Flucloxacillin


Thông tin thuốc gốc
Chỉ định và Liều dùng
Inhalation/Respiratory
Infections due to staphylococci resistant to benzylpenicillin
Adult: 125-250 mg powd for inj dissolved in water for inj and inhaled by nebuliser 6 hrly in conjunction w/ systemic therapy.
Child: <2 yr Quarter of the adult dose; 2-10 yr Half of the adult dose.

Intra-articular
Infections due to staphylococci resistant to benzylpenicillin
Adult: 250-500 mg daily in conjunction w/ systemic therapy.
Child: <2 yr Quarter of the adult dose; 2-10 yr Half of the adult dose.

Intramuscular
Infections due to staphylococci resistant to benzylpenicillin
Adult: 250 mg 6 hrly. Dose may be doubled in severe infections.
Child: <2 yr Quarter of the adult dose; 2-10 yr Half of the adult dose.

Intrapleural
Infections due to staphylococci resistant to benzylpenicillin
Adult: 250 mg daily in conjunction w/ systemic therapy.
Child: <2 yr Quarter of the adult dose; 2-10 yr Half of the adult dose.

Intravenous
Infections due to staphylococci resistant to benzylpenicillin
Adult: 0.25-1 g 6 hrly, via slow inj over 3-4 min, or by infusion. Dose may be doubled in severe infections.
Child: <2 yr Quarter of the adult dose; 2-10 yr Half of the adult dose.

Intravenous
Endocarditis
Adult: ≤85 kg: Up to 8 g daily in 4 divided doses; >85 kg: Up to 12 g daily in 6 divided doses.

Intravenous
Osteomyelitis
Adult: Up to 8 g daily in 3-4 divided doses.
Child: <2 yr Quarter of the adult dose; 2-10 yr Half of the adult dose.

Oral
Infections due to staphylococci resistant to benzylpenicillin
Adult: 250 mg 4 times daily. Dose may be doubled in severe infections.
Child: <2 yr 62.5 mg 4 times daily; 2-10 yr 125 mg 4 times daily.

Parenteral
Prophylaxis of surgical infections
Adult: 1-2 g IV at induction of anaesth followed by 500 mg 6 hrly, IV or IM.
Child: <2 yr Quarter of the adult dose; 2-10 yr Half of the adult dose.
Renal Impairment
Severe (CrCl <10 mL/min): Dosage adjustment may be necessary.
Cách dùng
Should be taken on an empty stomach. Take 30 min-1 hr before meals.
Hướng dẫn pha thuốc
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.
Tương kỵ
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.
Chống chỉ định
Hypersensitivity to flucloxacillin and other penicillins. Patient w/ history of flucloxacillin-associated jaundice/hepatic dysfunction.
Thận trọng
Patient w/ spirochaete infections (e.g. syphilis, leptospirosis), history of hypersensitivity to β-lactam antibiotics. Newborn infants. Hepatic or renal impairment. Pregnancy and lactation.
Phản ứng phụ
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.
MonitoringParameters
Monitor renal, hepatic and haematological status during prolonged and high-dose therapy.
Quá liều
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.
Tương tác
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.
Food Interaction
Absorption is reduced by the presence of food.
Lab Interference
False-positive results w/ Coombs' test, falsely high urinary glucose results w/ the copper sulfate test and falsely high urinary protein results.
Tác dụng
Description: 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.
Đặc tính

Chemical Structure Image
Flucloxacillin

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

Bảo quản
Store below 25°C. Reconstituted soln: Store between 2-8°C.
Phân loại MIMS
References
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.

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