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.
Types of action of medicinal substances.
M-anticholinergic drugs. Classification. Mechanism of action. Side effects. Contraindications Comparative evaluation of drugs.
Nitrates used for coronary heart disease. Classification. Mechanism of action. Side effects. Contraindications Comparative evaluation of drugs.
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).
Antiseptic agents are used to affect pathogens on the surface of the human body.
Chemotherapeutic agents are drugs of various chemical groups with antimicrobial and antiviral properties that suppress the vital activity of pathogens in the human body. By retarding the growth or causing the death of pathogens, they should not disrupt the basic functions of the human body (macroorganism).
Chemotherapy drugs must necessarily come into contact with the causative agent of the disease in the patient's body.
Basic principles of chemotherapy
1. Establishing an accurate bacteriological diagnosis, rational choice of a chemotherapeutic drug, determining the sensitivity of a microorganism
2. If it is impossible to carry out appropriate studies - the appointment of drugs with a wide spectrum of action.
3. Early start of treatment.
4. Creation and maintenance in the body of a constant effective concentration of the chemotherapeutic substance
5. To prevent the development of resistant strains of microorganisms, it is recommended to use chemotherapeutic agents in combination
6. Correct determination of the duration of treatment.
7. Along with the appointment of chemotherapeutic agents, measures should be taken to enhance the defenses of the macroorganism
Evaluation criteria - high activity, pronounced selectivity of action, antimicrobial spectrum, bactericidal nature of action, permeability through biological membranes (BBB), effectiveness in different biological media, development of resistance in microbes, sensitization of a macroorganism, absence of side effects, minimal toxicity, breadth of therapeutic action, as well as technical availability of manufacturing, low cost.
1. Conditions affecting the manifestation of the action of medicinal substances in the body. The importance of the psychogenic factor in the effectiveness of drug treatment; the word of the doctor and the prescription of drugs. The ethical side of the advertising of new drugs.
Age - there is perinatal pharmacology (from 24 weeks of the fetus to 4 weeks of newborn), newborns differ from adults (deficiency of enzymes, kidney function, ↑ BBB permeability, underdevelopment of the central nervous system). There is pediatric pharmacology - doses per kg of body weight. There is geriatric pharmacology - in people of age, the doses should be ↓ (since ↓ absorption, metabolism, excretion by the kidneys).
Gender - men are less sensitive to a number of substances than women (strychnine, nicotine).
Genetic factors - enzyme deficiency, atypical reactions (idiosyncrasy). Studying pharmacogenetics.
The state of the body - pharmacokinetics changes with illness, pregnancy, obesity.
Circadian rhythms (circadian) - studies chronopharmacology. The effect of substances changes qualitatively and quantitatively (pronounced effect during the period of maximum activity). Absorption, metabolism change during the day.
Psychogenic factor - if the patient is committed to treatment, trusts the doctor, follows the recommendations, the treatment will be effective. Otherwise, the effect of the treatment cannot be expected.
The word of the doctor is the therapeutic effect of the word of the doctor on the patient.
Ethics:
Ethical issues of drug advertising are relevant due to the following factors in the modern market:
low awareness of consumers about the features of medical products or services. Over-the-counter drugs put significantly more people in danger each year than all illicit drugs put together; conflicting conditions of competition in the pharmaceutical market, imperfection of legislative and regulatory acts that do not take into account all the nuances of a modern market economy (for example, experts point out that some parts of federal laws allow advertising of medicines, but with some restrictions, while other parts prohibit this advertising everywhere);
increased influence of suppliers on consumers by use in the pharmaceutical market, imperfection of legislative and regulatory acts that do not take into account all the nuances of a modern market economy (for example, experts point out that some parts of federal laws allow advertising of medicines, but with some restrictions, and other parts prohibit this advertisement everywhere);
increasing the influence of suppliers on consumers using new methods of pressure: forced distribution, imposing and incorrect anamnesis on the part of doctors involved in drug promotion, - leads to a significant complication of drug promotion among honest manufacturers and healthy competition.
2. Tranquilizers. Classification. Mechanism of action. Indications. Side effects. Contraindications Comparative assessment of drugs Possibility of developing dependence. The concept of "Daytime" tranquilizers.
Tranquilizers are substances that have a depressing effect mainly on the central nervous system. Eliminate negative emotional reactions (feelings of fear, anxiety).
Classification:
a) Benzodiazepine derivatives (benzodiazepines)
1.Closepide 9.Estazolm
2.Sibazone 10.Clorazepate
3.Phenazepam 11.Klobazam
4.Nosepam 12.Alprozolam
5.Lorazepam 13.Tetrazepam
6.Bromazepam 14.Tofisopam
7. Mezapam
8.Hidazepam
b) Carbamine ethers of substituted
propanediol
1.Meprotan
c) Diphenylmethane derivatives
1.Amisil 2.Hydroxyzine
d) Tranquilizers of different chemical groups
1.Buspirone 3.Mebikar
2.Oxidiline
Mechanism of action: for benzodiazepines - they inhibit the anxiety zone in the hypothalamus, impulses stop, inhibit the limbic system and reticular pharmacy. Characterized by a sedative effect, a decrease in skeletal muscle tone, a hypnotic effect, a decrease in aggressiveness, an anticonvulsant.
Indications: situational anxiety states, borderline states, insomnia, skeletal muscle spasms, relief of status epilepticus, premedication, ataralgesia.
Side effects: allergies, drowsiness, dizziness, uneven gait.
Contraindications: acute liver and kidney disease, myasthenia gravis, pregnancy, not for drivers.
Buspirone - a pronounced anxiolytic effect, no sedative, anticonvulsant, relaxing effect, no addiction.
Phenazepam is more active than diazepam in terms of anxiolytic and hypnotic action.
Dependence - with prolonged use of benzodiazepines, mental and physical drug dependence.
"Daytime" tranquilizers - mezapam, pronounced anxiolytic effect and no sedative-hypnotic effect.