Category and Chemical Name of Diazepam - Term Paper Example

Key Words: 7-chloro 3-dihydro methyl-5-phenyl-2H 4-benzodiazepin2-one, Derivatives, Valium, half-life, Metabolite N-Desmethyldiazepam, Valium (diazepam) History of Diazepam (Valium) An Austrian chemist by the name Dr. Leo Sternbach who was working in a pharmaceutical company of Hoffmann-La Roche discovered Benzodiazepines in 1954 (Shorter 99). The company’s laboratories submitted the drug for pharmacological evaluation whereby they unveiled it was more superior compared to other drugs in the same category. The first Benzodiazepine got its patent in 1959 and the manufacturers introduced it to the world as Librium in 1960 (Shorter 99). The drugs capabilities raised interest and a lot of testing was done on related compounds hence leading to the introduction of diazepam (Valium) in 1963. The capability of valium proved to be three times more powerful and had greater muscle relaxing power when compared to Librium. Further studies of benzodiazepines are always underway and many other derivatives are currently in the market. These derivatives are such as, Nitrazean, released in 1965, Flurazepan introduced in 1973 as well as Apprazolam of 1980s. Currently, manufacturers have developed over 2000 diverse benzodiazepines and more than three dozen of its derivatives are present in the market (Shorter 99). Category and Chemical Name Diazepam (Valium) falls under the benzodiazepine category and its chemical name is 7-chloro-1, 3-dihydro-1-methyl-5-phenyl-2H-1, 4-benzodiazepin2-one (Guy 368). It has an empirical formula of C16H13ClN2O and a molecular weight of 284.75. Valium is a crystalline compound that ranges from colourless to light yellow and is insoluble in water. Valium has been classified under anticonvulsants and sedatives. Administration and Mechanism of Action Physicians administer Diazepam (Valium) orally as tablets that contain 2, 5 or 10mg of diazepam. Other than this active ingredient, the tablets also contain inactive ingredients such as anhydrous lactose, corn and pregelatinized starch as well as calcium stearate. In addition, the 5mg tablets contain the dye FD and C Yellow (number 6 as) well as D and C Yellow (number 10). The 10mg mg tablets also contain a dye, which is the FD and C Blue (number 1). Valium 2mg tablets do not contain any dye. High prescription levels specifically for 20mg IVP, encompasses giving 5-10mg slow IVP at 5mg/minute (Guy 368). Titration of the drug is useful to seizure activity or until sedation occurs for synchronized cardiovascular muscles. For the 10mg, physicians administer the drug one time via a syringe or an auto injector for active seizures. Maximum administration for 10mg IVP or PR when dealing with children involves administering 0.2mg/kg slowly and IVP at 1mg/minute or 0.5mg/kg PR. Pedriatrics administer IV doses by titration to suppress seizure activity until sedation occurs for synchronized cardioversions. The physicians may repeat 0.25mg/kg PR in 15 minutes one time only, not to exceed maximum of 0.75mg/kg or total of 10mg (Guy 368). Valium has high affinity for the GABA binding sites. Valium acts on the brain by affecting the neurotransmitter gamma-amino butyric acid. Neuron-transmitters facilitate communication between brain cells and GABA works by decreasing the brain activity (Lehne 254). Pharmacology After oral administration, the body absorbs 90% of diazepam and for it to achieve maximum plasma concentration; it takes 1-1.5 hours. If one takes the drug and accompanies it with a heavy meal, he or she may delay or decrease the absorption of the drug. Diazepam binds highly to plasma proteins with up to 98%. Diazepam and its different metabolites are evident in breast milk and their concentrations are about one tenth of those present in maternal plasma. This is because diazepam and its metabolites have the ability to cross the barriers present in the placenta as well as the blood brain. In young males, the amount of distribution is 0.7-1.0L/kg at steady state. The distribution phase of diazepam lasts for about 1 hour and may range to up to 3hours or more. During metabolism, CYP3A4 and 2C19 de methylate Valium to the active metabolite desmethyldiazepam and it undergoes hydroxylation by CYP3A4 to temazepam. Temazepam and N-desmethyldiazepam further go through metabolism to Oxazepam. Temazepam and Oxazepam face elimination by glucuronidation (Tindall, William, John & Mona 288). After the distribution phase and metabolism, there is a prolonged trial elimination phase having half-life up to two days. This is terminal elimination of the dynamic Metabolite N-Desmethyldiazepam, which persists for approximately 100 hours. Diazepam together with other own metabolites encounter excretion though urine as their glucuronide conjugates. In youths, the elimination rate of diazepam is from 20 to almost 30 mL/min (Tindall, William, John & Mona 288). Upon high dosages, Valium accumulates and the terminal elimination period is prolonged. Indications Its indication is for the regulation of anxiety complications besides sometimes being effective for the short-lived ease of the anxiety symptoms (Guy 368). However, anxiety or tension of everyday life does not demand treatment with Valium. Valium is useful in the relief of acute agitation, panic, and hallucinations that accompany acute alcohol withdrawals (Guy 368). Valium is also useful to ease skeletal muscle tensions. This includes inflammation of muscle or joints or second art to trauma. In addition, it is useful in the healing spasticity caused by upper neuron disorders as well the stiff-man syndrome. Valium administrated orally has also been useful in convulsive disorders. Clinical studies have not yet established the effectiveness of long-term use of Diazepam (Valium). Contraindications Valium has contraindications like in patients who have a history of hypersensitivity to diazepam. Due to lack of enough clinical experience in paediatric patients of less than 6 months old, Valium also faces contraindications. Moreover, Valium faces contraindications in patients with severe respiratory complications, sleep apnea syndrome besides chronic hepatic sufficiency (Guy 368). In addition, as much as Valium is useful in open-angle glaucoma patients receiving appropriate therapy, physicians contraindicate Valium in narrow-angle glaucoma. Negative possibilities in the use of Valium Negative possibilities that accompany use of Valium include when physicians use it during labour and child delivery (Tindall, William, John & Mona 289). High singe doses have chances of producing irregularities in the children’s heart rate, poor sucking, hypothermia as well as mild respiratory complications in the neonates. The drug will also have adverse effects if administered to children because the enzyme system necessary in the breakdown the drug has not yet fully developed in their bodies. This is especially the case in premature infants. Breastfeeding patients should not receive Valium because it will pass into breast milk. Women with childbearing potential should not use diazepam unless the clinical situation warrants protection to the foetus. If they get pregnant during therapy, they should consider talking to their physicians so that they can be advised whether to discontinue the drug usage. Valium has the capability for abuse and people should not use it without prescription (King, Tekoa, & Brucker 212). During the first days of Valium therapy, a patient experiences side effect such as sleepiness and lack of co-ordination. If the drug is used for a long time, the body develops tolerance for it hence; they will need large doses to achieve the same initial effects. Since part of Valium’s function is lowering the brain’s activities, ones a person stops, the brain’s activity can go out of control leading to seizures and other harmful consequences. Anyone who has plans of discontinuing Valium therapy should first speak with a physician. If someone abuses Valium at high doses, it can cause unconsciousness and death (King, Tekoa, & Brucker, 212). Beneficial Uses of Valium Valium is a depressant for the Central Nervous System and is in a category of drugs that slow normal brain functioning. Diazepam (Valium) exerts anxiolytic, muscle relaxant, sedative, anti-convulsing and amnesic effects. In addition, valium relaxes skeletal muscles and decreases patients recall (Guy 368). Valium increases the activity of GABA hence producing a drowsy or calming effect hence it becomes of benefit to those suffering from anxiety or sleep disorders (Lehne 254). In higher doses, valium is also useful as a general anaesthetic. In my personal opinion, as much as Valium is a beneficial drug, it has major side effects and hence people should not consume them without prescription. Women who are pregnant or those planning to get pregnant should not use this drug unless they have undergone clinical examination and harm to foetus has been ruled out. Children are also a sensitive populace when it comes to the use of Valium hence the consultation of a physician is necessary. Work Cited Guy, Jeffrey S. Pharmacology for the Prehospital Professional. , 2011. Print. King, Tekoa L. & Mary C. Brucker. Pharmacology for Womens Health. Sudbury, Mass: Jones and Bartlett Publishers, 2011. Print. Lehne, Richard A. Pharmacology for Nursing Care. St. Louis, Mo: Elsevier/Saunders, 2013. Print. Shorter, Edward. Before Prozac: The Troubled History of Mood Disorders in Psychiatry. Oxford: Oxford University Press, 2009. Internet resource. Tindall, William N, John M. Boltri & Mona, Sedrak. Patient-centered Pharmacology: Learning System for the Conscientious Prescriber. 2014. Internet resource. Read More