INTRODUCTIONMexazolam is indicated for the management of anxiety with or without psychoneurotic conditions. In adult patients, the recommended daily dosage of mexazolam is 1-3 mg, administered three times daily. The objective of this article is to review the available information on the benzodiazepine (BZD) mexazolam and its clinical utility in treating patients with anxiety.METHODSThe PubMed database was searched using the keyword "mexazolam" with no date or language restrictions applied to the search. As only 11 papers were retrieved, some previously published manuscripts of interest known by the authors (not indexed on PubMed) have been added for completeness. Relevant information was selected for inclusion by the authors.RESULTSA number of early studies demonstrated the ability of mexazolam to reduce anxiety symptoms with few side effects in patients with disorders associated with anxiety. Following on from this preliminary evidence, controlled studies directly comparing mexazolam with other BZDs showed that the drug is more effective than bromazepam and oxazolam, and is at least as effective as alprazolam. A larger, multicenter, phase IV study also showed that mexazolam 2 or 3 mg/day rapidly improved Hamilton Anxiety Rating Scale scores and substantially reduced the frequency and severity of numerous somatic anxiety symptoms in patients with anxiety disorders. With regard to safety, the clinical evidence indicates that mexazolam is generally well tolerated, with a low incidence of drowsiness and sedation. Furthermore, the lack of psychomotor or cognitive performance impairment following mexazolam administration may lead to better treatment compliance.CONCLUSIONThe available clinical evidence suggests that mexazolam is an effective therapeutic option for the management of anxiety. However, larger, well-controlled clinical trials are needed to directly compare and contrast mexazolam's efficacy and safety with other BZDs.

01 Jan 2014·Mutation Research/Fundamental and Molecular Mechanisms of Mutagenesis

Comparison of the biological effects of MMS and Me-lex, a minor groove methylating agent: Clarifying the role of N3-methyladenine

Article

Author: Foggetti, Giorgia ; Monti, Paola ; Menichini, Paola ; Gold, Barry ; Fronza, Gilberto ; Inga, Alberto

N3-methyladenine (3-mA), generated by the reaction of methylating agents with DNA, is considered a highly toxic but weakly mutagenic lesion. However, due to its intrinsic instability, some of the biological effects of the adduct can result from the formation of the corresponding depurination product [an apurinic (AP)-site]. Previously, we exploited Me-lex, i.e. {1-methyl-4-[1-methyl-4-(3-methoxysulfonylpropanamido)pyrrole-2-carboxamido]-pyrrole-2 carboxamido}propane, a minor groove equilibrium binder with selectivity for A/T rich sequences that efficiently reacts with DNA to afford 3-mA as the dominant product, to probe the biology of this lesion. Using human p53 cDNA as a target in a yeast system, a weak increase in mutagenicity was observed in the absence of Mag1 (3-methyladenine-DNA glycosylase 1, mag1), the enzyme devoted to remove 3-mA from DNA. Moreover, a significant increase in mutagenicity occurred in the absence of the enzymes involved in the repair of AP-sites (AP endonucleases 1 and 2, apn1apn2). Since methyl methanesulfonate (MMS) has been extensively used to explore the biological effects of 3-mA, even though it produces 3-mA in low relative yield, we compared the toxicity and mutagenicity induced by MMS and Me-lex in yeast. A mutagenesis reporter plasmid was damaged in vitro by MMS and then transformed into wild-type and Translesion Synthesis (TLS) Polζ (REV3) and Polη (RAD30) deficient strains. Furthermore, a mag1rad30 double mutant strain was constructed and transformed with the DNA plasmid damaged in vitro by Me-lex. The results confirm the important role of Polζ in the mutagenic bypass of MMS and Me-lex induced lesions, with Polη contributing only towards the bypass of Me-lex induced lesions, mainly in an error-free way. Previous and present results point towards the involvement of AP-sites, derived from the depurination of 3-mA, in the observed toxicity and mutagenicity.

01 Jan 2012·Iranian journal of pharmaceutical research : IJPRQ4 · MEDICINE

Enhanced Controlled Transdermal Delivery of Mexazolam Using Ethylene-vinyl Acetate.

Q4 · MEDICINE

Article

Author: Cheong Weon Cho ; Sang Chul Shin

Repeated oral administration of mexazolam, an anti-anxiety agent, may cause adverse effects such as gastric disturbance, drowsiness, and ataxia due to transiently high blood levels. Transdermal administration would avoid the systemic side effects and gastric disorders after oral administration. We have developed a matrix using ethylene-vinyl acetate (EVA), a heat-processible and flexible material, for transdermal delivery of mexazolam. Drug solubility was highest at 40% PEG-400 volume fraction. The release and permeation profiles through the rat skin were determined for 24 h using a modified Keshary-Chien diffusion cell. The drug release was increased by increasing the concentration with a linear relationship between the release rate and the square root of loading dose. Increasing temperature increased drug release from the EVA matrix. The activation energy (Ea), which was measured from a slope of log P versus 1000/T plot, was 8.64 Kcal/mol for a 1.5% loading dose. To reduce the brittleness and increase the pore of the EVA matrix, diffrent plasticizers were used. Among the plasticizers, including the citrates or the phthalate groups, diethyl phthalate showed the highest effect on the release of mexazolam. To increase the skin permeation of mexazolam from the EVA matrix, enhancers such as the fatty acids, the pyrrolidones, the propylene glycol derivatives, the glycerides, and the non-ionic surfactants were added to the EVA matrix, respectively, and skin permeation was evaluated using a modified Keshary-Chien diffusion cell fitted with intact excised rat skin. Among the several enhancers used, N-methyl-2-pyrrolidone showed the best enhancement factor. In conclusion, enhanced transdermal delivery of mexazolam through an EVA matrix containing plasticizer and a permeation enhancer could be useful in the development of a transdermal drug delivery system.

100 Deals associated with Mexazolam

External Link

KEGG	Wiki	ATC	Drug Bank
D01316	Mexazolam	N03AE N05CD N05BA	DB15489

R&D Status

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Neurotic Disorders	JP	Alfresa Pharma Corp.	21 Sep 1983

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis