Cloxacillin


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Bacterial infections
Adult: Staphylococcal infections resistant to benzylpenicillin: 250-500 mg 6 hourly. Dose and duration of therapy may vary depending on infecting organism, severity of infection and patient’s clinical response. Max: 6,000 mg daily.
Child: ≤20 kg: 25-50 mg/kg daily in divided doses; >20 kg: Same as adult dose.

Parenteral
Bacterial infections
Adult: Staphylococcal infections resistant to benzylpenicillin: As cloxacillin Na: 250-500 mg 6 hourly via IM inj, IV inj or IV infusion; may be increased in severe infections. Dose and duration of therapy may vary depending on infecting organism, severity of infection and patient’s clinical response. Max: 6,000 mg daily.
Child: ≤20 kg: 25-50 mg/kg daily in divided doses; >20 kg: Same as adult dose.
Cách dùng
Should be taken on an empty stomach. Take 1 hr before or 2 hr after meals.
Hướng dẫn pha thuốc
IM: Dilute with appropriate volume of sterile water for inj to a final concentration of 125 mg/mL or 250 mg/mL. IV inj: Dilute with appropriate volume of sterile water for inj to a final concentration of 50 mg/mL or 100 mg/mL. IV infusion: Dilute with appropriate volume of sterile water for inj to make a concentration of 250 mg/mL; dilute further with a compatible solution (e.g. normal saline solution, dextrose 5% in water). Oral susp: Dilute with appropriate amount of water as specified in the bottle. Shake vigorously until suspended.
Tương kỵ
Incompatible with aminoglycosides.
Chống chỉ định
Hypersensitivity to cloxacillin, other penicillins, or cephalosporins.
Thận trọng
Patients with asthma, blood disorders, history of seizure disorder, inflamed meninges. Patients undergoing cardiopulmonary bypass. Children. Renal and hepatic impairment. Pregnancy and lactation.
Phản ứng phụ
Significant: Haematologic disorders (e.g. neutropenia, agranulocytosis, anaemia, thrombocytopenia), bacterial or fungal superinfection (including pseudomembranous colitis, C. difficile-associated diarrhoea).
Gastrointestinal disorders: Diarrhoea, loose stools, nausea, vomiting, flatulence, epigastric distress, abdominal pain, stomatitis.
General disorders and administration site conditions: Lethargy, fever.
Immune system disorders: Urticaria, serum sickness-like reaction.
Investigations: Increased serum ALT, AST, alkaline phosphatase.
Musculoskeletal and connective tissue disorders: Twitching.
Nervous system disorders: Myoclonus, seizure.
Psychiatric disorders: Confusion.
Renal and urinary disorders:
Haematuria, proteinuria, renal insufficiency, renal tubular disease, interstitial nephritis.
Respiratory, thoracic and mediastinal disorders: Laryngospasm, bronchospasm, sneezing, wheezing.
Vascular disorders: Hypotension, thrombophlebitis.
Potentially Fatal: Anaphylactoid/hypersensitivity reactions.
MonitoringParameters
Monitor CBC with differential prior to initiation of treatment and weekly thereafter; periodic tests for renal (e.g. urinalysis, BUN, creatinine) and hepatic function. Monitor for signs of anaphylaxis during the 1st dose.
Tương tác
Increased serum concentration with probenecid. May increase serum concentration of methotrexate. May interfere with the anticoagulant effect of vitamin K antagonists (e.g. warfarin). Tetracycline may diminish the effect of cloxacillin.
Food Interaction
Food reduces cloxacillin absorption.
Lab Interference
May cause false-positive test results for urine and serum proteins, uric acid and urinary steroids. May interfere with urinary glucose tests using cupric sulfate (Benedict's solution, Clinitest).
Tác dụng
Description: Cloxacillin is a bactericidal antibiotic that binds to 1 or more of the penicillin-binding proteins (PBPs) which in turn inhibit the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thereby inhibiting cell wall synthesis. This results to bacterial lysis due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.
Pharmacokinetics:
Absorption: Incompletely absorbed from the gastrointestinal tract. Food reduces absorption by approx 50%. Time to peak plasma concentration: 1-2 hours (oral); 30 minutes (IM).
Distribution: Widely distributed into body fluids and bone. Crosses the placenta and enters breast milk. Little diffusion into the CSF, except when the meninges are inflamed. Plasma protein binding: Approx 94%, mainly to albumin.
Metabolism: Limited.
Excretion: Via urine (approx 35% of an oral dose, as unchanged drug and metabolites) and bile (≤10%). Plasma half-life: 0.5-1.5 hours.
Đặc tính

Chemical Structure Image
Cloxacillin

Source: National Center for Biotechnology Information. PubChem Database. Cloxacillin, CID=6098, https://pubchem.ncbi.nlm.nih.gov/compound/Cloxacillin (accessed on Jan. 21, 2020)

Bảo quản
Cap: Store below 30°C. Protect from light. Powder for susp: Store below 25°C; refrigerate (2-8°C) after reconstitution and discard after 14 days. Powder for inj: Store between 15-30°C. Reconstituted solution: Store below 25°C (stable for 24 hours) or between 2-8°C (stable for 48 hours).
Phân loại MIMS
Phân loại ATC
J01CF02 - cloxacillin ; Belongs to the class of beta-lactamase resistant penicillins. Used in the systemic treatment of infections.
References
Anon. Cloxacillin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/11/2019.

Buckingham R (ed). Cloxacillin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 31/10/2019.

Cloxacillin Capsule/Powder for Syrup (Idaman Pharma Manufacturing Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my/. Accessed 04/11/2019.

Cloxacillin Injectable. Medecins Sans Frontieres. https://medicalguidelines.msf.org/. Accessed 04/11/2019.

Dyna Cloxacillin Capsule (Dynapharm Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my/. Accessed 04/11/2019.

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