Description

Simple

A medication used to treat certain types of seizures and nerve pain.

Clinical

An anticonvulsant medication used in the management of peripheral neuropathic pains, postherpetic neuralgia, and partial-onset seizures.

Overview

Gabapentin is a structural analogue of the inhibitory neurotransmitter gamma-aminobutyric acid ([GABA]) that was first approved for use in the United States in 1993.[16] It was originally developed as a novel anti-epileptic for the treatment of certain types of seizures[14,5] - today it is also widely used to treat neuropathic pain.[8,10] Gabapentin has some s... Read more

Pharmacology

Indication

In the United States, gabapentin is officially indicated for the treatment of postherpetic neuralgia in adults and for the adjunctive treatment of partial-onset seizures, with or without secondary generalization, in patients 3 years of age and older.[ Read more

Pharmacodynamic

Gabapentin is an anti-convulsant medication that inhibits the release of excitatory neurotransmitters, allowing for its use against pathologic neurotransmission such as that seen in neuropathic pain and seizure disorders.[ Read more

Mechanism of action

The precise mechanism through which gabapentin exerts its therapeutic effects is unclear.[16, Read more

Absorption

Absorption of gabapentin is thought to occur solely via facilitated transport by the LAT1 transporter within the intestines.[ Read more

Protein binding

Less than 3% of an orally administered dose of gabapentin is bound to plasma proteins.[16, Read more

Volume of distribution

The apparent volume of distribution of gabapentin after IV administration is 58±6 L.[16, Read more

Clearance

Both the plasma clearance and renal clearance of gabapentin are directly proportional to the patient's creatinine clearance due to its primarily renal elimination.[16, Read more

Half life

The elimination t1/2 of gabapentin in patients with normal renal function is 5-7 hours.[16, Read more

Route of elimination

Gabapentin is eliminated solely in the urine as unchanged drug.[16,17] Cimetidine,... Read more

Toxicity

The oral TDLo of gabapentin in humans is 2.86 mg/kg and the LD50 in rats has been found to be >8000 mg/kg.[21] Symptoms of overdose are consistent with the drug's adverse effect profile and involve CN... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Dizziness US
  • Kind: experimental
    • Percent: 28
  • Kind: placebo
    • Percent: 8
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 21
  • Kind: placebo
    • Percent: 5
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 19
  • Kind: placebo
    • Percent: 9
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 17
  • Kind: placebo
    • Percent: 7
  • Clinical Trial
    Ataxia US
  • Kind: experimental
    • Percent: 13
  • Kind: placebo
    • Percent: 6
  • Clinical Trial
    Viral Infection US
  • Kind: experimental
    • Percent: 11
  • Kind: placebo
    • Percent: 3
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 11
  • Kind: placebo
    • Percent: 5
  • Clinical Trial
    Fever US
  • Kind: experimental
    • Percent: 10
  • Kind: placebo
    • Percent: 3
  • Clinical Trial
    Hostility US
  • Kind: experimental
    • Percent: 8
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 8
  • Kind: placebo
    • Percent: 5
  • Clinical Trial
    Nausea and vomiting US
  • Kind: experimental
    • Percent: 8
  • Kind: placebo
    • Percent: 7
  • Clinical Trial
    Nystagmus US
  • Kind: experimental
    • Percent: 8
  • Kind: placebo
    • Percent: 4
  • Clinical Trial
    Peripheral Edema US
  • Kind: experimental
    • Percent: 8
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: 7
  • Kind: placebo
    • Percent: 3
  • Clinical Trial
    Diplopia US
  • Kind: experimental
    • Percent: 6
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 6
  • Kind: placebo
    • Percent: 3
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: 6
  • Kind: placebo
    • Percent: 5
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 5
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Infection US
  • Kind: experimental
    • Percent: 5
  • Kind: placebo
    • Percent: 4
  • Clinical Trial
    Emotional Lability US
  • Kind: experimental
    • Percent: 4
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Amblyopia US
  • Kind: experimental
    • Percent: 4
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 4
  • Kind: placebo
    • Percent: 3
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 4
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Respiratory Infection US
  • Kind: experimental
    • Percent: 3
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Bronchitis US
  • Kind: experimental
    • Percent: 3
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Hyperkinesia US
  • Kind: experimental
    • Percent: 3
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 3
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 3
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Increased weight US
  • Kind: experimental
    • Percent: 3
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 3
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Increased weight US
  • Kind: experimental
    • Percent: 3
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Amblyopia US
  • Kind: experimental
    • Percent: 3
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Abnormal thinking US
  • Kind: experimental
    • Percent: 3
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Ataxia US
  • Kind: experimental
    • Percent: 3
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 3
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Accidental injury US
  • Kind: experimental
    • Percent: 3
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Impotence US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Coughing US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Abnormal thinking US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Depression US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Amnesia US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Dysarthria US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Dental Abnormalities US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Dry mouth or throat US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Dyspepsia US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Peripheral Edema US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Back Pain US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Incoordination US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Abnormal Gait US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 0
  • Clinical Trial

    Contraindications

    • Hypersensitivity:
      • true
    • Regions: US

    Food Interactions

    Avoid alcohol. Gabapentin possesses CNS depressant activity that may be potentiated by co-administration with alcohol.

    Take with or without food. Co-administration with food slightly alters pharmacokinetics, but not to a clinically significant extent.