In 2011, Germany, Norway and the United Kingdom were the first countries to report the emergence of another designer, BZD, etizolam. Furthermore, the risk of polydrug use involving BZDs and opioids (both traditional and synthetic ones) are furtherly intensified by NPS belonging to these new/designer BZDs . Tolerance and dependence may occur shortly after consumption has started, which requires dose increase and may trigger drug-seeking behaviours 1, 3. Furthermore, BZDs may be classified according to their chemical structure and designer BZDs are mainly classified as either 1,4-benzodiazepines (a structure shared by most ‘traditional’ BZDs), triazolo-BZDs, or thienotriazolodiazepines (Table 1) . Plasma half-life (t½) represents the hours required for the concentration of the drug in the body to be reduced to half of the maximum concentration.
Report Of A Massive Oral Overdose
By analogy to traditional BZDs, the desired effects may include sociability, muscle relaxation, sleep-inducing and anxiolytic effects, as a reducer of chronic pain, and nervousness. Between 2012 and 2019, new compounds classified as ‘designer BZDs’ started to be distributed by online retailers, mostly labelled as ‘research chemicals’ . Most designer BZDs possess a liver metabolism, primarily by oxidative metabolism mediated by the CYP450 family, mainly CYP3A4 . These compounds are sold as tablets, powder, pellets, capsules or blotters, and recently liquids under their own names, at very affordable prices 37, 211, 212. However, beside these BZDs, there are also completely new and recently synthetised NPS BZDs (i.e., pyrazolam, flubromazepam, etc.), some of them were previously research trial compounds whose development did not proceed to clinical use 79, 210. A low dose is mg, a typical dose is mg whilst a strong effect is experienced with mg or more .
Of these, 11 underwent SFST, 5 had roadside drug tests, 3 CTI, while 1 driver refused to perform SFST, and symptoms of impairment were provided by the officer’s observations. There also are 19 DUID and a drug offense cases included in Table 1. Patients exhibited both motor and functional impairment and depressant effects. Three subjects were admitted to the ED after ingesting illicit phenazepam purchased on the Internet. It is metabolized to the active metabolite 3-hydroxyphenazepam by different isoforms of CYP450 114,135. Phenazepam was reported to EMCDDA in July 2011 by Germany and UK.
Duration Of Effects
- 3-Hydroxyphenazepam is an active metabolite of both phenazepam (7-bromo-5-(2-chlorophenyl)-1,3-dihydro-1,4-benzodiazepin-2-one) and cinazepam 120, 121.
- However, in a recent report by WHO ECDD on flualprazolam, more than 25 deaths with confirmed exposure to flualprazolam and around 30 non-fatal poisonings with suspected exposure have been reported so far .
- The onset of symptomatology happens in minutes, and effects may last 5-10 hours and after-effects for hours .
- Check out our blog posts and resource links for the latest information on substance abuse.
- There are several anecdotal reports from psychonaut fora which describe it as “relatively fast sublingual onset” which gives it a strong ‘anti-panic effect’ .
At lower doses, BZDs may cause drowsiness, fatigue and lethargy; whilst, at higher doses motor coordination disorders, mood swings, dizziness and sometimes euphoria have been reported . Furthermore, there have been sporadic reports of the use of these designer BZDs as either adulterants or diluents in heroin or other synthetic opioids or cannabinoids, with consequent respiratory depression documented 8, 213, 214. In fact, some of them are also sold on the illicit drug market as counterfeit forms of other traditional/pharmaceutical BZDs (e.g., diazepam, alprazolam, etc.), which may increase the risk of unintentional overdose and intoxication 9, 10, 170. Symptomatology happens minutes after oral intake, effects may last 3-6 hours and after-effects for 1-8 hours after administration .
What Are The Phenazepam Withdrawal Symptoms?
Side effects include dizziness, loss of coordination and drowsiness, along with anterograde amnesia which can be quite pronounced at high doses. However, abusing phenazepam can lead to severe adverse effects and be fatal. It's occasionally used as a recreational drug in the U.S. for its euphoric effects. However, illegally purchasing prescription drugs is extremely dangerous and never recommended. Some people may experience adverse effects when using the drug, even if it's legally prescribed.
Phenazepam and nimetazepam were the first DBZD identified in Europe on the internet in 2007, followed by etizolam in 2011 . However, they are illicit, with a relatively short life cycle in the NPS market, the majority of DBZD have not undergone clinical trials and our knowledge of their pharmacokinetics and toxicity is lacking and limited to self-reported experiences 43,44. Slight alterations of the BZD core at different positions generated a large number of designer compounds, mainly 1,4-benzodiazepines, triazolobenzodiazepines and thienotriazolodiazepines. These new psychoactive substances (NPS) have the same chemical structure as legal BZD, with an aromatic ring fused to a 1,4-diazepine ring and an aryl group in position R5 34,35,36,37. Due to controlled neuronal inhibition and lower CNS depression risk, BZD rapidly replaced older medications such as barbiturates, meprobamate and chloral hydrate, becoming the most prescribed drug class in the world during the 1970s 11,12. Etizolam, flualprazolam flubromazolam and phenazepam were implicated in the majority of adverse-events, drug offenses and deaths.
Where To Buy Phenazepam Online
To date, correlations between dose and response, duration of action, metabolism, and onset of action are still poorly understood, making it harder for users to accurately dose the compound they purchased, increasing the prospect of potential intoxication. The patients may not be aware of the identity or concentration of DBZD in a drug product before suffering symptoms of intoxication . Clinicians should be asking patients about substance abuse including NPS and DBZD during routine preventive care and ED visits. For most NPS placed under international control, the number of reports decreased rapidly the year after the scheduling decision . DBZD are widely available on the Internet in different forms, i.e., blotters, liquids, pills, powders and tablets, and sold at low prices .
The drug is ten times stronger than diazepam, with higher doses sometimes prescribed for severe anxiety or epileptic seizures. The recommended dose generally comes in 0.5 mg to 1 mg tablets. However, the drug's powerful anti-anxiety and muscle relaxant properties make it twice as likely to be abused. When illegally obtained, it's often combined with other drugs, like synthetic cannabinoid products. When overdosed, phenazepam is extremely dangerous and potentially fatal. In some cases, people have taken what they thought was a typical dose of Valium but was actually a high dose of phenazepam.
Bentazepam was firstly seized by the Swedish Police, on 3 March 2014, in Borlänge in a sample of 6 white round tablets. Bentazepam is not currently controlled under the 1971 United Nations Convention on Psychotropic Substances or the 1961 Single Convention on Narcotic Drugs. Its peak plasma concentration is reached within 1-3 hours after oral administration and it has a t ½ of approximately 3.3 hours . It exerts anxiolytic, anticonvulsant, sedative and muscle relaxant effects 203, 204.
Fonazepam is structurally related to the internationally controlled substance flunitrazepam (aka ‘Rohypnol®’), from which it differs only due to the absence of an N-methyl group . Symptomatology occurs minutes after oral and/or sublingual intake, with effects lasting hours and after-effects for 2-24 hours . The 3-hydroxyphenazepam molecule was first identified in a collected sample of white powder by the Medical Centre in the University of Freiburg, Institute of Forensic Medicine, Forensic Toxicology Department on 19 October 2015 69, 110. 3-Hydroxyphenazepam is not currently controlled under the 1971 United Nations Convention on Psychotropic Substances or the 1961 Single Convention on Narcotic Drugs. 3-hydroxyphenazepam appears to be pharmacologically active with some 5- to 10-fold higher potency than diazepam, probably due to the bromine atom in the molecule .
Phenazepam as well as nimetazepam were also detected a few years earlier in Europe in 2007 (UNODC 2013) in seizures by customs and law enforcement agencies in Europe, but at the time, there had been no cases of detection in human samples, either clinical or post-mortem. Before 2007, benzodiazepines were diverted from both legal sources (false prescriptions, pharmacies) and also illicitly manufactured, but the illicit use of benzodiazepines were benzodiazepines that were available for prescription in that country (Ibañez, Levi-Minzi, Rigg, & Mooss, 2013). The source for abused benzodiazepines has changed over time. This has risen to 36 recently because of the emergence of NPS benzodiazepines (International Narcotics Control Board (INCB) 2016). Because of their recognized abuse, in 1971, 33 benzodiazepines were placed under control by the UN Convention on Psychotropic Substances. The abuse of benzodiazepines was recognized quickly after their release onto the market in 1961.
Side Effects
He had previously ingested a large quantity of etizolam tablets. In the third ED admission, diclazepam was the sole drug reported. On 1 September 2014, the UK Focal Point reported that the substance was confirmed after analysis of a blue seized tablet .
- Illegally, phenazepam is sold as a fine white powder or liquid.
- The maximum safe dosage of phenazepam is 10 mg per day.7
- BZDs are a class of drugs widely prescribed for the short-term treatment of anxiety, epilepsy, muscle spasm, alcohol withdrawal and insomnia.
- However, abusing phenazepam can lead to severe adverse effects and be fatal.
Phenazepam Uses, Side Effects, & Risk Of Addiction
The tablets were white in colour with the markings “D/CD” and weighed 0.35 grams on average. Adinazolam was first identified in a sample of 1 gram of white powder collected by the Medical Centre in the Institute of Forensic Medicine at the University of Freiburg (Germany) on 5 September 2015. Adinazolam is not currently controlled under the 1971 United Nations Convention on Psychotropic Substances or the 1961 Single Convention on Narcotic Drugs. A human study comparing the subjective effects and abuse potential of adinazolam (30 mg and 50 mg) with diazepam, lorazepam and a placebo showed that adinazolam causes the most “mental and physical sedation” and the greatest “mental unpleasantness” .
Why Is Phenazepam Abused?
Methylclonazepam showed relatively potent muscle relaxant and extremely potent anti-pentetrazol convulsing action as compared to diazepam, even though it has been reported to be approximately 5-times more potent than diazepam in impairing rotarod performance in mice . Behavioural effects of methyl clonazepam were compared with diazepam in rats and mice . Methylclonazepam is a 1,4-BZD, structurally related to clonazepam, being its N-methyl derivative, and to internationally controlled flunitrazepam, from which it differs due to the substitution of the fluorine atom present in flunitrazepam with a chlorine atom . The substance was analytically confirmed by the Swedish National Forensic Centre using GC-MS, GC-IRD, LC-HRMS and NMR . Thionordazepam was first identified in 2 grams of pale-yellow powder seized by Swedish Customs in Stockholm on 20 June 2017. Thionordazepam is not currently controlled under the 1971 United Nations Convention on Psychotropic Substances or the 1961 Single Convention on Narcotic Drugs.
Bentazepam is a thienodiazepine that differs from the previously notified thienodiazepines (i.e., etizolam, metizolam and fluclotizolam) due to the presence of cyclohexane fused to the thiophene instead of a triazole . Clobromazolam was first identified in 20 white capsules containing white powder seized by Swedish Police in Luleå on 11 March 2016 . Clobromazolam is not currently controlled under the 1971 United Nations Convention on Psychotropic Substances or the 1961 Single Convention on Narcotic Drugs. The presence of this molecule in the material seized in relation to an ‘anesthesia robbery’ case has recently been reported . However, in a recent report by WHO ECDD on flualprazolam, more than 25 deaths with confirmed exposure to flualprazolam and around 30 non-fatal poisonings with suspected exposure have been reported so far . The substance was analytically confirmed using GC-MS, HPLC-TOF, IC, FTIR-ATR, GC-(MS)-IR condensed phase at the Slovenian National Forensic Laboratory and by NMR at the Faculty of Chemistry and Chemical technology, University of Ljubljana .
Non-prohibited benzodiazepines are introduced onto the global drug market and scheduled as rapidly as possible by international authorities. The rising use of designer benzodiazepines (DBZD) is a cat-and-mouse game between organized crime and law enforcement. It has quieting and entrancing properties and has recognized in unlawful tablets.2 This thing is gotten ready for research and criminological applications. Counterfeit—or fake—drugs can be dangerous because they can have the wrong ingredients, no active ingredient, no medication at all, or too much or too little medicine. According to the official investigation report, effects of phenazepam on pilot Pavel Gruzin may have contributed to errors that caused the crash of Crossair Flight 498.
The onset of symptomatology happens in minutes, and effects may last 5-10 hours and after-effects for hours . There are several anecdotal reports from psychonaut fora, which described mostly an “anxiolytic and muscle relaxant effect … with a low tolerance shows hypnotic effects. The onset of symptomatology occurs after minutes, effects may last 2-5 hours and after-effects for 1-16 hours . A seizure of 105 tablets was reported shortly afterwards (8 September 2015) by the Swedish Focal point, following a seizure by the Swedish police in Gottenburg. The same study notes that despite reports of “unpleasantness” the participants of the study rated the substance of high “street value”, capable of producing “physical and mental highness” according to the Addiction Research Criteria Inventory (ARCI) . Ataxia, dysarthria, weakness, diminished reflexes, confusion, coma and a paradoxical excitement in children have been reported, in addition to signs of overdose .
