Busulphan

Also known as: Busulfan

Drug #113

Busulphan is a bifunctional cytotoxic alkylating agent and prototype agent of alkyl sulfonates. Busulphan is a antineoplastic agent, also known as anticancerous drug, unrelated to nitrogen mustards. All alkylating agents have or can form an alkyl group that becomes covalently bound to cellular constituents. Busulphan is used in combination of different types of anticancerous drugs to obtain better therapeutic effects and to reduce the side effects or toxicities.

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Primary Characteristics

Busulphan is also known as Busulfan.

It is of Synthetic origin and belongs to Alkyl Sulphonate.

It belongs to Alkylating Agents pharmacological group on the basis of mechanism of action and also classified in Antineoplastic Agent, Alkylating Agent pharmacological group.

Molecular Weight: 246.3 · Solubility in Water: insoluble · Solubility in Alcohol: 1 in 1000 · Non-proprietary name: Busulphan.

Pharmacokinetics

Distribution: Busulphan has a volume of distribution is 0.99l/kg. plasma protein binding is 7.4%.

Elimination: it is metabolised via extensive, plasma half-life is 2-3 hr, renal excretion is 10-50% (inactive etabolite), 1% (unchaged).

Indications

Busulphan is primarily indicated in conditions like Chronic myeloid leukaemia, Granulocytic leukemia, Polycythemia vera.

Busulphan is also indicated for secondary conditions like Myelofibrosis, Thrombocythaemia.

Contraindications

Busulphan is contraindicated in conditions like Anaemia, Thrombocytopenia, Leukopenia.

Dosage

Busulphan's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
0.057 mg/kg	0.057 mg/kg	Every 24h	PO	-
Paediatric Dosage (20kg)
0 – 0	—	—		Not used in children
Neonatal Dosage (3kg)
No data.

Drug Interactions

Unknown2 interactions

5 interactions

Major2 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Busulphan in overdosage may give rise to further complications which include Addison's disease, Hyperpigmentation .

Busulphan produces potentially life-threatening effects which include Bone marrow suppression, Thrombocytopenia . Careful monitoring is needed with proper medical management.

The signs and symptoms that are produced after acute overdosage of Busulphan are Hematological toxicity.

Warnings / Precautions

Busulphan is not recommended for use during pregnancy or lactation. Immunosuppressant drug should not be given, where possible, to patients with acute infection, dosage reduction or withdrawal should be considered if infection develops, until the infection has been controlled. Blood counts and measurement of hemoglobin concentration should be carried out routinely; it helps to predict the onset of bone marrow depression. It must be handled with great care and avoid contact with skin and eyes and should not be inhaled.

Available Brands

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Single Ingredient

Tabs

2 mg

Storage Conditions

Busulphan should be stored Tab.

Drug Classification

1.8.2 — Cytotoxic (anti-neoplastic) drugs

Manufacturers

Manufacturers of Busulphan in Pakistan:

Pharmedic