AbstractThis report will focus on how flunitrazepam, a lipophilic drug,works in the organism and its effectiveness against a target. Generally,lipophilic drugs are accurately absorbed and well ingested within the humansystem.Figure 1.3D structure of flunitrazepam where grey corresponds to Carbon atoms; Oxygenatoms are red; Nitrogen atoms lavender; Fluorine atoms green and Hydrogen white.Source: data created from Scigress.Introduction Flunitrazepam, also known as narcozep, or primum, is a fast actingbenzodiapine – group of neuroactive drugs.
There is similarity in chemicalstructure, pharmacodynamics and pharmacokinetic properties to otherbenzodiazepines, e.g., diazepam. (T, 2001) Firstly, a pharmaceuticalcompany identified it in 1975 by experimenting moderation on benzodiapineclass.
Doctors prescribed this drug in Europe, Latin America, Asia andAustralia to treat insomnia, in tablet format, and as an oral premedicationbefore surgery through injections. Due to the presence of nitro group and afluorine atom in the molecular structure, shown in molecule stated above, theeffects of the drug are hypnotic generally but also, sedative, anxiolytic, musclerelaxing and anticonvulsant. (Simmons, 1998)Adolescents and young individuals misuse the drug tablets through amixing with alcohol or other dangerous products to extent the effect of those;however, the consequences can be fatal. Besides, the abuse of flunitrazepam isan important issue of concern globally because of the high rate of no correctapplication and illegal demand that is unceasingly increasing. Hence, thisexplains the drowsiness effect, also identified by the Log P value, 2.06.
The objective of this essay is to study the outcomes of how thedrug proceed once inside the organism focusing in the two types of routes –whether it differs or not; how the injection works, an abstract content of thetablets and how it reacts (advantages or disadvantages) among the impacts.AdministrationGenerally, the enteral method (oral administration) is the preferredroute due to the easy way of self-administration and low expenses. In otherwords, the oral administration is more reliable, but when ingested, the drugenters the organism through the gastrointestinal tract – GI tract –, whichcomprehend, from mouth to lower intestines. When the drug is taken in, dose of1.5-2 mg (depending on age), it does follow a route through the stomach, wherea great percentage of flunitrazepam will break down and decompose due to pHlevels- pH=2, basic-. The resting product proceed to the gut wall to finallyenter the bloodstream and finally the liver, where the enzymes will cataboliseflunitrazepam (metabolism) (Graham L.
, 2017).On the other hand, If the administration is via intra-arterialinjection, dosage of 2 mg, the drug will enter bloodstream precisely,accurately and almost immediately meaning that it does not lose any proportionof the dose, although is more hazardous. In fact, the dose is specific; therefore,it cannot be more than prescribed amount since it could be fatal and lead todeath of the patient (M.
A.K. & H.M.
, 1980). AbsorptionThere are amine functional groups, which comprise flunitrazepam; therefore,the overall pKa will have a basic low value, 1.8. Thus, it will define whether it is water-solubleor not; in this case, the drug will facilitate the absorption (Graham L., 2017)of the drug through the cell membrane, common way of transport denominated transcellulartransport (blood, interactions). If the absorption take place slowly, the ratewill be less than if it occurs at high speed. As the character of flunitrazepamis lipophilic and the Log P value is greater than two i.
e. 2.06, it will stimulatea drowsiness outcome from the blood brain barrier – BBB. Additionally, themolecular weight (313 umas) could differ in the absorption effectivenessalthough is not relevant as the drug is satisfactory absorbed across the cellmembrane. By contrast, the injection method conducts to activation of receptorsof the brain by the synaptic acid, GABA, that affects the limbic system causingshort period amnesia, relaxation as mentioned before, decrease of cardiacfunctionality and respiration (M.A.K. & H.
M., 1980).In fact, the tablet format is the most adequate.DistributionGraham (2017) revealed that after absorption, the bioavailabilityof flunitrazepam is between the explicit ranges 80 %- 90%, approximately 85%,it quickly distributes into body tissues from the plasma and AUC, concentration-timecurve.
Therefore, the transportation of blood to reach the target, cellmembrane, along the organism throughout the width vessels depends on the rateproportion of flunitrazepam. Once inside the blood supply, the drug interactwith the proteins to bind to the receptor located in the cell membrane. Flunitrazepamis a non-polar compound; this favours the penetration into the central nervoussystem and cause drowsiness. The basic amine functional groups and thelipophilicity will allow a perfectly bind to the target after ionisation, whichwill facilitate this process. Nevertheless, if the lipophilic characterdimensions are high, the organism could not react accordingly by not reachingthe cell membrane and requiring a higher dosage. Consequently, the volume distributionwould be larger or less than 2.
86 L kg-1, depending in the individualweight i.e. an intravenous injection to anorexic patients will be less thannormal, in other words, the dosage will decrease to avoid overdose.