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