Penicillins

Penicillin group of antibiotics, derived from the culture fluid of different moulds of Penicillium genus. Penicillins possess high antibacterial activity mainly for most grampolaugitionah (staphylococci, streptococci, pneumococci, diphtheria Bacillus, pathogens gas gangrene, tetanus drumsticks, drumsticks anthrax, wand botulism), as well as some gram (gonorrhea, meningococci) microorganisms and spirochetes. Using drugs penicillin for treatment of angina, pneumonia, wound and purulent infections of the skin, soft tissues and mucous membranes, pleurisy, peritonitis, anesthetic, septicemia and pielii, osteomyelitis, diphtheria, erysipelas, scarlet fever,- epidemic cerebrospinal meningitis, anthrax, syphilis and other infectious diseases caused by susceptible to penicillin microorganisms.
Currently there are the following drugs penicillin.
Benzylpenicillin sodium salt (Benzylpenicillinum-natrium; list B); benzylpenicillin potassium salt (Benzylpenicillinumkalum; list B). Both drugs is administered in the form of a solution intramuscularly, subcutaneously, in Vienna, in the cavity (abdominal, chest), in the form of aerosol, eye drops. Endolyumbalno enter only the sodium salt of benzylpenicillin. For introduction into the muscle and under the skin appoint 50 000-200 000 IU in 1 ml of 0.25 - 1% solution novokaina after 3-4 hours. The highest daily dose 1 200 000 IU. Release form: bottles of 100 000, 200 000, 300 000, 400 000, 500 000 and 1 000 000 IU.
Dental novokainova salt (Benzylpenicillinum-novocainum; list B). For a drug prepared ex tempore suspension of 2-4 ml of sterile water for injection or izotoniceski solution of sodium chloride. The drug used intramuscularly in a dose of 300 000 IU 2-3 times a day. The highest daily intake - 1 200 000 IU. Release form: bottles of 100 000 and 300 000 and 600 000 E. D.
Economically (Ecmonovocillinum; list B) - suspension salt benzylpenicillin procaine in a water solution of akmolina, are ex tempore. Is only intramuscularly 300 000-600 000 IU once a day. Released in two vials: in one procaine salt benzylpenicillin, in another - a solution of akmolina. Keep at room temperature.
Bicillin-1 (Bicillinum-1; list B). N, N'-dibenzylethylenediamine salt benzylpenicillin. The drug prolonged effect, applied diseases caused by susceptible to penicillin pathogens. Also shown for the prevention of rheumatic fever and treatment of syphilis. Suspension are ex tempore in 2-3 ml of sterile water for injection or izotoniceski solution of sodium chloride. Being injection. Before the introduction you need to ensure that the needle is not named in Vienna. Appoint 300 000 - 600 000 IU once a week or 1 200 000 IU once in two weeks. Release form: bottles of 300 000 and 600 000, 1 200 000 and 2 400 000 UNIT.
Bicillin 3 (Bicillimim-C; list B) - a mixture of equal parts of potassium (or sodium) salt benzylpenicillin procaine salt dental and bicillin-1. Indications and usage are the same as bicillin-1. Appoint 300 000 IU once in three days or 600 000. ED once in 6-7 days. Release form: bottles of 300 000 and 600 000 and 900 000 and 1 200 000 IU.
Bicillin-5 - a mixture of bicillin-1 (1 200 000 IU) and salt benzylpenicillin procaine (300 000 UNITS). Effective tool for the prevention of rheumatic attacks. The way of application is the same as bicillin-1. Assign 1 500 000 IU once in 3-4 weeks. Release form: bottles of 1 500 000 UNITS.
Dentists (Phenoxymethylpenicillinum; list B). In contrast to these dental products, it breaks acid gastric juice, which allows you to assign him into 100 000-200 000 IU 4-5 times a day. The highest single dose of 400 000 IU daily, 1 200 000 E. D. Forms: tablets and pills 100 000 and 200 000 IU.
Epically (Aephycillinum; list B) is a drug benzylpenicillin that has the property to selectively accumulate in the lung tissue. Applied mainly for the treatment of pneumonia, bronchitis, bronhoektasia, pleuritis , etc. is Injected intramuscularly in the form of suspension, prepared ex tempore in 4 ml of 0.5% solution novokaina, 500000 to 1 000 000 IU once a day.
Methicillin (Methicillinum; list B) and oxacillin (Oxacillinum; list B) is a semi - synthetic penicillins, effective against Staphylococcus, which have become resistant to other drugs penicillin. Apply at furuncles, carbuncles, phlegmon, wound infections, abscesses, pneumonia, osteomyelitis, septicemia, and other infections caused by penicillinonline forms of staphylococci. Methicillin intramuscularly in the form of a solution in 1.5 ml of sterile water for injection, 1 g every 4-6 hours, oxacillin - inside, capsules of 0.5-1 g every 4-6 hours.
Ampicillin (Ampicillinum; list B) is a semisynthetic broad-spectrum penicillin actions by antimicrobial benzylpenicillin and, in addition, activity against some gram-negative microorganisms (bacteria and dysenteric coli, Salmonella, Proteus, and others)is Successfully used for chronic bronchitis, urinary tract infections, enterocolitis, diseases of the gallbladder. Assign inside of 250-500 mg - 1 g 4-6 times a day. The form of release: tablets of 250 mg of penicillin Drugs can cause side effects in the form of allergic reactions. In some cases, possible anaphylactic shock. Penicillin is contraindicated in patients with a heightened sensitivity to penicillin and other antibiotics; patients suffering from bronchial asthma, hives, hay fever. Cm. also Antibiotics.


Penicillin (Penicillinum) - antibiotics, derived from the culture fluid after growing different kind of mold Penicillium. In 1929 Fleming (A. Fleming) was the first to prove that under cultivation P. notatum in the artificial environment produces a substance called "penicillin"which diffuses in the environment and has a devastating effect on bacteria growing on the environment. 12 years later after opening Fleming large group of English scientists [Abraham, Cheyne, Flory (E. P. Abraham, that is, Chain, M. E. Florey) and others] have been able to isolate pure and install Henichesk structure of substances from cultural liquid for growing different kinds of mold type P. notatum and especially P. chrysogenum. It turned out that in the cultural liquid contains various substances, similar in structure but with different biological properties.
All these penicillins can be seen as derivative 6-aminopenicillanic acid (APC):
Among the first isolated penicillins were: 1) penicillin W (G) = benzyl-acetamido-penitsillanovoy acid, or penicillin; 2) penicillin X=p-hydro-xianliezhong-penitsillanovoy acid, or P-oxybenzene; 3) penicillin f (F) = Δ2-pentenoate-aminopenicillanic acid or 2-interpretilor; 4) dihydromonacolin f (P)=p-unilaterally acid, or p-humilination. In addition, artificial add to the nutrient medium of certain chemicals (precursors) managed to get through biosynthesis and other penicillins. Of particular importance has recently become penicillin V, or dentists, which, unlike other natural P., have a high resistance to acids, is well absorbed from the gastrointestinal tract and is therefore suitable for the reception per os. Initially budgeted P. only penicillin G (G) has found wide application in clinical practice. It is easily soluble in ether, alcohol, acetone, weakly - in benzene and carbon tetrachloride. As monobasic acid forms with metals easily soluble salts.
Penicillin - light powder, soluble in water, hygroscopic and sensitive to moisture, high temperature, ultraviolet rays, acids, salts of heavy metals and oxidants (H2O2, KMnO4, chloramine and others). P. has high bactericidal activity against most gram-positive and some gram-negative microorganisms - gonokokkov, meningokokkov and spirochete (Treponema pallidum and others). The P. activity determine biological and chemical methods and expressed in units of (ED). 1 UNIT=0,6 mcg crystalline penicillin G (G); thus, in the 1 mg P. this contains 1666 ED.
Bactericidal effect P. connected to infringement of process of formation of certain components of the cell membrane of bacteria. Therefore, P. valid only for bacterial cells in a state of active multiplication. The so-called cells alone are not exposed to P. In this regard, both in vitro and in vivo after the action P. found individual experiencing individuals ("persisters").
Activity P. significantly limited by the fact that sensitive P. bacteria often develop resistance to the antibiotic, which is associated with the emergence of their ability to form an enzyme penitsillinazou, inactivating P. Certain bacteria have a natural resistance to P. (for example, the number of strains of staphylococci). The problem of struggle against bacterial resistance to P., especially those that form penitsillinazou, is solved by the implementation of new semi-synthetic P. (see below).
Penicillin is released in the form of crystalline sodium or potassium salt, intended mainly for intramuscular injection in doses of 50, 000 to 300 000 UNITS. In the day you can enter up to 1 000 000 - 2 000 000 IU. Solutions P. you can also enter the inside of the cavity (pleural, articular), sometimes intradermally and intratrahealno. Enter P. endolyumbalno should be used with caution, because the drug can have toxic effects on the Central nervous system
Penicillin V is applied per os in the form of tablets containing 100 000 and 200 000 E. D. Dose 200 000 IU it is advisable to repeat 3-4 times a day.
Before treatment P. it is advisable to test the sensitivity to it of the patient (tests on sensitization), because regardless of the method of application and doses the patient may develop on the severity and nature of allergic reactions, sometimes life-threatening (anaphylactic shock). The use of P. may cause other side effects. Caution must be exercised in the treatment of P. syphilis Central nervous system or the organs of blood circulation.
To reduce the number of injections and build a more permanent antibiotic concentrations in the blood used drugs macromolecular, for example N-N-dibenzylethylenediamine salt dibenyline, or bicillin (see), which long circulates in the body due to the fact that there is much slower than usual P. There are also a number of combined medicinal forms in which penicillin associated with novocaine, akmolina and other applied intramuscularly to prolong the circulation of drugs in the body.