Noxafil Tablets / Gastro-Resistant
Posaconazole
100mg
Merck Sharp & Dohme B.V.
| Pack size | 24's (12's Blister x 2) |
|---|---|
| Dispensing mode | POM |
| Source | NETHERLANDS |
| Agent | CITY MEDICAL STORE |
| Retail Price | 3923.50 AED |
Indications
Noxafil Tablets / Gastro-Resistant is used for:
Prophylaxis of invasive Aspergillus, Candida Infections, Oropharyngeal candidiasis
Adult Dose
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
Adult: As oral susp: 100 mg bid on the 1st day, then 100 mg once daily, for 13 days.
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.
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.
Child Dose
Invasive Aspergillus & Candida Infections
Indicated for prophylaxis of invasive Aspergillus and Candida infections in patients who are at high risk of developing these infections due to being severely immunocompromised (eg, hematopoietic stem cell transplant recipients with GVHD, hematologic malignancies with prolonged neutropenia from chemotherapy)
<18 years (IV): Safety and efficacy not established
<13 years (tablets and oral suspension): Safety and efficacy not established
>13 years
Oral suspension: 200 mg (5 mL) TID
Tablet: 300 mg PO BID on Day 1, then 300 mg PO qDay
Duration of therapy is based on recovery from neutropenia or immunosuppression
Oropharyngeal Candidiasis
Oral suspension is indicated for oropharyngeal candidiasis
<13 years: Safety and efficacy not established
>13 years
Oral suspension: 100 mg (2.5 mL) PO BID on Day 1, then 100 mg PO qDay for 13 days
Refractory to itraconazole and/or fluconazole: 400 mg (10 mL) PO BID; duration based on severity of underlying disease and clinical response
Renal Dose
Moderate-to-severe renal impairment (IV)
eGFR <50 mL/min: Avoid IV administration unless benefit/risk assessment justifies use
Accumulation of the IV vehicle, SBECD, is expected to occur
Serum creatinine levels should be closely monitored; if increases occur, consideration should be given to changing to oral posaconazole therapy
Severe renal impairment (tablets or oral suspension)
Variability of systemic exposure with tablets or oral suspension observed
Monitored closely for breakthrough fungal infections
Administration
IV Preparation
Equilibrate the refrigerated vial to room temperature
Aseptically transfer 16.7 mL (300 mg) of solution to an IV bag/bottle containing approximately 150 mL of 5% dextrose in water or sodium chloride 0.9%
Should only be administered with these diluents; use of other infusion solutions may result in particulate formation
Posaconazole injection is a single dose sterile solution without preservatives; once admixed, the product should be used immediately
The diluted solution ranges from colorless to yellow
IV Administration
Must be administered through a 0.22 micron polyethersulfone (PES) or polyvinylidene difluoride (PVDF) filter
Should be administered via a central venous line, including a central venous catheter or peripherally inserted central catheter (PICC), by slow IV infusion over ~90 minutes
If a central venous catheter is not available, may administer through a peripheral venous catheter by slow IV infusion over 30 minutes only as a single dose in advance of central venous line placement or to bridge the period during which a central venous line is replaced or is in use for other IV treatment
When multiple dosing is required, the infusion should be done via a central venous line
Not for IV bolus injection
Oral Administration
Tablets and oral suspension are not interchangeable because of differences in dosing for each formulation
Tablets
Take tablets with food
Tablets: Swallow whole; do not divide, crush, or chew
Oral suspension
Oral suspension should be taken with a full meal or liquid nutritional supplement or an acidic carbonated beverage (eg, ginger ale) in patients unable to eat a full meal
Contra Indications
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).
Precautions
Patient w/ potentially proarrhythmic conditions. Hepatic impairment. Pregnancy and lactation. Patient Counselling May impair ability to drive or operate machinery.
Monitoring Parameters Monitor hepatic and renal function, electrolyte disturbances (e.g. Ca, Mg, K), CBC, breakthrough fungal infections and adequate oral intake.
Pregnancy-Lactation
Pregnancy
Available data in pregnant women are insufficient to establish a drug- associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes; based on findings from animal data, therapy may cause fetal harm when administered to pregnant women
Animal data
Skeletal malformations (cranial malformations and missing ribs) and maternal toxicity (reduced food consumption and reduced body weight gain) observed when dosed orally to pregnant rats; during organogenesis at doses greater than or equal to 1.4 times the 400 mg twice daily oral suspension regimen recommended in humans; in pregnant rabbits dosed orally during organogenesis, increased resorptions, reduced litter size, and reduced body weight gain of females were seen at doses 5 times the exposure achieved with the 400 mg twice daily oral suspension regimen; doses of ?3 times the clinical exposure caused an increase in resorptions in these rabbits; based on animal data, advise pregnant women of potential risk to a fetus
Lactation
There are no data on presence of drug in human milk, effects on breastfed infant, or on milk production; drug is excreted in milk of lactating rats; when a drug is present in animal milk, it is likely that the drug will be present in human milk; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for drug and any potential adverse effects on breastfed child from drug or from underlying maternal condition
Interactions
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.
Adverse Effects
Side effects of Posaconazole :
>10%
Fever (45%)
Diarrhea (42%)
Nausea (38%)
Hypokalemia (30%)
Headache (28%)
Abd pain (27%)
Anemia (25%)
Cough (24%)
Nausea (38%)
Thrombocytopenia (29%)
Constipation (21%)
Dyspnea (20%)
Febrile neutropenia (20%)
Rigors (20%)
Rash (19%)
Bacteremia (18%)
HTN (18%)
Hypomagnesemia (18%)
Fatigue (17%)
Insomnia (17%)
Mucositis (17%)
Musculoskeletal pain (16%)
Anorexia (15%)
Herpes simplex (15%)
Leg edema (15%)
CMV infection (14%)
Epistaxis (14%)
Hypotension (14%)
Pharyngitis (12%)
Arthralgia (11%)
Dizziness (11%)
Hypoglycemia (11%)
Petechiae (11%)
Pruritus (11%)
Back pain (10%)
Dyspepsia (10%)
Vaginal hemorrhage (10%)
1-10%
Anxiety (9%)
Edema (9%)
Hypocalcemia (9%)
Weakness (8%)
URI (7%)
Mechanism of Action
Blocks the synthesis of ergosterol, a key component of the fungal cell membrane, through the inhibition of the enzyme lanosterol 14-α-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.
Note
Noxafil 100mg Tablets / Gastro-Resistant manufactured by Merck Sharp & Dohme B.V.. Its generic name is Posaconazole. Noxafil is availble in United Arab Emirates.
Farmaco UAE drug index information on Noxafil Tablets / Gastro-Resistant is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.