pharmacopeia
GET
/api/v1/drug/gabapentin
2D structure
2-[1-(aminomethyl)cyclohexyl]acetic acid
SMILES C1CCC(CC1)(CC(=O)O)CN
InChIKey UGJMXCAKCUNAIE-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

The precise mechanisms by which gabapentin produces its analgesic and antiepileptic actions are unknown. Gabapentin is structurally related to the neurotransmitter gamma-aminobutyric acid (GABA) but has no effect on GABA binding, uptake, or degradation.

Indications

Sourced from openFDA
  • Gabapentin Capsules, USP are indicated for: Management of postherpetic neuralgia in adults Adjunctive therapy in the treatment of partial onset seizures, with and without secondary generalization, in adults and pediatric patients 3 years and older with epilepsy Gabapentin Capsules, USP are indicated for Postherpetic neuralgia in adults (1) Adjunctive therapy in the treatment of partial onset seizures, with and without secondary generalization, in adults and pediatric patients 3 years and older with epilepsy (1)ICD-10: G40.909

Contraindications

Sourced from openFDA
  • Gabapentin is contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients.contraindicated

Dosage & administration

Sourced from openFDA

DOSAGE AND ADMlNlSTRATION Postherpetic Neuralgia (2.1) Dose can be titrated up as needed to a dose of 1800 mg/day Day 1: Single 300 mg dose Day 2: 600 mg/day (i.e., 300 mg two times a day) Day 3: 900 mg/day (i.e., 300 mg three times a day) Epilepsy with Partial Onset Seizures (2.2) Patients 12 years of age and older: starting dose is 300 mg three times daily; may be titrated up to 600 mg three times daily Patients 3 to 11 years of age: starting dose range is 10 to 15 mg/kg/day, given in three divided doses; recommended dose in patients 3 to 4 years of age is 40 mg/kg/day, given in three divided doses; the recommended dose in patients 5 to 11 years of age is 25 to 35 mg/kg/day, given in three divided doses. The recommended dose is reached by upward titration over a period of approximately 3 days Dose should be adjusted in patients with reduced renal function ( 2.3 , 2.4 ) 2.1 Dosage for Postherpetic Neuralgia In adults with postherpetic neuralgia, Gabapentin may be initiated on Day 1 as a single 300 mg dose, on Day 2 as 600 mg/day (300 mg two times a day), and on Day 3 as 900 mg/day (300 mg three times a day). The dose can subsequently be titrated up as needed for pain relief to a dose of 1800 mg/day (600 mg three times a day).

Warnings & precautions

Sourced from openFDA

Drug Reaction with Eosinophilia and Systemic Symptoms (Multiorgan hypersensitivity): Discontinue if alternative etiology is not be established (5.1) Anaphylaxis and Angioedema: Discontinue and evaluate patient immediately (5.2) Driving impairment; Somnolence/Sedation and Dizziness: Warn patients not to drive until they have gained sufficient experience to assess whether their ability to drive or operate heavy machinery will be impaired (5.3, 5.4) Increased seizure frequency may occur in patients with seizure disorders if Gabapentin is abruptly discontinued (5.5) Suicidal Behavior and Ideation: Monitor for suicidal thoughts / behavior (5.6) Respiratory depression: May occur with gabapentin when used with concomitant central nervous system (CNS) depressants, including opioids, or in the setting of underlying respiratory impairment. Monitor patients and adjust dosage as appropriate ( 5.7 ) Neuropsychiatric Adverse Reactions in Children 3 to 12 Years of Age: Monitor for such events ( 5.8 ) 5.1 Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)/Multiorgan Hypersensitivity Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS), also known as multiorgan hypersensitivity, has occurred with Gabapentin. Some of these reactions have been fatal or life-threatening. DRESS typically, although not exclusively, presents with fever, rash, and/or lymphadenopathy, in association with other organ system involvement, such as hepatitis, nephritis, hematological abnormalities, myocarditis, or myositis sometimes resembling an acute viral infection. Eosinophilia is often present.

Adverse reactions

Sourced from openFDA

The following serious adverse reactions are discussed in greater detail in other sections: Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)/Multiorgan Hypersensitivity [see Warnings and Precautions (5.1) ] Anaphylaxis and Angioedema [see Warnings and Precautions (5.2) ] Somnolence/Sedation and Dizziness [see see Warnings and Precautions (5.4) ] Withdrawal Precipitated Seizure, Status Epilepticus [see see Warnings and Precautions (5.5) ] Suicidal Behavior and Ideation [see see Warnings and Precautions (5.6) ] Respiratory Depression [see Warnings and Precautions (5.7) ] Neuropsychiatric Adverse Reactions (Pediatric Patients 3 to 12 Years of Age) [ see Warnings and Precautions (5.8) ] Sudden and Unexplained Death in Patients with Epilepsy [see Warnings and Precautions (5.10) ] Most common adverse reactions (incidence ≥8% and at least twice that for placebo) were: Postherpetic neuralgia: Dizziness, somnolence, and peripheral edema (6.1) Epilepsy in patients >12 years of age: Somnolence, dizziness, ataxia, fatigue, and nystagmus (6.1) Epilepsy in patients 3 to 12 years of age: Viral infection, fever, nausea and/or vomiting, somnolence, and hostility (6.1) To report SUSPECTED ADVERSE REACTIONS, contact ACI HealthcareUSA, Inc. at 1-888-802-1213 or www.acihealthcareusa.com or FDA at1-800-FDA-1088 or www.fda.gov/medwatch.

Use in specific populations

Sourced from openFDA

Pregnancy: Based on animal data, may cause fetal harm (8.1) 8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to antiepileptic drugs (AEDs), such as Gabapentin, during pregnancy. Encourage women who are taking Gabapentin during pregnancy to enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry by calling the toll free number 1-888-233-2334 or visiting http://www.aedpregnancyregistry.org/. Risk Summary There are no adequate data on the developmental risks associated with the use of Gabapentin in pregnant women. In nonclinical studies in mice, rats, and rabbits, gabapentin was developmentally toxic (increased fetal skeletal and visceral abnormalities, and increased embryofetal mortality) when administered to pregnant animals at doses similar to or lower than those used clinically [see Data]. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. The background risk of major birth defects and miscarriage for the indicated population is unknown.

Pharmacokinetics

Sourced from openFDA
Metabolism
All pharmacological actions following gabapentin administration are due to the activity of the parent compound; gabapentin is not appreciably metabolized in humans. Oral Bioavailability Gabapentin bioavailability is not dose proportional; i.e., as dose is increased, bioavailability decreases.

Overdosage

Sourced from openFDA

Signs of acute toxicity in animals included ataxia, labored breathing, ptosis, sedation, hypoactivity, or excitation. Acute oral overdoses of gabapentin have been reported. Symptoms have included double vision, tremor, slurred speech, drowsiness, altered mental status, dizziness, lethargy, and diarrhea. Fatal respiratory depression has been reported with gabapentin overdose, alone and in combination with other CNS depressants. Gabapentin can be removed by hemodialysis. If overexposure occurs, call your poison control center at 1-800-222-1222.

Approval history

Sourced from openFDA
  • Dec 30, 1993NDANDA020235Viatris
  • Oct 9, 1998NDANDA020882Viatris
  • Mar 2, 2000NDANDA021129Viatris
  • Sep 12, 2003ANDAANDA075350Actavis Elizabeth
  • Mar 23, 2005ANDAANDA075477Cspc Ouyi
  • Apr 6, 2005ANDAANDA075360Granules
  • Jan 28, 2011NDANDA022544Almatica
  • Apr 6, 2011NDANDA022399Azurity

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
359,782 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Drug Ineffective29,4508.2%
  2. 2Fatigue24,8816.9%
  3. 3Nausea22,4306.2%
  4. 4Pain21,0605.9%
  5. 5Off Label Use19,5075.4%
  6. 6Diarrhoea17,8605.0%
  7. 7Headache17,6624.9%
  8. 8Dizziness16,3344.5%
  9. 9Fall15,4294.3%
  10. 10Dyspnoea14,0203.9%
  11. 11Vomiting11,9713.3%
  12. 12Asthenia11,8443.3%
  13. 13Pain In Extremity11,5403.2%
  14. 14Arthralgia11,3363.2%
  15. 15Death10,9973.1%

Literature

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Recent PubMed references pinned to Gabapentin as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 567 ClinicalTrials.gov registrations naming Gabapentin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Gabapentin work?
The precise mechanisms by which gabapentin produces its analgesic and antiepileptic actions are unknown. Gabapentin is structurally related to the neurotransmitter gamma-aminobutyric acid (GABA) but has no effect on GABA binding, uptake, or degradation.
What is Gabapentin used for?
According to FDA labeling, Gabapentin carries indications including: Gabapentin Capsules, USP are indicated for: Management of postherpetic neuralgia in adults Adjunctive therapy in the treatment of partial onset seizures, with and without secondary generalization, in adults and pediatric patients 3 years and older with epilepsy Gabapentin Capsules, USP are indicated for Postherpetic neuralgia in adults (1) Adjunctive therapy in the treatment of partial onset seizures, with and without secondary generalization, in adults and pediatric patients 3 years and older with epilepsy (1). This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Gabapentin?
Gabapentin is classified as Gabapentinoids, Unknown Cellular or Molecular Interaction, Decreased Central Nervous System Disorganized Electrical Activity, Decreased Disorganized Electrical Activity, Decreased Organized Electrical Activity.
What are the brand names for Gabapentin?
Gabapentin is marketed under brand names including Gabarone, Gralise, Horizant, Neurontin, Relgaabi.
What are the contraindications for Gabapentin?
Gabapentin labeling lists contraindications including: Gabapentin is contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients.. Always consult the full prescribing information and a clinician.
Note. Data for gabapentin is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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