Daptomycin


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Complicated skin and skin structure infections
Adult: 4 mg/kg once daily for 7-14 days given via infusion over 30 minutes or by injection over 2 minutes.
Child: 1-<2 years 10 mg/kg once daily via infusion over 60 minutes. 2-6 years 9 mg/kg once daily via infusion over 60 minutes. 7-11 years 7 mg/kg once daily via infusion over 30 minutes. 12-17 years 5 mg/kg once daily via infusion over 30 minutes. All doses are given for 14 days.

Intravenous
Staphylococcus aureus bacteraemia
Adult: 6 mg/kg once daily for 2-6 weeks given via infusion over 30 minutes.
Child: 1-6 years 12 mg/kg once daily via infusion over 60 minutes. 7-11 years 9 mg/kg once daily via infusion over 30 minutes. 12-17 years 7 mg/kg once daily via infusion over 30 minutes. Treatment duration may vary according to clinical response for up to 42-44 days.

Intravenous
Right-sided Staphylococcus aureus infective endocarditis
Adult: Caused by methicillin-susceptible and methicillin-resistant strains: 6 mg/kg once daily for 2-6 weeks given via infusion over 30 minutes.
Suy thận
Complicated skin and skin structure infections:
CrCl (mL/min) Dosage
<30 4 mg/kg once every 48 hours.

Staphylococcus aureus
bacteraemia; Right-sided Staphylococcus aureus infective endocarditis:
CrCl (mL/min) Dosage
<30 6 mg/kg once every 48 hours.
Hướng dẫn pha thuốc
Reconstitute vial labelled as 500 mg or 350 mg with 10 mL and 7 mL of 0.9% NaCl injection respectively. Gently rotate the vial to wet the powder and allow to stand for 10 minutes. Then, gently swirl or rotate the vial for a few minutes to obtain a clear reconstituted solution. Do not shake/agitate vial vigorously. For IV infusion, further dilute the reconstituted solution with 50 mL 0.9% NaCl injection.
Tương kỵ
Dextrose-containing solutions.
Chống chỉ định
Hypersensitivity.
Thận trọng
Patient with persisting or relapsing Staphylococcus aureus bacteraemia or endocarditis. Renal impairment. Children. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Eosinophillic pneumonia, drug reaction with eosinophilia and systemic symptoms (DRESS), hypersensitivity reactions, anaphylaxis, myopathy/rhabdomyolysis, peripheral neuropathy; fungal or bacterial superinfection, including C. difficile-associated diarrhoea (prolonged use); tubulointerstitial nephritis.
Blood and lymphatic system disorders: Anaemia.
Cardiac disorders: Supraventricular tachycardia, extrasystole.
Ear and labyrinth disorders: Vertigo.
Gastrointestinal disorders: Abdominal pain, nausea, vomiting, constipation, diarrhoea, flatulence, bloating, distention, dyspepsia, glossitis.
General disorders and administration site conditions: Infusion site reactions, pyrexia, asthenia.
Infections and infestations: Fungal infection, urinary tract infection, candida infection, fungaemia.
Investigations: Increased INR, ALT, AST, alkaline phosphatase, creatinine phosphokinase.
Metabolism and nutrition disorders: Decreased appetite, hyperglycaemia, electrolyte imbalance.
Musculoskeletal and connective tissue disorders: Limb pain.
Nervous system disorders: Dizziness, headache.
Psychiatric disorders: Anxiety, insomnia.
Skin and subcutaneous tissue disorders: Rash, pruritus.
Vascular disorders: Hypertension, hypotension.
Potentially Fatal: Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), pseudomembranous colitis.
Chỉ số theo dõi
Monitor CPK at least weekly during therapy. Monitor for signs and symptoms of eosinophilic pneumonia, muscle pain or weakness (especially in distal extremities), new onset or worsening peripheral neuropathy.
Tương tác
Enhanced adverse/toxic effects (e.g. myopathy) with HMG-CoA reductase inhibitors (e.g. simvastatin). Increased plasma concentration with NSAIDs. Synergistic antibacterial effects against staphylococci and enterococci with aminoglycosides, rifampicin, and β-lactam anti-infectives.
Ảnh hưởng đến kết quả xét nghiệm
False prolongation of prothrombin time (PT) and elevation of INR.
Tác dụng
Description: Daptomycin is a cyclic lipopeptide antibacterial. It binds to bacterial cell membranes and causes rapid depolarisation thereby leading to inhibition of DNA, RNA and protein synthesis thus resulting in bacterial cell death.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: 0.5-0.8 hours.
Distribution: Primarily distributed into extracellular space. Crosses the blood-brain barrier and placenta. Volume of distribution: 0.1 L/kg. Plasma protein binding: 90-93%, mainly to serum albumin.
Metabolism: Little or no metabolism is known, although minor amounts of oxidative metabolites have been detected.
Excretion: Via urine (78%, primarily as unchanged drug); faeces (approx 6%). Elimination half-life: 8-9 hours.
Đặc tính

Chemical Structure Image
Daptomycin

Source: National Center for Biotechnology Information. "PubChem Compound Summary for CID 16134395, Daptomycin" PubChem, https://pubchem.ncbi.nlm.nih.gov/compound/Daptomycin. Accessed 27 October, 2021.

Bảo quản
Store between 2-8°C. Avoid excessive heat. Reconstituted solution: Store at 25°C, stable for 12 hours; or between 2-8°C, stable for 24 hours.
Phân loại MIMS
Các loại kháng sinh khác
Phân loại ATC
J01XX09 - daptomycin ; Belongs to the class of other antibacterials. Used in the systemic treatment of infections.
Tài liệu tham khảo
Anon. Daptomycin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 11/08/2021.

Buckingham R (ed). Daptomycin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/08/2021.

Cubicin 350 mg Powder for Solution for Injection or Infusion (Merck Sharp & Dohme [UK] Limited). MHRA. https://products.mhra.gov.uk. Accessed 11/08/2021.

Cubicin 500 mg for Injection per vial (Merck Sharp & Dohme [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 11/08/2021.

Cubicin 500 mg Powder for Solution for Injection or Infusion (Merck Sharp & Dohme [UK] Limited). MHRA. https://products.mhra.gov.uk. Accessed 11/08/2021.

Cubicin Injection, Powder, Lyophilized for Solution (Merck Sharp & Dohme Corp.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 11/08/2021.

Daptomycin 500 mg Powder for Solution for Injection/Infusion (Xelia Pharmaceuticals ApS). MHRA. https://products.mhra.gov.uk. Accessed 11/08/2021.

Joint Formulary Committee. Daptomycin. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/08/2021.

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