Oxacillin - instructions for use, dose, side effects, contraindications

Bactericidal antibiotic from the group of semisynthetic penicillins, is resistant to the action of penicillinase. It blocks the synthesis of the bacterial cell wall by disrupting the late stages of peptidoglycan synthesis (prevents the formation of peptide bonds by inhibiting transpeptidase), causes lysis of fissile bacterial cells.

It is active against gram-positive microorganisms: Staphylococcus spp. (including those producing penicillinase), Streptococcus spp., including Streptococcus pneumoniae, Corynebacterium diphtheriae, Bacillus anthracis, anaerobic spore-forming rods, Gram-negative cocci (Neisseria gonorrhoeae, Neisseria meningitidis), Actinomyces spp., Treponema spp.

It is inactive with respect to the majority of gram-negative bacteria, rickettsia, viruses, protozoa, fungi. Sustainability develops slowly.

Pharmacokinetics:Absorption is fast and complete. It is stable in slightly acidic medium. Connection with plasma proteins - about 90%.

The half-life of the drug is 30 minutes. The time to reach the maximum concentration of the drug in the plasma after intramuscular injection is 1-2 hours, the concentration rapidly decreases to 4 hours. With parenteral administration, higher concentrations are achieved in the blood than when ingested. In the pleural fluid is found in a concentration reaching 10%, synovial and ascitic fluid - 50%, bile - 5-8% in relation to its concentration in the blood serum. It does not penetrate the intact blood-brain barrier, with inflammation of the meninges, penetration increases. Penetrates through the placental barrier, is found in breast milk.

More than 40% of the drug after intramuscular injection is excreted by the kidneys, with bile 10%.

Indications:

Infectious diseases caused by gram-positive microorganisms that produce and do not produce penicillinase (septicemia, sepsis, abscess, phlegmon, cholecystitis, pielit, cystitis, osteomyelitis, postoperative, wound infections, infected burns, bacterial endocarditis, meningitis, sinusitis, pneumonia, empyema).

Contraindications:

Hypersensitivity, including other beta-lactam antibiotics.

Carefully:

Allergic reactions in the anamnesis and / or bronchial asthma, chronic renal failure, antibiotic-associated diarrhea (in the anamnesis).

Pregnancy and lactation:

The use of the drug during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

Action category for the fetus by FDA - AT.

Oxacillin is excreted in breast milk, therefore, if it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

Intravenous and intramuscular: adults and children over 6 years of age - 2-4 g / day, children under the age of 3 months - 60-80 mg / kg / day, from 3 months to 2 years - 1 g / day, 2 to 6 years - 2 g / day, newborns and premature infants - 20-40 mg / kg / day. Multiplicity of administration 4 times a day (every 4-6 hours).

When preparing solutions for intramuscular injection in a bottle with 0.5 g add 3 ml of water for injection.

When preparing solutions intended for intravenous fluid administration, every 0.5 g is dissolved in 5 ml of water for injection or 0.9% solution of sodium chloride and injected slowly, for 5-10 minutes.

For drip introduction, dissolve in a 0.9% solution of sodium chloride or in a 5% solution of glucose to a concentration of 0.5-2 mg / ml and injected for 1-2 hours at a rate of 60-100 cap / min. The duration of treatment is usually 7-10 days. In severe forms of the disease (sepsis, septic endocarditis, etc.), treatment can last for 2-3 weeks or more.

Side effects:

Allergic reactions: itching, hives, less often - angioedema, bronchospasm, in rare cases anaphylactic shock, eosinophilia.

From the cardiovascular system and blood: agranulocytosis, neutropenia, bone marrow suppression.

From the digestive system: dyspepsia (nausea, vomiting, diarrhea), pseudomembranous enterocolitis, candidiasis of the oral cavity, hepatotoxic effect - more often with a dose of 6 g / day (hyperthermia, nausea, vomiting, jaundice of the skin and sclera, increased activity of liver transaminases).

From the urinary system: hematuria, proteinuria, interstitial nephritis.

Other: vaginal candidiasis, with intravenous administration may develop thrombophlebitis.

Interaction:Increases the toxicity of methotrexate (competition for tubular secretion); it may be necessary to increase the doses of calcium folinate (antidote of folic acid antagonists) and its longer use.

The combination of ampicillin or benzylpenicillin with oxacillin is rational, since the latter, suppressing the activity of penicillinase, reduces thereby the destruction of ampicillin and benzylpenicillin. The spectrum of action with this combination becomes wider.

It is necessary to avoid joint use with other drugs that have a hepatotoxic effect.

It is not recommended to prescribe concomitantly with bacteriostatic antibiotics (decreased efficacy).

Drugs that block tubular secretion, increase the concentration of oxacillin in the blood.

Antacids and laxative drugs reduce the absorption of the drug from the gastrointestinal tract.

Special instructions:

It is inappropriate to use in infections caused by microorganisms that are sensitive to benzylpenicillin.

When allergic reactions occur, the antibiotic is canceled and desensitizing therapy is performed.

Effect on the ability to drive transp. cf. and fur:

Studies to evaluate the effect of the drug on the ability to drive vehicles and engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions have not been carried out.

Form release / dosage:

Powder for solution for intravenous and intramuscular injection, 0.5 g.

Packaging:

0.5 g of active substance into glass bottles with a capacity of 10 ml, hermetically sealed with rubber stoppers, crimped with aluminum caps or aluminum combined caps.

Vials with a drug of 20, 40, 50 vials are placed in a box with cardboard partitions, with an equal number of instructions for the use of the drug (for hospitals).

1 bottle with the drug and instructions for use are placed in a pack of cardboard.

Storage conditions:

In a dry place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N000394 / 01

Date of registration:02.05.2012 / 08.05.2013

Expiration Date:Unlimited

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Representation: & nbspBIOSINTEZ JSC BIOSINTEZ JSC Russia

Information update date: & nbsp24.05.2017

Illustrated instructions

Instructions

Oxacillin (Oxacillin)