Contraindications: Kanamycin is contraindicated in inflammation of the auditory nerve, impaired liver and kidney function (with the exception of tuberculous lesions).
Individual intolerance to the drug.
Epilepsy.
Severe psychosis.
Tendency to seizures.
History of poliomyelitis.
History of toxic hepatitis due to taking GINK drugs.
Acute hepatic and renal failure.
An absolute contraindication to the appointment of streptomycin is the lack of sensitivity of Koch's bacilli to it.
Side effect:Dizziness, discomfort in the region of the heart, tinnitus, headache (often due to a decrease in blood pressure, mainly systolic). Anaphylactic shock, vestibular disorders, hearing loss, deafness, drug fever, skin rash, contact dermatitis, muscle weakness and joint pain, dizziness, tinnitus, palpitations and pain in the region of the heart. In severe cases, paresthesias, insomnia, memory loss, muscle twitching, polyneuritis, ataxia, convulsions occur (due to the developing deficiency of pyridoxine and thiamine chloride). Changes in blood are possible: agranulocytosis, eosinophilia. Convulsive states, lesions of the optic nerve and polyneuritis are also possible. Endocrine system disorders: gynecomastia in men, dysmenorrhea in women, "cushingoid", hyperglycemia.
1) Types of drug therapy. The dependence of the action of pharmacological agents on the initial state of the organism (the influence of age, sex, genetic factors, circadian rhythms and pathological background).
Types of drug therapy include:
Etiotropic - when drug treatment is aimed at correcting or eliminating the cause of the disease (antibiotics for pneumonia);
Pathogenetic - when the mechanism of development of the disease is influenced (the effect of diuretics + ACE inhibitors + calcium antagonists in arterial hypertension);
Symptomatic - when it is not possible to influence the cause or pathogenesis of the disease (temperature lowering agents for infectious diseases, narcotic drugs for myocardial infarction);
· Substitutional - when there is a deficiency of natural biologically active substances and there is a need for their appointment (insulin in diabetes mellitus);
Prophylactic - when the drug is prescribed to prevent the onset of a disease (aspirin to prevent myocardial infarction or stroke in elderly patients with atherosclerosis).
a) from age: in children and the elderly, sensitivity to drugs is increased (since children have a deficiency of many enzymes, renal function, increased BBB permeability, in old age, drug absorption is slowed down, metabolism is less efficient, the rate of excretion of drugs by the kidneys is reduced )
b) from the floor:
1) antihypertensive drugs - clonidine, b-blockers, diuretics can cause sexual dysfunction in men, but do not affect the functioning of the reproductive system of women.
2) anabolic steroids are more effective in women than in men.
c) from the individual characteristics of the organism: a deficiency or excess of certain enzymes of drug metabolism leads to an increase or decrease in their action (deficiency of blood pseudocholinesterase - abnormally prolonged muscle relaxation when using succinylcholine)
d) from daily rhythms: a change in the effect of drugs on the body, quantitatively and qualitatively, depending on the time of day (maximum effect with maximum activity)
C) GENETIC FACTORS
Drug susceptibility can be genetically determined. This manifests itself both quantitatively and qualitatively. For example, with genetic deficiency of blood plasma cholinesterase, the duration of action of the muscle relaxant ditilin increases sharply and can reach 6-8 hours or more (under normal conditions, ditilin acts for 5-7 minutes).
It is known that the acetylation rate of the anti-tuberculosis drug isoniazid varies widely. Individuals with fast and slow metabolizing activity are distinguished. It is believed that people with slow inactivation of isoniazid have a deficiency in genes that regulate the synthesis of an enzyme that provides acetylation of this drug.
E) VALUE OF DAILY RHYTHMS
Circadian rhythms2 are essential for physiological functions. It is well known that the alternation of wakefulness and sleep has a significant effect on the activity of the nervous system and endocrine glands and, accordingly, on the state of other organs and systems. In turn, this affects the body's sensitivity to various substances. The study of the dependence of the pharmacological effect on the daily periodism is one of the main tasks of the new direction, called chronopharmacology.
2. Anticholinesterase drugs. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs. Cholinesterase reactivators. FOS poisoning, assistance measures.
Anticholinesterase drugs- indirect cholinomimetics. These substances do not act on cholinergic receptors, but block the enzyme acetylcholinesterase, as a result of which acetylcholine is less destroyed, accumulates and stimulates cholinergic receptors.
Mechanism of action:Anticholinesterase agents inhibit acetylcholinesterase, an enzyme that hydrolyzes acetylcholine in the synaptic cleft and blood plasma cholinesterase (butyrylcholinesterase, pseudocholinesterase, pseudocholinesterase). Inhibition of acetylcholinesterase in cholinergic synapses leads to an increase in the concentration of acetylcholine in the synaptic cleft, as a result of which the action of acetylcholine is significantly enhanced and lengthened. Thus, all the effects of anticholinesterase drugs are due to endogenous acetylcholine.
Classification: Reversible cholinesterase blockers
Tertiary amines: Physostigmine is an alkaloid of Calabar beans. Galantamine (nivalin) is an alkaloid of Voronov's snowdrops tubers.
Amiridine is a synthetic derivative of quinoline (it blocks potassium channels).
Tacrine is a synthetic derivative of acridine.
Quaternary amines:
Neostigmine is a simplified analogue of physostigmine.
Pyridostigmine bromide (Kalimin) is a proserin derivative with a longer lasting effect.
D ystigmina
bromide (ubretide) symmetric bisammonium compounds, according to
Oksazil
Quinotilin activities are superior to proserin.
Irreversible action: Phosphacol, Armin, FOS (phosphorus-organic compounds).
Indications: Glaucoma (increased IOP) using eye drops or ointments
• Atony of the gastrointestinal tract, biliary, urinary tract,
uterus;
• Myasthenia gravis;
• Paresis, paralysis after suffering strokes, brain trauma, neuroinfections, neurosurgical interventions;
• To eliminate the effects of antidepolarizing muscle relaxants;
• Alzheimer's disease (TACRIN, RIVASTIGMINE);
• In case of poisoning with M-anticholinergics, as physiological antagonists.
Side effects: Involuntary twitching of small muscle groups (face, neck, tongue);
Increased irritability, tremors, insomnia;
• Visual impairment in the distance;
• Decreased AV conduction, bradycardia;
• Bronchospasm, bronchorrhea;
• Increased sweating;
• Hypersalivation;
• Spasm of the stomach, intestines, biliary tract;
• Spasms of the urinary tract;
• Strengthening of intestinal motility, diarrhea;
• Increased tone of the uterus;
Contraindications: • Epilepsy
• insomnia
• Heart rate <60 beats per minute, AV blockade
• Myocardial infarction with impaired conduction
• Bronchial asthma
• Peptic ulcer, hyperacid forms of gastritis
• Spasms of the gastrointestinal tract
• Cholelithiasis
• Urolithiasis disease
• Any acute inflammatory processes in the abdominal cavity
• Pregnancy (may cause miscarriage)
Comparative evaluation of drugs: Preparations from the group of tertiary amines are well absorbed from the gastrointestinal tract and penetrate well through the BBB, providing both peripheral and central effects
• Drugs from the group of quaternary amines are less absorbed from the gastrointestinal tract and poorly penetrate the BBB, providing mainly peripheral effects
• FOS do not have an ammonium structure, penetrate well through the BBB
Cholinesterase reactivators: Dipiroxime and isonitrazine. They interact with the residues of FOS associated with acetylcholinesterase, releasing the enzyme and restoring its physiological activity.
FOS poisoning, first aid:
Life-threatening symptoms:
• Severe bradycardia up to cardiac arrest
• Bronchospasm and bronchorrhea, impaired respiratory function
• Convulsions
Specific assistance measures:
• In case of an overdose of reversible drugs, a physiological antagonist is used - the M-anticholinergic antagonist ATROPIN
• In case of an overdose of irreversible drugs (including FOS), use the M-anticholinergic blocker ATROPIN + chemical antagonists (antidotes) - cholinesterase reactivators (DIPYROXIM, IZONITROSIN). Preference is given to ISONITROSINE, because it penetrates well into the central nervous system.
3) Drugs that stimulate erythropoiesis. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.
Classification:
1. Used for hypochromic anemia
a) With iron deficiency anemia
1) Iron preparations:
Iron ferrous sulfate
Iron ferrous lactate
Feramide
Indications: - with IDA (with chronic bleeding, impaired absorption of iron, with
pregnancy)
Side effects: - constipation (due to the binding of hydrogen sulfide in the intestine, which is physiological
stimulant of his motor skills)
If the absorption of iron in the intestine is impaired, then parenteral drugs are prescribed:
Ferrum Lek; Ferkoven
Side effects: - in case of an overdose of Ferkoven - hyperemia of the skin of the face, neck, back pain, sensation
compression in the chest area
- Preparations of cobalt-Coamid: promotes the absorption of iron and its inclusion in metabolic processes. Stimulates the production of erythropoietin and thus activates erythropoiesis. Increases the synthesis of amino acids, the activity of succinate dehydrogenase, cytochrome oxidase, increases the content of DNA and RNA in tissues.
b) With anemia arising from chronic diseases
Human recombinant erythropoietin in drugs
Epoetin Alfa, Epoetin Beta
- erythropoietin itself is a growth factor that regulates erythropoiesis
- stimulate proliferation and differentiation of red blood cells
Indications: - anemia associated with chronic kidney failure, with rheumatoid arthritis,
malignant tumors, AIDS with anemia in premature babies
Side effects: - headache, arthralgia; - hyperkalemia; - skin rash
2. Used for hyperchromic anemia
1) Cyanocobalamin (vitamin B12)
- normalizes the blood picture in case of mischief. anemia
- eliminates or weakens neurological disorders and mucosal lesions
language
Indications: - malignant (pernicious, megaloblastic) anemia (it is associated with impaired absorption of cyanocobalamin, since such patients lack Castle's intrinsic factor.)
2) Folic acid (vitamin Vs) - normalizes the blood picture in case of malignant anemia, but only in combination with Cyanocobalamin, as it can enhance changes in the nervous system
Indications: - macrocytic anemia (with a deficiency of folic acid, macrocytes are formed)
- sprue (this is a chronic disease manifested by diarrhea, glossitis, anemia, general exhaustion and hypofunction of the endocrine glands); - anemia of pregnant women
Contraindications: gastric ulcer and 12 duodenal ulcer, gastritis and enteritis, hemolytic anemia, hemosiderosis.
four). Classification of antibiotics.
1.By chemical structure:
● b-lactam (penicillins, cephalosporins, carbapenems, monobactams)
● Macrolides and azalides
● Aminoglycosides
● Tetracyclines
● Lincosamides
● Glycopeptides
● Amphenicol
● Polymyxins
● Phosphonates
● Polyenes
● Rifamycins
2. By the nature of the action on the bacterial cell:
–Bactericidal (causing the death of bacteria)
–Bacteriostatic (stopping the growth and division of bacteria)
3. By the mechanism of action:
–Disorders of cell wall synthesis
- Violating the permeability of the cytoplasmic membrane
–Disorders of protein synthesis on ribosomes
–Disorders of RNA synthesis
4. According to the spectrum of antimicrobial action:
–Preparations of a wide spectrum of action
–Preparations with a predominant effect on Gr (+) flora
–Preparations with a predominant effect on Gr (-) flora
–Antifungal antibiotics
5. For clinical use:
–Basic antibiotics (drugs of choice)
–Reserved antibiotics (alternative)
6. By sources of receipt:
–Natural (biosynthetic)
- semi-synthetic