Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0030193 (pain)
 261,466 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Gabitril (tiagabine) is a potent selective inhibitor of the principal neuronal gamma-aminobutyric acid (GABA) transporter (GAT-1) in the cortex and hippocampus. By slowing the reuptake of synaptically-released GABA, it prolongs inhibitory postsynaptic potentials. In animal models of epilepsy, tiagabine is particularly effective against kindled (limbic) seizures and against reflexly-induced generalized convulsive seizures. These data are predictive of its efficacy in complex partial seizures in humans. Possible clinical applications outside the field of epilepsy include bipolar disorder and pain.
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PMID:Basic mechanisms of gabitril (tiagabine) and future potential developments. 1061 55

To evaluate the effect of tiagabine hydrochloride in painful neuropathy in a pilot, open-label study. Painful neuropathy is characterized by preferential involvement of small sensory and autonomic fibers. Tiagabine increases gamma-aminobutyric acid and might enhance the central pain-control mechanisms. Seventeen patients (10 men, 7 women; mean age 51.4 +/- 7.7 y) with chronic painful neuropathy (>6 months) were enrolled in this study. Week 0: All pain medications were discontinued. Weeks 1-4: Dose of tiagabine was increased weekly by 4 mg orally up to 16 mg in week 4. Quantitative sensory testing for vibration, cooling, and heat-pain, and quantitative sudomotor axon reflex test (QSART) were done at week 0 and week 4. The McGill Pain Questionnaire was administered weekly. Nine patients completed the study; 8 patients discontinued the treatment. Baseline pain intensity was 6.2 +/- 3.1 on the McGill Pain Questionnaire scale (0-10 range). Low doses (4-8 mg) of tiagabine reduced pain symptoms by 16-38%, improving surface pain (37.5%), skin sensitivity (32.8%), burning (38.6%), cold (25.4%) and pain sharpness (29%; p <0.03). Dull and deep pain did not improve. Quantitative sensory testing abnormalities diminished with treatment (p <0.02). Autonomic test results did not change. This pilot study evaluated the potential of tiagabine hydrochloride (Gabitril) in treatment of painful sensory neuropathy. Pain symptoms and quantitative sensory test results improved with treatment, especially at low doses of tiagabine (4-8 mg). Higher doses (12-16 mg) were associated with increased number of adverse events. Tiagabine may have potential benefits for treatment of painful neuropathy; however, assessment of its efficacy in a larger study is needed.
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PMID:Treatment of painful sensory neuropathy with tiagabine: a pilot study. 1179 16

Older generation antiepileptic drugs like Phenobarbital (Luminal), carbamazepine (Tegretol), phenytoin (Dilantin), and valproic acid (Depakote) have several shortcomings such as suboptimal response rates, significant adverse effects, several drug interactions, and a narrow therapeutic index. New antiepileptic drugs have been developed in the last decade to overcome some of these problems. These newer generation antiepileptics like felbamate (Felbatol), gabapentin (Neurontin), lamotrigine (Lamictal), levetiracetam (Keppra), oxcarbazepine (Trileptal), tiagabine (Gabitril), topiramate (Topamax), and zonisamide (Zonegran) have better tolerability profiles, low interaction potential, and significantly less enzyme inducing or inhibiting properties. As the use of antiepileptic drugs has expanded to include treatment of neuropathic pain, newer side effects have been reported. In addition to the common side effects of antiepileptic drugs, like dizziness, drowsiness, and mental slowing; other side effects like weight gain, metabolic acidosis, nephrolithiasis, angle closure glaucoma, skin rash, hepatotoxicity, colitis, and movement and behavioral disorders, to name a few, have been brought to our attention. This review is an attempt to highlight the features and incidences of some of these side effects.
Pain Pract 2004 Sep
PMID:Side effects of antiepileptics--a review. 1717 1