Aminoglycosides: preparations (list, names, classification, instructions for use)

The emergence of new antibiotics on the pharmacological market, which have a wide range of effects, such as fluoroquinolones, cephalosporins, led to the fact that doctors began to rarely prescribe aminoglycosides (preparations). The list of drugs included in this group is quite extensive, and includes such well-known drugs as Penicillin, Gentamicin, Amikacin. Until now, in the resuscitative and surgical departments the most demanded are drugs of the aminoglycoside series.

Brief description of the group

Aminoglycosides - drugs (a list of drugs we will consider below), characterized by semi-synthetic or natural origin. This group of antibiotics has a rapid and powerful bactericidal effect on the body.

The medicines are characterized by a wide spectrum of action. Their antimicrobial activity is pronounced in relation to gram-negative bacteria, but it decreases significantly in the control of gram-positive microorganisms. And aminoglycosides against anaerobes are completely ineffective.

This group of drugs produces an excellent bactericidal effect due to the ability to irreversibly inhibit protein synthesis in sensitive microorganisms at the level of the ribosomes. Medications are active against both breeding and resting cells. The degree of activity of antibiotics depends entirely on their concentration in the patient's serum.

The group of aminoglycosides is very limited today. This is due to the high toxicity of these medications. Most often suffer from such drugs are the kidneys and hearing organs.

An important feature of these means is the impossibility of their penetration into the living cell. Thus, aminoglycosides are absolutely powerless in the fight against intracellular bacteria.

Advantages and disadvantages

These antibiotics are widely used, as mentioned above, in surgical practice. And this is not accidental. Physicians emphasize the many virtues that aminoglycosides possess.

The effect of drugs on the body is characterized by such positive moments:

• High antibacterial activity;
• Absence of a painful reaction (with an injection);
• A rare occurrence of allergies;
• The ability to kill the multiplying bacteria;
• Enhanced therapeutic effect when combined with beta-lactam antibiotics;
• High activity in the fight against dangerous infections.

However, along with the benefits described above, this group of medicines also has disadvantages.

Minuses of aminoglycosides are:

• Low activity of drugs in the absence of oxygen or in an acidic environment;
• Poor penetration of the main substance in body fluids (bile, cerebrospinal fluid, sputum);
• The emergence of many side effects.

Classification of medicines

There are several classifications.

Thus, taking into account the sequence of introduction of aminoglycosides into medical practice, the following generations stand out:

1. The first drugs used to combat infectious diseases were Streptomycin, Monomycin, Neomycin, Kanamycin, and Paromomycin.
2. The second generation includes more modern aminoglycosides (preparations). The list of medicines: "Gentamicin", "Tobramycin", "Sizomycin", "Netilmitsin".
3. This group includes semi-synthetic medicines, such as Amikacin, Izepamycin.

In the spectrum of action and the emergence of resistance, the aminoglycosides are classified somewhat differently.

Generations of medicines are distinguished by the following:

1. To 1 group include such drugs: "Streptomycin", "Kanamycin", "Monomycin", "Neomycin". These medicines allow to fight with the pathogens of tuberculosis and some atypical bacteria. However, against a multitude of gram-negative microorganisms and staphylococci, they are powerless.

2. The representative of the second generation of aminoglycosides is the drug "Gentamicin". It is distinguished by a large antibacterial activity.

3. Improved medicines. They have high antibacterial activity. Applied against kelbisiella, enterobaktera, Pseudomonas aeruginosa is the third generation of aminoglycosides (preparations). The list of medicines is as follows:

- "Sizomycin";

- "Amikacin";

- "Tevomycin";

- "Netilmitsin".

4. The fourth group includes the drug "Izepamycin". It is distinguished by the additional ability to effectively combat the cytobacter, aeronamas, and nocardia.

In medical practice, another classification is developed. It is based on the use of medications depending on the clinic of the disease, the nature of the infection, and also the method of administration.

This classification of aminoglycosides is as follows:

1. Drugs for systemic exposure, injected into the body parenterally (injectively). To treat bacterial purulent infections that occur in severe forms provoked by conditionally pathogenic anaerobic microorganisms, prescribe such drugs: Gentamicin, Amikacin, Nethylmicin, Tevomycin, Sizomycin. The treatment of dangerous monoinfections, based on obligate pathogens, is effective when included in the therapy of drugs "Streptomycin", "Gentomycin." With mycobacteriosis, the drugs "Amikacin", "Streptomycin", "Kanamycin" are very helpful.
2. Drugs that are used exclusively inside with special indications. Such are: "Paromycin", "Neomycin", "Monomycin".
3. Medicines for topical use. They are used to treat purulent bacterial infections in otorhinolaryngology and ophthalmology. For local effects, preparations "Gentamicin", "Framicetin", "Neomycin", "Tobramycin" were developed.

Indications for use

The use of aminoglycosides is useful for the destruction of a wide variety of aerobic gram-negative pathogens. Medications can be used as monotherapy. Often they are combined with beta-lactams.

Aminoglycosides are prescribed for treatment of:

• Hospital infections of various localizations;
• Suppurative postoperative complications;
• Intra-abdominal infections;
• Sepsis;
• Infective endocarditis ;
• Pyelonephritis, taking place in severe forms;
• Infected burns;
• Bacterial purulent meningitis;
• Tuberculosis;
• Dangerous infectious diseases (plague, brucellosis, tularemia);
• Septic arthritis, provoked by gram-negative bacteria;
• Urinary tract infections;
• Ophthalmic diseases: blepharitis, bacterial keratitis, conjunctivitis, keratoconjunctivitis, uveitis, dacryocystitis;
• Otorhinolaryngological ailments: external otitis, rhinopharyngitis, rhinitis, sinusitis;
• Protozoal infections.

Side effects

Unfortunately, during therapy with this category of drugs, the patient can feel a number of undesirable effects. The most important drawback of medicines is high toxicity. That's why only the doctor should prescribe to the patient aminoglycosides.

Side effects can be manifested:

1. Ototoxicity . Patients complain of hearing loss, the appearance of ringing, noise. Often they point to the stuffiness of the ears. Most often, such reactions are observed in the elderly, in people who initially suffer from hearing impairment. Similar reactions develop in patients with prolonged therapy or high doses.
2. Nephrotoxicity . The patient develops a strong thirst, changes the amount of urine (can both increase and decrease), increases the level of creatinine in the blood, reduces glomerular filtration. This symptomatology is peculiar to people suffering from kidney dysfunction.
3. Neuromuscular blockade. Sometimes during therapy, breathing is depressed. In some cases, even paralysis of the respiratory muscles is observed. As a rule, such reactions are peculiar to patients with neurological diseases or with impaired renal function.
4. Vestibular disorders. They are manifested in a violation of coordination, dizziness. Very often such side effects appear when the patient is prescribed the drug Streptomycin.
5. Neurological disorders. There may be paresthesia, encephalopathy. Sometimes the therapy is accompanied by a lesion of the optic nerve.

Very rarely aminoglycosides cause allergic manifestations, such as a skin rash.

Contraindications

The described medicines have some limitations to the use. Most often, aminoglycosides (the names of which were listed above) are contraindicated in such pathologies or conditions:

• Individual hypersensitivity;
• Violation of excretory function of the kidneys;
• Hearing disorders;
• Development of neutropenic severe reactions;
• Vestibular disorders;
• Myasthenia gravis, botulism, parkinsonism;
• Depressed breathing, stupor.

In addition, they should not be used for treatment if a history of the patient had a negative reaction to any medication from this group.

Consider the most popular aminoglycosides.

Amicacin

The drug has a pronounced bacteriostatic, bactericidal and anti-tuberculosis effect on the human body. He shows great activity in the fight against many gram-positive and gram-negative bacteria. So the instruction on the use of the drug "Amikacin" testifies to this. The injections are effective in the treatment of staphylococci, streptococci, pneumococci, salmonella, E. coli, mycobacterium tuberculosis.

The medicine can not be absorbed through the digestive tract. Therefore, it is used only intravenously or intramuscularly. The highest concentration of active substance is observed in the blood serum after 1 hour. Positive therapeutic effect persists for 10-12 hours. Due to this property, injections are performed twice a day.

When does the application guide "Amikacin" recommend application? The injections are indicated for the purpose with the following ailments:

• Pneumonia, bronchitis, lung abscess;
• Infectious diseases of the peritoneum (peritonitis, pancreatitis, cholecystitis);
• Diseases of the urinary tract (cystitis, urethritis, pyelonephritis);
• Pathologies of the skin (ulcerative lesions, burns, bedsores, infected wounds) ;
• Osteomyelitis;
• Meningitis, sepsis;
• Tuberculosis infections.

Often, this tool is used for complications, provoked by a surgical procedure.

The use of the drug in pediatric practice is permitted. This fact confirms the instruction for the use of Amicacin. For children from the first days of life, this medicine can be prescribed.

Dosages are determined exclusively by the doctor, depending on the age of the patient and the weight of his body.

The instruction gives such recommendations:

1. For 1 kg of the weight of the patient (both adult and child) should account for 5 mg of the drug. Under this scheme, a second injection is given after 8 hours.
2. If 7.5 mg of medicament is taken per 1 kg of body weight, the interval between injections is 12 hours.
3. Pay attention, as recommends the use of the drug "Amikacin" for newborns instructions for use. For children who have just appeared, the dosage is calculated as follows: for 1 kg - 7.5 mg. The interval between injections is 18 hours.
4. The duration of therapy can be 7 days (with IV) or 7-10 days (with intravenous injections).

"Netilmicin"

This medicine has the same antimicrobial effect as Amicacin. In this case, cases are known where "Netilmicin" was highly effective against those microorganisms in which the above-described drug was powerless.

The drug has a significant advantage in comparison with other aminoglycosides. As the instructions for use to the drug "Netilmicin" indicate, the drug has less nephro- and ototoxicity. The medication is intended solely for parenteral use.

"Nethylmicin" application instruction recommends the appointment of:

• With septicemia, bacteremia,
• For the therapy of a presumptive infection provoked by gram-negative microbes;
• With infections of the respiratory system, urogenital tract, skin, ligaments, osteomyelitis;
• Newborns in the case of serious staphylococcal infections (sepsis or pneumonia);
• With wound, preoperative and intraperitoneal infections;
• In the case of the risk of postoperative complications in surgical patients;
• With infectious diseases of the digestive tract.

The recommended dose is determined only by the doctor. It can be from 4 mg to 7.5. Depending on the dosage, the condition of the patient and his age within a day, 1-2 injections are recommended.

"Penicillin"

This medication is one of the main medicines in the group of antibiotics. It has activity against a number of microorganisms.

Sensitive to the effects of Penicillin:

• Streptococci;
• Gonococci;
• Meningococci;
• Pneumococci;
• Causative agents of diphtheria, anthrax, tetanus, gas gangrene;
• Certain strains of staphylococcus, protea.

Physicians note the most effective effect on the body with intramuscular entry. With such an injection, after 30-60 minutes, the highest concentration of Penicillin is observed in the blood.

Aminoglycosides of the penicillin series are prescribed in the following cases:

1. These medicines are highly in demand in the therapy of sepsis. They are recommended for the treatment of gonococcal, meningococcal, pneumococcal infections.
2. Penicillin is prescribed for patients who underwent surgery to prevent complications.
3. It helps to fight with purulent meningitis, brain abscesses, gonorrhea, sycosis, syphilis. It is recommended for severe burns and wounds.
4. Therapy with Penicillin is prescribed for patients suffering from inflammation of the ear and eyes.
5. The drug is used to treat focal and croupous pneumonia, cholangitis, cholecystitis, septic endocarditis.
6. People suffering from rheumatism, this medication is prescribed for treatment and prevention.
7. The drug is used for newborns and infants who have umbilical sepsis, septicopyemia or septic toxic disease.
8. The drug is included in the treatment of the following ailments: otitis, scarlet fever, diphtheria, purulent pleurisy.

With intramuscular injection, the active substance of the drug is rapidly absorbed into the blood. But after 3-4 hours of medication in the body is no longer observed. That is why, to ensure the necessary concentration, it is recommended to repeat the injection every 3-4 hours.

The drug "Gentamicin"

Produced in the form of ointment, solution for injection and tablets. The drug has pronounced bactericidal properties. It provides a disastrous effect on many gram - negative bacteria, proteins, campylobacteria, escherichia, staphylococcus, salmonella, Klebsiella.

The drug "Gentamicin" (tablets or solution), getting into the body, destroys the pathogens of infection at the cellular level. Like any aminoglycoside, it provides a violation of protein synthesis of pathogens. As a result, such bacteria lose their ability to further reproduce and can not spread throughout the body.

An antibiotic is prescribed for infectious diseases that affect various systems and organs:

• Meningitis;
• Peritonitis;
• Prostatitis;
• Gonorrhea;
• Osteomyelitis;
• Cystitis;
• Pyelonephritis;
• Endometritis;
• Empyema of the pleura;
• Bronchitis, pneumonia;

The drug "Gentamicin" is quite in demand in medicine. It allows patients to be cured of serious infections of the respiratory and urinary tract. This remedy is recommended for infectious processes that cover the peritoneum, bones, soft tissues or skin.

Aminoglycosides are not intended for self-therapy. Do not forget that only a qualified doctor can pick up the necessary antibiotic. So do not self-medicate. Entrust your health to professionals!