Tiagabine

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Tiagabine
Systematic (IUPAC) name
(3S)-1-[4,4-bis(3-methylthiophen-2-yl)but-3-enyl] piperidine-3-carboxylic acid
Identifiers
CAS number 115103-54-3
ATC code N03AG06
PubChem 60648
DrugBank APRD00344
Chemical data
Formula C20H25NO2S2 
Mol. mass 375.55 g/mol
Pharmacokinetic data
Bioavailability 90%
Protein binding 96%
Metabolism Hepatic (CYP450 system)
Half life 7-9 hours
Excretion Fecal and renal
Therapeutic considerations
Pregnancy cat.

B3 (Au), C (U.S.)

Legal status

POM (UK), ℞-only (U.S.)

Routes Oral

Tiagabine (pronounced /taɪˈæɡəbiːn]/[1]) is an anti-convulsive medication produced by Cephalon and marketed under the brand name Gabitril. The drug was discovered at Novo Nordisk in Denmark in 1988. and was co-developed with Abbott. After a period of co-promotion, Cephalon licensed Tiagabine from Abbott/Novo and now are the exclusive producer. The medication is also used in the treatment of panic disorder as are a few other anticonvulsants.

Contents

[edit] Pharmacology

It is believed that the pharmacology is related to its ability, documented in in vitro experiments, to enhance the activity of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. These experiments have shown that tiagabine binds to recognition sites associated with the GABA uptake carrier. It is thought that, by this action, tiagabine blocks GABA uptake into presynaptic neurons, permitting more GABA to be available for receptor binding on the surfaces of post-synaptic cells. evidence is available that it operates as a selective GABA reuptake inhibitor.[1]

[edit] Side effects

Tiagabine's most common side effects include confusion, difficulty speaking clearly/stuttering, mild sedation, and in doses over 8 mg, a tingling sensation (paresthesia) in the body's extremities, particularly the hands and fingers.

[edit] References

[edit] External links

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