November 21, 2019

Abstract and pharmacokinetic properties to other benzodiazepines, e.g., diazepam.

Abstract

This 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 human
system.

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Figure 1.
3D structure of flunitrazepam where grey corresponds to Carbon atoms; Oxygen
atoms 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 acting
benzodiapine – group of neuroactive drugs.  There is similarity in chemical
structure, pharmacodynamics and pharmacokinetic properties to other
benzodiazepines, e.g., diazepam. (T, 2001)

 Firstly, a pharmaceutical
company identified it in 1975 by experimenting moderation on benzodiapine
class. Doctors prescribed this drug in Europe, Latin America, Asia and
Australia to treat insomnia, in tablet format, and as an oral premedication
before surgery through injections. Due to the presence of nitro group and a
fluorine atom in the molecular structure, shown in molecule stated above, the
effects of the drug are hypnotic generally but also, sedative, anxiolytic, muscle
relaxing and anticonvulsant. (Simmons, 1998)

Adolescents and young individuals misuse the drug tablets through a
mixing with alcohol or other dangerous products to extent the effect of those;
however, the consequences can be fatal. Besides, the abuse of flunitrazepam is
an important issue of concern globally because of the high rate of no correct
application and illegal demand that is unceasingly increasing. Hence, this
explains the drowsiness effect, also identified by the Log P value, 2.06.

The objective of this essay is to study the outcomes of how the
drug 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 the
tablets and how it reacts (advantages or disadvantages) among the impacts.

Administration

Generally, the enteral method (oral administration) is the preferred
route due to the easy way of self-administration and low expenses. In other
words, the oral administration is more reliable, but when ingested, the drug
enters the organism through the gastrointestinal tract – GI tract –, which
comprehend, from mouth to lower intestines. When the drug is taken in, dose of
1.5-2 mg (depending on age), it does follow a route through the stomach, where
a great percentage of flunitrazepam will break down and decompose due to pH
levels- pH=2, basic-. The resting product proceed to the gut wall to finally
enter the bloodstream and finally the liver, where the enzymes will catabolise
flunitrazepam (metabolism) (Graham L., 2017).

On the other hand, If the administration is via intra-arterial
injection, dosage of 2 mg, the drug will enter bloodstream precisely,
accurately and almost immediately meaning that it does not lose any proportion
of 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 to
death of the patient (M.A.K. & H.M., 1980).

 

Absorption

There 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-soluble
or 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 transcellular
transport (blood, interactions). If the absorption take place slowly, the rate
will be less than if it occurs at high speed. As the character of flunitrazepam
is lipophilic and the Log P value is greater than two i.e. 2.06, it will stimulate
a drowsiness outcome from the blood brain barrier – BBB. Additionally, the
molecular weight (313 umas) could differ in the absorption effectiveness
although is not relevant as the drug is satisfactory absorbed across the cell
membrane. By contrast, the injection method conducts to activation of receptors
of the brain by the synaptic acid, GABA, that affects the limbic system causing
short period amnesia, relaxation as mentioned before, decrease of cardiac
functionality and respiration (M.A.K. & H.M., 1980).

In fact, the tablet format is the most adequate.

Distribution

Graham (2017) revealed that after absorption, the bioavailability
of flunitrazepam is between the explicit ranges 80 %- 90%, approximately 85%,
it quickly distributes into body tissues from the plasma and AUC, concentration-time
curve. Therefore, the transportation of blood to reach the target, cell
membrane, along the organism throughout the width vessels depends on the rate
proportion of flunitrazepam. Once inside the blood supply, the drug interact
with the proteins to bind to the receptor located in the cell membrane. Flunitrazepam
is a non-polar compound; this favours the penetration into the central nervous
system and cause drowsiness. The basic amine functional groups and the
lipophilicity will allow a perfectly bind to the target after ionisation, which
will facilitate this process. Nevertheless, if the lipophilic character
dimensions are high, the organism could not react accordingly by not reaching
the cell membrane and requiring a higher dosage. Consequently, the volume distribution
would be larger or less than 2.86 L kg-1, depending in the individual
weight i.e. an intravenous injection to anorexic patients will be less than
normal, in other words, the dosage will decrease to avoid overdose.

 

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