The new generation of anti-epileptic drugs

Patsalos, Philip N.

doi:10.1517/14728214.4.1.87

Cited by 9 publications

(5 citation statements)

References 38 publications

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“…During the past decade, several new drugs such as lamotrigine, oxcarbazepine, felbamate, gabapentin, topiramate, fospenytoin sodium, tiagabine, zonisamide, and levetiracetam have been approved [1]. Even though new anticonvulsants are already in clinical use, some type of seizures are not adequately treated and they only produce satisfactory seizure control in 60 -70% of patients with current therapy.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Some Oxime Ether Derivatives of 1‐(2‐Naphthyl)‐2‐(1,2,4‐triazol‐1‐yl)ethanone and Their Anticonvulsant and Antimicrobial Activities

Karakurt

Aytemir

Stables

et al. 2006

Archiv der Pharmazie

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In this study, oxime and oxime ether derivatives of [1-(2-naphthyl)-2-(1,2,4-triazol-1-yl)ethanone] were prepared as potential anticonvulsant and antimicrobial compounds. The oxime was synthesized by the reaction of ketone and hydroxylamine hydrochloride. O-Alkylation of the oxime by various alkyl halides gave the oxime ether derivatives. Anticonvulsant activity of the compounds was determined by maximal electroshock and subcutaneous metrazole tests in mice and rats according to procedures of the Anticonvulsant Screening Program of National Institutes of Health. Neurotoxicity was determined by the rotorod test in mice and the positional sense test, gait and stance test in rats. In addition to anticonvulsant tests, all compounds were also evaluated against the following microorganisms: S. aureus, E. coli, P. aeruginosa, E. faecalis, C. albicans, C. parapsilosis, and C. krusei using microdilution broth method for possible antibacterial and antifungal activities. Although most of the O-alkyl substituted oxime ethers exhibited both anticonvulsant and antimicrobial activities, the O-arylalkyl substituted compounds were found to be inactive in both screening paradigms.

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Section: Introductionmentioning

confidence: 99%

Synthesis of Some Oxime Ether Derivatives of 1‐(2‐Naphthyl)‐2‐(1,2,4‐triazol‐1‐yl)ethanone and Their Anticonvulsant and Antimicrobial Activities

Karakurt

Aytemir

Stables

et al. 2006

Archiv der Pharmazie

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“…The life‐time chance of developing epilepsy is 3 – 5% ( Sander & Shorvon, 1987 ). Even though globally, since 1989, nine new antiepileptic drugs have been licensed for clinical use ( Patsalos, 1999 ), they have had little impact on the prognosis of refractory epilepsy and therefore there is still a need for new antiepileptic drugs with improved risk/benefit ratios ( Marson & Chadwick, 2001 ) and with simple pharmacokinetics to aid clinical use ( Patsalos, 2000 ).…”

Section: Introductionmentioning

confidence: 99%

A microdialysis study of the novel antiepileptic drug levetiracetam: extracellular pharmacokinetics and effect on taurine in rat brain

Tong

Patsalos

2001

British J Pharmacology

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1 Using a rat model which allows serial blood sampling and concurrent brain microdialysis sampling, we have investigated the temporal kinetic inter-relationship of levetiracetam in serum and brain extracellular¯uid (frontal cortex and hippocampus) following systemic administration of levetiracetam, a new antiepileptic drug. Concurrent extracellular amino acid concentrations were also determined. 2 After administration (40 or 80 mg kg 71 ), levetiracetam rapidly appeared in both serum (T max , 0.4 ± 0.7 h) and extracellular¯uid (T max , 2.0 ± 2.5 h) and concentrations rose linearly and dosedependently, suggesting that transport across the blood-brain barrier is rapid and not rate-limiting. The serum free fraction (free/total serum concentration ratio; mean+s.e.mean range 0.93 ± 1.05) was independent of concentration and con®rms that levetiracetam is not bound to blood proteins. 3 The kinetic pro®les for the hippocampus and frontal cortex were indistinguishable suggesting that levetiracetam distribution in the brain is not brain region speci®c. However, t 1/2 values were signi®cantly larger than those for serum (mean range, 3.0 ± 3.3 h vs 2.1 ± 2.3 h) and concentrations did not attain equilibrium with respect to serum. 4 Levetiracetam (80 mg kg 71 ) was associated with a signi®cant reduction in taurine in the hippocampus and frontal cortex. Other amino acids were una ected by levetiracetam. 5 Levetiracetam readily and rapidly enters the brain without regional speci®city. Its prolonged e ux from and slow equilibration within the brain may explain, in part, its long duration of action. The concurrent changes in taurine may contribute to its mechanism of action.

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“…Earlier study has shown that valproate is highly bound to plasma proteins and readily displaces other bound anticonvulsant drugs. 21 Diazepam and valproate have been reported to have a synergistic effect. 22 Number of mice protected with combination of phenobarbitone with diazepam (4) were less than the total of number of mice protected with phenobarbitone alone (2) and number of mice protected with diazepam alone (3), though the protective effect seem to be antagonistic (combination showed 66.66% protection), p value was not significant (p>0.05) when compared with control group.…”

Section: Interactions Seen Between Anti-epileptics With Diazepammentioning

confidence: 99%

Study of potential drug-drug interactions between benzodiazepines and four commonly used antiepileptic drugs in mice

Shah

Rana

Patel

2014

Int J Basic Clin Pharmacol

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The new generation of anti-epileptic drugs

Cited by 9 publications

References 38 publications

Synthesis of Some Oxime Ether Derivatives of 1‐(2‐Naphthyl)‐2‐(1,2,4‐triazol‐1‐yl)ethanone and Their Anticonvulsant and Antimicrobial Activities

Synthesis of Some Oxime Ether Derivatives of 1‐(2‐Naphthyl)‐2‐(1,2,4‐triazol‐1‐yl)ethanone and Their Anticonvulsant and Antimicrobial Activities

A microdialysis study of the novel antiepileptic drug levetiracetam: extracellular pharmacokinetics and effect on taurine in rat brain

Study of potential drug-drug interactions between benzodiazepines and four commonly used antiepileptic drugs in mice

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