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

● blockade of the enzyme transpeptidase, which provides the connection of peptidoglycan chains with pentaglycine bridges, the final stage of the synthesis of the peptidoglycan polymer;

● oppression of the endogenous inhibitor of autolysins, resulting in an increase in the activity of autolysins and destruction of peptidoglycan. The cleavage of peptidoglycan plays a key role in the division of bacterial cells.

As a result, a breakdown in the structure of the peptidoglycan of a microbial cell and the subsequent death of bacteria occur. This determines the bactericidal effect.

The drug is active against mainly gram-positive bacteria - Staphylococcus spp., (including penicillinase-forming), Streptococcus spp., Streptococcus pneumoniae, Corynebacterium diphtheria and Bacillus anthracis, anaerobic spore-forming strains, some gram-negative microorganisms (Neisseria gonorrhoeae, Neisseria meningitides), Actinomyces spp.

Pharmacokinetics:

Quickly and completely absorbed in the gastrointestinal tract. The time to reach the maximum concentrationafter intramuscular injection - 1-2 hours, the concentration decreases rapidly to 4 hours. The connection with plasma proteins is 93%. 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. The drug penetrates the placental barrier and is excreted in breast milk. Does not penetrate intact GEB, with inflammation of the meninges, penetration increases. Metabolised by the liver. The half-life is 30 minutes. The drug is excreted by the kidneys.

Indications:

Infectious-inflammatory diseases caused by sensitive microorganisms, prevention of such infections:

sepsis;
abscess;
phlegmon;
cholecystitis;
pyelitis;
cystitis;
osteomyelitis;
postoperative, wound infections, infected burns;
bacterial endocarditis;
meningitis;
sinusitis.

ICD-10

I.A30-A49.A41.2 Septicemia caused by unspecified staphylococcus

I.A50-A64.A53.9 Syphilis, unspecified

VI.G00-G09.G00 Bacterial meningitis, not elsewhere classified

VI.G00-G09.G00.3 Staphylococcal meningitis

IX.I30-I52.I33 Acute and subacute endocarditis

X.J00-J06.J01 Acute Sinusitis

X.J00-J06.J03 Acute tonsillitis

X.J00-J06.J04 Acute laryngitis and tracheitis

X.J10-J18.J15 Bacterial pneumonia, not elsewhere classified

X.J10-J18.J15.2 Pneumonia caused by staphylococcus aureus

X.J20-J22.J20 Acute bronchitis

X.J30-J39.J31 Chronic rhinitis, nasopharyngitis and pharyngitis

X.J30-J39.J32 Chronic Sinusitis

X.J30-J39.J35.0 Chronic tonsillitis

X.J30-J39.J37 Chronic laryngitis and laryngotracheitis

X.J40-J47.J42 Chronic bronchitis, unspecified

X.J85-J86.J86 Pythothrace

XI.K80-K87.K81 Cholecystitis

XII.L00-L08.L01 Impetigo

XII.L00-L08.L02 Abscess of skin, boil and carbuncle

XII.L00-L08.L03 Phlegmon

XII.L00-L08.L08.0 Pyoderma

XIII.M00-M03.M00 Pyogenic arthritis

XIII.M86-M90.M86 Osteomyelitis

XIV.N10-N16.N12 Tubulointerstitial nephritis, not specified as acute or chronic

XIV.N30-N39.N30 Cystitis

XIX.T20-T32.T30 Thermal and chemical burns, unspecified

XIX.T79.T79.3 Post-traumatic wound infection, not elsewhere classified

Contraindications:

Hypersensitivity.

Carefully:

Allergic reactions in the anamnesis, kidney disease, bronchial asthma, enterocolitis on the background of antibiotics, pregnancy and lactation.

Pregnancy and lactation:

Category FDA - B. Apply if only the potential benefit to the mother exceeds the risk to the fetus. When taking during breastfeeding, you should stop breastfeeding.

Dosing and Administration:

Dosing regimen is individual.

Inside appoint for 1 h before meals or 2-3 hours after meals.

Single dose for adults, children and adolescents with a body weight of more than 40 kg with oral administration - 0.5-1 g every 4-6 hours; at intramuscular / intravenous administration - 0,25-1 g every 4-6 hours. Children weighing less than 40 kg inside - 12.5-25 mg / kg every 6 hours; at intramuscular / intravenous administration - 12,5-25 mg / kg every 4-6 hours.

Newborn and premature babies intramuscularly / intravenously 6.25 mg per kg every 6 hours.

The maximum daily dose is 6 g.

The duration of treatment is usually 7-10 days, with severe diseases (sepsis, septic endocarditis) - 2-3 weeks and more.

Side effects:

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

From the side digestive system: increased activity of hepatic transaminases, nausea, vomiting, diarrhea, liver disease.

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

Other: dysbacteriosis, candidiasis of the oral cavity, thrombophlebitis, vaginal candidiasis, pseudomembranous colitis.

Overdose:

Increased side effects. Treatment is symptomatic.

When the drug is prescribed in a dose higher than 6 g per day, a hepatotoxic effect develops (hyperthermia, nausea, vomiting, icteric sclera or skin, increased activity of "liver" transaminases).

Interaction:

Tetracyclines and others bacteriostatic antibiotics reduce the effectiveness of oxacillin.

Application simultaneously with methotrexate increases the hepatotoxicity of the latter (competition for tubular secretion). It may be necessary to increase the doses of calcium folinate (antidote for antagonists of folic acid) and its longer use.

Combination ampicillin or benzylpenicillin with oxacillin is rational, since oxacillin Penicillin-resistant and the spectrum of action with this combination becomes wider.

Probenecid, blocking tubular secretion, prolongs elimination and increases the concentration of oxacillin in the serum.

Do not use with drugs that have a hepatotoxic effect.

Special instructions:

Impact on the ability to drive vehicles and manage mechanisms not found.

Instructions

Oxacillin (Oxacillinum)