Gabapentin

Gabapentin Brand Names

Active-PAC with Gabapentin | Gabarone | Gralise | Horizant | Neurontin

What is Gabapentin

Gabapentin is an analog of gamma-aminobutyric acid (GABA) that has GABA agonist activity. Its unique pharmacokinetic properties make it especially useful in certain patients.

Gabapentin possesses high lipid solubility, is not metabolized by the liver, has no protein binding, and is devoid of enzyme induction-related drug interactions.

Originally developed as an anticonvulsant, gabapentin has been shown to be effective as adjunct therapy in the treatment of partial seizures with or without secondary generalized tonic-clonic seizures. Efficacy in the treatment of painful neuropathies has also been demonstrated.

Investigational uses include monotherapy of refractory partial seizure disorders, treatment of spasticity in multiple sclerosis, and tremor. In addition, gabapentin appears to be effective in reducing hot flashes in menopausal women or women with breast cancer.

Data from well-controlled clinical trials have not demonstrated a treatment advantage for gabapentin over placebo in the treatment of bipolar disorder, even when used adjunctively. At this time, the clinical evidence does not support the use of this drug for bipolar I disorder.

This medication has been designed as an orphan drug in the treatment of amyotrophic lateral sclerosis (ALS) and postherpetic neuralgia (PHN).

Gabapentin (Neurontin) was approved by the FDA in December 1993 for the treatment of partial seizures and in May 2002 for the treatment of PHN. A once-daily tablet (Gralise) was approved in January 2011 for PHN.

Gabapentin enacarbil (Horizant) extended-release tablets were approved by the FDA in April 2011 for the treatment of moderate to severe primary restless legs syndrome (RLS) in adults and in June 2012 for the treatment of PHN in adults.

Indications

  1. alcohol dependence
  2. amyotrophic lateral sclerosis (ALS)
  3. diabetic neuropathy
  4. dysautonomia
  5. fibromyalgia
  6. hot flashes
  7. menopause
  8. multiple sclerosis
  9. nystagmus
  10. partial seizures
  11. postherpetic neuralgia
  12. pruritus
  13. restless legs syndrome (RLS)
  14. short-lasting unilateral neuralgiform headache with conjunctival injection and tearing
  15. singultus (hiccups)
  16. spasticity
  17. tremor

Side Effects

  1. amblyopia
  2. amnesia
  3. anaphylactoid reactions
  4. angioedema
  5. anorexia
  6. appetite stimulation
  7. asthenia
  8. ataxia
  9. back pain
  10. blurred vision
  11. bullous rash
  12. choreoathetosis
  13. confusion
  14. conjunctivitis
  15. constipation
  16. cough
  17. dehydration
  18. depression
  19. diarrhea
  20. diplopia
  21. dizziness
  22. drowsiness
  23. Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)
  24. dysarthria
  25. dyspepsia
  26. dyspnea
  27. dystonic reaction
  28. emotional lability
  29. eosinophilia
  30. erythema multiforme
  31. fatigue
  32. fever
  33. flatulence
  34. headache
  35. hepatitis
  36. hostility
  37. hyperglycemia
  38. hypertension
  39. hyponatremia
  40. impaired cognition
  41. infection
  42. insomnia
  43. involuntary movements
  44. irritability
  45. jaundice
  46. lethargy
  47. libido decrease
  48. memory impairment
  49. nausea
  50. nystagmus
  51. peripheral edema
  52. peripheral vasodilation
  53. pharyngitis
  54. rash
  55. respiratory depression
  56. restlessness
  57. rhabdomyolysis
  58. rhinitis
  59. skin irritation
  60. Stevens-Johnson syndrome
  61. suicidal ideation
  62. teratogenesis
  63. tolerance
  64. tremor
  65. vertigo
  66. vomiting
  67. weight gain
  68. withdrawal
  69. xerostomia

Monitoring Parameters

  • serum creatinine/BUN
  • WBC

Contraindications

  • abrupt discontinuation
  • breast-feeding
  • chronic obstructive pulmonary disease (COPD)
  • coadministration with other CNS depressants
  • depression
  • dialysis
  • driving or operating machinery
  • geriatric
  • pregnancy
  • pulmonary disease
  • renal failure
  • renal impairment
  • respiratory depression
  • substance abuse
  • suicidal ideation

Interactions

  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
  • Acetaminophen; Codeine
  • Acetaminophen; Dextromethorphan; Doxylamine
  • Acetaminophen; Diphenhydramine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Pentazocine
  • Acetaminophen; Propoxyphene
  • Acetaminophen; Tramadol
  • Acrivastine; Pseudoephedrine
  • Alfentanil
  • Alprazolam
  • Aluminum Hydroxide
  • Aluminum Hydroxide; Magnesium Carbonate
  • Aluminum Hydroxide; Magnesium Hydroxide
  • Aluminum Hydroxide; Magnesium Hydroxide; Simethicone
  • Aluminum Hydroxide; Magnesium Trisilicate
  • Amitriptyline; Chlordiazepoxide
  • Amobarbital
  • Amoxapine
  • Amphetamines
  • Antacids
  • Apomorphine
  • Aripiprazole
  • Asenapine
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Citric Acid; Sodium Bicarbonate
  • Aspirin, ASA; Oxycodone
  • Atropine
  • Atropine; Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Atropine; Difenoxin
  • Atropine; Diphenoxylate
  • Atropine; Edrophonium
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Azelastine
  • Azelastine; Fluticasone
  • Baclofen
  • Barbiturates
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Belladonna; Opium
  • Benzhydrocodone; Acetaminophen
  • Benzodiazepines
  • Brexpiprazole
  • Brompheniramine
  • Brompheniramine; Carbetapentane; Phenylephrine
  • Brompheniramine; Dextromethorphan; Guaifenesin
  • Brompheniramine; Dextromethorphan; Phenylephrine
  • Brompheniramine; Guaifenesin; Hydrocodone
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Brompheniramine; Pseudoephedrine
  • Buprenorphine
  • Buprenorphine; Naloxone
  • Bupropion
  • Bupropion; Naltrexone
  • Butabarbital
  • Butorphanol
  • Calcium Carbonate
  • Calcium Carbonate; Magnesium Hydroxide
  • Calcium Carbonate; Risedronate
  • Calcium Carbonate; Simethicone
  • Cannabidiol
  • Capsaicin; Metaxalone
  • Carbetapentane; Chlorpheniramine
  • Carbetapentane; Chlorpheniramine; Phenylephrine
  • Carbetapentane; Diphenhydramine; Phenylephrine
  • Carbetapentane; Phenylephrine; Pyrilamine
  • Carbetapentane; Pyrilamine
  • Carbidopa; Levodopa
  • Carbidopa; Levodopa; Entacapone
  • Carbinoxamine
  • Carbinoxamine; Dextromethorphan; Pseudoephedrine
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Carbinoxamine; Phenylephrine
  • Carbinoxamine; Pseudoephedrine
  • Cariprazine
  • Carisoprodol
  • Cenobamate
  • Cetirizine
  • Cetirizine; Pseudoephedrine
  • Chlophedianol; Dexbrompheniramine
  • Chlophedianol; Dexchlorpheniramine; Pseudoephedrine
  • Chloral Hydrate
  • Chlorcyclizine
  • Chlordiazepoxide
  • Chlordiazepoxide; Clidinium
  • Chlorpheniramine
  • Chlorpheniramine; Codeine
  • Chlorpheniramine; Dextromethorphan
  • Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Phenylephrine
  • Chlorpheniramine; Pseudoephedrine
  • Chlorpromazine
  • Chlorthalidone; Clonidine
  • Chlorzoxazone
  • Clemastine
  • Clobazam
  • Clonazepam
  • Clonidine
  • Clorazepate
  • Clozapine
  • Codeine
  • Codeine; Guaifenesin
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • Colesevelam
  • Cyclizine
  • Cyclobenzaprine
  • Cyproheptadine
  • Dantrolene
  • Deutetrabenazine
  • Dexchlorpheniramine
  • Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Dexmedetomidine
  • Dextromethorphan; Diphenhydramine; Phenylephrine
  • Dextromethorphan; Promethazine
  • Diazepam
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Dimenhydrinate
  • Diphenhydramine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Diphenhydramine; Ibuprofen
  • Diphenhydramine; Naproxen
  • Diphenhydramine; Phenylephrine
  • Doxylamine
  • Doxylamine; Pyridoxine
  • Droperidol
  • Enflurane
  • Entacapone
  • Esketamine
  • Estazolam
  • Eszopiclone
  • Ethanol
  • Etomidate
  • Fenfluramine
  • Fentanyl
  • Flibanserin
  • Fluoxetine; Olanzapine
  • Fluphenazine
  • Flurazepam
  • Fospropofol
  • General anesthetics
  • Guaifenesin; Hydrocodone
  • Guaifenesin; Hydrocodone; Pseudoephedrine
  • Guanfacine
  • Haloperidol
  • Halothane
  • Homatropine; Hydrocodone
  • Hydrochlorothiazide, HCTZ; Methyldopa
  • Hydrochlorothiazide, HCTZ; Propranolol
  • Hydrocodone
  • Hydrocodone; Ibuprofen
  • Hydrocodone; Phenylephrine
  • Hydrocodone; Potassium Guaiacolsulfonate
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Hydrocodone; Pseudoephedrine
  • Hydromorphone
  • Hydroxychloroquine
  • Hydroxyzine
  • Ibuprofen; Oxycodone
  • Iloperidone
  • Isocarboxazid
  • Isoflurane
  • Ketamine
  • Lanthanum Carbonate
  • Lasmiditan
  • Lemborexant
  • Levocetirizine
  • Levodopa
  • Levorphanol
  • Lithium
  • Lofexidine
  • Lorazepam
  • Loxapine
  • Lumateperone
  • Lurasidone
  • Magnesium Hydroxide
  • Maprotiline
  • Meclizine
  • Mefloquine
  • Melatonin
  • Meperidine
  • Meperidine; Promethazine
  • Mephobarbital
  • Meprobamate
  • Metaxalone
  • Methadone
  • Methocarbamol
  • Methohexital
  • Methyldopa
  • Metoclopramide
  • Midazolam
  • Mirtazapine
  • Molindone
  • Monoamine oxidase inhibitors
  • Morphine
  • Morphine; Naltrexone
  • Nabilone
  • Nalbuphine
  • Nefazodone
  • Olanzapine
  • Omeprazole; Sodium Bicarbonate
  • Orphenadrine
  • Oxazepam
  • Oxycodone
  • Oxymorphone
  • Paliperidone
  • Pemoline
  • Pentazocine
  • Pentazocine; Naloxone
  • Pentobarbital
  • Perampanel
  • Perphenazine
  • Perphenazine; Amitriptyline
  • Phenelzine
  • Phenobarbital
  • Phenylephrine; Promethazine
  • Pimavanserin
  • Pimozide
  • Pramipexole
  • Pregabalin
  • Primidone
  • Prochlorperazine
  • Promethazine
  • Propofol
  • Propoxyphene
  • Propranolol
  • Quazepam
  • Quetiapine
  • Ramelteon
  • Rasagiline
  • Remifentanil
  • Risperidone
  • Ropinirole
  • Rotigotine
  • Safinamide
  • Scopolamine
  • Secobarbital
  • Selegiline
  • Sevoflurane
  • Sodium Bicarbonate
  • Sodium Oxybate
  • Sufentanil
  • Suvorexant
  • Tapentadol
  • Tasimelteon
  • Temazepam
  • Tetrabenazine
  • Thalidomide
  • Thiopental
  • Thioridazine
  • Thiothixene
  • Tizanidine
  • Tolcapone
  • Tramadol
  • Tranylcypromine
  • Trazodone
  • Triazolam
  • Tricyclic antidepressants
  • Trifluoperazine
  • Triprolidine
  • Valerian, Valeriana officinalis
  • Valproic Acid, Divalproex Sodium
  • Zaleplon
  • Ziprasidone
  • Zolpidem