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| Clinical data | |
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| Trade names | Matulane, Natulan, Indicarb, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a682094 |
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| Routes of administration | By mouth (gel capsule),intravenous |
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| Pharmacokinetic data | |
| Metabolism | liver,kidney |
| Eliminationhalf-life | 10 minutes |
| Excretion | kidney |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.010.531 |
| Chemical and physical data | |
| Formula | C12H19N3O |
| Molar mass | 221.304 g·mol−1 |
| 3D model (JSmol) | |
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Procarbazine is achemotherapy medication used for the treatment ofHodgkin lymphoma andbrain cancers.[1] For Hodgkin lymphoma it is often used together withchlormethine,vincristine, andprednisone while for brain cancers such asglioblastoma multiforme it is used withlomustine andvincristine.[1] It is typically taken by mouth.[1]
Common side effect includelow blood cell counts and vomiting.[1] Other side effects include tiredness and depression.[2][3] It is not recommended in people with severe liver or kidney problems.[4] Use inpregnancy is known to harm the baby.[1] Procarbazine is in thealkylating agents family of medication.[1] How it works is not clearly known.[1]
Procarbazine was approved for medical use in the United States in 1969.[1] It is on theWorld Health Organization's List of Essential Medicines.[5][6] In the United Kingdom a month of treatment cost theNational Health Service 450 to 750 pounds.[4][relevant?]
When used to treatHodgkin lymphoma, it is often delivered as part of theBEACOPP regimen that includesbleomycin,etoposide,adriamycin,cyclophosphamide,vincristine (tradename Oncovin),prednisone, and procarbazine. The first combination chemotherapy developed for Hodgkin lymphoma (HL),MOPP also included procarbazine (ABVD has supplanted MOPP as standard first line treatment for HL, with BEACOPP as an alternative for advanced/unfavorable HL). Alternatively, when used to treat certain brain tumors (malignant gliomas), it is often dosed as PCV when combined withlomustine (often called CCNU) and vincristine.
Dose is adjusted for kidney disease or liver disease.
Very common (greater than 10% of people experience them) adverse effects include loss of appetite, nausea and vomiting.[2] Other side effects of unknown frequency includereduction in leukocytes,reduction in platelets,reduction in neutrophils, which can lead to increased infections including lung infections; severe allergy-like reactions that can lead toangioedema and skin reactions; lethargy; liver complications includingjaundice and abnormal liver function tests; reproductive effects includingreduction in sperm count andovarian failure.[2]
When combined withethanol, procarbazine may cause adisulfiram-like reaction in some people.[2]
It weakly inhibits MAO in the gastrointestinal system, so it can cause hypertensive crises if associated with the ingestion of tyramine-rich foods such as aged cheeses; this appears to be rare.[2]
Procarbazine rarely causeschemotherapy-induced peripheral neuropathy,[7] a progressive, enduring, often irreversible tingling numbness, intense pain, and hypersensitivity to cold, beginning in the hands and feet and sometimes involving the arms and legs.[8]
Procarbazine works, in part, as analkylating agent and methylates guanine at the O-6 position (much likedacarbazine also does[9]). Guanine is one of the four nucleotides that makes up DNA. The methylated DNA is prone to breakage, and RNA and protein synthesis is inhibited.[10] Proliferating cancer cells need to replicate their DNA and undergo programmed cell death (apoptosis) in response to DNA strand breaks. Normal or non-proliferating cells are more apt to repair the DNA damage, but still some of the healthy cells will be damaged. Procarbazine is metabolized in the liver to an azo-derivative and then further metabolized by thecytochrome P-450 system to an active azoxy-derivative.
