Tiagabine

Indications
 Oral
Adjunct in refractory partial seizures
Adult: 5 mg bid for 1 wk, may increase on a wkly basis by increments of 5-10 mg. Usual maintenance dose: 15-30 mg daily, in 3 divided doses; higher doses of 30-45 mg daily may be used in patients on enzyme-inducing antiepileptics.
Hepatic impairment: Mild-moderate: Initial maintenance dose of 5-10 mg daily. Avoid in severe impairment.
Warnings / Precautions
 Discontinue treatment if there is sign of hypersensitivity. Hepatic impairment. Safety and efficacy have not been established in children <12 yr. Avoid abrupt withdrawal. Monitor for any sign/symptom (e.g. behaviour changes, anxiety, depression) of suicidal tendency or ideation. Pregnancy and lactation.
Adverse Reactions
 CNS depression, dizziness, nervousness, somnolence. Nausea, diarrhoea, abdominal pain, tremor, weakness, chest pain, oedema, hypertension, palpitation, peripheral oedema, syncope, tachycardia, vasodilation.
Potentially Fatal: Severe reactions, including toxic epidermal necrolysis and Stevens-Johnson syndrome.
Overdose Reactions
 Symptoms include somnolence, impaired consciousness, agitation, confusion, speech difficulty, hostility, depression, weakness, and myoclonus. There is no specific antidote. Unabsorbed drug may be removed by emesis or gastric lavage. General supportive care including monitoring of vital signs and observation of clinical status of the patient should be administered when needed.
Drug Interactions
 Increased sedation when used with other sedative drugs or ethanol. Valproate may increase free tiagabine levels. Concurrent use with CYP3A4 inhibitors (e.g. azole antifungals, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, telithromycin and verapamil) may increase levels of tiagabine. CYP3A4 inducers (e.g. aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin and rifamycins) may decrease levels of tiagabine.
See Below for More tiagabine Drug Interactions
Food Interactions
 St John's wort may decrease tiagabine levels. Avoid valerian, kava kava, gotu kola (may increase CNS depression).
Mechanism of Actions
 Tiagabine is a nipecotic acid derivative that is used as an adjunct in the treatment of partial seizures. The exact mechanism not known but in vitro experiments show that it increases the activity of gamma aminobutyric acid (GABA) by binding to the GABA uptake carrier, thus inhibiting the uptake of GABA into presynaptic neurons, resulting in an increased amount of GABA to be available to postsynaptic neurons.
Absorption: Readily absorbed after oral admin.
Distribution: Widely distributed throughout the body. Plasma protein binding: 96%.
Metabolism: Largely metabolised in the liver.
Excretion: Excreted as metabolites in the faeces and, to a lesser extent, in the urine. <2% of a dose is eliminated as unchanged drug. Elimination half-life: 7-9 hr.
Administration
 Should be taken with food.
Storage Conditions
 Oral: Store at 20-25°C.
ATC Classification
 N03AG06 - tiagabine ; Belongs to the class of fatty acid derivatives antiepileptic.
Storage
 Oral: Store at 20-25°C.
Available As
  • Tiagabine 12 mg
  • Tiagabine 2 mg
  • Tiagabine 4 mg

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