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Procarbazine: Wikis

  

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Procarbazine
Systematic (IUPAC) name
N-isopropyl-4-[(2-methylhydrazino)methyl]benzamide
Identifiers
CAS number 671-16-9
ATC code L01XB01
PubChem 4915
DrugBank APRD00695
Chemical data
Formula C 12H19N3O 
Mol. mass 221.299 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic, Renal
Half life 10 minutes
Excretion Renal
Therapeutic considerations
Pregnancy cat. D(AU) D(US)
Legal status Prescription only
Routes Oral (Gel Capsule), intravenous
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Procarbazine (Matulane (US), Natulan (Canada), Indicarb (India) is an antineoplastic chemotherapy drug for the treatment of Hodgkin's lymphoma and certain brain cancers (such as Glioblastoma multiforme). It is a member of a group of medicines called alkylating agents. It gained FDA Approved in July 1969. The drug is metabolized and activated in the liver. It also inhibits MAO thus increasing the effects of sympathomimetics, TCAs, and tyramine.

Contents

Pharmacology

Its mechanism of action is not fully understood. Metabolism yields azo-procarbazine and hydrogen peroxide which results in the breaking of DNA strands.

Indications

When used to treat Hodgkin's Lymphoma, it is often delivered as part of the MOPP regimen that includes Mechlorethamine, Vincristine (tradename Oncovin), Prednisone, and Procarbazine. Alternatively, when used to treat certain brain tumors (malignant gliomas), it is often dosed as PCV when combined with Lomustine (often called CCNU) and Vincristine.

Procarbazine is also part of the more modern BEACOPP regimen used for Hodgkin's lymphoma.

Side Effects/ Adverse Reactions

When combined with ethanol, procarbazine may cause a disulfiram-like reaction in some patients. It also inhibits the liver's CYP450 microsomal system, which leads to an increased effect of barbiturates, phenothiazenes, and narcotics normally metabolized by the CYP450 enzymes. It is also highly carcinogenic—patients have a 5–10% risk of developing acute leukemia, especially in combination with radiation therapy. Has monamine oxidase inhibition properties (MAOI), and should not be taken with most antidepressants and certain migraine medications.

Dose

Adult: 2–4mg/kg/day either in a single dose or divided, given for 7 days then increased to 4–6mg/kg/day until response is obtained or mylosupression occurs. Dose should be adjusted for renal (kidney) disease or hepatic (liver) disease.

Dosage Form

50 mg capsules.

Pricing

Procarbazine is manufactured by Sigma-Tau Pharmaceuticals, Inc. and is generally priced at $50/capsule in the United States.[1].

References

External links








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