Anti-convulsant

Neuronal excitotoxicity AEA levels are elevated in the hippocampus of mice treated with kainic acid. 2-AG levels are elevated in rats treated with pilocarpine These are two animal models of epileptic seizures, where the endocannabinoids play an anti-convulsant and protective function Inhibitors of cellular re-uptake... 

Dragunow, M (1986) Adenosine, the brain s natural anti-convulsant. Trends Pharmacol. Sci. 15 128-129. 

Kent, AP and Webster, RA (1983) The evaluation of different types of anti-convulsant drug activity against leptazol-induced epileptogenic activity in the anaesthetised rat. Brit. J. Pharmac. 78 553-559. 

This peripheral activity may be a rational basis for the use of systemic local anaesthetics in neuropathic states since ectopic activity in damaged nerves has been shown to be highly sensitive to systemic sodium channel blockers. This too is probably part of the basis for the analgesic effects of established effective anti-convulsants that block sodium channels such as carbamazepine, although central actions are important and may even predominate. The precise actions of excitability blockers therefore remains hazy as does any clear basis for the effectiveness of antidepressants and other adrenergic agents in the treatment of neuropathic pain as both central and peripheral actions, including sympathetic effects are possible. 

After decontamination by emesis or lavage, patients should be carefully monitored for alterations in liver and kidney function, and treated symptomatically if necesseray. Seizures can be treated with anti-convulsant drugs. Because the toxin produces a deficiency of y-amino-butyric acid (GABA), specific treatment with pyridoxine (vitamin Bg) has been recommended. 

N-Alkylamino carbazoles (e.g., 494 and 495) possess significant anti-convulsant and diuretic activity. Introduction of an aminopropyl chain at the N-atom seems to enhance the anti-convulsant activity in combination with methoxy groups at positions 2, 3, and 4, or a chlorine atom at the C-2 and C-3 positions (458). 

In experiments done many years ago on epileptic patients who were undergoing brain surgery, small brain biopsies were taken at operation. The concentration of anti-convulsant drug was measured in both the brain tissue and in the plasma from simultaneously-withdrawn venous blood. For the drugs phenobarbitone and phenytoin, a linear correlation was observed between plasma and brain concentrations. This suggested that plasma concentrations of anti-convulsants could reflect brain concentrations, and therefore, presumably concentrations at the receptor sites within the brain substance. 

The second problem is that of drugs, which can saturate their elimination mechanisms at plasma concentrations, which are within the therapeutic range. Perhaps the most important example is that of the anti-convulsant, phenytoin. 

Rifampicin, the anti-convulsants phenytoin, phe-nobarbitone and carbamazepine, and the steroid dex-amethasone, are amongst the best recognized inducers of enzyme function, and their action nearly... 

You are called to the Emergency Department where a known epileptic is having recurrent grand mal seizures. A friend, who has come with him, says he knows he has not taken any of his anti-convulsant medication for at least a week, as he has been travelling and he had left the drugs behind. 

Tiagabine is an anti-convulsive medication also used in the treatment for panic disorder as are a few other anticonvulsants. It does appear to operate as a selective GABA reuptake inhibitor. Tiagabine s most common side effects include confusion, difficulty speaking clearly/stuttering and mild sedation. 

Anti-convulsant activity. Methanol (50%) extract of the dried leaf, administered to mice, was active vs leptazol-induced convulsions . Ethanol (70%) extract of the fresh leaf, administered intraperito-neally to mice of both sexes at variable doses, was active vs metrazole- and strychnine-induced convulsions . Anti-estrogenic effect. Aqueous extract of the dried leaf smoke, administered to female adults at a concentration of 25.0 pL/plate, was active on granulosa cells. Results significant atp < 0.001 level . 

Walson, P.D. (1994) Role of therapeutic drug monitoring (TDM) in pediatric anti-convulsant drug dosing. Brain Dev 16 23-26. 

Coulam CB, Annegers JF. Do anti-convulsants reduce the efficacy of oral contraceptives Epilepsia 1979 20 519-525. 

Tatulian, L., Delmas, P., Abogadie, F. C., Brown, D. A. Activation of expressed KCNQ potassium currents and native neuronal M-type potassium currents by the anti-convulsant drug retigabine, The Journal of Neuroscience 2001, 21, 5535-5545. 

Wickenden, A. D., Yu, W., Zou, A., Jegla, T., Wagoner, P. K. Retigabine, a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels, Molecular Pharmacology 2000, 58, 591-600. 

Montanine alkaloids are members of the alkaloids of the plant family of Amarylli-daceae. They represent a relatively small class of compounds with the typical methanomorphanthridine skeleton exhibiting some anxiolytic, anti-depressive and anti-convulsive activities [135, 136]. The total syntheses of the natural (-)-mon-tanine enantiomers are only mentioned, not described, here (for these (—(-enantiomers see, e.g. literature cited in [137]). 

Cramers et al5 described high resolution gas chromatography for the quantitative determination of underivatized anti-convulsant drugs with support coated open tubular columns. 

The anti-convulsant phensuximide 37, being an imide, comes from a dicarboxylic acid 38 with a 1,4-relationship between the two carbonyl groups. Changing one to cyanide we get back to cinnamic acid 40 as the available starting material. 

With the PTZ procedure, pro- or anti-convulsant activity is indicated both by the frequency of the convulsant events (clonic convulsions, tonic convulsions, deaths) and by their latency of occurrence. Latency is the measure which most clearly identifies pro-convulsant activity, whereas frequency is the measure most useful for detecting anticonvulsant activity. A statistical problem arises when the test substance completely blocks convulsions in some of the animals. 

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