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 ( ethanol) It is quickly oxidized and not delayed in the tissues. Only neurotropic effects are summed up.

Reducing the effectiveness of substances with their re-application - 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 certain substances (usually neurotropic) when they are re-administered drug addiction. 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. Cancellation of the drug in this case causes heavy conditionwhich, in addition to sharp mental changes, is manifested in a variety, often heavy somatic violationsassociated with the disorder of the functions of many organism systems up to the deadly outcome. This is the so-called abstine syndrome.

Usually, the pharmacological effect increases in proportion to the increase in the dose. The concentration of the drug on the surface and inside the cell may depend on the factors involving the suction rate, distribution, transformation and removal, therefore, the dependence between the dose and the pharmacological effect may be linear (fluorotan), hyperbolic (morphine), parabolic ( sulfanimide drugs), sigmoidal or S-shaped (norepinephrine).

Repeated administration medicines It may cause a decrease or increase in the body's reaction on them. The reduced reaction of the body into drugs (hyporeactivity) is called an addictive, which is manifested by tolerance or tachyphilaxia. The increased response of the body (hyperreactivity) is manifested by allergies, sensing and idiosyncrazia. With repeated administration of drugs, special conditions may develop - a drug dependence, which also relates to reduced reactions, and cumulation.

Increased body reactions to the administration of drugs are allergic reactions that can be divided into 4 types:

Type 1. Immediate type of allergic reactions is developing within a few hours after the administration of the dose of the drug. The leading role is played by IGE - antibodies, binding to an antigen on the surface of the fat cells, leading them to degranulation, highlighting histamine. Manifested by urticaria, edema, anaphylactic shock, etc. (cause penicillins).

Type 2. Cytolithic type of reactions when IgG and IgM - antibodies, activating the complement system, interact with an antigen on the surface of blood shaped elements, causing them lysis (methyloft causes them hemolytic anemia, Analgin - agranulocytosis).

Type 3. Immunocomplex type of reactions when IgE - antibodies form complexes with an antigen and complement that interact with endothelium (damaging it). At the same time, serum disease manifested by fever, urticaria, itching, etc. (cause sulfonamides).

Type 4. Slowing type of allergic reactions in which cellular mechanisms are involved, including sensitized T-lymphocytes and macrophages. It is manifested in the form of contact dermatitis, for example, when applied to the skin of irritant drugs.

Increased reactions include idiosyncrasy (Greek. IDIOS is a kind; Synkrasis is a merger, mixing), that is, an increased genetically caused by the body's reaction with the introduction of medicines in small doses associated with the insufficient activity of some enzymes. Thus, with the hereditary insufficiency of cholinesterase serum, the elongation of dichilin action is associated with up to 2-3 hours.

Questions of computer tests on pharmacology at less 5 on the topic

Pharmacodynamics "- 2008

What is included in the concept of "pharmacodynamics"?

$ Mechanisms actions.

Transformation medicinal substances in organism.

$ Pharmacological effects.

Distribution of medicinal substances in the body.

$ Localization action.

Three types of action.

The effect of the medicinal substance arising in the place of application of the substance:

Resorbative.

$ Local.

The effect of the medicinal substance, developing after its suction:

Local.

$ Resorbative.

For local application The medicinal substance can have:

$ Local action.

$ Direct action.

$ Reflex action.

There are no correct answers.

The reflex is called an action that occurs when the receptor drug stimulation occurs:

$ Afferent reflex link.

Central reflex links.

Efferent reflex link.

The main "targets" for the action of medicinal substances:

Structural proteins.

$ Ion channels.

$ Specific receptors.

$ Enzymes.

$ Transport systems.

Specific receptors are:

Receptors existing in the body for medicinal substances.

$ Receptors that exist in the body for endogenous ligands (mediators, hormones, etc.), with which drug substances can interact.

Internal activity is:

The ability of the substance to contact specific receptors.

$ Ability of a substance when binding to specific receptors to stimulate them and cause effect.

The ability of a substance when binding to specific receptors to block them and cause effect.

The affinity is:

$ Ability to communicate with specific receptors.

The ability of the substance to stimulate specific receptors.

The ability of the substance to cause the effect when interacting with specific receptors.

Substances with low internal activity are called:

Antagonist agonists.

$ Partial agonists.

Antagonists.

Full agonists.

Substances with high internal activity are called:

Antagonist agonists.

Partial agonists.

Antagonists.

$ Full agonists.

Medicinal substances exciting alone receptors and blocking others, referred to as:

$ Antagonist agonists.

Partial agonists.

Antagonists.

Full agonists.

The affinity (affinity) of the substance to the receptors is characterized by:

Constant Elimination.

$ Dissociation constant.

Constant ionization.

Medicinal substances with affinity and internal activity when interacting with specific receptors are called:

$ Agonists.

Antagonists.

Antagonist agonists.

Substances that have affinity to specific receptors do not have internal activity and impede the action on the receptors of endogenous ligands and agonists, are called:

$ Antagonists.

Partial agonists.

Antagonist agonists.

Substances that, when interacting with specific receptors, cause maximum stimulation of receptors and the maximum reaction, are called:

$ Full agonists.

Partial agonists.

Antagonist agonists.

Antagonists.

Substances causing with the stimulation of specific receptors reaction less than the maximum, are called:

Full agonists.

$ Partial agonists.

Antagonist agonists.

Antagonists.

The measure of the activity of the drug substance is:

The magnitude of the semi-maximal effect.

The magnitude of the maximum effect.

$ Dose, in which the substance causes a semi-aximal effect (ED50).

$ Minimum effective dose of substance.

$ Average therapeutic dose of substance.

$ Dose, in which the substance causes an effect equal to half the maximum effect.

Dose equal to half of the highest therapeutic dose of matter.

$ Is a measure of substance activity.

It is a measure of the effectiveness of the substance.

The effectiveness of the medicinal substance can be judged:

At the minimum effective dose.

$ Largest effect.

At a dose, in which the substance causes the maximum effect.

What is the term indicate unusual reactions to drugs associated, as a rule, with genetically determined enzymopathies and arising from the first introduction of substances?

Sensitization.

Tahofilaxia.

$ Idiosyncrasy.

Abstinence.

Getting used.

Idiosyncrasy is:

$ Unusual body reaction to the first administration of the medicinal substance.

Improving the sensitivity of the body to the medicinal substance.

Accumulation in the body of the medicinal substance.

Reducing the effect when re-administering the drug substance.

What phenomena may occur when re-administering medicinal substances?

$ Addictive.

$ Tahofilaxia.

Potentiation.

$ Drug addiction.

$ Cumulation.

Cumulation is:

Weakening sensitivity to the medicinal substance when it is repeated administration.

Improving the sensitivity to the drug in its repeated administration.

$ Amplification of the drug substance with its repeated administrations associated with the accumulation of the drug substance or its effect.

1. Addictive - gradual decrease in sensitivity to the action of the drug. For several months, years. Any substance is a xenobiotic.

2. Tahofilaxia – fast development sensitivity to the action of the drug. Rare phenomenon, but it is found. Developed within 30 minutes. Ephedrine and reflex stimulants of breathing. Works if there is an intermediary substance.

3. Addiction / Drug addiction mental and physical / addiction - an irresistible desire for receipt of the drug. In the absence of the patient, there is an abstineent syndrome, breaking. Narcotic analgesics, sleeping pills, tranquilizers, alcohol.

4. Cumulation - accumulation of medicinal substance in the body. a) material - the medicine is falling in the body as such. b) Functional - not the substance accumulates, and its ether. Characteristic to ester alcohol.

5. Increased sensitivity.

but) ideosynKrosia - congenital or primary Pathological sensitivity to the action of a medicinal substance. Genetic defect, enzyme failure. Formism is the reaction to the reception of horse beans?, Characterized by the Mediterranean.

b) allergy / Sensitization- occurs repeated and subsequent contacts with a medicine that acts as an allergen. D formation classic allergic reaction Requires primary contact with medicinal substance, synthesis in the body of antibodies. When re-administered, the antibody interacts with the antibody with an antibody, a histamine emission occurs, which determines the severity of the subsequent pathological reaction. Which can manifest itself from local manifestations to anaphylactic shock.

The strongest allergens Local anesthetics, antibiotics of a number of penicillins, derivatives of sulfanimamides.

Allergic is worth carrying a dose of adrenaline to chollow yourself if necessary.

Combined use of medicinal substances

Puts himself aim to change strength and severity pharmacological effect medicinal substances. The combination can follow the principle of synergies (joint action) and antagonism.

For synergies May be observed:

a) The amount of effect is a simple arithmetic addition of two or several effects of medicinal substances.

b) Potentation - a significant increase in the effect of two or more medicinal substances.

Neyroleptanalyzia. - The combination of narcotic analgesics and neuroleptics, which is used to treat psychiatric patients. This allows you to conduct surgical intervention without connecting the CNS.

Antagonism- Typical example: the use of antidotes, that is, antidote in poisoning.

Classification of drug interaction

1. Physico-housing. Activated coal and toxins - a typical example.
2. Chemicalinteraction. Hydrochloric acid (gastric juice) and lumps, in particular, drinking soda.
3. Pharmaceutical. Substances interact with direct contact. Furasimide is not a neighborhood tolerance with friendly substances. Tetracycline, in combination with milk, form insoluble compounds in the lumen. Eufillin does not combine with glucose. B12 should also be combined, except for finished drugs. The ACC is also very aggressive.
4. Pharmacokineticinteraction.
5. Pharmacodynamic interaction.

Side effects

Among side Effects Additional effects may be marked.

1. Distance syndrome - The exacerbation after the rapid abolition of the drug occurs a sharp aggravation of the underlying disease. For example, Clafilin. A potent drug cannot be abruptly canceled. Sleeping, glucocorticoids enterferon, etc. Cancel gradually, reduce the dose of half, to a quarter.

1. Oblasting syndrome - Against the background of the introduction of vasodilating drugs there is a deterioration in the blood supply of the heart or brain.

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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