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Gabapentin is an active ingredient commonly used with other drugs to prevent and control partial seizures or to relieve neuropathic pain after shingles in adults. Although it is widely used because Gabapentin has good clinical effect, the mechanism of action of this active ingredient is not clear yet.1. What is Gabapentin?
Gabapentin drugs are usually prepared in the form of capsules, hard capsules, oral solution, film-coated tablets... With the main active ingredient being Gabapentin and excipients suitable for each other dosage form. together. Gabapentin drugs have many different strengths: Gabapentin 100mg, Gabapentin 300mg ... however Gabapentin 300mg content is most commonly used today. So what disease does Gabapentin 300mg treat? Gabapentin is an active substance that is structurally similar to the neurotransmitter GABA (g-aminobutyric acid), but the mechanism of action of Gabapentin is very different from some drugs that interact on GABA synapses such as valproate, barbiturates , benzodiazepines, GABA transaminase inhibitors, GABA reuptake inhibitors, GABA receptor agonists, GABA precursors... Accordingly, Gabapentin at therapeutic doses does not bind to the receptors of these drugs. brain neurotransmitters such as: GABAA, GABAB, benzodiazepine, glutamate, glycine or N-methyl-d-aspartate receptors. Gabapentin also does not interact with sodium channels. Therefore, the mechanism of Gabapentin is different from that of phenytoin and carbamazepine. It can be seen that Gabapentin does not act directly on GABA receptors, does not change the structure, release, metabolism and absorption of GABA.
Gabapentin is an antiepileptic and neuropathic pain reliever with a currently unknown mechanism. In experimental animals, the drug has an anti-extensive effect on the extremities after electric shock and also inhibits seizures caused by pentylenetetrazol.
2. What disease does Gabapentin treat?
Gabapentin is indicated as monotherapy in the treatment of partial seizures with/without secondary generalization in adults and children over 12 years of age. The safety and efficacy of gabapentin monotherapy in children under 12 years of age have not been established. Gabapentin is indicated for adjunctive treatment in the treatment of partial seizures with/without secondary generalization in adults and children 3 years of age and older. The safety and efficacy of gabapentin use in pediatric patients under 3 years of age have not been established. Gabapentin is also used to treat neuropathic pain (such as postherpetic peripheral neuritis, diabetic neuropathy...) in people 18 years of age and older. persons under 18 years of age have not been established. Gabapentin is not effective in absence seizures.3. Dosage and how to take Gabapentin
3.1. Gabapentin for epilepsy Gabapentin is an oral medication that can be taken with or without food. Dosage of Gabapentin for the treatment of epilepsy in adults and pediatric patients over 12 years of age: Adjunctive or monotherapy for partial seizures with or without generalized seizures as follows:
First day: 300mg x 1 time/ day, day 2: 300 mg/time x2 times/day, day 3: 300mg/time x3 times/day. Or the first day: 300mg/time x 3 times, then the dose can be increased in increments of 300mg (in 3 divided doses) every 2-3 days, based on the patient's response, until an effective therapeutic dose is reached. fruit, usually 900 - 3600 mg/day divided into 3 times. The maximum dose is 4800 mg/day, the total daily dose of Gabapentin should be divided equally among 3 dosing times and the maximum dosing interval should not exceed 12 hours to avoid convulsions. For patients with impaired renal function and patients on hemodialysis, the dose should be reduced according to Clcr as follows:
Creatinine clearance 50 - 79 (ml/min): 600 - 1800 mg/day, divided into 3 times; Creatinine clearance 30 - 49 (ml/min): 300 - 900 mg/day, divided into 3 times; Creatinine clearance 15 - 29 (ml/min): 300 - 600 mg/day, divided into 3 times, taken every other day; Creatinine clearance < 15 (ml/min): 300mg/day, divided into 3 times, taken every other day; Hemodialysis patients: The loading dose is 300 - 400 mg of Gabapentin for first-time patients on Gabapentin, then 200 - 300 mg of Gabapentin every 4 hours on hemodialysis. Note that on non-dialysis days, do not take Gabapentin. Gabapentin adjuvant treatment of partial seizures with/without generalized seizures in children 2 - under 6 years old:
First day: 10 mg/kg x1 time/day; day 2: 10 mg/kg x2 times/day; Day 3: 10 mg/kg x3 times/day, then gradually increase the dose of gabapentin depending on the child's response to the usual dose of 30 - 70 mg/kg/day in 3 divided doses. Children 6 - 12 years old:
First day: 10 mg/kg (maximum 300 mg) x1 time/day; day 2: 10 mg/kg (maximum 300 mg) x2 times/day; Day 3: 10 mg/kg (maximum 300 mg) x 3 times/day. The usual dose of Gabapentin: 25-35 mg/kg/day, divided into 3 times, the maintenance dose of Gabapentin is 900 mg/day for children weighing 26-36 kg and 1200 mg/day for children weighing 37-50 kg, total. Gabapentin dose / day, divided into 3 times. Maximum dose: 70 mg/kg/day, divided into 3 times. Some children cannot tolerate daily increases in gabapentin, and extended intervals (up to weeks) may be more appropriate. There are no reviews of the use of Gabapentin in children under 12 years of age with renal impairment.
3.2. Gabapentin treatment of neuropathic pain Adults: First day: 300mg x 1 time/day, day 2: 300mg/time x 2 times/day, day 3: 300mg/time x3 times/day. Or the first day: 300mg/time x3 times, then the dose of Gabapentin can be increased in increments of 300mg (in 3 divided doses) every 2-3 days, based on the patient's response until an effective therapeutic dose is reached. , the maximum dose is 3600 mg/day.
4. Gabapentin overdose
Acute life-threatening poisoning has not been reported with doses of Gabapentin up to 49g. Gabapentin overdose symptoms included: dizziness, double vision, slurred speech, lethargy, mild diarrhea and all were completely reversible with supportive treatment. The decrease in absorption of Gabapentin at high doses at the time of an overdose minimizes the degree of toxicity from Gabapentin overdose.
Although Gabapentin can be removed by hemodialysis, it is usually not necessary. Accordingly, only patients with severe renal impairment may require hemodialysis.
5. Contraindications of Gabapentin
Gabapentin is contraindicated in patients with known hypersensitivity to Gabapentin or any of its ingredients.
6. Gabapentin side effects
Gabapentin is well tolerated, side effects are usually mild or moderate and tend to subside within 2 weeks with continued treatment.
Common side effects of Gabapentin:
Loss of coordination, nystagmus, dizziness, edema, drowsiness, memory loss, children from 3 to 12 years old may experience neurological problems such as: anxiety, behavioral changes (irritability, euphoria or depression, agitation, opposition...); Indigestion, dry mouth, constipation, diarrhea; Peripheral angioedema; Rhinitis, pharyngitis, cough, pneumonia; Double vision, visual impairment; Muscle pain, joint pain; Itching, skin rash; Leukopenia; Impotence, viral infection. Gabapentin side effects are less common:
Memory loss, aphasia, depression, irritability, decreased or loss of libido, headache; Gastrointestinal disturbances, stomatitis, loss or disturbance of taste; Low blood pressure, angina, palpitations; Other: Weight gain, enlarged liver. Gabapentin side effects are rare:
Nerve paralysis, increased libido, decreased motor function, mental disorders, personality disorders; Gastric - duodenal ulcer , esophagitis, colitis/rectum; Cough, hoarseness, respiratory inflammation, pulmonary hypoventilation, pulmonary edema; Eye itching, lacrimation, retinal pathology, iritis; Cartilaginitis, osteoporosis; Leukopenia; Fever or chills; Stevens-Johnson syndrome.
7. Gabapentin drug interactions
Gabapentin does not change the pharmacokinetics of commonly used antiepileptic drugs such as: carbamazepine, phenytoin, valproic acid, phenobarbital, diazepam; Antacids containing aluminum and magnesium can reduce the bioavailability of Gabapentin by 20% by interfering with absorption. Gabapentin must be taken at least 2 hours after the antacid; Morphine reduces the clearance of Gabapentin, when using both drugs, it is necessary to control the symptoms of CNS depression in order to adjust the dose accordingly. Cimetidine reduces the renal clearance of Gabapentin.
8. Be careful when using Gabapentin
Gabapentin should be used with caution in all patients receiving or starting treatment with any anticonvulsant, and patients should be closely monitored, as depression or worsening of depression may occur. worsening, suicidal thoughts, or unusual changes in mood. In addition, patients do not arbitrarily change the treatment regimen without consulting the doctor. Anticonvulsants such as gabapentin must not be stopped suddenly, as this may increase seizures (epilepsy). Discontinuation of gabapentin and/or the addition of another anticonvulsant should be done gradually over at least 1 week. Gabapentin should be used with caution in people with a history of mental disorders, people with impaired renal function, patients on hemodialysis, people operating vehicles or operating machinery. Gabapentin has the potential to cause false positives when performing a proteinuria test. Gabapentin is teratogenic in rodents, however the same effect has not been observed in humans, so it is better to use Gabapentin during pregnancy only when clearly needed and after carefully weighing the benefits against the risks. muscle for the fetus. When taken orally, Gabapentin is likely to pass into breast milk. Gabapentin should be given to a nursing woman only when clearly needed after carefully weighing the benefits and risks. Gabapentin is an active ingredient commonly used with other medications to prevent and control partial seizures or to relieve neuropathic pain after shingles in adults. To ensure the effectiveness of treatment and avoid side effects, patients need to take the medicine exactly as directed by the doctor, professional pharmacist.Follow Vinmec International General Hospital website to get more health, nutrition and beauty information to protect the health of yourself and your loved ones in your family.
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