-          Cloxacillin is indicated for the treatment of sensitive staphylococcal infections: respiratory infections, otorhinolaryngologic infections, renal infections,  urogenital infections, neuro-meningeal infections, bone and joint infections, endocarditis, and treatment of skin infections caused by sensitive staphylococci and/or streptococci 

-          Cloxacillin is also indicated as preventive treatment of postoperative infections in neurosurgery

 

Monoclox injection is for intramuscular or intravenous administration.

Preparation of the solution for i.m administration: Add 5 ml of water for injections into each vial of Monoclox 1g, respectively and shake well until complete dissolution. The solution should not be mixed with another product. Any solution left pending must be discarded.

The content of each vial of Monoclox 250 mg should be dissolved in 1.5ml of water for injections and shake well until complete dissolution. The solution should not be mixed with another product. Any solution left pending must be discarded.

The content of each vial of Monoclox 500 mg should be dissolved in 2.5ml of water for injections and shake well until complete dissolution. The solution should not be mixed with another product. Any solution left pending must be discarded.

 

DO NOT USE INTRAMUSCULAR SOLVENT BY INTRAVENOUS ROUTE.

Preparation for i.v. administration: Add 20 ml of water for injections into each vial of Monoclox 1g, respectively and shake well. For intravenous injection each vial of Monoclox 250 mg and 500 mg, respectively, should be dissolved in 10-20ml water for injection and shake well. 

For slow intravenous infusion Monoclox can be further diluted in 100 ml of an infusion fluid. Infuse the solution slowly over a period of 60 minutes.

Dosage (in patients with normal renal and hepatic function): 

-          Treatment of infections:

Adults: 8 to 12 g / day, divided into 4-6 daily administrations

 

-          Children: 100 to 200 mg / kg / day divided into 4-6 daily administrations, without exceeding 12 g / day.

 

-          - Prevention of postoperative infections in adults: the antibioprophylaxis must be of short duration, usually limited to the intraoperative period, 24 hours, but never more than 48 hours:

-          2 g IV with induction of anesthesia,

-          thereafter 1 g IV every 2 hours in case of prolonged intervention

The duration of treatment should cover the entire duration of the surgery until skin closure.

 

  

Monoclox is contraindicated to patients who are hypersensitive to cloxacillin or other penicillins, cephalosporins, or penicillamine. Monoclox should not be administered by sub-conjunctival injection. The administration of cloxacillin in newborns is contraindicated.

Cloxacillin should be given with caution to patients who have had previous hypersensitivity reactions (anaphylactic reactions) to the cephalosporin’s, penicillin’s or other drugs. If serious acute hypersensitivity or allergic reactions take place, patients should be treated with pressor amines, antihistamines corticosteroids and/or other emergency measures. Hypersensitivity reactions can sometimes be quite severe or even fatal. Even though anaphylaxis is more likely to happen after parenteral administration they have also been induced by oral administration as well.

 

Extensive use of antibiotics may encourage the overgrowth of non-susceptible organisms, including fungi. In such a case, appropriate measures should be taken. It is also advised to evaluate, periodically, the renal, hepatic and hematopoietic systems.

 

In streptococcal infections, treatment must be adequate to eliminate the organism (10 days minimum); otherwise the sequelae of streptococcal disease may occur. The cultures should be taken when the treatment has finished so to determine whether streptococci have been eradicated.

 

 

 

Bacteriostatic antibiotics given concurrently with cloxacillin might decrease the bacteriocidal effect of penicillins as it has been shown in vitro. Nevertheless, the clinical significance of this interaction is not well documented.

Beta-adrenergic blockers given with cloxacillin can induce anaphylactic reactions that would  make it even more difficult to treat anaphylaxis due to allergic reaction.

Chloramphenicol and cloxacillin co-administration would result to weaken the penicillin’s effect and to increase the half-life of chloramphenicol. 

Oral anticoagulants or heparin administrated in conjunction with high dosage of IV penicillins turn the anticoagulants agents less effective and possibly increase the risk of bleeding.

Probenecid tends to block the renal tubular secretion of penicillins and in consequence penicillins stays longer in the blood circulation.

Oral contraceptives and concomitant use of penicillins has been related with unintended pregnancies and menstrual changes. The reason being that penicillins interfere with the absorption of oral contraceptives.

 

In clinical practice , analysis of a large number of exposed pregnancies did not appear to reveal any malformative or foetotoxic effect of penicillins.

Therefore, cloxacillin may be prescribed during pregnancy if necessary.

 

Lactation

Because cloxacillin passes into breast milk, possible suspension of breast feeding should be envisaged.

 

Cloxacillin does not influence the patient’s ability to drive or operate machinery.

Cloxacillin, as other penicillins produces rarely adverse reactions and they are usually mild and ephemeral.  Allergic reactions have been reported whose symptoms are fever, urticarial rash, eosinophilia, Quincke’s edema, and very seldom anaphylactic shock.

Skin rashes maculopapular have been reported which may be of allergic origin or not. Very rare there have been reported cases Stevens-Johnson syndrome  and polymorph erythema.

Gastrointestinal disorders have been reported which include nausea, vomit, diarrhea. 

Colitis pseudo membranous has seldom been reported and in such case the uptake of cloxacillin should be discontinue. 

Cholestatic jaundice has infrequently been produced. 

Augmentation of the transaminase enzymes ASAT and ALAT and hepatic icterus have rarely been induced.

Possibility of acute immuno-allergic interstitial nephritis.

Hematological reactions which are reversible including anemia, thrombopenia and leucopenia have occasionally occurred.

High dosage of cloxacillin given to patients especially to those with renal insufficiency, may induce encephalopathies which includes conscience troubles, non-physiological movement and sudden attacks of convulsion. 

 

There has not been reported any incident of overdose of cloxacillin but should it occur discontinue medication, treat symptomatically and institute supportive measures as required.

 

ANTIBACTERIAL ANTIBIOTICS of the beta-lactam family of the penicillin M group (J : Anti-infectious)

 

ANTIBACTERIAL ACTIVITY SPECTRUM

 

Critical concentrations separate the sensitive strains from the strains with intermediate sensitivity and the latter from the resistant ones:

Oxacillin (staphylococcus): S ≤ 2 mg/l and R > 2 mg/l

The prevalence of acquired resistance may vary according to geography and the weather for certain species. It is therefore useful to have information on local resistance prevalence, especially for the treatment of severe infections. These data can only give an indication about the probability of a bacterial starin’s sensitivity to this antibiotic.

Cloxacillin is stable in gastric environment. It is well absorbed by the digestive mucous (70%).

 

Distribution

-          After oral administration, maximum blood concentrations are obtained after 1 hour and are proportional to the administered dose. They are in order of 9 mg/l for one dose of 500 mg.

 

-          After intramuscular injection, maximum blood concentrations are obtained after about 45 minutes. In adults, they are 26 mg/l for one dose of 1g, 15 mg/l for one dose of 500 mg and 8 mg/l for one dose of 250 mg.

 

-          After intravenous injection of 2g perfused for 20 minutes, the value of serum peak obtained at the end of the perfusion is 280 mg/l.

 

-          Half-life is in the order of 45 minutes in patients with normal renal functions.

 

-          Plasma protein bounding is in the order of 90%.

 

-          The product diffuses the foetal blood, synovial liquid and bone tissue into the amniotic fluid.

 

 

Biotransformation

Cloxacillin is metabolized to a limited extend. 

 

Excretion

 

After oral administration, the non-absorbed fraction is eliminated by the intestinal route in an inactive form. The absorbed fraction is eliminated in an active form essentially through urine and for 10% through the bile duct.

After administration by injection, the elimination is:

-Urinary, in an active form, in 6 hours, approximately 70 to 80% of the injected dose - Biliary, in an active form, 20 to 30% of the injected dose.

 

Animal studies showed no teratogenesis, carkinogenesis or mutagenesis. There have been no relevant studies with humans.

None

Cloxacillin is incompatible with solutions of aminoacids, lipid emulsions and blood for transfusion

24 months (2 years) Reconstituted solution: The product should be used immediately.

below 25°C.

Colourless soda lime type III glass vials, nominal capacity 8 ml sealed with 20mm rubber stopper, and aluminium caps, labelled, and packed in a card carton. Boxes of 1, 10, 25, 50 and 100 vials are available.

 

None