Ticket 11

1. Dependence of the effect on the dose (concentration) of the active substance. The breadth of the therapeutic action. The value of the choice of dosage forms and methods of drug administration.

Depending on the dose of the drug, the rate of development of the effect, its severity, duration, and sometimes character change. Usually, with an increase in the dose (concentration), the latency period decreases and the severity and duration of the effect increases.

Dose -the amount of substance per dose. It is indicated in grams or fractions of a gram. For a more accurate dosage of drugs, their amount is calculated per 1 kg of body weight. Sometimes substances are dosed based on the size of the body surface (per 1 m ^ 2)

Therapeutic doses:

 minimum (threshold) therapeutic dose - the minimum amount of a drug that causes a therapeutic effect;

 average therapeutic dose - the range of doses in which a drug has an optimal prophylactic or therapeutic effect in most patients;

 maximum therapeutic dose - the maximum amount of a drug that does not have a toxic effect.

Lethal doses:

 the minimum lethal dose (LD10) is the dose that causes death in 10% of cases;

 the average lethal dose (LD50) is the dose that causes death in 50% of cases;

 maximum lethal dose (LD100) - the dose that causes the death of all poisoned animals.

Breadth of therapeutic action - the range between average and maximum therapeutic doses.

To achieve a quick therapeutic effect, drugs are sometimes prescribed in shock doses (antibiotics, sulfonamides). Drugs capable of cumulation are used in maintenance doses. In pediatric practice, drugs are dosed based on the weight or surface of the child's body.

The method of administration of the drug is directly related to its dosage form. So liniment is applied externally, rubbing with a thin layer on the affected area. Tablets are used enterally, and solutions in ampoules are used parenterally.

2. Antipsychotics. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs. The concept of neuroleptanalgesia

Antipsychotics - ggroup of drugs with antipsychotic properties, i.e. the ability to eliminate or suppress the productive symptoms of psychosis in the form of disorders of thinking (delirium), perception (auditory, visual, olfactory hallucinations) and motor activity.

Classification:

BUT. Typical antipsychotics (often cause extrapyramidal disorders)

1.Phenothiazine derivatives: AMINAZINE, TRIFTHAZINE, FLUOROPHENAZINE, ETHAPERAZINE

2. Derivatives of butyrophenone: GALOPERIDOL, DROPERIDOL

3. Derivatives of thioxanthene : CHLORPROTIXENE

B. "Atypical" antipsychotics (do not cause or very rarely cause extrapyramidal disorders)

1. Derivatives of dibenzodiazepine: KLOZAPIN, QUETIAPIN

2. Benzamide derivatives: SULPIRIDE

3. Derivatives of benzisoxazole: RISPERIDON

The main mechanism of action of neuroleptics is blockade of dopamine receptors of the mesolimbic system, this action determines their ability to eliminate delusions, hallucinations, psychomotor agitation... In addition, antipsychotics can block serotonin, histamine, and alpha-adrenergic receptors in the central nervous system....

AMINAZINE has a pronounced effect on the central nervous system, as well as on peripheral innervation, executive organs and metabolism.

AMINAZIN is characterized by antipsychotic and sedative effects, the ability to cause extrapyramidal disorders with prolonged use. In large doses, it pulls out a hypnotic effect. Aminazine causes a decrease in motor activity, inhibits the center of heat regulation, hypotremia is observed, has an antiemetic effect, potentiates the action of neutrotropic drugs (anesthesia, opioid analgesics). Reduces blood pressure.

TRIFTHAZINEcharacterized by more selective than chlorpromazine, antipsychotic effect and less pronounced sedative. Differs in weak hypotensive and muscle relaxant action.

Indications for use - Psychoses of various origins - Acute psychomotor agitation - Vomiting of central genesis - Premedication - Neuroleptanalgesia - Hyperthermia - Severe hypertensive crises (chlorpromazine, droperidol) - Withdrawal syndrome in alcoholism and drug addiction

Side-by-side: - Extrapyramidal Disorders - fromdullness, lethargy, muscle weakness, depression - Hyperprolactinemia, galactorrhea, gynecomastia, amenorrhea, infertility, decreased potency - Increased appetite and body weight - Impaired thermoregulation (hypothermia) - Decreased blood pressure, orthostatic hypotension - Hematopoietic disorders (lekopenia, agranulocytosis, hemolytic anemia - Photosensitization and skin pigmentation

Contraindications: - Cardiovascular disease with decompensation - Pathology of the liver, kidneys (hepatitis, cirrhosis, nephritis) - ddepression - Parkinsonism - Hematopoietic disorders (leukopenia) - Diabetes - Glaucoma - Pregnancy, lactation

Neuroleptanalgesia is a combined method of intravenous general anesthesia, in which the patient is conscious, but does not experience emotions (neurolepsy) and pain (analgesia).