Penicillin analogues have opened up new treatment options for doctors infectious diseases. They are more resistant to the aggressive environment of the stomach and have fewer side effects.
About penicillins
Penicillins are the oldest known antibiotics. They have many species, but some of them have lost their relevance due to resistance. The bacteria were able to adapt and became insensitive to the effects of these drugs. This forces scientists to create new types of mold, analogues of penicillin, with new properties.
Penicillins have low toxicity to the body, are widely used and good indicator bactericidal action, but they are found much more often than doctors would like. This is explained by the organic nature of antibiotics. Another negative quality is the difficulty in combining them with other medications, especially those of a similar class.
Story
The first mention of penicillins in literature took place in 1963, in a book about Indian healers. They used mixtures of fungi for medicinal purposes. For the first time in the enlightened world, Alexander Fleming managed to obtain them, but this did not happen on purpose, but by accident, like all great discoveries.
Before World War II, English microbiologists worked on the issue of industrial production of medicine in the required volumes. The same problem was solved in parallel in the USA. From that moment on, penicillin became the most common medicine. But over time, others were isolated and synthesized, which gradually displaced him from the podium. In addition, microorganisms began to develop resistance to this drug, which complicated the treatment of severe infections.
Principle of antibacterial action
Part cell wall bacteria contains a substance called peptidoglycan. The penicillin group of antibiotics affects the process of synthesis of this protein, suppressing the formation of necessary enzymes. The microorganism dies due to the inability to renew the cell wall.
However, some bacteria have learned to resist such brutal invasion. They produce beta-lactamase, which destroys enzymes that affect peptidoglycans. In order to overcome this obstacle, scientists had to create analogues of penicillin that could also destroy beta-lactamase.
Danger to humans
At the very beginning of the era of antibiotics, scientists began to think about how toxic they would become for the human body, because almost all living matter consists of proteins. But after conducting a sufficient amount of research, we found out that there is practically no peptidoglycan in our bodies, which means that the drug cannot cause any serious harm.
Spectrum of action
Almost all types of penicillins act on gram-positive bacteria of the genus Staphylococcus, Streptococcus, and the causative agent of plague. Also, their spectrum of action includes all gram-negative microorganisms, gonococci and meningococci, anaerobic bacilli and even some fungi (for example, actinomycetes).
Scientists are inventing more and more new types of penicillins, trying to prevent bacteria from becoming accustomed to their bactericidal properties, but this group of drugs is no longer suitable for treatment. One of the negative properties of this type of antibiotics is dysbiosis, since the human intestines are colonized by bacteria that are sensitive to the effects of penicillin. This is worth remembering when taking medications.
Main types (classification)
Modern scientists propose a modern division of penicillins into four groups:
- Natural, which are synthesized by fungi. These include benzylpenicillins and phenoxymethylpenicillin. These drugs have a narrow spectrum of action, mainly on
- Semi-synthetic drugs that are resistant to penicillinases. Used to treat a wide range of pathogens. Representatives: methicillin, oxacillin, nafcillin.
- Carboxypenicillins (carbpenicillin).
- A group of drugs with a wide spectrum of action:
- ureidopenicillins;
- amidopenicillins.
Biosynthetic forms
As an example, it is worth citing a few of the most common ones. this moment medicines that correspond to this group. Probably the most famous of the penicillins can be considered “Bicillin-3” and “Bicillin-5”. They discovered a group of natural antibiotics and were the leaders in their category until more advanced forms of antimicrobial drugs appeared.
- "Extencillin". The instructions for use state that it is a long-acting beta-lactam antibiotic. Indications for its use are exacerbations of rheumatic disease and diseases caused by treponemes (syphilis, yaws and pinta). Available in powders. "Extencillin" instructions for use do not recommend combining it with non-steroidal anti-inflammatory drugs (NSAIDs), as a competitive interaction is possible. This may negatively affect the effectiveness of treatment.
- "Penicillin-V" belongs to the group of phenoxymethylpenicillins. It is used to treat infectious diseases of the ENT organs, skin and mucous membranes, gonorrhea, syphilis, tetanus. It is used as preventative measure after surgical interventions, to maintain remission in rheumatism, chorea minor, bacterial endocarditis.
- The antibiotic "Ospen" is an analogue of the previous drug. It is available in the form of tablets or granules. It is not recommended to combine with NSAIDs and oral contraceptives. Often used in the treatment of childhood diseases.
Semi-synthetic forms
This group of drugs includes chemically modified antibiotics obtained from mold fungi.
- The first on this list is Amoxicillin. Instructions for use (price - about one hundred rubles) indicate that the drug has a wide spectrum of action and is used for bacterial infections of almost any localization. Its advantage is that it is stable in the acidic environment of the stomach, and after absorption the concentration in the blood is higher than that of other representatives of this group. But you should not idealize Amoxicillin. Instructions for use (price may vary in different regions) warn that the drug should not be prescribed to patients with mononucleosis, allergy sufferers and pregnant women. Long-term use is not possible due to a significant number of adverse reactions.
- Oxacillin sodium salt is prescribed when bacteria produce penicillinase. The drug is acid-resistant, can be taken orally, and is well absorbed in the intestine. It is quickly excreted by the kidneys, so it is necessary to constantly maintain the desired concentration in the blood. The only contraindication is an allergic reaction. Available in tablet form or in bottles as liquid for injection.
- The last representative of semisynthetic penicillins is ampicillin trihydrate. Instructions for use (tablets) indicate that it has a wide spectrum of action, affecting both gram-negative and gram-positive bacteria. It is well tolerated by patients, but should be prescribed with caution to those taking anticoagulants (for example, people with pathologies of the cardiovascular system), since the drug potentiates their effect.
Solvent
Penicillins are sold in pharmacies in the form of powder for injection. Therefore, for intravenous or intramuscular administration they must be dissolved in liquid. At home, you can use distilled water for injection, sodium chloride or a solution of two percent novocaine. It must be remembered that the solvent should not be too warm.
Indications, contraindications and side effects
Indications for antibiotic treatment are the following diagnoses: lobar and focal pneumonia, pleural empyema, sepsis and septicemia, septic endocarditis, meningitis, osteomyelitis. Bacterial tonsillitis, diphtheria, scarlet fever, anthrax, gonorrhea, syphilis, purulent skin infections.
There are few contraindications to treatment with the penicillin group. Firstly, the presence of hypersensitivity to the drug and its derivatives. Secondly, an established diagnosis of epilepsy, which does not make it possible to administer the drug inside the spinal column. As for pregnancy and lactation, in this case the expected benefits should significantly exceed the possible risks, because the placental barrier is permeable to penicillins. While taking the medicine, the child must be temporarily switched to another method of feeding, since the drug passes into the milk.
Side effects can occur on several levels at once.
From the central nervous system, nausea, vomiting, excitability, meningism, convulsions and even coma are possible. Allergic reactions manifest themselves in the form of skin rashes, fever, joint pain and swelling. There have been cases of anaphylactic shock and deaths. Due to the bactericidal effect, candidiasis of the vagina and oral cavity, as well as dysbacteriosis, is possible.
Features of use
Caution should be used in patients with impaired liver and kidney function and established heart failure. It is not recommended to use them for people prone to allergic reactions, as well as for those who are hypersensitive to cephalosporins.
If five days after the start of therapy there are no changes in the patient’s condition, then it is necessary to use penicillin analogues or replace the group of antibiotics. At the same time as prescribing, for example, the substance "Bicillin-3", care must be taken to prevent fungal superinfection. For this purpose, antifungal drugs are prescribed.
It is necessary to clearly explain to the patient that interrupting the medication without good reason causes resistance of microorganisms. And to overcome it, you will need stronger drugs that cause severe side effects.
Penicillin analogues have become indispensable in modern medicine. Although this is the earliest discovered group of antibiotics, it still remains relevant for the treatment of meningitis, gonorrhea and syphilis, and has a wide enough spectrum of action and mild side effects that it can be prescribed to children. Of course, like any medicine, penicillins have contraindications and side effects, but they are more than compensated for by the possibilities for use.
Penicillins (penicillina)- a group of antibiotics produced by many types of molds of the genus Penicillium, active against most gram-positive, as well as some gram-negative microorganisms (gonococci, meningococci and spirochetes). Penicillins are classified as so-called. beta-lactam antibiotics (beta-lactams).
Beta-lactams are a large group of antibiotics, which have in common the presence of a four-membered beta-lactam ring in the structure of the molecule. Beta-lactams include penicillins, cephalosporins, carbapenems, and monobactams. Beta-lactams are the most numerous group of those used in clinical practice antimicrobial drugs, which occupy a leading place in the treatment of most infectious diseases.
Historical information. In 1928, the English scientist A. Fleming, who worked at St. Mary's Hospital in London, discovered the ability of a filamentous green mold fungus (Penicillium notatum) cause the death of staphylococci in cell culture. Active substance A fungus with antibacterial activity was called penicillin by A. Fleming. In 1940, in Oxford, a group of researchers led by H.W. Flory and E.B. Cheyna isolated significant amounts of the first penicillin from culture in pure form. Penicillium notatum. In 1942, the outstanding domestic researcher Z.V. Ermolyeva received penicillin from a mushroom Penicillium crustosum. Since 1949, virtually unlimited quantities of benzylpenicillin (penicillin G) have become available for clinical use.
The penicillin group includes natural compounds produced by various types of molds. Penicillium, and a number of semi-synthetic ones. Penicillins (like other beta-lactams) have a bactericidal effect on microorganisms.
The most common properties of penicillins include: low toxicity, a wide range of dosages, cross-allergy between all penicillins and some cephalosporins and carbapenems.
Antibacterial effect beta-lactams is associated with their specific ability to disrupt the synthesis of bacterial cell walls.
The cell wall of bacteria has a rigid structure; it gives microorganisms their shape and protects them from destruction. Its basis is a heteropolymer - peptidoglycan, consisting of polysaccharides and polypeptides. Its cross-linked network structure gives the cell wall strength. Polysaccharides include amino sugars such as N-acetylglucosamine, as well as N-acetylmuramic acid, which is found only in bacteria. Associated with amino sugars are short peptide chains, including some L- and D-amino acids. In gram-positive bacteria, the cell wall contains 50-100 layers of peptidoglycan, in gram-negative bacteria - 1-2 layers.
About 30 bacterial enzymes are involved in the process of peptidoglycan biosynthesis; this process consists of 3 stages. It is believed that penicillins disrupt the late stages of cell wall synthesis, preventing the formation of peptide bonds by inhibiting the enzyme transpeptidase. Transpeptidase is one of the penicillin-binding proteins with which beta-lactam antibiotics interact. Penicillin-binding proteins—enzymes that take part in the final stages of bacterial cell wall formation—in addition to transpeptidases, include carboxypeptidases and endopeptidases. All bacteria have them (for example, Staphylococcus aureus there are 4 of them, Escherichia coli- 7). Penicillins bind to these proteins at different rates to form a covalent bond. In this case, inactivation of penicillin-binding proteins occurs, the strength of the bacterial cell wall is disrupted and the cells undergo lysis.
Pharmacokinetics. When taken orally, penicillins are absorbed and distributed throughout the body. Penicillins penetrate well into tissues and body fluids (synovial, pleural, pericardial, bile), where they quickly reach therapeutic concentrations. The exceptions are cerebrospinal fluid, internal media of the eye and secretions prostate gland— here the concentrations of penicillins are low. The concentration of penicillins in the cerebrospinal fluid may vary depending on the conditions: normally - less than 1% serum, with inflammation it can increase to 5%. Therapeutic concentrations in the cerebrospinal fluid are created during meningitis and the administration of drugs in high doses. Penicillins are quickly eliminated from the body, mainly by the kidneys through glomerular filtration and tubular secretion. Their half-life is short (30-90 min), the concentration in urine is high.
There are several classifications Medicines belonging to the penicillin group: by molecular structure, by sources of production, by spectrum of activity, etc.
According to the classification presented by D.A. Kharkevich (2006), penicillins are divided as follows (classification is based on a number of characteristics, including differences in production routes):
I. Penicillin preparations obtained by biological synthesis (biosynthetic penicillins):
I.1. For parenteral administration (destroyed in the acidic environment of the stomach):
Short acting:
benzylpenicillin (sodium salt),
benzylpenicillin (potassium salt);
Long-lasting:
benzylpenicillin (novocaine salt),
Bicillin-1,
Bicillin-5.
I.2.
phenoxymethylpenicillin (penicillin V).
II. Semi-synthetic penicillins
II.1. For parenteral and enteral administration (acid-resistant):
Penicillinase-resistant:
oxacillin (sodium salt),
nafcillin;
Broad spectrum of action:
ampicillin,
amoxicillin.
II.2. For parenteral administration (destroyed in the acidic environment of the stomach)
Broad spectrum of action, including Pseudomonas aeruginosa:
carbenicillin (disodium salt),
ticarcillin,
azlocillin.
II.3. For enteral administration (acid-resistant):
carbenicillin (indanyl sodium),
carfecillin.
According to the classification of penicillins given by I.B. Mikhailov (2001), penicillins can be divided into 6 groups:
1. Natural penicillins (benzylpenicillins, bicillins, phenoxymethylpenicillin).
2. Isoxazolepenicillins (oxacillin, cloxacillin, flucloxacillin).
3. Amidinopenicillins (amdinocillin, pivamdinocillin, bacamdinocillin, acidocillin).
4. Aminopenicillins (ampicillin, amoxicillin, talampicillin, bacampicillin, pivampicillin).
5. Carboxypenicillins (carbenicillin, carfecillin, carindacillin, ticarcillin).
6. Ureidopenicillins (azlocillin, mezlocillin, piperacillin).
The source of production, spectrum of action, as well as combination with beta-lactamases were taken into account when creating the classification given in the Federal Guide (formulary system), issue VIII.
1. Natural:
benzylpenicillin (penicillin G),
phenoxymethylpenicillin (penicillin V),
benzathine benzylpenicillin,
benzylpenicillin procaine,
benzathine phenoxymethylpenicillin.
2. Antistaphylococcal:
oxacillin.
3. Extended spectrum (aminopenicillins):
ampicillin,
amoxicillin.
4. Active in relation Pseudomonas aeruginosa:
Carboxypenicillins:
ticarcillin.
Ureidopenicillins:
azlocillin,
piperacillin.
5. Combined with beta-lactamase inhibitors (inhibitor-protected):
amoxicillin/clavulanate,
ampicillin/sulbactam,
ticarcillin/clavulanate.
Natural (natural) penicillins - These are narrow-spectrum antibiotics that affect gram-positive bacteria and cocci. Biosynthetic penicillins are obtained from the culture medium on which certain strains of molds are grown (Penicillium). There are several varieties of natural penicillins, one of the most active and persistent of them is benzylpenicillin. IN medical practice benzylpenicillin is used in the form various salts- sodium, potassium and novocaine.
All natural penicillins have similar antimicrobial activity. Natural penicillins are destroyed by beta-lactamases and are therefore ineffective for therapy staphylococcal infections, because in most cases, staphylococci produce beta-lactamases. They are effective primarily against gram-positive microorganisms (incl. Streptococcus spp., including Streptococcus pneumoniae, Enterococcus spp.), Bacillus spp., Listeria monocytogenes, Erysipelothrix rhusiopathiae, gram-negative cocci (Neisseria meningitidis, Neisseria gonorrhoeae), some anaerobes (Peptostreptococcus spp., Fusobacterium spp.), spirochete (Treponema spp., Borrelia spp., Leptospira spp.). Gram-negative microorganisms are usually resistant, with the exception of Haemophilus ducreyi And Pasteurella multocida. Penicillins are ineffective against viruses (causative agents of influenza, polio, smallpox, etc.), mycobacterium tuberculosis, the causative agent of amebiasis, rickettsia, and fungi.
Benzylpenicillin is active mainly against gram-positive cocci. The antibacterial action spectra of benzylpenicillin and phenoxymethylpenicillin are almost identical. However, benzylpenicillin is 5-10 times more active than phenoxymethylpenicillin against sensitive Neisseria spp. and some anaerobes. Phenoxymethylpenicillin is prescribed for infections medium degree gravity. The activity of penicillin preparations is determined biologically by antibacterial effect on a specific strain Staphylococcus aureus. The activity of 0.5988 mcg of chemically pure crystalline sodium salt of benzylpenicillin is taken as a unit of action (1 unit).
Significant disadvantages of benzylpenicillin are its instability to beta-lactamases (with enzymatic cleavage of the beta-lactam ring by beta-lactamases (penicillinases) to form penicillanic acid, the antibiotic loses its antimicrobial activity), insignificant absorption in the stomach (requiring injection routes of administration) and relatively low activity against most gram-negative microorganisms.
Under normal conditions, benzylpenicillin preparations penetrate poorly into the cerebrospinal fluid, but with inflammation of the meninges, permeability through the BBB increases.
Benzylpenicillin, used in the form of highly soluble sodium and potassium salts, acts for a short time - 3-4 hours, because is quickly eliminated from the body and requires frequent injections. In this regard, poorly soluble salts of benzylpenicillin (including novocaine salt) and benzathine benzylpenicillin were proposed for use in medical practice.
Prolonged forms of benzylpenicillin, or depot penicillins: Bicillin-1 (benzathine benzylpenicillin), as well as combined drugs based on them - Bicillin-3 (benzathine benzylpenicillin + benzylpenicillin sodium + benzylpenicillin novocaine salt), Bicillin-5 (benzathine benzylpenicillin + benzylpenicillin novocaine salt ), are suspensions that can only be administered intramuscularly. They are slowly absorbed from the injection site, creating a depot in muscle tissue. This allows you to maintain the concentration of the antibiotic in the blood for a significant time and thus reduce the frequency of drug administration.
All benzylpenicillin salts are used parenterally, because they are destroyed in the acidic environment of the stomach. Of the natural penicillins, only phenoxymethylpenicillin (penicillin V) has acid-stable properties, although to a weak extent. Phenoxymethylpenicillin differs in chemical structure from benzylpenicillin in the presence of a phenoxymethyl group in the molecule instead of a benzyl group.
Benzylpenicillin is used for infections caused by streptococci, including Streptococcus pneumoniae (community-acquired pneumonia, meningitis), Streptococcus pyogenes(streptococcal tonsillitis, impetigo, erysipelas, scarlet fever, endocarditis), with meningococcal infections. Benzylpenicillin is the antibiotic of choice in the treatment of diphtheria, gas gangrene, leptospirosis, and Lyme disease.
Bicillins are indicated, first of all, when it is necessary to maintain effective concentrations in the body for a long time. They are used for syphilis and other diseases caused by Treponema pallidum (yaws), streptococcal infections (excluding infections caused by group B streptococci) - acute tonsillitis, scarlet fever, wound infections, erysipelas, rheumatism, leishmaniasis.
In 1957, 6-aminopenicillanic acid was isolated from natural penicillins and the development of semisynthetic drugs began on its basis.
6-Aminopenicillanic acid is the basis of the molecule of all penicillins (“penicillin core”) - a complex heterocyclic compound consisting of two rings: thiazolidine and beta-lactam. A side radical is associated with the beta-lactam ring, which determines the essential pharmacological properties of the resulting drug molecule. In natural penicillins, the structure of the radical depends on the composition of the medium in which they grow Penicillium spp.
Semi-synthetic penicillins are obtained by chemical modification by adding various radicals to the 6-aminopenicillanic acid molecule. In this way, penicillins were obtained with certain properties:
Penicillinase (beta-lactamase) resistant;
Acid-resistant, effective when administered orally;
Having a wide spectrum of action.
Isoxazolepenicillins (isoxazolyl penicillins, penicillinase-stable, antistaphylococcal penicillins). Most staphylococci produce a specific enzyme beta-lactamase (penicillinase) and are resistant to benzylpenicillin (80-90% of strains are penicillinase-forming Staphylococcus aureus).
The main antistaphylococcal drug is oxacillin. The group of penicillinase-resistant drugs also includes cloxacillin, flucloxacillin, methicillin, nafcillin and dicloxacillin, which due to high toxicity and/or low effectiveness have not found clinical use.
The spectrum of antibacterial action of oxacillin is similar to that of benzylpenicillin, but due to the resistance of oxacillin to penicillinase, it is active against penicillinase-forming staphylococci that are resistant to benzylpenicillin and phenoxymethylpenicillin, as well as resistant to other antibiotics.
In terms of activity against gram-positive cocci (including staphylococci that do not produce beta-lactamase), isoxazolepenicillins, incl. oxacillin are significantly inferior to natural penicillins, therefore, for diseases caused by microorganisms sensitive to benzylpenicillin, they are less effective compared to the latter. Oxacillin does not show activity against gram-negative bacteria (except Neisseria spp.), anaerobes. In this regard, drugs of this group are indicated only in cases where it is known that the infection is caused by penicillinase-forming strains of staphylococci.
The main pharmacokinetic differences between isoxazolepenicillins and benzylpenicillin:
Rapid, but not complete (30-50%) absorption from the gastrointestinal tract. These antibiotics can be used both parenterally (IM, IV) and orally, but 1-1.5 hours before meals, because they have low resistance to hydrochloric acid;
High degree of binding to plasma albumin (90-95%) and the impossibility of removing isoxazolepenicillins from the body during hemodialysis;
Not only renal, but also hepatic excretion, no need to adjust the dosage regimen for mild renal failure.
The main clinical value of oxacillin is the treatment of staphylococcal infections caused by penicillin-resistant strains Staphylococcus aureus(except infections caused by methicillin-resistant Staphylococcus aureus, MRSA). It should be taken into account that strains are common in hospitals Staphylococcus aureus, resistant to oxacillin and methicillin (methicillin - the first penicillinase-resistant penicillin, discontinued). Nosocomial and community-acquired strains Staphylococcus aureus, resistant to oxacillin/methicillin, are usually multidrug-resistant - they are resistant to all other beta-lactams, and often also to macrolides, aminoglycosides, and fluoroquinolones. The drugs of choice for MRSA infections are vancomycin or linezolid.
Nafcillin is slightly more active than oxacillin and other penicillinase-resistant penicillins (but less active than benzylpenicillin). Nafcillin penetrates the BBB (its concentration in the cerebrospinal fluid is sufficient to treat staphylococcal meningitis), is excreted primarily in bile (the maximum concentration in bile is much higher than the serum concentration), and to a lesser extent by the kidneys. Can be used orally and parenterally.
Amidinopenicillins - These are penicillins with a narrow spectrum of action, but with predominant activity against gram-negative enterobacteria. Amidinopenicillin preparations (amdinocillin, pivamdinocillin, bacamdinocillin, acidocillin) are not registered in Russia.
Penicillins with an extended spectrum of activity
In accordance with the classification presented by D.A. Kharkevich, semi-synthetic broad-spectrum antibiotics are divided into the following groups:
I. Drugs that do not affect Pseudomonas aeruginosa:
Aminopenicillins: ampicillin, amoxicillin.
II. Drugs active against Pseudomonas aeruginosa:
Carboxypenicillins: carbenicillin, ticarcillin, carfecillin;
Ureidopenicillins: piperacillin, azlocillin, mezlocillin.
Aminopenicillins - broad-spectrum antibiotics. All of them are destroyed by beta-lactamases of both gram-positive and gram-negative bacteria.
Amoxicillin and ampicillin are widely used in medical practice. Ampicillin is the founder of the aminopenicillin group. In relation to gram-positive bacteria, ampicillin, like all semisynthetic penicillins, is inferior in activity to benzylpenicillin, but superior to oxacillin.
Ampicillin and amoxicillin have similar action spectra. Compared to natural penicillins, the antimicrobial spectrum of ampicillin and amoxicillin extends to sensitive strains of enterobacteria, Escherichia coli, Proteus mirabilis, Salmonella spp., Shigella spp., Haemophilus influenzae; act better than natural penicillins on Listeria monocytogenes and sensitive enterococci.
Of all the oral beta-lactams, amoxicillin has the greatest activity against Streptococcus pneumoniae, resistant to natural penicillins.
Ampicillin is not effective against penicillinase-forming strains Staphylococcus spp., all strains Pseudomonas aeruginosa, most strains Enterobacter spp., Proteus vulgaris(indole positive).
Combination drugs are available, for example Ampiox (ampicillin + oxacillin). The combination of ampicillin or benzylpenicillin with oxacillin is rational, because the spectrum of action with this combination becomes wider.
The difference between amoxicillin (which is one of the leading oral antibiotics) and ampicillin is its pharmacokinetic profile: when taken orally, amoxicillin is absorbed more quickly and well in the intestine (75-90%) than ampicillin (35-50%), bioavailability does not depend on food intake . Amoxicillin penetrates better into some tissues, incl. into the bronchopulmonary system, where its concentrations are 2 times higher than those in the blood.
The most significant differences in the pharmacokinetic parameters of aminopenicillins from benzylpenicillin:
Possibility of administration internally;
Insignificant binding to plasma proteins - 80% of aminopenicillins remain in the blood in free form - and good penetration into tissues and body fluids (with meningitis, concentrations in the cerebrospinal fluid can be 70-95% of concentrations in the blood);
Multiplicity of appointment combination drugs- 2-3 times a day.
The main indications for prescribing aminopenicillins are infections of the upper respiratory tract and ENT organs, kidney infections and urinary tract, gastrointestinal infections, eradication Helicobacter pylori(amoxicillin), meningitis.
A feature of the undesirable effect of aminopenicillins is the development of an “ampicillin” rash, which is a maculopapular rash of a non-allergic nature, which quickly disappears when the drug is discontinued.
One of the contraindications to the administration of aminopenicillins is Infectious mononucleosis.
Antipseudomonas penicillins
These include carboxypenicillins (carbenicillin, ticarcillin) and ureidopenicillins (azlocillin, piperacillin).
Carboxypenicillins are antibiotics that have a spectrum of antimicrobial action similar to aminopenicillins (except for the effect on Pseudomonas aeruginosa). Carbenicillin is the first antipseudomonas penicillin, and is inferior in activity to other antipseudomonas penicillins. Carboxypenicillins act on Pseudomonas aeruginosa (Pseudomonas aeruginosa) and indole-positive Proteus species (Proteus spp.) resistant to ampicillin and other aminopenicillins. Clinical significance carboxypenicillins are currently decreasing. Although they have a broad spectrum of action, they are inactive against most strains Staphylococcus aureus, Enterococcus faecalis, Klebsiella spp., Listeria monocytogenes. Almost do not pass through the BBB. The frequency of administration is 4 times a day. Secondary resistance of microorganisms quickly develops.
Ureidopenicillins - These are also antipseudomonas antibiotics, their spectrum of action coincides with carboxypenicillins. The most active drug from this group is piperacillin. Of the drugs in this group, only azlocillin retains its importance in medical practice.
Ureidopenicillins are more active than carboxypenicillins against Pseudomonas aeruginosa. They are also used in the treatment of infections caused by Klebsiella spp.
All antipseudomonas penicillins are destroyed by beta-lactamases.
Pharmacokinetic features of ureidopenicillins:
Administered only parenterally (i.m. and i.v.);
Not only the kidneys, but also the liver take part in excretion;
Frequency of application - 3 times a day;
Secondary bacterial resistance develops rapidly.
Due to the emergence of strains with high resistance to antipseudomonas penicillins and the lack of advantages over other antibiotics, antipseudomonas penicillins have practically lost their importance.
The main indications for these two groups of antipseudomonas penicillins are nosocomial infections caused by susceptible strains Pseudomonas aeruginosa, in combination with aminoglycosides and fluoroquinolones.
Penicillins and other beta-lactam antibiotics have high antimicrobial activity, but microbial resistance can develop to many of them.
This resistance is due to the ability of microorganisms to produce specific enzymes - beta-lactamases (penicillinases), which destroy (hydrolyze) the beta-lactam ring of penicillins, which deprives them of antibacterial activity and leads to the development of resistant strains of microorganisms.
Some semisynthetic penicillins are resistant to beta-lactamases. In addition, to overcome acquired resistance, compounds have been developed that can irreversibly inhibit the activity of these enzymes, the so-called. beta-lactamase inhibitors. They are used to create inhibitor-protected penicillins.
Beta-lactamase inhibitors, like penicillins, are beta-lactam compounds but have minimal antibacterial activity on their own. These substances irreversibly bind to beta-lactamases and inactivate these enzymes, thereby protecting beta-lactam antibiotics from hydrolysis. Beta-lactamase inhibitors are most active against beta-lactamases encoded by plasmid genes.
Inhibitor-protected penicillins are a combination of a penicillin antibiotic with a specific beta-lactamase inhibitor (clavulanic acid, sulbactam, tazobactam). Beta-lactamase inhibitors are not used alone, but are used in combination with beta-lactams. This combination makes it possible to increase the stability of the antibiotic and its activity against microorganisms that produce these enzymes (beta-lactamases): Staphylococcus aureus, Haemophilus influenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, Escherichia coli, Klebsiella spp., Proteus spp., anaerobes, incl. Bacteroides fragilis. As a result, strains of microorganisms resistant to penicillins become sensitive to the combined drug. The spectrum of antibacterial activity of inhibitor-protected beta-lactams corresponds to the spectrum of the penicillins they contain, only the level of acquired resistance differs. Inhibitor-protected penicillins are used to treat infections various localizations and for perioperative prophylaxis in abdominal surgery.
Inhibitor-protected penicillins include amoxicillin/clavulanate, ampicillin/sulbactam, amoxicillin/sulbactam, piperacillin/tazobactam, ticarcillin/clavulanate. Ticarcilin/clavulanate has antipseudomonal activity and is active against Stenotrophomonas maltophilia. Sulbactam has its own antibacterial activity against gram-negative cocci of the family Neisseriaceae and families of non-fermenting bacteria Acinetobacter.
Indications for the use of penicillins
Penicillins are used for infections caused by pathogens sensitive to them. They are mainly used for upper respiratory tract infections, in the treatment of sore throat, scarlet fever, otitis, sepsis, syphilis, gonorrhea, gastrointestinal infections, urinary tract infections, etc.
Penicillins should only be used as directed and under the supervision of a physician. It must be remembered that the use of insufficient doses of penicillins (as well as other antibiotics) or stopping treatment too early can lead to the development of resistant strains of microorganisms (this is especially true for natural penicillins). If resistance occurs, therapy with other antibiotics should be continued.
The use of penicillins in ophthalmology. In ophthalmology, penicillins are used topically in the form of instillations, subconjunctival and intravitreal injections. Penicillins do not pass well through the blood-ophthalmic barrier. On the background inflammatory process their penetration into the internal structures of the eye increases and their concentrations reach therapeutically significant levels. So, when instilled in conjunctival sac therapeutic concentrations of penicillins are determined in the stroma of the cornea; when applied topically, they practically do not penetrate into the moisture of the anterior chamber. With subconjunctival administration, drugs are detected in the cornea and the humor of the anterior chamber of the eye, in vitreous body- concentrations below therapeutic.
Solutions for local application prepare ex tempore. Penicillins are used to treat gonococcal conjunctivitis (benzylpenicillin), keratitis (ampicillin, benzylpenicillin, oxacillin, piperacillin, etc.), canaliculitis, especially caused by actinomycetes (benzylpenicillin, phenoxymethylpenicillin), abscess and orbital phlegmon (ampicillin/clavulanate, ampicillin/sulb actam, phenoxymethylpenicillin and etc.) and other eye diseases. In addition, penicillins are used for the prevention infectious complications for injuries of the eyelids and orbit, especially when a foreign body penetrates into the orbital tissue (ampicillin/clavulanate, ampicillin/sulbactam, etc.).
The use of penicillins in urological practice. In urological practice, inhibitor-protected drugs are widely used among penicillin antibiotics (the use of natural penicillins, as well as the use of semi-synthetic penicillins as drugs of choice is considered unjustified due to the high level of resistance of uropathogenic strains.
Side and toxic effects of penicillins. Penicillins have the lowest toxicity among antibiotics and a wide range of therapeutic effects (especially natural ones). Most serious side effects are related to hypersensitivity. Allergic reactions are observed in a significant number of patients (according to various sources, from 1 to 10%). Penicillins are more likely than drugs from other pharmacological groups to cause drug allergies. In patients who have had a history of allergic reactions to the administration of penicillins, with subsequent use these reactions are observed in 10-15% of cases. Less than 1% of people who have not previously experienced such reactions have an allergic reaction to penicillin when given again.
Penicillins can cause an allergic reaction at any dose and in any dosage form.
When using penicillins, both immediate and delayed allergic reactions are possible. It is believed that an allergic reaction to penicillins is associated mainly with an intermediate product of their metabolism - the penicillin group. It is called a large antigenic determinant and is formed when the beta-lactam ring ruptures. Small antigenic determinants of penicillins include, in particular, unchanged penicillin molecules and benzyl penicilloate. They are formed in vivo, but are also determined in penicillin solutions prepared for administration. It is believed that early allergic reactions to penicillins are mediated mainly by IgE antibodies to small antigenic determinants, delayed and late (urticaria) - usually by IgE antibodies to large antigenic determinants.
Hypersensitivity reactions are caused by the formation of antibodies in the body and usually occur within a few days of starting penicillin use (times can range from a few minutes to several weeks). In some cases, allergic reactions manifest themselves in the form of skin rash, dermatitis, and fever. In more severe cases, these reactions are manifested by swelling of the mucous membranes, arthritis, arthralgia, kidney damage and other disorders. Possible anaphylactic shock, bronchospasm, abdominal pain, cerebral edema and other manifestations.
A severe allergic reaction is an absolute contraindication to future administration of penicillins. The patient must be explained that even a small amount of penicillin that enters the body with food or during a skin test can be fatal to him.
Sometimes the only symptom allergic reaction to penicillins is fever (the nature is constant, remitting or intermittent, sometimes accompanied by chills). Fever usually disappears 1-1.5 days after stopping the drug, but sometimes it can last for several days.
All penicillins are characterized by cross-sensitization and cross-allergic reactions. Any preparations containing penicillin, including cosmetics, and food products, may cause sensitization.
Penicillins can cause various side and toxic effects of a non-allergic nature. These include: when taken orally - irritating effects, incl. glossitis, stomatitis, nausea, diarrhea; with intramuscular injection - pain, infiltration, aseptic muscle necrosis; with intravenous administration - phlebitis, thrombophlebitis.
There may be an increase in reflex excitability of the central nervous system. When using high doses, neurotoxic effects may occur: hallucinations, delusions, dysregulation of blood pressure, convulsions. Seizures are more likely in patients receiving high doses of penicillin and/or in patients with severely impaired liver function. Due to the risk of severe neurotoxic reactions, penicillins cannot be administered endolumbarally (with the exception of benzylpenicillin sodium salt, which is administered extremely carefully, for health reasons).
When treated with penicillins, the development of superinfection, candidiasis of the oral cavity, vagina, and intestinal dysbiosis is possible. Penicillins (usually ampicillin) can cause antibiotic-associated diarrhea.
The use of ampicillin leads to the appearance of an “ampicillin” rash (in 5-10% of patients), accompanied by itching and fever. This side effect most often occurs on the 5-10th day of using large doses of ampicillin in children with lymphadenopathy and viral infections or with concomitant use of allopurinol, as well as in almost all patients with infectious mononucleosis.
Specific adverse reactions when using bicillins are local infiltrates and vascular complications in the form of Aune syndrome (ischemia and gangrene of the limbs when accidentally introduced into an artery) or Nicolau syndrome (embolism of pulmonary and cerebral vessels when it enters a vein).
When using oxacillin, hematuria, proteinuria, and interstitial nephritis are possible. The use of antipseudomonas penicillins (carboxypenicillins, ureidopenicillins) may be accompanied by the appearance of allergic reactions, symptoms of neurotoxicity, acute interstitial nephritis, dysbacteriosis, thrombocytopenia, neutropenia, leukopenia, eosinophilia. When using carbenicillin, hemorrhagic syndrome is possible. Combined drugs containing clavulanic acid can cause acute liver damage.
Use during pregnancy. Penicillins pass through the placenta. Although adequate and strictly controlled safety studies in humans have not been conducted, penicillins, incl. inhibitor-protected, are widely used in pregnant women, with no complications recorded.
In studies on laboratory animals, when penicillins were administered in doses 2-25 (for different penicillins) higher than therapeutic ones, fertility disorders and effects on reproductive function not detected. Teratogenic, mutagenic, embryotoxic properties were not detected when penicillins were administered to animals.
In accordance with the internationally recognized FDA (Food and Drug Administration) recommendations, which determine the possibility of using drugs during pregnancy, drugs of the penicillin group for their effect on the fetus belong to FDA category B (reproduction studies in animals did not reveal any adverse effects of drugs on the fetus, but adequate and There are no strictly controlled studies in pregnant women).
When prescribing penicillins during pregnancy, one should (as with any other drugs) take into account the duration of pregnancy. During therapy, it is necessary to strictly monitor the condition of the mother and fetus.
Use during breastfeeding. Penicillins pass into breast milk. Although no significant complications have been reported in humans, the use of penicillins by nursing mothers can lead to sensitization of the child, changes in intestinal microflora, diarrhea, the development of candidiasis and the appearance of skin rashes in infants.
Pediatrics. When using penicillins in children, no specific pediatric problems have been reported, however, it should be borne in mind that insufficiently developed kidney function in newborns and young children can lead to the accumulation of penicillins (and therefore there is an increased risk of neurotoxicity with the development of seizures).
Geriatrics. No specific geriatric problems have been reported with the use of penicillins. However, it should be remembered that in older people, age-related renal dysfunction is more likely, and therefore dose adjustment may be required.
Impaired kidney and liver function. In case of renal/liver failure, cumulation is possible. In case of moderate and severe insufficiency of renal and/or liver function, dose adjustment and an increase in the periods between administrations of the antibiotic are required.
Interaction of penicillins with other drugs. Bactericidal antibiotics (including cephalosporins, cycloserine, vancomycin, rifampicin, aminoglycosides) have a synergistic effect, bacteriostatic antibiotics (including macrolides, chloramphenicol, lincosamides, tetracyclines) have an antagonistic effect. Caution must be exercised when combining penicillins active against Pseudomonas aeruginosa. (Pseudomonas aeruginosa), with anticoagulants and antiplatelet agents (potential risk of increased bleeding). It is not recommended to combine penicillins with thrombolytics. When combined with sulfonamides, the bactericidal effect may be weakened. Oral penicillins may reduce the effectiveness of oral contraceptives due to disruption of the enterohepatic circulation of estrogen. Penicillins can slow down the elimination of methotrexate from the body (inhibit its tubular secretion). When ampicillin is combined with allopurinol, the likelihood of skin rash increases. The use of high doses of benzylpenicillin potassium salt in combination with potassium-sparing diuretics, potassium supplements or ACE inhibitors increases the risk of hyperkalemia. Penicillins are pharmaceutically incompatible with aminoglycosides.
Due to the fact that with long-term orally antibiotics can suppress the intestinal microflora that produces vitamins B1, B6, B12, PP; it is advisable to prescribe B vitamins to patients to prevent hypovitaminosis.
In conclusion, it should be noted that penicillins are a large group of natural and semi-synthetic antibiotics that have a bactericidal effect. The antibacterial effect is associated with a violation of the synthesis of cell wall peptidoglycan. The effect is due to the inactivation of the enzyme transpeptidase, one of the penicillin-binding proteins located on the inner membrane of the bacterial cell wall, which takes part in the later stages of its synthesis. The differences between penicillins are associated with the characteristics of their spectrum of action, pharmacokinetic properties and the range of undesirable effects.
Over several decades of successful use of penicillins, problems associated with their misuse have arisen. Thus, prophylactic administration of penicillins at risk of bacterial infection is often unjustified. Incorrect treatment regimen - incorrect selection of dose (too high or too low) and frequency of administration can lead to the development of side effects, decreased effectiveness and the development of drug resistance.
Thus, currently most strains Staphylococcus spp. resistant to natural penicillins. In recent years, the frequency of detection of resistant strains has increased Neisseria gonorrhoeae.
The main mechanism of acquired resistance to penicillins is associated with the production of beta-lactamases. To overcome the widespread acquired resistance among microorganisms, compounds have been developed that can irreversibly inhibit the activity of these enzymes, the so-called. beta-lactamase inhibitors - clavulanic acid (clavulanate), sulbactam and tazobactam. They are used to create combined (inhibitor-protected) penicillins.
It should be remembered that the choice of one or another antibacterial drug, incl. penicillin should be determined, first of all, by the sensitivity of the pathogen that caused the disease to it, as well as the absence of contraindications to its use.
Penicillin is the very first in the world, which became a real salvation for millions of people. With its help, doctors were able to declare war on diseases that were considered fatal at that time: pneumonia, tuberculosis,. However, treatment of pathologies with antibiotics should be carried out only after an accurate diagnosis has been established and strictly as prescribed by the doctor.
History of discovery
The discovery of the antibacterial properties of penicillin occurred in 1928. The famous scientist Alexander Fleming, as a result of conducting a routine experiment with colonies, discovered stains of ordinary mold in some cups with cultures.
As it turned out upon further study, there were no harmful bacteria in the cups with mold stains. Subsequently, it was from ordinary green mold that a molecule was derived that was capable of killing bacteria. This is how the first modern antibiotic, Penicillin, appeared.
Penicillium group
Nowadays, penicillins are a whole group of antibiotics produced by certain types of mold (genus Penicillium).
They can be active against entire groups of gram-positive microorganisms, as well as some gram-negative ones: staphylococci, spirochetes, meningococci.
Penicillins belong to a large group of beta-lactam antibiotics, which contain a special beta-lactam ring molecule.
Indications
Antibiotics of the penicillin group are used in the treatment of a huge number of infectious diseases. They are prescribed when pathogenic microorganisms are sensitive to the drug for the treatment of the following pathologies:
- many types of pneumonia;
- osteomyelitis;
- infections genitourinary system, most of the gastrointestinal tract;
- scarlet fever;
- diphtheria;
- anthrax;
- gynecological diseases;
- diseases of the ENT organs;
- syphilis, gonorrhea and many others.
This type of antibiotic is also used in the treatment of wounds infected with bacteria. As a prevention of purulent complications, the drug is prescribed in the postoperative period.
The drug can be used in childhood for umbilical sepsis, pneumonia, otitis in newborns and infants, as well as young children. Penicillin is also effective for purulent pleurisy and meningitis.
Use of penicillin in medicine:
Contraindications
The use of penicillins to treat infections is not always possible. People who are highly sensitive to the drug are strictly prohibited from taking the drug.
The use of this antibiotic is also contraindicated in patients suffering from asthma of various origins, hay fever, or a history of other active substances.
Release form
Modern pharmacological companies produce penicillin preparations for injections or in tablet form. Products for intramuscular administration are produced in bottles (made of glass), sealed with rubber stoppers and metal caps on top. Before administration, the substrate is diluted with sodium chloride or water for injection.
Tablets are produced in cell packaging in dosages from 50 to 100 thousand units. It is also possible to produce ecmoline lozenges. Dosage in in this case does not exceed 5 thousand units.
Mechanism of action
The mechanism of action of penicillin is the inhibition of enzymes involved in the formation of the cell membrane of microorganisms. The cell membrane protects bacteria from environmental influences; disruption of its synthesis leads to the death of pathogenic agents.
This is the bactericidal effect of the drug. It acts on some types of gram-positive bacteria (streptococci and staphylococci), as well as several types of gram-negative ones.
It is worth noting that penicillins can only act on multiplying bacteria. In inactive cells, membranes are not built, so they do not die due to enzyme inhibition.
Instructions for use
The antibacterial effect of penicillin is achieved when intramuscular injection, when taken orally, as well as when local action. More often, the injection form is used for treatment. When administered intramuscularly, the drug is quickly absorbed into the blood.
However, after 3-4 hours it completely disappears from the blood. Therefore, regular administration of the drugs at equal intervals from 4 times a day is recommended.
The drug can be administered intravenously, subcutaneously, or into the spinal canal. For the treatment of complex pneumonia, meningitis or syphilis, a special regimen is prescribed, which can only be prescribed by a doctor.
When taking penicillin in tablet form, the dosage must also be determined by your doctor. As a rule, for bacterial infections, 250-500 mg is prescribed every 6-8 hours. If necessary, a single dose can be increased to 750 mg. The tablets should be taken half an hour before meals or 2 hours after. The duration of the course will be determined by the doctor.
Side effects
Since penicillins are a natural drug, they have minimal toxicity among other groups of artificially bred antibiotics. However, allergic reactions are still possible.
The tablet form of penicillin should be taken with plenty of liquid. During treatment with penicillin antibiotics, it is important not to skip the recommended doses, since the effect of the drug may be weakened. If this happens, the missed dose should be taken as quickly as possible.
It happens that after 3-5 days after regular use or administration of the drug, improvement does not occur, then you should consult a doctor to adjust the course of treatment or dose of the drug. It is not recommended to interrupt the course of treatment without consulting a doctor.
Rules for the use of antibiotics:
Drug interactions
When prescribing penicillin, attention should be paid to its interaction with other drugs used. This antibiotic should not be combined with the following medications:
- reduces the effectiveness of penicillin antibiotics.
- Aminoglycosides can conflict with penicillin in a chemical aspect.
- Sulfonamides also reduce the bactericidal effect.
- Thrombolytics.
Penicillin price
Penicillin is considered one of the most inexpensive antibacterial drugs. The price of 50 bottles of powder to create a solution varies from 280 to 300 rubles. The cost of 250 mg tablets numbered 30 is just over 50 rubles.
Cheap
Cheap analogues of penicillin include Ampicillin and Bicillin. Their cost in tablet form also does not exceed 50 rubles.
Drug synonyms
Synonyms for the drug are Procaine-benzylpenicillin, Benzylpenicillin sodium, potassium, novocaine salt.
Natural analogues
Natural medicinal penicillins include:
- Phenkoxymethylpenicillin;
- Benzathine benzylpenicillin;
- Benzylpenicillin salts (sodium, potassium, novocaine).
Conditions for dispensing from pharmacies
On prescription.
Storage conditions and shelf life
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Mushrooms are a kingdom of living organisms. Mushrooms are different: some of them end up in our diet, others cause skin diseases, and others are so poisonous that they can lead to death. But fungi of the genus Penicillium save millions of human lives from pathogenic bacteria.
Penicillin antibiotics are still used in medicine.
Discovery of penicillin and its properties
In the 30s of the last century, Alexander Fleming conducted experiments with staphylococci. He studied bacterial infections. Having grown a group of these pathogens in a nutrient medium, the scientist noticed that there were areas in the dish around which there were no living bacteria. The investigation showed that ordinary green mold, which likes to settle on stale bread, is to blame for these stains. The mold was called Penicillium and, as it turned out, produced a substance that kills staphylococci.
Fleming studied this issue further and soon isolated pure penicillin, which became the world's first antibiotic. The principle of action of the medicine is as follows: when a bacterial cell divides, each half restores its cell membrane using a special chemical element - peptidoglycan. Penicillin blocks the formation of this element, and the bacterial cell simply “resolves” in the environment.
Ask your question to a neurologist for free
Irina Martynova. Graduated from Voronezh State Medical University named after. N.N. Burdenko. Clinical resident and neurologist of the BUZ VO \"Moscow Polyclinic\".
But difficulties soon arose. Bacterial cells learned to resist the drug - they began to produce an enzyme called beta-lactamase, which destroys beta-lactams (the basis of penicillin).
Expert opinion
Astafiev Igor Valentinovich
Neurologist - Pokrovsk City Hospital. Education: Volgograd State Medical University, Volgograd. Kabardino-Balkarian State University them. HM. Berbekova, Nalchik.
For the next 10 years, an invisible war took place between pathogens that destroy penicillin, and scientists who modify this penicillin. This is how many modifications of penicillin were born, which now form the entire penicillin series of antibiotics.
Pharmacokinetics and principle of action
The drug for any method of use spreads quickly throughout the body, penetrating almost all its parts. Exceptions: cerebrospinal fluid, prostate and visual system. In these places the concentration is very low; under normal conditions it does not exceed 1%. With inflammation, a rise of up to 5% is possible.
Antibiotics do not affect the cells of the human body, since the latter do not contain peptidoglycan.
The medicine is quickly eliminated from the body; after 1-3 hours, most of it exits through the kidneys.
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Classification of antibiotics
All drugs are divided into: natural (short and long-acting) and semi-synthetic (antistaphylococcal, broad-spectrum drugs, antipseudomonas).
Natural
These drugs obtained directly from mold. At the moment, most of them are obsolete, as pathogens have developed immunity to them. In medicine, benzylpenicillin and Bicillin are most often used, which are effective against gram-positive bacteria and cocci, some anaerobic bacteria and spirochetes. All these antibiotics are used only as injections into the muscles, since the acidic environment of the stomach quickly destroys them.
Benzylpenicillin in the form of sodium and potassium salts is a natural antibiotic short acting. Its effect wears off after 3-4 hours, so frequent repeated injections are necessary.
Trying to eliminate this deficiency, pharmacists created natural long-acting antibiotics: Bicillin and benzylpenicillin novocaine salt. These drugs are called “depot forms” because after injection into the muscle they form a “depot” in it, from which the drug is slowly absorbed into the body.
Expert opinion
Mitrukhanov Eduard Petrovich
Doctor - neurologist, city clinic, Moscow. Education: Russian State Medical University, Russian State Budgetary Educational Institution of Further Professional Education medical Academy postgraduate education of the Ministry of Health of the Russian Federation, Volgograd State Medical University, Volgograd.
Examples of drugs: benzylpenicillin salt (sodium, potassium or novocaine), Bicillin-1, Bicillin-3, Bicillin-5.
Semi-synthetic antibiotics of the penicillin group
Several decades after penicillin was obtained pharmacists were able to isolate its main active ingredient, and the process of modification began. Most drugs, after improvement, became resistant to the acidic environment of the stomach, and semi-synthetic penicillins began to be produced in tablets.
Isoxazolepenicillins are drugs that are effective against staphylococci. The latter have learned to produce an enzyme that destroys benzylpenicillin, and drugs from this group prevent their production of the enzyme. But you have to pay for the improvement - drugs of this type are less well absorbed in the body and have a smaller spectrum of action compared to natural penicillins. Examples of drugs: Oxacillin, Nafcillin.
Aminopenicillins are broad-spectrum drugs. They are inferior to benzylpenicillins in the fight against gram-positive bacteria, but cover a wider range of infections. Compared to other drugs, they remain in the body longer and penetrate better through some body barriers. Examples of drugs: Ampicillin, Amoxicillin. You can often find Ampiox - Ampicillin + Oxacillin.
Carboxypenicillins and ureidopenicillins – antibiotics effective against Pseudomonas aeruginosa. At the moment, they are practically not used, since infections quickly become resistant to them. Occasionally you can find them as part of a comprehensive treatment.
Examples of drugs: Ticarcillin, Piperacillin
List of drugs
Pills
Sumamed
Active ingredient: azithromycin.
Indications: respiratory tract infections.
Contraindications: intolerance, severe renal failure, children under 6 months of age.
Price: 300-500 rubles.
Oxacillin
Active ingredient: oxacillin.
Indications: infections sensitive to the drug.
Price: 30-60 rubles.
Amoxicillin Sandoz
Indications: respiratory tract infections (including sore throat, bronchitis), genitourinary system infections, skin infections, other infections.
Contraindications: intolerance, children under 3 years of age.
Price: 150 rubles.
Ampicillin trihydrate
Indications: pneumonia, bronchitis, tonsillitis, other infections.
Contraindications: hypersensitivity, liver failure.
Price: 24 rubles.
Phenoxymethylpenicillin
Active ingredient: phenoxymethylpenicillin.
Indications: streptococcal diseases, mild to moderate infections.
Price: 7 rubles.
Amoxiclav
Active ingredient: amoxicillin + clavulanic acid.
Indications: respiratory tract infections, urinary system, infections in gynecology, other infections sensitive to amoxicillin.
Contraindications: hypersensitivity, jaundice, mononucleosis and lymphocytic leukemia.
Price: 116 rubles.
Injections
Bicillin-1
Active ingredient: benzathine benzylpenicillin.
Indications: acute tonsillitis, scarlet fever, wound infections, erysipelas, syphilis, leishmaniasis.
Contraindications: hypersensitivity.
Price: 15 rubles per injection.
Ospamox
Active ingredient: amoxicillin.
Indications: infections of the lower and upper respiratory tract, gastrointestinal tract, genitourinary system, gynecological and surgical infections.
Contraindications: hypersensitivity, severe gastrointestinal infections, lymphocytic leukemia, mononucleosis.
Price: 65 rubles.
Ampicillin
Active ingredient: ampicillin.
Indications: infections of the respiratory and urinary tract, gastrointestinal tract, meningitis, endocarditis, sepsis, whooping cough.
Contraindications: hypersensitivity, impaired renal function, childhood, pregnancy.
Price: 163 rubles.
Benzylpenicillin
Indications: severe infections, congenital syphilis, abscesses, pneumonia, erysipelas, anthrax, tetanus.
Contraindications: intolerance.
Price: 2.8 rubles per injection.
Benzylpenicillin novocaine salt
Active ingredient: benzylpenicillin.
Indications: similar to benzylpenicillin.
Contraindications: intolerance.
Price: 43 rubles for 10 injections.
Amoxiclav, Ospamox, Oxacillin are suitable for treating children. But Before using the medicine, you must consult your doctor to adjust the dose.
Indications for use
Antibiotics of the penicillin group are prescribed for infections; the type of antibiotics is selected based on the type of infection. These can be various cocci, rods, anaerobic bacteria, and so on.
Most often, infections of the respiratory tract and genitourinary system are treated with antibiotics.
Features of application
When treating children, follow the instructions of the doctor who prescribes the right antibiotic and adjust the dose.
In case of pregnancy, antibiotics must be used with extreme caution, as they penetrate into the fetus. During lactation, it is better to switch to mixtures, since the medicine also penetrates into the milk.
There are no special guidelines for older people, although the doctor should consider the condition of the patient's kidneys and liver when prescribing treatment.
Contraindications and side effects
The main and, often, the only contraindication is individual intolerance. It occurs frequently - in approximately 10% of patients. Additional contraindications depend on the specific antibiotic and are specified in its instructions for use.
List of side effects
- The development of allergies - from itching and fever to anaphylactic shock and coma.
- Instant development of an allergic reaction in response to the administration of the drug into a vein.
- Dysbacteriosis, candidiasis.
If side effects occur, you should immediately seek medical help, discontinue the drug and carry out symptomatic treatment.
Content
The first antibiotics were penicillin drugs. Medicines have helped save millions of people from infections. The drugs are still effective today - they are constantly modified and improved. Many popular antimicrobial agents have been developed based on penicillins.
General information about penicillin antibiotics
The first antimicrobial drugs developed on the basis of waste products of microorganisms are penicillins (Penicillium). Benzylpenicillin is considered their ancestor. The substances belong to a wide range of β-lactam antibiotics. A common feature beta-lactam group is the presence of a four-membered beta-lactam ring in the structure.
Penicillin antibiotics inhibit the synthesis of a special polymer - peptidoglycan. It is produced by the cell to build the membrane, and penicillins prevent the formation of the biopolymer, which leads to the impossibility of cell formation, causes lysis of the exposed cytoplasm and death of the microorganism. On cellular structure In humans or animals, the medicine does not have a harmful effect due to the fact that there is no peptidoglycan in their cells.
Penicillins combine well with other medications. Their effectiveness weakens with complex treatment together with bacteriostatics. The penicillin series of antibiotics is effectively used in modern medicine. This is possible due to the following properties:
- Low toxicity. Among all antibacterial drugs, penicillins have the smallest list of side effects, provided they are prescribed correctly and the instructions are followed. Medicines are approved for use in the treatment of newborns and pregnant women.
- Wide range actions. Modern penicillin antibiotics are active against most gram-positive and some gram-negative microorganisms. Substances are resistant to alkaline environment stomach and penicillinase.
- Bioavailability. The high level of absorption ensures the ability of beta-lactams to quickly spread through tissues, penetrating even into the cerebrospinal fluid of the brain.
Classification of penicillin antibiotics
Antimicrobial agents based on penicillin are classified according to many criteria - affiliation, compatibility, mechanism of action. The inability of natural penicillin substances to resist penicillinase determined the need to create synthetic and semi-synthetic drugs. Based on this, classification of this type antibiotics by production method is informative for understanding pharmacological properties penicillins.
Biosynthetic
Benzylpenicillin is produced by molds Penicillium chrysogenum and Penicillium notatum. By molecular structure the active substance is an acid. For medicine it chemically combine with potassium or sodium, resulting in salts. They are the basis of powders for injection solutions, which are quickly absorbed into tissues. The therapeutic effect occurs within 10-15 minutes after administration, but after 4 hours the effect of the substance ends. This necessitates the need for multiple injections.
The active substance quickly penetrates into the mucous membranes and lungs, and to a lesser extent into the bones, myocardium, synovial and cerebrospinal fluid. To prolong the action of drugs, benzylpenicillin is combined with novocaine. The resulting salt at the injection site forms a medicinal depot, from where the substance slowly and constantly enters the blood. This helped reduce the number of injections to 2 times a day while maintaining the therapeutic effect. These drugs are aimed at long-term treatment of syphilis, streptococcal infections, and rheumatism.
Biosynthetic penicillins are active against most pathogenic microorganisms, except spirochetes. To treat moderate infections, a benzylpenicillin derivative, phenoxymethylpenicillin, is used. The substance is resistant to of hydrochloric acid stomach juice, so it is produced in tablet form and administered orally.
Semi-synthetic antistaphylococcal
Natural benzylpenicillin is not active against staphylococcus strains. For this reason, oxacillin was synthesized, which inhibits the action of beta-lactamases of the pathogen. Semi-synthetic penicillins include methicillin, dicloxacillin, cloxacillin. These drugs are rarely used in modern medicine due to their high toxicity.
Aminopenicillins
This group of antibiotics includes ampicillin, amoxicillin, talampicillin, bacampicillin, pivampicillin. The agents are active against a wide range of pathogens and are available in tablets. The disadvantage of the drugs is the ineffectiveness of amoxicillin and ampicillin against staphylococcus strains. To treat such diseases, substances are combined with oxacillin.
Aminopenicillins are rapidly absorbed and act for a long time. 2-3 tablets are prescribed per day according to the doctor’s decision. The only side effects observed are allergic rash, which quickly passes after discontinuation of the drug. The drugs are used to treat the following conditions:
- upper respiratory and urinary tract infections;
- sinusitis;
- enterocolitis;
- otitis;
- causative agent of stomach ulcers (Helicobacter pylori).
Antipseudomonas
Antibiotics of the penicillin group have a similar effect to aminopenicillins. The exception is pseudomonas. The substances are effective in the treatment of diseases caused by Pseudomonas aeruginosa. Drugs in this group include:
Inhibitor-protected combination
Drugs in this group are artificially synthesized to increase the resistance of the active substance to most microorganisms. Medicines are obtained by combining with clavulanic acid, tazobactam, sulbactam, which provide immunity to beta-lactamases. Protected penicillins have their own antibacterial effect, enhancing the effect of the main substance. The drugs are successfully used in the treatment of severe nosocomial infections.
Penicillin tablets
The use of penicillin tablets is convenient and beneficial for patients. There is no need to spend money on injection syringes; treatment is carried out at home yourself. Penicillin antibiotics:
|
Name |
Active substance |
Indications |
Contraindications |
Price, rub |
|
Azithromycin |
Azithromycin dihydrate |
Acute bronchitis, impetigo, chlamydial urethritis, borreliosis, erythema |
Kidney disease, intolerance to components, myasthenia gravis |
|
|
Oxacillin |
oxacillin |
Infections of joints, bones, skin, sinusitis, bacterial meningitis and endocarditis |
Hypersensitivity to penicillins |
|
|
Amoxicillin Sandoz |
amoxicillin |
Tonsillitis, bacterial pharyngitis and enteritis, community-acquired pneumonia, cystitis, endocarditis |
Sensitivity to penicillin, cross-allergy with other beta-lactams |
|
|
Phenoxymethylpenicillin |
phenoxymethylpenicillin |
Sore throat, bronchitis, pneumonia, syphilis, gonorrhea, tetanus, anthrax |
Pharyngitis, aphthous stomatitis, sensitivity to penicillins |
|
|
Ampicillin |
ampicillin trihydrate |
Infections of the gastrointestinal tract, bronchopulmonary and urinary tract, meningitis, sepsis, erysipelas |
Lymphocytic leukemia, infectious mononucleosis, liver dysfunction |
|
|
Amoxicillin |
amoxicillin |
Urethritis, pyelonephritis, pneumonia, bronchitis, listeriosis, gonorrhea, leptospirosis, Helicobacter |
Allergic diathesis, hay fever, infectious mononucleosis, asthma, lymphocytic leukemia, liver, blood and central nervous system diseases |
|
|
azithromycin |
Infections of soft tissues, skin, respiratory tract, Lyme disease, cervicitis, urethritis |
Sensitivity to azithromycin, liver disease, combination with dihydroergotamine and ergotamine |
||
|
Amoxiclav |
amoxicillin, clavulanate |
Acute otitis media, sinusitis, bronchitis, retropharyngeal abscess, pneumonia, skin infections, gynecological, biliary tract, connecting and bone tissue |
Liver diseases, lymphocytic leukemia, infectious mononucleosis, hypersensitivity to penicillins |
In injections
For injection, penicillin G sodium salt is used 500 thousand or 1 million units. The powder is dispensed in glass bottles sealed with a rubber cap. Before use, the product is diluted with water. Examples of drugs:
|
Name |
Active substance |
Indications |
Contraindications |
Price, rub |
|
Ampicillin |
ampicillin sodium salt |
Cystitis, pyelonephritis, bacterial sinusitis, intra-abdominal and female genital infections |
Liver and kidney disorders, colitis, leukemia, HIV |
|
|
Bicillin-1 |
benzathine benzylpenicillin |
Syphilis, scarlet fever, bacterial infection skin |
Intolerance to components, tendency to allergies |
|
|
Benzylpenicillin |
benzylpenicillin |
Sepsis, pyemia, osteomyelitis, meningitis, diphtheria, actinomycosis, scarlet fever, blenorrhea |
Hypersensitivity to penicillins and cephalosporins |
|
|
Ospamox |
amoxicillin |
Pneumonia, otitis media, bronchitis, prostatitis, endometritis, gonorrhea, erysipelas, typhoid fever, listeriosis |
Epilepsy, acute lymphocytic leukemia, asthma, allergic diathesis, hay fever |
|
|
Benzylpenicillin novocaine salt |
benzylpenicillin |
Lobar and focal pneumonia, syphilis, diphtheria, meningitis, septicemia, blenorrhea |
Hypersensitivity to penicillins, epilepsy - for endolumbar injections |
