What is Gabapentin?

Gabapentin is also known as Norritin; Gabapentin; Carbavantin; Neurontin; GO-3450. It is the first anti-epileptic drug developed by Warner-Lanbert in the United States. It was first marketed in the United Kingdom in 1993. Gabapentin is a novel drug. Antiepileptic drugs. It is white to off-white crystalline powder with molecular formula C9H17NO2, molecular weight 171.23700, melting point 162 ° C, boiling point 314.4ºC at 760 mmHg, and stable chemical properties at room temperature and pressure. For epilepsy patients with localized seizures whose conventional antiepileptic drugs cannot be satisfactorily controlled or intolerable, and for epilepsy patients with localized seizures and then systemicization. The product is an antiepileptic drug that prevents the use of chemicals such as imprint Toxins, bicuculline, strychnine, etc.) and non-chemical stimuli (such as sound source, electric shock, etc.); convulsions induced by partial seizures and secondary systemic tonic-clonic seizures, in Partial epileptic seizures that cannot be satisfactorily controlled or tolerated with conventional anticonvulsants alone or in combination, and additional therapies for partial seizures secondary to systemic seizures. ^[1-2]

Drug Name: Gabapentin
Alias: Norritin; Gabapentin; Carbavantin; Neurontin; GO-3450
Foreign name: Gabapentin
Whether prescription drugs: prescription
Main indications: Partial seizures, refractory incomplete epilepsy
Adverse reactions: Lethargy, dizziness, ataxia, headache, etc.

Main medication contraindications: Allergic to gabapentin and breastfeeding are prohibited
Dosage form: 100mg, 300mg, 400mg
Drug type: chemical
Molecular formula: C9H17NO2
Molecular weight: 171.23700
Density: 1.058 g / cm3
Melting point: 162 ° C
CAS: 60142-96-3

Gabapentin Information

Chinese name

Chinese alias: 1- (aminomethyl) cyclohexaneacetic acid;

1- (aminomethyl) cyclohexaneacetic acid;

Gaba;

1- (methylamino) cyclohexaneacetic acid;

Gabapentin GABA;

Gabapentin hydrochloride;

Gabapentin;

1- (aminomethyl) cyclohexaneacetic acid hydrochloride;

English name: gabapentin

English alias: GABAPENTIN;

NEURONTIN;

GABAPENTINE;

Gababentin;

Gabapentin hydrochloride;

2- (1- (Aminomethyl) cyclohexyl) acetic acid;

CAS number: 60142-96-3 ^[1]

Molecular formula: C9H17NO2

Molecular weight: 171.23700

Chemical structure:

Exact mass: 171.12600

PSA: 63.32000

LogP: 2.07060 ^[1]

Gabapentin physical and chemical properties

Appearance and properties: white to off-white crystalline powder

Density: 1.058 g / cm3

Melting point: 162 ° C

Boiling point: 314.4ºC at 760 mmHg

Flash point: 144ºC

Refractive index: 1.484

Stability: Stable at normal temperatures and pressures.

Storage conditions: Keep tightly closed. ^[1]

Gabapentin Safety Information

Customs code: 2922499990

WGK Germany: 3

Danger category code: R61

Safety instructions: S53-S26-S36 / 37 / 39-S45

RTECS number: GU6496000

Dangerous goods mark: T ^[1]

Overview of Gabapentin Drug Basic Information

Gabapentin drug name

Chinese name

English name: Gabapentin, Neurontin

Alias: Norritin; Gababantin; Carbavantin; Neurontin; GO-3450 ^[2]

Gabapentin classification

Neurological Drugs> Antiepileptic Drugs> Others ^[2]

Gabapentin dosage form

100mg, 300mg, 400mg. ^[2]

Gabapentin pharmacological effects

1. Gabapentin is the first anti-epileptic drug developed by Warner-Lanbert Company in the United States. It was first marketed in the United Kingdom in 1993. Gabapentin is a novel antiepileptic drug. It is a derivative of -aminobutyric acid (GABA). Its pharmacological effect is different from existing antiepileptic drugs. Recent studies have shown that the effect of gabapentin changes GABA metabolism. Gabapentin has been shown to prevent epilepsy in various animal models. In addition, it has also been shown to be useful in animal models of spasm, analgesia and amyotrophic cord sclerosis. Gabapentin has a high affinity for the novel binding points of brain tissue. It can pass some barriers in the body through amino acid transfer bodies. Compared with other anticonvulsants, gabapentin has less behavioral and cardiovascular side effects.

2. Gabapentin has a similar structure to -aminobutyric acid (GABA), but it is not an agonist of GABA receptors. The receptors bound to neurons in brain tissue have not yet been determined, so its mechanism of action has not been clarified. Gabapentin is often used as an adjuvant when traditional antiepileptic drugs are ineffective or patients cannot tolerate it. Studies have shown that when treated with gabapentin, the frequency of seizures is significantly reduced, long-term efficacy is satisfactory, and fewer adverse reactions occur. After seizure control, only gabapentin is effective in some patients. Ineffective for denervation. ^[2-3]

Gabapentin pharmacokinetics

Gabapentin is absorbed from the gastrointestinal tract by a saturable mechanism, and usually reaches its peak in 3 hours. Steady-state blood drug concentration can be achieved in 1-2 days. Widely distributed throughout the body, with little binding to plasma proteins. tl / 2 is about 5-7 hours. It is basically not metabolized in the body, most of the dose is excreted in urine with the original drug, and the rest is excreted in feces. ^[2-3]

Gabapentin indication

1. Used to control partial seizures.

2. Refractory incomplete epilepsy. It has been reported that the combination of the anti-anxiety drug gabapentin and the antiviral drug valacyclovir can reduce the risk of post-herpetic neuralgia. ^[2-3]

Gabapentin contraindications

Allergic to gabapentin and breastfeeding are prohibited. ^[2]

Gabapentin precautions

Use with caution in patients with impaired renal function. ^[2]

Gabapentin adverse reactions

1. Common causes are drowsiness, dizziness, dyskinesia, fatigue, nystagmus, headache, tremor, diplopia, rhinitis, and nausea and vomiting. These reactions are usually reduced after continued administration.

2. Occasionally convulsions, pharyngitis, dysphonia, weight gain, indigestion, forgetting, and nervousness.

3. Pancreatitis, impaired liver function and Stewart syndrome rarely occur. ^[2]

Gabapentin dosage

The starting dose for adults and adolescents over 12 years old is 300 mg on the first day, taken before bedtime; then 300 mg is added daily and taken in divided portions until the onset is controlled. The recommended dose is 900 to 1200 mg per day, divided into 3 doses; if necessary, it can reach 2.4 g per day. ^[2]

Gabapentin drug interactions

1. Antacids can reduce the absorption of gabapentin from the gastrointestinal tract.

2 Cimetidine may reduce gastric clearance, but has no practical clinical significance. ^[2]

Gabapentin Expert Reviews

Gabapentin is a new type of antiepileptic drug. Its pharmacological effects are different from existing antiepileptic drugs. Gabapentin has shown epilepsy prevention in various animal models. In addition, it is used in animal models of spasm, analgesia and amyotrophic lateral sclerosis The effect is also shown in. Compared with other anticonvulsants, gabapentin has less behavioral and cardiovascular side effects. ^[2]