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An in-depth look into Flualprazolam

Flualprazolam is categorized as a novel benzodiazepine, Even Though its synthesis and Action

Have been described in the literature. Benzodiazepines are neural system
depressants. Novel benzodiazepines, frequently pirated from early drug discovery or pharmaceutical

Studies, have appeared on novel and illegal drug markets in latest years. These substances have

Caused adverse events, such as death, as described in the literature. Flualprazolam is structurally comparable to the traditional benzodiazepine alprazolam, a Schedule IV substance from the USA, and also the novel benzodiazepines flunitrazolam, clonazolam, and flubromazolam.

Flualprazolam was added to the NPS library database at March 2019. Through data mining of datafiles obtained in 2018, flualprazolam was identified in a blood sample. In June 2019, flualprazolam was identified in two additional blood samples through sample mining,

A procedure our laboratory developed for real-time detection and detection of NPS.

General Pharmacology

Routes of administration and dosage

Oral doses of 0.125mg — two mg are described in the published literature (Zawilska and Wojcieszak, 2019, Moosmann and Auwarter, 2018). A report in the on-line forum described doses in this range (0.25 mg — 0.5mg) (Reddit, 2019).

Pharmacokinetics

Is a triazolo-benzodiazepine, which differ from benzodiazepines
Like diazepam, and offer unique differences in pharmacological activity and at timecourse of effect (Garzone and Kroboth, 1989). Information about flualprazolam

Pharmacokinetics is scarce info is available for the structurally comparable 1,4-Triazolobenzodiazepines, alprazolam and triazolam. The printed literature demonstrates

That alprazolam and triazolam have high affinities for the benzodiazepine receptor (Garzone and Kroboth, 1989). Peak alprazolam and triazolam concentrations occur within an hour, representing absorption. The volume of distribution of alprazolam and Triazolam is about 1L and the two are bound to plasma proteins; alprazolam (70 percent ) and triazolam (~ 85%). The mean elimination half-life to get alprazolam in adults

Ranges from 9.5 to 12 hours (Garzone and Kroboth, 1989). For alprazolam elimination,

Liver disease prolongs elimination, but failure doesn’t. Onset of action for
flualprazolam is reported to be 10-30 minute with a duration 6-14h (Zawilska and Wojcieszak,
2019). A single report by an on-line forum suggest an onset of action in
Approximately 30-40minutes (Reddit, 2019).

The 1,4-triazolo ring prevents the oxidative metabolic process of the classical benzodiazepines

Which results in formation of active metabolites with long elimination half-lives.

Pharmacodynamics

Limited descriptions of the effects of flualpraozlam are available. One on-line report described sedition and impairment from this dose reported (Reddit, 2019). It’d be estimated that these effects are made in a comparable way to other benzodiazepines, which is via modulation of the GABA reception, potentiating the action of GABA, leading to sedative effects and handicap.

The only studies describing severe and pre-clinical effects of alprazolam were reported from the patent application (Hester, 1976). Preclinical studies described in the patient application indicate that flualprazolam demonstrated sedative effects on the Chimney Test

With intraperitoneal (IP) doses of 0.09 mg/kg; along with a sedative dose at the Dish test of 0.15 ng/kg with IP administration, and 0.045mg/kg when administered orally.

Sedative/tranquilizer effects were also seen on the Pedestal Test at doses IP of 0.20 mg/kg or oral doses of 0.9mg/kg. Flualprazolam was shown to be protective from smoking induced convulsions and tonic extensor matches and passing at doses of 0.04mg/kg (oral), also had muscle relaxant or antispasmodic activity against the effects of strychnine administration at 1mg/kg.

Toxicology

No studies were identified that had examined the acute toxicity or chronic
health effects of flualprazolam or its metabolites in animals.

The UN Office on Drugs and Crime (UNODC) Early Caution Advisory on NPS
Toxicology Portal (Tox-Portal), an on-line tool established in 2017 that gathers data on toxicology and harm related to the use of NPS, comprised 42 reports that included flualprazolam. These reports predominantly represented people aged 15-24 years old (26 of 42 cases), and predominantly male (37 of 42 cases). Forty of the 42 cases were reported in the USA with just two cases from Finland. In five cases the samples were documented to have been collected post mortem and 21 were noted to be ante-mortem samples. The rest of the cases had no additional information on context. Most cases given an indication of the contribution or effect of a material on the case. In five cases flualprazolam was determined to be causal to the event (that’s, a higher probability of causality). In 22 cases flualprazolam was documented to possess a chance of causality, in one case the contribution of flualprazolam was assessed to have a low probability of causality. There were 12 further cases the contribution of the flualprazolam was documented to be undetermined.

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