For re-application L.V. An amplification or weakening may be observed. pharmacological effect.

I. Cumulation - Accumulation

1. Material cumulation - accumulation of the substance itself. it happens

absolute cumulation- related to the properties of L.V. It occurs with long-term use of substances that are long delayed in the body and are very slowly removed (barbatura, SG, bromides, anticoagulants of indirect type of action ...)

relative cumulation - occurs during the disease of the liver or kidney, i.e. those organs that ensure the destruction and elimination of alien substances. Cumulation Correction: - Dose reduction, reduction of receptions

2. Functional cumulation - accumulation of "pharmacological effect", i.e. The substance from the body is excreted quickly, but the changes that it caused in the body (anticoagulants of an indirect type of action, ethanol - "white hot", sympatholytolitis, etc.)

II. Addictive (tolerance \u003d stability) - reducing the effect when long use L.V. (Sleeping, hypotensive, analgesics, laxatives, ng, etc.). To obtain the effect of the necessary strength requires an increase in dose.

Reasons: a) lowering the sensitivity of recipes; b) acceleration of the destruction of LV; c) the inclusion of the compensatory reactions of the organism d) exhaustion of endogenous metabolites involved in Pharmacodynamics L.V. (NG, antidiabetic produce. Sulfanylmurochina).

To prevent addiction, rationally combine preparations with a different mechanism of action.

Tahofilaxia - acute form addiction. Reducing the effect during re-administration L.V. After short intervals (ephedrine).

Drug addiction - Drug addiction, addiction. This is an insurmountable desire for receiving L.P. In order to eliminate physical or mental discomfort. It is often characteristic of substances acting on the CNS (psychotropic means). Such drugs cause a feeling of mental comfort, good health and mood, euphoria, sometimes unusual mental reactions, hallucinations, feeling of tide of strength or pleasant relaxation.

Allocate:

BUT) mental addiction - Cancellation of the drug causes emotional discomfort, worsening mood, insomnia, the presence of unpleasant experiencing and sensations;

B) physical addiction - Cancellation is accompanied by disorders in the activities of various organs and systems, i.e. somatic violations;

IN) abstinence - cancellation syndrome, developing as a result of a drop in the concentration of narcotic substance in the blood. Accompanied by severe emotional and vegetative disorders up to death (anxiety, anxiety, sleep disorder, nausea, vomiting, sweating, severe pain, tear, diarrhea, temperature increase and blood pressure, tachycardia, respiratory disorders, etc.)

With repeated administrations of medicinal substances, an addiction, drug dependence (addiction), cumulation, sensitization, can be observed, followed by an allergic reaction.

Getting used. A gradual weakening of the action of a medicinal substance, forcing the dose of the drug or replacing it to others, is called addiction. Sometimes the reason for addiction can be explained by the accelerated process of metabolism medication in the body. To some medicinal substances, addictive develops very quickly. For example, when re-administered ephedrine with small spots (20-30 minutes) there is a significant decrease in the vasoconstrictor effect after 2-3 injections. This phenomenon is called tahifilacia (from Greek. Tachys - fast, phylax- is - protection). Addiction should not be identified with medicinal dependence (addiction). These are completely different concepts.

Drug addiction (addiction). This phenomenon is characterized by a strong, sometimes irresistible, desire to systematic use of some medicinal and other substances causing euphoria (peculiar intoxication, pleasant mood). Euphoria can cause some substances affecting the psyche: morphine, heroin, cocaine, alcohol, hashish, nicotine, a fenamine, etc. Most of these substances are drugs, so the systematic use of their drug addiction is called drug addict. The addiction is usually combined with addiction phenomena, so the euphorizing dose of the drug is steadily growing, which leads to chronic poisoning of the body. Patients who suffer from drug addiction are called addicts.

Currently, the term "addiction" is replaced by the concept "Drug addiction ».

Such a definition shows that the drug (or another substance) in the process of long use becomes the necessary part of the cells of the Central nervous systemAnd the body is addressed to this substance. Indeed, the discontinuity of drug reception leads to severe subjective sensations and violations of the function internal organs. These phenomena are called abstinence (from Lat. Abstinentia - abstinence, deprivation), they quickly pass when renewing drug reception.

Distinguish mental and physical drug addiction. Mental drug addiction is accompanied by unpleasant emotional phenomena, oppressed mood, sometimes aggressiveness. With physical dependence, the state of the drug addict is exacerbated by violations of the function of cardio-vascular system and other organs. An acute cardiovascular failure may occur (collapse).

Cumulation. As a result of slow metabolism or removal of drugs in the body, their cumulation may occur (lats. SSPIIO - cluster). In such cases, repeated administration of drugs in therapeutic doses may lead to a significant increase in their concentration in the body (material cumulation) and poisoning.

There is still a functional cumulation when the effect of the previous drug intake is preserved and enhanced when it is repeated receptions. Cumulation may be positive, as it allows for a long time to maintain the healing effect of the medication with rare introduced it into the body.

For drugs capable of causing, certain rules for use (breaks during treatment, a gradual reduction in dose), and leave from pharmacies. Pharmacists need to know these rules and give the appropriate clarification of the patients, especially in cases where the medicine is released without a recipe. Failure to comply with the established rules can lead to severe poisoning.

Sensitization (increasing sensitivity) of the body during repeated administrations of drugs and the occurrence of allergic reactions are regarded as a pathological phenomenon and complication of drug therapy.

Drug allergies are a peculiar reaction of the body to re-administer the drug, regardless of its dose. And the basis of the allergic reaction is immune processes. There are allergic reactions of immediate (anaphylaxia) and slowdown types, characterized by the variety of symptoms: urticaria and other skin rashes, bleasting, serum disease, bronchial asthma, anaphylactic shock, etc.

Mutagenicity and carcinogenicity of some chemical compounds must be taken into account when creating new medicines. Mutagenity - Ego The ability of substances to cause persistent damage to the genetic apparatus of the germ cell, which is manifested in the change in the genotype of offspring. Carcinogenicity is the ability of substances to cause the development of malignant tumors.

The increase in the effect of a number of substances is associated with their ability to cumulation. Under the material cumulation, they mean accumulation in the body pharmacological substance. It is typically for a long time. acting drugswhich are slowly removed or firmly binds to the body (for example, some heart glycosides from the group of spots). The accumulation of substance when it is reused may be the cause of the development of toxic effects. In this regard, it is necessary to dose such drugs, taking into account the cumulation, gradually reducing the dose or increasing the intervals between the drugs.

Examples of functional cumulation are known, at which the effect accumulates, and not the substance. So, with alcoholism, the increasing CNS changes lead to white hot. In this case, the substance (ethyl alcohol) is quickly oxidized and not delayed in the tissues. Only neurotropic effects are summed up.

Reducing the effectiveness of substances in their reuse - addictive (tolerance) - is observed when used various drugs (Analgesics, hypotensive and laxatives). It may be associated with a decrease in the suction of the substance, an increase in the speed of its inactivation and (or) an increase in the elimination, a decrease in the sensitivity of receptors or a decrease in their density in the tissues. In case of addiction to obtain the original effect, the dose of the drug should be raised or one substance is replaced by another. In the last option, it should be borne in mind that there is a cross-habituation to substances interacting with the same receptors. A special type of addiction is tachyphylaxia - addictive, arising very quickly, sometimes after one-time reception of the drug.

In relation to some substances (usually neurotropic), during their re-administration, drug addiction is developing. It is manifested by an insurmountable desire for receiving a substance, usually in order to improve mood, improve well-being, eliminating unpleasant experiences and sensations, including those arising from the abolition of substances causing drug addiction. In the case of mental dependence, the termination of the administration of the drug (cocaine, hallucinogens) causes only emotional discomfort. When receiving some substances (morphine, heroin), physical dependence is developing. The abolition of the drug in this case causes a difficult state, which, in addition to sharp mental changes, is manifested in various, often severe somatic disorders associated with the disorder of the function of many organism systems up to the deadly outcome. This is the so-called abstine syndrome.

With repeated use of medicines, the action may increase or decrease.

Strengthening effect

2. Sensitization.

Cumulation.The increase in the effect of a number of substances is associated with their ability to cumulation. Under material cumulation They mean accumulation in the body of the pharmacological substance. It is typically for long-term drugs (for example, some hearty glycosides from the group of ingredi). The accumulation of the substance during its reappointments may cause toxic effects. In this regard, it is necessary to dose such drugs, taking into account the cumulation, gradually reducing the dose or increasing the intervals between the drugs.

Known examples and the so-called functional cumulationat which the effect "accumulates", and not the substance. So, with alcoholism, the increasing changes in the function of the CNS can lead to the development of white hot. In this case, the substance (ethyl alcohol) is quickly oxidized and not delayed in the tissues. Only its neurotropic effects are summed up.

Sensitization. It is based on the reaction of the formation of the antigen anti-antibody complex.

Weakening effect

• Addictive
• Tahofilaxia

Reducing the effectiveness of the substance when they are repeated addictive (tolerance) is observed when using various drugs (analgesics, hypotensive, laxatives, etc.). It may be connected

With a decrease in suction of the substance,

An increase in the speed of its inactivation,

Increasing the intensity of removal,

Reduced sensitivity to medications receptor formations.

Special view of addiction is tahofilaxia - addictive arising very quickly, sometimes after the first introduction of the substance. So, for example, ephedrine during re-use with an interval of 10-20 min causes a smaller rise arterial pressurethan with first injection.

Drug addiction

For some substances (usually to neurotropic), during re-administration, drug addiction is developing. It is manifested by an insurmountable desire for the reception of a substance, usually in order to improve the mood, improving the well-being, elimination of unpleasant experiences and sensations, including those arising from the abolition of substances causing drug addiction. There are mental and physical drug addiction. In the case of mental dependence, the termination of the introduction of drugs (for example, cocaine) causes only emotional discomfort. When receiving some substances (morphine, heroin), physical drug addiction is developing. This is a more pronounced degree. The abolition of the drug in this case causes a severe condition, which, in addition to sharp mental changes, is manifested in various and often serious somatic disorders associated with the disorder of the functions of many organism systems up to a deadly outcome. This is the so-called abstinence syndrome, or phenomenon of deprivation.

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The repeated introduction of the same drug substance can lead to a quantitative (increase or decrease) and to a qualitative change in the pharmacological effect.

Among the phenomena observed during repeated administration of drugs, there is a cumulation, sensitization, addiction (tolerance) and drug dependence.

Cumulation (from lat. cumulatio -increase, accumulation) - accumulation in the body of the pharmacologically active substance or effects caused by them.

If, with each new administration of the medicinal substance, its concentration in the blood and / or tissues increases compared with the previous administration, such a phenomenon is called material cumulation. Drugs can accumulate during repeated administrations, which are slowly inquisitive and slowly output from the body, as well as medicinal substances that are firmly associated with blood plasma proteins or in tissue depot, for example, some snow pills from a group of barbiturates, heartstarting glycosides. This may cause toxic effects, in connection with which such drugs should be dispensed, taking into account their ability to cumulation.

If, with repeated administrations of the drug substance, an increase in the effect is observed without increasing the concentration of the substance in the blood and / or tissues, such a phenomenon is called functional cumulation. This type of cumulation takes place when repeated alcohol intakes. With the development of alcoholic psychosis (white hot) in susceptible individuals, nonsense and hallucinations are developing at a time when ethyl alcohol has already been metabolized and is not determined in the body. However, the increasing changes in the function of the CNS occur. Functional cumulation is also characteristic of Mao inhibitors.

Sensitization. Many medicinal substances form complexes with plasma proteins, which, under certain conditions, acquire antigenic properties. This is accompanied by the formation of antibodies and sensitization. Repeated administration of the same medicinal substances in a sensitized organism manifests itself allergic reactions. Often such reactions occur during repeated administrations of penicillins, procaine, water soluble vitamins, sulfanimamides, etc.

Addictive (tolerance, from lat. tolerantia.- Patience) - Reduction of the pharmacological effect during repeated administrations of the drug in the same dose. The addictive may be due to a change in the pharmaceutical chinetics of the drug substance (reduction of suction, increasing the speed of metabolism and removal), as well as a decrease in the sensitivity of receptors and / or a decrease in their density on the postsynaptic membrane. For example, addiction to barbiturates may be a consequence of an increase in the intensity of their metabolism due to the induction of enzymes under the action of the same barbiturates. Drug addicts can develop from several days to several months. In the event of addiction to obtain the same pharmacological effect, an increase in the dose of the drug is necessary, which may result in strengthening it. side Effects. Therefore, they often take a break in the use of this substance, and if necessary, preparations are prescribed similar actionbut from another chemical group. When replacing one substance to another, independently of its chemical structure, there may be a cross-addiction if these substances interact with the same substrate (for example, a receptor or an enzyme)

A special case of addiction is Tahofilaxia (from Greek. tachys.- fast, phytaxis.- Protection) - fast development Treatment with repeated administrations of the drug after short intervals (10-15 min). Tahofilaxia to Ephedrine is well known, which is due to the exhaustion of N-Radrenaline reserves in the end of sympathetic nerve fibers. With each subsequent administration of the ephedrine, the amount of norepinephrine released into the synaptic slit decreases and the hypertensive effect of the drug (lifting blood pressure) after the 2nd or 3rd administration decreases.

Another particular case of addiction is mitridatism - the gradual development of insensitivity to the action of medicines and poisons, which occurs during their long-term use is first in very small, and then in increasing doses. According to ancient Greek legend, the king Mithridat thus acquired insensitivity to many poisons.

With repeated reception of some substances causing extremely pleasant sensations (euphoria), drug addiction develops in predisposed persons.

Drug addiction is the urgent need (irresistible desire) in a constant or periodically renewable reception of a certain medicinal substance or a group of substances.

Initially, the reception is associated with the aim of achieving the state of Euphoria, to eliminate painful experiences and sensations, to achieve the feeling of well-being and comfort, to obtain new sensations in the development of hallucinations. However, after a certain time, the need for repeated reception becomes an insurmountable, which is aggravated by the cancellation syndrome - the occurrence of the receipt of this substance heavy conditionassociated not only with changes in the mental sphere, but also with somatic disorders (violations of the function of organs and systems of the body). Such a state is denoted by the term "abstinence" (from the lat. abstinentia -abstinence).

There are mental and physical drug addiction.

Mental drug addiction is characterized sharp deterioration Mood and emotional discomfort, feeling fatigue at the deprivation of the drug. It occurs when the use of cocaine and other psychostimulants (amphetamine), hallucinogen (diethylamide Lizerginic acid - LSD-25), nicotine, Indian cannabis (Anasha, Gashish, plan, marijuana).

Physical drug addiction is characterized not only by emotional discomfort, but also the occurrence of abstinence syndrome.

Physical dosage dependence develops to opioids (heroin, morphine), barbiturates, benzodiazepines, alcohol ( ethyl alcohol). , w.Drug addiction is often combined with addiction, while all major doses of the substance are required to obtain euphoria. The most severe drug dependence occurs in the case of a combination of mental dependence, physical dependence and addiction.

The use of substances in order to obtain an infusion action is called toxicomia.

Drug addiction is a particular case of toxicing, when a substance assigned to the list of substances causing drug dependence (narcotic substances) and to be controlled is used as an infrared agent.