Cerubidine

Cerubidine Uses, Dosage, Side Effects, Food Interaction and all others data.

Cerubidine forms a stable complex with DNA and interferes with the nucleic acid synthesis. It is a cell-cycle nonspecific agent, but its cytotoxic effects are mostly marked in the S-phase. It also has immunosuppressant and antibacterial effects.

Cerubidine is an antineoplastic in the anthracycline class. General properties of drugs in this class include: interaction with DNA in a variety of different ways including intercalation (squeezing between the base pairs), DNA strand breakage and inhibition with the enzyme topoisomerase II. Most of these compounds have been isolated from natural sources and antibiotics. However, they lack the specificity of the antimicrobial antibiotics and thus produce significant toxicity. The anthracyclines are among the most important antitumor drugs available. Doxorubicin is widely used for the treatment of several solid tumors while daunorubicin and idarubicin are used exclusively for the treatment of leukemia. Cerubidine may also inhibit polymerase activity, affect regulation of gene expression, and produce free radical damage to DNA. Cerubidine possesses an antitumor effect against a wide spectrum of tumors, either grafted or spontaneous. The anthracyclines are cell cycle-nonspecific.

Cerubidine
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Cerubidine
Availability	Prescription only
Generic	Daunorubicin
Daunorubicin Other Names	Acetyladriamycin, Daunomycin, Daunorubicin, Daunorubicina, Daunorubicine, Daunorubicinum, Leukaemomycin C, Rubidomycin
Related Drugs	Venclexta, prednisone, methotrexate, cyclophosphamide, Deltasone, vincristine, venetoclax, Cytoxan, azacitidine, cytarabine
Weight	20mg, 5mg/ml,
Type	Injection, Intravenous, Intravenous Powder For Injection, Intravenous Solution
Formula	C₂₇H₂₉NO₁₀
Weight	Average: 527.5199 Monoisotopic: 527.179146153
Protein binding	97% binding-albumin
Groups	Approved
Therapeutic Class	Cytotoxic Chemotherapy
Manufacturer	Makers Labs
Available Country	India, Canada, United States, Netherlands,
Last Updated:	September 19, 2023 at 7:00 am

Uses

Cerubidine in combination with other approved anticancer drugs is used for remission induction in acute nonlymphocytic leukemia (myelogenous, monocytic, erythroid) of adults and for remission induction in acute lymphocytic leukemia of children and adults.

Cerubidine is also used to associated treatment for these conditions: Acute Lymphocytic Leukemia (ALL), Acute Myeloid Leukemia (AML), Acute Myeloid Leukemia With Myelodysplasia-Related Changes, Acute erythroid leukemia, Acute monocytic leukaemia, Newly diagnosed Therapy-Related Acute Myeloid Leukemia

How Cerubidine works

Cerubidine has antimitotic and cytotoxic activity through a number of proposed mechanisms of action: Cerubidine forms complexes with DNA by intercalation between base pairs, and it inhibits topoisomerase II activity by stabilizing the DNA-topoisomerase II complex, preventing the religation portion of the ligation-religation reaction that topoisomerase II catalyzes.

Dosage

Cerubidine dosage

Intravenous-

Acute leukaemias:

Adult:30-45 mg/m2BSA daily on days 1-3 of the induction course and days 1 and 2 for the subsequent courses. Admin as a solution in 0.9% sodium chloride into a fast-running infusion of sodium chloride or glucose. May repeat course 3-6 wk later. Max (total cumulative dose): 550 mg/m2in patients without risk factors for cardiotoxicity and 400 mg/m2in patients who have received chest radiotherapy.
Child:For acute lymphoblastic leukaemia: 25 mg/m2BSA once wkly in combination with other regimens. <2 yr old or BSA <0.5 m2: 1 mg/kg once wkly. Max (total cumulative dose): 300 mg/m2and in children <2 yr: 10 mg/kg.

AIDS-related Kaposi's sarcoma:

Adult:As the liposomal formulation: Initially, 40 mg/m2once every 2 wk, diluted in glucose 5% to a concentration of 0.2-1 mg/ml and given over 30-60 minutes. May continue for as long as disease control can be maintained.

Side Effects

GI disturbances; stomatitis; alopoecia and dermatological reactions. Extravasation of daunorubicin may cause severe local tissue necrosis damaging surrounding muscles, tendons and nerves. IV infusion, back pain, flushing and chest tightness.

Toxicity

LD₅₀=20 mg/kg (mice, IV); LD₅₀=13 mg/kg (rat, IV)

Precaution

Regular blood count and ECG monitoring; elderly, children. Hepatic or renal impairment may increase risk of toxicity. Pre-existing cardiac disease and previous treatment with doxorubicin. Myocardial toxicity leading to potentially fatal congestive heart failure may occur during therapy or mth to yr after therapy cessation. Incidence of myocardial toxicity increases after total cumulative dose exceeds 400-550 mg/m2in adults, 300 mg/m2 in children >2 yr, or 10 mg/kg in children <2 yr. Risk of severe myelosuppression leading to infection or haemorrhage.

Interaction

Increased risk of cardiotoxicity when used with cyclophosphamide. Increased risk of hepatic toxicity when used with hepatotoxic drugs e.g. high-dose methotrexate.

Food Interaction

No interactions found.

Cerubidine Drug Interaction

Moderate: diltiazem, diltiazemMinor: sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprimUnknown: RHO Immunoglobulin , RHO Immunoglobulin , diphenhydramine, diphenhydramine, meperidine, meperidine, dexamethasone, dexamethasone, glucose, glucose, metoprolol, metoprolol, metoprolol, metoprolol, acetaminophen, acetaminophen

Cerubidine Disease Interaction

Major: congestive heart failure, infections, myelosuppressionModerate: hepatic dysfunction, renal dysfunction

Half Life

18.5 hours

Elimination Route

Twenty-five percent of an administered dose of daunorubicin hydrochloride is eliminated in an active form by urinary excretion and an estimated 40% by biliary excretion.

Pregnancy & Breastfeeding use

Pregnancy Category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Contraindication

Heart failure. Pregnancy, lactation.

Special Warning

Renal Impairment: Based on serum-creatinine concentrations: 105-265 micromoles/l: 75% of the usual dose; >265 micromoles/l: 50% of the usual dose.

Hepatic Impairment: Based on serum bilirubin concentrations of 12-30 mcg/ml: 75% of the usual dose; >30 mcg/ml: 50% of the usual dose.