Benzylpenicillin

General characteristics. Structure:

Active ingredient: benzylpenicillin;
1 bottle contains benzylpenicillin of sodium salt sterile - 500 000 PIECES or 1 000 000 PIECES.

Pharmacological properties:

Pharmacodynamics. Benzylpenicillin possesses antimicrobic bactericidal action. Mechanism
actions: drug interferes with formation of peptide bonds at the expense of transpeptidase inhibition, breaks late stages of synthesis of a peptidoglikan of a cell wall that leads to a lysis of the sharing cells. Drug is active concerning gram-positive bacteria of Staphylococcus spp., Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis, some
gram-negative microorganisms (including Neisseria gonorrhoeae, Neisseria meningitidis), anaerobic spore-forming sticks, and also Actinomyces spp., Spirochaetaceae. Drug is not active concerning the majority of gram-negative bacteria, rickettsiae, viruses, protozoa, mushrooms. Collapses a penicillinase. Change of sensitivity of gonokokk, hemolitic streptococci, stafilokokk and pneumococci to benzylpenicillin is in recent years noted.

Pharmacokinetics. At intramuscular introduction the maximum concentration of drug in blood is created in 30-60 minutes, in 3-4 hours after a single injection at blood there are antibiotic traces. At hypodermic introduction the speed of absorption is less constant, usually maximum concentration in blood is noted in 60 minutes. Concentration and duration of circulation of benzylpenicillin in blood depend on the entered dose. Contacts blood proteins for 60%. The antibiotic well gets into bodies, fabrics and liquids of an organism, except for liquor, tissues of an eye and prostate, but at an inflammation of covers of a brain its concentration in cerebrospinal fluid increases.
The elimination half-life makes 30-60 minutes, at a renal failure – 4-10 hours, and at a simultaneous abnormal liver function and kidneys – till 16-30 o'clock. Out of an organism it is quickly brought by kidneys (glomerular filtering and canalicular secretion) in not changed look. In insignificant quantities it is excreted with saliva, then, breast milk, bile. Has no cumulative effect.
Pharmaceutical characteristics.
Main physical and chemical properties: crystal powder of white or almost white color.
Incompatibility.
It is inadmissible to mix benzylpenicillin in one capacity with other medicines.
It is not recommended to apply Ringer's solution or other natriysoderzhashchy solutions which contain glucose as solvent. Drug is incompatible with ions of metals and sympathomimetic amines.

Indications to use:

The infections caused by microorganisms, sensitive to drug:
– respiratory infection and ENT organs: quinsy, pneumonia, purulent pleurisy, diphtheria, scarlet fever, actinomycosis of lungs;
– infections of urinogenital system: cystitis, syphilis, gonorrhea, colpitis, endocervicitis, endometritis, adnexitis, salpingo-oophoritis;
– infections of an organ of sight: conjunctivitis, blepharitis, dacryocystitis;
– purulent infections of skin and soft tissues;
– septic endocarditis, sepsis;
– osteomyelitis;
– wound fevers;
– ugly face;
– malignant anthrax;
– meningitis;
– peritonitis;
– infections of biliary tract.

Route of administration and doses:

Before introduction it is necessary to carry out preliminary skin test on portability of drug and novocaine on condition of its use for cultivation, in the absence of contraindications to its carrying out. The drug is administered intramusculary, subcutaneously, intravenously (struyno and kapelno),
intratekalno, in an organism cavity. The intramuscular way of introduction is most widespread.
Intravenously: at moderately severe infections the single dose of drug for adults makes usually 250 000-500 000 PIECES, daily – 1 000 000-2 000 000 PIECES, at heavy infections enter up to 10 000 000-20 000 000 PIECES a day, at gas gangrene – to 40 000 000-60 000 000 PIECES. Usually daily dose for children aged till 1 year makes 50 000-100 000 PIECES/kg, 1 years – 50 000 PIECES/kg are more senior, if necessary it is possible to increase a daily dose to 200 000-300 000 PIECES/kg, according to vital indications – to 500 000 PIECES/kg. Frequency rate of administration of drug – 4-6 times a day. Benzilpenitsillin's solution is prepared just before its use. For intravenous jet administration a single dose (1 000 000-
2 000 000 PIECES) drug dissolve in 5-10 ml of sterile water for injections or 0,9% of solution of sodium of chloride and enter slowly within 3-5 minutes. For intravenous drop administration of 2 000 000-5 000 000 PIECES of an antibiotic dissolve 0,9% of solution of sodium of chloride or 5% of solution of glucose in 100-200 ml and enter with a speed of 60-80 thaws of 1 minute.
Intravenously the drug is administered by 1-2 times a day, combining with intramuscular introductions. Intramusculary: at moderately severe infections the single dose of drug for adults makes usually 250 000-500 000 PIECES, daily – 1 000 000-2 000 000 PIECES, at heavy infections enter up to 10 000 000-20 000 000 PIECES a day, at gas gangrene – to 40 000 000-60 000 000 PIECES. Usually daily dose for children aged till 1 year makes 50 000-100 000 PIECES/kg, 1 years – 50 000 PIECES/kg, if necessary a daily dose are more senior
it is possible to increase up to 200 000-300 000 PIECES/kg, according to vital indications – to 500 000 PIECES/kg. Frequency rate of administration of drug – 4-6 times a day. For intramuscular introduction add to bottle contents 1-3 ml of sterile water for injections or 0,9% of solution of sodium of chloride, or 0,5% of solution of novocaine. The formed solution is entered deeply into a muscle in an upper outside quadrant of a buttock. Subcutaneously: Benzylpenicillin apply to an obkalyvaniye of infiltrates in concentration 100 000-200 000 PIECES in 1 ml of 0,25-0,5% of solution of novocaine. Into cavities (belly, pleural, etc.) Benzilpenitsillin's solution the adult enter into concentration 10 000-20 000 PIECES in 1 ml, to children – 2 000-5 000 PIECES in 1 ml. Dissolve in
to sterile water for injections or 0,9% chloride sodium solution. Treatment duration – 5-7 days with the subsequent transition to intramuscular introduction. Intratekalno: the drug is administered at purulent diseases of a head, spinal cord, a meninx. The adult appoint 5 000-10 000 PIECES in a dose, to children 1 years – 2 000-5 000 PIECES are more senior, enter slowly – 1 ml a minute of 1 times a day. Drug is dissolved in sterile water for injections or in 0,9% chloride sodium solution at the rate of 1 000 PIECES on 1 ml. Before an injection from the spinal channel delete 5-10 ml of cerebrospinal fluid and add it to antibiotic solution in an equal ratio. Injections are repeated within 2-3 days then they pass to intramuscular introduction. Treatment of patients with syphilis, gonorrhea is carried out according to specially developed schemes. Depending on a form and weight of a disease Benzilpenitsillin apply from 7-10 days to 2 months and more (sepsis, a septic endocarditis, etc.).

Features of use:

Use during pregnancy or feeding by a breast. Use during pregnancy is possible only in that case when the expected advantage for the woman exceeds potential risk for a fruit. In need of use of drug it is necessary to stop feeding by a breast. Children. With extra care children under 2 years should use drug.

Before an initiation of treatment of patients it is necessary to check for hypersensitivity. After inspection and administration of drug for 30 minutes it is necessary to be ready to administration of adrenaline. Patients should be warned concerning possibility of allergic reactions, and if necessary to report about them to the doctor. Those at whom allergic reactions to drug developed should stop treatment and to appoint symptomatic therapy adrenaline, antihistaminic drugs and corticosteroids. Benzilpenitsillin's solutions use right after preparation. Use
drug perhaps only at the pathological processes caused by microorganisms, sensitive to it. At emergence of resistance of activators to drug it is replaced with other antibiotics. If the effect of use of drug is absent through
3-5 days after an initiation of treatment, it is necessary to pass to use of other antibiotics or to combine Benzilpenitsillin with other antibiotics or synthetic chemotherapeutic means. At the same time it is necessary to consider a possibility of strengthening of side effect. The patient 60 years are more senior and pregnant women are not recommended to appoint high doses (higher than 10 000 000 PIECES a day). At prolonged treatment it is necessary to control electrolytic balance, a blood count and function of kidneys. With the person
care drug should be used to babies, patients sick syphilis, a heavy cardiomyopathy, allergic diathesis, bronchial asthma, a hypovolemia, epilepsy, to patients with renal failures and a liver, and also a sick diabetes mellitus. At patients with the known hypersensitivity to cephalosporins the cross allergy is possible. Long heavy diarrhea can entail suspicion concerning development of pseudomembranous colitis. This state is life-threatening therefore drug needs to be cancelled urgently with the subsequent complex treatment. At Benzilpenitsillin's dissolution in solution of novocaine muddy can be formed
solution owing to formation of novocainic salt of benzylpenicillin that is not an obstacle for intramuscular administration of drug. Ability to influence speed of response at control of motor transport or work with other mechanisms. Does not influence ability to manage vehicles and work with other difficult mechanisms.

Side effects:

Hypersensitivity reactions: skin rash, itch, fever, fever, arthralgia, hypostases, small tortoiseshell, mnogoformny exudative erythema, exfoliative dermatitis, Quincke's disease of Quincke, acute anaphylaxis.
From a respiratory organs: bronchospasm.
From the central and peripheral nervous system: dizziness, headache, sonitus. Endolumbar introduction can cause neurotoxicosis (nausea, vomiting, symptoms of a meningism, a spasm).
From a digestive tract: nausea, stomatitis, glossitis, diarrhea pseudomembranous colitis, abnormal liver function.
From urinogenital system: intersticial nephrite.
From cardiovascular system: fluctuations of arterial pressure, disturbance of pumping function of a myocardium.
From blood and lymphatic system: eosinophilia, positive takes of the test of Koombs, hemolitic anemia, leukopenia, thrombocytopenia, агрунолоцитоз.
Another: the weakened patients, newborns, elderly people at prolonged treatment can have a superinfection caused by microflora, steady against drug (drozhzhepodobny mushrooms, gram-negative microorganisms). Patients who receive medical treatment concerning syphilis can have Yarisha-Gerksgeymer's raktion for the second time to a bacteriolysis.

Interaction with other medicines:

In combination with aminoglycosides, macroleads, sulfanamide drugs benzylpenicillin shows synergy action. The effect of drug is reduced by bacteriostatic medicines (chloramphenicol), and inhibitors beta лактамаз increase its activity. It is not recommended to combine benzylpenicillin with non-steroidal anti-inflammatory drugs, ethinylestradiol, drug increases efficiency of indirect anticoagulants. Diuretics, Allopyrinolum, blockers of kanaltsiyevy secretion, non-steroidal anti-inflammatory drugs block kanaltsiyevy secretion, in the investigation of what concentration of benzylpenicillin in a blood plasma increases, the period of its semi-removal increases and the risk of toxic action increases. At combined use with Allopyrinolum the risk of development of skin rash increases. Benzylpenicillin reduces clearance and increases toxicity of a methotrexate, can reduce effect of oral contraceptives.

Contraindications:

– Hypersensitivity to benzylpenicillin and to other β-laktamny antibiotics (to penicillin, cephalosporins, karbapenem);
– bronchial asthma;
– hay fever;
– urticaria and other allergic diseases;
– epilepsy (for endolumbar introduction);
– feeding period breast.

Overdose:

It is shown by toxic action on TsNS (more often at endolumbar introduction). There is a reflex excitement, a headache, nausea, vomiting, spasms, a mialgiya, an arthralgia, symptoms of a meningism, lump. In such cases administration of drug should be stopped. Treatment – symptomatic which includes a hemodialysis it is necessary to pay peritoneal dialysis, special attention water electrolytically to balance.

Storage conditions:

Period of validity 3 years. To store in original packaging at a temperature not above 25 °C in unavailable for
children place.

Issue conditions:

According to the recipe

Packaging:

On 500 000 PIECES or 1 000 000 PIECES in bottles; in bottles No. 10 in a pack.