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Ticket 36

1) The founder of Russian pharmacology N.P. Kravkov. The main directions of the school of N.P. Kravkov.

2) Local anesthetic substances. Classification. Mechanism of action. Indications for use. Contraindications Comparative evaluation of drugs.

3) Anti-atherosclerotic drugs. Classification, Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation

4) Antimalarial drugs. Classification. Mechanism of action, indications for use. Contraindications Side Effects Comparative assessment of preparations.

1) The founder of Russian pharmacology N.P. Kravkov. The main directions of the school of N.P. Kravkov.Nikolay Pavlovich Kravkov (1865-1924) - pharmacologist, founder of Russian pharmacology, headed the Department of Pharmacology at the St. Petersburg Military Medical Academy.

Kravkov was the first to study the effect of pharmacological substances on isolated organs. He studied the problems of general pharmacology: the dependence of the biological effect on dose and concentration, the combined effect of drugs, the relationship between the structure of compounds and their physiological activity, studied the pharmacodynamics and pharmacokinetics of substances against the background of diseases. He also worked on toxicology (gasolines, BOV), offered a drug for intravenous anesthesia (hedonal), combined anesthesia. Wrote the manual "Fundamentals of Pharmacology".

Among other things, the outstanding scientist N.P. Kravkov founded the national school of pharmacologists (S.V. Anichkov, V.V. Zakusov, etc.). The main directions of the scientific school of N.P. Kravkov are the study of life processes, the search for new medicinal substances, means of symptomatic and pathogenetic therapy.

2. Local anesthetic substances. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Local anesthetics - drugs that reversibly inhibit the excitation of afferent nerve endings, as well as the generation and conduction of nerve impulses along the fibers with the loss of all types of sensitivity.

Mechanism of action: they block voltage-gated sodium channels, prevent both the emergence of an action potential and its conduction.

Classification of local anesthetics

Aromatic acid esters

Aromatic amine amides

[Cocaine]

Lidocaine

Procaine (novocaine)

Trimecaine

Tetracaine (dicain)

Articaine (ultracaine)

Benzocaine (anesthesin)

Bupivacaine (marcaine)

Oxybuprocaine (inocaine)

Ropivacaine (Naropine)

Indications for the use of local anesthetics:

1. Infiltration anesthesia. Apply 0.25-0.5% solutions of procaine, 0.125-0.5% solutions of lidocaine, 0.125-0.25% solutions of bupivacaine. The duration of procaine anesthesia usually does not exceed 20-30 minutes, lidocaine - up to 1 hour, bupivacaine - more than 2 hours.

2. Conductive anesthesia. Use 1-2% solutions of procaine, lidocaine, articaine and 0.25-0.5% solutions of bupivacaine and ropivacaine. When repositioning dislocations, reposition of bone fragments, blockade of the trigeminal nerve, brachial, sacral plexuses.

3. Spinal anesthesia (subdural). It is more often produced with a 2-5% solution of lidocaine, sometimes with a 0.25-0.5% solution of bupivacaine or ropivacaine. In the absence of these drugs, procaine (5% solution) can be used. When carrying out lower-thoracic, urological operations.

4. Terminal anesthesia of the mucous membranes is achieved by using solutions of tetracaine (rarely), lidocaine or trimecaine (with the addition of epinephrine, preferably just before anesthesia).

5. Epidural anesthesia for abdominal operations, in obstetric and gynecological practice, in the postoperative period.

6. Lidocaine, trimecaine with ventricular extrasystole and tachycardia, especially with MI, prevention of ventricular fibrillation.

Comparative evaluation: by duration: long-term - anesthesin, pyromecaine, lidocaine, bupivacaine;

short-acting - cocaine, novocaine, dicaine; toxicity: the most toxic dicain, less toxic - novocaine, mepivacaine, pyromecaine.

Contraindications: hypersensitivity to drugs, decompensated heart failure, severe organic lesions of the central nervous system, septicemia.

Side effects:

  1. drowsiness, lethargy, dizziness, impaired consciousness, thermor, convulsions;

  2. tachycardia, bradycardia, decreased A, arrhythmias, collapse;

  3. blurred vision, diplopia;

  4. allergic reactions;

  5. respiratory depression.

3) Anti-atherosclerotic drugs. Classification, Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation.

1. Lipid-lowering drugs

A. Drugs that lower blood levels predominantly of cholesterol

a) inhibitors of cholesterol synthesis LOVASTATIN MEVASTATIN SIMVASTATIN

b) Inhibitors of absorption of cholesterol from the intestine EZETIMIB

c) drugs that increase the excretion of bile acids and cholesterol from the body CHOLESTYRAMINE COLESTIPOL

d) different drugs PROBUKOL

B. Drugs that lower blood levels of mainly triglycerides

a) derivatives of fibric acid GEMFIBROSIL FENOFIBRATE CLOFIBRATE

B. Drugs that lower blood cholesterol and triglycerides

NICOTINIC ACID

2. Endotheliotropic drugs

a) antioxidants PARMIDINE TOCOPHEROL ASCORBIC ACID

b) antiplatelet agents NICOTINIC ACID DIPIRIDAMOL PARMIDINE

3. Lipotropic drugs

LIPOCAINE. LIPAMIDE ESSENTIALE

Cholesterol synthesizer inhibitors - statins. The mechanism of action of statins is related to their ability to suppress the enzyme responsible for the formation of mevalonic acid, which is a precursor of cholesterol. In addition to the lipid-lowering effect, statins inhibit the development of smooth muscle cells - they prevent the formation of atherosclerotic plaques. Patients receiving statins should be regularly tested for hepatic transaminase activity. Indications for taking statins - acute or chronic exacerbations of liver disease MEDOSTATIN

Indications

- primary hypercholesterolemia

-increased blood cholesterol

-

Side effects

- taste disturbance, dry mouth, nausea, diarrhea, constipation

- headache, sleep disturbances, convulsions

- hemolytic anemia, leukopenia

Contraindications

- surge arrester

-pregnancy

Lactation

-increased sensitivity

NICOTINIC ACID - under its influence, the ratio of cholesterol / phospholipids in LDL decreases, while the content of cholesterol and phospholipids in LDL increases

Indications

- for all GLP except the first type

Side effects

- redness of the face, a feeling of rush of blood to the head

- nausea, vomiting, diarrhea

- attacks of angina pectoris

Contraindications

-intolerance

-stomach ulcer

-good

-sd

4) Antimalarial drugs. Classification. Mechanism of action, indications for use. Contraindications Side Effects Comparative assessment of preparations. Classification of antimalarial drugs by chemical affiliation of drugs

P / p #

Group

chemical compounds

A drug

one.

4-methanolquinoline derivatives

quinine, mefloquine

2.

7-chloroquinolines

hingamin (delagil)

3.

4-Aminoquinolines

chloroquine, amodiaquine

four.

Acridines

akrikhin,

aminoacriquine,

five.

8-Aminoquinolines

primaquine,

quinocide

6.

Biguanides

bigumal

7.

Diaminopyrimidines

chloridine,

trimethoprim

eight.

Sulfonamides

sulfapyridazine, sulfamethoxin, sulfalene,

sulfadimethoxine

nine.

Tetracyclines

tetracycline,

doxycycline

10.

Combined drugs

fancidar

Classification of antimalarial drugs according to the spectrum of antimalarial action

Spectrum of action

Drugs

1. Blood schizocytic drugs (destroy asexual forms of plasmodia in the stage of schizogony in erythrocytes)

Quinine, Akrikhin,

hingamin, chloridine,

fancidar

2. Primary tissue schizontocytic agents (affect the pre-erythrocytic tissue forms of plasmodia)

Bigumal, chloridin,

fancidar

3. Secondary tissue schizontocytic agents (destroy para-erythrocytic tissue forms of plasmodia)

Chloridine, primaquine,

hinocid, fancidar

4. Gametocidal agents (inhibit the development of gametes)

Quinocid, primaquine,

chloridine, fancidar

5. Sporontocidal agents (block the sexual development cycle of gametes in the body of a mosquito)

Bigumal, chloridin,

fancidar

By the mechanism of action of group 2: Group 1 includes antimalarial drugs with a strong schizontocidal effect. The mechanism of action of these drugs is not specific. They disrupt the properties of both microbial DNA and human cells. This group includes acriquine, chloroquine, primaquine and quinine.

The drugs of the second group are characterized by schizontocidal action, which occurs rather slowly. Resistance to them develops easily both in experiment and in practice. Their mechanism of action is specific. They competitively displace para-aminobenzoic acid (PABA) from the enzyme systems of the microbial cell, but they cannot perform the function of this metabolite. The drugs either interfere with the conversion of PABA to folic acid, or block dihydrofolic reductase. They have no effect on the cells of the macroorganism. This group includes bigumal, chloridine and their derivatives, as well as sulfonamides.