In the United States, the zeal of the federal government, which looks like a desire to eradicate drugs, is directly related to the extent to which the government is co-opted by the values ​​of fundamentalist Christianity. We harbor the illusion of a constitutional separation of church and state in the United States. But in fact, the federal government, by encouraging the prohibition of alcohol during the period of prohibitions, interfering with the rights to freedom of childbearing or consumption of peyote in America’s Aboriginal religious rituals, foolishly trying to regulate the consumption of food and certain substances, acts as a pressure lever in favor of the values ​​of the right wing fundamentalists .

In the end, the right to determine for oneself food and the preferences of certain psychoactive substances will be considered as a natural consequence of human dignity as long as it is done in such a way that it does not restrict the rights of others. The signing of the Magna Carta Charter, the abolition of slavery, the granting of voting rights to women – these are cases in which the evolving definition of what constitutes justice has been swept away by ossified social structures that have increasingly begun to rely on the “fundamentalist” reading of their first principles. The war on drugs is schizophrenic carried out by governments that consider trafficking to be reprehensible, while they themselves are nevertheless the main guarantors and patrons of the international drug business. Such an approach is doomed to failure.

The war on drugs was not meant to be victorious. On the contrary, it will continue as long as possible to allow various intelligence agencies to conduct their operations and squeeze out the remaining hundreds of millions of dollars in illegal profits from a planetary sale of narcotic substances, and then it will be declared defeat. And “defeat” will mean, as in the case of the Vietnam War, that the media faithfully portray the situation and name its real participants and that the public’s aversion to crime, stupidity and venality of the establishment will force them to reconsider the policy. In this cynical manipulation of people and entire nations in connection with drugs and stimulants, modern governments have tied themselves up with an ethical catastrophe,comparable with the revival of the slave trade in the XVIII century or with the recently rejected provisions of Marxism-Leninism.

The conclusion seems obvious: only legalization can lay the foundation for a sound policy on psychoactive substances. In fact, even the most disinterested commentators on this issue came to this opinion, although the political consequences of upholding legalization only contributed to slowing down its discussion. In his latest book The Great War on Drugs, Arnold Trebach formulated convincing arguments for a revolution in substance-related politics.

Another guiding model for dealing with the abuse of relevant substances can be found in how America historically dealt with different conflicting religions; in fact, they are all accepted as a suitable moral choice, which should be available to those who believe in it. The problem of psychoactive substances should be approached in the same way – more like religion than science. I would like law and medicine to recognize the personal, unscientific nature of the sphere of substance abuse, the introduction of some form of First Amendment of the guarantee of freedom to choose a personal doctrine of adherence to certain substances, but somewhat limited by reasonable medical principles. / Arnold S. Trebach. The Great Drug War (New York: Macmillan. 1987), p. 363 /

What he doesn’t discuss, he doesn’t even mention at all, these are the roles that hallucinogens will play in the public scenario after the period of their suppression. In fact, psychedelics seem to be insignificant, if only a measure of the social impact of substances is estimated in the millions of dollars from street sales. Only LSD continues to sometimes distinguish among psychedelics as a possible large-scale problem. However, estimates of the amount of psychedelics produced and consumed in the United States have been politicized, and therefore unreliable and meaningless.

But another measure of the social significance of substances shows that we neglect, at first, at least, the discussion of the social impact of psychedelic consumption when we consider the issue of legalization of psychoactive substances. The key to this other measure lies in the interest shown to the psychedelics of the CIA and military intelligence in the 60s in projects such as MK (“brain control” – mind control) and MK — ULTRA. The widespread belief that the conclusion of these studies was that television is the drug of choice for mass hypnosis, although reasonable, but it should not be taken at face value. I am sure that if psychoactive substances were legalized, fears of a cocaine epidemic or a general addiction to heroin would have been unfounded. I am also convinced that the interest in psychedelics would increase,and their consumption would increase, and that this possibility is of great importance for the ruling circles. This new interest in psychedelics should be foreseen and foreseen. If the use of psychedelics makes it easier to understand the social attitudes and assumptions of the original cultures of the partnership style, then ultimately the public nurturing institutions may wish to support this awareness.

It seems that some new planetary consensus is being built. What was previously in its infancy and unconsciously, now becomes conscious and at the same time logically built. The collapse of the Marxist alternative to a democratic consumer society for compact media and high technology was quick and complete. For the first time in the entire history of the planet, there is some definite, albeit dimly definable consensus regarding “democratic values”. This trend will meet the real resistance of various forms of monotheistic religious fundamentalism in the 90s. All this is a phenomenon of expanded consciousness caused by an information explosion. Democracy is an expression of the Archaic idea of ​​an equal group of nomads. In its purest terms, she is psychedelic through and through, and her triumph seems ultimately unmistakable.

The “Drug Problem” acts against the tendency of a planetary expansion of consciousness through the spread of democratic values. There is no doubt that a society that intends to control the consumption of psychoactive substances by its citizens is heading for the slippery slope of totalitarianism. No arbitrariness by the police, no supervision or interference in people’s lives will be enough to influence the “drug problem”. Therefore, there will be no limit to repressions that frightened public institutions and their brainwashing specialists can cause.

A policy of respect for democratic values ​​in the matter of psychoactive substances would be to educate people so that they could make an intelligent choice based on their own needs and ideals. This kind of simple prescription is necessary and, unfortunately, already late. A general plan for those who are seriously seeking to come to terms with the American drug problem might contain several choice points, including those listed below.

1. A 200% federal tax on tobacco and alcohol should be introduced. All government tobacco subsidies need to be stopped. More serious warnings should be printed on the packages. Twenty percent of the federal sales tax must be levied on sugar and its substitutes; it is necessary to stop all support for sugar production. On sugar packs, there should also be cautions, and sugar should be a mandatory topic in the school education program.

2. It is necessary to legalize all types of cannabis and introduce a 200% federal tax on the sale of hemp products. Information on the content of “THC” products (tetrahydrocannabiol) and current information on its effect on health should be printed on the package.

3. The lending activities of the International Monetary Fund and the World Bank should be closed in countries that produce hard drugs. Only an international inspection and a certificate stating that the country is not engaged in such activities will restore the right to receive a loan.

4. Strict control should be established, both for manufacturers and for owners of weapons. It was the wide availability of firearms that led to the close intertwining of the problems of violent crime and drug abuse.

5. The legality of nature, and therefore the legality of all plants for their cultivation and use, must be recognized.

6. Psychedelic therapy should be made legal and included in the existing insurance system.

7. It is necessary to strengthen the legislation on currency and banking operations. Today, a secret agreement between banks and criminal cartels allows for large-scale money laundering.

8. There is a direct need for serious support for research related to all aspects of substance use and abuse, as well as for serious public education.

9. One year after the implementation of the above, it is necessary to legalize psychoactive substances that are still considered illegal in the United States. The mediation is eliminated, the government can sell the substances at their price plus 200%, and this money can be placed in a special fund to pay the social, medical and educational costs of the legalization program. Money from taxation on alcohol, tobacco, sugar and hemp can also be placed in this fund.

10. At the end of this year, all drug offenders who did not use firearms and did not display criminal acts should also be pardoned.

If these proposals seem too radical, it is only because we have moved far from the ideals that were originally the most American. The basis of the American theory of social policy is the notion that the right to “life, liberty, and the search for happiness” belongs to our undivided rights. To declare that the right to seek happiness does not include the right to experiment with psychoactive plants and substances is to put forward an argument, narrow at best, at worst, ignorant and primitive. The only religions that are more than the traditionally sanctioned moral code are the religions of trance, dance ecstasy, and intoxication with hallucinogens. This is a living fact of the secret of being, and an inherent religious right is the opportunity to approach it in our own way.A civilized society will make this principle a law.

In order to somewhat simplify the presentation, cases were considered with the use of only one drug. Pharmacology also studies the effects of taking two or more psychoactive substances. Several drugs may be taken at the same time, or some next drug may be taken before the previous one is removed from the body.
Taking two or more drugs at once complicates the nature of the end result, since several drugs can interact with each other while being administered into the body. An interaction occurs when the action of one drug affects the action of another. Such interaction can be considered qualitatively and quantitatively. In pharmacology, the quantitative aspect is much better studied, that is, the strength of action of substances. In this sense, there are two types of interaction: the reinforcing effect of drugs and reducing it.
Combinations that enhance the effect. The term “synergism” is used to denote the interaction between drugs, which enhances their effect. If two specific drugs are synergistic, then the effect of their joint use will be greater than the sum of the effects of their separate use. In practice, it is difficult to determine whether certain drugs are synergistic, that is, whether the final effect is the simple result of adding the effects of two substances, or whether the drugs somehow reinforce each other.

In quantitative studies, drug interactions are presented as changes in the line of action of the dose. The case of synergism between the two drugs A and B is presented in Figure 4-7. The solid line is a typical dose response curve for a drug, which was analyzed in Figure 4-2. Drug synergism shifts this curve to the left (dashed line in the figure). It can be seen that if there is a drug B, drug A has a stronger effect.
Combinations that reduce the effect. The weakening of the effect of one drug in the presence of another in the body is indicated by the term “antagonism”. It is easy to guess that in case of antagonism of two drugs, the line of action of the dose in Figure 4-7 will move to the right. For example, amphetamines that stimulate the nervous system, are antagonists of alcohol and reduce its depressive effects. However, they do not interfere with alcohol to impair coordination of movements.

Importance of drug interaction. Knowledge of the nature of the interaction of substances is very important in medicine, since many drugs can be used in combination with others for more effective treatment of diseases. Thus, this interaction plays into the hands of medicine. On the other hand, it can create doctors and problems. Difficulties usually arise in the case when the doctor, prescribing the patient the medicine, does not know what other medicines he takes. One substance may negate the therapeutic effects of another. Moreover, the combination of certain drugs can have unhealthy or even deadly effects.
The interaction of substances in the body creates problems with the combination of drugs taken for treatment and other drugs. The most common situations of this kind are the mixing of substances that suppress the nervous system (depressants). For example, the simultaneous intake of alcohol and barbiturates can be fatal, since these substances enhance the sleeping effect of each other. This combination is often used for suicide, but sometimes death occurs as a result of careless mixing of these substances.

Drug interactions significantly affect the causes and nature of their use. People can deliberately mix drugs with the same or similar effect to get a “super effect”. It happens, on the contrary, used drugs with opposite effects to weaken the action of one of them. In rehabilitation centers, you can often meet people who have used alcohol with its depressive effects to overcome excessive stimulation caused by cocaine. Often they drink a lot of black coffee after drinking. Caffeine is an antagonist of alcohol, and it partly relieves the depressive effect of the latter on the central nervous system. These examples show actions related to the quantitative effect of drugs: people try to change the power of their actions. By mixing drugs, one can also achieve qualitative interaction between them. So,if a person takes a depressant (say, some of the benzodiazepines) along with LSD, then as a result he will experience complete peace of mind combined with a change in perception that will cause LSD.

These are the last two terms that are introduced here to describe the effects of drugs. They arose from the fact that individual reactions to the same dose of the drug are very diverse. As a result, to determine the effect produced by a given dose, it is not enough to examine one person. The effect is often described in comparative terms or in a quantitative ratio of people who have this effect at a certain dose.
Figure 4-6 shows the dose lines of action for two effects. The difference of this graph from the previous ones is that on the vertical axis is not the magnitude of the effect of the drug, but the percentage of people who have this effect. This change is made to better illustrate effective and lethal doses. These terms clearly define the effect. We consider the change in the percentage of people experiencing this effect, with an increase in the dose of the drug.

The effective dose (ED) is the percentage of people who have the desired effect at a given dose. This can also be expressed as the dose at which a given number of people have an effect of interest to us. To find the ED on our graph, you need to draw a line from a certain percentage of people to the dose curve and then lower the other line to the horizontal axis. The point of intersection will give us an ED for a given percentage of people. Figure 4-6 shows the standard pharmacological term ED 50, in this case for the sedative effect of a certain drug. ED 50 means that 50% of people who have received a given dose of a drug will be sleepy. Similarly, you can define an ED for any other percentage. Figure 4-6 shows two more such effective doses.

Lethal dose (LD) is a specific case of an effective dose. As the name implies, the effect of interest in this case is death, and thus, LD represents the percentage of animals (people in experiments with lethal doses, of course, are not used) who die from a given dose of a drug over time. Pharmacological standard and here 50%. LD 50 is the dose at which 50% of the animals that received it die during a given time. The dose of LD 50 for humans is determined by extrapolating data obtained from animals. In Figure 4-6, the LD 50 of our imaginary drug is presented on the right line.
Knowledge of these two doses is very important. For example, medical institutions need to know what the discrepancy is between the ED and LD of a given substance. If the discrepancy is small, then the risk of unintentional suicides of people who use these substances not in therapeutic purposes. For some drugs, say caffeine and marijuana, the difference between ED and LD is large. But other drugs pose big problems. Occasional death from a heart attack while taking cocaine. Another example is alcohol. If a person weighing 70 kg and has an average tolerance for alcohol, drink 100 grams per hour on an empty stomach, he will feel relaxed. LD 50 for such a person will be 0.75 liters of whiskey per hour. Such doses are used much more often than you can imagine, and lead to severe poisoning and death. Moreover, if you mix drugs (say, alcohol and barbiturates), then the total ED and LD get very close together and the risk of death increases.

And the last note: the divergence of these doses is always taken into account when prescribing drugs for medical purposes. Doctors are looking for substances, a certain dose of which would produce the desired therapeutic effect (that is, was an effective dose) for all patients, did not give side effects and thus was not fatal. The therapeutic index is displayed: this is the LD 50 / ED 50 ratio for the drug. The most common ED is to relieve the symptoms of any illness or poisoning. You see, the higher the therapeutic index of a substance, the bolder it can be used in medicine. As a rule, the steeper the slope of the dose line, the lower the therapeutic index of the substance. Knowing the therapeutic index of the drug, the doctor can easily determine whether to prescribe it in this case.

To determine the dose of a substance, you need to know the magnitude of the effect it produces. Above, you saw that the narcotic effect depends on the dose taken. There may be hundreds of dose sizes, and it would be rather difficult to understand the various effects. Therefore, we need a tool that will present the data clearly and definitely, to the extent possible. In pharmacology, such a tool is a dose action line. This is a common form of image effects obtained from taking different doses. Several groups of people will take different doses of alcohol and after a certain time they will be asked to describe the degree of their relaxation. From the average data for each group, a schedule is compiled, which will be the dose action line.
In fig. 4-2 shows a sample of such a line. Vertical presents the changes of interest to us, let us designate them as the “effect size”. The nature of the changes to which special attention is paid in this book is determined by generally accepted methods for measuring the mood, behavior or functioning of the nervous system. Examples are memory testing, mood assessment, measurement of physiological parameters such as pulse. Doses are marked on the horizontal axis (often their logarithms). The studies cover at least three doses. After that, it remains to plot the data on the strength of the effect of the studied drug on people who have received a certain dose. Either different doses are given to different groups of people, or the same group receives these doses over several days.In both cases, we get the average effect of each dose studied.

Thus, the graph depicts the functional dependence of the magnitude of the effect on the dose of the drug.
From Figure 4-2, it can be seen that the effect varies with dose change. The shape of the line suggests that an accurate dose is needed to accurately determine the magnitude of the effect. For example, the larger the dose of the drug in Figure 4-2, the greater the effect it produces. But there is a limit: at the highest doses, the schedule tends to move to a horizontal line. This means that increasing the dose over a certain level does not enhance the effect. You can illustrate this with the effect of alcohol on the time it takes a person to have a simple reaction, for example, say yes or no in response to the presence or absence of any stimulus, say light. For an “average” drinking person, taking two 0.33-liter doses of beer per hour had practically no effect on the reaction time. After four doses, the time required for a response has increased markedly.After five doses, responses began to be given even more slowly. If a person took nine or more doses of beer per hour, he was very sleepy, and thus measuring the further deterioration of the reaction as alcohol was consumed would be simply useless. At this point, when a person has to make great efforts not to disconnect, the possibilities and benefits of such a measurement will tend to zero. After a ninefold dose, the line of action will take a horizontal position on the graph.the possibilities and benefits of such a measurement will tend to zero. After a ninefold dose, the line of action will take a horizontal position on the graph.the possibilities and benefits of such a measurement will tend to zero. After a ninefold dose, the line of action will take a horizontal position on the graph.

This experience with alcohol and the time of a simple reaction shows that the question is not what effect a particular drug produces at all, but how much the effect is at a particular dose.
Variation of dose action lines. Graphs of the effect of dose size may differ from that shown in Figure 4-2. One option is a biphasic narcotic effect. This means that up to a certain point with increasing dose, the effect increases, but then, despite the continued increase in dose, it falls. This case is shown in the figure.
The magnitude of the effect here increases with increasing doses from small to moderate. At higher doses, the line changes direction, noting a decrease in the narcotic effect. In this example, the magnitude of the effect returns almost to the original level obtained at the lowest doses. Pulse is one of the biphasic effects of alcohol and marijuana.

Any drug produces many effects, the strength of which is measurable, and therefore a dose action line can be constructed for any such effects. Many lines have similarities, and as a rule they belong to the type shown in Figure 4-2. Nevertheless, some dose lines of a single drug may look completely different. It depends on what effects to compare with each other.

We know that the line of action of the dose depends on the magnitude of the measured effect. This is illustrated in Figure 4-4, representing the results of laboratory studies of how sexual arousal feelings change in female students (first effect) and physiological parameters (blood flow to the genitals) of their arousal (second effect) when they consume small and moderate doses of alcohol. A negative narcotic effect is also shown on the vertical axis. According to the schedule, with an increase in the dose of alcohol to moderate, the students felt an increase in sexual arousal (large doses were not studied). At the same time, the physiological parameters of female sexual arousal decreased with increasing dose.
Slope, maximum effect and power of action. These are terms used in pharmacology to describe in more detail the action of a drug. They are presented in Figure 4-5, where dose action lines for two drugs, A and B, are constructed. Graphs have a slope, its characteristic is steepness. It is associated with time passing to achieve a strong effect. This inclination is taken into account in practical activities: in drafting a prescription for drugs or predicting life-threatening effects of drugs. An example of the latter is the sedative effect of barbiturates or the effect that the simultaneous use of benzodiazepines and alcohol gives. In Figure 4-5, line A has a steeper slope than line B, and since these curves then take a horizontal direction, this dose of drug A produces a greater effect.

Figure 4-5 also presents two other concepts: maximum effect and strength of action of a drug. The maximum effect of this drug corresponds to the highest point of the dose action line. In the figure, this is the moment when the curves stop growing. In this case, we have two drugs with the same maximum effect. The power of action – the dose of the drug, giving this maximum effect. If you draw a line from the point of maximum effect down to the horizontal axis, the point of intersection will be the force of action of the given drug for a particular effect.

Drugs can be eliminated directly from the body or first decompose into substances whose metabolites are less likely to be re-absorbed. These secondary substances are also excreted from the body. Liver enzymes play a major role in drug metabolism. It is important that these enzymes are also found in other organs, such as the kidneys and the digestive tract. Therefore, a drug ingested by mouth undergoes partial decomposition by enzymes. Thus, less substance reaches the required place than was accepted. Some drug metabolites are pharmacologically active. They cause, for example, side effects of various drugs. There are two examples of metabolites with psychoactive properties: these are diazepam (Valium) and chlordiazepoxide (Librium) metabolites. One of the metabolites of diazepam is removed from the body more slowly,than diazepam itself. Their action is terminated by further metabolism or elimination from the body along with urine.

The main organ responsible for the removal from the body of both drugs and their metabolites is the kidneys. But removal can go in other ways. For example, drugs ingested by mouth are sometimes excreted along with feces. Drug metabolites can be removed along with bile.
Drugs are released in human milk, and although the quantity of drug withdrawn in this way is small, the infant is at serious risk. Drugs can also be removed through the lungs: this is why the breath of a person who has taken alcohol smells like alcohol. Finally, drugs are removed with sweat. Drug testing Discussion of the process of removing drugs from the body brings us to the question of how to test a person for drugs. There are many methods for determining whether a person has taken drugs using urine or blood tests. Urinalysis is more sensitive because there can be found metabolites of the drug. If the drug is found in the blood, it indicates a very recent use of it.

The success of the test depends on many factors, including the magnitude of the last dose taken, the specific test method and the exact procedure followed. The ability to detect a drug depends mainly on the rate of its elimination from the body and the rate of elimination of its metabolites. Table 4-4 shows the time of excretion of drugs (and their metabolites) from the body and the time after which it is possible to detect them in the body after use. Less time in the second column corresponds to the removal of the drug itself from the body, more time – its metabolites.
For alcohol, only one time is indicated, since its metabolites are widely distributed in the body, and the alcohol test for its metabolites will be unreliable.

The third column indicates the maximum time during which the test can produce results. This time is greatly increased if the content of drug metabolites in the body can be measured. This time is usually much shorter than the period of excretion of drugs and their metabolites from the body. This is because testing has limited sensitivity and cannot detect the content of metabolites after a certain limit. This limit depends on the specific metabolite and testing methodology. This means that a positive review of pharmacokinetics has led you to the result; however, it does not inform us of the exact time of drug use. The exception is, as noted, the detection of a drug in the blood, which indicates a very recent use.Traces of a large dose of marijuana can be detected within eight days of use. In the body of people who constantly use marijuana, you can find traces of it more than a month after taking the last dose.

Farcodynamics 

Let us turn to understanding the mechanism of action of drugs. This is a subject of pharmacodynamics. In the remainder, terms will be introduced in which pharmacologists describe the effects of drugs, as well as graphical expressions of such effects.

The transfer of drugs to the place of their action is strongly influenced by the biochemical properties of both the organism and the drugs. Since the drug is transported by blood, it is natural that those parts of the body that are more supplied with blood receive and more drug. Indeed, after the absorption of a drug, the heart, brain, kidneys, liver and other organs that require a lot of blood receive most of it. To parts of the body in which the blood circulation is not so intense (muscles, internal organs and fatty tissue), the drug comes much later. In addition to circulation, the transmission capacity of the membranes and tissues affects the nature of the spread. Fabrics with higher throughput get the drug faster.

Drug properties have a significant effect on distribution. The main example is solubility in fats. The better the drug dissolves in them, the easier it passes through the shells and quickly reaches its place of action.
The solubility of a substance in fats greatly depends on how much it enters the brain. The volume of blood passing through the brain is so large that the brain could become a real depot of drugs (and other chemicals) entering the body. But before any substance enters the brain, it must overcome the barrier. As mentioned in Chapter 3, this barrier serves as a blood filter, and removes toxins from it before they enter the brain. Filtering is based on the fact that the pores of the capillaries of the brain are very small and close to each other, which makes it impossible for foreign substances to pass through them. In addition, the capillaries are surrounded by a thin wall of glial cells that make up the second line of defense. If the drug is well soluble in fats, like benzodiazepine diazepam (Valium), then it easily passes through the capillaries,and through glial cell membranes. But these obstacles are insurmountable for less fat-soluble substances.

Another chemical property of drugs that affects their distribution is the ability to combine with elements of the body. For example, some drugs, such as barbiturates, interact with certain plasma proteins. The more selectively the drug reacts with the elements of the body, the slower it is transferred to the right place. Likewise, the chemical structure of some drugs makes them susceptible to reaction with the tissue of the body. In this case, the drug can be released from this tissue only after a long time. It may appear in the blood, but its release from adipose tissue is so slow that it has a very minor effect on the psyche. A good example of a drug that reacts with fat is marijuana. Due to the selective nature of the compound with the molecules of the body, it does not spread throughout the body,and its effect is weakened. Part of the dose taken can not quickly reach its place of action.

Thus, the processes of absorption and distribution of the drug show that the drug in the body violates the biochemical equilibrium and causes resonance throughout the system. Absorption and distribution are complex bases of bioavailability, that is, the amount of a drug that reaches its site of action. Bioavailability is very important when considering the effects of drugs on the body. To understand the long-term effects of drugs, you need to trace their destruction or elimination from the body.

In medicine, this method usually replaces the ingestion, if the substance can adversely affect the digestive tract. Acceptance through the skin is not particularly effective for most drugs, because the skin is a barrier to many chemical compounds and is relatively impermeable. But there are drugs that freely penetrate even through intact skin, and for them this method is quite applicable.
The absorption of drugs through the skin can be accelerated by selecting those parts of the body where the skin circulation is strongest. In addition, to improve the penetration of the drug can be mixed with other substances (for example, to make an oil mixture). In the form of a patch, you can take nitroglycerin – this removes the problem of the metabolism of a substance before it reaches its destination.
The choice of method depends on the properties of a particular substance, the purpose of its reception, as well as the advantages and disadvantages of a particular method of taking this substance in these circumstances. In tab. 4-2 are the main considerations for the eight drug intake methods that we discussed above. Table 4-3 shows the intake methods used for some substances.

Absorption of a drug 15

Absorption can also be defined as the rate and extent of a substance leaving a place where it was introduced. It is very important for the action of the drug. Absorption and the factors inactive on it are extremely important because they affect bioavailability. This is the part of the dose taken, reaching the place of its action or falling into the liquid, which will transfer it to its destination. Thus, the bioavailability of a drug is directly related to its effect.
Differences in the rate of absorption for different methods of administration are determined by many factors. Let’s give some examples. In all cases, except for intravenous injection, the drug must pass through at least one of the shell before it begins to spread throughout the body. Since shells are mainly composed of lipids (fats), those drugs that are better dissolved in fats are absorbed much faster. Alcohol is an example of a fat-soluble drug. Another factor is the form in which the drug is injected: it is absorbed faster in aqueous solution than in suspension, in a fat mixture or in solid form. This is due to the fact that in the state of an aqueous solution, it is already completely ready for absorption. The solubility of a substance taken in solid form depends on the conditions in the part of the body where absorption takes place. For example,Aspirin is practically insoluble in the acidic environment of the stomach, which limits the possibility of its absorption. The condition of the digestive tract affects the absorption of substances ingested through the mouth. Strong blood circulation in the place of absorption accelerates it. Finally, the area of ​​the absorbing surface matters: the larger it is, the faster the substances are absorbed into the blood.
The factors affecting absorption are many, and they can act separately or all at once. Therefore, it is very difficult to accurately determine the effect of a drug on a person in certain conditions and at a certain time. Intravenous injection is the most effective way to deliver a drug to the site of its operation: the drug immediately connects with blood, the main element in the distribution system of substances in the body, and therefore many factors that delay absorption do not work.

As noted in Chapter 2, the most important thing that determines the effect of a substance entering the body is its quantity (these are components 1 and 2 in table 4-1). Pharmacology dose is determined on the basis of human weight, because the body of a larger person contains more fluid than the body of a smaller one. Consequently, if two such people take the same amount of a drug, then its concentration will be lower in the body (and, accordingly, in the organ on which this substance acts) of a larger person. The greater the content of the drug in one or another part of the body, the, as a rule, the stronger the effect. Therefore, the amount of the substance taken should be accurately calculated based on the weight of the person.
First, determine the desired dose of the drug in milligrams per kilogram of human weight. Then the patient is weighed. Then it is easy to calculate the desired dose for this person. For example, if the required dose is 0.8 mg / kg, a person weighs 80 kg, then he should be given 0.8 x 80 = 6.4 mg of the drug.

Methods of administration

In pharmacology, the expression “method of administration” means exactly how the substance enters the body. The strength of the substance (component 3 of table 4-1) largely depends on the method of administration. In this section, we will discuss eight ways. These are the five most common: oral administration, injection (includes three types – subcutaneous, intravenous and intramuscular) and inhalation. Three other important ways are intranasal (inhalation), sublingual (placement under the tongue) and transdermal (through the skin).
Orally. Swallowing is probably the most familiar way to take medicine. Such drugs come in the form of pills, capsules, powders, liquids. These are a variety of headache medications, cough syrups, cold pills, etc., that are available in every pharmacy. Virtually all of the most affordable medicines are taken by mouth. This is the safest, most convenient, and economical way to take medicine.
After ingestion, the substance enters the stomach and is absorbed in the small intestine. Both the speed and the strength of its action depend on how the substance makes this way. The main factor determining the final effect is the food that is in the digestive tract during the intake of the substance. The more food, the slower the stomach is emptied, and in addition, it can reduce the concentration of the drug. As a result, absorption begins late, and the level of the substance in the blood is low. (This result is clearly noticeable if you compare the degree of intoxication from drinking alcohol after a heavy meal and on an empty stomach.) In addition, food can envelop the substance, and it will be released from the body along with feces. Finally, the substance taken by mouth is absorbed by the blood more slowly than if taken in other ways.

Thus, the advantages of ingestion through the mouth (comparative safety, convenience and economy) are balanced by disadvantages – a long time before absorption and a low efficiency. Moreover, gastric acids released during digestion partially destroy some substances, in particular, heroin. Once in the blood, such altered substances pass through the liver, the main organ responsible for the metabolism of most substances, and therefore only a small part of the substance reaches the brain, which inevitably reduces its effect.

Injection. The basis of the three other most common methods of drug intake is an injection of a substance using a syringe. They are usually dissolved beforehand in a liquid (“carrier”) or mixed with it. Methods of administration associated with the injection of substances subcutaneous, intravenous and intramuscular. Subcutaneous intake Injecting a substance under the skin is the simplest of these three methods, since it suffices to pierce the skin with a needle. This method is used by many novice drug addicts. It is also used in medicine for the introduction into the body of substances that do not irritate tissues (because substances introduced in this way are absorbed gradually and slowly, although faster than when taken by mouth). You can pick up a carrier fluid with which the substance is absorbed into the blood the fastest.The subcutaneous route of administration is not suitable in two cases: if the substance is irritating to the tissue and if too much solution is required to obtain the desired effect.
Intramuscular intake. In order to inject a substance into a muscle, a deeper needle penetration is needed than with a subcutaneous injection. But if the substance injected in this way is dissolved in water, and there is intensive blood circulation in the muscle, it is absorbed faster. The rate of absorption depends on which muscle group is injected. It is also influenced by the type of carrier fluid in which the substance is dissolved. The lack of an intramuscular injection is that it causes pain at the injection site. In addition, such an injection should be done by a specially trained person, otherwise there is a high risk of blood poisoning and tissue damage.

Intravenous intake. This method removes most of the problems associated with absorption. The solution of the substance is injected directly into the vein, and it begins to act immediately. Therefore, this method is used in the provision of emergency medical care. You can enter the exact dose needed by this person. In addition, irritating substances can be administered intravenously (as well as irritating “carriers”), because the walls of blood vessels are relatively insensitive, and the substance also dissolves in the blood.

The benefits of intravenous administration are obvious. The main reason for its relatively rare use is that it is more likely to be associated with possible complications, because a large amount of the substance reaches the target organ very quickly. Another consideration is that if a substance is injected through a vein for a long time, it should be strong and healthy. In general, intravenous injection is associated with the risk that it should be done slowly and monitor the patient’s response. Of course, these requirements are met in a medical institution, but it is unlikely that the same thing happens where people take drugs.
People who regularly take heroin, cocaine or their mixture (“speedball”) intravenously are often referred to as “well-established” drug addicts. They inject the drug into the vein because they want immediate and strong action. The usual dangers of intravenous use in combination with the sudden strong effect of the drug cause a great deal of damage to human health. Today, the fatal outcome of intravenous drug use is common among drug addicts.

To prevent infection by diseases such as AIDS, hepatitis, or tetanus, sterile needles and solutions should be used when injecting drugs intravenously. Drugs introduced into the body in any of the three methods of injection bypass such protective mechanisms as the skin and mucosa. Thus, pathogenic microorganisms that the body cannot neutralize can be brought in with a dirty needle or non-sterile solution. Therefore, street addicts are at great risk of contracting AIDS.

Inhalation. Some drugs can be absorbed through the membranes of the lungs. With inhalation of such drugs, the desired effect is achieved quickly (faster than with subcutaneous or intramuscular injection). In order for the drug to be inhaled, it must be in a certain state. Inhalation is applicable to drugs that can be brought into the gaseous state. For example, you can inhale substances that are components of ordinary and affordable industrial products. Such substances with psychoactive properties are called inhalants. This, for example, benzene, toluene and ligroin. You can inhale drugs that are intended for use in the form of drops. Moreover, it is possible to inhalate a mixture of gas and narcotic with small particles. These are tobacco smoke and crack crack. Inhalation of the drug gives almost complete and rapid absorption.The disadvantage of inhalation is that only small amounts of the substance can be taken at a time.
Inhalation. A powder drug is inhaled through the nose. It is absorbed through the nasal mucosa and sinuses. Cocaine, heroin and snuff are usually taken in this way. Inhalation through the nose is a good way to quickly and completely absorb poorly soluble substances. True, if you inhale an annoying drug, it can disrupt blood circulation and cause serious harm. In this regard, we can give an example of the destructive effects of cocaine on the nasal septum and nasal tissue.

Dissolving under the tongue. A tablet of substance is placed under the tongue and dissolves with saliva. The substance is absorbed through the mucous membrane of the oral cavity. In this way, nitroglycerin is usually taken, used to relieve pain in the heart. This way you can take nicotine in the form of tobacco gum or “raw” powder.

Intake under the tongue gives a faster and more complete absorption of the substance than ingestion. In addition, this way you can take drugs that irritate the stomach and cause vomiting. In the form of pills, you can use almost any substance with narcotic properties. However, this method is less popular than one would expect, because many drugs have an unpleasant taste.

• Orally
  • One of the safest, most convenient and cost-effective ways to receive.
  • The presence in the stomach of food slows down the absorption and reduces the amount of substance entering the blood.
  • Gastric acids destroy some drugs, and thus reduce their effect.
• Subcutaneous injection
  • The easiest of the three methods of injection.
  • Absorption is faster than when taken by mouth, but slower than with other types of injections.
  • A good way to take drugs that do not irritate the tissues, because they dissolve slowly and gradually, and the substance has a lasting effect.
  • The method cannot be used if the substance is irritating to the tissue, or if a large volume of fluid is to be injected.
• Intramuscular injection
  • It requires a deeper penetration into the tissue, but with proper preparation of the solution and the choice of a site with an intensive blood circulation for injection, it gives a faster absorption.
  • Causes pain at the injection site.
  • The use of this method by people without special training is associated with the risk of blood poisoning or tissue damage.
• Intravenous injection
  • Gives the fastest absorption of all methods of administration.
  • The substance has an immediate effect, so the method is good for emergency medical care.
  • Since the substance acts immediately, you can enter the exact dose needed by a particular person.
  • The best method of injection is for receiving irritating tissue drugs, since the walls of blood vessels are relatively insensitive, and the drug is further dissolved in the blood.
  • Associated with the potential danger that a large amount of the drug will immediately reach the scene of action.
  • Frequent use of this method requires healthy and strong veins.
  • In order to avoid complications, the dose of the substance should be introduced gradually and following the reaction of the person.
• Inhalation
  • If the drug can be inhaled, it is absorbed almost completely and faster than with subcutaneous or intramuscular injection.
  • At one time you can not enter a large number of substances.
• Inhalation through the nose
  • If the drug is poorly soluble, it is the best way to take it.
  • Inhalation of a drug that irritates tissue or interferes with blood circulation can cause serious harm.
• Dissolving under the tongue
  • In principle, this method can take almost any drug (in the form of pills).
  • The substance is absorbed faster and more fully than when ingested.
  • A good way to take drugs that irritate the stomach and cause vomiting.
  • The method is applied less frequently than is possible, since many drugs have an unpleasant taste.
• Through the skin
  • Alternative to ingestion through the mouth, if the substance is bad for the digestive tract.
  • Many substances cannot be taken in this way, since their skin is relatively poorly permeable.
  • You can speed up absorption by choosing places with the best skin circulation, and improve the penetration of the drug through the skin by mixing it with another substance.