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., incl. 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. The connection with plasma proteins is about 90%. The half-life (T_1/2- 30 min). Time to reach the maximum concentration (TC_mOh) after intramuscular injection (w / m) - 1-2 hours, the concentration decreases rapidly 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. Does not penetrate the intact blood-brain barrier (BBB), with inflammation of the meninges, penetration increases. Penetrates through the placental barrier, is found in breast milk.

More than 40% after the / m introduction quickly excreted by the kidneys, with bile - 10%.

Indications:

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

Contraindications:

Hypersensitivity, including other beta-lactam antibiotics.

Carefully:

Allergic reactions in the anamnesis and / or bronchial asthma, chronic renal failure (CRF), enterocolitis on the background of antibiotics (in the anamnesis).

Pregnancy and lactation:

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

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

Dosing and Administration:

Intravenously (intravenously) and intramuscularly (in / m).

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, from 2 to 6 years - 2 g / day.

Newborn and premature children - 20-40 mg / kg / day.

Multiplicity of administration 4 times a day (every 4-6 hours).

When preparing solutions for intravenous injections in a bottle with 250 mg, add 1.5 ml, with 500 mg - 3 ml of water for injection.

In the preparation of solutions intended for intravenous administration, 250 mg or 500 mg are dissolved in 5 ml of water for injection or 0.9% solution of sodium chloride and injected slowly, for 5-10 minutes.

For IV injection of oxacillin, the sodium salt is dissolved in a 0.9% solution of sodium chloride or in a 5% solution of dextrose 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 2-3 weeks or more.

Side effects:

Allergic reactions (skin itching, hives, less often - angioedema, bronchospasm, in rare cases, anaphylactic shock, eosinophilia); dyspepsia (nausea, vomiting, diarrhea); pseudomembranous enterocolitis, candidiasis of the oral cavity, vaginal candidiasis; hepatotoxic effect - often develops at a dose higher than 6 g / day (hyperthermia, nausea, vomiting, icteric sclera or skin, increased activity of "liver" transaminases); hematuria, proteinuria, interstitial nephritis.

With the / in the introduction - 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 (drugs) that have a hepatotoxic effect.

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

LS, which block tubular secretion, increase the concentration of oxacillin in the blood.

Special instructions:

During pregnancy and lactation, they are prescribed only for "vital" indications.

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

Form release / dosage:

Powder for the preparation of solution for intravenous and intramuscular injection, 250 mg, 500 mg.

Packaging:

250 mg, 500 mg of oxacillin in bottles with a capacity of 10 ml or 20 ml.

1, 5, 10 bottles with instructions for use are placed in a pack of cardboard.

50 bottles are placed in a box of cardboard with the application of 5 instructions for use for delivery to hospitals.

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:Р N000067 / 03

Date of registration:18.09.2008

Expiration Date:Unlimited

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia

Information update date: & nbsp24.05.2017

Illustrated instructions

Instructions

Oxacillin (Oxacillin)