Busulfan

Registered South African indications:

• Chronic granulocytic leukaemia

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Pregnancy
• Patients whose disease has demonstrated resistance to busulfan

Cautions

• Breastfeeding
• Renal impairment
• Hepatic impairment
• Recent radiotherapy
• Once blast transformation has occurred
• High doses
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption

Forms avail. in SA and covered in this monograph: tab

Used for the treatment of

Chronic granulocytic leukaemia
- Palliative treatment of the chronic phase

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Consult specialist for dosages and regimens

Paed. forms avail. In SA and covered in this monograph: tab

Used for the treatment of

Chronic granulocytic leukaemia
- Palliative treatment of the chronic phase

---

Consult specialist for dosages and regimens

Pregnancy

• FDA Pregnancy Category D

Breastfeeding

• Caution; not recommended

Renal Impairment

• Caution; no information available

Hepatic Impairment

• Caution; no dose adjustment recommended

Elderly            

• No dose adjustment recommended

Central Nervous System Disorders

• Convulsion
• Myasthenia gravis
• Anxiety
• Depression
• Insomnia
• Confusional state
• Delirium
• Nervousness
• Hallucination
• Agitation

Cardiovascular Disorders

• Cardiac tamponade 
• Tachycardia
• Arrhythmia
• Atrial fibrillation
• Cardiomegaly
• Pericarditis
• Ventricular extrasystoles
• Bradycardia
• Hypertension
• Hypotension
• Thrombosis
• Vasodilation
• Femoral artery thrombosis
• Capillary leak syndrome
• Chest pain

Respiratory Disorders

• Hyperventilation
• Respiratory failure
• Asthma
• Atelectasis
• Pleural effusion
• Idiopathic pneumonia syndrome
• Interstitial lung disease
• Abnormal breath sounds

Gastrointestinal Disorders

• Nausea and vomiting
• Diarrhoea
• Mouth ulceration
• Abdominal pain
• Dyspepsia
• Ascites
• Constipation
• Anorectal discomfort
• Haematemesis
• Ileus
• Oesophagitis
• Gastrointestinal haemorrhage

Hepatobiliary Disorders

• Hyperbilirubinaemia
• Jaundice
• Venoocclusive liver disease 
• Biliary fibrosis with hepatic atrophy and necrosis
• Jaundice 
• Abnormal hepatic function
• Biliary fibrosis

Genitourinary Disorders

• Cystitis haemorrhagic
• Dysuria
• Oliguria
• Haematuria
• Renal insufficiency
• Ovarian failure
• Male infertility
• Azoospermia 
• Testicular atrophy 
• Ovarian disorder 
• Amenorrhoea 
• Menopausal symptoms 
• Gynaecomastia
• Increased blood creatinine
• Increased blood urea 
• Decreased ejection fraction

Endocrine and Metabolic Disorders

• Hyperglycaemia
• Hypocalcaemia
• Hypokalaemia
• Hypomagnesaemia
• Hypophosphataemia
• Hyponatraemia
• Increased weight 

Musculoskeletal Disorders

• Myalgia
• Back pain
• Arthralgia
• Dysplasia

Skin and Subcutaneous Tissue Disorders

• Alopecia 
• Skin hyperpigmentation 
• Skin reactions 
• Urticaria
• Erythema multiforme
• Erythema nodosum
• Porphyrianon
• Rash
• Dry skin 
• Fragility of the skin 
• Anhydrosis cheilosis
• Sjögren's syndrome
• Oedema

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity
• Leukaemia 
• Bone marrow failure
• Leukopenia 
• Thrombocytopenia
• Aplastic anaemia
• Chills
• Pyrexia

Sensory Disorders

• Lens disorder 
• Cataract 
• Corneal thinning 

• Live vaccines
• Other cytotoxics 
• Phenytoin 
• Itraconazole 
• Metronidazole 
• Cyclophosphamide 
• Paracetamol 

• Full blood count with differential
• Hepatic function

Busulphan  is a bifunctional alkylating agent and appears to act through the alkylation of DNA. This results in the interference of DNA replication and RNA transcription, which leads to the disruption of nucleic acid function.

Tablet 2mg

• Myleran (Pharmacare) originator

Injection (per ml) 6mg

• Accoran (Accord Healthcare)
• Busulfan 6mg/ml Fresenius (Fresenius Kabi)
• Vexfan (Eurolab)