Flucloxacillin

Inhalation/Respiratory
Infections due to staphylococci resistant to benzylpenicillin

Intra-articular
Infections due to staphylococci resistant to benzylpenicillin

Intramuscular
Infections due to staphylococci resistant to benzylpenicillin

Intrapleural
Infections due to staphylococci resistant to benzylpenicillin

Intravenous
Infections due to staphylococci resistant to benzylpenicillin

Intravenous
Endocarditis

Intravenous
Osteomyelitis

Oral
Infections due to staphylococci resistant to benzylpenicillin

Parenteral
Prophylaxis of surgical infections

Severe (CrCl <10 mL/min): Dosage adjustment may be necessary.

Should be taken on an empty stomach. Take 30 min-1 hr before meals.

Intramuscular:
Add 1.5 mL of water for inj to 250 mg vial contents or 2 mL of water for inj to 500 mg vial contents.
Intravenous:
Dissolve 250-500 mg in 5-10 mL water for inj or 1 g in 15-20 mL water for inj. For IV infusion, further dilute in suitable IV fluids (e.g. water for inj, NaCl 0.9%, glucose 5%, NaCl 0.18% w/ glucose 4%).
Intrapleural:
Dissolve 250 mg in 5-10 mL water for inj.
Intra-articular:
Dissolve 250-500 mg in up to 5 mL water for inj or lidocaine HCl 0.5% soln for inj.
Inhalation:
Dissolve 125-250 mg powd for inj in 3 mL water for inj.

Aminoglycosides, amiodarone, atropine sulfate, buprenorphine, Ca gluconate, chlorpromazine HCl, ciprofloxacin, clarithromycin, diazepam, dobutamine HCl, erythromycin lactobionate, gentamicin sulfate, metoclopramide HCl, morphine sulfate, netilmicin sulfate, ofloxacin, papaveretum, pethidine HCl, prochlorperazine edisilate, promethazine HCl, tobramycin, verapamil HCl. Flucloxacillin should not be mixed w/ blood products or other proteinaceous fluids (e.g. protein hydrolysates) or w/ IV lipid emulsions.

Hypersensitivity to flucloxacillin and other penicillins. Patient w/ history of flucloxacillin-associated jaundice/hepatic dysfunction.

Patient w/ spirochaete infections (e.g. syphilis, leptospirosis), history of hypersensitivity to β-lactam antibiotics. Newborn infants. Hepatic or renal impairment. Pregnancy and lactation.

Transient leucopenia, thrombocytopenia, haemolytic anaemia, agranulocytosis, neutropenia, sensitivity reactions (e.g. urticaria, maculopapular rashes, pruritus, fever, joint pains, angioedema), serum sickness-like reactions, nephropathy, acute interstitial nephritis, electrolyte disturbances, hallucinations, convulsions, dyspnoea, bronchospasm, diarrhoea, nausea, vomiting, candidiasis, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema nodosum, pemphigoid reactions, non-thrombocytopenic purpura, vasculitis, acute attacks of porphyria, phlebitis (IV).
Potentially Fatal: Anaphylaxis, pseudomembranous colitis, Jarisch-Herxheimer reaction (in patients w/ spirochaete infections, esp in CV syphilis). Rarely, hepatitis, cholestatic jaundice.

Monitor renal, hepatic and haematological status during prolonged and high-dose therapy.

Symptoms: Neurotoxicity (e.g. convulsions, encephalopathy), GI effects (e.g. nausea, vomiting, diarrhoea), blood disorders (e.g. neutropenia, haemolytic anaemia, prolongation of bleeding time, defective platelet function), electrolyte disturbances. Management: Symptomatic treatment.

May increase the risk of methotrexate toxicity. May decrease the efficacy of oestrogen-containing OC. Enhanced plasma concentrations w/ probenecid. Bacteriostatic drugs (e.g. chloramphenicol, tetracycline) may interfere w/ the bactericidal effect of flucloxacillin. May prolong bleeding time in patients on oral anticoagulants.

Absorption is reduced by the presence of food.

False-positive results w/ Coombs' test, falsely high urinary glucose results w/ the copper sulfate test and falsely high urinary protein results.

Description:
Mechanism of Action: Flucloxacillin inhibits the 3rd and last step of bacterial cell wall synthesis by binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall. It is active against penicillinase-producing and non-penicillinase-producing staphylococci.
Pharmacokinetics:
Absorption: Absorbed from the GI tract. Absorption is reduced by the presence of food. Time to peak plasma concentration: Approx 1 hr (oral); approx 30 min (IM).
Distribution: Diffuses well into most tissue and enters breast milk (small amounts). Plasma protein binding: Approx 95%.
Metabolism: Limited metabolism.
Excretion: Via urine as unchanged drug and metabolites (oral: approx 66%, parenteral: 76%) and bile (small amount). Plasma half-life: Approx 1 hr.

Source: National Center for Biotechnology Information. PubChem Database. Flucloxacillin, CID=21319, https://pubchem.ncbi.nlm.nih.gov/compound/Flucloxacillin (accessed on Jan. 21, 2020)

Store below 25°C. Reconstituted soln: Store between 2-8°C.

Penicillins

Anon. Flucloxacillin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 26/06/2014.

Buckingham R (ed). Flucloxacillin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 26/06/2014.