Penicillin analogues have opened up new treatment options for doctors infectious diseases. They are more resistant to the aggressive environment of the stomach, have less 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; wide application And good indicator bactericidal action, but they are found much more often than doctors would like. This is explained organic nature antibiotics. More to negative qualities It can also be difficult to combine 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 in 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 question industrial production medicines in 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

Included 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 it is impossible to apply any serious harm the drug cannot.

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 rods 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:

1. Natural, which are synthesized by fungi. These include benzylpenicillins and phenoxymethylpenicillin. These drugs have a narrow spectrum of action, mainly on
2. Semi-synthetic drugs that are resistant to penicillinases. Used for treatment wide range pathogens. Representatives: methicillin, oxacillin, nafcillin.
3. Carboxypenicillins (carbpenicillin).
4. 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. at the 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 leaders in their category until more perfect forms antimicrobial drugs.

1. "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.
2. "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.
3. 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 NVPS 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.

1. 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 acidic environment 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.
2. 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.
3. 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. Well tolerated by patients, but caution should be used in those taking anticoagulants (for example, people with pathology 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. The field of action includes 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 orally spinal column. As for pregnancy and lactation, in this case the expected benefit should significantly exceed 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 as 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 have increased sensitivity to cephalosporins.

If, five days after the start of therapy, no changes in the patient’s condition have occurred, 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 more strong drugs, causing severe side effects.

Penicillin analogues have become indispensable in modern medicine. Although this is the earliest open group antibiotics, it still remains relevant for the treatment of meningitis, gonorrhea and syphilis, 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.

Penicillin is the first artificially synthesized antibiotic. It was isolated by the famous British bacteriologist Alexander Fleming in 1928. Penicillin is a beta-lactam drug. It is capable of inhibiting synthesis cell membrane microorganisms, which leads to their destruction and death (bactericidal effect).

For a long time this antibiotic was the drug of choice for many bacterial infections caused by staphylococci, streptococci, corynebacteria, neisseria, anaerobic pathogens, actinomycetes and spirochetes. Now penicillin is mainly used for the following indications:

The indisputable advantage of penicillin is its low range of side effects, which allows it to be used for almost all categories of patients. Sometimes there are different allergic reactions- hives, rash, anaphylactic shock and others. At long-term use Cases of candida infection have been described.

However, the active use of penicillin in clinical practice led to the development of resistance. For example, staphylococci began to produce a special enzyme, penicillinase, which is capable of breaking down this antibiotic. That's why it appeared current issue regarding what to replace penicillin with.

Amoxicillin is a newer drug from the penicillin group.

The drug also has a bactericidal effect and easily passes through the blood-brain barrier. Partially metabolized in the liver and excreted from the patient's body through the kidneys.

Among the disadvantages of amoxicillin is the need for multiple doses. Today this drug widely used to treat infections respiratory tract(pharyngitis, tonsillitis, sinusitis, tracheitis, bronchitis), genitourinary system(cystitis, urethritis, pyelonephritis), as well as salmonellosis, leptospirosis, listeriosis, borreliosis and peptic ulcer stomach caused by Helicobacter pylori infection.

Amoxicillin should not be prescribed in case of hypersensitivity to drugs penicillin series, infectious mononucleosis(a specific rash or liver damage occurs). Side effects include various allergic reactions, Stevens-Johnson syndrome, dyspeptic disorders, transient anemia and headache.

The drug is presented in pharmacies under the names “Amoxicillin”, “Amofast”, “V-Mox”, “Flemoxin Solutab”. The price varies greatly depending on the manufacturer.

Adults are usually prescribed amoxicillin 500 mg 3 times a day, and children weighing less than 40 kg are prescribed at a rate of 25-45 mg per 1 kg. Treatment for diseases with mild or moderate severity treatment lasts for a week; for more serious pathologies, the course is extended to 10 or more days.

Ampicillin, as an analogue of penicillin, has been used to treat bacterial pathologies since 1961. It also belongs to the group of penicillins and has a bactericidal effect.

But unlike previous drugs, its spectrum of action includes not only gram-positive microorganisms, but also gram-negative ones (Escherichia coli, Proteus, Haemophilus influenzae and others). However, many bacteria can break it down using penicillinase.

Today ampicillin is used for:

Ampicillin should not be prescribed if there is a history of allergic reactions to penicillins, liver dysfunction, infectious mononucleosis, leukemia and VIL infection. Cases have been described neurological symptoms after taking the drug. Dyspeptic symptoms, candidiasis, toxic hepatitis and pseudomembranous colitis are also sometimes observed.

The drug is available in tablet form for oral administration 0.25 g or powder for internal administration. There are the following trade names: “Ampicillin”, “Ampicillin-Norton”.

You can replace penicillin with Augmentin - combination drug antibiotic amoxicillin and clavulanic acid. The latter is a specific inhibitor of penicillinase, which is produced by streptococci, staphylococci, enterococci and neisseria. This avoids destruction antibacterial drug, which significantly increases its effectiveness in situations of increased resistance of microorganisms. Augmentin was first synthesized and produced by the British pharmaceutical company Beecham Pharmaceuticals.

The drug is most often prescribed for bacterial inflammatory processes. respiratory system- bronchitis, tracheitis, laryngitis, otitis, sinusitis and community-acquired pneumonia. Augmentin is also used for cystitis, urethritis, pyelonephritis, osteomyelitis, gynecological pathologies, prevention of complications after surgery surgical operations and manipulation.

Contraindications include various disorders liver function, increased sensitivity of the patient's body to penicillin antibiotics, lactation period in women. Most often, taking the drug is accompanied by the following side effects:

• allergic reactions;
• dyspeptic disorders;
• pseudomembranous colitis;
• headache;
• dizziness;
• drowsiness or sleep disturbance;
• Quincke's edema;
• toxic transient hepatitis.

Augmentin is available in powder form for syrup or tablets for oral administration. The suspension is used for children weighing more than 5 kilograms at the rate of 0.5 or 1 ml of the drug per 1 kg. For adolescents and adults, tablet form is used. Typically take one tablet (875 mg amoxicillin/125 mg clavulanic acid) 2 times a day. The minimum duration of therapy is 3 days.

Cefazolin belongs to the group of first generation cephalosporins. Like penicillins, it contains a beta-lactam base, which gives it a bactericidal effect against a significant number of gram-positive bacteria.

This antibiotic is used only for intravenous or intramuscular administration. Therapeutic concentration in the blood remains for 10 hours after administration.

Cefazolin also does not penetrate the blood-brain barrier and is almost completely excreted from the body by the patient’s kidneys. Today, the drug is used primarily to treat mild forms of respiratory system infections, as well as bacterial inflammation. urinary tract(especially in children, pregnant women and the elderly).

Cefazolin should not be prescribed if the patient is hypersensitive to cephalosporins or penicillins, or combined with bacteriostatic drugs. When using it, allergic reactions sometimes develop, the filtration function of the kidneys is temporarily impaired, dyspeptic disorders appear, and a fungal infection occurs.

Cefazolin is produced in vials of 0.5 or 1.0 g active substance for preparing injections. The dose of the drug depends on the type and severity of the infection, but usually 1.0 g of antibiotic is prescribed 2 or 3 times a day.

Today, ceftriaxone is one of the most used antibiotics in hospitals. It belongs to the third generation of cephalosporins. Among the serious advantages of the drug are the presence of activity against gram-negative flora and anaerobic infection. Also, ceftriaxone, unlike cefazolin, penetrates well through the blood-brain barrier, which allows it to be actively used for the treatment of bacterial meningitis in situations where there are no results yet bacteriological research. In addition, resistance to it is observed much less frequently than to drugs penicillin group.

Ceftriaxone is used to treat inflammatory processes bacterial etiology respiratory, genitourinary and digestive systems. Antibiotics are also prescribed for meningitis, sepsis, infective endocarditis, Lyme disease, sepsis, osteomyelitis and for the prevention of complications during surgical procedures and operations.

Of particular importance is the use of ciftriaxone for neutropenia and other conditions with impaired hematopoiesis. This is due to the fact that the drug, unlike many other groups of antibiotics, does not inhibit proliferation shaped elements blood.

Ceftriaxone should not be given together with medicines containing calcium (Hartmann and Ringer solutions). When used in newborns, an increase in bilirubin levels in the blood plasma was noted. Also, before the first dose, it is necessary to test for the presence of hypersensitivity to the drug. Side effects include digestive disorders, allergic reactions and headaches.

The drug is produced in powder form in bottles of 0.5, 1.0 and 2.0 g under the names: “Altsison”, “Blitsef”, “Lendatsin”, “Norakson”, “Rotacef”, “Cefogram”, “Ceftriaxone” . The dosage and amount of administration depends on the age, pathology of the patient and the severity of his condition.

Video

The video talks about how to quickly cure a cold, flu or ARVI. Opinion of an experienced doctor.

Penicillin is the first artificially synthesized antibiotic. It was isolated by the famous British bacteriologist Alexander Fleming in 1928. Penicillin is a beta-lactam drug. It is capable of inhibiting the synthesis of the cell membrane of microorganisms, which leads to their destruction and death (bactericidal effect).

For a long time, this antibiotic was the drug of choice for a variety of bacterial infections caused by staphylococci, streptococci, corynebacteria, neisseria, anaerobic pathogens, actinomycetes and spirochetes. Now penicillin is mainly used for the following indications:

The indisputable advantage of penicillin is its low range of side effects, which allows it to be used for almost all categories of patients. Sometimes various allergic reactions are observed - urticaria, rash, anaphylactic shock and others. With long-term use, cases of candida infection have been described.

However, the active use of penicillin in clinical practice has led to the development of resistance. For example, staphylococci began to produce a special enzyme, penicillinase, which is capable of breaking down this antibiotic. Therefore, a pressing question arose regarding what to replace penicillin with.

Amoxicillin is a newer drug from the penicillin group.

The drug also has a bactericidal effect and easily passes through the blood-brain barrier. Partially metabolized in the liver and excreted from the patient's body through the kidneys.

Among the disadvantages of amoxicillin is the need for multiple doses. Today, this drug is widely used for the treatment of respiratory tract infections (pharyngitis, tonsillitis, sinusitis, tracheitis, bronchitis), genitourinary system (cystitis, urethritis, pyelonephritis), as well as salmonellosis, leptospirosis, listeriosis, borreliosis and gastric ulcer caused by Helicobacter pylori infection .

Amoxicillin should not be prescribed in case of hypersensitivity to penicillin drugs, infectious mononucleosis (specific rash or liver damage occurs). Side effects include various allergic reactions, Stevens-Johnson syndrome, dyspeptic disorders, transient anemia and headache.

The drug is presented in pharmacies under the names “Amoxicillin”, “Amofast”, “V-Mox”, “Flemoxin Solutab”. The price varies greatly depending on the manufacturer.

Adults are usually prescribed amoxicillin 500 mg 3 times a day, and children weighing less than 40 kg are prescribed at a rate of 25-45 mg per 1 kg. Treatment for diseases with mild or moderate severity is carried out for a week; for more serious pathologies, the course is extended to 10 or more days.

Ampicillin, as an analogue of penicillin, has been used to treat bacterial pathologies since 1961. It also belongs to the group of penicillins and has a bactericidal effect.

But unlike previous drugs, its spectrum of action includes not only gram-positive microorganisms, but also gram-negative ones (Escherichia coli, Proteus, Haemophilus influenzae and others). However, many bacteria can break it down using penicillinase.

Today ampicillin is used for:

Ampicillin should not be prescribed if there is a history of allergic reactions to penicillins, liver dysfunction, infectious mononucleosis, leukemia and VIL infection. Cases of neurological symptoms occurring after taking the drug have been described. Dyspeptic symptoms, candidiasis, toxic hepatitis and pseudomembranous colitis are also sometimes observed.

The drug is available in the form of tablets for oral use of 0.25 g or powder for internal administration. The following trade names exist: “Ampicillin”, “Ampicillin-Norton”.

You can replace penicillin with Augmentin, a combination drug of the antibiotic amoxicillin and clavulanic acid. The latter is a specific inhibitor of penicillinase, which is produced by streptococci, staphylococci, enterococci and neisseria. This avoids the destruction of the antibacterial drug, which significantly increases its effectiveness in situations of increased resistance of microorganisms. Augmentin was first synthesized and produced by the British pharmaceutical company Beecham Pharmaceuticals.

Most often the drug is prescribed for bacterial inflammatory processes of the respiratory system - bronchitis, tracheitis, laryngitis, otitis, sinusitis and community-acquired pneumonia. Augmentin is also used for cystitis, urethritis, pyelonephritis, osteomyelitis, gynecological pathologies, and the prevention of complications after surgical operations and manipulations.

Contraindications include various liver dysfunctions, increased sensitivity of the patient's body to penicillin antibiotics, and lactation in women. Most often, taking the drug is accompanied by the following side effects:

• allergic reactions;
• dyspeptic disorders;
• pseudomembranous colitis;
• headache;
• dizziness;
• drowsiness or sleep disturbance;
• Quincke's edema;
• toxic transient hepatitis.

Augmentin is available in powder form for syrup or tablets for oral administration. The suspension is used for children weighing more than 5 kilograms at the rate of 0.5 or 1 ml of the drug per 1 kg. For adolescents and adults, tablet form is used. Typically take one tablet (875 mg amoxicillin/125 mg clavulanic acid) 2 times a day. The minimum duration of therapy is 3 days.

Cefazolin belongs to the group of first generation cephalosporins. Like penicillins, it contains a beta-lactam base, which gives it a bactericidal effect against a significant number of gram-positive bacteria.

This antibiotic is used only for intravenous or intramuscular administration. Therapeutic concentration in the blood remains for 10 hours after administration.

Cefazolin also does not penetrate the blood-brain barrier and is almost completely excreted from the body by the patient’s kidneys. Today, the drug is used primarily to treat mild forms of respiratory system infections, as well as bacterial inflammation of the urinary tract (especially in children, pregnant women and the elderly).

Cefazolin should not be prescribed if the patient is hypersensitive to cephalosporins or penicillins, or combined with bacteriostatic drugs. When using it, allergic reactions sometimes develop, the filtration function of the kidneys is temporarily impaired, dyspeptic disorders appear, and a fungal infection occurs.

Cefazolin is produced in vials with 0.5 or 1.0 g of active ingredient for the preparation of injections. The dose of the drug depends on the type and severity of the infection, but usually 1.0 g of antibiotic is prescribed 2 or 3 times a day.

Today, ceftriaxone is one of the most used antibiotics in hospitals. It belongs to the third generation of cephalosporins. Among the serious advantages of the drug is the presence of activity against gram-negative flora and anaerobic infections. Also, ceftriaxone, unlike cefazolin, penetrates well through the blood-brain barrier, which allows it to be actively used for the treatment of bacterial meningitis in situations where there are no results of bacteriological testing yet. In addition, resistance to it is observed much less frequently than to drugs of the penicillin group.

Ceftriaxone is used to treat inflammatory processes of bacterial etiology of the respiratory, genitourinary and digestive systems. The antibiotic is also prescribed for meningitis, sepsis, infective endocarditis, Lyme disease, sepsis, osteomyelitis and for the prevention of complications during surgical procedures and operations.

Of particular importance is the use of ciftriaxone for neutropenia and other conditions with impaired hematopoiesis. This is due to the fact that the drug, unlike many other groups of antibiotics, does not inhibit the proliferation of blood cells.

Ceftriaxone should not be prescribed together with drugs containing calcium (Hartmann and Ringer solutions). When used in newborns, an increase in bilirubin levels in the blood plasma was noted. Also, before the first dose, it is necessary to test for the presence of hypersensitivity to the drug. Side effects include digestive disorders, allergic reactions and headaches.

The drug is produced in powder form in bottles of 0.5, 1.0 and 2.0 g under the names: “Altsison”, “Blitsef”, “Lendatsin”, “Norakson”, “Rotacef”, “Cefogram”, “Ceftriaxone” . The dosage and amount of administration depends on the age, pathology of the patient and the severity of his condition.

Video

The video talks about how to quickly cure a cold, flu or ARVI. Opinion of an experienced doctor.

Botulism bacillus), as well as some gram-negative (gonococci, meningococci) microorganisms and. Penicillin preparations are used in the treatment of sore throats, wound and purulent infections of the skin, soft tissues and mucous membranes, pleurisy, and osteomyelitis, diphtheria, erysipelas, -, anthrax, syphilis and other infectious diseases caused by microorganisms sensitive to penicillin.

Currently there are the following drugs penicillin.

Benzylpenicillin sodium salt(Benzylpenicillinum-natrium; ); benzylpenicillin potassium salt(Benzylpenicillinumkalum; list B). Both drugs are administered in the form of solutions intramuscularly, subcutaneously, into a vein, into cavities (abdominal, pleural), in the form of an aerosol, eye drops. Only the sodium salt of benzylpenicillin is administered endolumbarally. For injection into the muscles and under the skin, 50,000-200,000 units are prescribed in 1 ml of 0.25-1% novocaine solution after 3-4 hours. Higher daily dose 1,200,000 units. Release form: bottles of 100,000, 200,000, 300,000, 400,000, 500,000 and 1,000,000 units.

Benzylpenicillin novocaine salt(Benzylpenicillinum-novocainum; list B). To administer the drug, prepare an ex tempore suspension in 2-4 ml of sterile water for injection or isotonic sodium chloride solution. The drug is used only intramuscularly at a dose of 300,000 units 2-3 times a day. The highest daily dose is 1,200,000 units. Release form: bottles of 100,000, 300,000 and 600,000 units.

Ecmonovocillin(Ecmonovocillinum; list B) - suspension of novocaine salt of benzylpenicillin in aqueous solution ecmoline, prepared ex tempore. It is administered only intramuscularly at 300,000-600,000 units once a day. It is dispensed in two bottles: one contains novocaine salt of benzylpenicillin, the other contains a solution of ecmoline. Store at room temperature.

Bicillin-1(Bicillinum-1; list B). N, N"-dibenzylethylenediamine salt of benzylpenicillin. Drug long acting, used for diseases caused by penicillin-sensitive pathogens. Also indicated for the prevention and treatment of syphilis. The suspension is prepared ex tempore in 2-3 ml of sterile water for injection or isotonic sodium chloride solution. Administered only intramuscularly. Before insertion, you must make sure that the needle does not enter a vein. Prescribe 300,000-600,000 units once a week or 1,200,000 units once every two weeks. Release form: bottles of 300,000, 600,000, 1,200,000 and 2,400,000 units.

Bicillin-3(Bicillimim-Z; list B) - a mixture of equal parts of potassium (or sodium) salt of benzylpenicillin, novocaine salt of benzylpenicillin and bicillin-1. The indications and method of use are the same as for bicillin-1. Prescribe 300,000 units once every three days or 600,000 units once every 6-7 days. Release form: bottles of 300,000, 600,000, 900,000 and 1,200,000 units.

Bicillin-5- a mixture of bicillin-1 (1,200,000 units) and novocaine salt of benzylpenicillin (300,000 units). An effective remedy for the prevention of rheumatic attacks. The method of application is the same as for bicillin-1. Prescribe 1,500,000 units once every 3-4 weeks. Release form: bottles of 1,500,000 units.

Phenoxymethylpenicillin(Phenoxymethylpenicillinum; list B). Unlike the listed benzylpenicillin preparations, it is not destroyed by acid gastric juice, which allows it to be administered orally at 100,000-200,000 units 4-5 times a day. Higher single dose- 400,000 units, daily - 1,200,000 units. Forms of release: tablets and dragees, 100,000 and 200,000 units.

Eficillin(Aephycillinum; list B) is a benzylpenicillin preparation that has the property of selectively accumulating in lung tissue. It is used mainly for the treatment of pneumonia, bronchitis, bronchiectasis, etc. It is administered intramuscularly in the form prepared ex tempore in 4 ml of 0.5% novocaine solution, 500,000-1,000,000 units once a day.

Methicillin(Methicillinum; list B) and oxacillin(Oxacillinum; list B) - semi-synthetic penicillins, effective against staphylococci that have become resistant to other penicillin preparations. They are used for carbuncles, phlegmon, abscesses, pneumonia, osteomyelitis, septicemia and other infections caused by penicillin-resistant forms of staphylococci. Methicillin is prescribed intramuscularly as a solution in 1.5 ml of sterile water for injection, 1 g every 4-6 hours, oxacillin - orally, in capsules 0.5-1 g every 4-6 hours.

Ampicillin(Ampicillinum; list B) is a semi-synthetic broad-spectrum penicillin that has the antimicrobial properties of benzylpenicillin and, in addition, activity against a number of gram-negative microorganisms (Escherichia coli, dysentery coli, salmonella, Proteus, etc.) - Successfully used for chronic bronchitis, infections urinary tract, enterocolitis, gallbladder diseases. Prescribed orally 250-500 mg - 1 g 4-6 times a day. Release form: 250 mg tablets. Penicillin drugs can cause side effects in the form of allergic reactions. In some cases, anaphylactic shock is possible. Penicillins are contraindicated in patients with hypersensitivity to penicillin and other antibiotics; patients suffering from bronchial asthma, urticaria,. See also Antibiotics.

Penicillin (Penicillium) is an antibiotic obtained from the culture liquid after growing various molds of the genus Penicillium. In 1929, A. Fleming was the first to prove that when P. notatum is cultivated on artificial media, a substance called “penicillin” is formed, which diffuses into environment and has a detrimental effect on bacteria growing on this medium. 12 years after Fleming’s discovery, a large group of English scientists [Abraham, Chain, Florey (E. P. Abraham, E. Chain, M. E. Florey) and others] managed to isolate pure form and establish the chemical structure of substances formed in the culture liquid during cultivation various types molds such as P. notatum and especially P. chrysogenum. It turned out that the culture fluid contains various substances, similar in structure, but with different biological properties.

All these penicillins can be considered as derivatives of 6-aminopenicillanic acid (6APA):

Among the first isolated penicillins were: 1) penicillin G (G) = benzyl-acetamido-penicillanic acid, or benzylpenicillin; 2) penicillin X = p-hydroxyphenylacetamido-penicillanic acid, or P-hydroxybenzylpenicillin; 3) penicillin F (F) = Δ2-pentenoacetamidopenicillanic acid, or 2-pentenylpenicillin; 4) dihydropenicillin F (P) = p-amylacetamidopenicillanic acid, or p-amylpenicillin. In addition, with the artificial addition of certain chemical components (precursors) to the nutrient medium, it was possible to obtain other penicillins through biosynthesis. Has acquired particular importance in lately penicillin V, or phenoxymethylpenicillin, which, unlike other natural penicillins, is highly resistant to acids, is well absorbed from gastrointestinal tract and therefore suitable for oral administration. Of the initially isolated penicillins, only penicillin G (G) has found widespread use in clinical practice. It is easily soluble in ether, alcohol, acetone, slightly soluble in benzene and carbon tetrachloride. As a monobasic acid, it forms salts with metals that are easily soluble in water.

Penicillin is a light powder, highly soluble in water, hygroscopic and sensitive to moisture, high temperature, ultraviolet rays, acids, salts heavy metals and oxidizing agents (H 2 O 2, KMnO 4, chloramine, etc.). Penicillin has high bactericidal activity against most gram-positive, as well as some gram-negative microorganisms - gonococci, meningococci and spirochetes ( Treponema pallidum etc.). The activity of penicillin is determined by biological and by chemical means and are expressed in action units (AU). 1 unit = 0.6 μg crystalline penicillin G (G); Thus, 1 mg of this penicillin contains 1666 units.

The bactericidal effect of penicillin is associated with disruption of the formation of certain components cell membrane of bacteria. Therefore, penicillin only acts on bacterial cells in a state of active reproduction. The so-called resting cells are not affected by penicillin. In this regard, both in vitro and in vivo, individual survivors (“persisters”) are found after the action of penicillin.

The activity of penicillin is significantly limited by the fact that bacteria sensitive to penicillin often become resistant to this antibiotic, which is associated with their ability to form the enzyme penicillinase, which inactivates penicillin. Some types of bacteria are naturally resistant to penicillin (for example, a number of strains of staphylococci). The problem of combating bacterial resistance to penicillin, especially those that form penicillinase, is being solved by introducing new semi-synthetic penicillins into practice (see below).

Penicillin is produced in the form of crystalline sodium or potassium salts, intended primarily for intramuscular administration in doses of 50,000 to 300,000 units. Up to 1,000,000-2,000,000 units can be administered per day. Penicillin solutions can also be administered inside cavities (pleural, articular), sometimes intradermally and intratracheally. Penicillin should be administered endolumbarally with great caution, as the drug may have toxic effect on the central nervous system.

Penicillin V is used per os in the form of tablets containing 100,000 and 200,000 units. It is advisable to repeat a dose of 200,000 units 3-4 times a day.

Before treatment with penicillin, it is advisable to test the patient’s sensitivity to it (sensitization tests), since regardless of the method of application and the dose, the patient may develop allergic reactions of varying severity and nature, sometimes life-threatening (anaphylactic shock). The use of penicillin can cause other side effects. Caution should be exercised when treating patients with central nervous system or circulatory system syphilis with penicillin.

To reduce the number of injections and create a more constant concentration of the antibiotic in the blood, large molecular drugs are used, for example N-N-dibenzylethylenediamine salt of dipenicillin, or bicillin (see), which circulates in the body for a long time due to the fact that it is released much more slowly than regular penicillin. There are also a number of combined dosage forms, in which penicillin is associated with novocaine, ecmoline, etc., used intramuscularly to prolong the time of circulation of the drug in the body.

| Pencillinum

Analogs (generics, synonyms)

Recipe

Rp. Penicillini 200,000 units
D.t. d. N. 10
S. Dissolve directly in the bottle in 4 ml of 0.5% novocaine solution. Administer 100,000 units intramuscularly every 8 hours.

Rp. Penicillini natrii cryst. 100,000 units
D.t. d. N. 5
S. Dissolve directly in the vial in 5 ml of sterile isotonic sodium chloride solution or double-distilled water. Enter in spinal canal 25,000-50,000 units (for epidemic meningitis).

Rp. Penicillini 50,000 units
Sol. Adrenalini hydrochlorici 0.1% gtts X
Sol. Natrii chlorati isotonicae 15.0
M.D.S. 2-3 drops in each nostril 3-4 times a day (for acute rhinitis).

Rp. Penicillini 500,000 units
Sol. Natrii chlorati isotonicae 20.0
M.D.S. 30 drops per half glass of water for gargling.

Pharmacological action

This is the first antimicrobial agent, which was obtained using waste products of microorganisms as a basis. The history of this medicine begins in 1928, when the inventor of the antibiotic, Alexander Fleming, isolated it from a strain of the fungus Penicillium notatum. In the chapter that describes the history of the discovery of penicillin, Wikipedia testifies that the antibiotic was discovered by accident, after bacteria from external environment mold fungus, its bactericidal effect was noted.

Directions for use

Doctors believe that the greatest healing effect achieved by intramuscular or subcutaneous administration of Penicillin. Also this antibacterial agent often used in the form of solutions for rinsing, washing, drops for the nose and eyes.

For example, with intramuscular injection, after 30 minutes in the blood it is observed highest concentration antibiotic, after which it quickly spreads into the joint cavities, lungs and other muscles. To support required level concentration, the drug is administered every 3 to 4 hours. The dosage and duration of treatment is determined by the attending physician.

Indications

The use of penicillin is indicated for sepsis (especially streptococcal), in all sulfonamide-resistant cases of corresponding infections (pneumococcal, gonococcal, meningococcal infection etc.), with extensive and deeply localized infectious processes(osteomyelitis, severe phlegmon, gas gangrene), after injuries involving and infection of large musculoskeletal masses, in postoperative period for prevention purulent complications, with infected third and fourth degree burns, with soft tissue injuries, wounds chest, purulent meningitis, brain abscesses, erysipelas, gonorrhea and its sulfonamide-resistant forms, syphilis, severe furunculosis, sycosis, and various inflammations of the eye and ear.

In the internal medicine clinic, Penicillin is used to treat lobar pneumonia(together with sulfonamide drugs), focal pneumonia, acute sepsis, cholecystitis and cholangitis, prolonged septic endocarditis, as well as for the prevention and treatment of rheumatism.

In children, Penicillin is used: for umbilical sepsis, septicopyemia and septic-toxic diseases of newborns, pneumonia in newborns and infants and early age, otitis in infants and young children, septic form of scarlet fever, septic-toxic form of diphtheria (necessarily in combination with special serum), pleuropulmonary processes that are not amenable to the action of sulfonamide drugs, purulent pleurisy and purulent meningitis, with gonorrhea.

Contraindications

Penicillin, like any antibiotic, has contraindications for use. Many people have hypersensitivity to drugs of the penicillin group and sulfonamides. Therefore, it is better for such people to choose another antibacterial agent. It is not recommended to use this antibiotic for hay fever. bronchial asthma, urticaria, as well as pregnant women and nursing mothers. During treatment
Penicillin strictly prohibits the consumption of alcoholic beverages.

Side effects

Of the side effects that Penicillin can cause, the instructions for use note that the most common negative manifestations- These are allergic reactions. Human skin is especially affected. Exfoliative dermatitis, urticaria-like rash, urticaria, erythema, pustular, vesicular and macular rashes may appear.
The respiratory organs can respond with asthmatic bronchitis, laryngopharyngitis, and rhinitis. And the most severe complication- anaphylactic shock. Therefore, the doctor always asks the patient about the tolerability of this antibiotic.

Release form

Injectable preparations are available, as well as penicillin tablets.
The injection product is produced in glass bottles, which are closed with rubber stoppers and metal caps. The vials contain different doses of penicillin. It is dissolved before administration.
Penicillin-ecmoline tablets are also produced for resorption and oral administration. Sucking tablets contain 5000 units of penicillin. In tablets for oral administration – 50,000 units.
Penicillin tablets with sodium citrate may contain 50,000 and 100,000 units.

ATTENTION!

The information on the page you are viewing is created for informational purposes only and does not in any way promote self-medication. The resource is intended to familiarize healthcare workers with additional information about certain medications, thereby increasing the level of their professionalism. Use of the drug "" in mandatory involves consultation with a specialist, as well as his recommendations on the method of use and dosage of the medicine you have chosen.