Mercaptopurine (Monohydrate)
Also known as: 6MP
Mercaptopurine (Monohydrate) is oral, cell-cycle-phase specific antineoplastic agent used chiefly in the treatment of acute lymphoblastic leukemia. Mercaptopurine (Monohydrate) is a chemical analog of purine, a necessary building block used by cells for synthesizing DNA. Mercaptopurine is also closely related to another antimetabolite, thioguaninean (the two agents have similar indications, adverse effects, and cross-resistance). Mercaptopurine is also the metabolite of azathioprine, a commonly used immunosuppressive agent. It received FDA approval in 1953.it acts as an antimetabolite and is active in the S-phase. Mercaptopurine exhibits a couple of mechanisms of action. It can undergo triphosphorylation and can be incorporated into DNA in place of adenine, leading to a derangement in the DNA message. Mercaptopurine ribonucleotides also can be incorporated into RNA and can halt RNA synthesis. Second, the drug can be metabolized to a nucleotide that inhibits biosynthesis of purines needed for RNA and DNA synthesis. Together these effects lead to cell death.
Primary Characteristics
Mercaptopurine (Monohydrate) is also known as 6MP.
It is of Synthetic origin and belongs to Hypoxanthine.
It belongs to Antimetabolites (DNA acting) pharmacological group on the basis of mechanism of action and also classified in Antineoplastic Agnet, Antimetabolite pharmacological group.
Molecular Weight: 170.2 · pKa: 7.77, 11.17 · Solubility in Water: Insoluble · Solubility in Alcohol: 1 in 950 · Non-proprietary name: Mercaptopurine (Monohydrate).
Pharmacokinetics
Absorption: Mercaptopurine (Monohydrate) has an oral bioavailability is 25% (±25%).
Distribution: Mercaptopurine (Monohydrate) has a volume of distribution is 0.9±0.8 l/kg. plasma protein binding is 20%.
Elimination: it is metabolised via Hepatic(extensively), plasma half-life is 20-90 min, renal excretion is >50%.
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Indications
Mercaptopurine (Monohydrate) is primarily indicated in conditions like Acute leukemia, Crohn's disease, Non-hodgkin's lymphoma.
Mercaptopurine (Monohydrate) is also indicated for secondary conditions like Inflammatory bowel disease, Inflammatory bowel disease (unlicensed use).
Contraindications
Mercaptopurine (Monohydrate) is contraindicated in conditions like Hypersensitivity, Bone marrow suppression.
Dosage
Mercaptopurine (Monohydrate)'s dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 62.5 mg/sq.m | 62.5 mg/sq.m | Every 24h | PO | Initial , Or 2.5mg/kg |
| 137.5 mg/sq.m | 137.5 mg/sq.m | Every 24h | PO | maintenance , Or 1.5-2.5 mg/kg |
| Paediatric Dosage (20kg) | ||||
| No data. | ||||
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Mercaptopurine (Monohydrate) in overdosage may give rise to further complications which include Pancreatitis , Anorexia , Interstitial pneumonitis , Liver dysfunction , Liver necrosis.
Mercaptopurine (Monohydrate) produces potentially life-threatening effects which include Anemia, Thrombocytopenia , Myelosuppression , Granulocytopenia , Anemia, Leukopenia. Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Mercaptopurine (Monohydrate) are Myelosuppression , Anorexia , Nausea & vomiting, Liver dysfunction, Gastroentritis.
Mercaptopurine (Monohydrate) is known to cause more or less tolerable side effects which are usually transient. These include Anorexia , Diarrhea, Eosinophilia, Jaundice , Radiation recall reactions, StomatitisX.
Warnings / Precautions
Available Brands
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Single Ingredient
Storage Conditions
Drug Classification
- 1.8.2 — Cytotoxic (anti-neoplastic) drugs