Dacarbazine

  • IUPAC: 5 - (3,3- dimethyl-1- triazenyl )-imidazole -4-carboxamide
  • Latin: Dacarbazinum

L01AX04

Cytostatic

Risk

2147 mg · kg -1 ( LD50, rat, oral)

Template: Infobox chemical / molecular formula search available

Dacarbazine is an antineoplastic agent from the group of alkylating agents. It is used as a single agent or as part of combination regimens with other substances in malignant melanoma, soft tissue sarcoma, the ( EDIC scheme) and Hodgkin 's lymphoma ( ABVD regimen ). It is listed in the WHO list of essential medicines.

Dacarbazine is a soluble powder commercially. The solution is light sensitive and must be administered intravenously with a light-resistant infusion system.

Side effects

The administration of dacarbazine may be associated with serious side effects and is usually done only by an oncologist. Very common ( > 90 % ) leads to loss of appetite, nausea and vomiting, which is why it is given in combination with antiemetics. Frequently it comes to blood disorders (anemia, leukopenia, thrombocytopenia, pancytopenia rarely ), which is why blood count checks must be performed. Due to possible ( rare ) necrosis of the liver, the function of the same must be controlled. It may also occur in rare cases, kidney failure, allergic reactions, headaches, blurred vision, confusion, lethargy, convulsions, paresthesia, diarrhea, hair loss, erythema or hyperpigmentation of the skin as well as flu -like symptoms.

In case of accidental paravenous injection must be reckoned with local pain and necrosis.

Contraindications

Contraindications include pregnancy, lactation, leukopenia and / or thrombocytopenia and severe liver or kidney disease.

Pharmacology

Pharmacodynamics

The antineoplastic effect caused by dacarbazine ( cell cycle - independent ) inhibition of cell growth. This is achieved by inhibition of DNA synthesis by alkylating effect (see alkylating agents ).

Dacarbazine is a prodrug that is metabolized in the liver by cytochrome P450 by N-demethylation to 5 - aminoimidazole -4-carboxamide and methyl cation, the cytostatic effects are attributed.

Pharmacokinetics

Dacarbazine diffuses rapidly after intravenous administration in the tissue, the distribution half -life is about 20 minutes. The plasma half -life is 0.5-3.5 hours. The degradation occurs over several metabolites via the cytochrome P450 system of the liver, about one-third is excreted unchanged by the kidney.

Trade names

Monopreparations: Dacin (CH), dacarbazine Lipomed (D), Detimedac (D)

212404
de