Indications:

7. For the treatment of malaria in the acute period (malarial fever, malarial coma), hematoschizotropic agents are used

8. For the prevention of distant relapses of the disease (radical cure), patients who have had three or four days of malaria are treated with a histochizotropic agent acting on "dormant" schizonts (hypnozoites) - primaquine, the drug is prescribed according to the scheme.

9. For individual prophylaxis - chloroquine

10. For public prevention (especially three-day malaria) pyrimethamine + sulfadoxine (Fansidar).

11. FROMlaxity of labor; cardiac arrhythmias (in combination with digitalis drugs), whetherfever - derivatives of 4-methanolquinoline.

12. Malaria (tropical, three-day and four-day forms - for treatment and prevention) infectious polyarthritis, ankylosing spondylitis, glomerulonephritis, renal amyloidosis, paroxysmal atrial fibrillation, intestinal and extraintestinal forms of amoebic dysentery - derivatives of 7-chloroquinoline.

Contraindications:

4. Retinal diseases, Psoriasis, Porphyria.

5. Organic heart disease with arrhythmias, diffuse kidney damage, liver dysfunctions, blood diseases, psoriasis, diseases of the retina and cornea of ​​the eye, pregnancy.

6. Diseases of the middle and inner ear, auditory nerve, optic nerve diseases, cardiac decompensation, blood diseases, pregnancy after 4 months.

Side effects:

With long-term use of drugs are possible:

decreased appetite, abdominal pain, erythema, urticaria, headache, dizziness, sometimes tinnitus, sleep disturbances, nausea, vomiting, baldness, hair graying, blurred vision, corneal edema, irreversible changes in the retina (narrowing of the arteries, edema and yellow atrophy spots, scotoma).

Ticket 37

1. Basic principles (mechanisms) of action of medicinal substances. Their interaction with receptors.

2. M- and M, H-cholinomimetic substances. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs. Muscarine poisoning, measures of assistance.

3. Antihypertensive drugs of central neurotropic action. Classification. Mechanism of action. Side effects. Contraindications Comparative evaluation of drugs.

4. Antibiotics of the penicillin group... Classification. Mechanism of action. Side effects. Contraindications Comparative evaluation of drugs.

1. Basic principles (mechanisms) of action of medicinal substances. Their interaction with receptors.

Pharmacodynamics is a section of general pharmacology that studies the features of the effect of drugs on the body.

The mechanisms of action of drugs are the ways in which substances cause pharmacological effects. The main mechanisms of action of medicinal substances include:

1. Physical.The action of a medicinal substance is associated with its physical properties. For example, activated carbon is specially processed, and therefore has a high surface activity. This allows it to absorb gases, alkaloids, toxins, etc.

2. The mechanism of direct chemical interactionThis is a fairly rare mechanism of drug action, the essence of which is that the drug directly interacts with molecules or ions in the body. Such a mechanism of action is possessed, for example, by the drug unitiol, which belongs to the group of antidotes.

3. Membrane (physical and chemical).It is associated with the effect of drugs on ion currents (Na +, K +, Cl -, etc.), which determine the transmembrane electric potential. By this mechanism, drugs for anesthesia, antiarrhythmic drugs, local anesthetics, etc.

4. Enzymatic (biochemical).This mechanism is determined by the ability of some drugs to have an activating or depressing effect on enzymes. The arsenal of drugs with such a mechanism of action is very wide. For example, anticholinesterase drugs, monoamine oxidase inhibitors, proton pump blockers, etc.

5. Receptor... In the human body, there are highly specific biologically active substances (mediators) that interact with receptors and change the functions of certain organs or tissues of the body. When drugs interact with receptors, biochemical and physiological changes occur in the body, accompanied by one or another clinical effect

The ability of a substance to bind to cell receptors is called affinity1. Affinity is due to the fact that the spatial configuration of the drug can resemble the configuration of the endogenous ligand of this receptor. Intrinsic activity is the ability of a drug to cause receptor activation.

Allocate:

1. Agonists or mimetics are substances that, by binding to receptors, are capable of activating them, which causes the development of a response characteristic of this type of receptor.

2. Antagonists or blockers are medicinal substances that bind to receptors, but do not cause their activation (ie, their intrinsic activity is zero). Antagonists shield cytoreceptors and prevent the development of a response under the action of endogenous agonists.

3. Partial agonists are substances that bind to receptors and cause their activation, however, even if they occupy all receptors, these substances are not able to induce a maximum response for this type of receptor.

2. M- and M, H-cholinomimetic substances. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs. Muscarine poisoning, measures of assistance.

I. M-cholinomimetics:

one) Pilocarpine (ocular forms only)

2) Acyclidine (ophthalmic forms, tablets, injections.)

Mechanism of action: stimulates m-cholinergic receptors. They stimulate the central nervous system, narrow the pupil, reduce IOP, accommodation spasm, narrow the bronchi, bradycardia, increase the tone of smooth muscles in the bladder and uterus, increase the secretion of sweat glands, increase the tone of smooth muscles of the gastrointestinal tract, peristalsis.

Indications: glaucoma, intestinal atony, paralytic intestinal obstruction, xerostomia.

Contraindications: bronchial asthma, conduction disturbances in the myocardium, epilepsy, hyperkinesis, pregnancy.

Side effects: hyperexcitability, tremor, bradycardia, bronchospasm, spasm in the gastrointestinal tract and urinary tract, diarrhea, increased uterine tone.

II.M, H-cholinomimetics:

- Acetylcholine (only in experiments, quickly degrades)

- Carbocholine (eye forms only)

Mechanism of action: They act on both M- and H-cholinergic receptors, but the effect on H-cholinergic receptors is weak. The effects are the same as those of M-cholinomimetics.

Indications:

Glaucoma only.

Side effects and contraindications:

Like M-cholinomimetics.

Muscarine poisoning, measures of assistance: Use M-anticholinergics, most often atropine.