4. Antiblastic substances. Classification. Mechanism of action. Side effects. Contraindications Comparative evaluation of drugs.

Classification:

I. Alkylating agents:

a) derivatives of chloroethylamine (mustard gas) - dopane, sarcolysin;

b) derivatives of ethyleneimine - thiophosphamide, benzotef;

c) derivatives of methanesulfonic acid - mielosan.

II. Antimetabolites:

a) folic acid antagonists - methotrexate;

b) purine antagonists - mercaptopurine;

c) pyrimidine antagonists - fluorouracil.

III. Antineoplastic antibiotics - doxorubicin hydrochloride, dactinomycin.

IV. Herbal antineoplastic agents (alkaloids) - vinblastine, vincristine, colhamin.

V. Enzyme preparations with antitumor activity - L-asparaginase.

Vi. Hormonal drugs and their antagonists - phosphestrol, tamoxifen, prednisolone.

Vii. Interferons, interleukins - aldesleukin.

VIII. Preparations of various chemical groups.

a) Platinum preparations - cystplatin or platidiam, polyplatilen, platinum.

b) Urea derivatives - hydroxyurea, lomustine.

c) Triazenes — dacarbazine or DTIK.

Mechanism of action :

Alkylating: impairment of DNA replication due to cross-linking.

Antimetabolites: suppression of the synthesis of purines and NA

Antineoplastic antibiotics: suppression of nc synthesis and function

Plant-based: blocking mitosis at the metaphase stage

Hormonal drugs: suppression of NK synthesis of hormone-sensitive target cells.

Asparaginase enzymes: impaired protein synthesis due to asparagine deficiency

Indications: cisplastin - ovarian cancer, soft tissue sarcoma, breast cancer

Mercaptopurine - acute leukemia

Methotrexate - acute leukemia, breast cancer, uterine chorionepithelioma

Prospidin - laryngeal cancer

Colhamin - skin cancer

Rosevin - chorionepithelioma of the uterus, reticulosarcoma, lymphogranulomatosis

Vincristine - acute leukemia in children

Asparaginase - lymphosarcoma, acute lymphoblastic leukemia, reticulosarcoma

Adriamycin: acute leukemia, reticulosarcoma, lymphogranulomatosis

Glucocorticoids: lymphogranulomatosis, acute leukemia

Side effects: irritation of the gastrointestinal tract, cardio-, hepato-, nephrotoxic, immunosuppressive, mutagenic, teratogenic effects.

Contraindications: oppression of hematopoiesis, acute infections, liver and kidney disease.

Ticket 39

1. Types of action of medicinal substances.

2. M-anticholinergic drugs. Classification. Mechanism of action. Side effects. Contraindications Comparative evaluation of drugs.

3. Nitrates used for coronary heart disease. Classification. Mechanism of action. Side effects. Contraindications Comparative evaluation of drugs.

4. Differences between chemotherapeutic substances and antiseptics. Basic principles of HT. Criteria for evaluation.

1. Types of action of medicinal substances.

1. Local action - the action of drugs at the site of their application (before absorption into the blood, for example, astringents, local anesthetics).

2. Reflex action - the action that occurs when the drug stimulates the receptors of the afferent link of the reflex.

3. Resorptive action (general) - the action of drugs after their absorption into the blood.

4. Direct action - action directed directly at that organ or system where there are pathological changes and manifested along with the main action.

5. Indirect action (indirect) - the result of direct action, as a result of which the activity of another organ or system is improved.

6. The main (main) action is a manifestation of the pharmacological action of a medicinal substance, which is used in each case for therapeutic or prophylactic purposes.

7. Side effect - the effects of a medicinal substance in a therapeutic dose, which in a particular case are undesirable and are manifested along with the main action.

8. Teratogenic effect (from the Greek. Teras - freak) occurs from the beginning of 4 to 8-10 weeks of pregnancy and is accompanied by the development of anomalies of the internal organs and systems of the fetus, ie. various deformities.

9. Embryotoxic action (from the Greek embryon - embryo). It occurs in the first 3 weeks after fertilization and consists in the negative effect of drugs on the embryo in the lumen of the fallopian tubes or uterus.

10. Fetotoxic effect - the effect of the drug on the fetus at a later time, which does not cause deformity (from the Greek. Fetus - fruit). This is the result of the reaction of a ripening or already mature fetus to drugs, which is practically not much different from the reaction of an adult and can be the cause of severe pathology or even death of the fetus and newborn.

2. M-anticholinergic drugs. Classification. Mechanism of action. Side effects. Contraindications Comparative evaluation of drugs.

-Atropin-stimulates the central nervous system.

-Platifillin-dilates blood vessels.

-Pirenzepine-selectively blocks the receptors of the glands of the stomach, used for peptic ulcer disease.

-Scopolamine is rarely used, as it can cause disorientation and amnesia, depresses the central nervous system.

Mechanism of action: block M-cholinergic receptors, and prevent the interaction of acetylcholine with them. Dilatation of the pupil, increase in IOP, accommodation paralysis, tachycardia, expansion of the bronchi, decrease in peristalsis; bladder, ureters, uterus - decreased smooth muscle tone.

Indications: fundus examination, eye trauma, cholelithiasis, pancreatin, to relax the uterus, motion sickness, poisoning with M-cholinomimetics (atropine)

Side effects: increased IOP, impaired near vision, tachycardia, constipation, dysphagia.

Contraindications:

1.Glaucoma;

2. Heart rate more than 90 beats per minute;

3.Tachyarrhythmias;

4. Intestinal atony;

5.Adenoma of the prostate gland.

Poisoning of children with atropine-containing plants, measures of assistance: gastric lavage, activated charcoal, the use of anticholinesterase drugs - physostigmine, proserin.

3. Nitrates used in coronary heart disease.Classification. Mechanism of action. Side effects. Contraindications Comparative evaluation of drugs.

Classification:

I. NITROGLYCERIN PREPARATIONS:

A. Short-acting:

(The effect develops in 1-3 minutes, lasts 20-30 minutes, is used to stop an attack of angina pectoris.)

-Nitroglycerin - tablets, capsules, alcohol solution.

-Nitromint - aerosol

B. Average duration:

(the effect develops in 30-40 minutes, lasts 4-6 hours)

1. Tablets: sustac. (effect duration 7-8 hours)

2. Capsules: nitromac.

B. Long-acting:

(the effect develops in 1-2 hours, lasts 12-24 hours)

Plasters and transdermal discs: nitroderm.

The formation of addiction and a decrease in efficiency is possible.

II. DINITRATE ISOSORBIDE PREPARATIONS:

A. Average duration:

(the effect develops in 20-30 minutes, lasts 4-6 hours)

1. Tablets: nitrosorbide.

2. Capsules: isosorb.

B. Moderately prolonged:

(the effect develops in 30-40 minutes, lasts 6-8 hours)

1. Tablets: cardiket-retard.

III. ISOSORBIDE MONONITRATE PREPARATIONS:

(the effect develops in 20-30 minutes, lasts 10-12 hours)

Tablets: olicard.

Mechanism of action: expand peripheral veins and arteries - decrease in venous return to the heart and systemic vascular resistance, decrease in pre- and afterload on the heart, decrease in heart function. Expand large coronary vessels, suppression of the central links of coronary reflexes - increased delivery of blood and oxygen to the heart. All of these effects reduce the heart's need for oxygen.

SIDE EFFECTS :

1. Headaches.

2. Hypotension.

3. Reflex tachycardia (combination with alpha, beta-blockers or beta-blockers).

4. Increased intraocular pressure.

CONTRAINDICATIONS:

1. HELL is less than 100/60.

2. Tachycardia.

3. Increased intracranial pressure.

4. Glaucoma (especially open-angle).