Even less than a hundred years ago, many bacterial infections caused real pandemics and were fatal. Everything changed after the discovery of Fleming substances with antibacterial properties. The first antibiotic was penicillin. It began to be widely used during the Second World War to stop the development of purulent processes.
Today, even a special classification of penicillins has been developed, with the help of which they are divided according to different characteristics, since there are a lot of substances, and they are different. Despite the fact that many more modern synthetic antibiotics and other series have appeared, penicillins are still popular and widely used in medical practice.
General characteristics of penicillins
What group of antibiotics this substance includes is known to everyone. After all, penicillins are the most common antibacterial drugs. They relate to beta-lactams. This is a large group of antibacterial drugs that are similar in structure. They are most often used now to treat most infectious diseases. The first beta-lactam penicillin antibiotic was obtained from mold. Now this group includes many natural, semi-synthetic and synthetic substances with a wide spectrum of action.
These substances are able to inhibit the growth and reproduction of bacterial cells. Their action is based on blocking the synthesis of peptidoglycan, which leads to the death of microorganisms. Moreover, they do not act on living cells. Only bacterial, whose vital activity is precisely based on peptidoglycans. Penicillins are effective against gram-positive and gram-negative bacteria. Therefore, they are widely used in medical practice for the treatment of various infectious diseases.
All penicillins are well absorbed and distributed throughout the body. They penetrate into fluids and tissues, reaching a therapeutic concentration in a short time. But they are also quickly excreted from the body, mainly by the kidneys. Such antibiotics are most often used parenterally. Some of them are available in the form of tablets or suspensions for oral administration. Penicillins are also part of some antibacterial ointments, eye drops or sprays for the treatment of nasopharyngeal infections.
Advantages and disadvantages
Penicillins are the most common in medical practice due to a wide spectrum of action and low toxicity. They are used to treat tonsillitis, pneumonia, diphtheria, scarlet fever, meningitis, osteomyelitis. Purulent infections of the skin and soft tissues - erysipelas, abscess, as well as syphilis, gonorrhea, anthrax respond well to therapy. Most infectious diseases of ENT organs are also successfully treated with these drugs. Side effects in their use are rare and are mainly expressed by an allergic reaction.
The use of penicillins in medical practice over time has led to the fact that resistance to them has often become diagnosed. The number of cases of resistance of microorganisms to therapy with this substance is increasing. This also happens due to non-compliance with the intake regimen and unreasonable prescription of these drugs for prevention. Therefore, penicillins are not always effective. In addition, most of them can be used only in the form of injections, since they are destroyed by gastric juice.
Penicillin classification
In pharmacology, different principles are used to distinguish these drugs into groups. Species are distinguished by structure, principle of action, and by generation. The first generation of penicillins in the classification contains natural antibiotics - benzylpenicillins obtained from molds. Their peculiarity lies in the fact that they are very unstable, destroyed by the enzyme penicillinase produced by many bacteria, as well as the acidic environment of the stomach. Therefore, these antibiotics are most often used as injections. They are also called natural penicillins due to the fact that they are produced by mold fungi. The drugs have a narrow focus and are quite unstable. In addition, many bacteria quickly develop resistance to them.
Therefore, biosynthetic penicillins were created. In the classification, they include benzylpenicillin sodium salt, phenoxymethylpenicillin and benzathine benzylpenicillin. The most famous drug in this group is Bicillin. It is used for severe inflammatory diseases, meningitis, osteomyelitis, streptococcal infections.
Semi- synthetic penicillins are more modern . In the classification, several subgroups belong to them:
- oxacillin;
- aminopenicillins;
- carboxypenicillins;
- ureidopenicillins.
Inhibitor-protected preparations are isolated in which the main active ingredient is combined with clavulanic acid or sulbactam. This makes them more resilient and expands the spectrum of action. Sometimes in the classification of penicillins, their route of administration is taken into account, therefore, drugs for parenteral and oral administration are isolated.
Natural penicillins
These include various varieties of benzylpenicillin - preparations "Benzylpenicillin", "Bicillin", "Extentsillin", "Retarpen", "Procain penicillin." These drugs are active mainly in the treatment of infections caused by gram-positive bacteria. Against staphylococci, they are ineffective, since they are destroyed by their beta-lactamases. Natural penicillins are used in the form of injections due to instability to the action of the acidic environment of the stomach. The disadvantage is also the rapid elimination, which requires the use of the drug every 3-4 hours.
Used "Benzylpenicillin" and "Bicillin" with streptococcal tonsillitis, meningitis, scarlet fever, erysipelas, tonsillitis, endocarditis. These drugs are chosen for the treatment of gas gangrene, Lyme disease, leptospirosis, syphilis. To increase the stability of the active substance and lengthen the duration of action, it is combined with novocaine. This combination is present in the preparation "procaine benzylpenicillin." It is used in the chronic course of severe infections, for example, with syphilis or diphtheria.
"Oxacillin"
In the classification of penicillins, this drug belongs to isoxazolylpenicillins. In this group there are also Cloxacillin, Flucloxacillin, Methicillin, Nafcillin and Dicloxacillin, but they are used very rarely due to their high toxicity. The spectrum of action is similar to natural antibiotics. But sometimes they are also called staphylococcal penicillins, since they are more active against these bacteria.
"Oxacillin" or its analogue "Prostaflin" can be used as an injection, as for oral administration. It is rapidly absorbed and distributed in the tissues. This drug is used for pneumonia, sepsis, meningitis, various infections of the skin, joints and soft tissues.
Aminopenicillins
This group of penicillins includes Amoxicillin and Ampicillin. Medicines with a wide spectrum of action, many gram-positive and gram-negative bacteria are sensitive to them. Indications for the use of these penicillin preparations include the following diseases:
- Sinusitis, acute bronchitis, pneumonia.
- Cystitis, pyelonephritis.
- Meningitis.
- Acute intestinal infections, salmonellosis.
- Cholecystitis.
Amoxicillin is the most common penicillin antibiotic. In the classification, it belongs to the first generation of drugs, but has a wide spectrum of action. It is used not only in the form of injections, but also for oral administration, as it is resistant to the action of gastric juice. Therefore, it is Amoxicillin that is often used to eradicate Helicobacter pylori. The benefits of this tool also include the fact that it can be used 2-3 times a day. Amosicillin active preparations include Amosin, Espomox, Hiconcil, and others.
Inhibitor-resistant penicillins are formed in combination with clavulanic acid or sulbactam. These substances increase their stability and expand the spectrum of action. These are the preparations Amoxiclav, Augmentin, Flemoxin Solutab, Panklav, Arlet, Ampicillin Sulbactam. In the classification of penicillins by generation, they belong to the latter. These funds are more effective and easier to tolerate.
Other drugs
In the classification of penicillins, several more groups are distinguished: carboxypenicillins, ureidopenicillins and aminopenicillins. These are rarely used drugs. Basically, they have specific properties. For example, carboxypenicillins - "Ticarcillin" and "Carbenicillin" - are used mainly against Pseudomonas aeruginosa and some types of protea that are resistant to other drugs. They are prescribed for severe infectious diseases together with other antibiotics. You can use these funds 3 times a day, but their disadvantage is the rapid development of bacterial resistance.
Other drugs of the penicillin group are also rarely used. The list of them is small, but they are sold by prescription, therefore, they are mainly used for treatment in a hospital. These are meslocillin, azlocillin, piperacillin and metsillam. They have a wide spectrum of action, but are rarely used, as they are unstable to most beta-lactamases bacteria. It is mainly used as an injection for severe pathologies: lung abscess, sepsis, purulent infections of soft tissues, postoperative complications.
There are also combination antibiotics. The most famous of them is Ampioks. It is a combination of ampicillin and oxacillin. Due to this, the spectrum of action of the drug is expanding.
Application features
Despite the fact that penicillin group preparations are considered non-toxic and rarely cause side effects, they can be used only as directed by a doctor. Often with diseases of the upper respiratory tract, people start drinking antibiotics. But it is absolutely impossible to do this, since in most cases such diseases are caused by viruses, against which penicillins are powerless, like other antibacterial agents. On the contrary, they can lead to a decrease in immunity and a worsening of the patient's condition.
When taking antibiotics, be sure to observe the following rules:
- Before choosing a drug, you need to determine the causative agent of an infectious disease and apply only one to which microorganisms are sensitive;
- treatment should be started as early as possible and not end it after the patient has become easier, as bacteria resistance to antibiotics may develop;
- it is necessary to observe certain intervals between doses of the drug;
- the duration of treatment and the dosage is prescribed by the doctor, you can not arbitrarily increase or decrease it, as this is fraught with side effects.
Contraindications
Penicillin group antibiotics are widely used due to the fact that they have few contraindications. Do not prescribe them only with individual intolerance. It is undesirable to use them also for people suffering from allergic diseases and bronchial asthma.
It is contraindicated during breastfeeding during treatment, since penicillins pass into breast milk and can cause a severe allergic reaction in the baby. During pregnancy, these drugs are used when there is an urgent need, and the risk to the mother outweighs the possible danger to the baby. Penicillins are used with caution in case of impaired liver and kidney function and in old age. In these cases, individual dose adjustment is required.
Side effects
There are many drugs in the classification of penicillins, but only a few are widely used. They are popular not only because of high efficiency and good stability. These drugs also have low toxicity and rarely cause side effects. Usually negative reactions to taking penicillins can be:
- skin rash, urticaria, itching;
- anaphylactic shock, edema, bronchospasm;
- temperature rise;
- headache;
- abdominal pain, flatulence;
- dysbiosis, candidiasis;
- nausea, vomiting;
- electrolyte imbalance, swelling;
- increase in blood pressure;
- convulsions, neurotoxic reactions;
- inflammatory processes at the injection site.
Features of treating children
It is penicillin preparations that are most often prescribed in pediatric practice. They must be used strictly as prescribed by the doctor. In severe infections such as sepsis, meningitis, or pneumonia, benzylpenicillin is usually prescribed. In milder cases (with angina, bronchitis, sinusitis), less toxic drugs such as Amoxicillin, Amoxiclav, and Augmentin are used. Moreover, now they are available in a form convenient for children to take - suspension. It is easy to dose and give to babies. The most commonly prescribed "Flemoxin Solutab."
It is very important to carefully monitor the condition of the child during antibiotic treatment. Penicillin can accumulate in tissues and cause serious negative reactions, for example, convulsions. In addition, allergic reactions in the form of urticaria are more common for antibiotics of this group. It is also important to use drugs to protect the digestive tract and strengthen immunity while using such drugs. Therefore, treatment should be comprehensive and carried out under the supervision of a doctor.