- early start of treatment.
- creation and maintenance of a constant effective concentration of the antimicrobial drug in the body.
- it is desirable to use antimicrobial agents in combination (preventing the development of resistance).
- correct determination of the duration of treatment.
- in the complex of treatment, use means that increase the body's resistance (vitamins, serums).
Nitrofurans
Furadonin, Furagin, Furazolidone, Furacilin,
Nifuroxazide (enterofuril), Nifuratel (makmiror)
The nature of the action - bactericidal
Mechanism of action - violation of protein synthesis
Spectrum of activity - wide
Gr (+) cocci: streptococci, staphylococci (except MRSA),
enterococci are insensitive
Gr (-) coli: E. coli, salmonella, shigella, klebsiella, enterobacteria
The simplest: lamblia, Trichomonas (furazolidone, nifurantel), amoeba (nifurantel)
Resistant anaerobes, Pseudomonas aeruginosa, Proteus, Serrata, acinetobacters
Nitrofuran resistance is rare.
Furadonin and furagin create high concentrations in the urine, while the antimicrobial activity increases with an acidic reaction of urine and weakened - with an alkaline
• Acute cystitis, prevention of exacerbations in chronic pyelonephritis, prevention of infectious complications in urology (operations, cystoscopy, catheterization)
NB! In acute pyelonephritis, they are not used, because poorly penetrate the kidney tissue
Nifuroxazide (Enterofuril)used for intestinal infections (acute infectious diarrhea, enterocolitis). Practically not absorbed in the digestive tract. Does not disturb the normal intestinal microflora
Furazolidoneis currently used only for giardiasis as a reserve drug. NB! In combination with alcohol, it can cause a teturam-like reaction. Inhibits MAO, therefore, in combination with other MAO inhibitors, sympathomimetics, tricyclic antidepressants and tyramine-containing foods, there is a risk of developing a hypertensive crisis
Nifuratel (makmiror) used for intestinal infections (acute infectious diarrhea, enterocolitis), giardiasis, intestinal amebiasis, trichomonas vulvovaginitis
Furacilin is used as an antiseptic for treating wounds, skin, mucous membranes, for washing serous and articular cavities
Side effects
Hepatotoxicity: cholestasis, jaundice, hepatitis
Hematotoxicity: hemolytic anemia (with a deficiency of glucose-6-phosphate dehydrogenase in erythrocytes), leukopenia, agranulocytosis, thrombocytopenia
Neurotoxicity: dizziness, nystagmus, intracranial hypertension, paresthesia
Gastrointestinal tract: nausea, vomiting (taken with or after meals)
Allergic reactions
Pulmonary reactions (furadonin): bronchospasm, pulmonary edema, pulmonary fibrosis
Teturam-like effect (furazolidone)
Tyramine syndrome (furazolidone)
one). Changes in the body's reactions to medicinal substances during their repeated administration. Concepts of addiction, drug dependence, tachyphylaxis, sensitization. Cumulation of medicinal substances. Social aspects of drug abuse. The harm of self-medication.
Repeated administrations of the same drug substance can lead to a quantitative (increase or decrease) and qualitative change in the pharmacological effects.
Among the phenomena observed with repeated administration of drugs, there are cumulation, sensitization, addiction (tolerance) and drug dependence.
Cumulation (from Lat. cumulatio - increase, accumulation) - the accumulation of a medicinal substance in the body or the effects it causes.
Material cumulation - an increase in the blood and / or tissue concentration of a drug substance after each new administration in comparison with the previous concentration. Drugs that are slowly inactivated and slowly excreted from the body, as well as drugs that firmly bind to blood plasma proteins or are deposited in tissues, for example, some hypnotics from the barbiturate group, digitalis drugs, can accumulate with repeated injections. Material accumulation can cause toxic effects, which must be taken into account when dosing such drugs.
Functional cumulation is an increase in the effect of a drug with repeated injections in the absence of an increase in its concentration in the blood and / or tissues. This type of cumulation occurs with repeated intake of alcohol. With the development of alcoholic psychosis ("delirium tremens") in susceptible persons, delusions and hallucinations develop at a time when ethyl alcohol has already been metabolized and is not detected in the body. Functional cumulation is also characteristic of MAO inhibitors.
Sensitization.Many medicinal substances form complexes with blood plasma proteins, which acquire antigenic properties under certain conditions. This is accompanied by the formation of antibodies and sensitization of the body. Repeated administration of the same medicinal substances causes allergic reactions. Often such reactions occur with repeated injections of penicillins, procaine, water-soluble vitamins, sulfonamides, etc.
Addictive(tolerance, from Lat. tolerantia - patience) - a decrease in the pharmacological effect of a drug when it is repeated in the same dose. With the development of addiction, in order to achieve the previous effect, it is necessary to increase the dose of the drug. Tolerance develops to both the therapeutic and toxic effects of drugs. For example, with prolonged use of morphine, tolerance arises not only to its analgesic effect, but also to the depressing effect on the respiratory center. So, the main reason for addiction to phenobarbital is considered to be the activation of its metabolism due to the induction of liver enzymes caused by phenobarbital itself. Drug addiction can develop over days or months.
A special case of addiction is tachyphylaxis (from the Greek tachys - fast, phylaxis - protection) - the rapid development of addiction with repeated injections of the drug at short intervals (10-15 minutes). Another special case of addiction is mitridatism - the gradual development of insensitivity to the action of the drug and poisons, which occurs during their prolonged use, first in very small, and then in increasing doses.
Drug addiction - an urgent need (irresistible urge) to constantly or periodically resume the intake of a certain drug or group of substances. First, the substance is taken to achieve a state of euphoria, well-being and comfort, eliminate painful experiences, test new sensations. However, after a certain time, the need for repeated admission becomes insurmountable, which is aggravated by the withdrawal syndrome: the emergence of a severe condition associated with mental and somatic disorders (dysfunctions of organs and body systems) when the drug is discontinued. This condition is designated by the term "abstinence" (from Latin abstinentia - abstinence).
Distinguish between mental and physical drug dependence.
Psychic drug dependence is characterized by a sharp deterioration in mood and emotional discomfort, a feeling of fatigue when deprived of the drug. It occurs with the use of cocaine and other psychostimulants (amphetamine), hallucinogens (lysergic acid diethylamide, LSD-25), nicotine, Indian hemp (marijuana, hashish, plan, marijuana).
Physical drug dependence is characterized not only by emotional discomfort, but also by the occurrence of withdrawal symptoms.
Physical drug addiction develops to opioids (heroin, morphine), barbiturates, benzodiazepines, alcohol (ethyl alcohol).
Drug dependence is often combined with addiction, while increasing doses of the substance are required to obtain euphoria. The most severe drug dependence occurs in the case of a combination of mental dependence, physical dependence and addiction.
Classification of antiepileptic drugs according to the mechanism of action.
I. Means that block the sodium channels of neurons:Sodium valproate; Lamotrigine; Topiramate; Diphenin; Carbamazepine; Hexamidine
II. Drugs blocking calcium channels of neurons:Sodium Valproate; Etosuximide; Trimetin
1. Increasing the affinity of GABA to GABAA receptors: Benzodiazepines (diazepam, lorazepam, clonazepam); Phenobarbital; Topiramate
2. Contributing to the formation of GABA and preventing its inactivation: Sodium valproate
3. Interfering with GABA inactivation: Vigabatrin
4. Blocking neuronal and glial uptake of GABA: Tiagabin
5. Enhancing the release of GABA into the synaptic cleft: Gabapentin
1 drugs that reduce the release of glutamate from presynaptic endings: Lamotrigine
2.Media blocking glutamate receptors: Topiramate.
Mechanism of action: inhibit interneuronal transmission of excitation (by all mechanisms described in the classification).
Side effects:
1. Sedation, impaired ability to concentrate and slow down the speed of psychomotor reactions; 2. Dyspeptic disorders (nausea, vomiting, epigastric discomfort); 3. Inhibition of hematopoiesis; 4. Hepatotoxicity (diphenin, sodium valproate); 5. Allergic reactions; 6. Neurotoxicity; 7. Teratogenicity (sodium valproate, diphenin, carbamazepine); 8. Carbamazepine (with prolonged use) - bradycardia, arrhythmia, antidiuretic effect with the appearance of edema, in women - the risk of polycystic ovary disease; 9. Sodium valproate - weight gain, polycystic ovary; 10. Diphenin - gingival hyperplasia; 11. Etosuximide - parkinsonism, photophobia.
Contraindications:
1. Hypersensitivity to the drug; 2. Severe violations of the liver and kidneys; 3. Heart failure, bradycardia; 4. Pregnancy (I trimester); 5. Lactation period; 6. Myasthenia gravis; 7. Diseases of the hematopoietic system; 8. Potentially hazardous activities requiring increased attention and speed of psychomotor reactions.
Classification by mechanisms and localization of action:
1. Means directly affecting the function of the epithelium of the renal tubules:
● acting in the initial section of the distal tubules (blockers of Na + -Cl- transport, reduce sodium and water reabsorption)
–Thiazide diuretics - hydrochlorothiazide, cyclomethiazide
–Thiazide-like diuretics - clopamide, chlorthalidone, indapamide
● acting in the thick segment of the ascending part of Henle's loop ("loop" diuretics, blockers of Na + -K + transport, inhibits the reabsorption of chlorine and sodium)
–Furosemide, torasemide, ethacrynic acid, xypamide
● acting in the end section of the distal tubules and collecting ducts
–Blockers of Na + channels - triamterene, amiloride
- aldosterone antagonists - spironolactone (increase urinary excretion of sodium, chlorine and water).
2. Osmotic diuretics (act in all parts of the nephron, but to a greater extent - in the proximal tubules, increase the osmotic pressure in the renal tubules, while reducing the reabsorption of water and sodium).
mannitol (mannitol)
3. Carbonic anhydrase inhibitors (reduced reabsorption of bicarbonate, act in the proximal tubules)
acetazolamide (diacarb), dorzolamide (trussopt).
Mechanisms: from the classification.
Thiazide and thiazide-like diuretics.
Hypertension, edema in CHF; Spironolactone (an aldosterone antagonist) is also used for hyperaldosteronism.
Side: dyspeptic symptoms, azotemia, cramps in the lower extremities, hyperkalemia.
Osmotic diuretics
Mannitol (mannitol)
Designed for intravenous drip injection in a volume of 200-400 ml. Mannitol is filtered through the endothelium of the capillaries of the renal glomeruli and maintains a high osmotic pressure in the lumen of the nephron tubules. The drug is not reabsorbed and therefore retains water in all parts of the nephron, especially in the proximal tubules, resulting in a significant increase in urine volume. In addition to the diuretic effect, mannitol has a dehydrating effect by increasing the osmotic pressure of blood plasma.
Indications for use:Pulmonary edema, cerebral edema; Acute poisoning (for forced diuresis); Acute attack of glaucoma
NB! In case of impaired renal excretory function, mannitol is ineffective and contraindicated!
Side effects:
Dry mouth, tachycardia, nausea, vomiting, convulsive reactions are possible.
Carbonic anhydrase inhibitors
Indications for use:• After suffering strokes, brain injuries, neuroinfections, neurosurgical interventions • Intracranial hypertension • Internal hydrocephalus • Some forms of epilepsy, cerebral palsy • Chronic alcoholism • Open-angle glaucoma • Prevention and relief of mountain (high-altitude) sickness
Dorzolamide (Trusopt) is used topically in the form of eye drops for open-angle glaucoma.
Side effects:• Metabolic acidosis (for its prevention after 4-5 days of administration - a break of 2-3 days) • Increased blood glucose levels • Moderate hypokalemia and hypomagnesemia
• Diarrhea. • Teratogenic effect (contraindicated in pregnancy).
four). Dyes. Detergents. Oxidizing agents. Acids and alkalis. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.
Dyes:Brilliant green, methylene blue, ethacridine lactate
Detergents:Zerigel, roccal
Oxidants:Potassium permanganate, hydrogen peroxide solution
Acids and alkalis:Boric acid, salicylic xylot; ammonia solution, sodium bicarbonate.
Detergents (roccal, cerigel) - cationic soaps with detergent and antiseptic properties.
Mechanism of action: violation of the structure of the cell membrane, denaturation of proteins and inhibition of enzymes of the microbial cell.
Indications: treatment of the surgeon's hands, sterilization of instruments.
Side effects: they do not cause irritation of tissues in usual concentrations.
Cannot be combined with anionic soaps as their activity decreases.
Oxidants
Hydrogen peroxide
Mechanism of action:upon contact with tissues, it decomposes with the release of molecular oxygen, which is released in the form of bubbles from the wound, mechanically cleans it. It also has a deodorant and hemostatic effect.
Indications: used for the primary treatment of superficial contaminated wounds, cleansing wounds from pus and blood clots, stopping capillary bleeding (including nasal), for rinsing the mouth and throat).
Potassium permanganate
Mechanism of action:in the presence of organic substances, it splits off atomic oxygen, the antiseptic effect of atomic oxygen is more pronounced than molecular one; provides antimicrobial and deodorizing effects, and the resulting manganese oxide is an astringent.
Indications: it is used for treating wounds, rinsing the mouth and throat, 0.02-0.1% solution is used for washing and douching for gynecological and urological inflammatory diseases, as well as for washing the stomach in case of poisoning.