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busulfan (Rx)Brand and Other Names:Myleran, Busulfex

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

injectable solution

  • 6mg/mL

tablet

  • 2mg
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Chronic Myelogenous (Myeloid, Myelocytic, Granulocytic) Leukemia

Pre-medicate with anticonvulsants (e.g. benzodiazepines, phenytoin, valproic acid or levetiracetam) and antiemetic

Remission induction: 60 mcg/kg/day or 1.8 mg/m²; 4-8 mg PO qDay usual range 

Maintenance doses: 1-4 mg/day to 2 mg/week PO to maintain WBC 10,000-20,000 cells/mm³ may withhold drug when leukocyte count has declined to approximately 15,000/mcL

Examine patient at monthly intervals and resume treatment with induction dosage when total leukocyte count reaches approximately 50,000/mcL

Administered as component of busulfan/cyclophosphamide: 0.8 mg/kg IV q6hr for 4 days (in combo with cyclophosphamide) until WBC count= 15,000/mm³

Administration: take on empty stomach to decrease risk of N/V

Monitor: CBC, Hgb, LFTs

Brain Malignancies (Orphan)

Treatment of primary brain malignancies

Orphan indication sponsor

  • SuperGen, Inc; Two Annabel Lane, Suite 220; San Ramon, CA 94583

Stem Cell Transplantation (Orphan)

Liposomal busulfan (Busulipo)

Orphan designation for use as a conditioning regimen for patients with malignancies undergoing autologous or allogenic hematopoietic stem cell transplantation

Orphan sponsor

  • Pharmalink AB; Engelbrekts kyrkogata 7B, SE-114 26; Stockholm, Sweden

Hepatic Impairment

Not studied

Renal Impairment

Not studied

Other Indications & Uses

CML associated with Philadelphia chromosome

Safety and efficacy not established

Chronic Myelogenous (Myeloid, Myelocytic, Granulocytic) Leukemia

Remission induction: 60 mcg/kg/day or 1.8 mg/m²; 4-8 mg PO qDay usual range

Maintenance doses: 1-4 mg/day to 2 mg/week PO to maintain WBC 10,000-20,000 cells/mm³; may withhold drug when leukocyte count has declined to approximately 15,000/mcL

Examine patient at monthly intervals and resume treatment with induction dosage when total leukocyte count reaches approximately 50,000/mcL

Administered as component of busulfan/cyclophosphamide: 0.8 mg/kg IV q6hr for 4 days (in combo with cyclophosphamide) until WBC count= 15,000/mm³

Administration: take on empty stomach to decrease risk of N/V

Monitor: CBC, Hgb, LFTs

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Interactions

Interaction Checker

busulfan and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Neutropenia (nearly 100%)

            Myelosuppression (nearly 100%)

            Thrombocytopenia (98%)

            Nausea (97%)

            Stomatitis (96%)

            Anorexia (80%)

            Diarrhea (80%)

            Fever (80%)

            Insomnia (80%)

            Lymphopenia (79%)

            Hypomagnesemia (77%)

            Headache (69%)

            Hyperglycemia (66%)

            Hypokalemia (64%)

            Abdominal pain (62%)

            Anemia (62%)

            Asthenia (52%)

            Hypocalcemia (49%)

            Chills (47%)

            Dyspepsia (44%)

            Tachycardia (44%)

            Pain (41%)

            Constipation (38%)

            Hypertension (36%)

            Hypersensitivity (32%)

            Edema (27%)

            Thrombosis (27%)

            Dry mouth (26%)

            Vasodilation (25%)

            Mild epistaxis (25%)

            Inflammation at injection site (25%)

            Rectal disorder (25%)

            Abdominal enlargement (23%)

            Back pain (23%)

            Chest pain (22%)

            1-10%

            Grade 3/4 Hypertension (7%, IV)

            Hypotension (3%, IV)

            Cardiac tamponade (2%, oral)

            Third degree AV block (2%, IV)

            Left heart failure (2%, IV)

            Frequency Not Defined

            Dizziness

            Anxiety

            Depression

            Seizure

            Cough

            Dyspnea

            Rhinitis

            Bronchopulmonary dysplasia with pulmonary fibrosis (rare)

            Aplastic anemia (rare)

            Leukemia (rare)

            Graft versus host disease

            Adrenal gland disorder

            Pruritis

            Rash

            Cataract

            Hemorrhagic cystitis

            Amenorrhea

            Male infertility

            Ovarian dysfunction

            Postmarketing Reports

            Febrile neutropenia

            Tumor lysis syndrome

            Thrombotic micro-angiopathy (TMA)

            Severe bacterial, viral (eg, cytomegalovirus viremia), fungal infections, and sepsis

            Tooth hypoplasia

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            Warnings

            Black Box Warnings

            Bone marrow suppression is a common occurrence; reduce dose or discontinue oral administration for unusual suppression (bond marrow biopsy may be necessary); hematopoietic progenitor cell transplantation is required to prevent potentially fatal complications of prolonged myelosuppression

            Monitoring is very important after administering these doses

            This drug should be administered under the supervision of an experienced cancer chemotherapy physician

            Contraindications

            Hypersensitivity, resistance to busulfan

            Patients without definitive diagnosis of CML

            Cautions

            Bone marrow depression may occur

            Seizures reported with use; initiate anticonvulsant prophylactic therapy prior to treatment with busulfan; monitor patients with history of seizure disorder, head trauma or receiving epileptogenic drugs

            Cardiac temponade reported in children with thalassemia in combination with cyclophosphamide

            Ovarian failure may occur

            Secondary malignancies reported

            Antiemetics may be recommended to prevent nausea and vomiting

            Increased risk of developing hepatic veno-occlusive disease (HVOD) at AUC greater than 1,500 μM•min; monitor serum transaminases, alkaline phosphatase and bilirubin daily

            Bronchopulmonary dysplasia with pulmonary fibrosis reported and can be fatal; toxicity may be additive if used with other agents that cause pulmonary toxicity; discontinue therapy if busulfan toxicity develops

            Avoid pregnancy; can cause fetal harm; advise of potential risk to a fetus and use of effective contraception

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            Pregnancy & Lactation

            Pregnancy Category: D

            Lactation: Excretion in milk unknown/discontinue breastfeeding

            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.

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            Pharmacology

            Mechanism of Action

            Alkylating agent; interferes with DNA eplication and RNA transcription; cross-links DNA strands; has little immunosuppressive activity; affects myeloid cells more than lymphoid cells; very toxic to hematopoietic stem cells

            Pharmacokinetics

            Half-life elimination: 2.5 hr

            Onset: 1-2 wk

            Duration: 24 hr

            Time to peak serum: 1hr (PO); 5 min (IV)

            Bioavailability: 68-80% depending on age

            Protein Bound: 32%

            Vd: 0.6-1.0 L/kg (adults); 1.4-1.6 L/kg (children)

            Metabolism: Liver

            Metabolites: Methanesulfonic acid & 3-hydroxytetrahydrothiophene-1,1-dioxide

            Clearance: 2.52 mL/min/kg

            Excretion: Urine (25-60%)

            Dialyzable: Yes

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            Administration

            IV Preparation

            Dilute and administer as intravenous infusion; do not administer as intravenous push or bolus

            Do not infuse other medications simultaneously

            Dilute busulfan injection in NS or D5W; do not use other diluents

            Dilution volume should be 10x volume of busulfan concentrate, insuring final concentration is equal to or >0.5 mg/mL

            IV Administration

            Administer via a central venous catheter as a 2 hr infusion, q6hr for 4 consecutive days for a total of 16 doses

            Do not use polycarbonate syringes

            Storage

            Store unopened ampules (injection) under refrigeration at 2-8°C

            Prolonged storage (>8 hr) in D5W or NS at room temp causes 10%+ loss of potency

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            Images

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            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

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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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