Dacarbazine-LENS lyophilizate 100 mg

Pharmacodynamics

An alkylating antitumor agent. It interacts with SH-groups. Inhibits synthesis of purine bases and DNA.

Pharmacokinetics

Protein binding is low. It penetrates through the BBB in limited quantities. Intensively metabolized in the liver. T_1/2 in the initial phase is 19 min, in the final phase – 5 h.

In renal and hepatic disorders T_1/2 increases. It is excreted by the kidneys unchanged and as metabolites – 40% within 6 hours.

Indications

• Malignant melanoma;
• lymphogranulomatosis;
• soft tissue sarcomas.

Possible use as a second-line treatment for:

• testicular tumors;
• gastrointestinal malignancies and neuroblastoma.

Active ingredient

Dacarbazine

Composition

1 vial contains:

The active ingredient:

Dacarbazine 100 mg

Excipients:

citric acid 100 mg

mannitol 50 mg

How to take, the dosage

It is set individually, depending on the indication and stage of the disease, the state of the hematopoiesis system, the scheme of anti-tumor therapy.

Interaction

In co-administration with drugs – inducers of microsomal liver enzymes (including phenobarbital, rifampicin, phenytoin) dacarbazine metabolism may be increased.

Concomitant use with phenobarbital, azathioprine or 6-mercaptopurine increases the toxic effects of dacarbazine.

Special Instructions

The use of dacarbazine is not recommended in patients with chicken pox (including recent and after exposure to the disease), herpes zoster and other acute infectious diseases.

With caution, use in patients who have previously received cytotoxic drugs or radiation therapy.

Peripheral blood counts, urea nitrogen, creatinine, uric acid, liver transaminase activity, LDH and plasma bilirubin concentration should be monitored before and during treatment.

Vaccination of patients and their family members during therapy is not recommended.

In combination antitumor therapy, dacarbazine is used primarily in combination with bleomycin, cisplatin, 5-fluorouracil, vincristine and prednisolone.

The carcinogenic and mutagenic effects of dacarbazine have been established in experimental studies.

Contraindications

• Myelodepression;
• Pregnancy;
• High sensitivity to dacarbazine.

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Side effects

Blood system disorders: leukopenia, thrombocytopenia, anemia.

Digestive system disorders: anorexia, nausea, vomiting, diarrhea, stomatitis; in some cases – liver dysfunction, hepatic vein thrombosis, toxic liver dystrophy.

Reproductive system disorders: amenorrhea, azoospermia.

Dermatological reactions: alopecia, skin rash.

Others: hyperemia, facial hypoesthesia; in single cases – renal dysfunction.

After single high-dose administration: flu-like syndrome accompanied by fever and myalgia may occur.

Pregnancy use

Dacarbazine is contraindicated in pregnancy. Breast-feeding should be stopped if it is necessary to use it during lactation.

Women of childbearing age should use reliable methods of contraception.

Toxic effects of dacarbazine on the fetus have been found in experimental studies.