinesis, dysarthria, impaired coordination, hallucinations, movement disorders (choreoathetosis , dyskinesia, dystonia), impaired thinking, confusion, tics, paresthesia (dose-dependent), hyperkinesia, strengthening, weakening or absence of reflexes, anxiety, restlessness, hostility, insomnia.

From the digestive system: nausea, vomiting, abdominal pain, dyspepsia, increased appetite, dry mouth or throat, constipation, diarrhea, dental lesions, pancreatitis, hepatitis, jaundice, increased activity of “liver” transaminases, flatulence, anorexia, gingivitis.

From the side of the cardiovascular system: palpitations, symptoms of vasodilation. When administered with other drugs – increased blood pressure.

From the side of the hematopoietic system: leukopenia, thrombocytopenia.

From the musculoskeletal system: arthralgia, myalgia, fractures.

From the respiratory system: pharyngitis, rhinitis, when administered with other antiepileptic drugs – cough, pneumonia.

From the senses: visual impairment (amblyopia, diplopia), tinnitus.

From the genitourinary system: impotence, urinary incontinence, acute renal failure, an increase in the volume of the mammary glands, gynecomastia, when administered with other antiepileptic drugs – urinary tract infection.

Allergic reactions: skin rash, itching, urticaria, fever, angioedema, erythema multiforme exudative (including Stevens-Johnson syndrome).

Other: purpura, weight gain, discoloration of tooth enamel, swelling of the face, peripheral edema, generalized edema, acne, alopecia, fluctuations in blood glucose concentration in patients with diabetes mellitus.

In the treatment of neuropathic pain

General: accidental injuries, asthenia, back pain, influenza-like syndrome, headache, infections, pain of various localization.

From the digestive system: constipation, diarrhea, dyspepsia, dry mouth, flatulence, nausea, vomiting, abdominal pain.

Diseases of the nervous system: gait disturbance, disorientation, paresthesia, drowsiness, thinking disorder, tremor.

From the respiratory system: shortness of breath, pharyngitis.

On the part of the skin: skin rash.

From the senses: amblyopia.

Other: peripheral edema, weight gain.

In addition, hostility and hyperkinesia have been reported in children younger than 12 years of age when taking gabapentin as add-on therapy.

After abrupt discontinuation of gabapentin therapy, the most frequently observed were anxiety, insomnia, nausea, pain of various localization, and sweating.

Interactions

Antiepileptics: No interactions have been noted between gabapentin and phenytoin, carbamazepine, valproic acid and phenobarbital. The pharmacokinetics of gabapentin at steady state is similar in healthy subjects and in patients receiving other antiepileptic drugs.

Oral contraceptives: gabapentin does not affect the pharmacokinetics and efficacy of oral contraceptives containing norethisterone and/or ethinyl estradiol. However, the deterioration / termination of the contraceptive effect of these drugs is possible when TebantinĀ® is combined with other antiepileptic drugs that reduce the effectiveness of oral contraceptives.

Antacids: stomach acid antacids containing magnesium or aluminum reduce the bioavailability of gabapentin by 24%. TebantinĀ® capsules should be taken 2 hours after taking antacids.

Cimetidine: the combination of cimetidine with gabapentin slightly reduces the excretion of the latter by the kidneys, which probably has no clinical significance.

Alcohol and other drugs that affect the central nervous system: may increase unwanted side effects of gabapentin on the central nervous system (eg, drowsiness, ataxia).

Probenecid does not affect the renal excretion of gabapentin.

Morphine: Co-administration of gabapentin and morphine, when morphine in the form of controlled-release capsules of 60 mg was taken 2 hours before taking gabapentin, a 44% increase in gabapentin AUC was observed compared with gabapentin alone, which was accompanied by an increase in pain threshold (cold pressure test). The clinical significance of these changes has not been established. Gabapentin administered 2 hours after morphine administration did not alter the pharmacokinetic characteristics of morphine. The side effects of morphine when combined with gabapentin did not differ from those observed when taking morphine with placebo.

Urine protein laboratory results:

When gabapentin was added to other anticonvulsants, false-positive results were reported in the determination of total urinary protein using semi-quantitative tests. When positive results are obtained using such tests, it is recommended to use a more specific method of precipitation with sulfosalicylic acid or a biuret test.

Dosage and Administration

TebantinĀ® is administered orally with or without food.

Capsules should be taken without chewing with sufficient liquid. With triple administration, it should be borne in mind that the time between two doses should not exceed 12 hours.

Partial convulsions:

Adults and children over 12 years of age: 900 to 1200 mg/day usually provide an antiepileptic effect. The desired therapeutic effect is achieved within a few days after titration.

Recommended dosing regimens:

A. Day 1: 300 mg gabapentin daily (1 capsule 300 mg once daily or 1 capsule 100 mg 3 times daily)

Day 2: 600 mg gabapentin daily (1 capsule 300 mg 2 times a day or 2 capsules 100 mg 3 times a day)

Day 3: 900 mg gabapentin daily (1 capsule 300 mg 3 times a day or 3 capsules 100 mg 3 times a day)

From the 4th day: the daily dose can be increased to 1200 mg divided into 3 doses per day (for example, 1 capsule 400 mg 3 times a day ).

B. Alternative dosing regimen: initial dose on the first day – 1 capsule 300 mg 3 times a day (corresponding to 900 mg gabapentin), after which the dose can be increased to 1200 mg / day.

Depending on the effect obtained, the dose can be increased by 300-400 mg / day, but not exceeding the total daily dose (with three doses) of 2400 mg, due to insufficient data on the efficacy and safety of using higher doses.

Use of the drug as adjunctive therapy in children aged 3-12 years and weighing more than 17 kg up to 12 years as monotherapy.

The recommended daily dose of the drug (distributed into three doses) is 25-35 mg/kg/day. Table 1 contains the recommended daily doses of gabapentin per kg of body weight.

The effective dose is achieved by titration according to the following scheme:

Day 1: 10 mg/kg/day

Day 2: 20 mg/kg/day

Day 3: 30 mg/kg/day days, according to the method given in the table. Then, if necessary, the daily dose of gabapentin (divided into three doses) can be increased up to 35 mg/kg/day. Data from long-term clinical studies have confirmed good tolerability of doses of 40-50 mg/kg/day.

Treatment of neuropathic pain in adults (over 18 years of age)

The optimal therapeutic dose in the treatment of neuropathic pain is titrated by the attending physician based on efficacy and tolerability. Depending on the individual response of the patient, the dose can reach 3600 mg / day.

Recommended dosing regimens:

A. 1st day: 300 mg gabapentin per day (1 capsule 300 mg 1 time per day or 1 capsule 100 mg 3 times a day)

2nd day: 600 mg gabapentin per day (1 capsule 300 mg 2 times a day or 2 capsules 100 mg 3 times a day)

Day 3: 900 mg gabapentin per day (1 capsule 300 mg 3 times a day or 3 capsules 100 mg 3 times a day)

B. Alternative dosage regimen for severe pain: initial dose on the first day – 1 capsule 300 mg 3 times a day (corresponding to 900 mg gabapentin), after which the dose can be increased within 7 days to 1800 mg / day.

In some cases, in order to achieve the desired analgesic effect, the dose can be increased to a maximum of 3600 mg / day, divided into three doses. (In clinical studies, the dose was increased to 1800 mg during the first week, and to 2400 mg and 3600 mg during the second and third weeks, respectively.)

In debilitated patients, those with low body weight or who have undergone organ transplantation, the dose can be increased strictly by 100 mg per day.

In elderly patients, in accordance with the age-related decrease in creatinine clearance, as well as in patients with renal insufficiency (creatinine clearance < 80 ml / min) or those on hemodialysis, the therapeutic dose is selected individually.

Dosing regimen for hemodialysis: For patients on hemodialysis who have not previously taken gabapentin, it is recommended to prescribe a loading dose of 300-400 mg, then 200-300 mg every 4 hours of hemodialysis. On dialysis-free days, gabapentin should not be taken.

Overdose

Symptoms of acute, life-threatening poisoning were not observed even after a daily intake of 49 g of the drug. In case of overdose, dizziness, double vision, speech disturbance, drowsiness, lethargy and diarrhea were observed.

Treatment: symptomatic. Patients with severe renal insufficiency may be shown hemodialysis.

Special instructions

In the process of selecting the optimal therapeutic dose, it is not necessary to determine the concentration of the drug in plasma.

The drug is not effective for the treatment of absence seizures.

Need to control blood glucose in patients with diabetes mellitus; sometimes there is a need to change the dose of a hypoglycemic drug.

At the first sign of acute pancreatitis (prolonged abdominal pain, nausea, repeated vomiting), treatment with gabapentin should be discontinued. The patient should be subjected to a thorough examination (clinical and laboratory tests) for the purpose of early diagnosis of acute pancreatitis.

In case of lactose intolerance, please note that 100 mg capsule contains 22.14 mg lactose; 300 mg – 66.42 mg; 400 mg – 88.56 mg.

If necessary, reduce the dose, stop the drug or change it to an alternative drug should be gradual, over a period of at least one week. Abrupt cessation of therapy may provoke status epilepticus.

The safety and efficacy of gabapentin in children under 3 years of age as adjunctive therapy for epilepsy and in children under 12 years of age as monotherapy have not been established.

The safety and efficacy of the treatment of neuropathy in patients less than 18 years of age have not been established.

If in adults: drowsiness, ataxia, dizziness, fatigue, nausea and/or vomiting, weight gain, and in children: drowsiness, hyperkinesia and hostility, stop treatment and consult a physician.

Influence on the ability to drive vehicles and control mechanisms

During the period of treatment, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.