Buy Tiagabine (Gabitril) Cas115103-54-3

Tiagabine, sold under the brand name Gabitril, is an anticonvulsant medication which is used in the treatment of epilepsy.^[1][2][3][8] It is also used off-label in the treatment of insomnia^[9][10][11] and anxiety disorders.^[12] However, off-label use is discouraged as the drug has been associated with new-onset seizures in people without epilepsy.^[13][14][1] Tiagabine is taken orally.^[3][2]

Side effects of tiagabine include dizziness, asthenia, non-specific nervousness, muscle tremors, diarrhea, depression, and emotional lability.^[3][1] The drug acts as a selective GABA transporter 1 (GAT-1) blocker or GABA reuptake inhibitor, and hence acts as an indirect GABA receptor agonist, increasing GABAergic signaling in the brain.^{[3][15][16][17][6][18]} It may increase activation of both GABA_A and GABA_B receptors.^[17][19][20] The effects of tiagabine on sleep resemble those of GABA_A receptor agonists like gaboxadol and muscimol, primarily enhancing slow wave sleep, and differ from those of GABA_A receptor positive allosteric modulators like benzodiazepines and Z drugs.^{[21][18][9][22][17]} The drug’s elimination half-life is 4.5 to 9 hours, but can be shorter in people taking enzyme-inducing anticonvulsants.^[3][6][1][2]

Tiagabine was discovered in 1988^[23] and was introduced for medical use in 1997.^[24][8] Generic formulations have become available.^[25] The drug is not a controlled substance in the United States.^[26]

Tiagabine is approved by the United States Food and Drug Administration (FDA) as an adjunctive treatment for partial seizures in epilepsy in individuals of age 12 and up. It is effective as monotherapy and combination therapy with other anticonvulsant drugs in the treatment of partial seizure.^[27]

Tiagabine is used in the treatment of insomnia.^{[9][28][10][11]} Lower doses than those used in epilepsy, in the range of 2 to 16 mg, are used to treat insomnia.^[29][30]

The drug has been found to enhance slow wave sleep (SWS) in the context of insomnia.^{[9][28][31][32][33][34]} Its effects on SWS are dose dependent, with a 2- to 4-fold increase in SWS at doses of 8 to 16 mg but mixed findings for a dose of 4 mg.^{[9][32][34][31][33]} Findings are mixed in terms of the influence of tiagabine on sleep onset, sleep duration, nighttime awakenings, self-reported sleep ratings, and ratings of restorative or refreshing sleep.^{[9][31][32][33][34]} Tiagabine has been found to decrease the cognitive impairment and high cortisol levels caused by sleep restriction, with this being related to the drug’s SWS improvement.^{[9][35][28][36]} On the other hand, despite increasing SWS, tiagabine did not improve memory consolidation.^[37]

The effects of tiagabine on sleep, for instance primarily increasing SWS, resemble those of gaboxadol and muscimol but are very different from those of conventional GABA_A receptor positive allosteric modulators like benzodiazepines and Z drugs.^{[21][18][9][22][14][17][38]}

The American Academy of Sleep Medicine‘s 2017 clinical practice guidelines recommended against the use of tiagabine in the treatment of insomnia due to limited effectiveness and very low quality of evidence.^[10]

Tiagabine may be prescribed off-label to treat certain anxiety disorders, such as panic disorder and social anxiety disorder.^[39][40][41] Tiagabine may be used alongside selective serotonin reuptake inhibitors (SSRIs), serotonin–norepinephrine reuptake inhibitors (SNRIs), or benzodiazepines for anxiety.^[39] The drug was ineffective for generalized anxiety disorder.^[42][43][44]