Benzodiazepines

Bill S. Tchachito, Third-year professional student

https://en.wikipedia.org/wiki/Benzodiazepine#/media/File:Benzodiazepine.svg

Slang terms:

Alprazolam: Xannies, Bars, Brick, Planks, Upjohn Clonazepam: K, K-pin

Diazepam: Yellow V’s, Blue V’s, Tranqs, Old joes, Howard, Downers

The history of benzodiazepines started in 1955 when a German chemist with the name of Hoffman-La Roche. He accidentally identified the first benzodiazepine and entitled it to chlordiazepoxide (Librium). The history of benzodiazepine started in 1955 when a German chemist with the name of Hoffman-La Roche. He accidentally identified the first benzodiazepine and entitled it to chlordiazepoxide (Librium). The problem of abuse was pointed out long ago by many Scientifics, but the problem became important when in 1982 a British scientist named Malcolm directed a study of these drugs to create a change in the brain that led people to become more dependent on the drug. For some unknown reason, the documentary was sealed secret in the UK and was revealed in 2014.

1,4 benzodiazepines exert effect for the acute treatment of generalized anxiety disorder and panic disorder through binding to the benzodiazepine site of gamma-aminobutyric acid-A (GABA) receptors in the brain and enhances GABA-mediated synaptic inhibition.

Plasma levels of alprazolam increase proportionally to the dose over the range of 0.5 to 3.0 mg.

Absorption

Following oral administration, the peak plasma concentration of alprazolam (Cmax) occurs in 1 to 2 hours post-dose.

Distribution

Alprazolam is 80% bound to human serum protein, and albumin accounts for the majority of the binding.

Elimination

The mean plasma elimination half-life (T1/2) of alprazolam is approximately 11.2 hours (range: 6.3 to 26.9 hours) in healthy adults.

Metabolism

Alprazolam is extensively metabolized in humans, primarily by cytochrome P450 3A4 (CYP3A4), to 2 major active metabolites in the plasma: 4-hydroxyalprazolam and α-hydroxyalprazolam. The plasma circulation levels of the two active metabolites are less than 4% of the parent. The reported relative potencies in benzodiazepine receptor binding experiments and animal models of induced seizure inhibition are 0.20 and 0.66, respectively, for 4-hydroxyalprazolam and α-hydroxyalprazolam. The low concentrations and low potencies of 4-hydroxyalprazolam and α-hydroxyalprazolam indicate that they are unlikely to contribute much to the effects of alprazolam. Benzophenone derived from alprazolam is also found in humans. Its half-life appears to be similar to that of alprazolam.

Excretion: Alprazolam and its metabolites are excreted primarily in the urine.

Since benzodiazepines are primarily metabolized by the enzyme CYP3A4 drugs that will inhibit or increase the activity of the enzyme will impact the efficacy of a drug, such as ketoconazole, itraconazole, nefazodone, fluvoxamine, erythromycin, cimetidine, fluoxetine, carbamazepine, oral contraceptives, sertraline, warfarin, ritonavir, imipramine. There could be interactions with some natural products and drinks such as St John’s wort and grapefruit juice.

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Common signs and symptoms of overdose are primarily sedative-hypnotic effects and are a result of CNS and respiratory depression and may include sedation, dizziness, amnesia, ataxia, slurred speech, lethargy, problems with coordination, and respiratory difficulties. Acute, single-drug ingestions are typically mild and exhibit reversible symptomatology. Severe toxicity, albeit uncommon and more often associated with co-ingestions, may result in coma, hypotension, hypothermia, and respiratory depression and failure.

All benzodiazepines are currently categorized as schedule IV drugs in the United States. This means that a form of legal identification is required when picking up the medication. Contrary to other typical drugs, for which the length of the prescription is one year, a prescription for a benzodiazepine is only valid for six months. All prescriptions must include: date prescription was issued, prescriber’s signature, patient’s full name, medication name, strength, dosage form, quantity prescribed, direction of use, prescriber’s name, address, and registration number.

There are no major monitoring parameters when taking a benzodiazepine. A toxicology screen might be performed in cases of an overdose to see how much drug and presence of metabolites are in the bloodstream.

There are numerous medications available on the market or even on the black market that have therapeutic effects, but some people abuse the drugs to the point where they become dependent on them. This often leads to the development of legislation to halt the abuse. This is highlighted in the benzodiazepine class of pharmaceuticals. These drugs have a wide range of therapeutic applications, including the treatment of seizures, migraines, depression, and other medical disorders. If people could only use drugs when necessary and not just because there is access to them, I believe the phenomena of drug abuse would shrink and the regulations governing its availability would change. I believe benzodiazepines are great medicines for treating a wide range of medical ailments. Users should exercise greater caution when using them, and manufacturers and healthcare professionals should do more to educate the public about the dangers of these medications and their potential for addiction.

~Tbist

A Brief History of Benzodiazepines. Benzodiazepine Information Coalition. https://www.benzoinfo.com/a-brief-historyof-benzodiazepines/

A Brief History of Benzodiazepines. Benzodiazepine Information Coalition. Accessed October 11, 2022. https://www.benzoinfo.com/a-brief-history-of-benzodiazepines/

Popular Street Names for Benzodiazepines (Benzos). Published October 8, 2020. Accessed October 11, 2022. https://floridarecoverygroup.com/street-names-for-benzodiazepine/

DailyMed - XANAX- alprazolam tablet. Nih.gov. Published 2018. Accessed October 11, 2022. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=388e249d-b9b6-44c3-9f8f-880eced0239f

Purdue Web Authentication. Purdue.edu. Published 2015. Accessed October 14, 2022. https://online-lexi-com.ezproxy.lib.purdue.edu/lco/action/doc/retrieve/docid/310/1253640.

Alprazolam: MedlinePlus Drug Information. medlineplus.gov. Published May 15, 2021. Accessed October 13, 2022. https://medlineplus.gov/druginfo/meds/a684001.html