Matulane - General Information
An antineoplastic agent used primarily in combination with mechlorethamine, vincristine, and prednisone (the MOPP protocol) in the treatment of Hodgkin&
Pharmacology of Matulane
Matulane is an antineoplastic in the class of alkylating agents and is used to treat various forms of cancer. Alkylating agents are so named because of their ability to add alkyl groups to many electronegative groups under conditions present in cells. They stop tumor growth by cross-linking guanine bases in DNA double-helix strands - directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. In addition, these drugs add methyl or other alkyl groups onto molecules where they do not belong which in turn inhibits their correct utilization by base pairing and causes a miscoding of DNA. Matulane is cell-phase specific for the S phase of cell division.
Matulane for patients
Patients should be warned not to drink alcoholic beverages while on Matulane therapy since there may be an Antabuse (disulfiram)-like reaction. They should also be cautioned to avoid foods with known high tyramine content such as wine, yogurt, ripe cheese and bananas. Over-the-counter drug preparations which contain antihistamines or sympathomimetic drugs should also be avoided. Patients taking Matulane should also be warned against the use of prescription drugs without the knowledge and consent of their physician.
Patients should be advised to discontinue tobacco use.
To minimize CNS depression and possible potentiation, barbiturates, antihistamines, narcotics, hypotensive agents or phenothiazines should be used with caution. Ethyl alcohol should not be used since there may be an Antabuse (disulfiram)-like reaction. Because Matulane exhibits some monoamine oxidase inhibitory activity, sympathomimetic drugs, tricyclic antidepressant drugs (e.g., amitriptyline HCl, imipramine HCl) and other drugs and foods with known high tyramine content, such as wine, yogurt, ripe cheese and bananas, should be avoided. A further phenomenon of toxicity common to many hydrazine derivatives is hemolysis and the appearance of Heinz-Ehrlich inclusion bodies in erythrocytes.
No cross-resistance with other chemotherapeutic agents, radiotherapy or steroids has been demonstrated.
Matulane is contraindicated in patients with known hypersensitivity to the drug or inadequate marrow reserve as demonstrated by bone marrow aspiration. Due consideration of this possible state should be given to each patient who has leukopenia, thrombocytopenia or anemia.
Additional information about Matulane
Matulane Indication: For use with other anticancer drugs for the treatment of stage III and stage IV Hodgkin's disease.
Mechanism Of Action: The precise mode of cytotoxic action of procarbazine has not been clearly defined. There is evidence that the drug may act by inhibition of protein, RNA and DNA synthesis. Studies have suggested that procarbazine may inhibit transmethylation of methyl groups of methionine into t-RNA. The absence of functional t-RNA could cause the cessation of protein synthesis and consequently DNA and RNA synthesis. In addition, procarbazine may directly damage DNA. Hydrogen peroxide, formed during the auto-oxidation of the drug, may attack protein sulfhydryl groups contained in residual protein which is tightly bound to DNA.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Procarbazine
Synonyms: Ibenzmethyzine hydrochloride; Ibenzmethyzine; Ibenzmethyzin; IBZ; MBH; MIH; MIH Hydrochloride; PCB; PCB hydrochloride; Procarbazin [German]; Procarbazina [Inn-Spanish]; Procarbazine hydrochloride; Procarbazinum [Inn-Latin]; PCX; Procarbazin
Drug Category: Antineoplastic Agents
Drug Type: Small Molecule; Approved
Absorption: Procarbazine is rapidly and completely absorbed.
Toxicity (Overdose): LD50=785 mg/kg (orally in rats)
Protein Binding: Not Available
Biotransformation: Procarbazine is metabolized primarily in the liver and kidneys. The drug appears to be auto-oxidized to the azo derivative with the release of hydrogen peroxide. The azo derivative isomerizes to the hydrazone, and following hydrolysis splits into a benzylaldehyde derivative and methylhydrazine. The methylhydrazine is further degraded to CO2 and CH4 and possibly hydrazine, whereas the aldehyde is oxidized to N-isopropylterephthalamic acid, which is excreted in the urine.
Half Life: 10 minutes
Dosage Forms of Matulane: Capsule Oral
Chemical IUPAC Name: 4-[(2-methylhydrazinyl)methyl]-N-propan-2-ylbenzamide
Chemical Formula: C12H19N3O
Procarbazine on Wikipedia: https://en.wikipedia.org/wiki/Procarbazine
Organisms Affected: Humans and other mammals