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    Tiagabine molecular structure

    Tiagabine Stats & Data

    Gabitril
    NPS DataHub
    MW375.56
    FormulaC20H25NO2S2
    CAS115103-54-3
    IUPAC(3R)-1-[4,4-bis(3-methylthiophen-2-yl)but-3-enyl]piperidine-3-carboxylic acid
    SMILESO=C([O-])C1CCCN(CCC=C(c2sccc2C)c2sccc2C)C1.[H+]
    InChIKeyPBJUNZJWGZTSKL-MRXNPFEDSA-N
    Chemical Class medicine
    Psychoactive Class Depressant

    Pharmacology

    DrugBank
    Half-life 7-9 hours Protein binding 96% State Solid Clearance * 109 mL/min Healthy subjects

    Description

    Tiagabine is an anti-convulsive medication. It is also used in the treatment for panic disorder as are a few other anticonvulsants. Though the exact mechanism by which tiagabine exerts its effect on the human body is unknown, it does appear to operate as a selective GABA reuptake inhibitor.

    Mechanism of Action

    Though the exact mechanism by which Tiagabine exerts its effect on the human body is unknown, it does appear to operate as a selective GABA reuptake inhibitor.

    Pharmacodynamics

    Tiagabine is used primarily as an anticonvulsant for the adjunctive treatment of epilepsy. The precise mechanism by which Tiagabine exerts its antiseizure effect is unknown, although it is believed to be related to its ability to enhance the activity of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. 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.

    Metabolism

    Tiagabine is likely metabolized primarily by the 3A isoform subfamily of hepatic cytochrome P450.

    Absorption

    Tiagabine is nearly completely absorbed (>95%).

    Toxicity

    mptoms most often accompanying tiagabine overdose, alone or in combination with other drugs, have included: seizures including status epilepticus in patients with and without underlying seizure disorders, nonconvulsive status epilepticus, coma, ataxia, confusion, somnolence, drowsiness, impaired speech, agitation, lethargy, myoclonus, spike wave stupor, tremors, disorientation, vomiting, hostility, and temporary paralysis. Respiratory depression was seen in a number of patients, including children, in the context of seizures.

    Indication

    For the treatment of partial seizures

    Elimination

    Approximately 2% of an oral dose of tiagabine is excreted unchanged, with 25% and 63% of the remaining dose excreted into the urine and feces, respectively, primarily as metabolites.

    Tolerance & Pharmacokinetics

    drugs.wiki

    Tolerance Decay

    Full tolerance 3d Half tolerance 8d Baseline ~14d

    Experience Report Analysis

    Erowid
    7 Reports
    2003–2008 Date Range
    1 Effects Detected

    Demographics

    Gender Distribution

    Reports Over Time

    Effect Analysis

    Erowid

    Effects aggregated from 7 experience reports (7 Erowid)

    7 Reports
    1 Effects Detected
    1 Positive
    0 Adverse
    0 Neutral

    Effect Sentiment Distribution

    Confidence Distribution

    Positive Effects 1

    Sedation 57.1% 70%

    Adverse Effects 0

    Real-World Dose Distribution

    62K Doses

    From 7 individual dose entries

    Oral (n=7)

    Median: 36.0mg 25th: 18.0mg 75th: 54.0mg 90th: 64.8mg
    mg/kg median: 0.397 mg/kg 75th: 0.672

    Form / Preparation

    Most common forms and preparations reported

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