Indirect anticoagulants - all have a common mechanism. They have a structural similarity to vitamin K. They interfere with the metabolism and disrupt the synthesis in the liver of prothrombin, proconvertin, factors 9 and 10. The latent period is 24-72 hours, after cancellation the action lasts 2-5 days. Indications: thrombophlebitis, thrombosis, heart attack, ischemic heart disease. Cannot be used for endocarditis, peptic ulcer disease, pregnancy. Side effects - hemorrhages, cumulation.
four. Antibiotics of the group of Lincosamides and Glycopeptides. Classification. Mechanisms of action. The nature of the action. Spectrum of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.
Classification: lincosamides - lincomycin, clindamycin; glycopeptides - vancomycin.
Mechanism: lincosamides inhibit protein synthesis and ribosome function, glycopeptides disrupt cell wall synthesis.
Mode of action: lincosamides - bacteriostatic, glycopeptides - bactericidal.
Spectrum of action: anaerobes, streptococci, staphylococci.
Indications: for bacteroid infections, diphtheria.
Side effects: allergies, liver damage, leukopenia, lincosamides - pseudomembranous colitis.
Contraindications: pregnancy, liver disease, kidney disease.
Clindamycin is stronger than lincomycin, it does not penetrate the BBB. Vancomycin - penetrates the BBB, is toxic (nephro, oto). Lincomycin - accumulates in bone tissue, most effective in the treatment of bone diseases.
one. Basic principles of action of medicinal substances. Their interactions with recipes.
Local - d-e at the site of application (enveloping, surface anesthetics). Resorptive - e after absorption, entering the blood and tissues, depends on the routes of administration, the way to penetrate the barriers. Direct e - at the place of direct contact of the in-va with the tissue. Reflex d-e - influence on extero- and interoreceptors, the effect was manifested by changing the state of the nerve / centers or executing organs (mustard plasters, lobelin - a breathing stimulator).
Receptors, ion channels, enzymes, transport systems (proteins), and genes serve as targets for drugs. Receptors are active groups of substrate macromolecules, with which the substance interacts. Specific receptors provide the manifestation of e-I in-islands (adenosine, adreno-, angiotensin, bradykinin, histamine, dopamine, choline). The affinity of the substance to the receptor, leading to the image of a complex with it, is affinity. The way to stimulate the receptor and cause the effect is internal activity. Agonists are active internally (full agonist - maximal effect). Antagonists - when interacting with receptors, they do not stimulate them (there is no internal activity). There are receptors that bind to cats and do not cause any effects - nonspecific receptors.
Depending on the strength of the "in-in - receptor" bond, reversible and irreversible d-e are distinguished. Selects d-e - in-in interacts only with definite receptors and does not affect others. Intermediates that bind the receptor to the effector are G-proteins, enzymes (cyclases, phospholipases), secondary transmitters (cAMP, Ca ++).
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:
1) 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.
1.Anti-inflammatory drugs:
A. Non-hormonal drugs:
1) Mast cell membrane stabilizers - inhibit the release of histamine.
-Intal
-KETOTYPHENE
2) Leukotriene receptor blockers:
-CINALUKAST
3) Antihistamines - block H1-histamine receptors and reduce bronchospasm, capillary permeability.
-Erius
B. Glucocorticoids:
-DEXAMETHAZONE
-HYDROCORTISON
2.Bronchodilator:
1) Stimulants of adrenergic receptors:
Beta 2-adrenergic agonists: salbutamol.
Beta 1, beta 2 - adrenergic agonists: izadrin.
2) Blockers of M-cholinergic receptors:
-ATROPINE
-METACIN
3) Methylxanthines (myotropic antispasmodics) - inhibit the transport of Ca ions through the slow channels of cell membranes, inhibit the degranulation of mast cells and the release of inflammatory mediators;
-THEOPHILLINE
-EUFILLIN
Side effects: allergies, tachycardia, dry mouth, tremors.
Contraindications: atropine-glaucoma, izadrin-heart disease, bleeding,
Izadrin - can cause tachycardia.
Salbutamol - does not cause tachycardia, does not change blood pressure.
four. Differences between chemotherapeutic agents and antiseptics. Basic principles of chemotherapy. Criteria for evaluating the chemotherapeutic activity of drugs.
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.
Pharmacology is the science of the interaction of chemical compounds with living organisms. Pharmacon (Greek) - medicine (poison). Logos (Greek) - word, doctrine.
PURPOSE pharmacology is the search for means for the treatment, prevention and diagnosis of diseases. TASKSis the creation of new highly effective and safe drugs based on chemical synthesis products and raw materials of natural origin. Pharmacology studies the effect of drugs on biological systems (from the whole organism to individual cells, receptors and enzymes). As a biomedical science, pharmacology is also associated with experimental and practical medicine. Pharmacology influences the development of physiology and biochemistry (for example, many complex functions of the central nervous system have become available for study thanks to neutrotropic agents). Pharmacology is also important for practical medicine (as a result of the creation of highly effective drugs, pharmacotherapy has become a universal method of treating many diseases). Pharmacology plays an important role in the development of clinical disciplines (the emergence of drugs for anesthesia,
The experiment on animals was introduced in 19 and is an integral part of preclinical studies of drugs, since this allows you to determine the therapeutic efficacy of the drug, its effect on the main anatomical and physiological systems of the body. In the process of studying the pharmacodynamics of a substance, not only its specific activity is established, but also possible side reactions associated with pharmacological activity. In addition, the specific toxicity of the drug is established - oncogenicity, mutagenicity, embryotoxicity, including teratogenic effects.
2. Ethyl alcohol. Antimicrobial effect of alcohol, effect on the central nervous system, skin and mucous membranes, on digestion. Acute and chronic alcohol poisoning. Poisoning treatment.
Ethyl alcohol is a typical substance of a narcotic type of action. It has a depressing effect on the central nervous system, when applied topically, it is an antiseptic (70% alcohol - denaturation of microbial cell proteins). Also, 70% ethyl alcohol solution is used to treat the operating table and the surgeon's hands, 95% - for the treatment of suture material and instruments. It irritates tissues (40%) and therefore can be used as compresses. When taken orally, alcohol has an irritating agent on the CO of the oral cavity, stomach, and enhances the secretion of their glands. In high concentrations (90%) - drying and tanning effect.
Manifestation of central action:
- with a resorptive action, alcohol inhibits the central nervous system (like anesthetics) and in this case, 4 stages are distinguished in the action of alcohol: analgesia, agitation, anesthesia, paralysis)
- increases heat transfer, affecting thermoregulation (vasodilatation by suppressing the vasomotor center)
- a diuretic effect (the production of ADH by the posterior lobe of the pituitary gland decreases)
- enhances the secretory activity of the salivary glands
- 10% or less% alcohol is used to increase appetite and stimulate juice production
- 20% alcohol inhibits the secretion of hydrochloric acid and the digestive activity of gastric juice, resulting in a lot of mucus
- spasm of the pylorus and decreased gastric motility at high alcohol levels (70%)
Acute alcohol poisoning... A person poisoned with alcohol is unconscious, the skin is pale, breathing is rare, the pulse is frequent, the body temperature is low. The severity of poisoning depends on the dose of alcohol and its concentration.
Chronic poisoning. A symptom of aclogolism is a painful need to get drunk. A person develops the phenomena of unstable mood, irritability, sleep and digestive disorders. Decreases memory, mental and physical performance. Later - psychosis, neuritis, chronic gastritis, cirrhosis of the liver.
Poisoning treatment. Teturam is used - it delays the oxidation of alcohol at the acetaldehyde stage, this causes intoxication, a feeling of fear, nausea. As a result, a person develops negative reflexes to alcohol.
3. Means that reduce the tone and contractile activity of the myometrium. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.
The contractile activity and tone of the myometrium are regulated by neurohumoral mechanisms. In the myometrium there are m-cholinergic receptors, alpha and beta2-adrenergic receptors. Stimulation of m-cholino and alpha-adreno is a stimulating effect, and beta 2-adreno is a depressing one.
Drugs that weaken the contractile activity of the myometrium (tocolytic drugs)
Substances stimulating beta2-adrenergic receptors: PHENOTHEROL, SALBUTAMOL
Medication for anesthesia: SODIUM OXIBUTIRATE
Miscellaneous: MAGNESIUM SULFATE
PHENOTHEROL are prescribed to delay premature labor, with the threat of termination of pregnancy due to increased tone of the uterus and with violent labor. Fenoterol does not have a selective effect, therefore, when beta2-adrenergic receptors are stimulated, it not only relaxes the myometrium, but can also stimulate other organs. When administered enterally, fenoterol acts faster, but for a short time than salbutamol. Side effects include maternal and fetal tachycardia, fetal hyperglycemia
SODIUM OXIBUTIRATEused to weaken excessively strong labor pains. A side effect is hypokalemia and seizures.
MAGNESIUM SULPHATE violates the penetration of calcium ions into the cells of the myometrium, which are necessary for contractions.
4. Antibiotics from the group of macrolides and aminoglycosides. Classification. Mechanism of action. The nature of the action. Spectrum of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.
Macrolides are low-toxic agents for oral administration for infections caused by G + bacteria and intracellular microorganisms. There are 3 generations of macrolides:
Erythromycin, oleandomycin
Spiramycin, dirithromycin
Azithromycin (sumamed)
Mechanism of action of AB - inhibit microbial cell protein synthesis
Origin classification:
Natural - erythromycin, oleandomycin, spiromycin
Prodrugs - oleandomycin-troleandromycin esters
Semi-synthetic - azithromycin
Macrolides, depending on the type of microorganism and dose, can have a bracteriostatic or bactericidal effect. Spectrum of action: staphylococcus, streptococcus, pneumococcus, meningococcus, gonococcus, corynebacterium diphtheria, clostridium gas gangrene
Macrolides are prescribed orally and some intravenously (erythromycin).
Macrolides:
- have a mucoregulatory effect
- weaken the inflammatory reaction as a result of inhibition of the synthesis of PG, LTE and IL
- about immunomodulatory properties
Indications for use: - infections of the upper and lower respiratory tract - whooping cough and its prevention - diphtheria - infections of the skin and soft tissues - other functions of the oral cavity - trachoma - sexually transmitted infections |
Side-by-side: - nausea, vomiting - cramping abdominal pain - fever - jaundice - with i / v - thrombophlebitis, Hearing impairment |
Contraindications: - hypersensitivity - pregnancy - breast-feeding |