Posaconazole


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Prophylaxis of invasive fungal infections
Adult: 300 mg bid on the 1st day, then 300 mg once daily thereafter. Treatment duration is based on recovery from neutropenia or immunosuppression.

Oral
Oropharyngeal candidiasis
Adult: As oral susp: 100 mg bid on the 1st day, then 100 mg once daily, for 13 days.

Oral
Prophylaxis of invasive fungal infections
Adult: As delayed-release tab: 300 mg bid on the 1st day, then 300 mg once daily thereafter. As oral susp: 200 mg tid. Treatment duration is based on recovery from neutropenia or immunosuppression.

Oral
Oropharyngeal candidiasis refractory to itraconazole and/or fluconazole
Adult: As oral susp: 400 mg bid. Treatment duration is based on patient's underlying disease and clinical response.
Cách dùng
Should be taken with food. Take w/ a full meal or w/ a liqd nutritional supplement in patients who cannot eat a full meal.
Hướng dẫn pha thuốc
Intravenous:
Equilibrate the refrigerated vial to room temp. Contents of vial should be withdrawn and admixed w/ D5W or NSS 150 mL.
Chống chỉ định
Hypersensitivity. Co-admin w/ sirolimus, ergot alkaloids (e.g. ergotamine, dihydroergotamine), CYP3A4 substrates (terfenadine, astemizole, cisapride, pimozide, halofantrine, or quinidine), and HMG-CoA reductase inhibitors (e.g. simvastatin, lovastatin, atorvastatin).
Thận trọng
Patient w/ potentially proarrhythmic conditions. Hepatic impairment. Pregnancy and lactation.
Phản ứng phụ
Headache, nausea, abdominal pain, anorexia, asthenia, back pain, diarrhoea, dyspepsia, dizziness, dry mouth, dry skin, fatigue, fever, flatulence, hot flushes, insomnia, neutropenia, paraesthesia, pruritus, rash, somnolence, vomiting, increased liver enzyme values.
Potentially Fatal: Hypersensitivity reactions, including Stevens-Johnson syndrome. Severe hepatotoxicity, QT-prolongation.
Thông tin tư vấn bệnh nhân
May impair ability to drive or operate machinery.
MonitoringParameters
Monitor hepatic and renal function, electrolyte disturbances (e.g. Ca, Mg, K), CBC, breakthrough fungal infections and adequate oral intake.
Tương tác
Decreased plasma concentrations w/ efavirenz, fosamprenavir, cimetidine, esomeprazole, metoclopramide, phenytoin and rifabutin. May increase plasma concentration of ritonavir and atazanavir. May increase risk of neurotoxicity w/ vinca alkaloids (e.g. vincristine, vinblastine). May increase plasma concentrations of tacrolimus, ciclosporin, midazolam, Ca channel blockers (e.g. verapamil, diltiazem, nifedipine, nicardipine, felodipine) and digoxin.
Potentially Fatal: May increase sirolimus blood concentrations. May increase risk of QT prolongation or torsades de pointes of CYP3A4 substrates (e.g. terfenadine, astemizole, cisapride, pimozide, halofantrine, or quinidine). May increase risk of rhabdomyolysis w/ HMG-CoA reductase inhibitors (e.g. atorvastatin, lovastin, simvastatin). May increase risk of ergotism w/ ergot alkaloids (e.g. ergotamine and dihydroergotamine.
Food Interaction
Food, acidic carbonated beverages (e.g. ginger ale) or liquid nutritional supplement increases absorption.
Tác dụng
Description: Blocks the synthesis of ergosterol, a key component of the fungal cell membrane, through the inhibition of the enzyme lanosterol-14α-demethylase and accumulation of methylated sterol precursors. Posaconazole has activity against Candida spp., Aspergillus spp., Coccidioides immitis, Fonsecaea pedrosoi, and some species of Fusarium and zygomycetes.
Pharmacokinetics:
Absorption: Slowly absorbed from the GI tract. Absorption may be increased w/ food. Time to peak plasma concentration: Approx 5 hr.
Distribution: Plasma protein binding: >98%.
Metabolism: Not significantly metabolised; approx 15-17% is metabolised via hepatic glucuronidation.
Excretion: Mainly via faeces (77%; 66% as unchanged drug); urine (approx 14%, w/ only trace amounts excreted unchanged). Mean elimination half-life: 35 hr.
Đặc tính

Chemical Structure Image
Posaconazole

Source: National Center for Biotechnology Information. PubChem Database. Posaconazole, CID=468595, https://pubchem.ncbi.nlm.nih.gov/compound/Posaconazole (accessed on Jan. 23, 2020)

Bảo quản
Intravenous:
Store between 2-8°C.
Oral:
Tab: Store between 20-25°C. Oral susp: Store at 25°C.
Phân loại MIMS
References
Anon. Posaconazole. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 09/07/2014.

Buckingham R (ed). Posaconazole. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/07/2014.

McEvoy GK, Snow EK, Miller J et al (eds). Posaconazole. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 09/07/2014.

Noxafil Oral Suspension. U.S. FDA. https://www.fda.gov/. Accessed 14/07/2014.

Noxafil Suspension, Tablet Coated, Solution (Merck Sharp & Dohme Corp.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 09/07/2014.

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