Dosing and uses of Amphotec (amphotericin B cholesteryl sulfate)
Adult dosage forms and strengths
powder for injection
- 50mg/vial
- 100mg/vial
Aspergillosis
Indicated for treatment of invasive aspergillosis in patients where renal impairment or unacceptable toxicity precludes the use of amphotericin B deoxycholate (conventional) in effective doses, or where prior amphotericin B deoxycholate therapy has failed
3-4 mg/kg IV qDay
Initial infusion rate 1 mg/kg/hr; subsequent infusions may be shortened to infuse over 2 hr if tolerated
Test dose
- Administer immediately preceding first dose when commencing all new courses of treatment
- Infuse small amount of drug (eg, 10 mL of final preparation containing between 1.6-8.3 mg) over 15-30 minutes
- Carefully observe patient for next 30 minutes
Pediatric dosage forms and strengths
powder for injection
- 50mg/vial
- 100mg/vial
Aspergillosis
Indicated for treatment of invasive aspergillosis in patients where renal impairment or unacceptable toxicity precludes the use of amphotericin B deoxycholate (conventional) in effective doses, or where prior amphotericin B deoxycholate therapy has failed
As adults; 3-4 mg/kg IV qDay
Initial infusion rate 1 mg/kg/hr; subsequent infusions may be shortened to infuse over 2 hr if tolerated
Test dose
- Administer immediately preceding first dose when commencing all new courses of treatment
- Infuse small amount of drug (eg, 10 mL of final preparation containing between 1.6-8.3 mg) over 15-30 minutes
- Carefully observe patient for next 30 minutes
Amphotec (amphotericin B cholesteryl sulfate) adverse (side) effects
>10%
Chills (50-77%)
Fever (33-55%)
Hypokalemia (7-26%)
Elevated serum creatinine (12-21%)
Hyperbilirubinemia (2-19%)
Hypotension (9-12%)
Tachycardia (9-12%)
Nausea (8-12%)
Vomiting (6-11%)
Abnormal LFTs (4-11%)
1-10%
Hypertension (7-9%)
Hypoxia (5-9%)
Dyspnea (4-9%)
Headache (4-8%)
Hypomagnesemia (4-7%)
Increased alkaline phosphatase (3-7%)
Thrombocytopenia (1-7%)
Hyperglycemia (1-6%)
Warnings
Contraindication
Hypersensitivity
Cautions
Indicated for patients with progressive and potentially fatal fungal infections
Do not use for noninvasive fungal infections (eg, oral thrush, vaginal candidiasis, esophageal candidiasis) in patients with normal neurophil counts
Caution when coadministration with other drugs that cause hypokalemia (eg, corticosteroids, digoxin)
Caution with other nephrotoxic medications
Pregnancy and lactation
Pregnancy category: B
Lactation: Unknown whether distributed in breast milk, caution advised
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Amphotec (amphotericin B cholesteryl sulfate)
Half-Life, elimination: 27.5-28.2 hr
Half-Life, distribution: 3.5 min
Vd: 3.8-4.1 L/kg
AUC: 29-36 mcg/mL•h
Peak Plasma Concentration: 2.6-2.9 mcg/mL
Clearance: 0.105-9.112 L/hr/kg
Mechanism of action
Acts by binding to sterols in fungal cell membrane, leading to alterations in cell permeability and cell death
Administration
IV Incompatibilities
NaCl or other electrolytes
Y-site: alfentanil, amikacin, ampicillin, ampicillin Na-sulbactam, atenolol, aztreonam, bretylium, buprenorphine, butorphanol, calcium chloride, calcium gluconate, carboplatin, cefazolin, cefepime, ceftazidime, ceftazidime-Na, ceftriaxone, chlorpromazine, cimetidine, cisatracurium besylate, cisplatin, cyclophosphamide, cyclosporine, cytarabine, diazepam, digoxin, diphenhydramine, dobutamine, dopamine, doxorubicin, doxorubicin liposomal, droperidol, enalaprilat, esmolol, famotidine, fluconazole, fluorouracil, gatifloxacin, gentamicin, haloperidol, heparin, hydromorphone, hydroxyzine, imipenem/ cilastatin, labetalol, leucovorin, lidocaine, magnesium sulfate, meperidine, mesna, metoclopramide, metoprolol, metronidazole, midazolam, mitoxantrone, morphine, nalbuphine, naloxone, netilmicin, ofloxacin, ondansetron, paclitaxel, pentobarbital, phenobarbital, phenytoin, piperacillin, piperacillin-tazobactam, potassium chloride, prochlorperazine, promethazine, propranolol, ranitidine, remifentanil, sodium bicarbonate, ticarcillin/clavulanate, tobramycin, vancomycin, vecuronium, verapamil, vinorelbine
IV Compatibilities
Additive solution: Dextrose
Y-site: acyclovir, aminophylline, cefoxitin, ceftizoxime, clindamycin, dexamethasone Na-PO4, fentanyl, furosemide, ganciclovir, granisetron, hydrocortisone Na-succinate, ifosfamide, lorazepam, mannitol, methotrexate, methylprednisolone Na-succinate, nitroglycerin, sufentanil, TMP-SMX, vinblastine, vincristine, zidovudine
IV Preparation
Do not reconstitute lyophilized powder with NaCl or dextrose solutions, or admix the reconstituted liquid with saline or electrolytes; use of any solution other than those recommended, or the presence of a bacteriostatic agent (eg, benzyl alcohol) in the solution may cause precipitation
Reconstitute with sterile water for injection (nonbacteriostatic); reconstituted solution contains 5 mg/mL
Further dilute with 5% dextrose to final concentration approximately 0.6 mg/mL
Shake gently by hand, rotating the vial until all solids have dissolved
Fluid may be opalescent or clear
Do NOT filter
IV Administration
Do NOT use an in-line filter
Use separate infusion line; if an existing IV line is used, flush with D5W before infusion
Initial infusion rate 1 mg/kg/hr; subsequent infusions may be shortened to infuse over 2 hr if tolerated
Test dose
- Administer immediately preceding first dose when commencing all new courses of treatment
- Infuse small amount of drug (eg, 10 mL of final preparation containing between 1.6-8.3 mg) over 15-30 minutes
- Carefully observe patient for next 30 minutes
Storage
Store unopened vials at room temp; protect from light and excessive heat
After reconstitution, the drug should be refrigerated at 2-8°C (36-46°F) and used within 24 hr
After further dilution with 5% dextrose, refrigerate (2-8°C) and use within 24 hr
Do not freeze
Discard partially used vials
