Tiagabine

What is Tiagabine

Tiagabine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures. It is a derivative of nipecotic acid, a compound found in the betel nut from southeast Asia.

Tiagabine’s mechanism of action differs from other adjunctive therapies for partial seizures (e.g., gabapentin, lamotrigine, vigabatrin, topiramate) in that it inhibits the reuptake of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the CNS.

When added to other antiepileptic drug regimens, tiagabine significantly decreases seizure frequency (by 50% or more) in about 25% of patients with refractory complex partial seizures and in roughly 32% of patients with simple complex seizures.

About 45% of patients with secondary generalized tonic-clonic seizures achieve a 50% or greater reduction in seizure rate. The antiepileptic effects of tiagabine are dose-dependent, with a minimal effective dose of about 32 mg for most patients.

Some data indicate that this agent may also be effective for monotherapy in selected patients. Tiagabine was granted final FDA approval for the adjunctive treatment of partial seizures in September 1997. 

Brand Name

Gabitril

Indications

  • partial seizures

Side Effects

  1. abdominal pain
  2. agitation
  3. alopecia
  4. amblyopia
  5. amenorrhea
  6. anemia
  7. angina
  8. apnea
  9. appetite stimulation
  10. arthralgia
  11. asthenia
  12. ataxia
  13. atopic dermatitis
  14. blepharitis
  15. blurred vision
  16. breast enlargement
  17. bronchospasm
  18. bullous rash
  19. chest pain (unspecified)
  20. chills
  21. cholecystitis
  22. cholelithiasis
  23. choreoathetosis
  24. coma
  25. confusion
  26. contact dermatitis
  27. cough
  28. cystitis
  29. dehydration
  30. dental caries
  31. depression
  32. diarrhea
  33. dizziness
  34. drowsiness
  35. dysarthria
  36. dysgeusia
  37. dysmenorrhea
  38. dysphagia
  39. dyspnea
  40. dystonic reaction
  41. dysuria
  42. ecchymosis
  43. edema
  44. EEG changes
  45. elevated hepatic enzymes
  46. emotional lability
  47. encephalopathy
  48. epistaxis
  49. eructation
  50. esophagitis
  51. euphoria
  52. exfoliative dermatitis
  53. fecal incontinence
  54. furunculosis
  55. gastritis
  56. GI bleeding
  57. gingival hyperplasia
  58. gingivitis
  59. glossitis
  60. goiter
  61. halitosis
  62. hallucinations
  63. hearing loss
  64. hematuria
  65. hemoptysis
  66. hepatomegaly
  67. hiccups
  68. hirsutism
  69. hostility
  70. hyperacusis
  71. hypercholesterolemia
  72. hyperglycemia
  73. hyperhidrosis
  74. hyperkinesis
  75. hyperlipidemia
  76. hyperreflexia
  77. hypersalivation
  78. hypertension
  79. hypertonia
  80. hyperventilation
  81. hypoesthesia
  82. hypoglycemia
  83. hypokalemia
  84. hyponatremia
  85. hyporeflexia
  86. hypotension
  87. hypothyroidism
  88. hypotonia
  89. impotence (erectile dysfunction)
  90. infection
  91. influenza
  92. insomnia
  93. keratoconjunctivitis
  94. laryngitis
  95. leukopenia
  96. libido decrease
  97. libido increase
  98. lymphadenopathy
  99. maculopapular rash
  100. malaise
  101. mastalgia
  102. melena
  103. memory impairment
  104. menorrhagia
  105. migraine
  106. muscle cramps
  107. myalgia
  108. myasthenia
  109. myocardial infarction
  110. myoclonia
  111. nausea
  112. neuritis
  113. nocturia
  114. nystagmus
  115. ocular pain
  116. oral ulceration
  117. orthostatic hypotension
  118. otalgia
  119. pallor
  120. palpitations
  121. paranoia
  122. paresthesias
  123. parosmia
  124. pelvic pain
  125. peripheral edema
  126. peripheral vasodilation
  127. petechiae
  128. pharyngitis
  129. phlebitis
  130. photophobia
  131. photosensitivity
  132. polydipsia
  133. polyuria
  134. pruritus
  135. psoriasis
  136. psychosis
  137. rash
  138. renal failure (unspecified)
  139. seizures
  140. sinus tachycardia
  141. skin discoloration
  142. skin ulcer
  143. spontaneous fetal abortion
  144. Stevens-Johnson syndrome
  145. stomatitis
  146. suicidal ideation
  147. syncope
  148. teratogenesis
  149. thrombocytopenia
  150. tinnitus
  151. tremor
  152. urinary incontinence
  153. urinary retention
  154. urinary urgency
  155. urticaria
  156. vaginal bleeding
  157. vaginitis
  158. vertigo
  159. vesicular rash
  160. visual impairment
  161. vomiting
  162. weakness
  163. xerosis
  164. xerostomia

Monitoring Parameters

  • LFTs

Contraindications

  • abrupt discontinuation
  • bipolar disorder
  • breast-feeding
  • children
  • depression
  • driving or operating machinery
  • geriatric
  • hepatic disease
  • infants
  • mania
  • neonates
  • pregnancy
  • seizures
  • status epilepticus
  • suicidal ideation

Interactions

  • Alprazolam
  • Amitriptyline
  • Amitriptyline; Chlordiazepoxide
  • Amphetamines
  • Apalutamide
  • Aprepitant, Fosaprepitant
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Benzodiazepines
  • Boceprevir
  • Bupropion
  • Bupropion; Naltrexone
  • Chlordiazepoxide
  • Chlordiazepoxide; Clidinium
  • Chlorpromazine
  • Clomipramine
  • Clonazepam
  • Clorazepate
  • Cobicistat
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • Colesevelam
  • Conivaptan
  • Crizotinib
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Desipramine
  • Dextromethorphan; Promethazine
  • Diazepam
  • Doxepin
  • Dronedarone
  • Elbasvir; Grazoprevir
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Enzalutamide
  • Estazolam
  • Ethanol
  • Fluphenazine
  • Flurazepam
  • Hydantoins
  • Hydroxychloroquine
  • Idelalisib
  • Imipramine
  • Isavuconazonium
  • Isocarboxazid
  • Lesinurad
  • Lesinurad; Allopurinol
  • Lopinavir; Ritonavir
  • Lorazepam
  • Maprotiline
  • Mefloquine
  • Meperidine; Promethazine
  • Mesoridazine
  • Midazolam
  • Mitotane
  • Molindone
  • Monoamine oxidase inhibitors
  • Netupitant, Fosnetupitant; Palonosetron
  • Nortriptyline
  • Ombitasvir; Paritaprevir; Ritonavir
  • Oritavancin
  • Oxazepam
  • Pazopanib
  • Pemoline
  • Perphenazine
  • Perphenazine; Amitriptyline
  • Phenelzine
  • Phenobarbital
  • Phenothiazines
  • Phentermine; Topiramate
  • Phenylephrine; Promethazine
  • Posaconazole
  • Prochlorperazine
  • Promethazine
  • Protriptyline
  • Quazepam
  • Ritonavir
  • Selegiline
  • Simeprevir
  • St. John’s Wort, Hypericum perforatum
  • Telaprevir
  • Telotristat Ethyl
  • Temazepam
  • Thiethylperazine
  • Thioridazine
  • Topiramate
  • Tranylcypromine
  • Triazolam
  • Tricyclic antidepressants
  • Trifluoperazine
  • Trimipramine
  • Valproic Acid, Divalproex Sodium
  • Vemurafenib
  • Voriconazole
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