Anticonvulsants, anti-epileptics

BACKGROUND: Carvone is a monoterpene ketone in mint plants and some Mediterranean spices. In Carvone, chemical compounds occur in two enantiomers, S (+) carvone and R (-) carvone. These two enantiomeric forms of carvone are identical in terms of their physical and chemical characteristics and only differ in terms of their rotatory power based on their smell. Caraway has also been utilized to treat newborns' flatulent colic and to treat adults' anxious cardiac- gastric symptoms, spasmodic gastrointestinal complaints, flatulence, irritated stomach, indigestion, lack of appetite, and dyspepsia...

BACKGROUND: Epilepsy is one of the most common in all age groups and disabling neurologic disorders around the world. OBJECTIVES: This systematic review was to explore whether berberine (BBR) has any anti-seizure or anti-epileptic effects and also reviewed this possible mechanism. METHODS: The EMBASE, Scopus, Cochrane Library, PubMed, and Web of Science databases were searched before Sep 2023. All types of studies that investigated the effects of BBR on epilepsy or chemical-induced seizures were eligible for inclusion...

Epilepsy represents a prevalent neurological disorder in the population, and the existing antiepileptic drugs (AEDs) often fail to adequately control seizures. Inflammation is recognized as a pivotal factor in the pathophysiology of epilepsy. Luteolin, a natural flavonoid extract, possesses anti-inflammatory properties and exhibits promising neuroprotective activity. Nevertheless, the precise molecular mechanisms underlying the antiepileptic effects of luteolin remain elusive. In this study, we established a rat model of epilepsy using pentylenetetrazole (PTZ) to induce seizures...

UNLABELLED: In our continuous effort to develop novel antiepileptic drug, a new series of nipecotic acid derivatives having1,3,4-thiadiazole nucleus were designed and synthesized. This study aims to improve the lipophilicity of nipecotic acid by attaching some lipophilic anchors like thiadiazole and substituted aryl acid derivatives. In our previous study, we noticed that the N-substituted oxadiazole derivative of nipecotic acid exhibited significant antiepileptic activity in the rodent model...

Patients with epilepsy require improved medications. Purinergic receptors were identified as late as 1976 and are slowly emerging as potential drug targets for the discovery of antiseizure medications. While compounds interacting with these receptors have been approved for use as medicines (e.g., gefapixant for cough) and continue to be explored for a number of diseases (e.g., pain, cancer), there have been no purinergic receptor antagonists that have been advanced for epilepsy. There are very few studies on the channel conducting receptors, P2X3 and P2X4, that suggest their possible role in seizure generation or control...

Quinidine has been used as an anticonvulsant to treat patients with KCNT1-related epilepsy by targeting gain-of-function KCNT1 pathogenic mutant variants. However, the detailed mechanism underlying quinidine's blockade against KCNT1 (Slack) remains elusive. Here, we report a functional and physical coupling of the voltage-gated sodium channel NaV 1.6 and Slack. NaV 1.6 binds to and highly sensitizes Slack to quinidine blockade. Homozygous knockout of NaV 1.6 reduces the sensitivity of native sodium-activated potassium currents to quinidine blockade...

INTRODUCTION: Ziziphus mauritiana, sometimes called Indian jujube or Ber, belongs to the Rhamnaceae group of plants. The aqueous and ethanolic Ziziphus mauritiana formulations were shown to have analgesic, antipyretic, potent analgesic, anti-inflammatory, and anti-emetic properties. AIM & OBJECTIVES: The aim of this study is to investigate the sedative and anticonvulsant activities of Ziziphus mauritiana extract by governing 200 and 400 mg/kg body weight orally...

INTRODUCTION: Brain metastasis (BM) prognosis is incredibly poor and is often associated with considerable morbidity. Seizures are commonly present in these patients, and their biopsychosocial impact can be dangerous. The use of Anti-epileptic drugs (AED) as primary prophylaxis remains controversial. This systematic review and meta-analysis aim to evaluate the efficacy of AED prophylaxis in patients with brain metastasis. METHODS: MEDLINE via PubMed, Web of Science, EMBASE, and Cochrane were searched for articles pertinent to AED prophylaxis use in patients with BM...

Vigabatrin is an anti-epileptic drug that inhibits the enzyme γ-aminobutyric acid (GABA)-transaminase. The anticonvulsant effect of vigabatrin involves increasing GABA levels and attenuating glutamate-glutamine cycling. Vigabatrin indications include infantile spasms and refractory focal seizures. Despite having a significant role in paediatric epileptology, vigabatrin has adverse effects, such as retinal toxicity, in up to 30% of patients after 1 year of use and brain abnormalities on magnetic resonance imaging (MRI)...

A member of the Valerianacae family, Nardostachys jatamansi is the smallest, most primitive, perennial, dwarf, hairy, rhizomatous, herbaceous species. It has an enlarged antiquity of usage as ayurvedic medicine, homeopathic medicine, ethnomedicine, and the Indian system of medicine, and is now used in the modern medicine industry. In the ayurvedic medical system, the rhizomes of the plant are used as a bitter tonic, stimulant, antispasmodic, epileptic treatment, and for hysteria. Pharmacological reports on Nardostachys jatamansi revealed its antifungal activity, hepatoprotective activity, central nervous system activity, anticonvulsant activity, neuroprotective activity, antiparkinson's activity, antioxidant activity, antidiabetic activity, tranquilizing activity, antiestrogenic activity furthermore, Jatamansone has also been linked to anti-hypertensive, anti-arrhythmic, anti-asthmatic, nematicidal, and antibacterial effects...

ETHNOPHARMACOLOGICAL RELEVANCE: Epilepsy is a neurological disorder that presents with recurring and spontaneous seizures. It is prevalent worldwide, affecting up to 65 million people, with 80% of cases found in lower-income countries. Medicinal plants are commonly employed for managing and treating epilepsy and convulsions due to their unique therapeutic properties. With increasing research and clinical application, medicinal plants are gaining attention globally due to their potent therapeutic effects and fewer side effects...

Propofol is used for sedation, anxiolysis, anesthesia induction, and as an anticonvulsant. In cases of refractory status epilepticus (RSE), propofol is more efficient than barbiturates. We present a case of a 3-year-old female with RSE who developed propofol-related infusion syndrome (PRIS) despite low dosage after failed attempts with multiple anti-epileptic drips and bolus therapies. Careful consideration must be made before initiating propofol administration for RSE. We discuss our PRIS treatment approach with extracorporeal membrane oxygenation, therapeutic plasma exchange, and continuous renal replacement therapy leading to our patient recovering to baseline and being discharged home from the hospital...

Oxadiazoles and thiadiazoles are malleable heterocycles that have recently generated major interest in the field of medicinal chemistry. Compounds based on these moieties have versatile biological applications such as anticonvulsant, anticancer, antidiabetic, and antioxidant agents. Due to the versatile nature and stability of the oxadiazole and thiadiazole nucleus, medicinal chemists have changed the structural elements of the ring in numerous ways. These compounds have shown significant anticonvulsant effects, demonstrating their potential in the management of epileptic disorders...

BACKGROUND: Status epilepticus (SE) is a type of epileptic activity characterized by a failure of the inhibitory mechanisms that limit seizures, which are mainly regulated by the GABAergic system. This imbalance increases glutamatergic neurotransmission and consequently produces epileptic activity. It is also associated with oxidative stress due to an imbalance between reactive oxygen species (ROS) and antioxidant defences. Unfortunately, long-term treatment with anti-epileptic drugs (AEDs) may produce hepatotoxicity, nephrotoxicity, and haematological alterations...

Status epilepticus (SE) is described as continuous and self-sustaining seizures, which triggers hippocampal neurodegeneration, inflammation, and gliosis. N-formyl peptide receptor (FPR) has been associated with inflammatory process. N-formyl-methionyl-leucyl-phenylalanine (fMLP) peptide plays an anti-inflammatory role, mediated by the activation of G-protein-coupled FPR. Here, we evaluated the influence of fMLP peptides on the behavior of limbic seizures, memory consolidation, and hippocampal neurodegeneration process...

Cranioplasty, specifically a repair of the skull defect resulting from a previous decompressive craniectomy, is a relatively simple procedure associated with a minimal rate of complications. Even though seizures are seen in up to 30% of the patients postoperatively, status epilepticus is not commonly described. Cerebral oedema, ischaemia and neuro-inflammation have been reported as putative causes of seizures in this population. Here, we report a case of refractory status epilepticus unresponsive to standard anti-epileptic and anaesthetic agents...

Currently, prolong use of standard anti-epileptics may cause tolerance and ineffective for about 30% of epileptic patients. Medicinal plants provide an attractive therapeutic effect in preventing and treating seizures in traditional and folk medicine. In this study, we investigate the antiepileptic effects of PTAT decoction on acute and chronic seizure models in mice and explore the potential mechanisms. PTAT decoction dose-dependently protected mice against MES and PTZ induced seizure. Meanwhile, it decreased the seizure severity and reduced seizure-caused anxious behavior in the PTZ-kindling mice, suggesting a significant antiepileptic activity and anxiolytic/anxiogenic potential...

Somatostatin interneurons exhibited anti-epileptic activity. As a result, somatostatin agonists appear to be a promising target for antiepileptic drug development (AEDs). In this regard, we investigated the effects of octreotide, a somatostatin analog, on pentylenetetrazol (PTZ)-induced seizures in male Wistar rats. Animals were given octreotide at doses of 50 or 100µg/kg for seven days. The anxiolytic effects of octreotide were then evaluated using open field and elevated plus-maze tests. Following that, mice were intraperitoneally given a single convulsive dosage of PTZ (60mg/kg) and then monitored for 30minutes for symptoms of seizures...

OBJECTIVES: In October 2020 and March 2021, the Federal Drug Agency classified lamotrigine as class IB antiarrhythmic, announcing an increased risk of heart rhythm problems. We sought to investigate the nature of the arrhythmia signal with lamotrigine use compared to anticonvulsants with sodium and non-sodium blocking mechanisms. METHODS: This retrospective pharmacovigilance case-non-case study used disproportionality analysis to detect signals of adverse reaction of interest reported with lamotrigine to the FDA adverse event reporting system between 1998 and 2022...

The efficacy of many anti-epileptic drugs, including phenytoin (PHT), is reduced by plasma protein binding (PPB) that sequesters therapeutically active drug molecules within the bloodstream. An increase in systemic dose elevates the risk of drug side effects, which demands an alternative technique to increase the unbound concentration of PHT in a region-specific manner. We present a low-intensity focused ultrasound (FUS) technique that locally enhances the efficacy of PHT by transiently disrupting its binding to albumin...