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amphotericin B cholesteryl sulfate (Rx)Brand and Other Names:Amphotec

 
 
 

Dosing & Uses

AdultPediatric

Dosing Form & 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

Dosing Form & 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
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Adverse 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%)

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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

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Pregnancy & 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.

more...
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Pharmacology

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

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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

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Images

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Formulary

FormularyPatient Discounts

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  • View the formulary and any restrictions for each plan.
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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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