Benzodiazepines (BZD) represents an important class of compounds of a wide range of pharmacological effects and therapeutic uses. This project discusses the classification, mechanism of action, major pharmacological effects and adverse reactions of BZD. It also reports on the chemical synthesis and important physicochemical properties of BZD. The influence of the chemical structure’s modification of BZD upon drug's potency, physicochemical characteristics, pharmacokinetics and drug metabolism were elucidated. A problem of drug abuse of BZD either alone or in combination with other central nervous system (CNS) depressants was reviewed. Forensic analysis of BZD in biological samples for screening and confirmation of BZD abusers in forensic settings was demonstrated and the most important analytical techniques used for screening and measurement of BZD in forensic laboratory were described. In this project, selected gas chromatography-mass spectrometry (GC-MS) and Liquid Chromatography- Tandem Mass Spectrometry (LC-MS/MS) spectra of diazepam (MS lab, Prof M. Abdel-Hamid) for confirmation and quantitation of diazepam are presented. 1. Introduction: BZD are a group of chemically synthetic compounds that were firstly synthesized in late fifties. BZD share a common chemical structure features and their importance comes with relation to their effect on the CNS. BZD are known best to work by depressing the central nervous system and show an important role being used for several purposes such as, hypnotics, sedatives, antiepileptics and muscle relaxants. The emergence of benzodiazepines seemed to be very helpful due to their potent effect and low toxicity compared to barbiturates. Although being relatively safe compounds, drug depend... ... middle of paper ... ...ad/201105_import/20110509050.pdf 20. Fitzgerald, R., Rexin, D., & Herold, D. (1994). Detecting benzodiazepines: Immunoassays compared with negative chemical ionization gas chromatography/mass spectrometry. CLINICAL CHEMISTRY, 40(3), 373-380. 21. Boeck, G., samyn, N., Morris, M., & Wood, M. National Institute of Criminalistics and Criminology (NICC), Toxicology (2002). Development of a rapid and sensitive method for the quantification of benzodiazepines in human plasma by LC-MS/MS. Manchester, UK: MICROMASS. 22. Jones, C., Wlans, F., Martinez, L., & Merritt, G. (1989). Benzodiazepines identified by capillary gas chromatography-mass spectrometry, with specific ion screening used to detect benzophenone derivatives. Clinical Chemistry, 35(7), 1394-1398. Figure 3. Structure activity relationships of 1,4-benzodiazepines, Adapted from (6)
There are specific benzodiazepine receptors in the nervous system that mostly surrounds the cerebral cortex, cerebellum and limbic system. Barbiturates have their own binding sites and modulate the chloride channel. They increase the duration of this channel, while benzodiazepines increase the frequency. Also barbiturates are less selective than benzodiazepines on the CNS. Barbiturates are positive allosteric modulation of GABAA receptors. These drugs bind to this receptor at the beta end, which are distinct from GABA and benzodiazepine binding sites as well as block the AMPA receptor. Benzodiazepines increase the efficiency of GABA, which reduces neurons excitability, allowing functions in the brain to go in a calming effect due to less communication between neurons. Conduction of chloride ions across the cell membrane increases when the benzodiazepines bind to the GABA receptor. Benzodiazepines have many advantages over barbiturates making it favored in the pharmaceutical industry for hypnotics. The drugs have a much higher therapeutic index than barbiturates, making it a much safer drug to use due to a greater safety margin. Rem-type sleep is crucial for feeling rested after a sleep. Barbiturates suppress this greatly while Benzodiazepines doesn’t nearly as much. Both of these drugs assist with relaxation and tranquility but may also impair motor function. A possible side effect with patients who use barbiturate at a moderate dose is becoming hostile as well as being in a state of pleasurable intoxication. The danger of taking a high dose of barbiturates is severe as i...
Valium (Diazepam) is an anti anxiety association (benzodiazepine), used basically for transient alleviation of moderate to sensible uneasiness. Data innovation would likely likewise be used to mend signs and manifestations of great fermented drinks drink appropriations, to aid control epilepsy, or to simplicity ligament fits.
...ossible adverse interactions between an antidepressant medication and the substances a patient is abusing (such as the potential for increased sedation or intoxication).” (p 29).
Psychoactive drugs are classified into five different groups depending on how they affect the brain. In this essay I will be looking at three of these groups: stimulants, depressants and hallucinogens and how they exert influence on neural processing.
Zolpidem is a nonbenzodiazepine hypnotic in the imidazopyridine class of drug; meaning that the drug is an agonist to the GABAa receptors (Source 7). Zolpidem was introduced in the early 1900s and has helped to push insomnia treatments forward. The nonbenzodiazepine Zolpide...
Benzodiazepines, such as diazepam, achieves its pharmacodynamic effects by ultimately increasing the effect of the major inhibitory neurotransmitter GABA on GABAA receptors. The main roles of GABA include regulating neuronal excitability and regulation of muscle tone. Diazepam, as a positive allosteric modulator of GABAA receptors, binds and forms a receptor-drug complex which promotes the binding of GABA.
The Similarity Analysis Module in Spartan’14 was used the calculate the similarity score for each of the benzodiazepines compared to the benzodiazepine active site on the chloride receptor. Of the benzodiazepines studied, it was found that lorazepam has the best fit for the active site because it had the highest similarity score compared to the pharmacophore and the lowest number of collisions with the wall of the active site. AutoDock Vina was also used to calculate the binding affinity of each benzodiazepine with the active site on the chloride receptor. It was found that diazepam, lorazepam and midazolam all have the lowest binding affinity of -9.8 kcal/mol and therefore are more likely to bind to the active site. Combining these results
In America, the U.S. Food and Drug Administration is investigating Olanzapine pamoate following the demise of two persons following an injection of the drug.
Benzodiazepine or know as benzo on the street. Benzos effect the central nervous system by slowing down the ...
In the early 1900s MDMA was developed in Germany to synthesize other pharmaceuticals. Virtually dormant until 1953, MDMA was researched--and used--by a former pesticide chemist named Alexander Shulgin. Shulgin was on a quest for the ideal psychoactive drug but was frustrated by the regulations and required trials mandated before a medication could be produced; he quit working on this drug because of these restrictions(“History of Ecstasy (MDMA)”). Some psychiartrics began using MDMA during the 1970’s as a psychotherapeutic tool, even the the drug had never recieved formal clinical trials or go...
Anonymous. "Prescription Drugs: Their Use and Abuse." Scholastic Scope. 20 Feb. 2006: IA. eLibrary. Web. 07 Dec. 2013.
In the history of mankind, the hallucinogens have probably been the most important of the narcotics. Their fantastic effects made the...
Therapy can mean many different things from relaxation therapy to group therapy or even seeing a psychologist. Cognitive-behavioral therapy is one of the most effective treatment plans for patients dealing with anxiety. Cognitive-behavioral therapy deals with the patient’s problems, and helping them find different ways to cope with their situations. They help change negative thoughts into more supportive thoughts and answers. If a patient can realize what activates their anxiety they will be able to recognize when they need to talk to someone or even take their medications as prescribed. Promoting resilience is another way to help with patients cope with anxiety. “Resilience is the quality of being hardy or stress resistant.” (Karen M. Burke, 2011) Nurses or even family members can help older patients with anxiety by supporting their ADL’s, and that is encouraging resilience. The most common medications used to treat anxiety are benzodiazepines and sedative hypnotics. Benzodiazepines have a rapid onset and help react to the central nervous system. The most common side effects of benzodiazepines are sedation, weakness, lethargy, dizziness, and a decreased in organization. The most common benzodiazepines prescribed are Xanax, klonopin, valium, and Ativan. Sedative-hypnotic agents have a more sedative effect on the mind and help treat insomnia. Side effects include sedation, drowsiness, and dizziness. Most
There have been hundreds of cases involving various hallucinogens ranging from petty theft to murder. Why a few of these individuals are able to attain a lesser charge, be acquitted, or be placed into a psychiatric ward may be better understood with background of how these drugs impact the human brain and body.
Another goal of behavioral pharmacology is to develop animal behavioral models to screen chemical compounds with therapeutic potentials. Scientists who are studying this field typically use small animals to study psychotherapeutic drugs such as antipsychotics, antidepressants and anxiolytics, and drugs of abuse such as nicotine, cocaine, methamphetamine. [6]