The appearance on the pharmacological market of new antibiotics with a wide spectrum of effects, such as fluoroquinolones, cephalosporins, led to the fact that doctors began to rarely prescribe aminoglycosides (drugs). The list of medicines included in this group is quite extensive, and includes such well-known medicines as Gentamicin, Amikacin, Streptomycin. Streptomycin, by the way, is considered historically the first aminoglycoside. He is the second known antibiotic after penicillin. Aminoglycosides, or rather, aminoglycoside preparations, remain to this day the most popular in intensive care and surgical wards.
Brief description of the group
Aminoglycosides are drugs (we will consider the list of drugs below) that differ in semisynthetic or natural origin. This group of antibiotics has a fast and powerful bactericidal effect on the body.
Medicines have a wide range of effects. Their antimicrobial activity is pronounced against gram-negative bacteria, but significantly reduced in the fight against gram-positive microorganisms. And aminoglycosides are completely ineffective against anaerobes.
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 ribosomes. Medications are active against both multiplying and dormant cells. The degree of activity of antibiotics depends entirely on their concentration in the patient's blood serum.
The group of aminoglycosides is used today to a fairly limited extent. This is due to the high toxicity of these drugs. Most often, kidney and hearing organs suffer from such medications.
An important feature of these funds is the impossibility of their penetration into a living cell. Thus, aminoglycosides are completely powerless in the fight against intracellular bacteria.
Advantages and disadvantages
These antibiotics are widely used, as indicated above, in surgical practice. And this is no coincidence. Doctors emphasize the many advantages that aminoglycosides possess.
The effect of drugs on the body is characterized by such positive aspects:
- high antibacterial activity;
- the absence of a painful reaction (with injection);
- a rare occurrence of allergies;
- the ability to destroy breeding bacteria;
- enhanced therapeutic effect when combined with beta-lactam antibiotics;
- high activity in the fight against dangerous infections.
However, along with the advantages described above, this group of medicines also has disadvantages.
The disadvantages of aminoglycosides are:
- low activity of drugs in the absence of oxygen or in an acidic environment;
- poor penetration of the main substance into body fluids (bile, cerebrospinal fluid, sputum);
- the appearance of many side effects.
Drug Classification
There are several classifications.
So, given the sequence of introduction of aminoglycosides into medical practice, the following generations are distinguished:
- The first drugs used to combat infectious ailments were Streptomycin, Monomycin, Neomycin, Kanamycin, Paromomycin.
- The second generation includes more modern aminoglycosides (drugs). List of drugs: "Gentamicin", "Tobramycin", "Sisomycin", "Netilmicin."
- This group includes semi-synthetic medicines, such as Amikacin, Isepamycin.
According to the spectrum of action and the occurrence of resistance, aminoglycosides are classified somewhat differently.
Generations of medicines distinguish the following:
1. Group 1 includes such drugs: “Streptomycin”, “Kanamycin”, “Monomycin”, “Neomycin”. These medications can fight the causative agents of tuberculosis and some atypical bacteria. However, against many gram-negative microorganisms and staphylococci, they are powerless.
2. The representative of the second generation of aminoglycosides is the medicine "Gentamicin". It is distinguished by a large antibacterial activity.
3. Better medicines. They have high antibacterial activity. Used against Klebisiella, enterobacter, Pseudomonas aeruginosa is precisely the third generation of aminoglycosides (drugs). The list of medicines is as follows:
- "Sizomycin";
- "Amikacin";
- “Tobramycin”;
“Netilmicin.”
4. The fourth group includes the drug Isepamycin. It is distinguished by the additional ability to effectively deal with the cytobacter, airborne pump, and nocardia.
In medical practice, another classification has been developed. It is based on the use of drugs, depending on the clinic of the disease, the nature of the infection, as well as the method of use.
This classification of aminoglycosides is as follows:
- Medications for systemic exposure, administered parenterally (injection). For the treatment of bacterial purulent infections occurring in severe forms provoked by conditionally pathogenic anaerobic microorganisms, the following drugs are prescribed: Gentamicin, Amikacin, Netilmicin, Tobramycin, Sizomycin. Treatment of dangerous mono-infections, which are based on obligate pathogens, is effective when Streptomycin and Gentomycin are included in the therapy. With mycobacterioses, the medicines Amikacin, Streptomycin, and Kanamycin are excellent.
- Drugs that are used exclusively inside for special indications. Those are: “Paromycin”, “Neomycin”, “Monomycin”.
- Topical medications. They are used for the treatment of purulent bacterial infections in otorhinolaryngology and ophthalmology. Gentamicin, Framycetin, Neomycin, and Tobramycin preparations have been developed for local exposure.
Indications for appointment
The use of aminoglycosides is advisable 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 the treatment of:
- hospital infections of various localization;
- purulent postoperative complications;
- intra-abdominal infections;
- sepsis;
- infectious endocarditis ;
- pyelonephritis, occurring in severe forms;
- infected burns;
- bacterial purulent meningitis;
- tuberculosis
- dangerous infectious ailments (plague, brucellosis, tularemia);
- septic arthritis provoked by gram-negative bacteria;
- urinary tract infections;
- ophthalmic diseases: blepharitis, bacterial keratitis, conjunctivitis, keratoconjunctivitis, uveitis, dacryocystitis;
- otorhinolaryngological ailments: otitis externa, rhinopharyngitis, rhinitis, sinusitis;
- protozoal infections.
Side effects
Unfortunately, during therapy with this category of drugs, the patient may experience a number of undesirable effects. The main drawback of medicines is its high toxicity. That is why only a doctor should prescribe aminoglycosides to the patient.
Side effects may occur:
- Ototoxicity . Patients complain of hearing loss, the appearance of ringing, noise. Often they indicate congestion in the ears. Most often, such reactions are observed in the elderly, in people initially suffering from hearing impairment. Similar reactions develop in patients with prolonged therapy or the appointment of high doses.
- Nephrotoxicity The patient has a strong thirst, the amount of urine changes (it can either increase or decrease), the level of creatinine in the blood rises, and the glomerular filtration decreases. Such symptoms are characteristic of people suffering from impaired renal function.
- Neuromuscular blockade. Sometimes breathing is depressed during therapy. In some cases, even paralysis of the respiratory muscles. As a rule, such reactions are characteristic of patients with neurological diseases or with impaired renal function.
- Vestibular disorders. They are manifested by a violation of coordination, dizziness. Very often, such side effects appear when prescribing Streptomycin to a patient.
- Neurological disorders. Paresthesia, encephalopathy may appear. Sometimes therapy is accompanied by damage to the optic nerve.
Very rarely, aminoglycosides cause allergic manifestations, such as a skin rash.
Contraindications
The described medicines have some limitations for use. Most often, aminoglycosides (the names of which were given above) are contraindicated in such pathologies or conditions:
- individual hypersensitivity;
- impaired renal excretory function;
- hearing impairment;
- the development of severe neutropenic reactions;
- vestibular disorders;
- myasthenia gravis, botulism, parkinsonism;
- depressed breathing, stupor.
In addition, they should not be used for treatment if the patient had a negative reaction to any medication in this group.
Consider the most popular aminoglycosides.
Amikacin
The drug is characterized by pronounced bacteriostatic, bactericidal and anti-tuberculosis effects on the human body. It is highly active in the fight against many gram-positive and gram-negative bacteria. So the instructions for use indicate to the drug "Amikacin". The injections are effective in the treatment of staphylococci, streptococci, pneumococci, salmonella, E. coli, and mycobacterium tuberculosis.
The medicine is not able to be absorbed through the digestive tract. Therefore, it is used only intravenously or intramuscularly. The highest concentration of the active substance is observed in blood serum after 1 hour. The positive therapeutic effect lasts for 10-12 hours. Due to this property, injections are performed twice a day.
When does the drug "Amikacin" recommend use? Injections are indicated for use in the following ailments:
- pneumonia, bronchitis, lung abscesses;
- infectious diseases of the peritoneum (peritonitis, pancreatitis, cholecystitis);
- diseases of the urinary tract (cystitis, urethritis, pyelonephritis);
- skin pathologies (ulcerative lesions, burns, bedsores, infected wounds) ;
- osteomyelitis;
- meningitis, sepsis;
- tuberculosis infections.
Often this tool is used for complications provoked by surgical intervention.
The use of the drug in pediatric practice is allowed. This fact confirms the instructions for use for the drug "Amikacin". For children from the first days of life, this medicine may be prescribed.
Dosages are determined solely by the doctor, depending on the age of the patient and his body weight.
The instruction provides such recommendations:
- For 1 kg of patient weight (both an adult and a child), 5 mg of the drug should be taken. With this scheme, a second injection is given after 8 hours.
- If 7.5 mg of medication is taken per 1 kg of body weight, then the interval between injections is 12 hours.
- Pay attention to how the drug "Amikacin" recommends the use of the drug for newborns. For children who have just been born, the dosage is calculated as follows: for 1 kg - 7.5 mg. In this case, the interval between injections is 18 hours.
- The duration of therapy can be 7 days (with i / v input) or 7-10 days (with i / m injections).
Netilmicin
This medicine, by its antimicrobial effect, is similar to Amikacin. Moreover, there are cases when Netilmicin was highly effective against those microorganisms in which the above-described medicine was powerless.
The medication has a significant advantage over other aminoglycosides. As the instructions for use indicate to Netilmicin, the drug has less nephro- and ototoxicity. The medication is intended solely for parenteral use.
Netilmicin recommends the use of:
- with septicemia, bacteremia,
- for the treatment of an alleged infection provoked by gram-negative microbes;
- with infections of the respiratory system, urogenital tract, skin, ligaments, osteomyelitis;
- newborns in case of serious staphylococcal infections (sepsis or pneumonia);
- with wound, preoperative and intraperitoneal infections;
- in case of risk of postoperative complications in surgical patients;
- with infectious diseases of the gastrointestinal 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 during the day, 1-2 injections are recommended.
The drug "Gentamicin"
It is produced in the form of ointment, injection and tablets. The medication has pronounced bactericidal properties. It provides a detrimental effect on many gram - negative bacteria, protea, campylobacter, Escherichia, staphylococcus, salmonella, klebsiella.
The drug "Gentamicin" (tablets or solution), entering the body, destroys pathogens at the cellular level. Like any aminoglycoside, it provides a violation of the synthesis of protein pathogens. As a result, such bacteria lose the ability to further multiply and cannot spread throughout the body.
An antibiotic is prescribed for infectious diseases affecting various systems and organs:
- meningitis;
- peritonitis;
- prostate;
- gonorrhea;
- osteomyelitis;
- cystitis;
- pyelonephritis;
- endometritis;
- empyema of pleura;
- bronchitis, pneumonia;
The drug "Gentamicin" is quite in demand in medicine. It allows you to treat patients from serious infections of the respiratory and urinary tract. This tool is recommended for infectious processes covering the peritoneum, bones, soft tissues or skin.
Aminoglycosides are not intended for self-treatment. Do not forget that only a qualified doctor can choose the necessary antibiotic. Therefore, do not self-medicate. Entrust your health to professionals!