Anticonvulsants ; pharmacology ; therapeutic use ; Epilepsy ; drug therapy ; genetics ; Humans ; Pharmacogenetics

Epilepsy is a common and disabling disorder with a protracted course. Medical therapy is the keystone for the treatment of epilepsy. Most patients with more than one well-documented non-provoked seizures require prophylactic antiepileptic treatment. Those with underlying structural abnormalities or other risk factors should probably be treated after a single seizure. The goal of treatment should be the maintenance of normal life, avoidance of seizure-related brain or physical injuries including sudden unexpected death of epileptic patients. Nearly two-thirds of patients are well controlled on a single antiepileptic drug. If the first or second monotherapy improves control of seizure but does not produce seizure freedom, an antiepileptic drug with a different or multiple mechanisms can be added. Strategies for the choice of initial antiepileptic drug or combining drugs should involve the assessment of individual patient-related factors, including seizure types and epilepsy syndrome and pharmacology of antiepileptic drugs. The impact of adverse effects of antiepileptic drugs should not be underestimated. The introduction of many new antiepileptic drugs has provided a wider choice for patients and doctors.
Anticonvulsants* ; Brain ; Epilepsy ; Freedom ; Humans ; Pharmacology ; Risk Factors ; Seizures

The East Asian scorpion Buthus martensii Karsch (BmK) is one of the classical traditional Chinese medicines for treating epilepsy for over a thousand years. Neurotoxins purified from BmK venom are considered as the main active ingredients, acting on membrane ion channels. Voltage-gated sodium channels (VGSCs) play a crucial role in the occurrence of epilepsy, which make them become important drug targets for epilepsy. Long chain toxins of BmK, composed of 60-70 amino acid residues, could specifically recognize VGSCs. Among them, α-like neurotoxins, binding to the receptor site-3 of VGSC, induce epilepsy in rodents and can be used to establish seizure models. The β or β-like neurotoxins, binding to the receptor site-4 of VGSC, have significant anticonvulsant effects in epileptic models. This review aims to illuminate the anticonvulsant/convulsant effects of BmK polypeptides by acting on VGSCs, and provide potential frameworks for the anti-epileptic drug-design.
Animals ; Anticonvulsants/therapeutic use* ; Neurotoxins/pharmacology* ; Scorpion Venoms/pharmacology* ; Scorpions/chemistry* ; Voltage-Gated Sodium Channels

No abstract available.
Animal ; Animal Welfare ; Anticonvulsants/*pharmacology ; Drug Design ; Drug Interactions ; Epilepsy/*drug therapy ; Human ; Mice ; Pharmacokinetics ; Rats

ATP Binding Cassette Transporter, Sub-Family B ; metabolism ; Animals ; Anticonvulsants ; pharmacology ; Brain ; drug effects ; metabolism ; Rats

Tetrahydroisoquinoline alkaloids distributed widely in the nature and some have a broad application in clinic. More attention has been paid in recent years on this type of alkaloid, owing to the diverse range of biological activities exhibited by these alkaloids and the discovery of new functional mechanisms and molecular targets underlying these activities. This article summarized the recent advances in the biological activities and functional mechanism of tetrahydroisoquinoline, which included the activities such as antitumor, antibiotic, antivirus, anti-inflammatory, anticoagulation, bronchodilation, and the action on central nervous system, with the purpose of providing some ideas in the study of biological activity of this type of alkaloid and in the search for lead-compound and rational drug design.
Animals ; Anti-Inflammatory Agents ; pharmacology ; Anticonvulsants ; pharmacology ; Antifungal Agents ; pharmacology ; Antineoplastic Agents ; pharmacology ; Antiviral Agents ; pharmacology ; Bronchodilator Agents ; pharmacology ; Central Nervous System Agents ; pharmacology ; Fibrinolytic Agents ; pharmacology ; Humans ; Neuroprotective Agents ; pharmacology ; Tetrahydroisoquinolines ; chemical synthesis ; chemistry ; pharmacology

BACKGROUNDCurcumin can reduce the severity of seizures induced by kainate acid (KA), but the role of curcumin in amygdaloid kindled models is still unknown. This study aimed to explore the effect of curcumin on the development of kindling in amygdaloid kindled rats.

METHODSWith an amygdaloid kindled Sprague-Dawley (SD) rat model and an electrophysiological method, different doses of curcumin (10 mgxkg(-1)xd(-1) and 30 mgxkg(-1)xd(-1) as low dose groups, 100 mgxkg(-1)xd(-1) and 300 mgxkg(-1)xd(-1) as high dose groups) were administrated intraperitoneally during the whole kindling days, by comparison with the course of kindling, afterdischarge (AD) thresholds and the number of ADs to reach the stages of class I to V seizures in the rats between control and experimental groups. One-way or two-way ANOVA and Fisher's least significant difference post hoc test were used for statistical analyses.

RESULTSCurcumin (both 100 mgxkg(-1)xd(-1) and 300 mgxkg(-1)xd(-1)) significantly inhibited the behavioral seizure development in the (19.80 +/- 2.25) and (21.70 +/- 2.21) stimulations respectively required to reach the kindled state. Rats treated with 100 mgxkg(-1)xd(-1) curcumin 30 minutes before kindling stimulation showed an obvious increase in the stimulation current intensity required to evoke AD from (703.3 +/- 85.9) microA to (960.0 +/- 116.5) microA during the progression to class V seizures. Rats treated with 300 mgxkg(-1)xd(-1) curcumin showed a significant increase in the stimulation current intensity required to evoke AD from (735.0 +/- 65.2) microA to (867.0 +/- 93.4) microA during the progression to class V seizures. Rats treated with 300 mgxkg(-1)xd(-1) curcumin required much more evoked ADs to reach the stage of class both IV (as (199.83 +/- 12.47) seconds) and V seizures (as (210.66 +/- 10.68) seconds). Rats treated with 100 mgxkg(-1)xd(-1) curcumin required much more evoked ADs to reach the stage of class V seizures (as (219.56 +/- 18.24) seconds).

CONCLUSIONOur study suggests that curcumin has a potential antiepileptogenic effect on kindling-induced epileptogenesis.

Amygdala ; physiopathology ; Animals ; Anticonvulsants ; pharmacology ; Curcumin ; pharmacology ; Kindling, Neurologic ; drug effects ; Male ; Rats ; Rats, Sprague-Dawley ; Seizures

OBJECTIVETo study the sedative, hypnotic and antiseizure effects of the compound preparation of gardenia oil and jujube seed oil in mice and investigate the interaction of the two drugs in this preparation.

METHODSThe compound preparation was administered intragastrically in mice, whose spontaneous activity was observed along with their tolerance of the preparation after long-term administration. The hypnotic effect of the compound was assessed by investigating the changes in the pentobarbital sodium-induced sleeping. The compound was tested for its antiseizure effect in mice with pentetrazole-induced clonic and tonic convulsion. Diazepam was used as the standard control in all experiments.

RESULTSThe jujube seed oil, the gardenia oil and their compound all inhibited spontaneous activities of the mice. Compared with diazepam, the compound showed slow action in producing the sedative effect, which increased gradually with prolonged drug administration without obvious drug tolerance responses. The compound and the two oils all showed synergistic action with pentobarbital sodium in inducing sleeping of the mice. Prescription study showed that the compound produced stronger sedative and hypnotic effects than either of the oils. The two oils and the compound did not show significant antiseizure effects in mice.

CONCLUSIONThe compound of jujube seed oil and gardenia oil has sedative and hypnotic effects in mice, and the two oils in the compound show obvious synergistic effect.

Animals ; Anticonvulsants ; pharmacology ; Drugs, Chinese Herbal ; pharmacology ; Gardenia ; chemistry ; Hypnotics and Sedatives ; pharmacology ; Mice ; Mice, Inbred ICR ; Plant Oils ; pharmacology ; Seeds ; chemistry ; Ziziphus ; chemistry

OBJECTIVETo study the screening of essential oils of Skimmia laureola leaves (SLO) for acute toxicity, antinociceptive, antipyretic and anticonvulsant activities in various animal models.

METHODSSLO were extracted using modified Clevenger type apparatus. Acute toxicity test was used in mice to observe its safety level. Antinociceptive activity of SLO was evaluated in acetic acid induced writhing and hot plate tests. Yeast induced hyperthermic mice and pentylenetetrazole induced convulsive mice were used for the assessment of its antipyretic and anticonvulsant profile respectively.

RESULTSSubstantial safety was observed for SLO in acute toxicity test. SLO showed a high significant activity in acetic acid induced writhing test in a dose dependent manner with maximum pain attenuation of 68.48% at 200 mg/kg i.p. However, it did not produce any relief in thermal induced pain at test doses. When challenged against pyrexia evoked by yeast, SLO manifested marked amelioration in hyperthermic mice, dose dependently. Maximum anti-hyperthermic activity (75%) was observed at 200 mg/kg i.p. after 4 h of drug administration. Nevertheless, SLO had no effect on seizures control and mortality caused by pentylenetetrazole.

CONCLUSIONSIn vivo studies of SLO showed prominent antinociceptive and antipyretic activities with ample safety profile and thus provided pharmacological base for the traditional uses of the plant in various painful conditions and pyrexia. Additional detail studies are required to ascertain its clinical application.

Analgesics ; pharmacology ; Animals ; Anticonvulsants ; pharmacology ; Antipyretics ; pharmacology ; Body Temperature ; drug effects ; Female ; Male ; Mice ; Oils, Volatile ; pharmacology ; toxicity ; Plant Leaves ; chemistry ; toxicity ; Rutaceae ; chemistry ; Toxicity Tests

This article is brief review of study on alpha-asarone after 1996. The summary mainly includes the dosage forms, pharmacokinetics, bioavailability, pharmacological effects, toxicology and clinical uses during the past ten years.
Acorus ; chemistry ; Animals ; Anisoles ; administration & dosage ; isolation & purification ; pharmacology ; Anticonvulsants ; pharmacology ; Antineoplastic Agents, Phytogenic ; pharmacology ; Expectorants ; pharmacology ; Humans ; Phytotherapy ; Plants, Medicinal ; chemistry